Entries |
Document | Title | Date |
20080200509 | 3,4-DISUBSTITUTED 1H-PYRAZOLE COMPOUNDS AND THEIR USE AS CYCLIN DEPENDENT KINASE AND GLYCOGEN SYNTHASE KINASE-3 MODULATORS - The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. | 08-21-2008 |
20080200510 | Combination of Organic Compounds - The present invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, comprising of a DPP IV inhibitor or a pharmaceutically acceptable salt thereof and comprising at least one CB1 antagonist, or a pharmaceutically acceptable salt thereof. | 08-21-2008 |
20080207693 | Mitotic Kinesin Inhibitors - The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals. | 08-28-2008 |
20080234322 | Methods and apparatus for drug modeling and displaying drug models - Drug delivery models, displays, and systems may be configured to provide a clinician with readily intuitive information about the effects of one or more drugs on a subject. Interactive features may be included to provide a subject-specific model of the expected or predicted effects of one or more drugs on the subject. Additionally, interactive features that effect drug delivery to the subject may also be included. Drug delivery models, displays, and systems may be used in teaching, in advance of treatment, during treatment, or following treatment. | 09-25-2008 |
20080234323 | Amorphous and Three Crystalline Forms of Rimonabant Hydrochloride - The present invention describes novel forms of Rimonabant hydrochloride, processes for their preparation and pharmaceutical compositions containing them. Thus, the present invention discloses three new crystalline forms designated as Form II, Form III and Form IV of Rimonabant hydrochloride and novel amorphous forms of the salt. | 09-25-2008 |
20080255196 | Pesticide Thiazolyloxy Substituted Phenylamidine Derivatives - The present invention relates to aryloxy substituted phenylamidine derivatives of formula (I) wherein the substituents are as in the description, their process of preparation, their use as fungicide or insecticide active agents, particularly in the form of fungicide or insecticide compositions, and methods for the control of phytopathogenic fungi or damaging insects, notably of plants, using these compounds or compositions (I). | 10-16-2008 |
20080262041 | Beta-Lactams for Treatment of Cns Disorders - The present invention relates to novel compounds of formula (I): | 10-23-2008 |
20080269293 | PYRAZOLE DERIVATIVES AS ANTI-PLATELET AND ANTI-THROMBOTIC AGENTS - This invention relates to novel compounds of formula (I) | 10-30-2008 |
20080269294 | Benzamide Compounds Useful as Histone Deacetylase Inhibitors - The invention concerns benzamide compounds of formula (I), wherein R | 10-30-2008 |
20080269295 | SUBSTITUTED THIAZOLES AND THEIR USE FOR PRODUCING DRUGS - The present invention relates to substituted thiazoles, to methods for their production, to drugs containing these compounds and to the use of said compounds for producing drugs. | 10-30-2008 |
20080275086 | Dpp-Iv Inhibitors - The invention relates to compounds of formula (I) | 11-06-2008 |
20080280950 | Hydantoin Derivatives Useful as Metalloproteinase Inhibitors -
Formula (I) wherein R | 11-13-2008 |
20080300278 | Prodrugs of Pyrazoline Compounds, Their Preparation and Use as Medicaments - The present invention relates to prodrugs of pyrazoline compounds of formula I, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals. | 12-04-2008 |
20080300279 | PIPERIDINE-AMIDE DERIVATIVES - The invention is concerned with novel piperidine-amide derivatives of formula (I) | 12-04-2008 |
20080306114 | Human G Protein-Coupled Receptor and Modulators Thereof for the Treatment of Hyperglycemia and Related Disorders - The present invention relates to methods of identifying whether one or more candidate compounds is a modulator of a G protein-coupled receptor (GPCR) or a modulator of blood glucose concentration. In certain embodiments, the GPCR is human. The present invention also relates to methods of using a modulator of the GPCR. A preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for lowering blood glucose concentration, for preventing or treating certain metabolic disorders, such as insulin resistance, impaired glucose tolerance, and diabetes, and for preventing or treating a complication of an elevated blood glucose concentration, such as atherosclerosis, heart disease, stroke, hypertension and peripheral vascular disease. | 12-11-2008 |
20080306115 | Midazole-4-Carboxamide Derivatives For Use As Cb1 Modulators - The present invention relates to substituted 1,2-diphenylimidazol-4-carboxamide compounds of formula I | 12-11-2008 |
20080306116 | ARYLOXAZOLE, ARYLOXADIAZOLE AND BENZIMIDAZOLE DERIVATIVES - This invention relates to compounds of the formula | 12-11-2008 |
20080312282 | Inhibitors of Diacylglycerol O-acyltransferase Type 1 Enzyme - The present invention relates to compounds of formula (I): | 12-18-2008 |
20080319019 | Therapeutic Agents - The present invention relates to certain 1,2-diarylimidazoles of formula I | 12-25-2008 |
20080319020 | 4-Oxadiazolyl-Piperidine Compounds and Use Thereof -
4-Oxadiazolyl-piperidine compounds of formula (I) and (II), their compositions and use for the treatment of pain and diarrhoea. | 12-25-2008 |
20090005418 | Mitotic Kinesin Inhibitors - The present invention relates to dihydroisoxazoles that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals. | 01-01-2009 |
20090005419 | Organic Compounds - The invention relates to an assay for identifying an agent that modulates the interaction of a mRNA with a target protein, e.g. HuR and to organic compounds of formula I | 01-01-2009 |
20090012124 | 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide acid addition salts as kinase inhibitors - The invention provides an acid addition salt of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide and crystals thereof, the salt being formed with an acid selected from methanesulphonic acid and acetic acid and mixtures thereof. Also provided are the novel uses of salts of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide, processes for the preparation of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide and its salts and novel chemical intermediates. | 01-08-2009 |
20090012125 | Piperidine Derivatives, Their Process for Preparation, Their Use as Therapeutic Agents and Pharmaceutical Compositions Containing Them - The present invention provides a compound of a formula (I): [Chemical formula should be inserted here. Please see paper copy] wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state. | 01-08-2009 |
20090023780 | Therapeutic use of a derivative of thienylcyclohexylamine - The invention concerns the use of a thienylcyclohexylamine, on its own or associated with other substances with pharmaceutical activity, for preparing a medicine designed to prevent and/or treat pain and/or nociception. | 01-22-2009 |
20090030041 | N-substituted N-(4-piperidinyl) Amide Derivative - An N-substituted N-(4-piperininyl)amide derivative represented by the following formula (I): (wherein R | 01-29-2009 |
20090036489 | Novel Cyclic Aminophenylalkanoic Acid Derivative - The present invention provides cyclic aminophenylalkanoic acid derivatives that act as agonists for human peroxisome proliferator-activated receptors (PPARs), in particular human PPARα isoform, and are effective in the treatment of abnormal lipid metabolism, diabetes and other disorders. The present invention also provides addition salts of such cyclic aminophenylalkanoic acid derivatives and pharmaceutical compositions containing these compounds. | 02-05-2009 |
20090054488 | Isomigrastatin Analogs In The Treatment Of Cancer - The present invention provides compounds having formula (I): (I) wherein n, R | 02-26-2009 |
20090054489 | Multimediator Dopamine Transport Inhibitors, and Uses Related Thereto - The invention provides a class of DAT-5HT2 antagonists, packaged pharmaceuticals comprising such antagonists, and their uses in treating, or manufacturing medicaments for treating disease conditions, including a movement disorder, attention deficit disorder or attention-deficit hyperactivity disorder, anxiety, depression or psychotic disorder. Related business methods such as marketing the inhibitors to healthcare providers are also provided. | 02-26-2009 |
20090076081 | PIPERIDINE DERIVATIVES AS NK3 ANTAGONISTS - The invention relates to a compound of formula | 03-19-2009 |
