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Additional hetero ring attached directly or indirectly to the 1,4-diazine ring by nonionic bonding

Subclass of:

514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514183000 - Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., O,S,Se or Te) or nitrogen as the only ring hetero atoms DOAI

514247000 - Hetero ring is six-membered consisting of two nitrogens and four carbon atoms (e.g., pyridazines, etc.)

514252100 - 1,4 diazines

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Entries
DocumentTitleDate
20120202828FUSED AMINODIHYDROPYRIMIDONE DERIVATIVES - A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C08-09-2012
20100029686HCV PROTEASE INHIBITORS AND USES THEREOF - This invention relates to: (a) compounds of formula I and salts thereof that, inter alia, are useful as hepatitis C virus (HCV) inhibitors; (b) intermediates useful for the preparation of such compounds and salts; (c) pharmaceutical compositions comprising such compounds and salts; and (d) methods of use of such compounds, salts, and compositions.02-04-2010
20100016335NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION - The present invention relates to a compound of formula I:01-21-2010
20110195978COMPOUNDS FOR TREATMENT OF ALZHEIMER'S DISEASE - Described herein are compounds, and pharmaceutical compositions, methods, and uses thereof for treating Alzheimer's disease.08-11-2011
20080269251Substituted Pyrazinone Derivatives as Alpha2C-Adrenoreceptor Antagonists - The present invention concerns substituted pyrazinone derivatives according to the general Formula (I)10-30-2008
20130085148Pyridine Derivatives - The present application provides novel pyridine compounds and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CPY17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.04-04-2013
20130210836MICROBICIDES - The present invention relates to a compound of formula (I): wherein the substituents have the definitions as defined in claim 08-15-2013
20100075989Novel Compounds Having Selective Inhibiting Effect at GSK3 - Compounds of formula I03-25-2010
20100075988TETRAHYDROQUINAZOLINE COMPOUNDS AND THEIR USE IN PREPARING MEDICAMENTS FOR TREATING AND PREVENTING VIROSIS - The present invention relates to a compound of formula (I) or isomers thereof, or pharmaceutically acceptable salts or hydrates thereof. The present invention further relates to processes for the preparation of the compounds of formula (I) and optical isomers, and to the use of the compounds of formula (I), or isomers thereof, or pharmaceutically acceptable salts or hydrates thereof as medicaments, in particular as medicaments for the treatment and prevention of Hepatitis B.03-25-2010
20100075987ACYL BIPIPERIDINYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT - Bipiperidyl compounds of the formula: (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.03-25-2010
201300409674'-DEMETHYLEPIPODOPHYLLOTOXIN DERIVATIVE, PREPARATION METHOD AND USE THEREOF - A 4′-demethylepipodophyllotoxin derivative of formula(III) having anti-tumor activity is provided. After the activation of hydroxyl in position C4 of 4′-demethylepipodophyllotoxin, tetramethylpyrazine is introduced by transamination to obtain the 4′-demethylepipodophyllotoxin derivative which is preferably used to inhibit gastric cancer line BGC-823.02-14-2013
20120264766PSEUDOBASE BENZO[C]PHENANTRIDINES WITH IMPROVED EFFICACY, STABILITY AND SAFETY - Pseudobase benzo[c]phenanthridines and the pharmaceutically acceptable salts thereof of Formula I10-18-2012
20100144756NOVEL HETEROAROMATIC DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to novel compounds of Formula (I), wherein X06-10-2010
20100144757DERIVATIVES OF 7-ALKYNYL-1,8-NAPHTHYRIDONES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS - The disclosure relates to 7-alkynyl-1,8-naphthyridones of formula (I):06-10-2010
20100041674HCV PROTEASE INHIBITORS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.02-18-2010
20090156615ORGANIC COMPOUNDS - The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.06-18-2009
20100105700DECAHYDRO-1H-INDENOQUINOLINONE AND DECAHYDRO-3H-CYCLOPENTAPHENANTHRIDINONE CYP17 INHIBITORS - Provided herein are inhibitors of CYP17 enzyme. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions.04-29-2010
20090042908AMINO-5-(6-MEMBERED)HETEROARYLIMIDAZOLONE COMPOUNDS AND THE USE THEREOF FOR BETA-SECRETASE MODULATION - The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I02-12-2009
20110009424Co-Crystals and Pharmaceutical Compositions Comprising the same - The invention relates to co-crystals and compositions each comprising VX-950 and a co-crystal former selected from the group consisting of 3-methoxy-4-hydroxybenzoic acid, 2,4-dihydroxybenzoic acid, and 2,5-dihydroxybenzoic acid. Also within the scope of this invention are methods of making and using the same.01-13-2011
20130165451COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES - The invention relates to certain compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.06-27-2013
20130059863SUBSTITUTED N-HETEROARYL SPIROLACTAM BIPYRROLIDINES, PREPARATION AND THERAPEUTIC USE THEREOF - The present disclosure relates to a series of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I).03-07-2013
20110015210Pyrazinone derivatives as insulin secretion stimulators, methods for obtaining them and use thereof for the treatment of diabetes - The present invention relates to pyrazinone derivatives of formula (I), wherein n, R1, R2, R3 and R4 are as defined in claim 01-20-2011
20090270419COMBINATIONS OF CLASS-I SPECIFIC HISTONE DEACETYLASE INHIBITORS WITH PROTEASOME INHIBITORS - The present invention is concerned with combinations of a proteasome inhibitor and a class-I specific histone deacetylase inhibitor for inhibiting the growth of tumor cells, useful in the treatment of cancer.10-29-2009
20090270417Organic Compounds - Novel 3,4-di-, 3,3,4-di-, 3,4,4,-tri- and 3,3,4,4-tetra-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula (I) wherein the substituents are as described in the specification.10-29-2009
20090270416N-OXIDES OF DIARYLUREA DERIVATIVES AND THEIR USE AS Chk1 INHIBITORS FOR THE TREATMENT OF CANCER - The invention provides a Chk-1 kinase inhibiting compound of the formula (I) or a salt, solvate or tautomer thereof, wherein: G is CH10-29-2009
20090270415COMPOUNDS THAT INHIBIT PROTEASE CATHEPSIN S AND HCV REPLICATION - The present invention is directed to compounds that have the dual property of acting as cathepsin S inhibitors and of inhibiting HCV replication. Such compounds are therefore useful in treating disease states that include hepatitis C, Alzheimer's disease, and autoimmune disorders. The present invention is also directed to pharmaceutical compositions containing these compounds, and processes for preparing the compounds.10-29-2009
20120115882SPIRO AMINO COMPOUNDS SUITABLE FOR THE TREATMENT OF INTER ALIA SLEEP DISORDERS AND DRUG ADDICTION - A spiro-amino compound of Formula (VI) wherein m is 1 or 2 or 3, n is 1 or 2, R is selected from a 5- or 6-membered aromatic ring and a 5- or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O and N, such ring being substituted with one or two substituents selected from the group consisting of (C05-10-2012
20090258884Substituted amides - Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.10-15-2009
201202385881H-Pyrrolo[2,3-B]Pyridines - Derivatives of pyrrolo[2,3-b]pyridine which are useful as SGK-1 kinase inhibitors are described herein. The invention described herein also describes pharmaceutical compositions containing derivatives of pyrrolo[2,3-b]pyridine and methods of using pyrrolo[2,3-b]pyridine derivatives and pharmaceutical compositions thereof in the treatment of diseases mediated by SGK-1.09-20-2012
20120238587NOVEL PYRIDOPYRIMIDINE DERIVATIVES AND USE THEREOF - The invention provides novel substituted pyridopyrimidines represented by Formula I or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of the phosphoinositide 3′ OH kinase family (PI3K) for the treatment of inflammatory diseases, cancer, cardiovascular diseases, allergy, asthma and autoimmune disorders.09-20-2012
20120270885CHEMICAL COMPOUNDS - The use of a compound of formula I10-25-2012
20110034481NOVEL TETRAHYDROISOQUINOLINE DERIVATIVE - The present invention relates to a compound or a pharmacologically acceptable salt thereof having an excellent DGAT inhibitory effect and feeding suppressant effect. The present invention provides a compound represented by the general formula (I), or pharmacologically acceptable salt thereof:02-10-2011
20120101109ETHANOLAMINE SALT OF N- (3-METHOXY-5-METHYLPYRAZIN-2YL) -2- (4-[1, 3, 4-OXADIAZOLE-2-YL] PHENYL) PYRIDINE-3- SULPHONAMIDE - N-(3-Methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide ethanolamine salt and its uses are described.04-26-2012
