Entries |
Document | Title | Date |
20080227823 | AMIDE 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 both a diamide and aromatic functionality are disclosed of the general formula (1) where X | 09-18-2008 |
20080255201 | PPAR ACTIVE COMPOUNDS - Compounds are described that are active on at least one of PPARα, PPARδ, and PPARγ, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPARα, PPARδ, and PPARγ. | 10-16-2008 |
20080287504 | CB1 MODULATOR COMPOUNDS - Novel compounds of structural formula (I) are disclosed. As modulators of the Cannabinoid-1 (CB1) receptor, these compounds are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. As such, compounds of the present invention are useful as in the treatment, prevention and suppression of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders (e.g., multiple sclerosis, Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis), cerebral vascular accidents, head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith. | 11-20-2008 |
20080293774 | Treatment of the Symptoms of Bladder Irritation - Use of a compound corresponding to formula (I), for obtaining a medicinal product for use in the treatment of the symptoms of bladder irritation. | 11-27-2008 |
20080312285 | Substituted Indazoles as Inhibitors of Phosphodiesterase Type-Iv - The present invention relates to isoxazoline derivatives of structure Ia, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. Compounds disclosed herein can be useful in the treatment of CNS disorders, AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases especially in humans. Processes for the preparation of disclosed compounds are provided, as well as pharmaceutical compositions containing the disclosed compounds, and their use as phosphodiesterase (PDE) type IV inhibitors. Formula (Ia) | 12-18-2008 |
20090018170 | 5-LIPOXYGENASE-ACTIVATING PROTEIN (FLAP) INHIBITORS - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases. | 01-15-2009 |
20090036495 | Combinations Comprising Alpha-2-Delta Ligands and Ep4 Receptor Antagonists - The instant invention relates to a combination of an EP4-receptor antagonist and an alpha-2-delta ligand, and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof and their use in the treatment of pain, particularly inflammatory, neuropathic, visceral and nociceptive pain. | 02-05-2009 |
20090042949 | Indoles Useful in the Treatment of Inflammation - There is provided compounds of formula I, | 02-12-2009 |
20090048303 | Indole-2-carboxamidine derivatives as nmda receptor antago - The present invention relates therefore first to new indole-2-carboxamidine derivatives of formula (I)—wherein the meaning of X is hydrogen or halogen atom, C | 02-19-2009 |
20090048304 | Crystal Form of Besipirdine Chlorhydrate, Process Preparation and Use Thereof - Crystal form of besipirdine chlorhydrate (Form I) corresponding to the Formula (A) below: the aforementioned form being characterized at least by one of the following physico-chemical properties: a) In FTIR, it displays at least the following absorption bands of the infrared spectrum: 778, 1198, 1121, but not the following absorption bands of the infrared spectrum: 3395, 1583, 732, the aforementioned bands being expressed in cm | 02-19-2009 |
20090062348 | Antifungal Agent Containing Pyridine Derivative - The present invention provides an antifungal agent that has superior antifungal action and is also superior in terms of physical properties, safety and metabolic stability. The present invention discloses a compound represented by the formula (I): | 03-05-2009 |
20090118334 | METHOD OF TREATMENT OF CARDIAC AND/OR RENAL FAILURE USING A CALCIUM CHANNEL BLOCKER AND AN ANGIOTENSIN CONVERTING ENZYME INHIBITOR OR AN ANGIOTENSIN II RECEPTOR BLOCKER - A pharmaceutical composition including a calcium channel blocker and an angiotensin II receptor blocker or an angiotensin converting enzyme inhibitor. Also disclosed is a method of treating cardiovascular disease or renal disease by identifying a patient in need of such treatment, and administering a pharmaceutical composition disclosed herein to said patient. | 05-07-2009 |
20090137635 | DERIVATIVES OF 5-AMINO-4,6-DISUBSTITUTED INDOLE AND 5-AMINO-4,6-DISUBSTITUTED INDOLINE AS POTASSIUM CHANNEL MODULATORS - This invention provides compounds of formula I | 05-28-2009 |
20090143439 | NEW PYRIDINES AS FBPASE INHIBITORS FOR TREATMENT OF DIABETES - Compounds of formula (I) | 06-04-2009 |
