Entries |
Document | Title | Date |
20080200499 | Selective Insecticides and/or Acaricides Based on Substituted Cyclic Dicarbonyl Compounds and Safeners - The present invention relates to the use of selective insecticidal and/or acaricidal compositions, characterized in that they comprise an effective amount of an active compound combination comprising
| 08-21-2008 |
20080200500 | Quinoline Derivatives as Nk3 Antagonists - Compounds of Formula I | 08-21-2008 |
20080200501 | NOVEL CANNABINOID RECEPTOR LIGANDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND PROCESSES FOR THEIR PREPARATION - The present invention relates to novel cannabinoid receptor modulators, in particular cannabinoid 1 (CB1) or cannabinoid 2 (CB2) receptor modulators, and uses thereof for treating diseases, conditions and/or disorders modulated by a cannabinoid receptor (such as pain, neurodegenative disorders, eating disorders, weight loss or control, and obesity). | 08-21-2008 |
20080214603 | 5-Ht7 Receptor Antagonists - The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some tetrahydroisoquinoline substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT is involved, such as CNS disorders. | 09-04-2008 |
20080221156 | STABLE FORMULATIONS OF ACE INHIBITORS, AND METHODS FOR PREPARATION THEREOF - The present invention provides stable formulations of ACE inhibitors, especially enalapril maleate, that can be manufactured in a time efficient, cost effective manner. Such formulations can be prepared simply and on a large industrial scale. The present invention also provides methods for the preparation of stable formulations of ACE inhibitors, especially enalapril maleate. | 09-11-2008 |
20080234317 | METHODS FOR THE IMPROVEMENT OF MEMORY AND NEUROLOGICAL FUNCTION COMPRISING THE ADMINISTRATION OF COMPOSITIONS THAT ACT AS INHIBITORS OF THE SODIUM PROTON (NA+ /H+ ) EXCHANGER, SUBTYPE 5 (NHE-5) - The present invention comprises the use of pharmaceutical compositions that are effective in the inhibition of the Na | 09-25-2008 |
20080242698 | Organic Compounds - The invention relates to novel diamines of the formula | 10-02-2008 |
20080255188 | Muscarinic Receptor Antagonists - This present invention generally relates to muscarinic receptor antagonists of Formula (I), which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors. | 10-16-2008 |
20080262032 | Isoxazoline Derivative and Novel Process for Its Preparation - The present invention relates to an isoxazoline derivative having the cyclic carboxylic acid hemiketal moiety of formula (1) for use as caspase inhibitor, a process for preparing it, and a pharmaceutical composition comprising it. | 10-23-2008 |
20080287488 | Use of a Sulfonamide Compound For Improving the Pharmacokinetics of a Drug - A method for improving the pharmacokinetics of drugs, which are metabolized by cytochrome P450 monooxygenase is disclosed. More specifically it relates to a method for improving the pharmacokinetics of retroviral protease inhibitors and in particular for improving the pharmacokinetics of human immunodeficiency virus (HIV) protease inhibitors. A pharmaceutical composition and its use in the manufacture of a medicament for the inhibition or treatment of an HIV infection or AIDS in a human being are also part of the invention. | 11-20-2008 |
20080287489 | Ophthalmic compositions for treating ocular hypertension - This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans. | 11-20-2008 |
20080300269 | THERAPEUTIC COMPOUNDS - Disclosed herein are compounds of the formula | 12-04-2008 |
20090012117 | Bicyclic derivatives as modulators of ion channels - Bicyclic derivatives having formula (I) and a composition thereof are useful as ion channel antagonists: | 01-08-2009 |
20090030036 | Nuclear receptor binding agents - The present invention relates to a novel class of nuclear receptor binding agents (NRBAs). The NRBAs are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, inflammatory diseases, oxidative stress related disorders such as Parkinson's and stroke, neurological disorders, ophthalamic disorders, cardiovascular disease, and obesity. | 01-29-2009 |
20090048292 | SYNERGISTIC COMBINATION - Pharmaceutical combinations comprising as compound A at least one compound from the group of angiogenesis inhibitors of general formula I | 02-19-2009 |
20090054481 | Saquinavir Mesylate Oral Dosage Form - A solid unit oral pharmaceutical dosage form of saquinavir mesylate is provided comprising micronized saquinavir mesylate in an amount of from 250 mg to 800 mg calculated as free base, and a pharmaceutically acceptable binder, disintegrant, and water soluble carrier. A solid unit dosage form of saquinavir mesylate is provided comprising from 60% to 80% micronized saquinavir mesylate based on the mesylate salt, 4% to 8% water soluble binder, a disintegrant and a carrier, wherein each percentage is of the kernel weight. | 02-26-2009 |
20090082393 | New addition salts of angiotensin-converting enzyme inhibitors with no donor acids, a process for their preparation and pharmaceutical compositions containing them - Compounds of formula (I): | 03-26-2009 |
20090082394 | Tetrahydroisoquinoline Derivatives to Enhance Memory Function - The invention relates to the use of tetrahydroisoquinoline derivatives for the preparation of a medicament to enhance, maintain and/or restore all stages and/or types of short-, middle- and/or long-term memory. | 03-26-2009 |
20090088450 | 5-ht7 receptor antagonists - The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some tetrahydroisoquinoline propyl sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT is involved, such as CNS disorders. | 04-02-2009 |
20090099229 | Isoquinolines as IGF-1R Inhibitors - Compounds of the formula (I): | 04-16-2009 |
20090124654 | Aryl and Heteroaryl Compounds, Compositions, Methods of Use - This invention provides aryl and heteroaryl compounds of formula (X). The compounds of the invention may be useful as antagonists, or partial antagonist of factor IX and/or factor XI and thus, may be used to inhibit the intrinsic pathway of blood coagulation. Formula (X) wherein R | 05-14-2009 |