20100144755Novel Compounds - Novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds and compositions, and their use use in therapy as CSBP/RK/p38 kinase inhibitors.06-10-2010
20110144127AGENTS FOR TREATMENT OF GLAUCOMATOUS RETINOPATHY AND OPTIC NEUROPATHY - Agents that stimulate nuclear translocation of Nrf2 protein and the subsequent increases in gene products that detoxify and eliminate cytotoxic metabolites are provided in a method for treating glaucomatous retinopathy or optic neuropathy. The structurally diverse agents that act on the Nrf2/ARE pathway induce the expression of enzymes and proteins that possess chemically versatile cytoprotective properties and are a defense against toxic metabolites and xenobiotics. Agents include certain electrophiles and oxidants such as a Michael Addition acceptor, diphenol, thiocarbamate, quinone, 1,2-dithiole-3-thione, butylated hydroxyanisole, flavonoid, an isothiocyanate, 3,5-di-tert-butyl-4-hydroxytoluene, ethoxyquin, a coumarin, combinations thereof, or a pharmacologically active derivative or analog thereof.06-16-2011
201002677453-Pyridinecarboxamide Derivatives as HDL-Cholesterol Raising Agents - The present invention relates to a method of raising HDL cholesterol comprising administering to a patient in need thereof a compound of the formula10-21-2010
201002677433-(PHENOXYPYRROLIDIN-3-YL-METHYL)HETEROARYL, 3-(PHENYLPYRROLIDIN-3-YLMETHOXY)HETEROARYL, AND 3-(HETEROARYLPYRROLIDIN-3-YLMETHOXY)HETEROARYL COMPOUNDS - In one aspect, the invention relates to compounds of formula I:10-21-2010
20110294826PYRROLO[2,3-D]PYRIMIDINE COMPOUNDS - Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation.12-01-2011
20100099688NOVEL PHOSPHODIESTERASE INHIBITORS - The present invention relates to a compound according to formula I,04-22-2010
20090270418PYRAZOLE PYRAZINE AMINE COMPOUNDS AS KINASE INHIBITORS, COMPOSITIONS THEREOF AND METHODS OF TREATMENT THEREWITH - Provided herein are Pyrazole Pyrazine Amine Compounds having the following structure:10-29-2009
20080312255PIPERDINE COMPOUNDS AND USES THEREOF-911 - Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.12-18-2008
20090149474GABA-B RECEPTOR MODULATORS - The present invention relates to novel imidazole derivatives having a positive allosteric GABA06-11-2009
20120190692SELECTIVE SUBSTITUTED PYRIDINE LIGANDS FOR NEURONAL NICOTINIC RECEPTORS - The present application describes selective ligands of formula (I)07-26-2012
20090209556SOLUBLE GUANYLATE CYCLASE ACTIVATORS - A compound having the structure08-20-2009
20090143408COMPOSITIONS AND METHODS FOR INHIBITING CYTOCHROME P450 2D6 - Methods of inhibiting cytochrome P450 2D6 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450 2D6. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 2D6 enzymes.06-04-2009
20100120794Cycloalkylamino Acid Derivatives - The invention relates to compounds of formula I05-13-2010
20100125081NEW COMPOUNDS 574 - The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.05-20-2010
20130217705NAPHTHYRIDINE DERIVATIVE - The present invention provides, for example, the following compound:08-22-2013
20100120793Pyrrolidines - This invention relates to a class of pyrrolidine compounds of formula (I), and pharmaceutically acceptable derivatives thereof, to their use in medicine, to compositions containing them, and to processes for their preparation. It also relates to intermediates used in the preparation of such compounds and derivatives. In particular the compounds of formula (I) are useful for the treatment of EP2-mediated conditions, such as endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), chronic pelvic pain syndrome.05-13-2010
20090221609Gene Predictors of Response to Metastatic Colorectal Chemotherapy - The present invention provides for the identification of genes that are expressed in tumors that are responsive to a given therapeutic regime and whose expression correlates with responsiveness to that therapeutic regime. One or more of the genes of the present invention can be used as markers to identify patients that are likely to be successfully treated by a therapeutic regime.09-03-2009
20110136830CHROMENONE DERIVATIVES - Novel compounds of the formula I06-09-2011
20110136828SUBSTITUTED N-OXIDE PYRAZINE DERIVATIVES - N-oxide pyrazine derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof:06-09-2011
20090082365Trisubstituted Quinazolinone Derivatives as Vanilloid Antagonists - The present invention relates to quinazolinone compounds of the formula03-26-2009
20100249148NOVEL PYRIMIDINE COMPOUNDS HAVING BENZYL (HETEROCYCLIC METHYL) AMINE STRUCTURE AND MEDICAMENT COMPRISING THE SAME - A compound represented by the following general formula (I), wherein R09-30-2010
20100249147SULFONYL-SUBSTITUTED 6-MEMBERED RING DERIVATIVE - [Problem] To provide a compound that is useful as an agent in the prevention and treatment of circulatory system, nervous system, metabolic, reproductive system, and gastrointestinal diseases.09-30-2010
20100081670N-PYRAZINYL-PHENYLSULPHONAMIDES AND THEIR USE IN THE TREATMENT OF CHEMOKINE MEDIATED DISEASES - The invention provides N-pyrazinyl-phenyl-sulphonamides of formula (I) for use in the treatment of chemokine mediated diseases. Particularly inflammatory diseases, such as asthma.04-01-2010
20100249146HETEROARYLOXY QUINAZOLINE DERIVATIVE - Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc.09-30-2010
20100081672PH SENSITIVE MATRIX FORMULATION - The present invention provides formulations of therapeutic agents that benefit from a prolonged time of controlled release in the stomach and upper gastrointestinal (GI) tract, and from an enhanced drug exposure to the upper GI tract. The formulations of the invention comprise a therapeutic agent and one or more pH sensitive polymers that are designed for accelerated hydration, expansion, disintegration and dissolution at the higher pH of the upper GI tract, thereby, ensuring that any therapeutic agent that has not been released in the stomach is released in the upper GI tract, thus maximizing absorption of therapeutic agent that has a window of absorption located at the upper GI tract.04-01-2010
20100081673HETEROARYL ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS - Described herein are compounds that are antagonists of PGD04-01-2010
20100081671Cycloalkylamine substituted isoquinoline derivatives - The invention relates to 6-substituted isoquinoline derivatives of the formula (I)04-01-2010
20090181981CRYSTALLINE (R)-2-(4-CYCLOPROPANESULPHONYL-PHENYL)-N-PYRAZIN-2-YL-3-(TETRAHYDROPYRAN-- 4-YL)-PROPIONAMIDE - Crystalline R-2-(4-cyclopropanesulfonyl-phenyl)-N-pyrazin-2-yl-3-(tetrahydropyran-4-yl)-propionamide and methods of its preparation and use are disclosed.07-16-2009
20090176805DERIVATIVES OF ETHYLENE METHANEDISULFONATE AS CANCER CHEMOTHERAPEUTIC AGENTS - The present application discloses derivatives of ethylene methanedisulfonate as cancer chemotherapeutic agents and methods of synthesizing such derivatives. The derivatives include modifications of ethylene methanedisulfonate by replacing one or both of the chemically most reactive hydrogens of the cyclic sulfonate ester structure. The derivatives of ethylene methanedisulfonate are more active than the parent ester (i.e., ethylene methanedisulfonate) as anticancer agents against a variety of cancers.07-09-2009
20110172248SUBSTITUTED HETEROARYLAMIDE ANALOGS AS MGLUR5 NEGATIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING THE SAME - Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate 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.07-14-2011
20090170875COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS - This invention relates to compounds of the Formula (I):07-02-2009
20100125082NEW COMPOUNDS 578 - The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.05-20-2010
20100125080COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES - The invention relates to certain compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.05-20-2010
200901434093-PYRIDINECARBOXAMIDE DERIVATIVES AS HDL-CHOLESTEROL RAISING AGENTS - The present invention relates to a method of raising HDL cholesterol comprising administering to a patient in need thereof a compound of the formula06-04-2009
20080207642Thienopyrimidinediones and Their Use in the Modulation of Autoimmune Disease - The invention relates to a compound of formula (1):08-28-2008
20090281118Selective Ligands for the Neuronal Nicotinic Receptors and Uses Thereof - The present application describes selective ligands of formula (I)11-12-2009
20090291967SMALL MOLECULE MODULATORS OF CELL ADHESION - Compounds, particularly compounds having activity as modulators of cadherin-mediated cell adhesion having the following structure:11-26-2009
20120295921PYRIDYL PIPERIDINE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to pyridyl piperidine compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.11-22-2012
201202959205-AMINO-4-HYDROXYPENTOYL AMIDES - HIV inhibitors of formula11-22-2012