20090082400 | SOLUBLE PYRONE ANALOGS METHODS AND COMPOSITIONS - Methods and compositions are described that comprise pyrone analogs such as flavonoids and cyclodextrins including quercetin and quercetin derivatives and sulfoalkyl ether cyclodextrins. In some cases the compounds of the invention are administered with a therapeutic agent such as an analgesic. In some cases, treatment with the compositions of the invention can result in the modulation of central nervous system and/or fetal effects of substances. Methods and compositions are described for the modulation of efflux transporter activity to increase the efflux of drugs and other compositions out of a physiological compartment and into an external environment. In particular, the methods and compositions disclosed herein provide for the increase of efflux transporter activity at blood-brain, blood-CSF and placental-maternal barriers to increase the efflux of drugs and other compositions from physiological compartments, including central nervous system and fetal compartments. | 03-26-2009 |
20090082401 | DEUTERIUM-ENRICHED TIAGABINE - The present application describes deuterium-enriched tiagabine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-26-2009 |
20090099233 | HETEROARYL AMIDES USEFUL AS INHIBITORS OF VOLTAGE-GATED SODIUM CHANNELS - The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 04-16-2009 |
20090105304 | COMBINATION THERAPY FOR REDUCING SIDE EFFECTS USING CANNABINOID RECEPTOR LIGANDS - The present application describes a method of treating conditions treatable with a CB | 04-23-2009 |
20090111855 | SUBSTITUTED PHENOXY THIAZOLIDINEDIONES AS ESTROGEN RELATED RECEPTOR-alpha MODULATORS - The present invention relates to compounds of Formula (I), | 04-30-2009 |
20090124662 | Migrastatin analogs in the treatment of cancer - In one aspect, the present invention provides a method for treating colon and/or ovarian cancer in a subject comprising administering to a subject in need thereof a compound of general formula (I): wherein R1-R6, R, -R, Q, Y1, Y2 and n are as defined herein, wherein the compound is present in an amount effective to inhibit colon and/or ovarian tumor metastasis. | 05-14-2009 |
20090131479 | Small-volume oral transmucosal dosage - Small-volume oral transmucosal dosage forms or NanoTabs® comprising a predetermined amount of a pharmaceutically active drug are provided. Exemplary applications include use of the NanoTabs® to administer a drug for the treatment of acute, post-operative or breakthrough pain. | 05-21-2009 |
20090143435 | GABA enhancers in the treatment of diseases relating to reduced neurosteroid activity - The invention provides the use of a non-steroid compound which acts on the GABA receptor for the treatment of disorders relating to reduced neurosteroid activity. The non-steroid compounds may be GABA agonists, GABA uptake inhibitors or enhancers of GABAergic activity. | 06-04-2009 |
20090156642 | 5-Membered heterocyclic compound - The present invention provides 5-membered heterocycle compounds represented by the following general formula (I): | 06-18-2009 |
20090170900 | DOSING REGIMEN FOR WEIGHT LOSS - Disclosed are dosing regimens and methods for the treatment of obesity, overweight and/or overeating in mammals comprising administering to the mammal a pharmaceutically effective amount of a CB1 receptor antagonist as a unit dosage according to a continuous schedule having a dosing interval selected from the group consisting of once-weekly dosing, twice-weekly dosing, thrice-weekly dosing, biweekly and bimonthly. | 07-02-2009 |
20090197917 | USE OF RIMONABANT FOR THE PREPARATION OF MEDICAMENTS USEFUL IN THE PREVENTION AND TREATMENT OF TYPE 2 DIABETES - The invention relates to the use of rimonabant, either alone or combined with another active ingredient, for the preparation of medicaments useful in the prevention and treatment of type 2 diabetes or non-insulin-dependent diabetes and/or its complications. | 08-06-2009 |
20090215825 | SUBSTITUTED PYRAZOLES, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE - The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus. | 08-27-2009 |
20090239909 | TREATMENT OF METABOLIC SYNDROME WITH LACTAMS - The present invention relates to the treatment of metabolic syndrome or disorders associated with metabolic syndrome comprising administering a compound of the invention. | 09-24-2009 |
20090258902 | BIPHENYL-PYRAZOLECARBOXAMIDE COMPOUNDS - The present invention relates to biphenyl-pyrazole compounds and in particular biphenyl-pyrazolecarboxamides. The invention further provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by antagonism or inverse agonism of the CB | 10-15-2009 |
20090264469 | NOVEL DICARBOXYLIC ACID DERIVATIVES - The present patent application concerns new compounds of formula (I): displaying agonistic activity at sphingosine-1-phosphate (S1P) receptors, their process of preparation and their use as immunosuppressive agents. | 10-22-2009 |
20090264470 | CB1 Antagonists and Inverse Agonists - The present invention relates to methods of treating obesity, anorexia nervosa, or bulimia nervosa comprising administering a compound of the invention. The present invention further relates to the treatment of metabolic syndrome comprising administering a compound of the invention. | 10-22-2009 |
20090264471 | Compounds, Compositions and Methods Comprising Triazole Derivatives - The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-II) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease. | 10-22-2009 |
20090270454 | Sulfonamide containing compounds for treatment of inflammatory disorders - Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of an inflammatory condition, in particular asthma. The compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof: | 10-29-2009 |
20090270455 | Therapeutic agent for intestinal diseases and visceral pain - The present invention relates to a therapeutic agent for irritable bowel syndrome of diarrhea type, ulcerative colitis, visceral pain or abdominal pain, which contains a compound of the following formula and which has 5-HT7 receptor antagonistic effect or an analogue thereof; and this therapeutic agent has an excellent therapeutic effect and a high safety: | 10-29-2009 |
20090298883 | N-PIPERIDINYL ACETAMIDE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS - Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1). | 12-03-2009 |
20090306138 | PYRROLIDINE DERIVATIVES ACTING AS CCR3-RECEPTOR ANTAGONISTS - Compounds of formula I | 12-10-2009 |
20090306139 | HETEROARYL-SUBSTITUTED PIPERIDINES - The invention relates to novel heteroaryl-substituted piperidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular diseases and tumour diseases. | 12-10-2009 |
20090306140 | 3 or 4-Substituted Piperidine Compounds - There are disclosed racemic or enantiomerically enriched 3- or 4-substituted piperidine compounds represented by the following structural formula (I) | 12-10-2009 |
20090312369 | Renin Inhibitors - The present invention is directed to aspartic protease inhibitors represented by the following structural formula (I), or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the aspartic protease inhibitors of Structural Formula (I). Methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using these aspartic protease inhibitors are also disclosed. | 12-17-2009 |
20090318499 | COMPOUNDS HAVING ANALGESIC AND/OR IMMUNOSTIMULANT ACTIVITY - The compounds shown by their structural formulas in the specification have analgesic and or immunostimulant activity in mammals. | 12-24-2009 |
20090318500 | 4-(2, 6-Dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid (1-methanesulphonyl-piperidin-4-yl)-amide for the Treatment of Cancer - The invention provides the compound of formula (I) 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid (1-methanesulphonyl-piperidin-4-yl)-amide in a substantially crystalline form, therapeutic uses thereof and pharmaceutical compositions containing the crystalline compound. The invention also provides novel pharmaceutical formulations containing 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid (1-methanesulphonyl-piperidin-4-yl)-amide and novel processes for preparing the compound. | 12-24-2009 |
20090318501 | Piperidine derivatives as renin inhibitors - The present invention is directed to aspartic protease inhibitors represented by the following structural formula; or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the aspartic protease inhibitors of Structural Formula (I). Methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using these aspartic protease inhibitors are also disclosed. | 12-24-2009 |
20100004287 | Cyclic Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase - Cyclic amine derivatives 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; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis. | 01-07-2010 |