20090124655 | HETEROCYCLIC DERIVATIVES AS MODULATORS OF ION CHANNELS - The present invention relates to heterocyclic derivatives useful as inhibitors of ion 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. | 05-14-2009 |
20090143423 | SOLID DISPERSION PRODUCT CONTAINING N-ARYL UREA-BASED COMPOUND - A solid dispersion product comprising at least one N-aryl urea-based pharmaceutically active agent or an agent of related structural type is obtained by a) preparing a liquid mixture containing the at least one active agent, at least one pharmaceutically acceptable matrix-forming agent, at least one pharmaceutically acceptable surfactant and at least one solvent, and b) removing the solvent(s) from the liquid mixture to obtain the solid dispersion product. | 06-04-2009 |
20090156635 | BIARYLOXYMETHYLARENECARBOXYLIC ACIDS AS GLYCOGEN SYNTHASE ACTIVATORS - The present invention relates to compounds of formula (I) | 06-18-2009 |
20090170895 | S1P3 RECEPTOR ANTAGONIST - The present invention relates to a medicine, and more particularly to novel arylamidrazone derivatives having an antagonistic action against S1P | 07-02-2009 |
20090192188 | TETRAHYDROISOQUINOLINE DERIVATIVES - This invention relates to novel tetrahydroisoquinoline derivatives, their derivatives, pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a dual OX-1/OX-2 orexin antagonist. | 07-30-2009 |
20090197912 | Sulfonamide Derivatives for the Treatment of Diseases - The invention relates to compounds of formula (1) | 08-06-2009 |
20090203734 | F1F0-ATPASE INHIBITORS AND RELATED METHODS - The present invention relates to inhibitors of mitochondrial F | 08-13-2009 |
20090221633 | INHIBITORS OF AKT (PROTEIN KINASE B) - 4-[5-(2-Amino-ethanesulfonyl)-isoquinolin-7-yl]-phenol or a pharmaceutically acceptable salt thereof or a hydrate of the compound or the salt thereof as Akt inhibitors that are antineoplastic and/or antiviral agents as well as compositions comprising these compounds and methods of using these compounds. | 09-03-2009 |
20090247572 | AGENT FOR TREATING ATRIAL FIBRILLATION - It is intended to provide an agent for treating atrial fibrillation, comprising an I | 10-01-2009 |
20090247573 | (HETERO)ARYL CYCLOHEXANE DERIVATIVES - The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions. | 10-01-2009 |
20090247574 | 3-AMINO-PYRIDINE DERIVATIVES FOR THE TREATMENT OF METABOLIC DISORDERS - The present invention provides novel compounds represented by the general formula (I): | 10-01-2009 |
20090275607 | Tetrahydro isoquinoline derivatives, preparation methods and medicinal uses thereof - A kind of tetrahydro isoquinoline derivatives (I), their preparation methods, medicine compositions and medicinal uses thereof, especially their uses as κ-opioid receptor excitant in pain relieving, which belongs to the medicine chemistry. The substituents R | 11-05-2009 |
20090275608 | Methods of diagnosing and treating parp-mediated diseases - Disclosed are methods of identifying a disease treatable with modulators of differentially expressed genes in a disease, including at least PARP modulators, by identifying the level of expression of differentially expressed genes, including at least PARP, in a plurality of samples from a population, making a decision regarding identifying the disease treatable by modulators to the differentially expressed genes wherein the decision is made based on the level of expression of the differentially expressed genes. The method can further comprise treating the disease in a subject population with modulators of identified differentially expressed genes. The methods relate to identifying up-regulated expression of identified differentially-expressed genes in a disease and making a decision regarding the treatment of the disease. The level of expression of the differentially expressed genes in a disease can also help in determining the efficacy of the treatment with modulators to the differentially expressed genes. | 11-05-2009 |
20090275609 | Carboxamide Compounds and Methods for Using The Same - Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure | 11-05-2009 |
20090298869 | Crystalline pharmaceutical and methods of preparation and use thereof - Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention. | 12-03-2009 |
20090298870 | PODOPHYLLOTOXIN DERIVATIVES - 4-O esters of podophyllotoxin and 4′-demethylepipodophyllotoxin are provided. The compounds are 4-O esters of an alkanoic acid or substituted alkanoic acid and podophyllotoxin and 4′-demethylepipodophyllotoxin. The compounds are useful for treating cancer. | 12-03-2009 |
20090306130 | NOVEL TETRAHYDRO-ISOQUINOLINES - The present invention provides a compound selected from compounds of formula (A) as ligand binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. Compounds of formula (A) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events and heart valvular degenerative disease. Moreover, compounds of formula (A) can be used to decrease the side effects from cytotoxic cancer agents, radiation and to treat viral infections. | 12-10-2009 |
20090326006 | Benzazole Derivatives, Compositions, and Methods of Use as Beta-Secretase Inhibitors - The present invention is directed to benzazole compounds that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention of diseases in which BACE is involved, such as Alzheimer's disease. 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 BACE is involved. | 12-31-2009 |
20100022582 | Tetrahydroisoquinoline Compound and Medicinal Use Thereof - The present invention provide a tetrahydroisoquinoline compound having a superior ACAT-inhibitory activity and/or anti-oxidation action, particularly, novel compound represented by the formula (I) (wherein each symbol is as described in the specification) and a pharmaceutically acceptable salt thereof. | 01-28-2010 |
