Entries |
Document | Title | Date |
20080200477 | Retinoid-Containing Compositions Having Reduced Irritation Effect - The present invention features a composition including (i) a retinoid, and (ii) an interleukin-8 inhibitor. The composition provides reduced irritation to human skin. | 08-21-2008 |
20080200478 | ANTINEOPLASTIC AND CURCUMIN DERIVATIVES AND METHODS OF PREPARATION AND USE - This invention comprises antineoplastic curcumin derivatives and methods of preparation and use thereof. Particular reference is made to the following isomeric compounds | 08-21-2008 |
20080214575 | PIPERIDINE DERIVATIVES USEFUL AS CCR5 ANTAGONISTS - The present invention provides a compound of the formula | 09-04-2008 |
20080221127 | PPAR ACTIVE COMPOUNDS - Compounds are described that are active on at least one of PPARα, PPARδ, and PPARγ, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPARα, PPARδ, and PPARγ. | 09-11-2008 |
20080234293 | Tri-aryl/heteroaromatic cannabinoids and use thereof - Cannabinoid derivatives according to formula (I) are disclosed | 09-25-2008 |
20080242681 | N-4-(6-(Hetero)Aryl-Pyrimidin-4-Ylaminophenyl)-Benzenesulfonamides as Kinase Inhibitors - Compounds of a certain formula 1 in which R1 and R2 have the meanings indicated in the description are novel kinase inhibitors. Formula (1), in which R1 is phenyl, phenyl substituted by R3 and/or R4, naphthalenyl, naphthalenyl substituted by and/or R6, aryl1, aryl1 substituted by R7 and/or R8, R9, R10 or R11, R2 is phenyl, phenyl substituted by R12 and/or R13, naphthalenyl, naphthalenyl substituted by R14 and/or R15, aryl2, aryl2 substituted by R16 and/or R17 or a radical selected from Formula (2). | 10-02-2008 |
20080249110 | Novel Substituted 3-Sulfur Indoles - The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders. | 10-09-2008 |
20080249111 | Piperdine Derivatives as CCR5 Inhibitors - Disclosed are compounds of formula I: | 10-09-2008 |
20080255155 | KINASE INHIBITORS AND USES THEREOF - This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds, compositions and methods for the inhibition of kinase activity. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions. | 10-16-2008 |
20080261999 | Azabicycloalkane Derivatives Useful as Nicotinic Acetylcholine Receptor Agonists - Compounds of the formula I or a pharmaceutically acceptable salt thereof: processes for their preparation, pharmaceutical compositions which contain them and their uses in therapy. | 10-23-2008 |
20080269252 | Use of Compounds Derived From Pyrimidinetrione as Acetyl Cholinesterase Inhibitors, Compositions Containing Said Derivatives, and the Uses Thereof - The invention relates to the use of compounds derived from pyrimidinetrione of general formula (I) as acetyl cholinesterase (AChE) inhibitors. The invention also relates to the use of said compounds as insecticides, and to compositions containing the same. | 10-30-2008 |
20080269253 | Substituted Benzofused Derivatives and Their Use as Vanilloid Receptor Ligands - The present invention relates to substituted benzofused derivatives, which can be used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them. | 10-30-2008 |
20080269254 | KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFIC DISEASES AND OTHER PROLIFERATIVE DISEASES - Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant, melanomas, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, leukemias, papillary thyroid carcinoma, non small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocyctosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof. | 10-30-2008 |
20080269255 | 4-Phenylpiperidine Derivatives as Renin Inhibitors - Compounds of the present invention having the formula (I) exhibit inhibitory activity on the natural enzyme renin. Thus, compounds of formula (I) may be employed for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders. | 10-30-2008 |
20080269256 | PYRIDINE-2-CARBOXYAMIDE DERIVATIVES - The invention relates to compounds of formula I: | 10-30-2008 |
20080275062 | Chemical Compounds - There is provided compounds of Formula (I) and salts, solvates, and physiologically functional derivatives thereof: | 11-06-2008 |
20080275063 | Inhibitors of protein kinases - The present invention provides new compounds. The compounds are useful as CDK5 inhibitors, and accordingly they can be included in pharmaceutical compositions for treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases. | 11-06-2008 |
20080275064 | Substituted Pyrimidines as Adenosine Receptor Antagonists - Compounds of formula (I), including pharmaceutically acceptable salts, esters, solvates and stereoisomers thereof, R | 11-06-2008 |
20080280924 | PYRIDINE AND PYRIMIDINE DERIVATIVES AS MGLUR2 ANTAGONISTS - The present invention relates to compounds of formula (I) | 11-13-2008 |
20080287461 | Pyridinone Derivatives Against Malaria - 4-pyridone derivatives of Formula (1) and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations thereof and their use in chemotherapy of certain parasitic infections such as malaria, are provided. | 11-20-2008 |
20080287462 | NEW COMPOUNDS 834 - This invention relates to novel compounds having the structural formula I below: | 11-20-2008 |
20080293743 | Novel Hydantoin Derivatives as Metalloproteinase Inhibitors - The invention provides compounds of formula (I): wherein R | 11-27-2008 |
20080306091 | AMINO-5-(5-MEMBERED)HETERO-ARYLIMIDAZOLONE COMPOUNDS AND THE USE THEREOF FOR beta-SECRETASE MODULATION - The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I | 12-11-2008 |
20080318976 | Alpha-Hydroxy Amides as Bradykinin Antagonists or Inverse Agonists - α-Hydroxy amide derivatives of the general formula (I) are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. R | 12-25-2008 |
20080318977 | Condensed Pyridines as Kinase Inhibitors - New compounds of formula (I), wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors. | 12-25-2008 |
20090005399 | Substituted Imidazo[2,1-b]thiazole Compounds and Uses Thereof - Substituted imidazo[2,1-b]thiazole compounds corresponding to formula I, | 01-01-2009 |
20090012100 | Selective Insecticides Based on Substituted Cyclic Ketoenols and Safeners - The present invention relates to the use of selective insecticidal compositions, characterized in that they comprise an effective amount of an active compound combination comprising
| 01-08-2009 |
20090012101 | Mucarinic Agonists and Methods of Use Thereof - A method of forming analogs of CDD-0304, i.e., tetra(ethyleneglycol) (4-methoxy-1,2,5-thiadiazol-3-yl)[3-(1-methyl-1,2,4,5-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl]ether hydrochloride includes one or more of the following steps: a) replacing the tetrahydropyridine moiety with one of the following heterocyclic rings, including quinuclidine, [2.2.1]-exo-azabicy-cloheptane, [2.2.1]-endo-azabicycloheptane and terahydropyrimidine; b) varying the length of the linking group by replacing the tetra(ethylene) glycol moiety with one of: ethylene glycol, di(ethylene) glycol, penta(ethylene) glycol, or diether diol; and/or, c) replacing the 1,2,5-thiadiazole moiety with an ester isostere. Also, a method for an asymmetric analog CCD-0304 includes replacing at least one moiety with an ester isostere and at least a second moiety with an ammonium isostere. Also, such analogs compounds and their uses are disclosed. | 01-08-2009 |
20090023752 | N-Heterocyclylphthaldiamides as Insecticides - New N-heterocyclylphthaldiamides of structure (I) | 01-22-2009 |
20090023753 | 1,3-Thiazole-5-Carboxamides Useful as Cancer Chemotherapeutic Agents - This invention relates to novel 1,3-thiazole-5-carboxamide compounds, pharmaceutical compositions containing such compounds, and the use of those compounds or compositions as cancer chemotherapeutic agents. | 01-22-2009 |
20090030017 | THERAPEUTIC AGENT FOR DYSKINESIA - The present invention relates to a therapeutic agent for dyskinesia excluding tremor, comprising 1,2-dihydropyridine compound, a salt thereof, or a solvate thereof, which shows AMPA receptor antagonism and is highly useful as a pharmaceutical drug. | 01-29-2009 |
20090030018 | Benzimidazole derivatives and their use for modulating the gabaalpha receptor complex - This invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. | 01-29-2009 |
20090042909 | METHOD OF TREATING DERMATOLOGICAL DISORDERS - A method of treating a dermatological disorder in a subject includes the step of administering a therapeutically effective amount of at least one PPARγ agonist or derivative thereof to the subject. | 02-12-2009 |
20090042910 | QUINOLINE DERIVATIVES FOR TREATING CANCER - The invention concerns quinoline derivatives of Formula I | 02-12-2009 |
20090042911 | Drug combinations comprising (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyri- midin-5-YL](3R,5S)-3, 5-dihydroxyhept-6-enoic acid and an inhibitor, inducer or substrate of P450 isoenzyme 3A4 - The invention concerns safe non-interacting drug combinations of a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, which is (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl] (3R,5S)-3,5-dihydroxyhept-6-enoic acid or a pharmaceutically acceptable salt thereof (the Agent) and a drug which is either an inducer, inhibitor or a substrate of cytochrome P450, in particular cytochrome P450 isoenzyme 3A4. Particular combinations are useful in treating hyperlipidaemia in humans who are receiving immunosuppressive chemotherapy. A preferred combination is the Agent and a fibrate drug, the use of such a combination in treating hyperlipidaemia in mammals, and medicaments containing such a combination for use in such treatments. | 02-12-2009 |
20090048270 | Compounds, Methods And Devices for Inhibiting Neoproliferative Changes in Blood Vessel Walls - Methods, compositions and devices for inhibiting neoproliferative changes in blood vessel walls or other anatomical structures. One or more compounds of Formula I or I-A set forth herein are administered systemically and/or locally to human or veterinary patients to deter or prevent unwanted proliferative changes in blood vessels or other anatomical structures. The invention may be used to deter or prevent stenosis or restenosis of arteries following angioplasty and/or stent placement. In one embodiment, there is provided an implantable stent or stent graft from which one or more compounds of the present invention will elute or otherwise be delivered into an affected blood vessel wall. | 02-19-2009 |
20090054466 | Leukotriene B4 Inhibitors - Provided herein are compounds of the formula (I): | 02-26-2009 |
20090062310 | DEUTERIUM-ENRICHED VORICONAZOLE - The present application describes deuterium-enriched voriconazole, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-05-2009 |
20090069346 | SOLID HERBICIDAL COMPOSITION - To provide a solid herbicidal composition in which decomposition of the herbicidal active ingredient is suppressed, and favorable herbicidal activity is stably exhibited. A solid herbicidal composition comprising (1) 1-(4,6-dimethoxypyrimidin-2-yl)-3-(3-trifluoromethyl-2-pyridylsulfonyl)urea or its salt and (2) at least one surfactant selected from the group consisting of a naphthalene sulfonate condensed with formaldehyde, an alkylnaphthalene sulfonate condensed with formaldehyde, a dialkylnaphthalene sulfonate condensed with formaldehyde and a polycarboxylate. | 03-12-2009 |
20090076033 | Method for treating atherosclerosis employing an aP2 inhibitor and combination - A method is provided for treating atherosclerosis and related diseases, employing an aP2 inhibitor or a combination of an aP2 inhibitor and another antiatheroscletotic agent, for example, an HMG CoA reductase inhibitor such as pravastatin. | 03-19-2009 |
20090093499 | Pharmaceutical composition - A chemically stable formulation of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]-(3R, 5S)-3,5-dihydroxyhept-6-enoic acid or a pharmaceutically-acceptable salt thereof for oral use, such as tablets, capsules, powders, granules has been developed using the substances which stabilize against formation of degradation products: lactone and oxidation product. | 04-09-2009 |
20090093500 | PESTICIDAL COMPOSITIONS - The invention disclosed in this document is related to field of pesticides and their use in controlling pests. | 04-09-2009 |
20090093501 | Heterocyclic antiviral compounds - This invention relates to piperidine derivatives of formula I wherein R | 04-09-2009 |
20090099205 | Chemokine receptor binding compounds - The present invention relates to chemokine receptor binding compounds, pharmaceutical compositions and their use. More specifically, the present invention relates to modulators of chemokine receptor activity, preferably modulators of CCR5. These compounds demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV). | 04-16-2009 |
20090099206 | SOLID FORMS OF (S)-2-AMINO-3-(4-(2-AMINO-6-((R)-2,2,2-TRIFLUORO-1-(3'-METHOXYBIPHENYL-4-- YL)ETHOXY)PYRIMIDIN-4-YL)PHENYL)PROPANOIC ACID AND METHODS OF THEIR USE - Solid forms of (S)-2-amino-3-(4-(2-amino-6-((R)-2,2,2-trifluoro-1-(3′-methoxybiphenyl-4-yl)ethoxy)pyrimidin-4-yl)phenyl)propanoic acid and salts thereof are disclosed. | 04-16-2009 |
20090099207 | Cyclic sulfones useful as BACE inhibitors - The invention relates to novel heterocyclic compounds of the formula | 04-16-2009 |
20090099208 | NOVEL GUANIDINE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel guanidine derivatives useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention. | 04-16-2009 |
20090099209 | Compounds Useful in Therapy - Compounds of formula (I), | 04-16-2009 |
20090105278 | Selective inhibitors of human corticosteroid syntheses - The invention relates to compounds for selectively inhibiting human corticosteroid syntheses CYP11B1 and CYP11B2, to the production thereof and to their use for treating hypercortisolism and diabetes mellitus or insufficiency of the heart and myocardial fibrosis. | 04-23-2009 |
20090105279 | Antiviral protease inhibitors - The invention is related to compounds of Formula I: | 04-23-2009 |
20090105280 | Novel Aromatic Nitro Compounds - Pharmaceutical compositions comprising at least one compound of e.g. the formulas (Ie) and a pharmaceutically acceptable carrier which is useful in a medicine | 04-23-2009 |
20090124635 | CHEMICAL COMPOUNDS - The present invention provides compounds of formula (I) wherein R | 05-14-2009 |
20090124636 | CHEMICAL COMPOUNDS - The present invention provides compounds of formula (I) wherein R | 05-14-2009 |
20090137609 | VITAMIN D-LIKE COMPOUND - The present invention provides a compound represented by the following general formula (I): | 05-28-2009 |
20090137610 | SPIRO IMIDOZOLE DERIVATIVES AS PPAR MODULATORS -
The invention provides compounds (Ia), (Ib) and (Ic), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families. | 05-28-2009 |