20090149504 | Novel 5-Substituted Indole Derivatives As Dipeptidyl Peptidase IV (DPP-IV) Inhibitors - The present invention relates to 5-substituted indole derivatives of formula (I): having inhibitory potential of dipeptidyl peptidase IV (DPP IV) enzyme where x and R | 06-11-2009 |
20090149505 | Metabotropic Glutamate Receptor-Potentiating Isoindolones - Compounds of Formula I: | 06-11-2009 |
20090170906 | HCV INHIBITORS - The present invention relates to compounds that are useful in the treatment of viruses belonging to Flaviviridae, including flaviviruses, pestiviruses, and hepaciviruses. The invention includes compounds useful for the treatment or prophylaxis of dengue fever, yellow fever, West Nile virus, and HCV. | 07-02-2009 |
20090176840 | USE OF GALR3 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF DEPRESSION AND/OR ANXIETY AND COMPOUNDS USEFUL IN SUCH METHODS - This invention is directed to indolone derivatives which are antagonists or the GALR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. | 07-09-2009 |
20090176841 | NOVEL 6-5 SYSTEM BICYCLIC HETEROCYCLIC DERIVATIVE AND ITS PHARMACEUTICAL UTILITY - An object of the present invention is to provide a medicament as a thyroid hormone receptor ligand which is sufficient in drug efficacy and safety, and has the excellent action as a drug. The present invention provides a compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: | 07-09-2009 |
20090186922 | 2-ARYLINDOLE DERIVATIVES AS NPGES-I INHIBITORS - A 2-arylindole compound substituted in position 5, of formula (I): in which X, Y, Z, W, A, R and R′ have the meanings given in the description, a pharmaceutical composition comprising it, and also intermediate compounds and a preparation process therefor. | 07-23-2009 |
20090186923 | Compounds Having CRTH2 Antagonist Activity - Compounds of general formula (I) | 07-23-2009 |
20090209594 | METHOD OF TREATING OF DEMYELINATING DISEASES OR CONDITIONS - N-(Pyridinyl)-1H-indol-1-amines of formula I provide a unique combination of blocking properties for both the potassium and sodium channels. These compounds are useful for the treatment of Demyelinating Diseases and Conditions such as Multiple Sclerosis, Spinal Cord Injury, Traumatic Brain Injury and Stroke. The compounds are also useful for Stroke Rehabilitation, the treatment of Bladder Irritation and Dysfunction, and the treatment of Neuropathic Pain and Chemokine-Induced Pain. | 08-20-2009 |
20090209595 | METHOD OF TREATING OF DEMYELINATING DISEASES OR CONDITIONS - N-(Pyridinyl)-1H-indol-1-amines of formula I provide a unique combination of blocking properties for both the potassium and sodium channels. These compounds are useful for the treatment of Demyelinating Diseases and Conditions such as Multiple Sclerosis, Spinal Cord Injury, Traumatic Brain Injury and Stroke. The compounds are also useful for Stroke Rehabilitation, the treatment of Bladder Irritation and Dysfunction, and the treatment of Neuropathic Pain and Chemokine-Induced Pain. | 08-20-2009 |
20090270458 | METHOD OF TREATING OF DEMYELINATING DISEASES OR CONDITIONS - N-(Pyridinyl)-1H-indol-1-amines of formula I provide a unique combination of blocking properties for both the potassium and sodium channels. These compounds are useful for the treatment of Demyelinating Diseases and Conditions such as Multiple Sclerosis, Spinal Cord Injury, Traumatic Brain Injury and Stroke. The compounds are also useful for Stroke Rehabilitation, the treatment of Bladder Irritation and Dysfunction, and the treatment of Neuropathic Pain and Chemokine-Induced Pain. | 10-29-2009 |
20090270459 | Flea control agent containing N-Substituted indole derivative - Conventional control agents against fleas parasitic on animals do not have sufficient selective toxicity and are hence not safe for the animals to which the control agents are applied. The control agents are not always satisfactory also in control effect and quick-acting properties. Intensive studies were made on the insecticidal activity of N-substituted indole compounds against fleas and on the safety thereof for mammals including pets. As a result, it was found that an N-substituted indole derivative, e.g., 1-(3-chloro-5-trifluoromethylpyridin 2-yl)-3-(dichlorofluoromethylthio)indole, 1-(2,6-dichloro-4-trifluoromethylphenyl)-3-(dichlorofluoromethylthio)-indole, or 1-(2,6-dichloro-4-trifluoromethylphenyl)-3-(trifluoromethylthio)indole, has high insecticidal activity and quick-acting properties and is lowly toxic to mammals including pets. | 10-29-2009 |