20100280048Some 2-pyrazinone derivatives and their use as inhibitors of neutrophile elastase - The invention provides certain novel 6-heteroaryl-5-methyl-3-oxo-4-[3(trifluoromethyl)phenyl]-3,4-dihydropyrazine-2-carboxamide derivatives and pharmaceutically acceptable salts thereof and particular Forms thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of human neutrophil elastase.11-04-2010
20080275061METHOD FOR CONTROLLING PARTICULAR INSECT PESTS BY APPLYING ANTHRANILAMIDE COMPOUNDS - This invention pertains to a method for controlling lepidopteran, homopteran, hemipteran, thysanopteran and coleopteran insect pests comprising contacting the insects or their environment with an arthropodicidally effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof11-06-2008
20090170874Triazole-substituted arylamides as P2X3 and P2X2/3 antagonists - Compounds of the formula I:07-02-2009
20090170873Pyrazole-substituted arylamides as P2X3 and P2X2/3 antagonists - Compounds of the formula I:07-02-2009
20100267744Pharmaceutical Compositions - Forms and formulations of VX-950 and uses thereof.10-21-2010
20090149475Thioxanthine Derivatives and Their Use as Inhibitors of MPO - There are disclosed novel compounds of Formula (I) wherein L, R06-11-2009
20090264445PYRROLIDINONE GLUCOKINASE ACTIVATORS - Provided herein are compounds of the formula (I):10-22-2009
20090264444Organic compounds - The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.10-22-2009
20080269250Pyrrolidine and Piperidine Acetylene Derivatives for Use as Mglur5 Antagonists - The invention provides compounds of formula (I)10-30-2008
20110207746NEW COMPOUNDS I - The present invention relates to compounds of formula (I),08-25-2011
201102077472,5-Disubstituted Phenyl Carboxamide Orexin Receptor Antagonists - The present invention is directed to 2,5-disubstituted phenyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.08-25-2011
20090082367TRIAZOLE DERIVATIVE OR A SALT THEREOF - [Problem] To provide a compound which may be used in treating diseases in which 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is concerned, especially diabetes and insulin resistance.03-26-2009
20090137608Benzoimidazol-2-yl pyrimidines and pyrazines as modulators of the histamine H4 receptor - Benzoimidazol-2-yl pyrimidines and pyrazines, pharmaceutical compositions and methods for H05-28-2009
20090137607FUSED BICYCLIC PYRIMIDINES - Compounds of formula (I)05-28-2009
20090186907Pyrazinones As Cellular Proliferation Inhibitors - This invention pertains to a method of inhibiting undesired animal cellular proliferation said method comprising contacting an animal cell with a compound of Formula 1 and all pharmaceutically acceptable, salts, N-oxides, hydrates, solvates, or geometric and stereoisomers thereof:07-23-2009
20090143407ISOXAZOLO-PYRAZINE DERIVATIVES - The invention relates to isoxazolo-pyrazine derivatives and their pharmaceutically acceptable salts having affinity and selectivity for the GABA A α5 receptor binding site, their manufacture, and pharmaceutical compositions containing them. The compounds of present invention are inverse agonists of GABA A α5. The invention also relates to methods for enhancing cognition and for treating cognitive disorders like Alzheimer's disease.06-04-2009
20080234292Peptidase Inhibitors - The present invention relates to a series of novel compounds having the formula (I) wherein: X is NR09-25-2008
20080318975Indolylmaleimide Derivatives - A compound of formula (I)12-25-2008
20130217703SUSTITUTED 2,3,4,5-TETRAHYDRO-1H-PYRIDO[4,3-B]INDOLES, METHODS FOR USE THEREOF - The present invention relates to a method of antagonizing a 5-HT08-22-2013
20090062307AMINOPYRAZINE DERIVATIVES AND COMPOSITIONS - The present invention relates to aminopyrazine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such aminopyrazine derivatives are useful in the treatment of diseases associated with inappropriate tyrosine and/or serine/threonine kinase activity.03-05-2009
20090197897Novel Oxadiazole Derivatives and Their Use as Positive Allosteric Modulators of Metabotropic Glutamate Receptors - The present invention relates to new compounds which are Oxadiazole derivatives of formula (I) wherein B, P, Q, W, R08-06-2009
20110144126COMPOUNDS USEFUL FOR INHIBITING CHK1 - The present invention provides an aminopyrazole compound, or a pharmaceutically acceptable salt thereof or a solvate of the salt, that inhibits Chk1 and is useful in the treatment of cancer.06-16-2011
20090054465N-HYDROXYACRYLAMIDE COMPOUNDS - This invention relates to novel N-hydroxyacrylamide compounds of formula (I) and pharmaceutically acceptable salts thereof. More particularly, it relates to novel N-hydroxyacrylamide compounds and pharmaceutically acceptable salts thereof which act as a HDAC inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of HDAC-related disease.02-26-2009
20110224231Novel Lactams as Beta Secretase Inhibitors - Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment methods of synthesis, and intermediates are also disclosed.09-15-2011
20110224230BICYCLIC DIHYDROIMIDAZOLONE CGRP RECEPTOR ANTAGONISTS - Compounds of formula (I): wherein variables B, G09-15-2011
20110230498BIARYL CARBOXAMIDES - This invention provides compounds of Formula (I) which are PAFR antagonists: Formula (I) and the pharmaceutically acceptable salts thereof. The compounds are useful for treating PAF-mediated disorders, and can be used in methods for treating atherosclerosis and preventing or reducing risk for atherosclerotic disease events. The compounds are also useful for treating or ameliorating pain, e.g. inflammatory pain and/or nociceptive pain, and for treating or ameliorating autoimmune and/or inflammatory diseases, among other conditions.09-22-2011
200901921715-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.07-30-2009
20110230500Inhibitors of Phosphoinositide Dependent Kinase 1 (PDK1) - The instant invention provides for compounds that inhibit PDK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting PDK1 activity by administering the compound to a patient in need of treatment of cancer.09-22-2011
20110230499HSP90 INHIBITORS FOR THERAPEUTIC TREATMENT - The use of a Hsp90 inhibitor for the treatment of cancer of the bladder, the colon, the liver, the lung, the breast, the vagina, the ovaries, the pancreas, the kidney, the stomach, the gastrointestinal tract, the prostate, the head and neck, the peritoneal cavity, the thyroid, the bone, the brain, the central nervous system and/or the blood and/or for the treatment of myelodysplastic syndrome, systemic mastocytosis, von Hippel-Lindau syndrome, multicentric Castleman disease and/or psioriasis.09-22-2011
20090203715NOVEL 2-HETARYLTHIAZOLE-4-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND USE AS PHARMACEUTICALS - The present invention relates to 2-hetarylthiazole-4-carboxamide derivatives of the formula (I), the use thereof as medicament for the treatment of various disorders, and processes for the preparation thereof08-13-2009
20090105277AGENT FOR PREVENTING AND/OR TREATING MOVEMENT DISORDER - For example, an agent for preventing and/or treating movement disorder comprising, as an active ingredient, a triazolopyrimidine derivative having an adenosine A04-23-2009
20090082366DEUTERIUM-ENRICHED TELAPREVIR - The present application describes deuterium-enriched telaprevir, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-26-2009
20090054462Hydroisoindoline tachykinin receptor antagonists - The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.02-26-2009
20090093498AMINO-5,5-DIPHENYLIMIDAZOLONE DERIVATIVES FOR THE INHIBITION OF BETA-SECRETASE - The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated β-amyloid deposits or β-amyloid levels in a patient.04-09-2009
200902475503-TRIFLUOROMETHYL-PYRAZINE-2-CARBOXYLIC ACID AMIDE DERIVATIVES AS HDL-CHOLESTEROL RAISING AGENTS - The present invention relates to pyrazine derivatives of the formula10-01-2009
20090209554Thiazoliums as transketolase inhibitors - The present invention provides N-3′-pyridyl-methyl or N-2′-pyrazinylmethyl thiazolium derivatives of formula (I) which are useful as transketolase inhibitors wherein R08-20-2009
20090247549Methods of using saha and bortezomib for treating cancer - The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor such as suberoylanilide hydroxamic acid (SAHA), or a pharmaceutically acceptable salt or hydrate thereof, and a second amount of one or more anti-cancer agents, including Bortezomib. The HDAC inhibitor and the anti-cancer agent may be administered to comprise therapeutically effective amounts. In various aspects, the effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic.10-01-2009
20090247548PYRROLOPYRIMIDINE DERIVATIVES FOR TREATING PROLIFERATIVE DISEASES - The present invention relates to a compound of formula I10-01-2009