20090137611 | Fungicide N-Cyclopropyl-Sulfonylamide Derivatives - The present invention relates to N-cyclopropyl-sulfonylamide derivatives of formula (I) wherein the substituents are cyclic groups, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions: (I) | 05-28-2009 |
20090143410 | Isoxazolines for Controlling Invertebrate Pests - Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, | 06-04-2009 |
20090149476 | Novel vitronectin receptor antagonist derivatives, method for preparing same, use thereof as medicines and pharmaceutical compositions containing same - A subject of the invention is the compounds of formula (I): | 06-11-2009 |
20090149477 | 4,5-DIPHENYL-PYRIMIDINYL SUBSTITUTED CARBOXYLIC ACIDS, METHOD FOR THE PRODUCTION AND USE THEREOF AS MEDICAMENTS - This invention relates to a compound of formula I, | 06-11-2009 |
20090163516 | CARBOXAMIDES FOR CONTROLLING UNDESIRED MICRO-ORGANISMS IN PLANT PROTECTION - Novel carboxamides of the formula (I) | 06-25-2009 |
20090163517 | BENZOOXAZOLE, OXAZOLOPYRIDINE, BENZOTHIAZOLE AND THIAZOLOPYRIDINE DERIVATIVES - This invention is concerned with compounds of the formula | 06-25-2009 |
20090163518 | Novel Compounds - The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders. | 06-25-2009 |
20090176807 | GLUCOCORTICOID MIMETICS, METHODS OF MAKING THEM, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF - Compounds of Formula (I) | 07-09-2009 |
20090186908 | Use of 3-hydroxy-3-methylglutaryl coenzym a reductase inhibitors for the manufacture of a medicament for the treatment of diabetic neuropathy - The present invention relates to a new use of a statin drug in the improvement of diabetic neuropathy, specifically in improving nerve conduction velocity and nerve blood flow in patients suffering diabetes, in particular to pharmaceutical combinations of the statin drug and other agents known to improve diabetic neuropathy such as an aldose reductase inhibitor (ARI), an angiotensin converting enzyme (ACE) inhibitor or an angiotensin II (AII) antagonist which combinations are useful in the prevention and treatment of the complications of diabetes. | 07-23-2009 |
20090186909 | Oxadiazolidinedione Compound - [Problem] A compound which can be used as a pharmaceutical, particularly a insulin secretion promoter or a agent for preventing/treating disease in which GPR40 is concerned such as diabetes or the like, is provided. | 07-23-2009 |
20090192174 | Novel Aminopyridine Derivatives Having Aurora a Selective Inhibitory Action - The present invention relates to a compound of general formula I: | 07-30-2009 |
20090221610 | Compositions and Methods for Treating Cognitive Disorders - The present invention relates to the use of inhibitors or blockers of I | 09-03-2009 |
20090221611 | Fused Triazole Tachykinin Receptor Antagonists - The present invention is directed to certain fused triazole compounds which are useful as neurokinin-1 (NK-I) receptor antagonists, and inhibitors of tachykinin and in particular substance P- The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety. | 09-03-2009 |
20090247551 | SUBSTITUTED ENAMINOCARBONYL COMPOUNDS - The present invention relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects. | 10-01-2009 |
20090253715 | HETEROARYL-CONTAINING ISOFLAVONES AS AROMATASE INHIBITORS - Compounds and methods useful for treating and prevention of cancer, particularly hormone-dependent breast cancer. Provided are compounds of formula I: | 10-08-2009 |
20090258885 | Diphenylmethane Derivatives as Inhibitors of Leukotriene Biosynthesis - The instant invention provides compounds of Formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. | 10-15-2009 |
20090264446 | Condensed Pyridines as Kinase Inhibitors - New compounds of formula (I), wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors. | 10-22-2009 |
20090264447 | Pyrimidine compounds for combating pathogenic fungi and cancer - The present invention relates to the use of pyrimidine compounds of formula I | 10-22-2009 |
20090270422 | GPR119 receptor agonists in methods of increasing bone mass and of treating osteoporosis and other conditions characterized by low bone mass, and combination therapy relating thereto - The present invention relates to the use of GPR119 receptor agonists for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. The present invention further relates to the use of a GPR119 receptor agonist in combination with a dipeptidyl peptidase IV (DPP-IV) inhibitor for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. A GPR119 receptor agonist and the combination of a GPR119 receptor agonist and a DPP-IV inhibitor promote bone formation in an individual. | 10-29-2009 |
20090270423 | ANTIBACTERIAL SMALL MOLECULES AND METHODS FOR THEIR SYNTHESIS - The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use. | 10-29-2009 |
20090275598 | Conformationally constrained 3-(4-hydroxy-phenyl)-substituted-propanoic acids useful for treating metabolic disorders - The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: | 11-05-2009 |
20090281119 | ACID ADDITION SALTS OF N-ETHYI-N'-[2-METHOXY-4-(5-METHYI-4-PRYIMIDIN-2-YL)PHENYL]UREA AND USES THEREOF - The present invention provides an acid addition salt of N-ethyl-N′-[2-methoxy-4-(5-methyl-4-{[(1S)-1-pyridin-3-ylbutyl]amino}pyrimidin-2-yl)phenyl]urea and uses thereof including a method for the treatment of a hyperproliferation-related disorder. The present invention also provides a pharmaceutical composition comprising an acid addition salt of N-ethyl-N′-[2-methoxy-4-(5-methyl-4-{[(1S)-1-pyridin-3-ylbutyl]amino}pyrimidin-2-yl)phenyl]urea. | 11-12-2009 |
20090286810 | Pyrimidine Non-Classical Cannabinoid Compounds and Related Methods of Use - Disclosed are compounds of the formula I: | 11-19-2009 |
20090291968 | SUBSTITUTED INDAZOLE DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS - Objects of the present invention are the compounds of formula I | 11-26-2009 |
20090291969 | Fungicide hydroximoyl-tetrazole derivatives - The present invention relates to hydroximoyl-tetrazole derivatives of formula (I) wherein T represent a tetrazolyl substituent, A represents a carbo- or heterocycle, L | 11-26-2009 |
20090291970 | Substituted Aminoethers for the Treatment of Alzheimer's Disease - The invention provides compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation. | 11-26-2009 |
20090298854 | Indole acetic acid derivatives and their use as pharmaceutical agents - This invention is directed to indole acetic acid derivatives and their use in pharmaceutical compositions for the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic disease. The invention is also directed to intermediates useful in preparation of indole acetic derivatives and to methods of preparation. | 12-03-2009 |
20090298855 | Protein Tyrosine Kinase Inhibitors - The present invention relates to compounds of the Formula I, the pharmaceutically acceptable salts and stereoisomers thereof, which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions in mammals: | 12-03-2009 |
20090306096 | Novel Isoxazoles and Methods of Use Thereof - The invention relates to isoxazole derivatives, compositions comprising such compounds, and methods of preventing or treating conditions and disorders using such compounds and compositions. | 12-10-2009 |
20090318474 | PYRIDINE AND PYRIMIDINE DERIVATIVES AS MGLUR 2 ANTAGONISTS - The present invention relates to compounds of formula (I), a process for the manufacture thereof, pharmaceutical compositions containing them, and their use for treating CNS disorders: | 12-24-2009 |
20090325981 | Compounds and compositions as lxr modulators - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs). | 12-31-2009 |
20100004268 | Optically Pure Dihydropyrimidine Compounds and Their Uses for the Preparation of a Medicament for Treatment and Prevention of Viral Diseases - The present invention relates to an optically pure compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof, a process for preparing the optically pure compound of formula (I), and use of the optically pure compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof as a medicament, in particular as a medicament for the treatment and prevention of type B hepatitis. | 01-07-2010 |
20100010013 | DIHYDROPYRIMIDINE COMPOUNDS AND THEIR USES IN MANUFACTURE OF A MEDICAMENT FOR TREATMENT AND PREVENTION OF VIRAL DISEASES - The present invention relates to compounds of the formula (I) or pharmaceutically acceptable salts or hydrates thereof. The present invention further relates to processes for the preparation of the compounds of formula (I) and optical isomers and to use of the compounds of formula (I), isomers, pharmaceutically acceptable salts or hydrates thereof as medicaments, in particular as medicaments for the treatment and prevention of Hepatitis B. | 01-14-2010 |
20100010014 | AMINOPYRIMIDINE COMPOUNDS AND METHODS OF USE - The invention relates to aminopyrimidine compounds useful for treating diseases mediated by polo-like kinase 1 (Plk1). The invention also relates to the therapeutic use of such aminopyrimidine compounds and compositions thereof in treating disease states associated with abnormal cell growth and unwanted cell proliferation. | 01-14-2010 |
20100016337 | HETEROARYL-SUBSTITUTED CARBOXAMIDES AND THEIR USE AS PHARMACEUTICALS - The present invention relates to heteroaryl-substituted carboxamides of the formula I, | 01-21-2010 |
20100016338 | 5-[(3,3,3-Trifluoro-2-hydroxy-1-arylpropyl)amino]-1-arylquinolin-2-ones, a Process for their Production and their Use as Anti-inflammatory Agents - The present invention relates to compounds of formula I, | 01-21-2010 |
20100022559 | BISOXIMES AS FUNGICIDES - The invention relates to the novel use of bisoximes, some of which are known, for controlling unwanted microorganisms, and to processes for their preparation, and also to novel bisoximes, to processes for their preparation and to their use for controlling unwanted microorganisms and insects in crop protection and in the protection of materials. | 01-28-2010 |
20100029689 | PHOSPHODIESTERASE 4 INHIBITORS - PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: | 02-04-2010 |
20100029690 | NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS - Nitrogen-containing heterocyclic compounds represented by the following Formula (1) are provided. The compounds or salts thereof have a strong EP1 antagonistic activity when they are administered to a human or an animal, and they are useful as an effective component of a pharmaceutical agent for prophylaxis and/or treatment of an overactive bladder, for example. Furthermore, they are useful as an effective component of a pharmaceutical agent for the prophylaxis and/or treatment of symptoms including frequent urination, urinary urgency and urinary incontinence. | 02-04-2010 |
20100035897 | Pyridine, pyrimidine and pyrazine derivatives as gpcr agonists - Compounds of formula (I): R | 02-11-2010 |
20100041675 | METHODS FOR THE USE OF PYRIMIDINE DERIVATIVES WHICH ARE ANTAGONISTS OF VITRONECTIN RECEPTOR - A subject of the invention is the compounds of formula (I); | 02-18-2010 |
20100056547 | OPHTHALMIC COMPOSITIONS COMPRISING dDC - A composition comprising dDC and a polymer, wherein the composition is an aqueous liquid with a viscosity which increases upon contact with a surface of an eye is disclosed herein. | 03-04-2010 |
20100063065 | THIOPHENE DERIVATIVES AS PPAR AGONISTS I - The invention discloses compounds of formula (I); wherein: R is a carboxylic acid or a derivative thereof; R | 03-11-2010 |
20100063066 | RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF - Compounds of Formulas (I), (IIA) and (IIIA) are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formulas (I), (IIA) and (IIIA) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 03-11-2010 |
20100063067 | CYCLIC DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY - The present application describes modulators of MIP-1α of formula (I), or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n, A, T, R | 03-11-2010 |
20100063068 | Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, II, III, IV, and V, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 03-11-2010 |
20100063069 | GYRASE INHIBITORS AND USES THEREOF - The present invention relates to compounds that inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals. | 03-11-2010 |
20100069405 | DERIVATIVES OF HETEROARYL-ALKYLCARBAMATES, METHODS FOR THEIR PREPARATION AND USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS - The present invention is directed to compounds and compositions for the treatment of neurological diseases that cause neurogenic and neuropathic pain, inflammatory diseases, renal ischaemia, cardiovascular disease and other pathologies caused by the presence of endogenous cannabinoids and or other substrates resulting from the metabolic activities of fatty acid amido hydrolase (FAAH). These compounds are represented by the formula (I): | 03-18-2010 |
20100075990 | MULTIHETEROARYL COMPOUNDS AS INHIBITORS OF H-PGDS AND THEIR USE FOR TREATING PROSTAGLANDIN D2 MEDIATED DISEASES - Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin D | 03-25-2010 |
20100075991 | Post-translational regulation of catalytic activities of cytochrome P450 46A1 and uses thereof - Provided herein are methods and compounds for post-translational regulation of cytochrome P450 46A1 (CYP46A1) enzyme activity in the brain and retina. Also, a method for identifying a potential regulator of a CYP46A1 enzyme using crystal structures of the enzyme and a subsequent method for screening for a regulatory activity in the presence of CYP46A1 enzyme are provided. In addition, the regulator compounds that either inhibit or stimulate cholesterol hydroxylation by the CYP46A1 enzyme are provided. Further provided is a method of treating a pathoneurological condition associated with increased cholesterol levels in the brain and retina using the stimulatory compounds. | 03-25-2010 |
20100087448 | Dihydropyrimidine Compounds and Their Uses in Preparation of Medicaments for Treating and Preventing Antiviral Diseases - The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof, to a process for preparing the compound of formula (I), and to use of the compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof as a medicament, in particular as a medicament for the treatment and prevention of type B hepatitis. | 04-08-2010 |
20100087449 | HETEROARYLAMIDE PYRIMIDONE COMPOUNDS - The present invention discloses a series of pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: | 04-08-2010 |
20100093758 | PYRIDINE SULFONAMIDE MODULATORS OF ENDOTHELIN-A RECEPTOR - The present invention relates to new pyridine sulfonamide modulators of endothelin-A receptor, pharmaceutical compositions thereof, and methods of use thereof. | 04-15-2010 |
