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Ring nitrogen in the bicyclo ring system

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

514228800 - Hetero ring is six-membered and includes at least nitrogen and oxygen as ring hetero atoms (e.g., monocyclic 1,2- and 1,3-oxazines, etc.)

514231200 - Morpholines (i.e., fully hydrogenated 1,4- oxazines)

514231500 - Additional hetero ring attached directly or indirectly to the morpholine ring by nonionic bonding

514232800 - Polycyclo ring system having the additional hetero ring as one of the cyclos

514233500 - Bicyclo ring system having the additional hetero ring as one of the cyclos

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Entries
DocumentTitleDate
20130045976ISOINDOLINE COMPOUNDS AND METHODS OF THEIR USE - Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases.02-21-2013
20130045975BICYCLIC HETEROARYL INHIBITORS OF PDE4 - The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.02-21-2013
20100063048Remedy for angiospasm accompanying subarachnoid hemorrhage containing thrombin receptor antagonist as the active ingredient - A therapeutic agent for subarachnoid hemorrhage or a drug for improving prognosis of subarachnoid hemorrhage, comprising a compound having a PAR1 inhibitory effect, its pharmaceutically acceptable salt or a hydrate thereof03-11-2010
20110178084THERAPEUTIC COMPOUNDS - Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof are disclosed, wherein a dashed line represents the presence or absence of a bond; and, wherein Y, A, R, D, and n are as described. Methods, compositions, and medicaments related thereto are also disclosed.07-21-2011
20120202810SUBSTITUTED 4-AMINOCYCLOHEXANE DERIVATIVES - The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.08-09-2012
201300299863-(INDOLYL)- OR 3-(AZAINDOLYL)- 4-ARYLMALEIMIDE DERIVATIVES FOR USE IN THE TREATMENT OF COLON AND GASTRIC ADENOCARZINOMA - The present invention relates to the use of a compound of formula (I) wherein R01-31-2013
201000163091,2,3,4-Tetrahydroisoquinoline Derivatives, Preparation Process therefor and Pharmaceutical Composition Containing the Same - The invention provides a type of novel 1,2,3,4-tetrahydroisoquinoline derivatives with a structure of formula (I):01-21-2010
20100016314DERIVATIVES OF AZABICYCLO OCTANE, THE METHOD OF MAKING THEM AND THE USES THEREOF AS INHIBITORS OF DIPEPTIDYL PEPTIDASE IV - Derivatives of azabicyclo octane presented by formula (I), the method of making them, and the compositions containing the same and the uses thereof as inhibitors of dipeptidyl peptidase IV (DPP-IV), wherein the substitutes in formula (I) have the same meanings as what is mentioned in the descriptions.01-21-2010
20120184548CARBOXYLIC ACID ARYL AMIDES - Compounds of formula07-19-2012
20100152184PHARMACEUTICAL COMPOUNDS - The invention provides a compound for use in medicine, the compound being a compound of the formula (VI06-17-2010
20090192157INDOLE COMPOUNDS AND METHODS FOR TREATING VISCERAL PAIN - The invention features methods of treating visceral pain or a condition in a mammal caused by the action of nitric oxide synthase (NOS) or by the action of serotonin 5HT1D/1B receptors, by administering to a patient in need thereof a therapeutically effective amount of an indole compound of Formula (I), or a pharmaceutically acceptable salt or prodrug thereof. The methods of the invention may further comprise the administration of additional therapeutic agent. The invention also features new compounds of Formula (I), pharmaceutical compositions thereof, and methods of resolving enantiomeric mixtures.07-30-2009
200802750408-(1-Piperazinyl)-Quinoline Derivatives and Their Use in the Treatment of Cns Disorders - This invention relates to novel quinoline compounds having pharmacological activity, to processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.11-06-2008
20100075963Pharmaceutically Active Benzensulphonyl-Indols - 1-Benzenesulfonyl-1H-indoles, processes for their production and their use as pharmaceuticals, e.g. in the treatment of disorders which are mediated by CCR9, such as e.g. inflammatory bowel disease.03-25-2010
20100075962INDOL DERIVATIVES, THE METHOD FOR PREPARING THEREOF AND COMPOSITION FOR THE PREVENTION AND TREATMENT OF METABOLIC DISORDER CONTAINING THE SAME AS AN ACTIVE INGREDIENT - Disclosed are indole derivatives a preparation method thereof, and a composition for the prevention and treatment of metabolic diseases, containing the same as an active ingredient. The indole derivatives have inhibitory activity against DGAT (diacylglycerol acyltransferase), which causes metabolic diseases such as obesity and diabetes in the process of lipid metabolism. With the ability to effectively control lipid metabolism and energy metabolism, the composition is thus useful in the prevention and treatment of metabolic diseases, such as obesity and diabetes.03-25-2010