20100004288 | FUNGICIDAL AMIDES - Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, | 01-07-2010 |
20100010045 | PYRAZOLE-DERIVATIVES AS FACTOR Xa INHIBITORS - The present invention is directed to a compound of formula I, | 01-14-2010 |
20100022590 | Novel compounds - The present invention relates to novel isoxazole compounds of formula (I), | 01-28-2010 |
20100022591 | PIPERIDINE GPCR AGONISTS - Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes. | 01-28-2010 |
20100022592 | THIAZOLE DERIVATIVES AS MODULATORS OF G PROTEIN-COUPLED RECEPTORS - The invention provides compounds of formula (IA) or (IB) and pharmaceutical compositions thereof, which are useful for modulating G protein-coupled receptor 120 (GPR120), and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated GPR120. | 01-28-2010 |
20100022593 | Process for Producing Anticancer Agent LL-D45042 - The disclosure describes the production of anticancer agent LL-D45042, having the structure: | 01-28-2010 |
20100022594 | HETEROCYCLIC SULFONAMIDE INHIBITORS OF BETA AMYLOID PRODUCTION - Compounds of Formula (I), | 01-28-2010 |
20100029719 | ARYLSULFONAMIDE DERIVATIVES AS C-JUN-N-TERMINAL KINASES (JNK'S) INHIBITORS - The present invention relates to sulfonamide derivatives of formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are useful in the treatment of neuronal disorders, autoimmune diseases, cancer and cardiovascular diseases. Furthermore, said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and -3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. | 02-04-2010 |
20100035929 | UNNATURAL DISPYRIN ANALOGUES, PREPARATION AND USES THEREOF - Disclosed are dispyrin analogue compounds useful as H3 receptor activity modulators, methods of making same, pharmaceutical compositions comprising same, and methods of treating neurological and psychiatric disorders associated with histamine H3 receptor activity using same. In one aspect, the disclosed analogues can have a structure represented by a formula: | 02-11-2010 |
20100048631 | Piperidine GPCR Agonists - Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes. | 02-25-2010 |
20100048632 | Piperidine GPCR Agonists - Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes. | 02-25-2010 |
20100048633 | Piperidine-4-acrylamides - A compound of formula (I), wherein substituents are as given above, useful in the treatment of a disease mediated by the action of CCR3. | 02-25-2010 |
20100048634 | METHOD FOR TREATING APATHY SYNDROME - The present invention provides a method of treating apathy syndrome in a human subject. The human subject is first evaluated to determine whether one or more behavioral characteristics of apathy are observed. If such characteristics are observed, the subject is treated with a 2-oxopyrrolidine compound, such as nefiracetam, piracetam, aniracetam, pramiracetam, nebracetam, fasoracetam, levetiracetam, or oxiracetam, in an amount effective to produce an improvement in such apathy characteristics. The present invention is useful in treating apathy in a subject suffering from conditions associated with or characterized by frontal-subcortical dysfunction. The present invention is also useful in treating apathy in a subject suffering from a stroke, Alzheimer's disease, Parkinson's disease, traumatic brain injury, depression, schizophrenia, chronic hepatitis C infection, or HIV infection. | 02-25-2010 |
20100056574 | Crystalline Forms of Sufentanil - The present invention provides crystalline forms of sufentanil citrate and methods for preparing crystalline forms of sufentanil citrate. | 03-04-2010 |
20100063095 | HEMIASTERLIN DERIVATIVES AND USES THEREOF IN THE TREATMENT OF CANCER - The present invention provides compounds having formula (I): | 03-11-2010 |
20100069437 | THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN - 4-Tetrazolyl-4-phenylpiperidine Compounds, compositions comprising an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound, methods for treating or preventing pain or diarrhea in an animal comprising administering to an animal in need thereof an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound and methods for stimulating opioid-receptor function in a cell comprising contacting a cell capable of expressing an opioid receptor with an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound are disclosed. | 03-18-2010 |
20100076022 | NOVEL POLYMORPHS OF RIMONABANT - The present invention discloses novel and stable polymorphs of rimonabant, its hydrates and solvates, to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention further discloses a novel and stable amorphous form of rimonabant, process for its preparation and a pharmaceutical composition comprising it. The present invention also provides an improved process for the preparation of rimonabant crystalline Form II. Thus, for example, rimonabant is dissolved in methylene dichloride, stirred for 10 minutes at 25-30° C. and then the solvent distilled off under vacuum at 40° C. The resulting residue is stirred with water and the separated solid is collected at 25-30° C. to give a stable crystalline rimonabant hydrate. | 03-25-2010 |
20100076023 | AMORPHOUS SOLID COMPOSITION CONTAINING A PYRAZOLE-3-CARBOXAMIDE IN AMORPHOUS FORM AND STABILISING CARRIERS - The invention relates to a pyrazole-3-carboxamide in amorphous form, to an amorphous solid solution containing the same, and more generally to pharmaceutical composition containing the same | 03-25-2010 |
20100081692 | Novel 1-Benzyl-4-Piperidinamines that are Useful in the Treatment of COPD and Asthma - The invention provides 1-benzyl-4-piperidinamines of the general formula (I), processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are useful in the treatment of respiratory diseases such as chronic obstructive pulmonary disease and asthma. The compounds are inhibitors of the CCR1 receptor. | 04-01-2010 |
20100081693 | THIADIAZOLE COMPOUND AND USE THEREOF - A thiadiazole compound represented by the formula (I): | 04-01-2010 |
20100099712 | SUBSTITUTED PYRAZOLINE COMPOUNDS WITH ACAT INHIBITION ACTIVITY - The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals, especially in dyslipidaemia. | 04-22-2010 |
20100105735 | Small Volume Oral Transmucosal Dosage Forms Containing Sufentanil for Treatment of Pain - Compositions, methods and systems for administration of small volume sufentanil-containing drug dosage forms to the oral mucosa of a subject are disclosed. | 04-29-2010 |
20100113520 | KINASE KNOCKDOWN VIA ELECTROPHILICALLY ENHANCED INHIBITORS - Provided herein are electrophilically enhanced kinase inhibitors. Also provided herein are methods of making and utilizing the same. | 05-06-2010 |
20100113521 | PHARMACEUTICAL COMPOSITIONS COMPRISING 2-METHOXY-5-(5-TRIFLUOROMETHYL-TETRAZOL-1-YL-BENZYL)-(2S-PHENYLPIPERIDIN-- 3S-YL-) - The present invention relates to pharmaceutical compositions comprising the NK1 receptor antagonist [2-Methoxy-5-(5-trifluoromethyl-tetrazol-1-yl)-benzyl]-(2S-phenyl-piperidin-3S-yl)-amine, or a pharmaceutically acceptable salt or solvate thereof, and a sodium channel blocker, as a combined preparation for simultaneous or sequential administration and to the use of such compositions in the treatment of certain disorders, including epilepsy, mood disorders and pain. | 05-06-2010 |
20100120860 | THIA(DIA)ZOLES AS FAST DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS - The present invention relates to [1-(benzyl)-piperidin-4-yl]-([1,3,4]thiadiazol-2-yl)-amine and [1-(benzyl)-piperidin-4-yl]-(thiazol-2-yl)-amine derivatives of formula (I) that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects. | 05-13-2010 |
20100130551 | Sufentanil Solid Dosage Forms Comprising Oxygen Scavengers and Methods of Using the Same - Compositions and methods effective to minimize or eliminate the presence of oxidative degradation products in solid dosage forms comprising sufentanil are provided. | 05-27-2010 |
20100144791 | CANNABINOID RECEPTOR ANTAGONISTS/INVERSE AGONISTS USEFUL FOR TREATING OBESITY - The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders. | 06-10-2010 |
20100152241 | INHIBITORS OF STORE OPERATED CALCIUM RELEASE - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity. | 06-17-2010 |
20100168169 | SUBSTITUTED 1,3-DIOXANES USEFUL AS PPAR MODULATORS - Specifically useful stereoisomers of 1,3-dioxane derivatives are described and their use in the treatment of a disease or condition dependent on PPAR modulation, such as diabetes, cancer, inflammation, neurodegenerative disorders and infections as well as their use in the treatment of a disease related to TP, such as cardiovascular diseases. | 07-01-2010 |