20100093759 | BICYCLIC ANILIDE HETEROCYCLIC CGRP RECEPTOR ANTAGONISTS - Compounds of formula I: I (wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved. | 04-15-2010 |
20100099689 | METHODS OF MODULATING PPAR GAMMA-TYPE RECEPTORS - Novel compounds having the general formula (I) below: | 04-22-2010 |
20100105701 | GYRASE INHIBITORS AND USES THEREOF - The present invention relates to compounds which inhibit bacterial gyrase and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals. The present invention also relates to a method for preparing these compounds. | 04-29-2010 |
20100105702 | Heterocyclylethylamide derivatives - A compound of general formula (I). A process for preparing this compound. A fungicide composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it. | 04-29-2010 |
20100105703 | Synthetic Mimetics Of Host Defense And Uses Thereof - The present invention provides arylamide compounds and methods of making and using them as antibiotics. | 04-29-2010 |
20100113479 | PROCESS FOR THE PREPARATION OF TRI-SUBSTITUTED PYRIDINE AND TRI-SUBSTITUTED PYRIMIDINE DERIVATIVES USEFUL AS GDIR AGONISTS - The present invention is directed to novel processes for the preparation of tri-substituted pyridine and tri-substituted pyrimidine derivatives, useful as glucose dependent insulinotropic receptor agonist, for the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity. | 05-06-2010 |
20100113480 | PROCESS FOR THE PREPARATION OF TRI-SUBSTITUTED PYRIDINE AND TRI-SUBSTITUTED PYRIMIDINE DERIVATIVES USEFUL AS GDIR AGONISTS - The present invention is directed to novel processes for the preparation of tri-substituted pyridine and tri-substituted pyrimidine derivatives, useful as glucose dependent insulinotropic receptor agonist, for the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity. | 05-06-2010 |
20100113481 | USE OF SERUM AMYLOID A GENE IN DIAGNOSIS AND TREATMENT OF GLAUCOMA AND IDENTIFICATION OF ANTI-GLAUCOMA AGENTS - The present invention provides compositions and methods for treating glaucoma, methods for diagnosing glaucoma, and methods for identifying agents which may be useful in the treatment of glaucoma. More specifically, the present invention describes the use of agents that modulate the expression of serum amyloid A, wherein such agents are inhibitors of p38 MAPkinase. | 05-06-2010 |
20100120795 | POWDERS FOR RECONSTITUTION - This invention relates to powders for reconstitution comprising the NNRTI TMC278 dispersed in certain water-soluble polymers, which can be used in the treatment of HIV infection. | 05-13-2010 |
20100130511 | HETEROCYCLIC RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS - Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control. The compounds of the invention are orally active. | 05-27-2010 |
20100137336 | NOVEL AMIDO DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to novel compounds of Formula (I), wherein X | 06-03-2010 |
20100137337 | CO-CRYSTALS - The present invention relates to co-crystals of cyprodinil or pyrimethanil and a co-crystal forming compound which has at least one organic acid functional group. In particular, the present invention relates to co-crystals of cyprodinil and benzoic acid, succinic acid, fumaric acid, maleic acid, oxalic acid, pyrazine carboxylic acid, glycolic acid, levulinic acid, (2-methylphenoxy)acetic acid, hexanedioic acid, 4-(methylamino) benzoic acid, trimethyl acetic acid, pyruvic acid or 4-hydroxy-4′-biphenyl carboxylic acid. | 06-03-2010 |
20100137338 | INHIBITORS OF Akt ACTIVITY - Invented are novel pyrazole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis. | 06-03-2010 |
20100144760 | NOVEL COMPOUNDS - Disclosed are N-{[(1R,4S,6R)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives and their use as pharmaceuticals. | 06-10-2010 |
20100144761 | Antimicrobial Molecules For Treating Multi-Drug Resistant And Extensively Drug Resistant Strains Of Mycobacterium - The present invention provides methods of inhibiting the growth of | 06-10-2010 |
20100144762 | NOVEL SULFONAMIDES AS L-CPT1 INHIBITORS - The invention is concerned with novel sulfonamide derivatives of formula (I) | 06-10-2010 |
20100168134 | PYRIDYL PIPERIDINE OREXIN RECEPTOR ANTAGONISTS - The present invention is. directed to pyridyl piperidine compounds of formula (I) which are antagonists of orexin receptors, and which are useful' in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 07-01-2010 |
20100184780 | INHIBITORS OF PROTEIN KINASES - The present invention provides new compounds. The compounds are useful as CDK5 inhibitors, and accordingly they can be included in pharmaceuticals compositions for treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases. formula (I). | 07-22-2010 |
20100184781 | FXA INHIBITORS WITH CYCLIC AMIDINES AS P4 SUBUNIT, PROCESSES FOR THEIR PREPARATIONS, AND PHARMACEUTICAL COMPOSITIONS AND DERIVATIVES THEREOF - The present invention relates to novel oxazolidinone derivatives with cyclic amidines, and prodrugs, hydrates, solvates, isomers and pharmaceutically acceptable salts thereof, and processes for preparing the same, and pharmaceutical compositions comprising the same. The oxazolidinone derivatives with cyclic amidines, and prodrugs, hydrates, solvates, isomers and pharmaceutically acceptable salts thereof can be usefully employed as an anticoagulant for treating thromboembolism and tumors via inhibition of coagulation factor Xa. | 07-22-2010 |
20100190803 | BIS(STYRYL)PYRIMIDINE OR BIS(STYRYL)BENZENE COMPOUNDS, PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTION OR TREATMENT OF DISEASES FEATURING AMYLOIDS COMPRISING THE SAME AS AN ACTIVE INGREDIENT - Disclosed are bis(styryl)pyrimidine or bis(styryl)benzene compounds, represented by Chemical Formula 1, pharmaceutically acceptable salts, a method for preparing the same, and a pharmaceutical composition for the prevention and treatment of amyloidosis-associated diseases, comprising the same as an active ingredient. Having the ability to inhibit the deposition of beta amyloid and to reduce the toxicity of beta amyloid, the derivatives can improve learning and memory and can be useful in the prevention and treatment of amyloidosis-associated diseases. | 07-29-2010 |
20100204246 | 5-AMINOPYRAZOL-3-YL-3H-IMIDAZO (4,5-B) PYRIDINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CANCER - The present invention relates to compounds of Formula (I) and to their pharmaceutical compositions, and to their methods of use. These novel compounds provide a treatment for myeloproliferative disorders and cancer. | 08-12-2010 |
20100204247 | N-SUBSTITUTED OXINDOLINE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS - A series of N-substituted oxindole derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. | 08-12-2010 |
20100210666 | METHODS OF USING A G PROTEIN-COUPLED RECEPTOR TO IDENTIFY PEPTIDE YY (PYY) SECRETAGOGUES AND COMPOUNDS USEFUL IN THE TREATMENT OF CONDITIONS MODULATED BY PYY - The present invention relates to methods of using GPR119 receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY, such as conditions modulated by stimulation of NPY Y2 receptor (Y2R). Agonists of GPR119 receptor are useful as therapeutic agents for treating or preventing a condition modulated by PYY, such as a condition modulated by stimulation of Y2R. Conditions modulated by PYY such as may be a condition modulated by stimulation of Y2R include bone-related conditions, metabolic disorders, angiogenesis-related conditions, ischemia-related conditions, convulsive disorders, malabsorptive disorders, cancers, and inflammatory disorders. | 08-19-2010 |
20100216817 | Antitumoral Tetrahydro-Pyrimidines - Antitumoral compounds of the formula (I) wherein X is O, S, or NRa, obtained from a maze coral of the family Meandrinidae, genus | 08-26-2010 |
20100216818 | Inhibitors of Post-Amadori Advanced Glycation End Products - The present invention provides compounds, pharmaceutical compositions, and methods for treating or inhibiting development of AGE- and/or ALE-associated complications in subjects in need thereof. | 08-26-2010 |
20100234398 | INSECTICIDAL N-SUBSTITUTED (HETEROARYL)ALKYL SULFILIMINES - N-Substituted (heteroaryl)alkyl sulfilimines are effective at controlling insects. | 09-16-2010 |
20100240678 | LEUKOTRIENE B4 INHIBITORS - Provided herein are compounds of the formula (I): | 09-23-2010 |
20100240679 | 4-Phenylpiperidine Derivatives as Renin Inhibitors - Compounds of the present invention having the formula | 09-23-2010 |
20100249149 | Inhibitors of Protein Kinases - are useful as inhibitors of cyclin dependent kinases such as CDK9. | 09-30-2010 |
20100267747 | 5-(Arylsulfonyl)-Pyrazolopiperidines - The invention provides N-cyclic sulfonamido compounds of Formula I | 10-21-2010 |
20100273814 | ((PHENYL)IMIDAZOLYL)METHYLHETEROARYL COMPOUNDS - Disclosed herein is a compound of the formula wherein A and B are described herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed. | 10-28-2010 |
20100286172 | COMBINATION THERAPY FOR THE TREATMENT OF DIABETES AND CONDITIONS RELATED THERETO AND FOR THE TREATMENT OF CONDITIONS AMELIORATED BY INCREASING A BLOOD GLP-1 LEVEL - The present invention concerns combination of an amount of a GPR119 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-1 level in a subject over that provided by the amount of the GPR119 agonist or the amount of the DPP-IV inhibitor alone and the use of such a combination for treating or preventing diabetes and conditions related thereto or conditions ameliorated by increasing a blood GLP-1 level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-1 secretagogues. | 11-11-2010 |
20100286173 | FUNGICIDE HYDROXIMOYL-TETRAZOLE DERIVATIVES - The present invention relates to hydroximoyl-tetrazole derivatives, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. | 11-11-2010 |
20100292253 | PESTICIDAL COMPOSITIONS - This document discloses molecules having the following formula (“Formula I”): | 11-18-2010 |
20100298344 | Polycationic Compounds And Uses Thereof - Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis. | 11-25-2010 |
20100298345 | SYNTHETIC COMPOUNDS AND DERIVATIVES AS MODULATORS OF SMOKING OR NICOTINE INGESTION AND LUNG CANCER - Disclosed are nicotine-related compounds that selectively inhibit cytochrome P-450 2A6 (CYP2A6), selectively inhibit cytochrome P-450 2A13 (CYP2A13), and/or selectively modulate a nicotinic acetylcholine receptor (nAChR). Also disclosed are pharmaceutical compositions comprising a compound of the invention, as well as methods of using the pharmaceutical compositions for treating or preventing a disease or disorder associated with nicotine-ingestion, or a disease or disorder amenable to treatment by selective modulation of nAChRs. | 11-25-2010 |
20100298346 | NITROGENOUS HETEROCYCLIC COMPOUNDS WITH INSECTICIDAL ACTIVITY, AND THE PREPARATION AND USE THEREOF - The present invention relates to nitro-containing heterocyclic or ring-opening nitrogenous compounds of formula (A), wherein R | 11-25-2010 |
20100305142 | 3-AMINOIMIDAZO 1,2-A PYRIDINE DERIVATIVES HAVING AN SGLT1- AND SGLT2-INHIBITING ACTION FOR THE TREATMENT OF TYPE 1 AND TYPE 2 DIABETES - Novel compounds of the formula (I), in which W, T, R | 12-02-2010 |
20100317675 | 6-HETEROCYCLIC-IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - Compounds of formula (I): | 12-16-2010 |
20100324072 | PYRROLOPYRIDINE DERIVATIVES AND THEIR USE AS BACE INHIBITORS - This invention relates to novel compounds having the structural formula I below: (I) and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia. | 12-23-2010 |
20110003833 | NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION - The present invention relates to a compound of formula I: wherein: R | 01-06-2011 |
20110009427 | ARYL PYRIMIDINE DERIVATIVES, PREPARATION METHODS AND PHARMACEUTICAL USES THEREOF - The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof. Various substituents in the formula (I) are as defined in the specification. The present invention also relates to a pharmaceutical composition comprising the compound of formula (I), the preparation method of compound of formula (I), and the use of the compound for the preparation of a medicament for treating and/or preventing human peroxisome proliferators activated receptor δ (hPPARδ)-associated diseases and risk factors. | 01-13-2011 |
20110009428 | NOVEL ANDROGENS - The compounds of the subject invention have a structure according to formula I: | 01-13-2011 |
20110021540 | Bis-(Sulfonylamino) Derivatives in Therapy 066 - The invention provides compounds of formula wherein R | 01-27-2011 |
20110028493 | HETEROCYCLIC DERIVATIVE AND USE THEREOF - The present invention aims to provide a compound having superior pharmacological action, physicochemical properties and the like and useful as an sGC activation drug, or an agent for the prophylaxis and/or treatment of diseases such as hypertension, ischemic cardiac disease, cardiac failure, kidney disease, arteriosclerotic disease, atrial fibrillation, pulmonary hypertension, diabetes, diabetic complications, metabolic syndrome, peripheral arterial obstruction, erectile dysfunction and the like. | 02-03-2011 |
20110034482 | AMINE SALTS OF A CRTH2 ANTAGONIST - Provided are amine salts of {4,6-bis(dimethylamino)-2-(4-(4-(trifluoromethyl)benzamido)benzyl)pyrimidin-5-yl}-acetic acid, processes for their preparation, pharmaceutical compositions containing them, and their use for treating, preventing, or ameliorating one or more symptoms of a CRTH2-mediated disorder or disease. | 02-10-2011 |
20110034483 | 2-AMINOIMIDAZOLE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE - The present invention is directed to 2-aminoimidazole compounds of formula (I) | 02-10-2011 |
20110034484 | 1,5-DIPHENYL-PYRROLIDIN-2-ONE COMPOUNDS AS CB-1 LIGANDS - CB-1 receptor inverse agonist compounds of Formula (I) and pharmaceutical compositions for the treatment of obesity or cognitive impairment associated with schizophrenia. | 02-10-2011 |
20110034485 | NITRONE COMPOUNDS, PROCESS OF PREPARATION THEREOF, AND USE THEREOF IN MEDICAMENT MANUFACTURE - The present invention provides novel nitrones, their preparation and use. The novel compounds have the following formula: I The compounds of the present invention have strong antioxidative activity, and are thrombolytic. These compounds can be used to treat and/or prevent diseases caused by overproduction of free radicals and/or formation of thrombus. | 02-10-2011 |
20110039865 | Phenyl(oxy/thio)alkanol Derivatives - The present invention relates to novel phenyl(oxy/thio)alkanol derivatives, to processes for preparing these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators. | 02-17-2011 |
20110039866 | SELECTIVE SPHINGOSINE-1-PHOSPHATE RECEPTOR ANTAGONISTS - Described herein are compounds useful as antagonists of sphingosine-1-phosphate receptors. Further described herein is the use of these compounds and related pharmaceutical compositions to treat disorders associated with sphingosine-1-phosphate-3 (S1P3) receptor modulation. | 02-17-2011 |