20090275616 | STRAIGHTFORWARD ENTRY TO 7-AZABICYCLO[2.2.1]HEPTANE-1-CARBONITRILES AND SUBSEQUENT SYNTHESIS OF EPIBATIDINE ANALOGUES - The present invention relates to a group of substituted-7-azabicyclo-[2.2.1]heptyl derivatives with biological activity. The present invention also relates to synthetic methods for producing said substituted-7-azabicyclo-[2.2.1]heptyl derivatives. The present invention also relates to certain intermediates for producing such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as a synthetic method for producing such intermediates. The present invention also relates to pharmaceutical compositions comprising such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as their use as medicaments for the treatment of diseases mediated by a Nicotinic Acetylcholine Receptor or a receptor being a member of the Neurotransmitter-gated Ion Channel Superfamily, such as pain, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy and nicotine addiction. | 11-05-2009 |
20090281147 | METHOD OF TREATING OF DEMYELINATING DISEASES OR CONDITIONS - N-(Pyridinyl)-1H-indol-1-amines of formula I provide a unique combination of blocking properties for both the potassium and sodium channels. These compounds are useful for the treatment of Demyelinating Diseases and Conditions such as Multiple Sclerosis, Spinal Cord Injury, Traumatic Brain Injury and Stroke. The compounds are also useful for Stroke Rehabilitation, the treatment of Bladder Irritation and Dysfunction, and the treatment of Neuropathic Pain and Chemokine-Induced Pain. | 11-12-2009 |
20090291982 | New Substituted Oxindole Derivative 352 - The present invention relates to a new compound of formula (I) | 11-26-2009 |
20090291983 | 3-Oxoisoindoline-1-Carboxamide Derivatives as Analgesic Agents - Compounds of formula I | 11-26-2009 |
20090298886 | 2-INDOLINONE DERIVATIVES AS MULTI-TARGET PROTEIN KINASE INHIBITORS AND HISTONE DEACETYLASE INHIBITORS - The present invention relates to 2-indolinone derivatives which are capable of inhibiting protein kinases and histone deacetylases. The compounds of this invention are therefore useful in treating diseases associated with abnormal protein kinase activities or abnormal histone deacetylase activities. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing these compounds are also disclosed. | 12-03-2009 |
20090306144 | PYRIDINE DERIVATIVES OF ALKYL OXINDOLES AS 5-HT7 RECEPTOR ACTIVE AGENTS - New 3,3-disubstituted indol-2-one derivatives of the general formula (I) | 12-10-2009 |
20090318504 | Use of GAL3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods - This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety. This invention also provides a method of treating depression and/or anxiety in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist. | 12-24-2009 |
20090326011 | AZAB I CYCLO [3 . 1 . 0] HEXANE DERIVATIVES AS DOPAMIN D3 RECEPTOR MODULATORS - Disclosed herein are compounds of formula (I) | 12-31-2009 |
20100016371 | Indole Compounds - The present application relates to compounds of formula (I) or a pharmaceutically acceptable derivative thereof; wherein X, R | 01-21-2010 |
20100016372 | Benzimidazole Derivatives - Novel compounds of the formula I (I), in which R | 01-21-2010 |
20100063102 | TREATMENT OF FAECAL INCONTINENCE - Use of a compound corresponding to formula (I) in which R represents hydrogen or a group chosen from alkyl, alkylene, alkylidyne, cycloalkyl, cycloalkylene, cycloalkylidyne and —CONH2 groups, and the —COR′ and —COOR′ groups, in which R′ is chosen from alkyl, alkylene, alkylidyne, cycloalkyl, cycloalkylene and cycloalkylidyne groups, it being possible for said groups R and/or R′ to be substituted and/or interrupted with -0-, —COO—, —OCO—, —NHCO— or —CONH— functions, or a pharmaceutically acceptable salt of said compound, for obtaining a medicament for use in the treatment of faecal incontinence. | 03-11-2010 |
20100063103 | Compounds Having CRTH2 Antagonist Activity - Compounds of general formula (I) | 03-11-2010 |
20100093807 | SUBSTITUTED 7-AZABICYCLO[2.2.1]HEPTYL DERIVATIVES USEFUL FOR MAKING PHARMACEUTICAL COMPOSITIONS - This invention provides 1-substituted-7-azabicyclo[2.2.1]heptyl derivatives, intermediates and methods for producing them, which are therapeutic agents useful for the prevention and treatment of central nervous system disorders and diseases mediated by a Nicotinic Acetylcholine Receptor such as Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy, pain, nicotine addiction and dementia. | 04-15-2010 |