20100179191 | GLUCOPYRANOSYL-SUBSTITUTED CYCLOPROPYLBENZENE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING SUCH COMPOUNDS, THEIR USE AS SGLT INHIBITORS AND PROCESS FOR THEIR MANUFACTURE - Glucopyranosyl-substituted cyclopropyl-benzene derivatives defined according to claim | 07-15-2010 |
20100179192 | USE OF NITRIC OXIDE RELEASING COMPOUNDS IN THE TREATMENT OF CHRONIC PAIN - The present invention relates to nitrooxyderivative of antioxidant compounds of formula (I) and pharmaceutically acceptable salts or stereoisomers thereof for the treatment of chronic pain, in particular chronic neuropathic pain. The invention also describes composition comprising a nitrooxyderivative of a antioxidant compound of formula (I) and an analgesic drugs. | 07-15-2010 |
20100190827 | POLYMORPHIC FORM OF RIMONABANT, METHOD FOR PREPARING IT AND PHARMACEUTICAL COMPOSITIONS CONTAINING IT - The present invention relates to a novel crystalline polymorph of rimonabant, its method of preparation and the pharmaceutical compositions containing this novel polymorph. | 07-29-2010 |
20100190828 | Thiazolyl oxime ethers and hydrazones as crop protection agents - Thiazolyl oxime ethers and hydrazones of the formula (I), | 07-29-2010 |
20100216841 | 4-Fluoro-Piperidine T-Type Calcium Channel Antagonists - The present invention is directed to 4-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which T-type calcium channels 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 T-type calcium channels are involved. | 08-26-2010 |
20100234426 | Phenylpropionamide Compounds and the Use Thereof - The invention relates to phenylpropionamide compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A, B, R | 09-16-2010 |
20100249190 | Hepatitis C Virus Inhibitors - This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds. | 09-30-2010 |
20100261755 | ISOXAZOL-3(2H)-ONE ANALOGS AS THERAPEUTIC AGENTS - or a pharmaceutically suitable salt thereof, wherein,
| 10-14-2010 |
20100280073 | TRICYCLIC INHIBITORS OF HYDROXYSTEROID DEHYDROGENASES - The present invention provides tricyclic compounds according to formula (I): (I) where R | 11-04-2010 |
20100292273 | Cannabinoid Receptor Modulators - Compounds of formula (I) are modulators of cannabinoid receptor CB1, useful inter alia for treatment of obesity: Formula (I). Wherein: X is a bond, or a divalent radical selected from —C(R | 11-18-2010 |
20100292274 | HALOALKYL HETEROARYL BENZAMIDE COMPOUNDS - A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses. | 11-18-2010 |
20100292275 | FUNGICIDAL HETEROCYCLIC COMPOUNDS - Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, | 11-18-2010 |
20100298381 | GAMMA SECRETASE MODULATORS - In its many embodiments, the present invention provides a novel class of 5-membered, nitrogen-containing heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions. | 11-25-2010 |
20100317695 | GEL COMPOSITION FOR TREATING MYCOSIS - The present invention aims to provide a gel composition for mycosis treatment, which ensures good absorption and permeation of (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1H-1,2,4-triazol-1-yl)-butan-2-ol into a target site (skin and nail). The present invention also aims to provide a gel composition for mycosis treatment, which is excellent in stability of this drug. | 12-16-2010 |
20100324091 | Pyrazolone Derivative - A pyrazolone derivative represented by formula (I) below: | 12-23-2010 |
20110021568 | TUBULYSIN D ANALOGUES - The present invention provides novel tubulysin analogues, methods of making and methods of using such analogues and conjugates thereof. The compounds of the invention are highly potent cell-growth inhibitors have been developed that are smaller and considerably more stable than tubulysin D. | 01-27-2011 |
20110028517 | 4-METHYL-4,5-DIHYDRO-1H-PYRAZOLE-3-CARBOXAMIDE USEFUL AS A CANNABINOID CB1 NEUTRAL ANTAGONIST - The present invention relates to 4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide, and pharmaceutically acceptable salts and solvates thereof. It further concerns pharmaceutical compositions comprising this compound as active ingredient as well as processes and intermediates for preparing this compound and compositions. The referred compound is a cannabinoid CB1 neutral antagonist useful in the prophylaxis and treatment of food intake disorders. | 02-03-2011 |
20110034513 | Heterocyclic Sulfonamide Inhibitors of Beta Amyloid Production - Compounds of Formula (I), | 02-10-2011 |
20110053982 | ETHER BENZYLIDENE PIPERIDINE 5-MEMBERED ARYL CARBOXAMIDE COMPOUNDS USEFUL AS FAAH INHIBITORS - The present invention relates to compounds of the Formula (I), and pharmaceutically acceptable salts thereof, and their use in the treatment of FAAH-mediated diseases or condition. | 03-03-2011 |
20110053983 | (5R)-1,5-DIARYL-4,5-DIHYDRO-1H-PYRAZOLE-3-CARBOXAMIDINE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY - Embodiments of the invention relate to (5R)-1,5-diaryl-4,5-dihydro-1H-pyrazole-3-carboxamidine derivatives as cannabinoid-CB | 03-03-2011 |
20110082172 | PYRROLIDINONE CARBOXAMIDE DERIVATIVES - Pyrrolidinone carboxamide compounds are provided that are useful for inhibiting the binding of ligands to the ChemR23 receptor. | 04-07-2011 |
20110082173 | DIARYLMETHYLIDENE PIPERIDINE DERIVATIVES, PREPARATIONS THEREOF AND USES THEREOF - Compounds of formula: (I) wherein R | 04-07-2011 |
20110098321 | SALTS OF METHYL 2-((R)-(3-CHLOROPHENYL)((R)-1-((S)-2-(METHYLAMINO)-3-((R)-TETRAHYDRO-2H-P- YRAN-3-YL)PROPYLCARBAMOYL)PIPERIDIN-3-YL)METHOXY)ETHYLCARBAMATE - Mucic acid salts of a compound represented by the following structural formula: | 04-28-2011 |
20110105562 | ALKYNYL DERIVATIVES USEFUL AS DPP-1 INHIBITORS - The present invention is directed to novel alkynyl derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1. | 05-05-2011 |
20110112144 | METHODS OF PREPARING SUBSTITUTED HETEROCYCLES - The present disclosure relates to methods of preparing substituted thiophenes, which are useful for the treatment and prevention of cancers. Also disclosed are substituted thiophenes made by the methods disclosed herein. | 05-12-2011 |
20110112145 | Salts Of Methyl 2-((R))-(3-Chlorophenyl)((R)-1-((S)-2-(Methylamino)-3((R)-tetrahydro-2H-P- yran-3-YL)Propylcarbamoyl)Piperidin-3-YL)Methoxy)Ethylcarbamate - Disclosed are salts of methyl 2-((R)-(3-chlorophenyl)((R)-1-((S)-2-(methylamino)-3-((R)-tetrahydro-2H-pyran-3-yl)propylcarbamoyl)piperidin-3-yl)methoxy)ethylcarbamate and pharmaceutical compositions containing the same. Also disclosed are processes for the preparation thereof and methods for use thereof. | 05-12-2011 |
20110118314 | PIPERIDINE ANALOGS AS GLYCOGEN SYNTHASE ACTIVATORS - Provided herein are compounds of the formula (I): | 05-19-2011 |
20110124686 | SULTAM DERIVATIVES - The present invention relates to compounds according to formula 1, | 05-26-2011 |
20110136869 | Compounds Which Selectively Modulate The CB2 Receptor - Compounds of formula (I) | 06-09-2011 |
20110136870 | GACYCLIDINE FORMULATIONS - Improved formulations of gacyclidine for direct administration to the inner or middle ear. | 06-09-2011 |
20110160248 | PYRAZOLE COMPOUNDS AND USES THEREOF - The invention provides a compound of formula I: | 06-30-2011 |
20110166182 | Selective Estrogen Receptor Modulator for the Treatment of Osteoarthritis - The present invention is directed to a compound of the formula (A): or a pharmaceutically acceptable salt thereof; and also to compounds of formula (I): or a pharmaceutically acceptable salt thereof. | 07-07-2011 |
20110172274 | FLUORO-SUBSTITUTED 3,4-DIARYL-4,5-DIHYDRO-1H-PYRAZOLE-1-CARBOXAMIDINE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY - This invention concerns fluorinated 3,4-diaryl-4,5-dihydro-1H-pyrazole-1-carboxamidine derivatives as cannabinoid-CB | 07-14-2011 |
20110190349 | TETRAHYDRO-PYRAN DERIVATIVES - The present invention relates to a compound of formula I | 08-04-2011 |
20110195994 | Piperidinyl GPCR Agonists - Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of diabetes and obesity. | 08-11-2011 |
20110195995 | Methods of Optimizing Treatment of Estrogen-Receptor Positive Breast Cancers - Estrogen-receptor positive and progesterone-receptor positive breast cancer treatment can be optimized by determining the level of expression of genes in a breast sample from a human having an estrogen-receptor positive and progesterone-receptor positive breast cancer that identify a human with an increased likelihood of recurrence of the breast cancer. | 08-11-2011 |
20110224257 | Bis(difluoromethyl)pyrazoles as Fungicides - Bis(difluoromethyl)pyrazole derivatives of the formula (I) | 09-15-2011 |
20110224258 | FUNGICIDAL HETEROCYCLIC COMPOUNDS - Disclosed are compounds of Formula 1, including all geometric and stereoisomers, tautomers, N-oxides, and salts thereof, | 09-15-2011 |