20110039867 | PYRIMIDINE DERIVATIVES WHICH ARE ANTAGONIST OF THE VITRONECTIN RECEPTOR - A subject of the invention is the compounds of formula (I); | 02-17-2011 |
20110059990 | Substituted Phenyl(oxy/thio)alkanol Derivatives - The present invention relates to novel substituted phenyl(oxy/thio)alkanol derivatives, to processes for preparing these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators. | 03-10-2011 |
20110059991 | Selective Insecticides Based on Anthranilic Acid Diamides and Safeners - The present invention relates to the use of selective insecticidal compositions, characterized by an effective amount of an active compound combination comprising
| 03-10-2011 |
20110059992 | New Compounds - This invention relates to novel compounds having the structural formula I below: | 03-10-2011 |
20110065726 | Organic Compounds - The present invention is directed to a compound of the formula: | 03-17-2011 |
20110065727 | POLYSUBSTITUTED DERIVATIVES OF 2-HETEROARYL-6-PHENYLIMIDAZO[1,2-a]PYRIDINES, AND PREPARATION AND THERAPEUTIC USE THEREOF - Compounds of formula (I): | 03-17-2011 |
20110071165 | Aza- and polyazanthranyl amides and their use as medicaments - Aza- and polyazanthranyl amides and their use as medicaments in the treatment of diseases caused by persistent angiogenesis are described, as well as the intermediates used in the preparation of the aza- and polyazanthranyl amides. | 03-24-2011 |
20110098312 | METHODS FOR PREVENTING THE DEVELOPMENT OF RETINOPATHY BY THE ORAL ADMINISTRATION OF NNR LIGANDS - Method and compositions for delaying the onset or progression of retinopathy, including administering at least one neuronal nicotinic ligand are disclosed. | 04-28-2011 |
20110105533 | Heterocyclic Sulfonamides, Uses and Pharmaceutical Compositions Thereof - The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: | 05-05-2011 |
20110105534 | MOLLUSCICIDE - The present invention relates to the use of compounds for the control of gastropods. In particular, it relates to a method of controlling gastropods using strobilurin compounds. | 05-05-2011 |
20110105535 | INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE - Compounds of formula I | 05-05-2011 |
20110112115 | POLYMERIC MICROEMULSIONS - The invention provides novel self-emulsifying diblock copolymers and novel self-emulsifying compositions comprising an active ingredient and a diblock copolymer characterized in that the diblock copolymer is liquid at a temperature below 50° C. and the composition is non-aqueous and liquid at a temperature below 50° C. | 05-12-2011 |
20110118283 | Substituted Pyrrolidine-2-Carboxamides - There are provided compounds of the formula | 05-19-2011 |
20110124663 | SUBSTITUTED DIOXOPIPERIDINES AND DIOXOPYRROLIDINES AS MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION - In one aspect, the invention relates to compounds having a general structure: | 05-26-2011 |
20110124664 | Polycationic Compounds And Uses Thereof - Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis. | 05-26-2011 |
20110130410 | PROCESS FOR PREPARING METHYL METHYLCARBAMATE AND ITS PURIFICATION FOR USE AS PHARMACEUTICALLY ACTIVE COMPOUND - The present invention relates to a process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate of the formula (I) | 06-02-2011 |
20110130411 | PROCESS FOR PREPARING METHYL CARBAMATE AND ITS PURIFICATION FOR USE AS PHARMACEUTICALLY ACTIVE COMPOUND - The present invention relates to processes for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate, i.e. the compound of the formula (I) | 06-02-2011 |
20110136833 | Tetrahydropyridinyl and Dihydropyrrolyl Compounds and the Use Thereof - The invention relates to tetrahydropyridinyl and dihydropyrrolyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X, Y, Z, R | 06-09-2011 |
20110144128 | Heterocyclic Carboxamide Compounds as Steroid Nuclear Receptors Ligands - Heterocyclic carboxamide compounds are described herein as being useful in modulating the activity of steroid nuclear receptors. Pharmaceutical compositions containing the compounds, methods of using the compounds and processes for making the compounds are also described. | 06-16-2011 |
20110144129 | 3-Aminocyclopentanecarboxamides as Chemokine Receptor Agonists - There is provided a compound of Formula I(a) or I(b) | 06-16-2011 |
20110144130 | Use of 5-(7-methoxy-3,3-dimethyl-2,3-dihydro-1-benzoxepin-5-yl)-3-methyl-p- enta-2,4-dienoic acid as a cosmetic - The invention relates to 5-(7-methoxy-3,3-dimethyl-2,3-dihydro-1-benzoxepin-5-yl)-3-methyl-penta-2,4-dienoic acid and its use in compositions, especially topical, cosmetic and/or personal care compositions, and compositions containing said compound. | 06-16-2011 |
20110152292 | SALTS COMPRISING A PYRIMIDINECARBOXYLIC ACID DERIVATIVE FOR COSMETIC USE - The invention relates to novel compounds which comprise, as cationic or as anionic component, a pyrimidinecarboxylic acid derivative, in particular a derivative of ectoin or hydroxyectoin, to a process for the preparation thereof, and to the use thereof as ionic liquid or to the use thereof in pharmaceutical, cosmetic and dermatological formulations. | 06-23-2011 |
20110152293 | ARYLVINYLAZACYCLOALKANE COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF - Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain. | 06-23-2011 |
20110152294 | USE OF OSMOLYTES OBTAINED FROM EXTREMOPHILIC BACTERIA FOR THE PRODUCTION OF INHALABLE MEDICAMENTS FOR THE PROPHYLAXIS AND TREATMENT OF PULMONARY AND CARDIOVASCULAR DISEASES AND AN INHALATION DEVICE COMPRISING OSMOLYTE AS ACTIVE AGENT COMPONENT - The invention relates to the use of osmolytes, for example, ectoine, hydroxyectoine, firoin, firoin-A, diglycerol phosphate, cyclic diphosphoglycerate, 1,3-dimannosyl-di-myo-inositol-phosphate (DMIP) and/or diinositol phosphate and their equally effective derivatives and/or pharmacologically acceptable salts thereof, for the combating of pulmonary diseases caused by the effect of airborne particles and/or causally related cardiovascular diseases. | 06-23-2011 |
20110152295 | HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE - Heteroaromatic compounds of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis. | 06-23-2011 |
20110166162 | 1,2-Benzisothiazole Compounds Useful for Combating Animal Pests - The present invention relates to sulfonamide compounds of formula (I) | 07-07-2011 |
20110178104 | Anti-Heparin Compounds - The present invention provides compounds and methods for antagonizing the anticoagulant effect of an anticoagulant agent that is selected from UFH, LMWH, and a heparin/LMWH derivative in a patient comprising administering to the patient a compound of the invention or a salt thereof, or a composition comprising the same. | 07-21-2011 |
20110183999 | NOVEL POLYMORPHIC FORMS OF METHYL CARBAMATE - The invention relates to novel forms of methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate of the formula (I), in particular to the modification I, to processes for their preparation, to medicaments comprising them and to their use for fighting diseases. | 07-28-2011 |
20110195980 | Bicyclic Kinase Inhibitors - New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer. | 08-11-2011 |
20110201626 | 4,6-DIAMINOPYRIMIDINE STIMULATORS OF SOLUBLE GUANYLATE CYCLASE - The present invention relates to new 4,6-diaminopyrimidine stimulators of soluble guanylate cyclase, pharmaceutical compositions thereof, and methods of use thereof. | 08-18-2011 |
20110207748 | Tri-Aryl/Heteroaromatic Cannabinoids and Use Thereof - Cannabinoid derivatives according to formula (I) are disclosed | 08-25-2011 |
20110207749 | Glycine Chroman-6-Sulfonamides for Use as Inhibitors of Diacylglycerol Lipase - The present disclosure is generally directed to compounds that can inhibit DAGLα and/or β activity, compositions comprising such compounds, and methods for inhibiting DAGLα and/or β activity. | 08-25-2011 |
20110207750 | BENZIMIDAZOLE AND AZA-BENZIMIDAZOLE CARBOXAMIDES - This invention provides compounds of Formula I which are PAFR antagonists: I and the pharmaceutically acceptable salts thereof. The compounds are useful for treating PAF-mediated disorders, and can be used in methods for treating atherosclerosis and preventing or reducing risk for atherosclerotic disease events. The compounds are also useful for treating or ameliorating pain, e.g. inflammatory pain and/or nociceptive pain, and for treating or ameliorating autoimmune and/or inflammatory diseases, among other conditions. | 08-25-2011 |
20110224232 | Treatment of Pulmonary Fungal Infection With Voriconazole via Inhalation - A method of treating fungal infection by pulmonary administration of a solution of voriconazole and cyclodextrin is provided The fungal infection can be a pulmonary infection. The solution can be an inhalable aqueous formulation that can be administered via the mouth or nose. The cyclodextrin can be a water soluble cyclodextrin derivative such as sulfoalkyl ether cyclodextrin. The formulation can be administered via a spray device or nebulizer. | 09-15-2011 |
20110224233 | STEM CELL CULTURES - The present invention relates compounds for stabilizing cells and methods of their use. | 09-15-2011 |
20110237605 | Molecular Crystal of (4-(1,8-Naphthyridin-2-YL)Piperidin-1-YL)Pyrimidine Derivative - A molecular crystal form of (S)-3-(2,5-dimethyl-6-(4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)piperidin- | 09-29-2011 |
20110245272 | PYRIDO[4,3-B]INDOLES AND METHODS OF USE - This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 10-06-2011 |
20110245273 | NOVEL ALIPHATICALLY SUBSTITUTED PYRAZOLOPYRIDINES, AND THE USE THEREOF - The present application relates to novel aliphatically substituted pyrazolopyridines, to processes for their preparation, to their use, alone or in combination, for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders. | 10-06-2011 |
20110245274 | ISOXAZOLINES DERIVATIVES AND THEIR USE AS PESTICIDE - Novel isoxazoline compounds, compositions containing the compounds and methods for making the compounds are disclosed. The compounds and compositions have pesticidal properties and are suitable for controlling ectoparasites on non-human animals. | 10-06-2011 |
20110257196 | COMPOUNDS FOR TREATMENT OF CANCER - The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer. | 10-20-2011 |
20110257197 | Pharmaceutical Formulations Comprising Voriconazole and Processes for Preparation Thereof - The present invention provides a pharmaceutical formulation comprising voriconazole or a pharmaceutically acceptable derivative thereof, and an excipient of formula (I), i.e., monomethoxy poly(ethylene glycol)-poly (D,L-lactic acid) block copolymers (mPEG-PDLLA). The pharmaceutical formulation of the present invention has been shown to be stable and safe by experiments. | 10-20-2011 |
20110257198 | PIPERIDINE DERIVATIVES USEFUL AS OREXIN ANTAGONISTS - Disclosed are imidazopyridylmethylene substituted piperidine derivatives of Formula (I): | 10-20-2011 |
20110257199 | NOVEL TERARYL COMPOUNDS AS ANTIPARASITIC AGENTS - Novel dicationic terphenyl compounds and their aza analogues. Methods for combating microbial infections with novel dicationic terphenyl compounds and their aza analogues. Processes for synthesizing novel dicationic terphenyl compounds and their aza analogues. | 10-20-2011 |
20110263613 | COMPOUNDS AND COMPOSITIONS FOR COGNITION-ENHANCEMENT, METHODS OF MAKING, AND METHODS OF TREATING - Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function. | 10-27-2011 |
20110263614 | Novel compounds - The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders. | 10-27-2011 |
20110263615 | PYRIDINE AND PYRIMIDINE DERIVATIVES AS MGLUR2 ANTAGONISTS - The present invention relates to compounds of formula (I) | 10-27-2011 |
20110281893 | COMPOUND, SYNTHESIS, COMPOSITION AND USES THEREOF - The instant application provides the disclosure for a compound of formula I, synthesis of compound of formula I and its pharmaceutical acceptable salts, as well as its polymorphs, solvates, and hydrates thereof. The pharmaceutically acceptable salt may be formulated for oral administration, systemic administration, transdermal administration and injection. The compound of formula I and its pharmaceutical compositions may be used to treat cancer in mammal. | 11-17-2011 |
20110281894 | HEMIFUMARATE SALT - The present invention relates to a hemifumarate salt of the compound (1S)-1-(2-(difluoromethyl)pyridin-4-yl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine, Form A thereof and its pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. | 11-17-2011 |
20110281895 | SYNTHESIS AND NOVEL SALT FORMS OF (R)-5-((E)-2-PYRROLIDIN-3YLVINYL)PYRIMIDINE - The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-yl)pyrimidine, novel salt forms, and novel polymorphic forms of these salts. | 11-17-2011 |
20110294828 | PROCESS FOR PREPARING A POLYMORPH OF THE CHOLINE SALT OF A PYRIMIDIN-5-YL ACETIC ACID DERIVATIVE - Provided is a process for preparing a choline salt of [4,6-bis(dimethylamino)-2-(4-{[4-(trifluoromethyl)benzoyl]amino}benzyl)pyrimidin-5-yl]acetic acid. The process of the invention is useful for preparing the salt in purer forms of the salt. Also disclosed is a more pure form of the of choline salt of [4,6-bis(dimethylamino)-2-(4-{[4-(trifluoromethyl)benzoyl]amino}benzyl)pyrimidin-5-yl]acetic acid. | 12-01-2011 |
20110294829 | FUNGICIDE HYDROXIMOYL-HETEROCYCLES DERIVATIVES - The present invention relates to hydroximoyl-heterocycle derivatives of formula (I) | 12-01-2011 |
20110294830 | NITROGEN-CONTAINING COMPOUNDS AND HARMFUL ORGANISM CONTROL AGENTS - The present invention provides a nitrogen-containing compound represented by formula (I | 12-01-2011 |
20110301180 | Reducing Platelet Activation, Aggregation and Platelet-Stimulated Thrombosis or Blood Coagulation by Reducing Mitochondrial Respiration - It has been discovered that inhibiting mitochondrial respiration in platelets reduces platelet activation or platelet aggregation. Certain heterocyclic compounds significantly reduced one or more platelet functions including clumping, sticking or platelet-stimulated clotting. Thus diseases or disorders mediated by inappropriately high levels of platelet activation or platelet aggregation can be treated by administering a therapeutically effective amount of a heterocyclic compound or nonheterocyclic mitochondrial inhibitor that significantly reduces one or more platelet functions including clumping, sticking or platelet-stimulated clotting, preferably in a reversible manner. | 12-08-2011 |
20110301181 | halogen-substituted compounds - The invention relates to compounds of the general formula (I), | 12-08-2011 |