20100130557 | SUBSTITUTED ARYLSULPHONYLGLYCINES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS - The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim | 05-27-2010 |
20100130558 | NOVEL SUBSTITUTED OCTAHYDROCYCLOPENTA[C]PYRROL-4-AMINES AS CALCIUM CHANNEL BLOCKERS - The present application relates to calcium channel inhibitors containing compounds of formula (I) | 05-27-2010 |
20100168182 | COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly TrkA, TrkB, TrkC, PDGFR and c-kit. | 07-01-2010 |
20100184808 | 3-AZA-BICYCLO[3.3.0]OCTANE COMPOUNDS - The invention relates to 3-aza-bicyclo[3.3.0]octane derivatives of the formula (I) wherein R | 07-22-2010 |
20100190830 | (3-Amino-1,2,3,4-Tetrahydro-9H-Carbazol-9-yl)-Acetic Acid Derivatives - The present invention relates to (3-amino-1,2,3,4-tetrahydro-9H-carbazol-9-yl)-acetic acid derivatives of Formula (I) wherein R | 07-29-2010 |
20100227892 | Compounds, Compositions and Methods for Treatment and Prevention of Orthopoxvirus Infections and Associated Diseases - Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus. | 09-09-2010 |
20100286210 | Carbazole derivative, solvate thereof, or pharmaceutically acceptable salt thereof - An object of the present invention is to provide novel carbazole derivatives, solvates thereof, or pharmaceutically acceptable salts thereof having an excellent adipose tissue weight reducing effect, hypoglycemic effect, and hypolipidemic effect, which are useful as a preventive and/or therapeutic agent for fatty liver, obesity, lipid metabolism abnormality, visceral adiposity, diabetes, hyperlipemia, impaired glucose tolerance, hypertension, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and the like. | 11-11-2010 |
20110009456 | Compounds, Compositions and Methods for Treatment and Prevention of Orthopoxvirus Infections and Associated Diseases - Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus. | 01-13-2011 |
20110015235 | NOVEL PHENYLETHYNYL DERIVATIVES OF 8-AZA-BICYCLO[3.2.1]OCTANE AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - This invention relates to novel phenylethynyl derivatives of 8-aza-bicyclo[3.2.1]octane 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. | 01-20-2011 |
20110021572 | FUNGICIDE HYDROXIMOYL-TETRAZOLE DERIVATIVES - The present invention relates to hydroximoyl-tetrazole derivatives, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. | 01-27-2011 |
20110028519 | SMALL MOLECULE INSULIN MIMETICS ABSENT QUINONES - Compounds of Formula I are described | 02-03-2011 |
20110034515 | INDOLE MODULATORS OF THE ALPHA 7 NICOTINIC ACETYLCHOLINE RECEPTOR - This invention relates to modulation of the α7 nicotinic acetylcholine receptor (nAChR) by a compound of formula (I) or a salt thereof | 02-10-2011 |
20110060009 | Hydroxamate-Based Inhibitors of Deacetylases - The present teachings relate to compounds of Formula I: | 03-10-2011 |
20110060010 | SALTS OF 3-(4-AMINO-1-OXO-1,3-DIHYDRO-ISOINDOL-2-YL)PIPERIDINE-2,6-DIONE AND DERIVATIVES THEREOF, OR POLYMORPHS OF SALTS, PROCESS FOR PREPARING SAME AND USE THEREOF - The present invention provides a pharmaceutically acceptable strong acid salt of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione, a solvate thereof, a process for preparing the same and use in the preparation of a medicament for treating diseases or physiological abnormities by inhibiting inflammatory factors or angiogenesis. The water-solubility of the pharmaceutically acceptable strong acid salts of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione is quite higher than that of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione. The present invention also provides polymorphs of a pharmaceutically acceptable strong acid salt of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione and a solvate thereof. | 03-10-2011 |
20110071195 | NOVEL ALKENE OXINDOLE DERIVATIVES - The present invention provides compounds of formula (I), | 03-24-2011 |
20110086885 | Indole-2-carboxylic acid amides - Compounds represented by Formula (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants. | 04-14-2011 |
20110112148 | INDOLINE COMPOUNDS - This invention provides new 2,3-dihydro-indole compounds, their use for the treatment or prevention of melatonin-ergic disorders and its compositions. | 05-12-2011 |