20130137686BENZENE, PYRIDINE, AND PYRIDAZINE DERIVATIVES - Disclosed are compounds and pharmaceutically acceptable salts of Formula I05-30-2013
201300793431,3,6-Substituted Indole Derivatives Having Inhibitory Activity for Protein Kinase - Disclosed are a 1,3,6-substituted indole compound having inhibitory activity for protein kinases, a pharmaceutically acceptable thereof, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth including the compound as an active ingredient.03-28-2013
20090163492Substituted Oxindole Derivatives, Drugs Containing Said Derivatives and the Use Thereof - The invention relates to novel oxindol derivative of general formula (I), wherein substituents R06-25-2009
20100099673DECAHYDROQUINOLINE ANALOGS AS CB2 RECEPTOR MODULATORS, USEFUL IN THE TREATMENT OF PAIN, RESPIRATORY AND NON-RESPIRATORY DISEASES - The present invention relates to compounds represented by Formula (I): and pharmaceutically acceptable salts thereof. The present invention also provides pharmaceutical compositions comprising the instant compounds. This invention further provides methods to treat and prevent pain, respiratory and non-respiratory diseases.04-22-2010
20100056518CYCLOALKYLAMINE SUBSTITUTED ISOQUINOLONE DERIVATIVES - The invention relates to 6-substituted isoquinolone derivatives of the formula (I)03-04-2010
20100041652TYROSINE KINASE INHIBITORS - The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises an indole-sulfonamide moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.02-18-2010
20090156600Quinolines and Their Therapeutic Use - Compounds of formula [1] are CRTH2 antagonists, useful in the treatment of conditions having an inflammatory component; in which: R06-18-2009
201001056812,6-QUINOLINYL AND 2,6-NAPHTHYL DERIVATIVES, PROCESSES FOR PREPARING THEM AND THEIR USES AS VLA-4 INHIBITORS - The present invention concerns 2,6-quinolinyl and 2,6-naphthyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.04-29-2010
20100105680SUBSTITUTED DIMETHYLCYCLOBUTYL COMPOUNDS, THEIR PREPARATION AND USE IN MEDICAMENTS - The present invention relates to substituted dimethylcyclobutyl compounds of general formula I, a process for their preparation, medicaments comprising said substituted dimethylcyclobutyl compounds as well as the use of said substituted dimethylcyclobutyl compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via sigma receptors.04-29-2010
20090124617QUINOLONE DERIVATIVE OR SALT THEREOF - A platelet aggregation inhibitor comprising a quinolone derivative or a pharmaceutically acceptable salt thereof as an active ingredient, and a novel quinolone derivative or a pharmaceutically acceptable salt thereof useful as a platelet aggregation inhibitor.05-14-2009
200901246167-NONSUBSTITUTED INDOLE MCL-1 INHIBITORS - Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.05-14-2009
20090042881SUBSTITUTED 6-CYCLOHEXYLALKYL SUBSTITUTED 2-QUINOLINONES AND 2-QUINOXALINONES AS POLY(ADP-RIBOSE) POLYMERASE INHIBITORS - The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I)02-12-2009
20090312324Compositions and Methods Related to RAD51 Inactivation in the Treatment of Neoplastic Diseases, and Especially CML - Chronic myelogenous leukemia (CML), and in particular imatinib resistant CML is treated using compositions and methods in which a Rad51-inhibitor and a kinase inhibitor are administered. Most preferably, the Rad51 inhibitor comprises an indolyl isoquinoline structure and the kinase inhibitor is a BCR-ABL inhibitor.12-17-2009
20090306073Thiazole and Thiophene Analogues, and Their Use in Treating Autoimmune Diseases and Cancers - Thiazole and thiophene compounds are disclosed having utility in treating inflammatory conditions, immunoinflammatory conditions, autoimmune diseases, and cancers. Methods for the synthesis of these compounds are also disclosed.12-10-2009
20090306074THIAZOLIDINEDIONE DERIVATIVES AS P13 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using thiazolidinedione derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of thiazolidinedione derivatives.12-10-2009