20090253714Methods of reducing risk of infection from pathogens - Prophylactic treatment methods are provided for protection of individuals and/or populations against infection from airborne pathogens. In particular, prophylactic treatment methods are provided comprising administering amiloride, benzamil, phenamil or pharmaceutically acceptable salts thereof to one or more members of a population at risk of exposure to or already exposed to one or more airborne pathogens, either from natural sources or from intentional release of pathogens into the environment.10-08-2009
20100152203THIADIAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds of the formula I:06-17-2010
20090048269CHEMICAL COMPOUNDS-821 - The invention relates to chemical compounds of the formula (I),02-19-2009
20100261733THERAPEUTIC AGENTS 927 - (2S)-2-[1-(2-Chloro-6-cyano-phenyl)pyrazolo[4,5-e]pyrimidin-4-yl]oxy-3-[(1R)-2-hydroxy-1-methyl-ethoxy]-N-(5-methylpyrazin-2-yl)propanamide or a pharmaceutically acceptable salt thereof is useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK or GK), leading to a decreased glucose threshold for insulin secretion.10-14-2010
20100261734Methods of Treating Bladder Dysfunction Using Netupitant - The present invention relates to methods for reducing the frequency of bladder contractions without significantly affecting micturition pressure, comprising administering a pharmaceutical composition comprising a therapeutically effective amount of netupitant, or a pharmaceutically acceptable salt or prodrug thereof. The method can be used to treat bladder dysfunction without significantly increasing residual volume, including urgency, frequency, pollakiuria, nocturia, low deferment time, suboptimal volume threshold, neurogenic bladder, or combinations thereof.10-14-2010
201100599893,5-DIAMINO-6-CHLORO-PYRAZINE-2-CARBOXYLIC ACID DERIVATIVES AND THEIR USE AS EPITHELIAL SODIUM CHANNEL BLOCKERS FOR THE TREATMENT OF AIRWAY DISEASES - A compound of Formula I03-10-2011
20110059988ISOXAZOLINE COMPOSITIONS AND THEIR USE AS ANTIPARASITICS - This invention relates to methods for controlling parasitic infestations of animals and their environments, and, more particularly, to methods using isoxazolines to control parasites in or on animals or in their environments, as well as treat parasitoses of animals. The isoxazolines include 4-(isoxazolinyl)-benzamides (specifically, substituted 4-(5-(halomethyl)-5-phenylisoxazolin-3-yl)-benzamides) and 4-(isoxazolinyl)-benzothioamides (specifically, substituted 4-(5-(halomethyl)-5-phenyl-isoxazolin-3-yl)-benzothioamides). This invention also relates to compositions comprising the isoxazolines for use in such methods, the use of the isoxazolines to make medicaments for use in such methods, and kits comprising the isoxazolines for carrying out such methods. This invention further relates to the use of the isoxazolines as medicaments, particularly medicaments that can be used in the above-referenced method.03-10-2011
20110059987Co-Crystals and Pharmaceutical Compositions Comprising the Same - The invention relates to compositions and co-crystals each comprising VX-950 and a co-crystal former selected from the group consisting of 4-hydroxybenzoic acid, 4-amino salicylic acid, phenylalanine, threonline, tartaric acid, adipic acid, succinic acetate, proline, methyl 4-hydroxybenzoate, anthranilic acid, and d-Biotin. Also within the scope of this invention are methods of making and using the same.03-10-2011
20100222367PYRAZINE KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the inventions.09-02-2010
20100152202Tissue Factor Promoter Polymorphisms - The invention provides compositions and methods for determining the likelihood of successful treatment with a pyrimidine based antimetabolite chemotherapy drug such as 5-fluorouracil or in combination with a platinum based chemotherapy drug, such as 5-fluorouracil/oxaliplatin. The methods comprise determining the genomic polymorphism present in a predetermined region of a gene of interest and correlating the polymorphism to the predictive response. Patients identified as responsive are then treated with the appropriate therapy.06-17-2010
20100240677Compounds as PDE IV and TNF Inhibitors - This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF).09-23-2010
20100216813PYRROLIDINEANILINES - The present invention relates to a compound represented by the following formula I or a pharmaceutically acceptable salt thereof; wherein R08-26-2010
20100216814PYRIDO[4,3-B]INDOLES CONTAINING RIGID MOIETIES - This disclosure is directed to pyrido[4,3-b]indoles having rigid moieties. The compounds in one embodiment are pyrido[4,3-b]indoles having an unsaturated hydrocarbon moiety. The compounds in another embodiment are pyrido[4,3-b]indoles having a cycloalkyl, cycloalkenyl or heterocyclyl moiety. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.08-26-2010
20100216816PYRAZINYL AMIDE-T TYPE CALCIUM CHANNEL ANTAGONISTS - The present invention is directed to pyrazinyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.08-26-2010
20100216815N-SUBSTITUTED OXINDOLINE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS - A series of N-substituted oxindole derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.08-26-2010
20100120792Substituted 2,3,4,5-Tetrahyrdo-1H-Pyrido[4,3-B]Indoles, Methods for the Production and Use Thereof - The invention relates to antagonists of serotonin 5-HT05-13-2010
20130217702INDOLE DERIVATIVES - The present invention relates to the indole derivatives of formula (I), wherein R08-22-2013
20130217704COMPOSITIONS AND METHODS FOR INHIBITING CYTOCHROME P450 2D6 - Methods of inhibiting cytochrome P450 2D6 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450 2D6. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 2D6 enzymes.08-22-2013
20100222368N-(Heteroaryl)-1-heteroarylalkyl-1H-indole-2-carboxamide derivatives, preparation and therapeutic use thereof - The invention concerns compounds of general formula (I), wherein n, X09-02-2010
20100222365SUBSTITUTED TRIAZOLE DERIVIATIVES AS OXYTOCIN ANTAGONISTS - The present invention relates to a class of substituted triazoles of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction, particularly premature ejaculation (P.E.).09-02-2010
20100222366PIPERIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY - The present application describes modulators of MIP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators are disclosed.09-02-2010
20120142705ISATIN AND OXINDOLE COMPOUNDS - Provided herein are compounds of the formula (I):06-07-2012
20110028492Heteroaryl Compounds and Their Uses - The present invention provides a compound of formula (I):02-03-2011
20090221608PYRAZOLE COMPOUNDS - The present invention is directed to compounds of Formula (I),09-03-2009
20090170872Compounds and Their Pharmaceutical Use - The present invention relates to novel compounds of the general formula (I), their analogs, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and compositions. The present invention more particularly provides novel compounds of the general formula (I).07-02-2009
20090163515Compounds Which Bind to the Active Site of Protein Kinase Enzymes - The present invention relates to a compound and a group of compounds which are inhibitors of Rho kinase (ROK, ROCK). In addition, the invention relates to methods of treatment and use of the compounds in the manufacture of a medicament for application to a number of therapeutic indications including cardiovascular disease (coronary vasospasm, hypertensive disease, arteriosclerosis), stroke, cancer, erectile dysfunction, asthma, osteoporosis, glaucoma and AIDS. The compounds can be used in screening programmes against protein kinases. The invention also provides methods for making compounds and libraries that include these compounds.06-25-2009
20090318472AMINOPYRAZINE DERIVATIVES AND COMPOSITIONS - The present invention relates to aminopyrazine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such aminopyrazine derivatives are useful in the treatment of diseases associated with inappropriate tyrosine and/or serine/threonine kinase activity.12-24-2009
20100298342Spiropiperidine beta-secretase inhibitors for the treatment of Alzheimer's Disease - The present invention is directed to spiropiperidine compounds of formula (I) and tautomers thereof, which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme 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 the beta-secretase enzyme is involved.11-25-2010
20130131082Aminopyrazine Derivative and Medicine - The present invention relates to a compound represented by general formula [1] satisfying the following (I) or (II), or a pharmaceutically acceptable salt of the compound.05-23-2013
20130131083PEST CONTROL COMPOSITION - A pest control composition comprising a hydrazide compound shown by formula (1) below (in the formula, G, M, Q05-23-2013
20110046160Novel Class of Spiro Piperidines for the Treatment of Neurodegenerative Diseases - Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.02-24-2011