20100022583 | PYRIDINYL MODULATORS OF gamma-SECRETASE - The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, X, R | 01-28-2010 |
20100035923 | VR1 VANILLOID RECEPTOR ANTAGONISTS WITH A IONONIC SUBSTRUCTURE - The invention provides compounds of formula (I), wherein Y, R, n and X are as defined in the description, a process for their preparation and pharmaceutical compositions containing them. The compounds of formula (I) inhibit the Transient Receptor Potential Vanilloid 1 (TRPV1), which plays a pivotal role in the development of post-inflammatory analgesia, therefore they can be used as analgesic and anti-inflammatory drugs. | 02-11-2010 |
20100048617 | COMPOUNDS - The present invention relates to substituted 3-Aminopyrazole compounds of formula (I) | 02-25-2010 |
20100056566 | New substituted isoquinoline and isoquinolinone derivatives - The invention relates to 6-substituted isoquinoline and isochinolone derivatives of the formula (I) | 03-04-2010 |
20100056567 | NOVEL ALKYL SUBSTITUTED PIPERIDINE DERIVATIVES AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - This invention relates to novel alkyl substituted piperidine derivatives useful as monoamine neurotransmitter re-uptake inhibitors. 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. | 03-04-2010 |
20100076015 | Aminopyridine Derivatives - The present invention provides compounds of formula (I): | 03-25-2010 |
20100081687 | BIARYLCARBOXYARYLAMIDES AS VANILLOID-1 RECEPTOR MODULATORS - The present invention provides compounds of formula (I): wherein A and Z are as defined in the description, along with methods for preparing such derivatives and their use for the treatment of inflammatory diseases such as neuropathic pain. | 04-01-2010 |
20100087479 | Compositions 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. | 04-08-2010 |
20100093789 | SULFONAMIDE COMPOUND - A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; G | 04-15-2010 |
20100099702 | Therapeutic agent for neuropathic pain - Disclosed is a therapeutic agent for neuropathic pain having an excellent therapeutic effect on neuropathic pain which is a intractable disease. More specifically, disclosed are a therapeutic agent for neuropathic pain which comprises a peripheral benzodiazepine receptor antagonist (particularly PK 11195) as the active ingredient; a pharmaceutical composition for the treatment of neuropathic pain which comprises a peripheral benzodiazepine receptor antagonist as the active ingredient; a method for the treatment of neuropathic pain using a peripheral benzodiazepine receptor antagonist; and others. | 04-22-2010 |
20100113511 | Mono Quaternary Ammonium Salts and Methods for Modulating Neuronal Nicotinic Acetylcholine Receptors - Provided are monoquaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders. | 05-06-2010 |
20100120843 | PHARMACEUTICAL COMPOSITION FOR TREATING ALCOHOL-INDUCED LIVER INJURY COMPRISING (4S,5S)-5-FLUOROMETHYL-5-HYDROXY-4-(AMINO)-DIHYDROFURAN-2-ONE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - The present invention relates to a pharmaceutical composition for treating alcohol-induced liver injury comprising (4S,5S)-5-fluoromethyl-5-hydroxy-4-({[(5R)-5-isopropyl-3-(isoquinolin-1-yl)-4,5-dihydro-5-isoxazolyl]carbonyl}amino)-dihydrofuran-2-one or pharmaceutically acceptable salt thereof, and a use thereof. | 05-13-2010 |
20100120844 | TETRAHYDROISOQUINOLINE COMPOUND - The present invention relates a specific tetrahydroisoquinoline compound which is useful as a chemokine receptor type 3 (CCR3) antagonist, and a pharmaceutical composition comprising the same as an active ingredient. The tetrahydroisoquinoline compound of the present invention is useful for the treatment or prevention of a disease in which CCR3 participates. | 05-13-2010 |
20100120845 | ARYLOXYALKYLCARBAMATE-TYPE DERIVATIVES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS - The invention relates to a compound of formula (I): | 05-13-2010 |
20100130545 | BRIDGED SIX-MEMBERED RING COMPOUNDS - The invention relates to compounds of formula (I), wherein R | 05-27-2010 |
20100144785 | FUNGICIDE N-6-MEMBERED FUSED (HETERO) ARYL-METHYLENE-N-CYCLOALKYL CARBOXAMIDE DERIVATIVES - The present invention relates N-(aromatic, 6-membered, fused, (hetero)aryl-methylene)-N-cycloalkyl carboxamide derivatives, their thiocarboxamide or N-substituted carboximidamide analogues, all of formula (I) wherein A represents a carbo-linked 5-membered heterocyclyl group; T represents O, S, N—R | 06-10-2010 |
20100152234 | Substituted 4-(1,2,3,4-tetrahydroisoquinolin-2-yl)-4-oxobutyric acid amide as KCNQ2/3 modulators - The invention relates to substituted tetrahydroisoquinolinyl-4-oxobutyric acid amides, methods for the preparation thereof, medicinal products containing these compounds and the use of these compounds for the preparation of medicinal products. | 06-17-2010 |
20100152235 | OXADIAZOLE DERIVATIVES ACTIVE ON SPHINGOSINE-1-PHOSPHATE (S1P) - The present invention relates to a novel oxadiazole derivative having pharmacological activity, processes for its preparation, pharmaceutical compositions containing it and its use in the treatment of various disorders. | 06-17-2010 |
20100160370 | METHOD OF TREATMENT AND PHARMACEUTICAL COMPOSITIONS - The present invention relates to methods, uses, and compositions comprising the caspase inhibitor (R)-N-((2S,3S)-2-(fluoromethyl)-2-hydroxy-5-oxo-tetrahydrofuran-3-yl)-5-isopropyl-3-(isoquinolin-1-yl)-4,5-dihydroisoxazole-5-carboxamide, or a pharmaceutically acceptable salt thereof. | 06-24-2010 |