20130072485SOLUBLE MTOR COMPLEXES AND MODULATORS THEREOF - The present invention relates to small molecule modulators of mTORC1 and mTORC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, autoimmune diseases, diabetic retinopathy) and metabolic diseases. Novel small molecules are provided that inhibit one or more of mTORC1, mTORC2, and PI3K-related proteins. Novel methods of providing soluble mTORC1 and mTORC2 complexes are discussed, as well as methods of using the soluble complexes in a high-throughput manner to screen for inhibitory compounds.03-21-2013
20110059967THERAPEUTIC COMPOUNDS - Compounds comprising Formula (I) or a pharmaceutically acceptable salt thereof, are disclosed, wherein J03-10-2011
20110059966INDOLE DERIVATIVES AS HISTAMINE 3 RECEPTOR INHIBITORS FOR THE TREATMENT OF COGNITIVE AND SLEEP DISORDERS, OBESITY AND OTHER CNS DISORDERS - This invention relates to compounds having pharmacological activity, to compositions containing these compounds, and to a method of treatment employing the compounds and compositions. More particularly, this invention concerns certain indole derivatives and their salts and solvates. These compounds have H03-10-2011
20130059851Methods of Diagnosing and Treating Cancer in Patients Having or Developing Resistance to a First Cancer Therapy - A method of identifying a subject having cancer who is likely to benefit from treatment with a combination therapy with a RAF inhibitor and a second inhibitor is provided. A method of treating cancer in a subject in need thereof is also provided and includes administering to the subject an effective amount of a RAF inhibitor and an effective amount of a second inhibitor, wherein the second inhibitor is a MEK inhibitor, a CRAF inhibitor, a CrkL inhibitor or a TPL2/COT inhibitor. A method of identifying a kinase target that confers resistance to a first inhibitor is also provided.03-07-2013
20090291950BICYCLIC HETEROARYL INHIBITORS OF PDE4 - The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PD E4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.11-26-2009
20090270391THIENOPYRIDINE DERIVATIVE, OR QUINOLINE DERIVATIVE, OR QUINAZOLINE DERIVATIVE, HAVING c-MET AUTOPHOSPHORYLATION INHIBITING POTENCY - An objective of the present invention is to provide compounds having antitumor activity. According to the present invention, there is provided compounds represented by formula (I) and pharmaceutically acceptable salts thereof, and solvates thereof:10-29-2009
201000693845-ALKYLOXY-INDOLIN-2-ONE DERIVATIVES, PREPARATION THEREOF AND APPLICATION THEREOF IN THERAPY - The present invention relates to derivatives of 5-alkyloxy-indolin-2-one, their method of production and their therapeutic applications. These novel derivatives have affinity and selectivity for the V03-18-2010
20130065897COMPOUNDS, PREPARATION AND USES THEREOF - The present invention provides novel compounds of the Formula I, pharmaceutical compositions comprising such compounds and methods for using such compounds as agents or drugs for inhibiting perforin activity and for treating a subject at risk of or susceptible to a disease or disorder, or having a disease or disorder associated with undesirable perforin activity.03-14-2013
20120115866KINASE INHIBITOR COMPOUNDS - The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.05-10-2012
20090012085DOSAGE FORMS AND METHODS OF TREATMENT USING A TYROSINE KINASE INHIBITOR - This invention provides dosage forms of a compound of formula 1, 5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, or pharmaceutically acceptable salts or solvates thereof. The invention further provides methods of treating abnormal cell growth in a patient, such as cancers, by administering the dosage forms to the patient. The invention further provides methods of treating an angiogenesis- or VEGF-related ophthalmic disorder in a patient, by administering the dosage form to the patient.01-08-2009
20120238573PRODRUGS OF [4 [4-(5-AMINOMETHYL-2-FLUORO-PHENYL)-PIPERIDIN-1-YL]-(1H-PYRROLO-PYRIDIN-YL- )-METHANONES AND SYNTHESIS THEREOF - The present invention relates to substituted 2-amino-N-(4-fluoro-3-{1-[1-(alkyl)-1H-indole-3-carbonyl]-piperidin-4-yl}-benzyl)-acetamides (compounds of formula I)09-20-2012
20120238572USE OF SUBSTITUTED QUINAZOLINE COMPOUNDS IN TREATING ANGIOGENESIS-RELATED DISEASES - Quinazoline derivatives of the following formula:09-20-2012
20130165442Modulators of ATP-Binding Cassette Transporters - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.06-27-2013
20090088429Isoquinoline Derivatives - The invention relates to 6-piperidinyl-substituted isoquinoline derivatives of the formula (I)04-02-2009
20080255115THIAZOLIDINEDIONE DERIVATIVES AS PI3 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using thiazolidinedione derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of thiazolidinedione derivatives.10-16-2008