20110230521 | Pyrazole Compounds As CCR1 Antagonists - Disclosed are compounds of the formula (I) which block the interaction of CCR1 and its ligands and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes. | 09-22-2011 |
20110237625 | SUBSTITUTED PHENOXY THIAZOLIDINEDIONES AS ESTROGEN RELATED RECEPTOR-a MODULATORS - The present invention relates to compounds of Formula (I), | 09-29-2011 |
20110245295 | BIOACTIVE PRE-TUBULYSINS AND USE THEREOF - The invention relates to bioactive pre-tubulysin derivatives, their preparation and pharmacological use. | 10-06-2011 |
20110263650 | Tubulysin D Analogues - The present invention provides novel tubulysin analogues, methods of making and methods of using such analogues and conjugates thereof. The essential features for the potent cytotoxicity of tubulysin D have been established for the first time by the synthesis and evaluation of a series of analogues. By identifying functionality that surprisingly is not necessary for activity, highly potent cell-growth inhibitors have been developed that are smaller and considerably more stable than tubulysin D. | 10-27-2011 |
20110275673 | INHIBITORS OF SPHINGOSINE KINASE 1 - The invention relates to compounds of Formula (I). Compounds of the present invention are inhibitors of sphingosine kinase 3, and are useful in the treatment of various disorders and conditions, such as inflammatory disorders. | 11-10-2011 |
20110281913 | MELANOCORTIN RECEPTOR ANTAGONIST COMPOUNDS, PROCESS FOR PREPARING THEM AND USE THEREOF IN HUMAN MEDICINE AND COSMETICS - Melanocortin receptor antagonist compounds, processes for preparing them and uses thereof in human medicine and cosmetics are described. | 11-17-2011 |
20110288128 | Oral Transmucosal Administration of Sufentanil - Compositions and methods for administration of sufentanil-containing drug formulations to the oral mucosa of a subject are disclosed. | 11-24-2011 |
20110312999 | Ketoheteroarylpiperidine and -Piperazine Derivatives as Fungicides - Ketoheteroarylpiperidine and -piperazine derivatives of the formula (I), | 12-22-2011 |
20120010246 | Compositions and methods for treating diseases of the nail - Methods and compositions for treating disorders of the nail and nail bed. Such compositions contain a vehicle in which all components of the composition are dissolved, suspended, dispersed, or emulsified, a non-volatile solvent, a wetting agent, and a pharmaceutically active ingredient that is soluble in the non-volatile solvent and/or a mixture of the vehicle and the non-volatile solvent, which composition has a surface tension of 40 dynes/cm or less and has continuing spreadability, and which composition is effective in treating a disorder of the nail or nail bed. | 01-12-2012 |
20120022107 | 2-(PIPERIDIN-1-YL)-4-AZOLYL-THIAZOLE-5-CARBOXYLIC ACID DERIVATIVES AGAINST BACTERIAL INFECTIONS - Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described. | 01-26-2012 |
20120022108 | ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to new compounds of formula (I) wherein A, B, P, Q, W, R | 01-26-2012 |
20120022109 | OXADIAZOLE DERIVATIVES - The invention relates to oxadiazole compounds of formula I. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis. | 01-26-2012 |
20120035216 | SMALL VOLUME ORAL TRANSMUCOSAL DOSAGE FORMS CONTAINING SUFENTANIL FOR TREATMENT OF PAIN - Compositions, systems and methods for administration of small volume sufentanil drug dosage forms via the oral transmucosal route of a subject for treatment of pain. | 02-09-2012 |
20120046317 | NOVEL HETEROCYCLIC COMPOUNDS - The present invention relates to a new class of heterocyclic compounds and pharmaceutically acceptable salts thereof, process for preparing the same, pharmaceutical composition containing these compounds and to their use in treatment of diseases caused due to formation and accumulation of AGEs (Advanced Glycation end products). The compounds of the present invention are useful for the treatment of diabetic and aging-related complications caused by formation and accumulation of AGEs, such as neuropathy, nephropathy, microangiopathy, retinopathy, hypertension, heart failure, atherosclerosis, Alzheimer's disease & dermatological disorders. | 02-23-2012 |
20120065231 | THIOPHENE DERIVATIVE - The present invention provides a compound represented by the formula (I) or its salt, solvate, or physiologically functional derivative; and a pharmaceutical composition which is useful for treatment or prevention of conditions or disorders having sensitivity to selective androgen receptor modulation, the composition comprising the above-described compound; among others: | 03-15-2012 |
20120122928 | Heteroarylpiperidine and -Piperazine Derivatives as Fungicides - Heteroarylpiperidine and -piperazine derivatives of the formula (I) | 05-17-2012 |
20120122929 | HETEROARYLPIPERIDINE AND -PIPERAZINE DERIVATIVES AS FUNGICIDES - Heteroarylpiperidine and -piperazine derivatives of the formula (I) | 05-17-2012 |
20120157497 | COMPOUNDS HAVING ANALGESIC AND/OR IMMUNOSTIMULANT ACTIVITY - The compounds shown by their structural formulas in the specification have analgesic and or immunostimulant activity in mammals. | 06-21-2012 |
20120184580 | SUBSTITUTED DI-ARYLHYDANTOIN AND DI-ARYLTHIOHYDANTOIN COMPOUNDS AND METHODS OF USE THEREOF - Substituted di-arylhydantoin and di-arylthiohydantoins are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including CRPC and/or hormone-sensitive prostate cancer. | 07-19-2012 |
20120190712 | Methods for Treating Cognitive Disorders - Disclosed herein are methods of treating a patient suffering a cognitive disorder. | 07-26-2012 |
20120208846 | Therapeutic Methods For Type I Diabetes - The invention relates to the treatment and prevention of type I diabetes. More specifically, the invention relates to compounds that treat or prevent the body's immune system from destroying β-cells (i.e., insulin-producing cells in the pancreatic islets of Langerhans) by inhibition of JNK2, selective inhibition of JNK2, or inhibition of the expression of the MAPK9 gene or gene product. In one embodiment, the present invention contemplates the diagnosis, identification, production, and use of compounds which modulate MAPK9 gene expression or the activity of the MAPK9 gene product including but not limited to, JNK2, the nucleic acid encoding MAPK9 and homologues, analogues, and deletions thereof, as well as antisense, ribozyme, triple helix, antibody, and polypeptide molecules as well as small inorganic molecules. The present invention contemplates a variety of pharmaceutical formulations and routes of administration for such compounds. | 08-16-2012 |
20120208847 | Diagnostic and Therapeutic Alkyl Piperidine/Piperazine Compounds and Process - Described herein are piperidine and piperazine compounds useful for treating neurodegenerated diseases characterized by a lack of dopamine neuron activity. The compounds are also useful for imaging dopamine neurons. | 08-16-2012 |
20120208848 | GACYCLIDINE FORMULATIONS - Improved formulations of gacyclidine for direct administration to the inner or middle ear. | 08-16-2012 |
20120225906 | PIPERIDINE RENIN INHIBITORS - The present invention is directed to aspartic protease inhibitors represented by the following structural formula: | 09-06-2012 |
20120225907 | BENZAMIDE COMPOUNDS USEFUL AS HISTONE DEACETYLASE INHIBITORS - The invention concerns benzamide compounds of formula (I): compound of formula (I): | 09-06-2012 |
20120264784 | METHODS OF TREATING ELEVATIONS IN MTOR SIGNALING - Subjects having elevated signaling of a mammalian target of rapamycin (mTOR) are treated with compositions that include at least one compound that activates a Group 1 mGluR. In an embodiment, the subject has tuberous sclerosis complex (TSC). In an embodiment, the compound is a Group 1 mGluR agonist. In another embodiment, the compound is a Group 1 mGluR positive allosteric modulator. | 10-18-2012 |
20120277266 | Hepatitis C Virus Inhibitors - This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds. | 11-01-2012 |
20120295938 | ETHERS, SECONDARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together. | 11-22-2012 |
20120302606 | 3-(4-((1H-IMIDAZOL-1-YL)METHYL)PHENYL)-5-ARYL-1,2,4-OXADIAZOLE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS - Substituted 3-(4-((1H-imidazol-1-yl)methyl)phenyl)-5-phenyl-1,2,4-oxadiazole derivatives which are useful as sphingosine-1-phosphate modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors. | 11-29-2012 |