20110306621 | ACYLGUANIDINE DERIVATIVES - An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on a serotonin 5-HT | 12-15-2011 |
20110312977 | PROCESS FOR THE PREPARATION OF VORICONAZOLE - The present invention provides a process for preparation of racemic voriconazole in a single reaction vessel. The present invention also provides a process for preparation of voriconazole using racemic voriconazole and the process of making it therewith. | 12-22-2011 |
20110319428 | THIAZOLE DERIVATIVES AS PESTICIDES - The present application relates to novel heterocyclic compounds, to their use for controlling animal pests including arthropods and in particular insects, and to processes for preparing the novel compounds. | 12-29-2011 |
20110319429 | SUBSTITUTED 1,1,3,1-TETRAOXIDOBENZO[D][1,3,2]DITHIAZOLES AS MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION - Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and methods of using the compounds. | 12-29-2011 |
20110319430 | FUNGICIDAL PYRAZOLES - Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, | 12-29-2011 |
20110319431 | Bis Aromatic Compounds for Use as LTC4 Synthase Inhibitors - There is provided compounds of formula I, | 12-29-2011 |
20120004244 | Bis Aromatic Compounds for Use as LTC4 Synthase Inhibitors - There is provided compounds of formula I, | 01-05-2012 |
20120010222 | Gyrase Inhibitors and Uses Thereof - The present invention relates to methods of treating, preventing, or lessening the severity of resistant bacterial infections in mammals, utilizing compounds of formula I or formula VII or pharmaceutically salts thereof. The present invention also relates to methods of using compounds of formula I or formula VII in combination with one or more additional antibacterial agents and/or one or more additional therapeutic agents that increase the susceptibility of bacterial organisms to antibiotics. | 01-12-2012 |
20120022084 | Substituted 5-fluoro-1H-pyrazolopyridines and their use - The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders. | 01-26-2012 |
20120035189 | Quinuclidine Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligands - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders. | 02-09-2012 |
20120041000 | IMIDAZO [1,2-A]PYRIDINE DERIVATIVES AS FGFR KINASE INHIBITORS FOR USE IN THERAPY - The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. | 02-16-2012 |
20120041001 | CARBONYLAMINO-DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I) | 02-16-2012 |
20120046304 | TRICYCLIC PYRIDINE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR PREPARATION - The present invention relates to compounds defined by formula I | 02-23-2012 |
20120071496 | Aminopyrimidinamides As Pest Control Agents - The present application relates to novel aminopyrimidinamides, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects. | 03-22-2012 |
20120083501 | COMPOUNDS FOR TREATING NEURODEGENERATIVE DISEASES - The invention provides novel tricyclic compounds of Formula I′ that inhibit β-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases. | 04-05-2012 |
20120095023 | Novel Heterocyclic Compounds as Pesticides - The present application relates to novel amides and thioamides, to processes for preparation thereof and to the use thereof for controlling animal pests, in particular arthropods and especially insects. | 04-19-2012 |
20120095024 | TOLUIDINE SULFONAMIDES AND THEIR USE - The present invention provides novel compounds that inhibit cell proliferation and cell division and that inhibit the activation of Hypoxia Inducible Factor (HIF)-mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularisation. Also provided is a pharmaceutical composition comprising a compound of the invention and a second therapeutic agent or radiation useful for the treatment or prevention of the mentioned diseases or disorders. In a first aspect the present invention relates to a compound having a structure according to formula (I). | 04-19-2012 |
20120115883 | PYRIMIDINE DERIVATIVES WHICH ARE ANTAGONISTS OF THE VITRONECTIN RECEPTOR - A subject of the invention is the compounds of formula (I); | 05-10-2012 |
20120115884 | INSECTICIDAL COMPOUNDS - A compound of formula (I) wherein A, p, R | 05-10-2012 |
20120115885 | Quinolinone PDE2 Inhibitors - The present invention is directed to quinolinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. | 05-10-2012 |
20120122887 | SOLID STATE FORMS OF A POTENT HCV INHIBITOR - This invention relates to novel sodium salt forms of the following Compound (1), and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection: | 05-17-2012 |
20120136009 | INDOLE DERIVATIVE MODULATORS OF THE ALPHA 7 NACHR - This invention relates to modulation of the α7 nicotinic acetylcholine receptor (nAChR) by a compound of formula (I) or a salt thereof: | 05-31-2012 |
20120142707 | MODIFIED C-3 BETULINIC ACID DERIVATIVES AS HIV MATURATION INHIBITORS - Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, modified C-3 betulinic acid and other structurally related natural products derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS. | 06-07-2012 |
20120142708 | SUBSTITUTED PYRIDINE UREA COMPOUNDS - The present disclosure provides pyridine urea compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): | 06-07-2012 |
20120142709 | SUBSTITUTED PYRIDINONE-PYRIDINYL COMPOUNDS - The present disclosure provides pyridinone-pyridinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): | 06-07-2012 |
20120142710 | Ketolide Compounds Having Antimicrobial Activity - The invention relates to ketolide compound of Formula-I and the pharmaceutically acceptable salts thereof having antimicrobial activity. The invention also provides pharmaceutical compositions containing the compounds of invention and methods of treating or preventing microbial infections with the compound of invention. | 06-07-2012 |
20120157477 | REVERSAL OF L-DOPA-INDUCED DYSKINESIA BY NEURONAL NICOTINIC RECEPTOR LIGANDS - The present invention includes methods, uses, and compounds for treating or preventing L-dopa-induced dyskinesias. | 06-21-2012 |
20120165344 | Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 06-28-2012 |
20120165345 | Heterocyclic compounds as pesticides - The present application relates to novel heterocyclic compounds, to the use thereof for controlling animal pests, which include arthropods and especially insects, and to processes for preparing the novel compounds. | 06-28-2012 |
20120165346 | Compounds and their use as BACE inhibitors - The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. | 06-28-2012 |
20120165347 | Compounds and their use as BACE Inhibitors - The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. | 06-28-2012 |
20120172377 | PYRIDO[4,3-B]INDOLES AND METHODS OF USE - New heterocyclic compounds that may be used to modulate a histamine receptor in an individual are described. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 07-05-2012 |
20120184564 | SOLID FORMS OF GYRASE INHIBITOR (R)-1-ETHYL-3-[6-FLUORO-5-[2-(1-HYDROXY-1-METHYL-ETHYL)PYRIMIDIN-5-YL]-7-- (TETRAHYDROFURAN-2-YL)-1H-BENZIMIDAZOL-2-YL]UREA - The present application is directed to solid forms of compounds of formula I: | 07-19-2012 |
20120190694 | SELECTIVE SPHINGOSINE-1-PHOSPHATE RECEPTOR ANTAGONISTS - Described herein are compounds useful as antagonists of sphingosine-1-phosphate receptors. Further described herein is the use of these compounds and related pharmaceutical compositions to treat disorders associated with sphingosine-1-phosphate-3 (S1P3) receptor modulation. | 07-26-2012 |
20120190695 | PHENYLOXADIAZOLE DERIVATIVES AS PGDS INHIBITORS - This invention is directed to a compound of formula (I): | 07-26-2012 |
20120196875 | PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF RESPIRATORY AND INFLAMMATORY DISEASES - The present invention relates to pharmaceutical composition comprising a CRTH2 antagonist and at least one PDE4 inhibitor, medicaments containing said pharmaceutical compositions, and the use of said pharmaceutical compositions for treating respiratory and inflammatory diseases and conditions. | 08-02-2012 |
20120214823 | NOVEL COMPOUNDS THAT ARE ERK INHIBITORS - Disclosed are the ERK inhibitors of formula 1.0: (Formula (A1)), and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine ring that can have a bridge or a fused ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula A1. | 08-23-2012 |
20120232099 | Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, II, III, IV, and V, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 09-13-2012 |
20120245185 | ARYL AND HETEROARYL SULFONES AS MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION - In one aspect, the invention relates to sulfone compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction. | 09-27-2012 |
20120277252 | Antibacterial Agents and Methods of Use Thereof - The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use. For example, the present invention provides chalcone and cyanopyridine compounds, and derivatives thereof, exhibiting high antibacterial activities having multiple electron withdrawing group substituents, such as halogens and fluorinated alkyl groups, and optionally having hydroxyl and/or alkoxyl groups substituents. | 11-01-2012 |
20120283273 | INDOLE AND AZAINDOLE MODULATORS OF THE ALPHA 7 NACHR - This invention relates to modulation of the α7 nicotinic acetylcholine receptor (nAChR) by a compound of formula (I) or a pharmaceutically acceptable salt thereof. | 11-08-2012 |
20120295922 | Compounds For Use In Treatment Of Mucositis - The present invention provides methods for treating and/or preventing mucostitis with one or more compounds, or pharmaceutically acceptable salts thereof, disclosed herein, or compositions comprising the same. | 11-22-2012 |
20120295923 | Aminocyclohexanes and Aminotetrahydropyrans and Related Compounds As Gamma-Secretase Modulators - Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I | 11-22-2012 |
20120302584 | NOVEL SALTS FORMS OF PYRIMIDIN-5-YL ACETIC ACID DERIVATIVE - Provided are crystalline N-methyl-glucamine and sodium salts of [4,6-bis(dimethylamino)-2-(4-{[4-(trifluoromethyl)benzoyl]amino}benzyl)pyrimidin-5-yl] acetic acid, processes for their preparation, pharmaceutical compositions comprising the salts, and methods of their use for treating, preventing, or ameliorating one or more symptoms of a CRTH2-mediated disorder or disease. | 11-29-2012 |
20120309770 | Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 12-06-2012 |
20120309771 | NOVEL ANTIFUNGAL TRIAZOLE DERIVATIVES - Disclosed are novel triazole derivatives. Exhibiting excellent antifungal activity and in vivo safety, they are useful for the treatment or prevention of fungal infections caused by a wide spectrum of fungi. | 12-06-2012 |
20120316183 | NOVEL SOLVATES OF METHYLCARBAMATE - The invention relates to novel solvates of methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate, in particular the semi-ethanol solvate of the formula (Ia), to processes for their preparation, to medicaments comprising them and to their use for controlling diseases | 12-13-2012 |
20120329812 | CERTAIN KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF - Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity. | 12-27-2012 |
20130005743 | New positive allosteric modulators of nicotinic acetylcholine receptor - The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor. | 01-03-2013 |
20130005744 | INHIBITORS OF CATECHOL O-METHYL TRANSFERASE AND THEIR USE IN THE TREATMENT OF PSYCHOTIC DISORDERS - The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved. | 01-03-2013 |
20130035346 | AMIDE DERIVATIVES BEARING A CYCLOPROPYLAMINOACARBONYL SUBSTITUENT USEFUL AS CYTOKINE INHIBITORS - The invention concerns a compound of the Formula (I), wherein Qa is heteroaryl and is substituted with halogeno; R1 and R2 are hydrogen; and Qb is phenyl or heteroaryl, and Qb may optionally bear 1 or 2 substituents selected from hydroxy, halogeno and (1-6C)alkyl, or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines. | 02-07-2013 |
20130040968 | FAT OR OIL COMPOSITION - Provided is an oil or fat composition, including a vitamin B1 derivative or a salt thereof at a content of 44 to 8,000 ppm in terms of thiamine and having a hydroxyl value of 9 to 100 mg-KOH/g, in which the content C (ppm) of the vitamin B1 derivative or the salt thereof in terms of thiamine and the hydroxyl value X (mg-KOH/g) satisfy a relationship of the following expression (1): | 02-14-2013 |
20130045982 | BENZAMIDE DERIVATIVES - Disclosed are benzamide derivatives useful in slowing the expansion of cancer cells including the killing of cancer cells and in the treatment of cancer. | 02-21-2013 |
20130053404 | Tricyclic pyridine derivatives, medicaments containing such compounds, their use and process for their preparation - The present invention relates to compounds defined by formula I | 02-28-2013 |
20130059864 | INHIBITING NEUROTRANSMITTER REUPTAKE - This document relates to compounds as well as methods and materials involved in modulating neurotransmitter reuptake. For example, compounds, methods for synthesizing compounds, and methods for inhibiting neurotransmitter reuptake are provided. | 03-07-2013 |
20130065911 | N-(5-CYCLOALKYL- OR 5-HETEROCYCLYL-)-PYRIDIN-3-YL CARBOXAMIDES - The present invention relates to compounds of the formula | 03-14-2013 |
20130065912 | PESTICIDAL COMPOSITIONS - Pesticide compositions and their use in controlling pests are provided. | 03-14-2013 |
20130085149 | OSMOLYTE-CONTAINING PREPARATION FOR THE TREATMENT OF DRY MUCOUS MEMBRANES - The present invention relates to osmolyte-containing preparations for the local treatment of dry mucous membranes. It describes the use of osmolytes for the production of a medicament, medical product or cosmetic product for the prevention, therapy and/or care of dry mucous membranes. The present invention relates to topical compositions based on osmolytes to which sodium chloride and/or moisturizers can optionally be added. The group of osmolytes proposed by the invention embraces various low-molecular substances, in particular ectoine, homoectoine, hydroxyectoine, di-myo-inositol phosphate (DIP), cyclic 2,3-diphosphoglycerate (cDPG), 1,1-di-glycerol phosphate (DGP), β-mannosylglycerate (Firoin), β-mannosylglyceramide (Firoin-A), di-mannosyl di-inositol phosphate (DMIP), glucosylglycerol and/or a derivative, e.g. an acid, salt or ester, of these compounds. | 04-04-2013 |
20130090345 | Synthetic Mimetics Of Host Defense And Uses Thereof - The present invention provides arylamide compounds and methods of making and using them as antibiotics. | 04-11-2013 |
20130102619 | 2-PYRIDYLOXY-4-NITRILE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to 2-pyridyloxy-4-nitrile compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyl-oxy-4-nitrile compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 04-25-2013 |