20100004240Indole Compounds - Compounds of Formula (I) or a pharmaceutically acceptable derivative thereof: wherein R01-07-2010
20110034460Dihydroindolone compounds, a process for their preparation and pharmaceutical compositions containing them - Compounds of formula (I):02-10-2011
20110281869TETRAHYDROISOQUINOLINES AS ANTIMALARIAL AGENTS - The invention relates to novel tetrahydroisoquinoline derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria.11-17-2011
20110281870NOVEL SUBSTITUTED OCTAHYDROCYCLOPENTA[C]PYRROL-4-AMINES AS CALCIUM CHANNEL BLOCKERS - The present application relates to calcium channel inhibitors containing compounds of formula (I)11-17-2011
20110301163QUINOLINE COMPOUNDS AS INHIBITORS OF ANGIOGENESIS, HUMAN METHIONINE AMINOPEPTIDASE, AND SIRT1, AND METHODS OF TREATING DISORDERS - Described herein are methods of inhibiting methionine aminopeptidase or SirT1, inhibiting angiogenesis, and treating disorders (or symptoms thereof) associated with methionine aminopeptidase, SirT1 and/or angiogenesis, wherein a compound of the invention is administered to a subject.12-08-2011
20110294809TROPANE UREA DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATION THEREOF AS MODULATORS OF THE ACTIVITY OF 11BETAHSD1 - The invention relates to tropane urea derivatives of general formula (I) and to the application thereof as modulators of the activity of 11β-hydroxysteroid dehydrogenose type 1 (11βHSD1).12-01-2011
20080249091Indoles Useful in the Treatment of Inflammation - There is provided compounds of formula I,10-09-2008
20100022536Inhibitors of Cytosolic Phospholipase A2 - This invention provides chemical inhibitors of the activity of various phospholipase enzymes, particularly cytosolic phospholipase A01-28-2010
20090062280Ophthalmic Compositions for Treating Ocular Hypertension - This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.03-05-2009
20100029645Inhibitors of Cytosolic Phospholipase A2 - This invention provides chemical inhibitors of the activity of various phospholipase enzymes, particularly cytosolic phospholipase A02-04-2010
20090099180INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 - The present invention discloses novel compounds of Formula (I): having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity.04-16-2009
20090099179COMPOUNDS FOR DISEASES AND DISORDERS - The invention provides novel compounds useful for the treatment of disorders associated with a defect in vesicular transport (e.g., axonal transport). The compounds have a substituents chosen from -L-C(═O)OH, -L-CH═CHC(═O)OH, -L-C(═O)NH04-16-2009
20100113443LIQUID FORMULATIONS OF PHOSPHOLIPASE ENZYME INHIBITORS - The present invention relates to liquid formulations of inhibitors of phospholipase enzymes, such as cytosolic PLA05-06-2010
20090149460New Compounds - The present invention provides new compounds of formula Ia and Ib:06-11-2009
20100267719Enhanced Indolinone Based Protein Kinase Inhibitors - Alpha-hydroxy-omega-(2-oxo-indolylidenemethyl-pyrrole-3′-carbonyl)amino alkanoic acid and amide derivatives have enhanced and unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.10-21-2010
20110028474PROTEIN KINASE AND PHOSPHATASE INHIBITORS - The present invention provides a method for identifying inhibitors of protein kinases and/or protein phosphatases. Methods are also provided for inhibiting protein kinase and/or protein phosphatase activity. Specific non-peptide protein tyrosine kinase and/or protein phosphatase inhibitors are provided. The protein kinase or protein phosphatase inhibitors of the present invention may be used to treat a number of conditions in patients, including cancer, psoriasis, arthrosclerosis, immune system activity, Type II diabetes, and obesity.02-03-2011
20090170849QUINAZOLINONE DERIVATIVES HAVING B-RAF INHIBITORY ACTIVITY - The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.07-02-2009
20090163494PROTEIN KINASE INHIBITORS - This invention relates to selenophene compounds of formula (I) shown below:06-25-2009
20090291949SUBSTITUTE ISOQUINOLINES USEFUL IN THE TREATMENT OF DISEASES SUCH AS CANCER AND ATHEROSCLEROSIS - A compound of Formula (I):11-26-2009
20080207617Quinoline Derivatives and Quinazoline Derivatives Inhibiting Autophosphrylation of Flt3 and Medicinal Compositions Containing the Same - An objective of the present invention is to provide compounds and pharmaceuticals useful for the treatment of disease where the inhibition of autophosphorylation of FMS-like tyrosine kinase 3(Flt3) is therapeutically effective. The present invention relates to a pharmaceutical composition for use in the treatment or prevention of diseases where the inhibition of autophosphorylation of Flt3 therapeutically or prophylactically effective, which comprises a compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof:08-28-2008