20120316203 | Compositions and Methods for Inhibition of Cancers - Methods and compositions for treating cancers, including ovarian cancers, are described. The compositions generally include a redox based curcumin derivative, diarylidenylpiperiden-4-one (DAP) having a hydroxylamine moiety attached thereto. | 12-13-2012 |
20120322827 | COMPOUNDS AND METHODS - Disclosed are compounds having the formula: | 12-20-2012 |
20120329833 | USE OF ANTAGONISTS OF THE CBI RECEPTOR FOR THE MANUFACTURE OF A COMPOSITION USEFUL FOR THE TREATMENT OF HEPATIC DISEASES - The invention relates to the use of antagonists to the CB1 receptor for the preparation of a composition for the treatment of hepatic diseases and preferably to the use of N-piperidino5 5-(4-chlorophenyl)-1-(2, 4-dichloropenyl)-4-methylpyrazole-3-carboxamide. | 12-27-2012 |
20130005771 | OXADIAZOLE COMPOUNDS, THEIR PREPARATION AND USE - The present invention relates to oxadiazole compounds in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable prodrugs and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the oxadiazole compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the treatment of cancer, particularly chronic myeloid leukemia (CML). The present invention further provides a method of treatment of cancer by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof. | 01-03-2013 |
20130012544 | PYRAZOLONE DERIVATIVES AS PDE4 INHIBITORS - The compound 1-(2-{4-[3-(3,4-dimethoxyphenyl)-4,4-dimethyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl]piperidin-1-yl}-2-oxoethyl)pyrrolidine-2,5-dione is a novel effective inhibitor of the type 4 phosphodiesterase. | 01-10-2013 |
20130030022 | Compounds Which Selectively Modulate The CB2 Receptor - Compounds of formula (I) | 01-31-2013 |
20130045992 | Compositions and Methods for Enhancing Proteasome Activity - Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp 14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies. | 02-21-2013 |
20130053416 | 3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS - 3-Heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals The present invention relates to compounds of the formula I, | 02-28-2013 |
20130059890 | ANTIVIRAL AGENTS - The invention relates to agents for the treatment of hepatitis C virus infection. More specifically, the invention relates to antagonists of cannabinoid type 1 receptor signalling pathway proteins and their use for the treatment of hepatitis C virus infection. | 03-07-2013 |
20130059891 | SUBSTITUTED N-HETEROCYCLOALKYL BIPYRROLIDINYLPHENYL AMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - The present disclosure relates to a series of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I). | 03-07-2013 |
20130065925 | PYRROLIDIN-3-YLACETIC ACID DERIVATIVE - A compound represented by formula (1) or a pharmaceutically acceptable salt thereof has an inhibitory effect in the fractalkine-CX3CR1 pathway: | 03-14-2013 |
20130096160 | ARYLTHIAZOLYL PIPERIDINES AND RELATED COMPOUNDS AS MODULATORS OF SURVIVAL MOTOR NEURON (SMN) PROTEIN PRODUCTION - Aryl substituted thiazol-2-yl-piperidines and related compounds useful as modulators of survival motor neuron (SMN) protein production are provided herein. Without being bound to any particular theory it is believed the aryl substituted thiazol-2-yl-piperidines and related compounds provided herein act to increase production of the SMN2 form of survival motor neuron protein. These compounds are useful for treating spinal muscular atrophy. Pharmaceutical compositions containing a carrier and one or more of the aryl substituted thiazol-2-yl-piperidine or related compounds described herein are also provided. Methods of treating spinal muscular atrophy are also provided by this disclosure. | 04-18-2013 |
20130158074 | SMALL VOLUME ORAL TRANSMUCOSAL DOSAGE FORMS CONTAINING SUFENTANIL FOR TREATMENT OF PAIN - Compositions, methods and systems for administration of small volume sufentanil-containing drug dosage forms to the oral mucosa of a subject are disclosed. | 06-20-2013 |
20130158075 | HETEROCYCLIC COMPOUNDS AS DGAT1 INHIBITORS - The present invention relates to heterocyclic compounds of formula 1, in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, carboxylic acid isosteres and N-oxides. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof. | 06-20-2013 |
20130165481 | SMALL-VOLUME ORAL TRANSMUCOSAL DOSAGE FORMS - Small-volume oral transmucosal dosage forms or NanoTabs® comprising a predetermined amount of a pharmaceutically active drug are provided. Exemplary applications include use of the NanoTabs® to administer a drug for the treatment of acute, post-operative or breakthrough pain. | 06-27-2013 |
20130190353 | FUNGICIDE COMPOSITION COMPRISING A TETRAZOLYLOXIME DERIVATIVE AND A THIAZOLYLPIPERIDINE DERIVATIVE - The present invention relates to a pesticide composition intended for protecting plants, crops or seeds against fungal diseases or insect damages, and the corresponding methods of protection by application of the said composition. More precisely, the subject of the present invention is a pesticide composition based on a tetrazolyloxime derivative and a thiazolylpiperidine derivative, which may further comprise another fungicide and/or an insecticide active substance or compound. | 07-25-2013 |
20130197034 | Salts Of Methyl 2-((R)-(3-Chlorophenyl)((R)-1-((S)-2-(Methylamino)-3-((R)-Tetrahydro-2H-P- yran-3-Yl)Propylcarbamoyl)Piperidin-3-Yl)Methoxy)Ethylcarbamate - Mucic acid salts of a compound represented by the following structural formula: | 08-01-2013 |
20130203814 | Association of Rare Recurrent Genetic Variations to Attention-Deficit, Hyperactivity Disorder (ADHD) and Methods of Use Thereof for the Diagnosis and Treatment of the Same - Compositions and methods for the detection and treatment of ADHD are provided. | 08-08-2013 |
20130261155 | 1-(HETEROCYCLIC CARBONYL) PIPERIDINES - The present invention relates to fungicidal 1-(heterocyclic carbonyl) piperidines and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions. | 10-03-2013 |
20130267561 | Substituted 1,3-Dioxanes Useful as PPAR Modulators - Specifically useful stereoisomers of 1,3-dioxane derivatives are described and their use in the treatment of a disease or condition dependent on PPAR modulation, such as diabetes, cancer, inflammation, neurodegenerative disorders and infections as well as their use in the treatment of a disease related to TP, such as cardiovascular diseases. | 10-10-2013 |
20130274292 | Ketoheteroarylpiperdine and -Piperazine Derivatives as Fungicides - Ketoheteroarylpiperidine and -piperazine derivatives of the formula (I), | 10-17-2013 |
20130281490 | Disubstituted Beta-lactones as Inhibitors of N-Acylethanolamine Acid Amidase (NAAA) - The present invention provides compounds and pharmaceutical compositions for inhibiting N-acylethanolamine acid amidase (NAAA). Inhibition of NAAA is contemplated as a method to sustain the levels of palmitoylethanolamide (PEA) and oleylethanolamide (OEA), two substrates of NAAA, in conditions characterized by reduced concentrations of PEA and OEA. The invention also provides methods for treating inflammatory diseases and pain, and other disorders in which decreased levels of PEA and OEA are associated with the disorder. | 10-24-2013 |
20130317064 | MICROBIOCIDAL PYRAZOLE DERIVATIVES - The present invention provides compounds of formula I: wherein the substituents are as defined in claim | 11-28-2013 |
20130338193 | CHIRAL 1-(4-METHYLPHENYLMETHYL)-5-OXO--PYRROLIDINE-2-CARBOXAMIDES AS INHIBITORS OF COLLAGEN INDUCED PLATELET ACTIVATION AND ADHESION - Chiral 1-(4-methylphenylmethyl)-5-oxo-{N-[(3-t-butoxycarbonyl-aminomethyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamides as inhibitors of collagen induced platelet activation and adhesion The present invention provides chiral (2S)-1-(4-methyl-phenylmethyl)-5-oxo-(3S)-{N-[(3-t butoxycarbonyl aminomethyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamide, and (2S)-1-(4-methylphenylmethyl)-5-oxo-(3R)-{N-[(3-t-butoxycarbonyl amino methyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamide of formula 6 and 7 respectively. The present invention also relates to use of these moieties as inhibitors of collagen induced platelet adhesion and aggregation mediated through collagen receptors. The present invention provides a process for preparation of chiral carboxamides of formula 6 and 7 using the process which has advantage to avoid any racemization at the a-carboxylic center, during N-alkylation. The reagent LiHMDS is used at low temperatures to furnish methyl N-(p methylphenylmethyl)lpyroglutamate in good chiral purity. | 12-19-2013 |
20140005223 | ALFENTANIL COMPOSITION FOR THE TREATMENT OF ACUTE PAIN | 01-02-2014 |
20140005224 | HETEROARYL PIPERIDINE AND HETEROARYL PIPERAZINE DERIVATIVES AS FUNGICIDES | 01-02-2014 |