20130123277 | PYRIDO[3,4-B]INDOLES AND METHODS OF USE - This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in the variety of therapeutic application, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or neuronal disorder. | 05-16-2013 |
20130131084 | USE OF DERIVATIVES OF INDOLES FOR THE TREATMENT OF CANCER - The present invention relates to the use of derivatives of indoles having a general formula (I) as follow: | 05-23-2013 |
20130131085 | CYTOCHROME P450 OXIDASE INHIBITORS AND USES THEREOF - The present invention features compounds of formula I | 05-23-2013 |
20130131086 | METHODS OF USING A G PROTEIN-COUPLED RECEPTOR TO IDENTIFY PEPTIDE YY (PYY) SECRETAGOGUES AND COMPOUNDS USEFUL IN THE TREATMENT OF CONDITIONS MODULATED BY PYY - The present invention relates to methods of using GPR119 receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY, such as conditions modulated by stimulation of NPY Y2 receptor (Y2R). Agonists of GPR119 receptor are useful as therapeutic agents for treating or preventing a condition modulated by PYY, such as a condition modulated by stimulation of Y2R. Conditions modulated by PYY such as may be a condition modulated by stimulation of Y2R include bone-related conditions, metabolic disorders, angiogenesis-related conditions, ischemia-related conditions, convulsive disorders, malabsorptive disorders, cancers, and inflammatory disorders. | 05-23-2013 |
20130137706 | Antimicrobial Molecules For Treating Multi-Drug Resistant and Extensively Drug Resistant Strains Of Mycobacterium - The present invention provides methods of inhibiting the growth of | 05-30-2013 |
20130143900 | Process for preparing substituted 5-fluoro-1H-pyrazolopyridines - The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) | 06-06-2013 |
20130150377 | Tetrahydropyridinyl and Dihydropyrrolyl Compounds and the Use Thereof - The invention relates to tetrahydropyridinyl and dihydropyrrolyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X, Y, Z, R | 06-13-2013 |
20130158050 | PIPERIDINE DERIVATIVES - The present invention relates to a compound of formula I | 06-20-2013 |
20130190330 | BISARYL-BONDED ARYLTRIAZOLONES AND USE THEREOF - The present application relates to novel bisaryl-linked 5-aryl-1,2,4-triazolone derivatives, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders. | 07-25-2013 |
20130190331 | PYRIDO[4,3-B]INDOLES AND METHODS OF USE - New heterocyclic compounds that may be used to modulate a histamine receptor in an individual are described. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 07-25-2013 |
20130197011 | Phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones and the use thereof as medicament - Substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones which are glycine transporter-1 (GlyT1) inhibitors. These are useful for the treatment of schizophrenia, Alzheimer's Disease and other neurological and psychiatric disorders. | 08-01-2013 |
20130197012 | Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 08-01-2013 |
20130197013 | CYCLOPROPYLAMINE DERIVATIVES USEFUL AS LSD1 INHIBITORS - The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection. | 08-01-2013 |
20130203775 | Novel Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 08-08-2013 |
20130217709 | Cyclic Amine Azaheterocyclic Carboxamides - The invention provides novel cyclic amine azaheterocyclic carboxamide according to Formula (I), Formula (II) and Formula (III) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer. | 08-22-2013 |
20130225606 | N-HETARYLMETHYL PYRAZOLYLCARBOXAMIDES - The present invention relates to N-Hetarylmethyl pyrazolylcarboxamides derivatives or their thiocarboxamides derivatives, their process of preparation, their use as fungicide, particularly in the form of compositions. Formula (I), and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. | 08-29-2013 |
20130231352 | HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls having the general formula (I) and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p1 108 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML), Myelodysplastic syndrome (MDS), myelo-proliferative diseases (MPD), Chronic Myeloid Leukemia (CML), T-cell Acute Lymphoblastic leukaemia (T-ALL), B-cell Acute Lymphoblastic leukaemia (B-ALL), Non Hodgkins Lymphoma (NHL), B-cell lymphoma and solid tumors, such as breast cancer. | 09-05-2013 |
20130237550 | ARYLVINYLAZACYCLOALKANE COMPOUNDS FOR CONSTIPATION - The present invention relates to method of treating constipation and enhancing colonic motility by administration of 5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine or a pharmaceutically acceptable salt thereof. | 09-12-2013 |
20130237551 | Substituted 5-fluoro-1H-pyrazolopyridines and their use - The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders. | 09-12-2013 |
20130245042 | Positive Allosteric Modulators of MGLUR2 - The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds modulate the mGluR2 receptor and may be useful for the treatment of various disorders of the central nervous system. | 09-19-2013 |
20130252975 | NOVEL ROCK INHIBITORS - The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases. | 09-26-2013 |
20130261134 | MESYLATE SALT FORMS OF A POTENT HCV INHIBITOR - This invention relates to novel mesylate salt forms of the following Compound (1), and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in methods for the treatment of Hepatitis C Viral (HCV) infection: | 10-03-2013 |
20130261135 | METALLOENZYME INHIBITOR COMPOUNDS - The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes. | 10-03-2013 |
20130267540 | SOLID FORMS OF GYRASE INHIBITOR (R)-1-ETHYL-3-[6-FLUORO-5-[2-(1-HYDROXY-1-METHYL-ETHYL)PYRIMIDIN-5-YL]-7-- (TETRAHYDROFURAN-2-YL)-1H-BENZIMIDAZOL-2-YL]UREA - The present application is directed to solid forms of compounds of formula I: | 10-10-2013 |
20130274272 | METHYL/DIFLUOROPHENYL-METHOXY SUBSTITUTED PYRIDINONE-PYRIDINYL COMPOUNDS, METHYL-PYRIDINYL-METHOXY SUBSTITUTED PYRIDINONE-PYRIDINYL COMPOUNDS, AND METHYL-PYRIMIDINYL-METHOXY SUBSTITUTED PYRIDINONE-PYRIDINYL COMPOUNDS - The present disclosure provides methyl/difluorophenyl-methoxy substituted pyridinone-pyridinyl compounds, methyl-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds, and methyl-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): | 10-17-2013 |
20130281465 | PYRAZOLE DERIVATIVE - A compound represented by formula (IA) or a pharmaceutically acceptable salt thereof, which is useful for the treatment or prevention of diseases such sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, pain, gastrointestinal diseases, epilepsy, inflammation, immune-related diseases, endocrine-related diseases, and hypertension, and of which the action relies on an orexin (OX) receptor antagonistic activity. | 10-24-2013 |
20130289050 | INHIBITORS OF BETA-SECRETASE - The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates. | 10-31-2013 |
20130296341 | INDAZOLE INHIBITORS OF THE WNT SIGNAL PATHWAY AND THERAPEUTIC USES THEREOF - Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 11-07-2013 |
20130303549 | NOVEL BIAROMATIC COMPOUNDS THAT MODULATE PPARY TYPE RECEPTORS AND COSMETIC/PHARMACEUTICAL COMPOSITIONS COMPRISED THEREOF - Novel biaromatic compounds having the general formula (I): | 11-14-2013 |
20130310400 | SPIRO AMINIC COMPOUNDS WITH NK1 ANTAGONIST ACTIVITY - The invention concerns a spiro-amino compound of Formula (I), wherein A is selected from a 5- or 6-membered aromatic ring and a 5- or 6-membered heteroaromatic ring containing 1 to 3 nitrogen atom; X is a substituent selected from the group consisting of (C | 11-21-2013 |
20130324560 | ANTHRANILIC ACID DIAMIDE DERIVATIVE WITH HETERO-AROMATIC AND HETERO-CYCLIC SUBSTITUENTS - The present invention relates to new insecticides of the formula (I) | 12-05-2013 |
20140005206 | INDAZOLE INHIBITORS OF THE WNT SIGNAL PATHWAY AND THERAPEUTIC USES THEREOF | 01-02-2014 |
20140018372 | CRYSTALLINE FORM OF A INDOLINONE DERIVATIVE AND ITS USE - A crystalline form of 3-{3-[1-(4-Dimethylaminomethyl-phenylamino)-1-phenyl-meth-(Z)-ylidene]-2-oxo-2,3-dihydro-1H-indol-6-yl}-propynoic acid ethylamide. | 01-16-2014 |
20140018373 | FUSED HETEROCYCLIC COMPOUND AND USE FOR PEST CONTROL THEREOF - A fused heterocyclic compound the formula (1): wherein A | 01-16-2014 |
20140031373 | PYRIMIDINE DERIVATIVES AND USE THEREOF AS PESTICIDES - The present invention relates to novel substituted pyrimidine derivatives, to processes for preparing these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators. | 01-30-2014 |
20140031374 | TRIAZOLE DERIVATIVES AS WNT SIGNALING PATHWAY INHIBITORS - The present invention relates to compounds of formula (I), to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy: Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway and increased presence of nuclear β-catenin. For example, these may be used in preventing and/or retarding proliferation of tumor cells and metastasis, for example carcinomas such as colon carcinomas. | 01-30-2014 |
20140045862 | Cycloalkane Derivatives - Disclosed herein are therapeutic agents and/or preventive agents for pain or therapeutic agents and/or preventive agents for a sodium channel associated disease. The present invention provides compounds represented by the following formula (I) or pharmacologically acceptable salts thereof: | 02-13-2014 |
20140045863 | Muscarinic Agonists as Cognitive Enhancers - Methods of treating a mental condition by administering to a subject in need thereof an effective amount of compound CDD-102A, [5-(3-ethyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidine] are described. | 02-13-2014 |
20140051712 | BLOOD BRAIN BARRIER-PENETRATING OXIMES FOR CHOLISTENERASES REACTIVATION - The invention describes pharmaceutical agents capable of crossing the blood brain barrier to protect against organophosphate pesticides and nerve agents or other electrophiles by reactivating inhibited cholinesterase (i.e., acetylcholinesterase and butyrylcholinesterase) and other proteins in the peripheral and central nervous system. | 02-20-2014 |
20140057926 | SUBSTITUTED 4-PYRIDONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY - This invention relates to substituted 4-pyridones of formula 1 | 02-27-2014 |
20140057927 | INHIBITORS OF BETA-SECRETASE - The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates. | 02-27-2014 |
20140057928 | SOLID STATE FORMS OF A POTENT HCV INHIBITOR - This invention relates to novel sodium salt forms of the following Compound (1), and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection: | 02-27-2014 |
20140066460 | SYNTHESIS AND NOVEL SALT FORMS OF (R)-5-((E)-2-PYRROLIDIN-3YLVINYL)PYRIMIDINE - The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts. | 03-06-2014 |
20140073652 | Post-Translational Regulation of Catalytic Activities of Cytochrome P450 46A1 and Uses Thereof - Provided herein are methods and compounds for post-translational regulation of cytochrome P450 46A1 (CYP46A1) enzyme activity in the brain and retina. Also, a method for identifying a potential regulator of a CYP46A1 enzyme using crystal structures of the enzyme and a subsequent method for screening for a regulatory activity in the presence of CYP46A1 enzyme are provided. In addition, the regulator compounds that either inhibit or stimulate cholesterol hydroxylation by the CYP46A1 enzyme are provided. Further provided is a method of treating a pathoneurological condition associated with increased cholesterol levels in the brain and retina using the stimulatory compounds. | 03-13-2014 |
20140088118 | HETEROCYCLIC COMPOUNDS - The present invention provides a compound useful as an agent for the prophylaxis or treatment of neurodegenerative disease and the like, or a salt thereof. | 03-27-2014 |
20140088119 | Muscarinic Agonists as Enhancers of Working Memory and Cognitive Flexibility - Methods and compositions for treating a mental condition in a subject in need thereof, includes administering to a subject in need thereof an effective amount of a CDD-102A compound [5-(3-ethyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidine], or a pharmaceutically acceptable salt or hydrate thereof pharmaceutically acceptable salt or hydrate thereof. | 03-27-2014 |
20140094473 | INHIBITORS OF INFLUENZA VIRUSES REPLICATION - Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): | 04-03-2014 |
20140107134 | COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES - The invention relates to compounds of formula (I): | 04-17-2014 |
20140113916 | TRPV4 ANTAGONISTS - The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists. | 04-24-2014 |
20140121221 | SELECTIVE PDE4 B INHIBITION AND IMPROVEMENT IN COGNITION IN SUBJECTS WITH BRAIN INJURY - Provided herein are methods of improving cognitive ability or memory in a subject that has suffered a brain injury or spinal cord injury by administering a selective PDE4 B inhibitor. | 05-01-2014 |
20140128410 | TYROSINE KINASE INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to tyrosine kinase inhibitors that contain a zinc-binding moiety and their use in the treatment of tyrosine related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors. | 05-08-2014 |
20140135346 | Novel Heterocyclic Compounds as Pesticides - The present application relates to novel amides and thioamides, to processes for preparation thereof and to the use thereof for controlling animal pests, in particular arthropods and especially insects. | 05-15-2014 |
20140142119 | INHIBITORS OF INFLUENZA VIRUSES REPLICATION - Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): | 05-22-2014 |
20140148470 | PYRIMIDINE COMPOUNDS FOR TREATING HAIRLOSS - The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof for use in the treatment or prevention of hairloss, | 05-29-2014 |
20140148471 | Heterocyclic Compounds as Pesticides - The present application relates to novel heterocyclic compounds, to the use thereof for controlling animal pests, which include arthropods and especially insects, and to processes for preparing the novel compounds. | 05-29-2014 |
20140155415 | BENZODIOXEPINE AND BENZODIOXINE COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN FOR THE TREATMENT OF DIABETES - The present invention relates to compounds of formula I or II, | 06-05-2014 |
20140171448 | USE OF NICOTINIC ACETYLCHOLINE RECEPTOR ALPHA 7 ACTIVATORS - The invention concerns the use of a nicotinic acetylcholine receptor alpha 7 activators for the treatment, prevention or delay of progression of a Movement Disorder selected from Dystonia, Dyskinesia, Chorea, Restless Legs Syndrome, Tics, Tremor, Myoclonus, Startle, Stiff Person Syndrome, Gait Disorder, Parkinson's Disease and Symptomatic Parkinsonism. | 06-19-2014 |
20140171449 | SUBSTITUTED PYRIDINONE-PYRIDINYL COMPOUNDS - The present disclosure provides pyridinone-pyridinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): | 06-19-2014 |