200902755803-SPIROINDOLIN-2-ONE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - The subject of the present invention is a compound of formula (I):11-05-2009
20090286785Pyrimidine Derivatives - This invention relates to novel compounds (I) and processes for their preparation, methods of treating diseases, particularly cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly cancer.11-19-2009
20090042882SUBSTITUTED ACETAMIDES AS MODULATORS OF THE EP2 RECEPTOR - The present invention relates to substituted acetamides of the general formula I, process for their preparation, and the use thereof for the manufacture of pharmaceutical compositions for the treatment of disorders and indications connected with the EP02-12-2009
20090298825Bicycloheteroaryl Compounds as P2x7 Modulators and Uses Thereof - Bicycloheteroaryl compounds are disclosed that have a formula represented by the following: Formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.12-03-2009
201002223464-BENZYLAMINOQUINOLINES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY - The present invention relates to 4-benzylaminoquinolines of the formula (I) or physiologically tolerated salts thereof. The invention relates to pharmaceutical compositions comprising such quinolines, and the use of such quinolines for therapeutic purposes. The quinolines are GIyTI inhibitors.09-02-2010
20120289505INHIBITORS OF DIACYLGLYCEROL ACYL TRANSFERASE - The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.11-15-2012
20100298324Prolyl Hydroxylase Inhibitors - The invention described herein relates to certain 4-oxo-2-thioxo-1,2,3,4-tetrahydro-7-quinazolinecarboxamide derivatives of formula (I)11-25-2010
200802750413-Heterocyclyl-Indole Derivatives as Inhibitors of Glycogen Synthase Kinase-3 (Gsk-3) - Compounds of formula Ia or Ib11-06-2008
200802750424-Phenyl-5-Oxo-1,4,5,6,7,8-Hexahydroquinoline Derivatives for the Treatment of Infertility - The present invention relates to 4-phenyl-5-oxo-1,4)5,6,7,8-hexahydroquinoline derivatives according to Formula I, Formula I or a pharmaceutically acceptable salt thereof, wherein R11-06-2008
20080312233Therapeutic Morpholino-Substituted Compounds - Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation. The compounds are useful in treating PI 3-kinase-dependent conditions including cardiovascular diseases such as coronary artery occlusion, stroke, acute coronary syndrome, acute myocardial infarction, vascular restenosis, atherosclerosis, and unstable angina; respiratory diseases such as asthma, chronic obstructive pulmonary diseases (COPD), and bronchitis; inflammatory disorders; neoplasms including cancers such as glioma, prostate cancer, small cell lung cancer, and breast cancer; and diseases linked to disordered white blood cell function, such as autoimmune and inflammatory diseases.12-18-2008
20080312232Substituted amide derivatives and methods of use - Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.12-18-2008
200802692138-Hydroxyquinoline compounds and methods thereof - The present invention relates to 8-Hydroxyquinoline Compounds; compositions comprising an 8-Hydroxyquinoline Compound; and methods for treating or preventing a metalloproteinase-related disorder, such as, an arthritic disorder, osteoarthritis, malignant neoplasm, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, atherosclerosis, age-related macular degeneration, myocardial infarction, a corneal ulceration, an ocular surface disease, hepatitis, an aortic aneurysm, tendonitis, a central nervous system disorder, abnormal wound healing, angiogenesis, restenosis, cirrhosis, multiple sclerosis, glomerulonephritis, graft versus host disease, diabetes, an inflammatory bowel disease, shock, invertebral disc degeneration, stroke, osteopenia or a periodontal disease or comprising administering an effective dose of an 8-Hydroxyquinoline Compound to a mammal in need thereof.10-30-2008
20080269212Amino acid derivatives of indolinone based protein kinase inhibitors - Amino acid derivatives of pyrrolyl-indolinones and their amide or ester derivatives have enhanced and unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.10-30-2008