20140005225 | METHOD OF INHIBITING C-KIT KINASE | 01-02-2014 |
20140011844 | MIGRASTATIN ANALOGS AND USES THEREOF - The present invention provides compounds having formula (I): | 01-09-2014 |
20140011845 | CHEMICAL COMPOUNDS - Disclosed are cyclic dione derivatives represented by formula (I), wherein the substituents are as defined in the description. The preparation method, intermediate and use thereof are also provided. | 01-09-2014 |
20140057945 | Bis(difluoromethyl)pyrazoles as Fungicides - Bis(difluoromethyl)pyrazole derivatives of the formula (I) | 02-27-2014 |
20140073672 | NOVEL PYRAZOLONE-DERIVATIVES AND THEIR USE AS PDE-4 INHIBITORS - The compounds of Formula (I), | 03-13-2014 |
20140080870 | Transdermal Delivery Systems - Transdermal delivery systems for administering sufentanil through the skin are provided. The systems contain a sufficient amount of sufentanil to induce and maintain a constant state of analgesia when applied to a subject. The systems are characterized as having one or more features including a high degree of dosage form rate control over flux of sufentanil from the system, a high net flux of sufentanil from the system through the skin, lack of a permeation enhancer, an adhesive member demonstrating superior shear time, a low coefficient of variation in the net flux of sufentanil from the system, a high delivery efficiency, and a substantially constant steady state net flux of sufentanil from the system. Methods of using the transdermal delivery systems to administer a sufficient amount of sufentanil to induce and maintain analgesia for extended periods when applied to a subject are also provided. | 03-20-2014 |
20140107157 | PYRAZOLE DERIVATIVES AS CANNABINOID RECEPTOR 1 ANTAGONISTS - The invention provides compounds capable of acting as antagonists at cannabanoid receptors according to the following formula: Such compounds may be used to treat conditions for which the cannabinoid receptor system has been implicated, such as obesity, liver disease, diabetes, pain, and inflammation. | 04-17-2014 |
20140107158 | METHODS FOR TREATING COGNITIVE DISORDERS - Disclosed herein are methods of treating a patient suffering a cognitive disorder. | 04-17-2014 |
20140155433 | BIARYL DERIVATIVES AS NACHR MODULATORS - Disclosed is a compound of formula (I): wherein ‘D’, ‘E’, ‘m’, ‘n’ and R | 06-05-2014 |
20140221428 | ARYLSULFONAMIDE CCR3 ANTAGONISTS - Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition. | 08-07-2014 |
20140243371 | MICROBIOCIDAL PYRAZOLE DERIVATIVES - The present invention relates to compounds of formula (I) wherein R | 08-28-2014 |
20140275169 | Combination Therapies for Enhancing Protein Degradation - Disclosed herein are combination therapies for enhancing protein degradation. One component is an inhibitor of USP14, while the second component is an inhibitor of Hsp70. In certain embodiments, the invention relates to methods of treating or preventing a tauopathy, such as Alzheimer's disease. | 09-18-2014 |
20140303210 | Heteroarylpiperidine and - piperazine derivates as fungicides - Heteroarylpiperidine and -piperazine derivatives of the formula (I) | 10-09-2014 |
20140350054 | SMALL-VOLUME ORAL TRANSMUCOSAL DOSAGE FORMS - Small-volume oral transmucosal dosage forms or NanoTabs® comprising a predetermined amount of a pharmaceutically active drug are provided. Exemplary applications include use of the NanoTabs® to administer a drug for the treatment of acute, post-operative or breakthrough pain. | 11-27-2014 |
20140378509 | PYRAZOLONE DERIVATIVES AS PDE4 INHIBITORS - The compound 1-(2-{4-[3-(3,4-dimethoxyphenyl)-4,4-dimethyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl]piperidin-1-yl}-2-oxoethyl)pyrrolidine-2,5-dione is a novel effective inhibitor of the type 4 phosphodiesterase useful in the treatment of psoriasis or atopic dermatitis. | 12-25-2014 |
20150038534 | COMPOUNDS AND METHODS - Disclosed are compounds having the formula: | 02-05-2015 |
20150045393 | Novel Cysteine Protease Inhibitors and Uses Thereof - The invention provides for novel cysteine protease inhibitors and compositions comprising novel cysteine protease derivatives. The invention further provides for methods for treatment of neurodegenerative diseases comprising administration novel cysteine protease inhibitors or compositions comprising novel cysteine protease inhibitors. In some embodiments, the cysteine protease inhibitors are calpain inhibitors. | 02-12-2015 |
20150051249 | INHIBITION OF MCL-1 AND/OR BFL-1/A1 - This disclosure features compounds and pharmaceutically acceptable salts thereof that inhibit MCL-1 and/or BFL-1/A1 and compositions containing the same. This disclosure also features combinations that include one or more of the MCL-1/BFL-1/A1 inhibitor compounds described herein, or a pharmaceutically acceptable salt thereof; and one or more additional therapeutic agents (e.g., one or more chemotherapeutic agents (including small molecule and/or anti-body based chemotherapy and/or radiation); e.g., one or more therapeutic agents that modulate apoptosis; e.g., one or more therapeutic agents that bind to and inhibit anti-apoptotic proteins or modulate them indirectly; e.g., one or more therapeutic agents that bind to and inhibit, or indirectly modulate, anti-apoptotic BCL-2, BCL-XL, BCL-w, MCL-1, and/or BFL-1/A1; e.g., one or more therapeutic agents that directly bind to and inhibit anti-apoptotic BCL-2/BCL-XL; e.g., agents such as ABT-199, ABT-263 and ABT-737; e.g., ABT-737), or (where applicable) a pharmaceutically acceptable salt of the one or more therapeutic agents (as well as compositions containing the same). Also featured are methods of using such compounds, salts, combinations, and compositions, e.g., for the treatment or prevention of diseases, disorders, and conditions associated with deregulated apoptosis of cells (e.g., diseased or damaged cells; e.g., insufficient apoptosis of diseased or damaged cells or reduced apoptosis of diseased or damaged cells). | 02-19-2015 |
20150065541 | Bis(difluoromethyl)pyrazoles as Fungicides - Bis(difluoromethyl)pyrazole derivatives of the formula (I) | 03-05-2015 |
20150065542 | ANTI-VIRAL COMPOUNDS - The present invention relates to anti-HCV compounds, compositions comprising the same and methods of using the same to treat HCV infection. | 03-05-2015 |
20150073020 | COMPOSITIONS AND METHODS FOR TREATING DISEASES OF THE NAIL - Methods and compositions for treating disorders of the nail and nail bed. Such compositions contain a vehicle in which all components of the composition are dissolved, suspended, dispersed, or emulsified, a non-volatile solvent, a wetting agent, and a pharmaceutically active ingredient that is soluble in the non-volatile solvent and/or a mixture of the vehicle and the non-volatile solvent, which composition has a surface tension of 40 dynes/cm or less and has continuing spreadability, and which composition is effective in treating a disorder of the nail or nail bed. | 03-12-2015 |
20150087675 | NOVEL DISUBSTITUTED 3,4-DIAMINO-3-CYCLOBUTENE-1,2-DIONE COMPOUNDS FOR USE IN THE TREATMENT OF CHEMOKINE-MEDIATED DISEASES - Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds corresponding to general formula (I) are disclosed. Also disclosed, are pharmaceutical compositions including these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated diseases. | 03-26-2015 |
20150094337 | HETEROCYCLIC GROUP CONTAINED AMINO-METHANOL DERIVATIVE, AND SALT, SYNTHETIC METHOD AND USE THEREOF - The present invention provides a heterocyclic group contained amino-methanol derivative, and salt, a preparation method and use thereof, and belongs to the medical field. The heterocyclic group contained amino-methanol derivative and the salt thereof of the present invention are used for preparing medicines for immune suppression and for the treatment of organ transplant rejection, or medicines for treating immune mediated inflammatory diseases, such as multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis. | 04-02-2015 |
20150099785 | STABILIZED EFINACONAZOLE COMPOSITIONS - The present invention provides compositions containing efinaconazole, butylated hydroxytoluene, a salt of ethylenediaminetetraacetic acid, and optional citric acid. The compositions exhibit stable color profiles and are useful in the treatment of fungal infections. | 04-09-2015 |
20150105424 | SMALL VOLUME ORAL TRANSMUCOSAL DOSAGE FORMS CONTAINING SUFENTANIL FOR TREATMENT OF PAIN - Compositions, systems and methods for administration of small volume sufentanil drug dosage forms to the sublingual mucosa of a subject for treatment of pain using a device are disclosed. | 04-16-2015 |