20140171450 | SUBSTITUTED PYRIDINONE-PYRIDINYL COMPOUNDS - The present disclosure provides pyridinone-pyridinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): | 06-19-2014 |
20140171451 | Antibacterial cyclopenta[c]pyrrole substituted 3,4-dihydro-1H-[1,8]naphthyridinones - The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds. | 06-19-2014 |
20140194443 | Pyrazolyl-Based Carboxamides I - The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders. | 07-10-2014 |
20140194444 | AMINOPYRIMIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES - The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention. | 07-10-2014 |
20140194445 | SUBSTITUTED 3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS - The present invention relates to compounds of the formula I, | 07-10-2014 |
20140206702 | IMIDAZOPYRIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - The invention provides compounds of Formulas Ia-Ib, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R | 07-24-2014 |
20140235654 | USE OF DERIVATIVES OF INDOLES FOR THE TREATMENT OF CANCER - The present invention relates to the use of derivatives of indoles having a general formula (I) as follow: | 08-21-2014 |
20140249163 | MALIGNANT AND NON-MALIGNANT DISEASE TREATMENT WITH RAS ANTAGONISTS - The present disclosure describes new inhibitors or antagonists of Ras useful for the treatment of conditions resulting from Ras-induced or mediated cellular processes, including cellular proliferation, differentiation, apoptosis, senescence, and survival. These cellular processes may be associated with a non-malignant or malignant disease, disorder, or pathological condition. The present disclosure also describes a method for inhibiting such Ras-induced or mediated cellular processes. The method entails administering a Ras antagonist in an amount effective to inhibit such cellular processes. | 09-04-2014 |
20140275121 | CDC7 Inhibitors - The present invention provides isoindolinone compounds, or a pharmaceutically acceptable salt thereof, that inhibit CDC7 and, therefore may be useful in treating cancer. | 09-18-2014 |
20140275122 | Voriconazole Formulations - A voriconazole composition includes voriconazole, hydroxypropyl β-cyclodextrin, and an excipient selected from the group consisting of an amino acid and a disaccharide, where the composition is a solid. The solid composition may be made by forming a liquid mixture including a solvent, voriconazole, HPCD, and an excipient selected from the group consisting of an amino acid and a disaccharide, and lyophilizing the liquid mixture. | 09-18-2014 |
20140275123 | COMPOUNDS AND METHODS FOR CONTROLLING FUNGI - Various aspects disclosed herein relate to aryl substituted aminopyrimidines according to Formula 1: | 09-18-2014 |
20140288090 | N-ARYLYLMETHYLINDAZOLE MODULATORS OF PPARG - The invention provides molecular entities that bind with high affinity to PPARG (PPARγ), inhibit cdk5-mediated phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes or obesity. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided. | 09-25-2014 |
20140288091 | MONO-FLUORO BETA-SECRETASE INHIBITORS - Beta-secretase inhibitors, of formula (I) as described in the specification, pharmaceutical compositions comprising them and therapeutic methods using them for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's Disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. | 09-25-2014 |
20140288092 | HETEROARYL COMPOUNDS AS SODIUM CHANNEL BLOCKERS - The invention relates to aryl substituted compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein Het, G, A, R, and n are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain. | 09-25-2014 |
20140303187 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. | 10-09-2014 |
20140309240 | DERIVATIVES OF 1-(SUBSTITUTED SULFONYL)-2-AMINOIMIDAZOLINE AS ANTITUMOR AND ANTIPROLIFERATIVE AGENTS - The invention provides novel, water-soluble 2-aminoimidazoline derivatives having general Formula (I) as well as some precursors of Formula (I), which are very potent inducers of G2/M cell cycle arrest. In treated tumor cells, compounds of Formula (I) give gene expression profile distinct from known antimitotic agents. The invention also provides methods for preparing the compounds, and methods of using the compounds for the treatment of cancer or other mammalian diseases characterized by undesirably high levels of cell proliferation. The compounds of the invention are also expected to have utility as research tools. | 10-16-2014 |
20140315926 | Process for preparing substituted 5-fluoro-1H-pyrazolopyridines - The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) | 10-23-2014 |
20140315927 | Inhibitors of HIV Replication - The present invention relates to novel 2,3,4-substituted 5,6,7,8-tetrahydro[1]benzothieno[2,3-b]pyridine compounds and pharmaceutically acceptable salts thereof, to compositions containing such compounds and to the use of such compounds as inhibitors of HIV replication. | 10-23-2014 |
20140323501 | AMINO-PROPYLENE-GLYCOL DERIVATIVES, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITION AND USE THEREOF - Immune-modulators of formula (I) below are prepared: | 10-30-2014 |
20140323502 | HETEROCYCLIC SULFONAMIDES, USES AND PHARMACEUTICAL COMPOSITIONS THEREOF - The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: | 10-30-2014 |
20140343079 | THERAPEUTIC COMPOUNDS - The invention provides compounds of formulae (I), (II), (III), and (IV): and salts thereof, as well as pharmaceutical compositions comprising such compounds. The compounds are useful for treating cancers and Alzheimer's disease. | 11-20-2014 |
20140350032 | PROPENOATE DERIVATIVES OF BETULIN - The present invention relates to a compound characterized by the following Formula I: | 11-27-2014 |
20140357649 | Phenyl(oxy/thio)alkanol Derivatives - The present invention relates to novel phenyl(oxy/thio)alkanol derivatives, to processes for preparing these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators. | 12-04-2014 |
20140364442 | METHYL/FLUORO-PYRIDINYL-METHOXY SUBSTITUTED PYRIDINONE-PYRIDINYL COMPOUNDS AND FLUORO-PYRIMIDINYL-METHOXY SUBSTITUTED PYRIDINONE-PYRIDINYL COMPOUNDS - The present disclosure provides methyl/fluoro-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds and fluoro-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, including rheumatoid arthritis, having the structure of Formula (I): | 12-11-2014 |
20140364443 | 1,4-DIHYDRO-NAPHTHYRIDINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION AND USE THEREOF - Disclosed are 1,4-dihydro-naphthyridine derivatives and pharmaceutical composition and uses thereof. The 1,4-dihydro-naphthyridine derivatives are a compound capable of inhibiting acetylcholinesterase activity and preventing extracellular calcium from flowing into a cell via a calcium channel, i.e., having a dual-activity, which are of potential importance as a pharmaceutical and can be used to prepare the drugs for treating cardiovascular diseases, cerebrovascular diseases and dementia. | 12-11-2014 |
20140364444 | FUSED HETEROCYCLIC COMPOUND AND USE THEREOF FOR PEST CONTROL - A fused heterocyclic compound the formula (1): | 12-11-2014 |
20140371239 | MENIN-MLL INHIBITORS AND METHODS OF USE THEREOF - The present invention relates generally to compounds that inhibit the binding of menin and MLL or MLL fusion proteins and methods of use thereof. In particular embodiments, the present invention provides compositions comprising piperidine-containing compounds and methods of use thereof to inhibit the interaction of menin with MLL oncoproteins (e.g., MLL1, MLL2, MLL-fusion oncoproteins), for example, for the treatment of leukemia, solid cancers, diabetes, and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, MLL-PTD and/or menin. | 12-18-2014 |
20140371240 | NOVEL INSECTICIDAL AROMATIC AMIDES - The invention relates to compounds of the general formulae (I) and (II) | 12-18-2014 |
20150038516 | Inhibitors of Protein Kinases - Compounds of general Formula I: | 02-05-2015 |
20150038517 | Indole Derivative Modulators of the alpha 7 nAChR - This invention relates to modulation of the α7 nicotinic acetylcholine receptor (nAChR) by a compound of formula (I) or a salt thereof: | 02-05-2015 |
20150057293 | NEW COMPOUNDS - The invention relates to new naphthyridine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. | 02-26-2015 |
20150057294 | 1H-INDAZOLE-3-CARBOXAMIDE COMPOUNDS AS GLYCOGEN SYNTHASE KINASE 3 BETA INHIBITORS - The present invention relates to the 1H-indazole-3-carboxamide compounds having the following general formula (I) as glycogen synthase kinase 3 beta (GSK-3β) inhibitors and to their use in the treatment of GSK-3p-related disorders such as, for example, (i) insulin-resistance disorders; (ii) neurodegenerative diseases; (iii) mood disorders; (iv) schizophrenic disorders; (v) cancerous disorders; (vi) inflammation, (vii) substance abuse disorders; (viii) epilepsies; and (ix) neuropathic pain. | 02-26-2015 |
20150065523 | CHEMICAL COMPOUNDS - The present invention provides compounds of formula (I) including stereoisomers or a racemate or a mixture or a pharmaceutically acceptable salt thereof: wherein X is NH, or O; Q is 5-6 membered heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; A is phenyl or a 5-6 heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; B may assume different meanings from A and is phenyl or a 5-6 membered heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; and processes for their preparation, pharmaceutical compositions containing them and their use as dual antagonists of the Orexin 1 and Orexin 2 receptors. | 03-05-2015 |
20150072997 | ANTI-MALARIAL COMPOUNDS - The present invention provides tricyclic compounds, arylamide compounds, and other compounds, and compositions comprising the same, for treating malaria, and methods of treating malaria comprising administering such compounds to an animal. | 03-12-2015 |
20150080413 | Antibacterial cyclopenta[c]pyrrole substituted 3,4-dihydro-1H-[1,8]naphthyridinones - The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds. | 03-19-2015 |
20150080414 | SUBSTITUTED 5-FLUORO-1H-PYRAZOLOPYRIDINES AND THEIR USE - The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders. | 03-19-2015 |
20150080415 | THERAPEUTIC AGENT FOR ANXIETY DISORDERS - Provided are an agent for the treatment and/or prophylaxis of an anxiety disorder comprising, as an active ingredient, a thiazole derivative represented by the formula (I) wherein R | 03-19-2015 |
20150087657 | MULTICOMPONENT CRYSTALLINE SYSTEM OF VORICONAZOLE WITH FUMARIC ACID - A novel solid form of Voriconazole comprises the active ingredient (2R,3S)-2-(2,4-difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol and fumaric acid. The solid composition comprising the two components shows improved properties such as water solubility, crystallization behavior and stability. | 03-26-2015 |
20150087658 | SUBSTITUTED AMINOPYRIMIDINE COMPOUNDS AND METHODS OF USE - The invention relates to the preparation and use of new aminopyrimidine derivatives as drug candidates in free form or in pharmaceutically acceptable salt form and formulations thereof for the modulation of a disorder or disease which is mediated by the activity of the PI3K enzymes. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of disorders or diseases, such as disorders of immunity and inflammation in which PI3K enzymes play a role in leukocyte function, and hyperproliferative disorders associated with PI3K activity, including but not restricted to leukemias and solid tumors, in mammals, especially humans. | 03-26-2015 |
20150094317 | METHODS OF COLCHICINE ADMINISTRATION - The invention provides improved methods for coadministration of colchicine with drugs metabolized by CYP3A4 (anciently referred to as cytochrome P450 isozyme 3A4) or the P-glycoprotein transporter, but not both. The method enables non-toxic coadministration of colchicine and the second drug at their ordinary levels safely and effectively without reducing the dose or frequency for either drug. | 04-02-2015 |
20150094318 | METHODS OF COLCHICINE ADMINISTRATION - The invention provides improved methods for coadministration of colchicine with drugs metabolized by CYP3A4 (anciently referred to as cytochrome P450 isozyme 3A4) or the P-glycoprotein transporter, but not both. The method enables non-toxic coadministration of colchicine and the second drug at their ordinary levels safely and effectively without reducing the dose or frequency for either drug. | 04-02-2015 |
20150099765 | Compounds and Compositions for Cognition-Enhancement, Methods of Making, and Methods of Treating - Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function. | 04-09-2015 |
20150099766 | Novel halogen-substituted compounds - The invention relates to compounds of the general formula (I), | 04-09-2015 |
20150105404 | PHENYL LINKED QUINOLINYL MODULATORS OF RORyt - The present invention comprises compounds of Formula I. | 04-16-2015 |
20150105405 | N-substituted hetero-bicyclic compounds and derivatives for combating animal pests II - The invention relates to N-substituted hetero-bicyclic compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic compounds. | 04-16-2015 |
20150119404 | NOVEL COMPOUNDS - The invention relates to spiro derivatives, to the use of said derivatives in treating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivatives and processes for their preparation. | 04-30-2015 |
20150126528 | INHIBITORS OF BRUTON'S TYROSINE KINASE - The present invention provides a compound, solid forms, and compositions thereof, which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same. The present invention also provides methods of making provided compound and solid forms. | 05-07-2015 |
20150126529 | SUBSTITUTED BICYCLIC HETEROARYL COMPOUNDS - Disclosed are azaindazole compounds of Formula (I): | 05-07-2015 |
20150133472 | PHARMACEUTICAL COMPOSITION - The present invention relates to a pharmaceutical composition comprising voriconazole and an aqueous, non-aqueous, or oily vehicle, or a mixture thereof, and optionally one or more pharmaceutically acceptable excipients; to a process for preparing such a composition, and to the use of such a composition for the prevention or treatment of fungal infections. | 05-14-2015 |
20150133473 | NOVEL RING-SUBSTITUTED N-PYRIDINYL AMIDES AS KINASE INHIBITORS - The present invention provides a compound of formula (A): | 05-14-2015 |
20150133474 | GHRELIN O-ACYL TRANSFERASE INHIBITOR - The present invention provides novel GOAT inhibitors and their salts and pharmaceutical compositions thereof. | 05-14-2015 |
20150289508 | MACROCYCLIC PICOLINAMIDES AS FUNGICIDES - The disclosure relates to macrocyclic picolinamides of Formula I and their use as fungicides. | 10-15-2015 |