20100173936 | Compositions comprising renin-angiotensin aldosterone system inhibitors and lipoic acid compounds, and the use thereof for the treatment of renin-angiotensin aldosterone system-related disorders - Compositions are provided which can be useful in treating a renin-angiotensin aldosterone system-related disorder. These compositions include renin-angiotensin aldosterone system inhibitors and lipoic acid compounds, as well as other therapeutic agents, and are useful in treating hypertension, stroke, metabolic syndrome, or other renin-angiotensin aldosterone system-related disorders in a subject. The compositions are also useful in improving vasodilation, reducing proteinuria, and reducing insulin resistance in a subject. Pharmaceutical compositions and methods of treatment using the compositions are further provided. | 07-08-2010 |
20100190822 | Pharmaceutical Compositions As Inhibitors of Dipeptidyl Peptidase-IV (DPP-IV) - The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases. | 07-29-2010 |
20100204269 | Compounds and methods for treatment of chemotherapy-induced anemia - The invention relates to methods and compounds for treating chemotherapy-induced anemia. In particular, methods for treating chemotherapy-induced anemia in subjects refractory to treatment with recombinant human erythropoietin are encompassed herein. | 08-12-2010 |
20100216836 | 2,3-DIHYDROBENZO(1,4) DIOXIN-2-YLMETHYL DERIVATIVES AS ALPHA2C ANTAGONISTS FOR USE IN THE TREATMENT OF PERIPHERIC AND CENTRAL NERVOUS SYSTEME DISEASES - Compounds of formula I | 08-26-2010 |
20100234420 | TETRAHYDROQUINOLINE DERIVATIVES FOR TREATING POST-TRAUMATIC STRESS DISORDERS - The invention relates to methods of treating, reducing the symptoms of, or preventing a post-traumatic stress syndrome by administration of tetrahydroquinoline derivatives of formula I | 09-16-2010 |
20100273826 | METHODS OF USE AND COMPOSITIONS FOR THE DIAGNOSIS AND TREATMENT OF INFECTIOUS DISEASES - Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis. | 10-28-2010 |
20100273827 | OXADIAZOLE DERIVATIVES ACTIVE ON SPHINGOSINE-1-PHOSPHATE (S1p) - The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders. | 10-28-2010 |
20100280066 | ACYLATED AMINO ACID AMIDYL PYRAZOLES AND RELATED COMPOUNDS - This invention is directed to acylated amino acid amidyl pyrazoles and related compounds of Formula I. The invention is also directed to a pharmaceutical formation comprising such compound or in a pharmaceutically acceptable salt form thereof. The invention is further directed to a method for inhibiting β-amyloid peptide release and/or synthesis, a method for inhibiting γ-secretase activity, and a method for treating neurological disorders associated with β-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease. | 11-04-2010 |
20100286196 | NEW INHIBITOR OF DD-PEPTIDASE AND ITS USE AS ANTIBIOTIC OR ANTICANCER DRUG - A new compound is revealed and the strain of | 11-11-2010 |
20100286197 | Carboxamide Derivatives As Therapeutic Agents - This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis. | 11-11-2010 |
20100292269 | BIR DOMAIN BINDING COMPOUNDS - The present invention is directed towards an isomer, an enantiomer, a diastereoisomer, or a tautomer of a pyrrolidine compound represented by Formula I: | 11-18-2010 |
20100298373 | OXADIAZOLE DERIVATIVES ACTIVE ON SPHINGOSINE-1-PHOSPHATE (SIP) - The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders. | 11-25-2010 |
20100298374 | NITRILE DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS - Disclosed are nitrile derivatives and pharmaceutical compositions comprising nitrile derivatives. The pharmaceutical compositions comprise compounds of the formula I | 11-25-2010 |
20100311789 | 3-Substituted Propanamine Compounds - Racemic or enantiomerically enriched 3-substituted propanamine compounds represented by the following structural formula (I): | 12-09-2010 |
20110003850 | DERIVATIVES OF 4-(N-AZACYCLOALKYL) ANILIDES AS POTASSIUM CHANNEL MODULATORS - This invention provides a compound of formula IA | 01-06-2011 |
20110009446 | OLIGOMER-GUANIDINE CLASS CONJUGATES - The invention relates to (among other things) oligomer-guanidine class conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds. | 01-13-2011 |
20110039885 | METHODS FOR INCREASING ENDOTHELIAL PROGENITOR CELLS - The present invention relates to methods and compounds useful for increasing endothelial progenitor cell levels in blood and bone marrow. Methods and compounds for increasing endothelial progenitor cell mobilization are also provided. | 02-17-2011 |
20110105555 | SUBSTITUTED N-IMIDAZO[2,1-B]THIAZOLE-5-SULFONAMIDE DERIVATIVES AS 5-HT6 LIGANDS - The invention relates to compounds having pharmacological activity towards the 5-HT | 05-05-2011 |
20110124679 | 2-SUBSTITUTED-p-QUINONE DERIVATIVES FOR TREATMENT OF OXIDATIVE STRESS DISEASES - Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-substituted-p-quinone derivatives as disclosed herein. | 05-26-2011 |
20110136859 | Compounds - A compound of formula (I) | 06-09-2011 |
20110144153 | AMIDE COMPOUND - [Problems] A compound, which is useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy, is provided. | 06-16-2011 |
20110166176 | COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - 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 GPR119. | 07-07-2011 |
20110178123 | NONPEPTIDE HIV-1 PROTEASE INHIBITORS - Novel compounds and compositions for treating patients in need of relief from HIV, AIDS, and AIDS-related diseases are described. Methods for treating HIV, AIDS, and AIDS-related diseases using the compounds described herein are also described. | 07-21-2011 |
20110184017 | STABLE AQUEOUS SOLUTION COMPOSITION CONTAINING SULFONAMIDE COMPOUND - An aqueous solution composition containing (S)-1-(4-chloro-5-isoquinolinesulfonyl)-3-aminopyrrolidine or (S)-1-(4-chloro-5-isoquinolinesulfonyl)-3-(methylamino)pyrrolidine as an active ingredient, and not containing citric acid or a salt thereof, which has high stability so as to be storable at room temperature. | 07-28-2011 |
20110201643 | NOVEL N-SUBSTITUTED TETRAHYDROISOQUINOLINE/ISOINDOLINE HYDROXAMIC ACID COMPOUNDS - Compounds of a certain formula (I) wherein R1, R2, R3, X, Y, r, s, t, u and v have the meanings as defined in the specification, and the salts, solvates and hydrates thereof are novel effective HDAC 6 inhibitors. | 08-18-2011 |