20130137705PYRIDO[3,4-B]INDOLES AND METHODS OF USE - This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.05-30-2013
20100331346BETA-AMINO ACID DERIVATIVES FOR TREATMENT OF DIABETES - Novel heterocyclic compounds of the formula I12-30-2010
20110245271TRIAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds of the formula I:10-06-2011
20110118281COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES - The invention relates to certain compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.05-19-2011
20110118282Soluble Guanylate Cyclase Activators - A compound having the structure05-19-2011
20110130409SUBSTITUTED 1,2,3,4-TETRAHYDROCYCLOPENTA[B]INDOL-3-YL)ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS - The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.06-02-2011
20120245184SMALL ORGANIC MOLECULE REGULATORS OF CELL PROLIFERATION - The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a compound. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal patched pathway or agonizing smoothened or hedgehog activity.09-27-2012
20100179172N-PHENYL-METHANAMINE DERIVATIVE AND PESTICIDE CONTAINING IT - A novel pesticide is provided. The present invention provides a pesticide containing, as an active ingredient, an N-phenyl-methanamine derivative represented by the formula (I) or its salt:07-15-2010
20090197898SELECTIVE SUBTYPE ALPHA 2 ADRENERGIC AGENTS AND METHODS FOR USE THEREOF - The invention provides well-defined heterocyclic compounds that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptors.08-06-2009
20100063063Substituted Heteroaryls - The present invention provides Formula (1A) compounds03-11-2010
20100063064Substituted Triazole Derivatives As Oxytocin Antagonists - The present invention relates to a class of substituted 1,2,4-triazoles of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction, particularly premature ejaculation (P.E.).03-11-2010
20100069404TETRAHYDROCYCLOPENTA[b] INDOLE COMPOUNDS AS ANDROGEN RECEPTOR MODULATORS - The present invention provides a compound of the formula: Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly reduced bones mass, osteoporosis, osteopenia, or reduced muscle mass or strength, comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt thereof. X-17142.03-18-2010
20110098310NOVEL COMPOUNDS, USE AND PREPARATION THEREOF - The present invention relates to compounds of the general formula (I) wherein R04-28-2011
20110098311COMPOSITIONS FOR TREATMENT OF CYSTIC FIBROSIS AND OTHER CHRONIC DISEASES - The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.04-28-2011
20090069345Pharmaceutically Stable Compound Consisting of Timolol, Dorzolamide and Brimonidine - The present invention is related to ophthalmic formulations for the treatment of ocular ailments. More specifically, it is related to the pharmaceutical industry in the production of ophthalmic medication for the treatment of ocular hypertension. The advantage of the present invention over other state of the art treatments is that it achieves a composition of Dorzolamide Hydrochloride, Timolol Maleate and Brimonidine Tartrate with excellent properties of stability; it does not give rise to chemical reactions which produce modifications in the active molecules; with no antagonistic effects among the components. The present invention consists of a stable pharmaceutical composition for the treatment of ocular hypertension characterized by consisting of the following excipients: Polyoxyl 40 Stearate, Sodium Borate crystals, Sodium Chloride, Mannitol and Benzalkonium chloride.03-12-2009
20110082155Novel 2-Pyridone Compounds - The invention provides compounds of formula04-07-2011
20110071163USE OF AN OPIOID RECEPTOR ANTAGONIST FOR THE TREATMENT OR PREVENTION OF GASTROINTESTINAL TRACT DISORDERS - The disclosure relates to a method of treating or preventing a condition in a subject associated with the activation of an opioid receptor in the periphery by administering an effective amount of 5-(2-methoxy-4-{[2-(tetrahydro-pyran-4-yl)-ethylamino]-methyl}-phenoxy)-pyrazine-2-carboxamide (Compound I). In particular, the disclosure relates to a method of treating or preventing opioid-induced constipation or opioid-induced bowel dysfunction in a human without reducing centrally-mediated opioid analgesia or producing central opioid withdrawal symptoms by administering an effective amount of Compound I. The disclosure further relates to the use of Compound I for the preparation of a medicament for the treatment or prevention of a condition in a subject associated with the activation of an opioid receptor in the periphery.03-24-2011
20100234397ENZYME INHIBITORS - There is disclosed herein methods for using compounds of formula (I),09-16-2010
20090181982SUBSTITUTED PYRROLINE KINASE INHIBITORS - The present invention is directed to novel substituted pyrroline compounds useful as kinase inhibitors and methods for treating or ameliorating a kinase mediated disorder.07-16-2009
20110039864THERAPEUTIC COMPOUNDS - Disclosed herein is an alpha-adrenergic compound having a structure. Therapeutic methods, compositions, and medicaments for treating pain are also disclosed herein.02-17-2011
20130165452Substituted Heteroaryls - The present invention provides Formula (1A) compounds06-27-2013
20090030016BENZIMIDAZOLE POLY(ADP RIBOSE)POLYMERASE INHIBITORS - Compounds which inhibit the activity of poly(ADP-ribose)polymerase (PARP), compositions containing the compounds and methods of treating diseases using them are disclosed.01-29-2009
20080221125NOVEL HETEROCYCLIC BENZO[C]CHROMENE DERIVATIVES USEFUL AS MODULATORS OF THE ESTROGEN RECEPTORS - The present invention is directed to novel heterocyclic benzo[c]chromene derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders mediated by one or more estrogen receptors. The compounds of the invention are useful in the treatment of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.09-11-2008
20080221124Ethanolamine Salt of N- (3-Methoxy-5-Methylpyrazin-2Yl) -2- (4-[1, 3, 4-Oxadiazole-2-Yl] Phenyl) Pyridine-3-Sulphonamide - N-(Methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-yl]phenyl)pyridine-3-sulphonamide ethanolamine salt its synthesis and its uses are described.09-11-2008
200901183042-HETEROARYL-SUBSTITUTED INDOLE DERIVATIVE - Disclosed is a compound represented by the formula (I) below, which has a glucokinase-activating effect and is thus useful for treatment of diabetes or obesity, or a pharmaceutically acceptable salt thereof.05-07-2009
20110178101DUAL-ACTING THIOPHENE, PYRROLE, THIAZOLE AND FURAN ANTIHYPERTENSIVE AGENTS - In one aspect, the invention relates to compounds having the formula:07-21-2011
20080255154Amido Compounds And Their Use As Pharmaceuticals - The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.10-16-2008
20080255152DIARYL ETHERS AS OPIOID RECEPTOR ANTAGONISTS - A compound of the formula (I) wherein the variables X10-16-2008
20110021539Pyrazinylpyrazoles - Pyrazin-2-ylpyrazoles are described, as is the use thereof as insecticides and/or parasiticides.01-27-2011
20100286171PHENYLACETAMIDE DERIVATIVE - A phenylacetamide derivative having sulfonyl group and cycloalkyl group on the phenyl group and having heteroaryl group on the nitrogen atom in the amide has an excellent GK activation action, thereby completing the present invention. The compound of the present invention is useful as an agent for treating diabetes, in particular, type II diabetes, since it has an excellent GK activation action.11-11-2010
20090054464HDAC INHIBITOR - Compounds having the formula (I):02-26-2009
20110263612COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.10-27-2011
20120302583New Compounds I - The present invention relates to a method for the treatment or prevention of inflammation, an inflammatory disease, an immune or an autoimmune disorder, which comprises administering to a mammal in need of such treatment an effective amount of a compound compound of formula (I),11-29-2012
201002983435-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.11-25-2010
201101368293-(N-HETEROCYCLYL)-PYRROLIDINYL-PHENYL-OXAZOLIDINONES AS ANTIBACTERIAL AGENTS - The invention provides new oxazolidinone compounds of formula (I) wherein R, R06-09-2011
20100324070INDOLE, INDAZOLE AND BENZIMIDAZOLE ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds of the formula I:12-23-2010
20100324068CHEMICAL COMPOUNDS 785 - DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity12-23-2010
20100286169Antibacterial Sulfone and Sulfoxide Substituted Heterocyclic Urea Compounds - The present invention provides novel sulfone and sulfoxide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and methods of production are provided.11-11-2010
20090176806SUBSTITUTED PYRROLINE KINASE INHIBITORS - The present invention is directed to novel substituted pyrroline compounds useful as kinase inhibitors and methods for treating or ameliorating a kinase mediated disorder.07-09-2009