20110118318 | DERIVATIVES OF 5-AMINO-4,6-DISUBSTITUTED INDOLE AND 5-AMINO-4,6-DISUBSTITUTED INDOLINE AS POTASSIUM CHANNEL MODULATORS - This invention provides compounds of formula I | 05-19-2011 |
20110184025 | Methods and Compositions Using Immunomodulatory Compounds for the Treatment and Management of Spirochete and Other Obligate Intracellular Bacterial Diseases - Methods of treating, preventing and/or managing a spirochete and/or other obligate intracellular bacterial disease or disorder are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active agent. | 07-28-2011 |
20110230524 | SUBSTITUTED 2-(5-HYDROXY-2-METHYL-1H-INDOLE-3-YL)ACETIC ACIDS AND ETHERS THEREOF AND THE USE OF SAME TO TREAT VIRAL DISEASES - The present invention relates to novel substituted 2-(5-hydroxy-2-methyl-1H-indol-3-yl)acetic acids, to novel antiviral active ingredients, pharmaceutical compositions, antiviral medicaments, methods for prophylaxis and treatment of viral diseases particularly caused by influenza viruses and infectious hepatisis C (HCV) viruses. | 09-22-2011 |
20110275677 | INDOLE COMPOUNDS BEARING ARYL OR HETEROARYL GROUPS HAVING SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR BIOLOGICAL ACTIVITY - The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as sphingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors. | 11-10-2011 |
20110301202 | SPLA2 INHIBITOR CONJUGATE COMPOUNDS AND METHODS OF USE - The present application provides a novel set of compounds comprising a sPLA | 12-08-2011 |
20110301203 | CHEMICAL COMPOUNDS - This invention relates to non-steroidal compounds that are modulators of androgen receptor, and also to the methods for the making and use of such compounds. | 12-08-2011 |
20110306642 | 3-AZABICYCLO[3.1.0]HEXYL DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved. | 12-15-2011 |
20110319451 | 5-Ht6 Receptor and Modulators Thereof for the Treatment of Insulin-Related Disorders - The present invention relates to a method for identifying a glycemic stabilizing compound, by: a) contacting a candidate compound with a 5-HT | 12-29-2011 |
20120029027 | N-[(6-AZA-BICYCLO[3.2.1]OCT-5-YL)-ARYL-METHYL]-HETEROBENZAMIDE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE OF SAME - The invention relates to a compound of the general formula (I), where: R is a hydrogen atom or a group selected from the (C | 02-02-2012 |
20120101132 | New Substituted Oxindole Derivative - The present invention relates to a new compound of formula (I) | 04-26-2012 |
20120172400 | SULFONAMIDES WITH HETEROCYCLE AND OXADIAZOLONE HEADGROUP, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS - The invention relates to Sulfonamides with heterocycle and oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula (I), in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system. | 07-05-2012 |
20120184582 | NOVEL COMPOUNDS EFFECTIVE AS XANTHINE OXIDASE INHIBITORS, METHOD FOR PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME - The present invention relates to novel compounds which are effective as an inhibitor for xanthine oxidase, a process for preparing the same, and a pharmaceutical composition comprising a therapeutically effective amount of the same. | 07-19-2012 |
20120309794 | COMPOUNDS INHIBITORS OF ENZYME LACTATE DEHYDROGENASE (LDH) AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS - The present invention concerns compounds, some of which are novel, and their pharmaceutical applications. The compounds of the invention inhibit the enzyme lactate dehydrogenase (LDH) involved both in the metabolic process of hypoxic tumour cells, and in the process used by parasitic protozoa that cause malaria to obtain most of the energy they need. | 12-06-2012 |
20120322831 | COMPOSITIONS FOR REDUCING AB 42 PRODUCTION AND THEIR USE IN TREATING ALZHEIMER'S DISEASE (AD) - Novel small molecule compounds for reduction of Aβ 42 production and for treatment of Alzheimer's Disease and other neurodegenerative disorders, methods of making them and pharmaceutical compositions containing them are described. | 12-20-2012 |
20130012545 | Amido-Thiophene Compounds and Their Use - The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc. | 01-10-2013 |