20150291558 | 2-PYRIDYLOXY-3-SUBSTITUTED-4-NITRILE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to 2-pyridyloxy-3-substituted-4-nitrile compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-3-substituted-4-nitrile compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 10-15-2015 |
20150291559 | N-(PYRIDIN-2-YL)PYRIMIDIN-4-AMINE DERIVATIVES CONTAINING A SULFOXIMINE GROUP - The present invention relates to disubstituted N-(pyridin-2-yl)pyrimidin-4-amine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I). | 10-15-2015 |
20150292045 | ALTERNATIVE USES FOR HBV ASSEMBLY EFFECTORS - Described herein are methods for identifying compounds useful for the treatment of infection by hepatitis B virus (HBV). | 10-15-2015 |
20150307488 | CYCLOPROPYL IMIDAZOPYRIDINE PDE10 INHIBITORS - The present invention is directed to substituted cyclopropyl imidazopyridine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. | 10-29-2015 |
20150320747 | OSMOLYTE-CONTAINING PREPARATION FOR THE TREATMENT OF DRY MUCOUS MEMBRANES - The present invention relates to osmolyte-containing preparations for the local treatment of dry mucous membranes. It describes the use of osmolytes for the production of a medicament, medical product or cosmetic product for the prevention, therapy and/or care of dry mucous membranes. The present invention relates to topical compositions based on osmolytes to which sodium chloride and/or moisturizers can optionally be added. The group of osmolytes proposed by the invention embraces various low-molecular substances, in particular ectoine, homoectoine, hydroxyectoine, di-myo-inositol phosphate (DIP), cyclic 2,3-diphosphoglycerate (cDPG), 1,1-di-glycerol phosphate (DGP), β-mannosylglycerate (Firoin), β-mannosylglyceramide (Firoin-A), di-mannosyl di-inositol phosphate (DMIP), glucosylglycerol and/or a derivative, e.g. an acid, salt or ester, of these compounds. | 11-12-2015 |
20150322057 | TRIAZOLE DERIVATIVES AS WNT SIGNALING PATHWAY INHIBITORS - The present invention relates to compounds of formula I, to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy: | 11-12-2015 |
20150322060 | PYRROLIDINE DERIVATIVES AND THEIR USE AS COMPLEMENT PATHWAY MODULATORS - The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as a factor D inhibitor for the treatment of ophthalmic diseases. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. | 11-12-2015 |
20150335642 | PYRIMIDINE DIOL AMIDES AS SODIUM CHANNEL BLOCKERS - The present disclosure provides pyrimidine diol amides of Formula (I), and the pharmaceutically acceptable solvates and prodrugs thereof, wherein A | 11-26-2015 |
20150344425 | INDOLE CARBOXAMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS - The invention relates to indole carboxamide derivatives of formula (I), | 12-03-2015 |
20150344440 | Compounds and Methods of Use Thereof for Treating Tumors - The invention encompasses novel compounds and pharmaceutically acceptable salts thereof and compositions including therapeutically or prophylactically effective amounts of such compounds or pharmaceutically acceptable salts thereof. The invention also encompasses methods for treating or preventing diseases and disorders associated with abnormal cell growth, for example, treating or preventing cancer or tumor growth, which methods include administering to a mammal in need thereof a composition comprising a therapeutically or prophylactically effective amount of a compound of the invention or a pharmaceutically acceptable salt thereof. | 12-03-2015 |
20150344446 | TRIAZOLONE COMPOUNDS AND USES THEREOF - The invention disclosed herein is directed to compounds of Formula I | 12-03-2015 |
20150352092 | METHYL/FLUORO-PYRIDINYL-METHOXY SUBSTITUTED PYRIDINONE-PYRIDINYL COMPOUNDS AND FLUORO-PYRIMIDINYL-METHOXY SUBSTITUTED PYRIDINONE-PYRIDINYL COMPOUNDS - The present disclosure provides methyl/fluoro-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds and fluoro-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, including rheumatoid arthritis, having the structure of Formula (I): | 12-10-2015 |
20150373978 | NOVEL HETEROCYCLIC COMPOUNDS AS PESTICIDES - The present application relates to novel heterocyclic compounds, to processes for preparation thereof and to the use thereof for controlling animal pests, which also include arthropods and especially insects. | 12-31-2015 |
20150374691 | METHODS AND MATERIALS FOR TREATING ORTHOSTATIC HYPOTENSION OR POSTURAL TACHYCARDIA SYNDROME - This document provides methods and materials related to treating orthostatic hypotension and/or postural tachycardia syndrome. For example, methods and materials for using a composition containing 3,4-diaminopyridine, 4-aminopyridine, or both to treat patients with orthostatic hypotension, postural tachycardia syndrome, or both orthostatic hypotension and postural tachycardia syndrome are provided. | 12-31-2015 |
20150376147 | Substituted Phenyl(Oxy/Thio)Alkanol Derivatives - The present invention relates to novel substituted phenyl(oxy/thio)alkanol derivatives, to processes for preparing these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators. | 12-31-2015 |
20150376184 | FORMS OF METHYL METHYL CARBAMATE - This present invention relates to forms of methyl {4.6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3.4-b]pyridino-3-yl]pyrimidino-5-yl}methylcarbamate comprising its Modification I. Modification II. mono-DMSO solvate. sesqui-DMSO solvate and ¼-ethyl acetate solvate. | 12-31-2015 |
20160002207 | NEW DIHYDROQUINOLINE-2-ONE DERIVATIVES - The invention provides novel compounds having the general formula (I) | 01-07-2016 |
20160002208 | NOVEL HALOGEN-SUBSTITUTED COMPOUNDS - The invention relates inter alia to halogen-substituted compounds of the general formula (I) | 01-07-2016 |
20160002217 | FUNGICIDAL 3--OXADIAZOLONE DERIVATIVES - The present invention provides 3-{heterocyclyl[(heterocyclylmethoxy)imino]methyl}-oxadiazolinone derivatives of formula (I) | 01-07-2016 |
20160009648 | PROLYL HYDROXYLASE INHIBITORS AND METHODS OF USE | 01-14-2016 |
20160009658 | HYDANTOINS THAT MODULATE BACE-MEDIATED APP PROCESSING | 01-14-2016 |
20160009671 | PROCESS FOR PREPARING SUBSTITUTED 5-FLUORO-1H-PYRAZOLOPYRIDINES | 01-14-2016 |
20160016935 | 2-PYRIDYLOXY-4-ETHER OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to 2-pyridyloxy-4-ether compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ether compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 01-21-2016 |
20160024019 | HISTONE DEACETYLASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF - Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use. | 01-28-2016 |
20160024229 | CYCLODEXTRIN - The invention provides a method for preparing sulphoalkyl ether-β-cyclodextrin. The method comprises first contacting cyclodextrin with a base to form activated cyclodextrin. The method then comprises separately contacting the activated cyclodextrin with an alkyl sultone to form sulphoalkyl ether-β-cyclodextrin. The activation reaction is carried in batch and the sulphoalkylation reaction is carried out under continuous flow conditions. | 01-28-2016 |
20160039783 | Inhibitors of Viral Replication, Their Process of Preparation and Their Therapeutical Uses - The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV. | 02-11-2016 |
20160039814 | 6-ALKYNYL-PYRIDINE DERIVATIVES - 6-Alkynyl-pyridine of general formula (I) | 02-11-2016 |
20160045500 | SPIRO AMINIC COMPOUNDS WITH NK1 ANTAGONIST ACTIVITY - The invention concerns a spiro-amino compound of Formula (I), wherein A is selected from a 5- or 6-membered aromatic ring and a 5- or 6-membered heteroaromatic ring containing 1 to 3 nitrogen atom; X is a substituent selected from the group consisting of (C | 02-18-2016 |
20160050923 | N-SUBSTITUTED ACYL-IMINO-PYRIDINE COMPOUNDS AND DERIVATIVES FOR COMBATING ANIMAL PESTS - The invention relates to N-substituted acyl-imino-pyridine compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted acyl-imino-pyridine compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted acyl-imino-pyridine compounds. | 02-25-2016 |
20160051518 | BISARYL-BONDED ARYLTRIAZOLONES AND USE THEREOF - The present application relates to novel bisaryl-linked 5-aryl-1,2,4-triazolone derivatives, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders. | 02-25-2016 |
20160052911 | HETEROARYL COMPOUNDS AS SODIUM CHANNEL BLOCKERS - The invention relates to aryl substituted compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein Het, G, A, R, and n are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain. | 02-25-2016 |
20160052917 | PYRUVATE KINASE M2 MODULATORS, THERAPEUTIC COMPOSITIONS AND RELATED METHODS OF USE - Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer. | 02-25-2016 |
20160068510 | HYDROXY-SUBSTITUTED OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to hydroxy compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 03-10-2016 |
20160068514 | HALO AND TRIFLUOROMETHYL SUBSTITUTED OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to halo and trifluoromethyl substituted compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 03-10-2016 |
20160075684 | ALPHA 7 NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS AND USES THEREOF-III - The present invention relates to chemical compounds useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (α7 nAChR). | 03-17-2016 |
20160075698 | FLUORINATED INTEGRIN ANTAGONISTS - The present invention relates to fluorinated compounds of formula I and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing the fluorinated compounds of the invention, and methods of treating macular degeneration, diabetic retinopathy (DR), macular edema, diabetic macular edema (DME), and macular edema following retinal vein occlusion (RVO), by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 03-17-2016 |
20160101104 | QUINUCLIDINE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders. | 04-14-2016 |
20160102073 | 2-HYDROXYMETHYL-SUBSTITUTED OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to 2-hydroxymethyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 04-14-2016 |
20160108034 | NAPHTHYRIDINE DERIVATIVE COMPOUNDS - The invention relates to new naphthyridine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. | 04-21-2016 |
20160115154 | Quinoline Inhibitor of the Macrophage Stimulating 1 Receptor MSTR1 - The compound N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)-3-fluorophenyl)-5-ethyl-1-(pyrimidin-5-yl)-1H-pyrazole-4-carboxamide | 04-28-2016 |
20160115156 | PYRIMIDIN-4-YL)OXY)-1H-INDOLE-1-CARBOXAMIDE DERIVATIVES AND USE THEREOF - This invention relates to certain metabolites of N-(1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6-((methyl-amino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide In particular, the present invention relates to pharmaceutical compositions comprising these metabolites, as well as processes for their preparation and their use in the treatment of diseases. | 04-28-2016 |
20160122327 | STROBILURIN TYPE COMPOUNDS FOR COMBATING PHYTOPATHOGENIC FUNGI - The present invention relates to novel strobilurine type compounds I, processes for preparing these compounds, a use of compounds of the formula I and/or their agriculturally useful salts for controlling phytopathogenic fungi, to compositions comprising at least one such compound, to plant health applications, and to seeds coated with at least one such compound. | 05-05-2016 |
20160122347 | 4,6-DIAMINOPYRIMIDINE STIMULATORS OF SOLUBLE GUANYLATE CYCLASE - The present invention relates to new 4,6-diaminopyrimidine stimulators of soluble guanylate cyclase, pharmaceutical compositions thereof, and methods of use thereof. | 05-05-2016 |
20160129004 | SUBSTITUTED 5-FLUORO-1H-PYRAZOLOPYRIDINES AND THEIR USE - The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders. | 05-12-2016 |
20160130255 | ETHYNYL DERIVATIVES - The present invention relates to ethynyl derivatives as metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of, e.g., anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD). | 05-12-2016 |
20160130265 | SUBSTITUTED 4-PYRIDONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY - This invention relates to substituted 4-pyridones of formula 1 | 05-12-2016 |
20160145223 | Bicyclyl-Substituted Isothiazoline Compounds - The present invention relates to bicyclyl-substituted isothiazoline compounds of formula I | 05-26-2016 |
20160145238 | HETEROARYL SUBSTITUTED PYRAZOLES - Compounds of formula (I), which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals. | 05-26-2016 |
20160145239 | DIAMINOHETEROARYL SUBSTITUTED PYRAZOLES - Compounds of formula (I), and their use as pharmaceuticals. | 05-26-2016 |
20160151369 | SUBSTITUTED 3-PHENYLPROPYLAMINE DERIVATIVES FOR THE TREATMENT OF OPHTHALMIC DISEASES AND DISORDERS | 06-02-2016 |
20160152614 | INHIBITORS OF INFLUENZA VIRUSES REPLICATION | 06-02-2016 |
20160158230 | 2,4- OR 4,6-DIAMINOPYRIMIDINE COMPOUNDS AS IDH2 MUTANTS INHIBITORS FOR THE TREATMENT OF CANCER - Provided are compounds of formula (I), wherein: ring A and ring B are each independently an optionally substituted 5-6 membered monocyclic aryl or heteroaryl; one of X, Y and W is CH and the two others are N; and Z is H or —C(R1)(R2)(R3). The compounds are inhibitors of isocitrate dehydronenase 2 (IDH2) mutants useful for treating cancer. | 06-09-2016 |
20160168095 | NOVEL MICROBIOCIDES | 06-16-2016 |
20160176858 | OXAZOLE OREXIN RECEPTOR ANTAGONISTS | 06-23-2016 |
20160184306 | Novel Pyrimidinyl-DiazoSpiro Compounds - The invention relates to spiro derivatives, to the use of said derivatives in treating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivatives and processes for their preparation. | 06-30-2016 |
20160185768 | THIAZOLE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to thiazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the thiazole compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 06-30-2016 |
20160194324 | ANTIBACTERIAL CYCLOPENTAL[C]PYRROLE SUBSTITUTED 3,4 DIHYDRO-1H-[1,8]NAPHTHYRIDINONES | 07-07-2016 |
20160251349 | SOLID FORM OF PYRAZOLOPYRIDINE COMPOUND | 09-01-2016 |
20160375022 | sGC STIMULATORS - Compounds of Formulae I′ and I are described, which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed. | 12-29-2016 |
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20220133751 | METHODS OF TREATING MYELOPROLIFERATIVE DISORDERS - The present disclosure provides methods of treating a myeloproliferative disorder. In some aspects, the present disclosure provides methods of treating, stabilizing or lessening the severity or progression of one or more myeloproliferative disorders comprising administering to a patient previously treated with ruxolitinib a pharmaceutically acceptable composition comprising a compound of formula I, also known as fedratinib, or a pharmaceutically acceptable salt or hydrate thereof. | 05-05-2022 |