200902644273-Cyanoquinolines, Methods for Preparation and Use as Insulin-like Growth Factor Inhibitors - Imidazole-substituted 4-anilino-3-cyanoquinolines are described, which selectively inhibit IFGR kinase activity and are useful for treating disorders associated with IGFR kinases.10-22-2009
20090264426Bicyclic aromatic substituted pyridone derivative - Disclosed is a compound represented by the formula (I):10-22-2009
20090264425CHEMICAL COMPOUNDS - This invention relates to biaryl ether derivatives of formula (I)10-22-2009
20090298826NOVEL 1,2-DIHYDROQUINOLINE DERIVATIVE HAVING (SUBSTITUTED PHENYL OR SUBSTITUTED HETEROCYCLIC) CARBONYLOXY LOWER ALKYL GROUP AND ESTER-INTRODUCED PHENYL GROUP AS SUBSTITUENTS - The compounds represented in general formula (1) and a salt thereof are useful for glucocorticoid receptor modulator.12-03-2009
20090054434ISOQUINOLONE DERIVATIVES AS PHOSPHODIESTERASE 10 INHIBITORS - The present invention is directed to certain isoquinolin-1(2H)-one compounds, useful as PDE10 inhibitors, having the formula:02-26-2009
20090181966PGD2 receptor antagonists for the treatment of inflammatory diseases - Disclosed herein are compounds represented by Structural Formula (I) and (I-A):07-16-2009
20090163495MORPHOLIN-ACETAMIDE DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISEASES - There are provided according to the invention, novel compounds of formula (I)06-25-2009
20090143382FLUOROALKOXY-SUBSTITUTED 1,3-DIHYDRO-ISOINDOLYL COMPOUNDS AND THEIR PHARMACEUTICAL USES - The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4.06-04-2009
20090137586COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS - This invention relates to compounds of the Formula (I):05-28-2009
200902755793-SPIROINDOLIN-2-ONE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - The subject of the present invention is a compound of formula (I):11-05-2009
20090275578Isoindolone compounds and their use as metabotropic glutamate receptor potentiators - The present invention is directed to compounds of formula I:11-05-2009
20090143381MODULATORS OF ATP-BINDING CASSETTE-TRANSPORTERS - Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.06-04-2009
20090062279HETEROCYCLIC COMPOUNDS, THEIR PREPARATION AND THEIR USE AS MEDICAMENTS, IN PARTICULAR AS ANTI-ALZHEIMER AGENTS - The invention is related to compound which comprises at least one radical C═Y, Y being O or S, and an oxidable and non protonable nitrogen atom N wherein the distance (d) between the at least one carbon atom of the radical group C═Y and the nitrogen atom, when oxidized, is comprised between 0.3 and 0.8 nanometers. The invention is related to new heterocyclic compounds defined by formula G, their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of neurodegenerative or Alzheimer disease.03-05-2009
20130217685COMPOUNDS FOR MODULATING RNA BINDING PROTEINS AND USES THEREFOR - The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders.08-22-2013
20090023729Trisubstituted amine compound - The present invention relates to a compound of the general formula (1):01-22-2009
200900237281,2,3,4-Tetrahydroisoquinoline Derivatives, Preparations Thereof and Uses Thereof - Compounds of general formula (I) wherein D, E, R01-22-2009
20110224208NOVEL INHIBITORS OF FLAVIVIRUS REPLICATION - The present invention relates to a series of Isoquinolone derivatives which are suitable to treat infections with viruses belonging to the family of the Flaviviridae and more preferably infections with Hepatitis C virus (HCV). The present invention also relates to Isoquinolone compounds for use as a medicine for the prevention or treatment of viral infections, preferably infections with viruses belonging to the family of the Flaviviridae.09-15-2011
20110224206TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted pyrrole compounds of formula I and compositions comprising substituted tri-substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a tri-substituted’ triazole compound of the invention, or a pharmaceutical composition comprising such a compound.09-15-2011
20090069321CYANOMETHYL SUBSTITUTED N-ACYL TRYPTAMINES - The present invention relates to cyanomethyl substituted N-acyl tryptamines of the formula I03-12-2009
200901052483-MONOSUBSTITUTED TROPANE DERIVATIVES AS NOCICEPTIN RECEPTOR LIGANDS - Compounds of the formula04-23-2009
20080318952DIARYL-SUBSTITUTED TETRAHYDROISOQUINOLINES AS HISTAMINE H3 RECEPTOR AND SEROTONIN TRANSPORTER MODULATORS - Certain diaryl-substituted tetrahydroisoquinoline compounds are histamine H12-25-2008