20150133501 | ALFENTANIL COMPOSITION FOR THE TREATMENT OF ACUTE PAIN - There is provided pharmaceutical compositions for the treatment of pain e.g. short-term pain, which compositions comprise a mixture comprising:
| 05-14-2015 |
20150148378 | ANTI-INFECTIVE METHODS, COMPOSITIONS, AND DEVICES - The present invention provides methods for treating onychomycosis. In certain embodiments, the methods comprise comprising applying a pharmaceutically acceptable formulation containing 10% efinaconazole once a day for a treatment period of at least 36 weeks to the treatment area of an onychomycosis patient (a) without debriding the nail or nail-associated tissue initially or during the treatment period and/or (b) without removing the formulation from the treatment area during the treatment period. In certain embodiments, the formulation also comprises, water, cyclomethicone, diisopropyl adipate, alcohol, C12-15 alkyl lactate, butylated hydroxytoluene, citric acid anhydrous, and disodium edetate. | 05-28-2015 |
20150291554 | Bruton's Tyrosine Kinase Inhibitors - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 10-15-2015 |
20150291577 | CYCLOPROPANAMINE COMPOUND AND USE THEREOF - The present invention provides a compound having a lysine-specific demethylase-1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for schizophrenia, developmental disorders, particularly diseases having intellectual disability (e.g., autistic spectrum disorders, Rett syndrome, Down's syndrome, Kabuki syndrome, fragile X syndrome, Kleefstra syndrome, neurofibromatosis type 1, Noonan syndrome, tuberous sclerosis), neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, spinocerebellar degeneration (e.g., dentatorubural pallidoluysian atrophy) and Huntington's disease), epilepsy (e.g., Dravet syndrome) or drug dependence, and the like. A compound represented by the formula | 10-15-2015 |
20150307475 | Autotaxin inhibitors - The present invention relates to novel compounds of formula (I) (I) that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in the treatment of an ATX-dependent or ATX-mediated disease or condition. | 10-29-2015 |
20150313839 | CONTROLLED RELEASE AURIS SENSORY CELL MODULATOR COMPOSITIONS AND METHODS FOR THE TREATMENT OF OTIC DISORDERS - Disclosed herein are compositions and methods for the treatment of otic diseases or conditions with auris sensory cell modulating agent compositions and formulations administered locally to an individual afflicted with an otic disease or condition, through direct application of these compositions and formulations onto or via perfusion into the targeted auris structure(s). | 11-05-2015 |
20150313889 | HETEROARYLCARBOXYLIC ACID ESTER DERIVATIVE - Compounds represented by formula (I): | 11-05-2015 |
20150328189 | ANESTHETIC COMPOUNDS AND RELATED METHODS OF USE - Provided herein are compounds according to formula (I): provided herein is also a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and a method for providing anesthesia in a subject by administering such a pharmaceutical composition. | 11-19-2015 |
20150329522 | MELANOCORTIN RECEPTOR ANTAGONIST COMPOUNDS, PROCESS FOR PREPARING THEM AND USE THEREOF IN HUMAN MEDICINE AND COSMETICS - The present invention relates to novel melanocortin receptor antagonist compounds corresponding to the general formula (I) below: | 11-19-2015 |
20150335631 | METHOD OF TREATING THERMOREGULATORY DYSFUNCTION WITH PAROXETINE - The present invention relates to a method for treating a patient suffering from a thermoregulatory dysfunction, especially hot flashes and flushes associated with hormonal changes due to naturally occurring menopause (whether male or female) or due to chemically or surgically induced menopause. The method is also applicable to treating the hot flashes, hot flushes, or night sweats associated with disease states that disrupt normal hormonal regulation of body temperature. | 11-26-2015 |
20150351403 | Heteroarylpiperidine and -piperazine derivatives as fungicides - Heteroarylpiperidine and -piperazine derivatives of the formula (I) | 12-10-2015 |
20150353488 | BIPHENYL-ETHYL-PYRROLIDINE DERIVATIVES AS HISTAMINE H3 RECEPTOR MODULATORS FOR THE TREATMENT OF COGNITIVE DISORDERS - The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that modulate the activity of the histamine H3 receptor (Ia). Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders. | 12-10-2015 |
20150374679 | COMPOSITIONS AND METHODS FOR TREATING DISEASES OF THE NAIL - Methods and compositions for treating disorders of the nail and nail bed. Such compositions contain a vehicle in which all components of the composition are dissolved, suspended, dispersed, or emulsified, a non-volatile solvent, a wetting agent, and a pharmaceutically active ingredient that is soluble in the non-volatile solvent and/or a mixture of the vehicle and the non-volatile solvent, and which composition is effective in treating a disorder of the nail or nail bed. | 12-31-2015 |
20160075651 | GLYCOLIPID INHIBITION USING IMINOSUGARS - The application provides iminosugars with a high activity and specificity for inhibiting ceramide glucosyltransferase. | 03-17-2016 |
20160081995 | Selective NR2B Antagonists - The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system. | 03-24-2016 |
20160096822 | Novel Cannabinergic Nitrate Esters and Related Analogs - Biologically active cannabinergic nitrate esters and related analogs, process of preparation, pharmaceutical compositions and their methods of use as medicaments, pharmacological tools or biomarkers. Pharmaceutical compositions may include one or more of the nitrate ester compounds. Medicaments include one or more of the cannabinergic nitrate ester compounds and are useful in treating a variety of diseases. A method of treating, preventing or reducing the severity of a condition includes administering at least one of the disclosed nitrate ester compounds to an individual or animal in need thereof. | 04-07-2016 |
20160102085 | NOVEL (CYANO-DIMETHYL-METHYL)-ISOXAZOLES AND -[1,3,4]THIADIAZOLES - This invention relates to novel (Cyano-dimethyl-methyl)-isoxazolesand-[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions. | 04-14-2016 |
20160122317 | 1-SULFONYL PIPERIDINE DERIVATIVES AS MODULATORS OF PROKINETICIN RECEPTORS | 05-05-2016 |
20160135461 | PIPERIDINECARBOXYLIC ACID DERIVATIVES AS FUNGICIDES - Piperidinecarboxylic acidderivatives of the formula (I) | 05-19-2016 |
20160143896 | CHIRAL 1-(4-METHYLPHENYLMETHYL)-5-OXO--PYRROLIDINE-2-CARBOXAMIDES AS INHIBITORS OF COLLAGEN INDUCED PLATELET ACTIVATION AND ADHESION - Chiral 1-(4-methylphenylmethyl)-5-oxo-{N-[(3-t-butoxycarbonyl-aminomethyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamides as inhibitors of collagen induced platelet activation and adhesion. The present invention provides chiral (2S)-1-(4-methyl-phenylmethyl)-5-oxo-(3S)-{N-[(3-t-butoxycarbonyl aminomethyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamide, and (2S)-1-(4-methylphenylmethyl)-5-oxo-(3R)-{N-[(3-t-butoxycarbonyl amino methyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamide of formula 6 and 7 respectively. The present invention also relates to use of these moieties as inhibitors of collagen induced platelet adhesion and aggregation mediated through collagen receptors. The present invention provides a process for preparation of chiral carboxamides of formula 6 and 7 using the process which has advantage to avoid any racemization at the a-carboxylic center, during N-alkylation. The reagent LiHMDS is used at low temperatures to furnish methyl N-(p-methylphenylmethyl)1pyroglutamate in good chiral purity. | 05-26-2016 |
20160166562 | DISUBSTITUTED 3,4-DIAMINO-3-CYCLOBUTENE-1,2-DIONE COMPOUNDS FOR USE IN THE TREATMENT OF CHEMOKINE-MEDIATED DISEASES | 06-16-2016 |
20160168119 | AUTOTAXIN INHIBITORS | 06-16-2016 |
20160176817 | GLYOXAMIDE SUBSTITUTED PYRROLAMIDE DERIVATIVES AND THE USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF HEPATITIS B | 06-23-2016 |
20160176843 | SUBSTITUTED AMINO TRIAZOLES USEFUL AS ACIDIC MAMMALIAN CHITINASE INHIBITORS | 06-23-2016 |
20160176854 | Imidazolecarboxamides and Their Use as FAAH Inhibitors | 06-23-2016 |
20160198713 | Malonic ester derivatives of heteroarylpiperidines and -piperazines as fungicides | 07-14-2016 |
20160251344 | Novel crystalline form of 2-piperidin-4-yl)-1,3-thiazol-4-yl]-4,5-dihydro-1,2-oxazol-5-yl}-3-chloro- phenylmethanesulphonate | 09-01-2016 |
20180021324 | ILOPERIDONE FOR THE TREATMENT OF SCHIZOPHRENIA | 01-25-2018 |
20220135554 | NOVEL (CYANO-DIMETHYL-METHYL)-ISOXAZOLES AND -[1,3,4]THIADIAZOLES - This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions. | 05-05-2022 |