20110230518 | OXADIAZOLE FUSED HETEROCYCLIC DERIVATIVES USEFUL FOR THE TREATMENT OF MULTIPLE SCLEROSIS - The invention provides compounds of Formula (I) for the treatment of multiple sclerosis and other diseases. | 09-22-2011 |
20110263641 | Isoxazolines For Controlling Invertebrate Pests - Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, | 10-27-2011 |
20120004259 | METHOD OF TREATMENT OR PROPHYLAXIS - The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT | 01-05-2012 |
20120004260 | INHIBITION OF FATTY ACID SYNTHESIS BY IODO-NITROBENZAMIDE COMPOUNDS AND METHODS OF TREATMENT THEREOF - The present invention relates to a method of treating a fatty acid synthesis related disease comprising administering to a patient in need thereof an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis, wherein the fatty acid synthesis related disease is obesity, diabetes, or cardiovascular disease. The present invention also relates to a method of treating a cancer in a subject comprising: (i) identifying a level of fatty acid in a sample from the subject, and (ii) administering an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis in the subject, wherein the administration is based on the level of fatty acid, thereby treating the cancer in the subject. The present invention further relates to a method of treating Her-2 related cancers by administering to a patient in need thereof an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis. | 01-05-2012 |
20120022101 | SALT AND SOLVATES OF A TETRAHYDROISOQUINOLINE DERIVATIVE - (S)-2-(Diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid in substantially pure form is described together with its sodium salt and solvates. Methods for preparing the compound, its sodium salt and its solvates and pharmaceutical compositions comprising them are also described. | 01-26-2012 |
20120035210 | 2,3-DIHYDROBENZO(1,4) DIOXIN-2-YLMETHYL DERIVATIVES AS ALPHA2C ANTAGONISTS FOR USE IN THE TREATMENT OF PERIPHERIC AND CENTRAL NERVOUS SYSTEME DISEASES - Compounds of formula I | 02-09-2012 |
20120035211 | NOVEL POLYMORPHS OF SAQUINAVIR - The present invention provides novel polymorphs of saquinavir, processes for their preparation and pharmaceutical compositions comprising them. The present invention also provides a process for purification of saquinavir. The present invention further provides a novel process for preparation of known saquinavir crystalline form I. | 02-09-2012 |
20120046312 | 3-SUBSTITUTED PROPANAMINE COMPOUNDS - Racemic or enantiomerically enriched 3-substituted propanamine compounds represented by the following structural formula (I): | 02-23-2012 |
20120059032 | 1,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVES EFFECTIVE AS ANTIGLIOMA AGENTS, METHODS OF MAKING, AND THEIR USE - Disclosed are tetrahydroisoquinoline-derivative compounds effective for killing cancer cells, shrinking tumor size, and treating cancer. | 03-08-2012 |
20120095040 | CYCLOPENTA[C]PYRROLE-2-CARBOXYLATE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to compounds of the general formula (I) where: R | 04-19-2012 |
20120101125 | SUBSTITUTED ISOQUINOLINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS BETA-SECRETASE INHIBITORS - The present invention is directed to substituted isoquinoline derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which BACE is involved. | 04-26-2012 |
20120129886 | 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. | 05-24-2012 |
20120142726 | PHARMACEUTICAL COMPOSITIONS COMPRISING 3,4-DIHYDROISOQUINOLIN-2(1H)-YL-3-PHENYLUREA DERIVATIVES HAVING FORMYL PEPTIDE RECEPTOR LIKE-1 (FPRL-1) AGONIST OR ANTAGONIST ACTIVITY - The present invention relates to a method of treating a disorder associated with modulation of the FPRL-1 receptor which comprises administering a therapeutically effective amount of a pharmaceutical composition comprising a 3,4-dihydroisoquinolin-2(1H)-yl-3-phenylurea derivative. | 06-07-2012 |
20120142727 | NITROGENOUS-RING ACYLGUANIDINE DERIVATIVE - [Object] An excellent agent for preventing or treating dementia, schizophrenia, and the like, based on serotonin 5-HT | 06-07-2012 |
20120245200 | CRYSTAL FORM OF QUINOLINE COMPOUND AND PROCESS FOR ITS PRODUCTION - A method for producing a drug substance of crystalline pitavastatin calcium excellent in stability, is presented. In the production of a compound (pitavastatin calcium) represented by the formula ( | 09-27-2012 |
20120270898 | SULFONAMIDE COMPOUND AND CRYSTAL THEREOF - (S)-1-(4-Chloro-5-isoquinolinesulfonyl)-3-(methylamino)pyrrolidine monohydrochloride and a crystal thereof, and a crystal of the aforementioned monohydrochloride having a major peak or peaks at one or more positions selected from the group consisting of positions where 2θs are about 13.9°, 21.5°, 21.7°, 22.4°, 22.8°, 24.5° and 35.0° in a powder X-ray diffraction spectrum, which have excellent properties as active ingredient of a medicament for prophylactic and/or therapeutic treatment of glaucoma and the like. | 10-25-2012 |
20130059882 | 8-Phenylisoquinolines And Pharmaceutical Composition Used In Treatment For Sepsis - A compound is provided. The compound includes a formula of: | 03-07-2013 |
20130059883 | COMPOUNDS AND METHODS - Disclosed are compounds having the formula: | 03-07-2013 |
20130065918 | SOLUBLE GUANYLATE CYCLASE ACTIVATORS - The present invention relates to compounds of formula (I): | 03-14-2013 |
20130085157 | ARYLSUBSTITUTED THIAZOLOTRIAZOLES AND THIAZOLOIMIDAZOLES - This disclosure relates to compounds, compositions and methods for the treatment of various disorders. In particular, the disclosure relates to thiazolotriazole and thiazoloimidazole compounds which agonize the activity of the protein TGR5. | 04-04-2013 |
20130123299 | COMPOUNDS AND METHODS FOR TREATMENT OF SYSTEMIC LUPUS ERYTHEMATOSUS - Small molecule compounds are provided for treating lupus as are methods of treating lupus using these compounds. | 05-16-2013 |