20110201625Organic Comopunds - A compound of Formula I08-18-2011
20100029688BIPIPERIDINYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT - Bipiperidinyl compounds of the formula I, are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.02-04-2010
20100029684Pyrazinone Modulator of Corticotropin-Releasing Factor Receptor Activity - The invention relates to the compound (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-(6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino)-5-oxo-4,5-dihydropyrazine-2-carbonitrile, pharmaceutical compositions of the compound, and methods of using the compound for the treatment of psychiatric disorders and neurological diseases including depression, anxiety related disorders, irritable bowel syndrome, addiction and negative aspects of drug and alcohol withdrawal, and other conditions associated with CRF.02-04-2010
20100029685OXADIAZOLE AND THIADIAZOLE COMPOUNDS AND THEIR USE AS NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS - This invention relates to oxadiazolyl and thiadiazolyl derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.02-04-2010
20100016336HUMAN PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE - The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-β) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-β) inhibitors, and to methods for regulating angiogenesis.01-21-2010
20100324069OXAZOLONE AND PYRROLIDINONE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds of the formula I:12-23-2010
20120172376HETEROCYCLIC COMPOUNDS AND THEIR USE AS GLYCOGEN SYNTHASE KINASE-3 INHIBITORS - The present invention relates to novel heterocyclic compounds of formula I07-05-2012
20090054463Derivatives of urea and related diamines, methods for their manufacture, and uses therefor - The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.02-26-2009
200902095552-PYRAZINONE DERIVATIVES FOR THE TREATMENT OF DISEASE OR CONDITION IN WHICH INHIBITION OF NEUTROPHIL ELASTASE ACTIVITY IS BENEFICIAL - The invention provides compounds of formula08-20-2009
20120040999P38 KINASE INHIBITING AGENTS - Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: Formula (I); are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.02-16-2012
201200409982-ALKYL PIPERIDINE MGLUR5 RECEPTOR MODULATORS - The present invention is directed to 2-alkylpiperidines which are positive allosteric modulators of metabotropic glutamate receptors, particularly the mGluR5 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.02-16-2012
20120040997VINYL-ARYL DERIVATIVES FOR INFLAMMATION AND IMMUNE-RELATED USES - The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.02-16-2012
20090312347Novel oxadiazole derivatives and their medical use - This invention relates to novel oxadiazole derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.12-17-2009
20110172247SUBSTITUTED HETEROARYLAMINE CARBOXAMIDE ANALOGS AS MGLUR5 NEGATIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING THE SAME - Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate 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 invention07-14-2011
20080287460NEW COMPOUNDS 835 - This invention relates to novel compounds having the structural formula I below:11-20-2008
20120046303BENZIMIDAZOLE POLY(ADP RIBOSE)POLYMERASE INHIBITORS - Compounds which inhibit the activity of poly(ADP-ribose)polymerase (PARP), compositions containing the compounds and methods of treating diseases using them are disclosed.02-23-2012
20090062306NOVEL PYRIMIDINE COMPOUNDS HAVING BENZYL (HETEROCYCLIC METHYL) AMINE STRUCTURE AND MEDICAMENT COMPRISING THE SAME - A compound represented by the following general formula (I), wherein R03-05-2009
20120004243AMIDE DERIVATIVES BEARING A CYCLOPROPYLAMINOACARBONYL SUBSTITUENT USEFUL AS CYTOKINE INHIBITORS - The invention concerns a compound of the Formula (I), wherein Qa is heteroaryl and is substituted with halogeno; R1 and R2 are hydrogen; and Qb is phenyl or heteroaryl, and Qb may optionally bear 1 or 2 substituents selected from hydroxy, halogeno and (1-6C)alkyl, or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.01-05-2012
20120010219SALVINORIN DERIVATIVES AND USES THEREOF - The invention features salvinorin compositions that are selective for kappa opioid receptors; methods of treating mania by using a selective kappa receptor agonist; and methods of treating mood disorders, such as depressive disorders and manic disorders, using salvinorin compositions.01-12-2012
20120010220SPIROINDOLINEPIPERIDINE DERIVATIVES - Insecticidal, acaricidal, nematicidal or molluscicidal compounds of formula (I)01-12-2012
20120022083SMALL MOLECULE MODULATORS OF CELL ADHESION - Compounds, particularly compounds having activity as modulators of cadherin-mediated cell adhesion having the following structure:01-26-2012
20100144758AZAINDOLE P2X3 AND P2X2/3 MODULATORS - The application discloses compounds of the Formula I:06-10-2010
20110166160Pyrazinone Modulator of Corticotropin-Releasing Factor Receptor Activity - The invention relates to the compound (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-(6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino)-5-oxo-4,5-dihydropyrazine-2-carbonitrile, pharmaceutical compositions of the compound, and methods of using the compound for the treatment of psychiatric disorders and neurological diseases including depression, anxiety related disorders, irritable bowel syndrome, addiction and negative aspects of drug and alcohol withdrawal, and other conditions associated with CRF.07-07-2011
20110166159COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.07-07-2011
20110166158SUBSTITUTED PHENYLAMINE CARBOXAMIDE ANALOGS AS MGLUR5 NEGATIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING THE SAME - Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate 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.07-07-2011
20120015961ISOTHIOUREA DERIVATIVES OR ISOUREA DERIVATIVES HAVING BACE1 INHIBITORY ACTIVITY - The present invention provides, for example, a compound of the following formula (I):01-19-2012
20120022082PYRAZINE DERIVATIVES - The invention concerns pyrazine derivatives of the Formula I01-26-2012
20110009425TETRAHYDROTHIENO PYRIDINES - The present invention relates to tetrahydrothienopyridine compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.01-13-2011
201201086102-PYRAZINONE DERIVATIVES FOR THE TREATMENT OF DISEASE OR CONDITION IN WHICH INHIBITION OF NEUTROPHIL ELASTASE ACTIVITY IS BENEFICIAL - The invention provides compounds of formula05-03-2012
20120108609DIHYDROOXAZOL-2-AMINE DERIVATIVES - The invention relates to compounds of formula05-03-2012
20100035896Combination of N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyri- dine-3-sulphonamide and an anti-mitotic cytotoxic agent - A combination, comprising N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide and an anti-mitotic cytotoxic agent.02-11-2010
20110065724COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.03-17-2011
20110065725TRIAZOLE AMIDE DERIVATIVES FOR USE IN THERAPY - The invention relates to triazole amide derivatives of formula (I) for use in therapy, in particular for treating diseases and conditions mediated by antagonism of the mGluR03-17-2011
20120309769N-BENZYLINDOLE MODULATORS OF PPARG - The invention provides molecular entities that bind with high affinity to PPARG (PPARγ), and inhibit kinase-mediated (e.g., cdk5-mediated) phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. Side effects such as significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, can be avoided in the mammal receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.12-06-2012
20090099203COMPOSITION 064 - A pharmaceutical composition which comprises N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide with mannitol and/or microcrystalline cellulose is described.04-16-2009
20120122886THIADIAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds of the formula I:05-17-2012
20120122885PYRUVATE KINASE M2 MODULATORS, THERAPEUTIC COMPOSITIONS AND RELATED METHODS OF USE - Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.05-17-2012
20120122884COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.05-17-2012
20110105530ORGANIC COMPOUNDS - The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.05-05-2011
20110105529ERCC-1 Gene Expression Predicts Chemotherapy Outcome - The invention provides compositions and methods for determining the likelihood of successful treatment with a first line FOLFOX chemotherapy regimen or in further combination with PTK/ZK. The methods comprise determining the gene expression levels of a gene of interest and correlating the high or low expression to the predictive response. Patients identified as responsive are then treated with the appropriate therapy.05-05-2011
201101055281-(7-(HEXAHYDROPYRROLO [3, 4-C] PYRROL-2 (1H)-YL) QUINOLIN-4-YL) -3- (PYRAZIN-2-YL) UREA DERIVATIVES AND RELATED COMPOUNDS AS GLYCOGEN SYNTHASE KINASE 3 (GSK-3) - The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.05-05-2011