20130030023 | ORALLY BIOAVAILABLE DABIGATRAN PRODRUGS FOR THE TREATMENT OF DISEASES - The present invention relates to prodrug derivatives of dabigatran, their use in the treatment and/or prophylaxis of diseases, in particular thrombotic diseases, stroke, cardiac infarction and/or atrial fibrillation and cardiac arrhythmia, as well as oncological diseases of any pathogenesis. | 01-31-2013 |
20130059892 | Compositions and Methods for Cancer Detection and Treatment - Disclosed herein are compositions and methods for cancer detection and treatment. Compounds that inhibit PRMT5 are contemplated, as are pharmaceutical compositions comprising a therapeutically effective amount of at least one PRMT5 inhibitor. In some embodiments pharmaceutical compositions further comprising at least one HDAC inhibitor are contemplated. Methods of treating disorders in a mammal by inhibiting PRMT5 by administering to a mammal, a therapeutically effective amount of a PRMT5 inhibitor are also disclosed. | 03-07-2013 |
20130131114 | NOVEL ALKENE OXINDOLE DERIVATIVES - The present invention provides compounds of formula (I), | 05-23-2013 |
20130137728 | Compositions and Methods for the Treatment of Degenerative Diseases - Disclosed are compounds or pharmaceutically acceptable salts thereof, having the structure of formula I. Also disclosed are methods of preventing and/or treating degenerative disease in a subject, comprising administering to said subject a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions for preventing and/or treating de-generative disease in a subject comprising a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof. | 05-30-2013 |
20130172390 | Haloalkyl-Substituted Amides as Insecticides and Acaricides - The present invention relates to halogen-substituted amide derivatives of the general formula (I) | 07-04-2013 |
20130225637 | ISATIN DERIVATIVES, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USE THEREOF - One aspect of the invention relates to novel isatin derivative compounds and the pharmaceutical composition thereof. Another aspect of the invention relates to methods of using the isatin derivative compounds disclosed herein and the pharmaceutical compositions thereof. In certain embodiments, the method is used to treat a cancer or a tumor in a subject including, without limitation, prostate cancer, melanoma, pancreatic cancer, ovarian cancer, and lymphoma. In certain embodiment, the method is used to treat a condition in a subject that can be regulated by the activation of one or more proteins such as EGFR, Erk1/2, Her2/Neu, Jak2, Src, Stat3, Akt, Cyclin B1, and Cdc25C. In certain embodiment, the method is used to treat a condition in a subject that can be regulated by the disruption of microtubule formations. | 08-29-2013 |
20130274294 | 4-(Hetero)Aryl-Ethynyl-Octahydro-Indole-1-Esters - The invention relates to compound of the formula (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it. | 10-17-2013 |
20140039012 | Compounds Having CRTH2 Antagonist Activity - Compounds of general formula (II) | 02-06-2014 |
20140194471 | SUBSTITUTED 1-BENZYLINDOLIN-2-ONE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF MUSCARINIC ACETYLCHOLINE M1 RECEPTORS - In one aspect, the invention relates to substituted 1-benzylindolin-2-one analog compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M | 07-10-2014 |
20140194472 | VITAMIN D RECEPTOR-COREGULATOR INHIBITORS - Described herein are compounds, pharmaceutical compositions and methods for inhibiting the expression of a vitamin D receptor target gene, inhibiting interactions between the vitamin D receptor and at least one vitamin D receptor coactivator, for treating cancer in a subject, and for inhibiting angiogenesis in a subject. | 07-10-2014 |
20140213615 | Materials and Methods Useful to Induce Vacuolization, Cell Death, or a Combination Thereof - The present invention provides materials and methods to induce cell death by methuosis, a non-apoptotic cell death mechanism, to induce vacuolization without cell death, or to induce cell death without vacuolization. Small molecules herein are useful for treating cell proliferation disorders or anomalies, particularly, but not exclusively, cancer. Methods related to the research and pharmaceutical use of the small molecules are also provided herein. | 07-31-2014 |
20140221431 | NOVEL HISTONE DEACETYLASE INHIBITOR OF BENZAMIDES AND USE THEREOF - Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumours, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof. | 08-07-2014 |