20130137718 | PROCESS FOR THE PREPARATION OF 2-(CYCLOHEXYLMETHYL)-N--1,2,3,4-TETRAHYDROISOQUINOLINE-7-SULFONAMIDE - Industrially applicable process for preparing 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide, and salts thereof. | 05-30-2013 |
20130137719 | Novel 6,7-disubstituted-sioquinoline derivatives and their use - The present invention relates compounds of general formula (I) and stereoisomers and pharmaceutically acceptable salts and prodrugs thereof; wherein R′ and R | 05-30-2013 |
20130143916 | COMPOUND LIBRARIES MADE THROUGH PHOSPHINE-CATALYZED ANNULATION/TEBBE/DIELS-ALDER REACTIONS - A method for producing libraries of structurally and stereochemically diverse molecules that can be screened for biological or chemical activity. A library of 91 heterocyclic compounds composed of 16 distinct scaffolds was synthesized through a sequence of phosphine-catalyzed ring-forming reactions, Tebbe reactions, Diels-Alder reactions, and, in some cases, hydrolysis to illustrate the methods. Three compounds inhibiting migration of human breast cancer cells are identified from the library. | 06-06-2013 |
20130172384 | FATTY ACID SYNTHASE INHIBITORS - This invention relates to the use of triazolone and triazolethione derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones and triazolethiones in the treatment of cancer. | 07-04-2013 |
20130184309 | 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. | 07-18-2013 |
20130210859 | NOVEL CORTISTATIN A ANALOG AND USE THEREOF - A compound represented by the general formula (M): | 08-15-2013 |
20130253004 | LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS AND THEIR USE IN THE TREATMENT FIBROSIS - Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases. | 09-26-2013 |
20130274285 | COMPOUNDS AND METHODS FOR INHIBITING NHE-MEDIATED ANTIPORT IN THE TREATMENT OF DISORDERS ASSOCIATED WITH FLUID RETENTION OR SALT OVERLOAD AND GASTROINTESTINAL TRACT DISORDERS - The present disclosure is directed to compounds and methods for treating irritable bowel syndrome, chronic kidney disease and end stage renal disease by administering to a subject in need thereof a compound or a pharmaceutically acceptable salt thereof, wherein the compound has the structure | 10-17-2013 |
20130281486 | 2,3-DIHYDROBENZO(1,4) DIOXIN-2-YLMETHYL DERIVATIVES AS ALPHA2C ANTAGONISTS FOR USE IN THE TREATMENT OF PERIPHERIC AND CENTRAL NERVOUS SYSTEM DISEASES - Compounds of formula I | 10-24-2013 |
20130303566 | METHOD FOR TREATING MACULAR DEGENERATION - The present invention provides a method of treating a mammal with age-related macular degeneration (AMD) comprising administering a dosage of at least one of prostaglandin E1 (PGE1), papaverine, and an alpha-1-vasodilator, in a pharmaceutically acceptable carrier for a period of time effective to deliver a dosage effective to treat said AMD. | 11-14-2013 |
20130303567 | SMALL MOLECULE INHIBITORS OF PARP ACTIVITY - Compounds and pharmaceutical compositions are provided that inhibit the activity of poly ADP-ribose synthetase (PARP). Such compounds are useful in the treatment of various diseases, conditions and injuries such as stroke, myocardial infarction, ischemia-perfusion injury in various organs, traumatic brain injury, atherosclerosis, inflammatory diseases and cancer. | 11-14-2013 |
20130310419 | PYRROLE DERIVATIVES USED AS MODULATORS OF ALPHA7 NACHR - The present invention is related to pyrrole derivatives of formula I as the modulators of nicotinic acetylcholine receptors particularly the α7 subtype. The invention includes pyrrole derivatives, analogues, their prodrugs, their isotopes, their metabolites, pharmaceutically acceptable salts, polymorphs, solvates, optical isomers, clathrates, co-crystals, combinations with suitable medicament and pharmaceutical compositions thereof. The present invention also includes process of preparation of the said compounds and intended use in therapy of them. Owing to the modulatory activity of the pyrrole derivatives on the nicotinic acetylcholine receptors, the invention finds application in the prophylaxis and therapy of disorders encompassing the involvement of cholinergic transmission in the central and peripheral nervous system. The invention relates to the ability of pyrrole derivatives to modulate the cholinergic transmission and efficacy of the endogenous neurotransmitter ACh thorough the nicotinic acetylcholine receptors particularly the α7 subtype. | 11-21-2013 |
20140031387 | LFA-1 INHIBITOR AND METHODS OF PREPARATION AND POLYMORPH THEREOF - Methods of preparation and purification of a compound of Formula I, intermediates thereof, a polymorph thereof, and related compounds are disclosed. Formulations and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed. | 01-30-2014 |
20140051722 | TOPICAL LFA-1 ANTAGONISTS FOR USE IN LOCALIZED TREATMENT OF IMMUNE RELATED DISORDERS - This invention provides specifically formulated LFA-1 antagonists or pharmaceutically acceptable salts thereof that are suitable for topical delivery. In particular, the LFA-1 antagonists are particularly well suited for localized treatment by having a rapid systemic clearance rate. The invention also encompasses methods of treatment and prevention of immune related disorders using the LFA-1 topical formulations of the present invention. | 02-20-2014 |
20140066476 | MODULATORS OF CELLULAR ADHESION - The present invention provides compounds having formula (I): | 03-06-2014 |
20140066477 | Benzazole Derivatives, Compositions, and Methods of Use as Beta-Secretase Inhibitors - The present invention is directed to benzazole compounds that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention of diseases in which BACE is involved, such as Alzheimer's disease. 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 BACE is involved. | 03-06-2014 |
20140080864 | PHARMACETUICAL COMPOSITION COMPRISING DROTAVERINE - The present invention relates to a pharmaceutical composition of drotaverine hydrochloride in a solvent system suitable as a liquid fill composition. | 03-20-2014 |