20110105527PYRAZINES AS DELTA OPIOID RECEPTOR MODULATORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows:05-05-2011
20110105526SELECTIVE SUBTYPE ALPHA 2 ADRENERGIC AGENTS AND METHODS FOR USE THEREOF - The invention provides oxazolidine and thiazolidine derivatives that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptors.05-05-2011
20080318974Compounds Useful for Inhibiting Chk1 - Aryl- and heteroaryl-substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division also are disclosed.12-25-2008
20100093757THERAPEUTIC AGENTS 414 - A compound of Formula (I):04-15-2010
20100093756HETEROARYL SUBSTITUTED THIENO[2,3-d]PYRIMIDINE AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS - This invention relates to a novel thieno[2,3-d]pyrimidine, Z, and its therapeutic and prophylactic uses, wherein X, R04-15-2010
20120316182COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.12-13-2012
20090131454New compounds 067 - The present invention is directed to novel compounds, their use in therapy and pharmaceutical compositions comprising said novel compounds.05-21-2009
20120258973DISUBSTITUTED HETEROARYL-FUSED PYRIDINES - The invention relates to compound of the formula (I′) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.10-11-2012
20110183997HETEROCYCLIC COMPOUNDS AND COMPOSITIONS AS C-KIT AND PDGFR KINASE INHIBITORS - The invention provides a novel class of compounds of Formula I: (I) pharmaceutical compositions comprising such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFRα and PDGFRβ kinases.07-28-2011
20120165342Methods of Reducing Risk of Infection from Pathogens - Prophylactic treatment methods are provided for protection of individuals and/or populations against infection from airborne pathogens. In particular, prophylactic treatment methods are provided comprising administering a sodium channel blocker or pharmaceutically acceptable salts thereof to one or more members of a population at risk of exposure to or already exposed to one or more airborne pathogens, either from natural sources or from intentional release of pathogens into the environment.06-28-2012
20090111834NOVEL FLAVORS, FLAVOR MODIFIERS, TASTANTS, TASTE ENHANCERS, UMAMI OR SWEET TASTANTS, AND/OR ENHANCERS AND USE THEREOF - The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers, —savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.04-30-2009
20100204244AGENTS FOR TREATMENT OF DIABETIC RETINOPATHY AND DRUSEN FORMATION IN MACULAR DEGENERATION - Agents that stimulate nuclear translocation of Nrf2 protein and the subsequent increases in gene products that detoxify and eliminate cytotoxic metabolites are provided in a method for treating diabetic retinopathy or drusen formation in age-related macular degeneration. The structurally diverse agents that act on the Nrf2/ARE pathway induce the expression of enzymes and proteins that possess chemically versatile cytoprotective properties and are a defense against toxic metabolites and xenobiotics. Agents include certain electrophiles and oxidants such as a Michael Addition acceptor, diphenol, thiocarbamate, quinone, 1,2-dithiole-3-thione, butylated hydroxyanisole, flavonoid other than genistein, an isothiocyanate, 3,5-di-tert-butyl-4-hydroxytoluene, ethoxyquin, a coumarin, combinations thereof, or a pharmacologically active derivative or analog thereof.08-12-2010
20100280049ANTAGONISTS OF PGD2 RECEPTORS - Described herein are compounds and pharmaceutical compositions containing such compounds that antagonize the PGD2 activated chemoattractant receptor-homologous molecule expressed on TH2 cells (CRTH2). Also described herein are methods of using such CRTH2 antagonists, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2 mediated conditions or diseases.11-04-2010
20130172366BRIDGED HETEROCYCLIC COMPOUNDS AND METHODS OF USE - This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.07-04-2013
20120136008PYRIDO[4,3-B]INDOLES AND METHODS OF USE - New heterocyclic compounds that may be used to modulate a histamine receptor in an individual are described. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.05-31-2012
20120178764Novel Compounds - The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.07-12-2012
20100029687PIPERIDINE DERIVATIVE OR SALT THEREOF - [Problem] To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism.02-04-2010
20100292252VINYL-ARYL DERIVATIVES FOR INFLAMMATION AND IMMUNE-RELATED USES - The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.11-18-2010
20120083500OXAZOLONE AND PYRROLIDINONE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X 2/3 ANTAGONISTS - Compounds of the formula I:04-05-2012
20120225892[1,5]-Diazocin Derivatives - The present invention relates to compounds of formula (I) compositions, in particular pharmaceutical compositions, and medicaments comprising at least one compound of formula (I). The invention also relates to the use of such a compound for manufacturing a medicament. In particular the medicament and the pharmaceutical composition are intended to treat diseases linked with insulin regulation problems, such as diabetes. This invention aims also to methods for treating or preventing such diseases.09-06-2012
20120225891AMIDE DERIVATIVES, PROCESS FOR PREPARATION THEREOF AND USE THEREOF AS INSECTICIDE - A compound represented by Formula (1):09-06-2012
20090018144CAPPED PYRAZINOYLGUANIDINE SODIUM CHANNEL BLOCKERS - The present invention relates to compounds represented by formula (I):01-15-2009
20110124662Substituted Carbamate Derivatives as Modulators of Corticotropin-Releasing Factor Receptor Activity - The disclosure provides compounds of formula (I), including their salts, as well as compositions and methods of using the compounds. The compounds are CRF receptor antagonists and may be useful for treating disorders associated with abnormal CRF levels or aberrant functioning of CRF receptors.05-26-2011
20110124661OXAZOLOBENZIMIDAZOLE DERIVATIVES - The present invention is directed to oxazolobenzimidazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.05-26-2011
20110124660Novel Diazinylpyrazolyl Compounds - The present invention relates to diazinylpyrazolyl compounds of the formula (I)05-26-2011
20110003831N-(-3-METHOXY-5-METHYLPYRAZIN-2-YL)-2-(4-'1,3,4-OXADIAZOL-2-YL!PHENYL)PYRI- DINE-3 SULPHONAMIDE AS AN ANTICANCER AGENT - The use of N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide, or a pharmaceutically acceptable salt thereof, in the treatment of cancer and/or pain in a warm blooded animal such as man is described.01-06-2011
20100227872PYRAZINE DERIVATIVES - The present invention relates to compounds of the formula09-09-2010
20110046159Arylpyrazinone derivatives insulin secretion stimulators, methods for obtaining them and use thereof for the treatment of diabetes - The present invention relates to arylpyrazinone derivatives of formula (I), wherein R1, R2, R3 and A are as defined in claim 02-24-2011
20110046158CAPPED PYRAZINOYLGUANIDINE SODIUM CHANNEL BLOCKERS - The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.02-24-2011
20110046157Substituted hydroxamic acids and uses thereof - This invention provides compounds of formula (I):02-24-2011
20110230497BIOLOGICALLY ACTIVE AMIDES - The present invention is directed to biologically active amides which are ligands at the NPY Y5 receptor. The invention further 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 method of treating a subject suffering from certain disorders which comprises administering to the subject an amount of a compound of the subject invention. Furthermore, this invention also provides uses of a compound of the invention for the manufacture of a medicament for treating a subject suffering from certain disorders.09-22-2011
20100234396Tetrhydropyridoindole Derivatives - The invention relates to tetrahydropyridoindole derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions comprising one or more of those compounds and methods of treatment comprising administration of said compounds.09-16-2010
20120277251ANALOGS OF DEHYDROPHENYLAHISTINS AND THEIR THERAPEUTIC USE - Compounds represented by the following structure (II) are disclosed:11-01-2012
20100204245Amino-pyridines As Inhibitors Of Beta-secretase - The present invention provides an amino-pyridine compound of formula I08-12-2010
20120329811Heteroaromatic Derivatives and their use as positive allosteric modulators of metabotropic glutamate receptors - The present invention relates to novel compounds of Formula (I), wherein X12-27-2012
20110319425HETEROTRICYCLIC COMPOUNDS AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to novel compounds of Formula (I), wherein X12-29-2011
20120101111NOVEL OXAZOLIDINONE DERIVIATIVES - The present invention relates to oxazolidinone derivatives of formula (I) wherein Y, R04-26-2012