20140288126 | ORGANIC COMPOUNDS - The present invention provides novel organic compounds of Formula (I): methods of use, and pharmaceutical compositions thereof. | 09-25-2014 |
20140288127 | Novel Alkene Oxindole Derivatives - The present invention provides compounds of formula (I), | 09-25-2014 |
20140315956 | SMALL MOLECULE INHIBITORS OF IL-6 AND USES THEREOF - In one aspect, the invention relates to substituted 2-(1H-indol-3-yl)ethanol analogs and substituted 3,3a,8,8a-tetrahydro-2H-furo[2,3-b]indole analogs, derivatives thereof, and related compounds, which are useful as inhibitors of IL-6 mediated activation of the Jak2/STAT3 pathway; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a IL6 dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 10-23-2014 |
20140357674 | NICOTINIC RECEPTOR COMPOUNDS - Compounds and compositions for promoting smoking cessation or decreasing tobacco use or nicotine addiction are provided. The compounds are 2′-fluoro-3′-(substituted phenyl) deschloroepibatidine analogs. The compounds have been found to modulate neuronal nicotine acetylcholine receptors and are useful in methods for the treatment of conditions or disorders influenced by the modulation of neuronal nicotinic acetylcholine receptors. | 12-04-2014 |
20140364457 | COMPOSITIONS FOR REDUCING AB 42 PRODUCTION AND THEIR USE IN TREATING ALZHEIMER'S DISEASE (AD) - Novel small molecule compounds for reduction of Aβ 42 production and for treatment of Alzheimer's disease and other neurodegenerative disorders, methods of making them and pharmaceutical compositions containing them are described. | 12-11-2014 |
20150045395 | METHOD OF USING AN INDOLINONE MOLECULE AND DERIVATIVES FOR INHIBITING LIVER FIBROSIS AND HEPATITIS - This invention relates to methods of reversing and inhibiting liver fibrosis and hepatitis using a small indolinone molecule Hesperadin and related compounds. Methods of identifying such agents and using them to inhibit the expression of collagens and ECM proteins including MMPs and TIMPs in purified hepatic stellate cells are provided. In vivo data of Hesperadin in inhibiting induced collagen production are presented. This method of specifically targeting drugs to hepatic stellate cells in vivo, provides a novel therapy for liver diseases. | 02-12-2015 |
20150133505 | Arylethynyl derivatives - The present invention relates to ethynyl derivatives of formula I | 05-14-2015 |
20150307502 | NICOTINIC RECEPTOR COMPOUNDS - Compounds and compositions for promoting smoking cessation or decreasing tobacco use or nicotine addiction are provided. The compounds are 2′-fluoro-3′-(substituted phenyl) deschloroepibatidine analogs. The compounds have been found to modulate neuronal nicotine acetylcholine receptors and are useful in methods for the treatment of conditions or disorders influenced by the modulation of neuronal nicotinic acetylcholine receptors. | 10-29-2015 |
20160039761 | HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF E1 ACTIVATING ENZYMES - This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia. | 02-11-2016 |
20160039787 | Arylethynyl derivatives - The present invention relates to ethynyl derivatives of formula I | 02-11-2016 |
20160046614 | AUTOTAXIN INHIBITOR COMPOUNDS - Described herein are compounds that are autotaxin inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with autotaxin activity. | 02-18-2016 |
20160058745 | CASEIN KINASE 1DELTA (CK 1DELTA) INHIBITORS - The invention relates to pharmaceutical compositions having casein kinase 1 delta (CK1δ) inhibitors and to the use of the inhibitors in the treatment of neurodegenerative disorders such as Alzheimer's disease. | 03-03-2016 |
20160083363 | Substituted Indoles as Selective Protease Activated Receptor 4 (PAR-4) Antagonists - Embodiments of the invention include substituted indole compounds and compositions thereof to inhibit protease activated receptor-4. Also described are methods of preparation of compositions and methods for treating diseases related to thrombotic disorders by administration of the composition. | 03-24-2016 |
20160152598 | NITROGEN-CONTAINING HETEROCYCLIC COMPOUND | 06-02-2016 |
20160185721 | INDOLE-CARBOXAMIDES - The present invention relates to compounds of general formula | 06-30-2016 |
20160374991 | AUTOTAXIN INHIBITOR COMPOUNDS - Described herein are compounds that are autotaxin inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with autotaxin activity. | 12-29-2016 |