20140080865 | SALTS AND SOLVATES OF A TETRAHYDROISOQUINOLINE DERIVATIVE - (S)-2-(Diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid in substantially pure form is described together with its sodium salt and solvates. Methods for preparing the compound, its sodium salt and its solvates and pharmaceutical compositions comprising them are also described. | 03-20-2014 |
20140107152 | SENSORY RECEPTORS FOR CHRONIC FATIGUE AND PAIN AND USES - The present invention relates generally to the fields of pathological muscle pain/fatigue conditions. More specifically, the invention concerns methods and compositions useful for diagnosing and treating pathological muscle pain/fatigue conditions. | 04-17-2014 |
20140128427 | 5-CARBAMOYL-ADAMANTAN-2-YL AMIDE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AND PREPARATION PROCESS THEREOF - Provided are a novel derivative of 5-carbamoyl adamantan-2-yl amide or a pharmaceutically acceptable salt thereof, and a pharmaceutical use thereof for inhibiting the activity of 11β-hydroxystreroid dehydrogenase type 1 (11b-HSD1) or for preventing and/or treating various diseases mediated by 11β-hydroxystreroid dehydrogenase type 1. | 05-08-2014 |
20140243368 | PIPERIDINYL ALKYNE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to piperidinyl alkyne compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the piperidinyl alkyne 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. | 08-28-2014 |
20140249180 | TAU AGGREGATION INHIBITOR - A tau aggregation inhibitor reduces tau aggregation in cells. The tau aggregation inhibitor can include a catechol structure-containing compound or a salt thereof, and the catechol structure-containing compound can be one of isoprenaline, dopamine, dobutamine, levodopa, levodopa/carbidopa, trimetoquinol, hexoprenaline, methyldopa, and droxidopa. One example of the catechol structure-containing compound is isoprenaline, which can be d-enantiomer of isoprenaline or d/l-racemic mixture of isoprenaline. Tauopathies to be prevented or treated by the inhibitor include AD, Down's syndrome, Pick's disease, corticobasal degeneration, and progressive supranuclear palsy. | 09-04-2014 |
20140296286 | COMPOUNDS WITH INCREASED SPECIFICITY FOR THE TREATMENT OF GLIOMA - Disclosed are compounds for the treatment of cancer. Compounds disclosed herein are particularly effective for the selective inhibition of glioma cells. | 10-02-2014 |
20140309255 | COMPOUNDS AND METHODS FOR TREATMENT OF SYSTEMIC LUPUS ERYTHEMATOSUS - Small molecule compounds are provided for treating lupus as are methods of treating lupus using these compounds. | 10-16-2014 |
20140315946 | NONPEPTIDE HIV-1 PROTEASE INHIBITORS - Novel compounds and compositions for treating patients in need of relief from HIV, AIDS and AIDS-related diseases are described. Methods for treating HIV, AIDS, and AIDS-related diseases using the compounds described herein are also described. | 10-23-2014 |
20140323518 | NOVEL ESTROGEN RECEPTOR LIGANDS - Compounds of formula (I) or a pharmaceutically acceptable ester, amide, carbamate or salt thereof, including a salt of such an ester, amide or carbamate in which R | 10-30-2014 |
20140343093 | COMPOUNDS FOR INHIBITING THE INTERACTION OF BCL2 WITH BINDING PARTNERS - The present invention relates to compounds of formula I: in which R | 11-20-2014 |
20140357664 | 3,4-DIHYDROISOQUINOLIN-2(1H)-YL COMPOUNDS - The invention provides certain 3,4-dihydroisoquinolin-2(1H)-yl compounds, particularly compounds of formula I, and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat cognitive impairment associated with Parkinson's disease or schizophrenia. | 12-04-2014 |
20140357665 | Opsin-Binding Ligands, Compositions and Methods of Use - Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed. | 12-04-2014 |
20140357666 | COMPOUNDS FOR INHIBITING THE INTERACTION OF BCL2 WITH BINDING PARTNERS - The present invention relates to compounds of formula I: in which R | 12-04-2014 |
20140371265 | COMPOSITIONS AND METHODS FOR TREATMENT - The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists. | 12-18-2014 |
20140371266 | Mono Quaternary Ammonium Salts and Methods for Modulating Neuronal Nicotinic Acetylcholine Receptors - Provided are monoquaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and gastrointestinal tract disorders. | 12-18-2014 |
20140378506 | COMPOSITIONS AND METHODS FOR TREATMENT - The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists. | 12-25-2014 |
20150045387 | Bi-Aromatic And Tri-Aromatic Compounds As NADPH Oxidase 2 (Nox2) Inhibitors - Bi- and tri-aromatic compounds of the formula (I) wherein R1 to RIO and X are as defined, are Nox2 inhibitors that are useful as medicaments for the treatment of a disease or condition selected from: cardiovascular diseases, respiratory diseases, inflammatory diseases, cancers, ageing and age related disorders, kidney diseases, neurodegenerative diseases, diabetes and conditions associated with diabetes. The compounds, their preparation and pharmaceutical compositions comprising them are disclosed. | 02-12-2015 |
20150065538 | TRPA1 ANTAGONISTS - Compounds of formula (I) | 03-05-2015 |
20150080428 | COMPOUNDS FOR INHIBITING THE INTERACTION OF BCL2 WITH BINDING PARTNERS - The present invention relates to compounds of formula (I) in which R | 03-19-2015 |
20150105422 | SALTS AND SOLVATES OF A TETRAHYDROISOQUINOLINE DERIVATIVE - (S)-2-(Diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid in substantially pure form is described together with its sodium salt and solvates. Methods for preparing the compound, its sodium salt and its solvates and pharmaceutical compositions comprising them are also described. | 04-16-2015 |
20150111921 | CORTISTATIN ANALOGUES AND SYNTHESES THEROF - The present invention relates to analogs of cortistatin A, J, K, and L, having the general formula: I and salts thereof, wherein R | 04-23-2015 |