20090118305PYRIDINE AND PYRAZINE DERIVATIVES - 083 - The invention concerns pyridine and pyrazine derivatives of Formula I05-07-2009
20120101110Diaza-spiro[5.5]undecanes - The invention relates to compound of the formula I04-26-2012
20120289520CHEMICAL COMPOUNDS 785 - DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity11-15-2012
20120142706SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT - Substituted cyclopropyl compounds of the formula I: are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.06-07-2012
20100168131NOVEL COMPOUNDS - Disclosed are N-{[(1S,4S,6S)-3-(2-pyridinylcarbonyl)-3-azabicyclo [4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives and their use as pharmaceuticals.07-01-2010
20100168132QUINUCLIDINE DERIVATIVES AND THEIR USE AS MUSCARINIC M3 RECEPTOR ANTAGONISTS - Compounds of Formula (I) ; in salt or zwitterionic form wherein R07-01-2010
20100130510COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES - The invention relates to certain compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.05-27-2010
20130023543HUMAN PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE - The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-β) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-β) inhibitors, and to methods for regulating angiogenesis.01-24-2013
20080255153New compounds - The present invention relates to compounds of formula (I):10-16-2008
20080227794Metabotropic Glutamate-Receptor-Potentiating Isoindolones - Compounds of formula I:09-18-2008
20080214574Inhibition of the Activity of the Capsaicin Receptor in the Treatment of Obesity or Obesity-Related Diseases and Disorders - The present invention provides a method of treating diseases or disorders benefiting from inactivating or down regulating the activity of the capsaicin receptor in a mammal by inhibiting the activity of the capasaicin receptor.09-04-2008
20080214573Compounds Useful for Inhibiting Chk1 - Substituted urea compounds useful in the treatment of diseases and C09-04-2008
20130096139Compounds Useful as Inhibitors of ATR Kinase - The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.04-18-2013
20130096140HUMAN PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE - The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-β) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-β) inhibitors, and to methods for regulating angiogenesis.04-18-2013
201301026183-AMINO-5,6-DIHYDRO-1H-PYRAZIN-2-ONE DERIVATIVES USEFUL FOR THE TREATMENT OF ALZHEIMER'S DISEASE AND OTHER FORMS OF DEMENTIA - The present invention relates to novel 3-amino-5,6-dihydro-1H-pyrazin-2-one derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid.04-25-2013
20130102617METHOD OF TREATING DIABETES, METABOLIC SYNDROME AND OBESITY USING PHENYLACETAMIDE DERIVATIVE - Phenylacetamide compounds of the formula04-25-2013
20130203774NOVEL COMPOUNDS, USE AND PREPARATION THEREOF - The present invention relates to compounds of the general formula (I) wherein R08-08-2013
20130143899COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds of Formula (I) (wherein A, Y, R06-06-2013
20080207641CYCLOHEXENYL-ARYL COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES - The invention relates to compounds of structural formula (I):08-28-2008
201301580497-AZAINDOLE INHIBITORS OF CRAC - Disclosed are compounds of Formula (I):06-20-2013
20080200476ALAPHATIC PYRAZINOYLGUANIDINE SODIUM CHANNEL BLOCKERS - The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.08-21-2008
20110224229Novel Crystalline Form - Crystalline Forms of 6-[2-(4-cyano-phenyl)-2H-pyrazol-3-yl]-5-methyl-3-oxo-4-(3-trifluoromethyl-phenyl)-3,4-dihydro-pyrazine-2-carboxylic acid ethylamide are disclosed together with processes for preparing the Forms, pharmaceutical compositions comprising the Forms, and the use of the Forms in therapy.09-15-2011
20110312976NOVEL ISOINDOLIN-1-ONE DERIVATIVE - The present invention relates to a compound represented by formula (I): (wherein R, R12-22-2011
20130150376Novel Sultam Compounds - Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.06-13-2013
20100286170(3-HYDROXY-4-AMINO-BUTAN-2-YL) -3- (2-THIAZOL-2-YL-PYRROLIDINE-1-CARBONYL) BENZAMIDE DERIVATIVES AND RELATED COMPOUNDS AS BETA-SECRETASE INHIBITORS FOR TREATING - The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating of Alzheimer's disease.11-11-2010
20100286168COMBINATION THERAPY FOR THE TREATMENT OF DIABETES AND CONDITIONS RELATED THERETO AND FOR THE TREATMENT OF CONDITIONS AMELIORATED BY INCREASING A BLOOD GLP-1 LEVEL - The present invention concerns combination of an amount of a GPR119 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-1 level in a subject over that provided by the amount of the GPR119 agonist or the amount of the DPP-IV inhibitor alone and the use of such a combination for treating or preventing diabetes and conditions related thereto or conditions ameliorated by increasing a blood GLP-1 level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-1 secretagogues.11-11-2010
20110312975CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS - Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of neuromuscular disorders, conditions having muscle wasting, claudication, frailty, metabolic syndrome, muscle atrophy associated with disuse, and muscle fatigue, and other indications.12-22-2011
20110312974HETEROARYL ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS - Described herein are compounds that are antagonists of PGD12-22-2011
20110312973SOLID COMPOSITIONS - The present invention features solid compositions comprising amorphous Compound I. A solid dispersion of the present invention also contains a pharmaceutically acceptable hydrophilic polymer and a pharmaceutically acceptable surfactant. Compound I may be formulated in an amorphous solid dispersion which comprises a pharmaceutically acceptable hydrophilic polymer and preferably a pharmaceutically acceptable surfactant.12-22-2011
20100317674Metabotropic Glutamate-Receptor-Potentiating Isoindolones - Compounds of formula I:12-16-2010
20100317673N-HETEROCYCLIC-IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION - Compounds of formula (I):12-16-2010
20120283272COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES - The invention relates to certain compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.11-08-2012
20120283271ISOINDOLINONE DERIVATIVES - The present invention relates to compounds of the formula I,11-08-2012
20130184292Processes for Making Compounds Useful as Inhibitors of ATR Kinase - The present invention relates to processes and intermediates for preparing compounds useful as inhibitors of ATR kinase, such as aminopyrazine-isoxazole derivatives and related molecules. The present invention also relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention.07-18-2013
20130123275PYRAZINE DERIVATIVES - The invention concerns pyrazine derivatives of the Formula I05-16-2013
20130123276USE OF TELAPREVIR AND RELATED COMPOUNDS IN ATHEROSCLEROSIS, HEART FAILURE, RENAL DISEASES, LIVER DISEASES OR INFLAMMATORY DISEASES - Use of Telaprevir and related compounds in atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases.05-16-2013
20110294827IAP BINDING COMPOUNDS - IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPs (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a K12-01-2011
20130190328PYRIDO[4,3-B]INDOLES AND METHODS OF USE - New heterocyclic compounds that may be used to modulate a histamine receptor in an individual are described. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.07-25-2013
20130190329PEST CONTROLLING COMPOSITION AND METHOD FOR CONTROLLING PEST - The present invention provides a composition having an excellent controlling activity on a pest. The composition comprising a compound represented by Formula (1) and one or more 1-(2,6-dichloro-α,α,α-trifluoroparatol)pyrazole compound(s) selected from Group (A) shows an excellent controlling activity on a pest. Group (A): a group consisting of acetoprole, ethiprole, fipronil, vaniliprole, pyriprole and pyrafluprole07-25-2013
20110319426Substituted Isoindoles - The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.12-29-2011
20110319424NAPHTHYRIDIN-2(1H) -ONE COMPOUNDS USEFUL AS ANTIBACTERIALS - Compounds of Formula (I),12-29-2011
20120095022DERIVATIVES OF 10-AMINO-1,2,3,4-TETRAHYDROPYRIDO[2,1-A]ISOINDOL-6(10BH)-ONES, METHOD FOR PREPARATION THEREOF AND THERAPEUTIC USES THEREOF - The present invention relates to compounds having the following general formula (I):04-19-2012
20120095021SYNTHSIS OF NEW BENZOTHIAZOLE DERIVATIVES AS POTENTIAL ANTI-TUBERCULAR AGENTS - The present disclosure provides a compound of general formula A useful as potential anti-tubercular agents.04-19-2012
20130210837Compounds and Their Use as BACE Inhibitors - The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.08-15-2013

Patent applications in class Additional hetero ring attached directly or indirectly to the 1,4-diazine ring by nonionic bonding