20090221576Pharmaceutical Use of 2-Hydroxy-3-[5-(Morpholin-4-Ylmethyl) Pyridin-2-YL]-1H-IN-Dole-5-Carbonitrile as a Free Base or Salts - New use of 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]1H-indole-5-carbonitrile as a free base or a pharmaceutically acceptable salt thereof, in a method of prevention and/or treatment of bone-related disorders, osteoporosis, increasing bone formation or increasing bone mineral density.09-03-2009
20090221575Sulfonamide derivatives and use thereof for the modulation of metalloproteinases - The present invention is related to sulfonamide derivatives of Formula (Ia)09-03-2009
200902398631-ARYL-OR 1- ALKYLSULFONYLBENZAZOLE DERIVATIVES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS - The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.09-24-2009
20110144106NOVEL CYCLOPROPANE INDOLINONE DERIVATIVES - The present invention relates to a compound of formula (I)06-16-2011
200902215745-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.09-03-2009
20100009986SUBSTITUTED HETEROARYL DERIVATIVES - The invention relates to substituted heteroaryl derivatives, to methods for the production thereof, to medicaments containing said compounds and to the use of substituted heteroaryl derivatives for producing medicaments.01-14-2010
20100152185DIPHENYL SUBSTITUTED CYCLOALKANES, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE - The instant invention provides compounds of formula I which are 5-lipoxygenase activating protein inhibitors.06-17-2010
20100016311NOVEL MINOR GROOVE BINDERS - There is provided compounds of formula (I), wherein R01-21-2010
20090018133Novel Adamantane Derivatives - The invention provides compounds of formula (I), in which m, A, R01-15-2009
20090048254SALTS AND POLYMORPHS OF A VEGF-R INHIBITOR - The invention relates to salts and free base forms of N,2-dimethyl-6-[7-(2-morpholinoethoxy)quinolin-4-yloxy]benzofuran-3-carboxamide. The invention further relates to pharmaceutical compositions of these salts and free base forms and methods of treating disorders such as cancer using such compositions.02-19-2009
20100184762PHTHALIMIDE DERIVATIVES THAT INFLUENCE CELLULAR VESICULAR SYSTEMS, PHARMACEUTICAL COMPOSITIONS, AND USE THEREOF - The present invention relates to compounds that are suitable for treatment of disease states and influence cellular vesicular systems, especially the formation and/or function of lipid droplets, said compound having the general formula I (I) wherein X are each independently hydrogen, halogen, —C07-22-2010
20090298827NOVEL 1,2-DIHYDROQUINOLINE DERIVATIVE HAVING SUBSTITUTED PHENYLAMINO LOWER ALKYL GROUP AND ESTER-INTRODUCED PHENYL GROUP AS SUBSTITUENTS - The compounds represented in general formula (1) and a salt thereof are useful for glucocorticoid receptor modulator.12-03-2009
20100197687Indoles Useful in the Treatment of Inflammation - There is provided compounds of formula I,08-05-2010
20110059965BICYCLIC DERIVATIVES AS MODULATORS OF ION CHANNELS - Bicyclic derivatives having formula (I) and a composition thereof are useful as ion channel antagonists:03-10-2011
20110059964PYRAZOLE DERIVATIVES AND USE THEREOF AS OREXIN RECEPTOR ANTAGONISTS - The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.03-10-2011
20100204227ISOINDOLINE COMPOUNDS AND METHODS OF THEIR USE - Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases.08-12-2010
20120142687INDOLECARBOXYLIC ACID DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONISTIC ACTIVITY - The present invention provides an indolecarboxylic acid derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. 06-07-2012
20100240651WATER-SOLUBLE THALIDOMIDE DERIVATIVES - A compound of formula (I),09-23-2010
20100240650SUBSTITUTED PYRROLINES AS KINASE INHIBITORS - The present invention is directed to novel substituted pyrroline compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.09-23-2010
20100234372SUBSTITUTED 2-MERCAPTOQUINOLINE-3-CARBOXAMIDES AS KCNQ2/3 MODULATORS - The invention relates to substituted 2-mercaptoquinoline-3-carboxamides, methods for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.09-16-2010
200903184464-(1H-Indol-3-yl)-Pyrimidin-2-Ylamine Derivatives and Their Use in Therapy - The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts thereof. The present invention seeks to provide further substituted heteroaryl-substituted pyrimidine derivatives. More specifically, the invention relates to compounds that have broad therapeutic applications in the treatment of a number of different diseases and/or that are capable of inhibiting one or more protein kinases.12-24-2009
20090076005Kinase inhibitor compounds - The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.03-19-2009
20090076004Indoles Useful in the Treatment of Inflammation - There is provided compounds of formula (I), wherein X03-19-2009