20150126548 | ANABOLIC COMPOUNDS FOR TREATING AND PREVENTING BONE LOSS DISEASES - There is provided compounds for treating bone loss diseases and for preventing bone loss. Specifically the present invention relates to compounds, preferable isoquinolene derivatives. | 05-07-2015 |
20150141456 | CYCLIC AMINO COMPOUNDS FOR USE IN THE TREATMENT OF CARDIAC DISORDERS - The present invention relates to tertiary amines of formula (I) for use in therapy, particularly for use in treating cardiovascular disorders. The compounds have been found to regulate phospholamban phosphorylation by interfering with the A-kinase anchor protein 18delta (AKAP18δ) binding to the PKA substrate phospholamban. The compounds share a tri(alkylaryl/alkylheteroaryl) amine structure. | 05-21-2015 |
20150315148 | MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF - Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein. | 11-05-2015 |
20150320737 | LFA-1 INHIBITOR FORMULATIONS - The present invention provides formulations, methods and kits for the treatment of dry eye diseases. In particular, stabilized pharmaceutical compositions comprising the compound of Formula 1 are described herein for a variety of uses including the treatment of dry eye syndrome. In one aspect, methods and ingredients for improving the stability of compositions of the compound of Formula 1 are described. | 11-12-2015 |
20150335634 | ISOQUINOLINE ALKALOID DERIVATIVE FOR ACTIVATING AMP-DEPENDENT PROTEIN KINASE - The present invention provides a method for activating the AMP-dependent protein kinase (AMPK) in a subject comprising administering the subject with a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound having the general Formula I, preferably salsolinol or reticuline. The pharmaceutical composition is able to activate AMPK, and thus is effective in the regulation of cell growth and metabolism, and the treatment of AMPK associated diseases. | 11-26-2015 |
20150336939 | LFA-1 INHIBITOR AND METHODS OF PREPARATION AND POLYMORPH THEREOF - Methods of preparation and purification of a compound of Formula I, intermediates thereof, a polymorph thereof, and related compounds are disclosed. Formulations and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed. | 11-26-2015 |
20150361045 | COMPOSITION AND METHOD FOR PREVENTION, MITIGATION OR TREATMENT OF AN ENTEROPATHOGENIC BACTERIAL INFECTION - Bicyclic compounds for decreasing the expression of bacterial virulence factors thereby preventing, mitigating, or treating bacterial infection are provided. | 12-17-2015 |
20150376201 | CORTISTATIN ANALOGUES AND SYNTHESES THEREOF - The present invention relates to analogs of cortistatin A, J, K, and L, having the general formula: | 12-31-2015 |
20160024059 | HETEROCYCLIC CARBOXYLIC ACIDS AS ACTIVATORS OF SOLUBLE GUANYLATE CYCLASE - The present invention relates to compounds of formula I: | 01-28-2016 |
20160031847 | GUANIDINOBENZOIC ACID ESTER COMPOUND - [Problem]To provide a compound which is useful as an agent for preventing and/or treating kidney diseases. | 02-04-2016 |
20160038476 | NONSTEROIDAL AND STEROIDAL COMPOUNDS WITH POTENT ANDROGEN RECEPTOR DOWN-REGULATION AND ANTI PROSTATE CANCER ACTIVITY - Nonsteroid and steroid compounds that cause down-regulation of the androgen receptor (AR), both full length and splice variant, induce apoptosis and inhibit proliferation of inhibiting proliferation and migration of androgen sensitive cancer cells. The steroid compounds and nonsteroid compounds may be agents for the prevention and/or treatment of cancer, including prostate cancer, castration resistant prostate cancer, bladder cancer, pancreatic cancer, hepatocellular carcinoma, benign prostatic hyperplasia (BPH), Kennedy's disease, androgenetic alopecia, breast cancer, androgen-insensitive syndrome, and spinal and bulbar muscular atrophy. | 02-11-2016 |
20160051533 | DIAGNOSIS AND PHARMACOLOGICAL TREATMENT OF SEASONAL AFFECTIVE DISORDER AND SYMPTOMS OF SEASONALITY - A method for reducing one or more symptoms associated with seasonal affective disorder and/or seasonality in symptoms of bipolar and/or premenstrual syndrome in an individual, the method including administering to the individual suffering from seasonal affective disorder and/or more generally, seasonality symptoms, a composition that comprises a therapeutically effective amount of an agent to down regulate the activity of an orexin selected from the group consisting of orexin A or orexin B, at one or more orexin receptors. | 02-25-2016 |
20160052889 | PHENOXYETHYL DIHYDRO-1H-ISOQUINOLINE COMPOUNDS - The present invention provides a compound of the Formula I: wherein R is H or F; or a pharmaceutically acceptable salt thereof. | 02-25-2016 |
20160075657 | Tetrahydroisoquinoline derivatives, pharmaceutical compositions and uses thereof - The invention relates to new pyrrolidine derivatives of the formula | 03-17-2016 |
20160101099 | H3 RECEPTOR ANTAGONIST FOR USE IN THE TREATMENT OF ALZHEIMER'S DISEASE - This disclosure relates to methods of using 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide in a disease modifying therapy of Alzheimer's disease, other tauopathies and related neurodegenerative diseases. | 04-14-2016 |
20160168100 | ANTI-HIV COMPOUNDS | 06-16-2016 |
20160176822 | HETEROCYCLIC COMPOUND | 06-23-2016 |
20170233376 | CARBOXYLIC ACID COMPOUND, METHOD FOR PREPARATION THEREOF, AND USE THEREOF | 08-17-2017 |
20180022736 | CARBOXYLIC ACID COMPOUND, METHOD FOR PREPARATION THEREOF, AND USE THEREOF | 01-25-2018 |
20220135548 | SOLID STATE FORMS OF N-[2-(2-{4-[2-(6,7-DIMETHOXY-3,4-DIHYDRO-2(1H)-ISOQUINOLINYL)ETHYL]PHENYL- }-2H-TETRAZOL-5-YL)-4,5- DIMETHOXYPHENYL]-4-OXO-4H-CHROMENE-2-CARBOXAMIDE AND OF ITS MESYLATE SALT - The present disclosure relates to solid state forms of Encequidar (previously referred to as HM-30181A) base, Encequidar ((HM-30181A) mesylate, co-crystals of Encequidar (HM-30181A) mesylate, processes for preparation thereof, as well as pharmaceutical compositions including the same. | 05-05-2022 |