201002106462-MORPHOLIN-4-YL-PYRIMIDINES AS PI3K INHIBITORS - The invention provides a pyrimidine compound of formula (I):08-19-2010
20100210647INDOLE COMPOUNDS AS AN INHIBITOR OF CELLULAR NECROSIS - The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient.08-19-2010
20090239862Substituted Imidazole 4-Carboxamides as Cholecystokinin-1 Receptor Modulators - Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1, such as obesity, and diabetes.09-24-2009
20090203693THERAPEUTIC AGENT FOR LIVER FIBROSIS - The present invention provides a therapeutic agent for hepatic fibrosis and a method for treatment of hepatic fibrosis. 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide or an analogue thereof can prevent the fibrillation in the liver, and therefore can be used as a therapeutic agent for hepatic fibrosis or in the method for treatment of hepatic fibrosis.08-13-2009
201301310603-(INDOLYL)- OR 3-(AZAINDOLYL)- 4-ARYLMALEIMIDE COMPOUNDS AND THEIR USE IN TUMOR TREATMENT - The present invention relates to a compound of formula (I) wherein R05-23-2013
20130131061Novel Estrogen Receptor Ligands - The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R05-23-2013
20130143881Hydrated Crystalline Forms of N-[3-fluoro-4-(oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxam- ide - This invention relates crystalline hydrates of N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, Compound (I). The invention provides methods for treatment of cancer by exploiting the modulation of protein kinase activity. The invention also provides pharmaceutical compositions containing a crystalline hydrate of Compound (I) and a pharmaceutically acceptable excipient.06-06-2013
20130143882HETEROCYCLIC COMPOUNDS AND THEIR USES - Compounds having the structure which are selective inhibitors of P13K (phosphatidylinositol 3-kinase-delta), for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions.06-06-2013
20100331328BICYCLYLARYL-ARYL-AMINE COMPOUNDS AND THEIR USE - The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicyclylaryl-aryl-amines compounds of the following formula (referred to herein as BCAA compounds), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation:12-30-2010
20100331327 7-SUBSTITUTED INDIRUBIN-3'OXIMES AND THEIR APPLICATIONS - The invention relates to new 3′-, 7-substituted-indirubins of formula (I) wherein R represents N—OH, N—O-alkyl or N—O—CO-alkyl, NO—(R12-30-2010
20100179146Indolinone Compounds as Kinase Inhibitors - Indolinone compounds of formula (I) or (II):07-15-2010
20110034462ORGANIC COMPOUNDS - The present invention relates to compounds of the formula; and their use in therapy.02-10-2011
20110034461SF5 DERIVATIVES AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS - The invention relates to novel compounds of formula I02-10-2011
20110118260GLUCOCORTICOID RECEPTOR AGONIST COMPRISING 2,2,4-TRIMETHYL-6-PHENYL-1,2-DIHYDROQUINOLINE DERIVATIVES HAVING SUBSTITUTED OXY GROUP - The present invention is related to glucocorticoid receptor agonists comprised of a compound represented by formula (1) which is 2,2,4-trimethyl-6-phenyl-1,2-dihydroquinoline derivative or a salt thereof and novel pharmacological effects of the glucocorticoid receptor agonists. In the formula (1), R05-19-2011
20110245247NOVEL SMALL MOLECULE POTENTIATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The present invention thus provides compounds of formula I10-06-2011
20100222348QUINOLINONE DERIVATIVES AS PARP INHIBITORS - Compounds of formula (I):09-02-2010
20110245248ISOQUINOLINE DERIVATIVES - The invention relates to 6-piperidinyl-substituted isoquinoline derivatives of the formula (I)10-06-2011
20100179147BENZIMIDAZOLE COMPOUNDS AND THEIR USE AS ANTICANCER AGENTS - Benzimidazole compounds of formula (I):07-15-2010
20090227580Bicyclic derivatives as CETP inhibitors - The present invention relates to novel compounds of formula (I)09-10-2009
20090048253BENZENOID ANSAMYCIN DERIVATIVE - The present invention provides a benzenoid ansamycin derivative represented by Formula (I)02-19-2009
20090312323COMPOUNDS FOR THE TREATMENT OF SPINAL MUSCULAR ATROPHY AND OTHER USES - Compounds of Formula (I) or (II) useful for the treatment of spinal muscular atrophy or other uses, as well as methods of using such compounds to increase SMN expression, increase EAAT2 expression, or increase the expression of a nucleic acid that encodes a translational stop codon introduced by mutation or frameshift.12-17-2009
20100056519COMPOSITION AND METHOD FOR REDUCING PLATELET ACTIVATION AND FOR THE TREATMENT OF THROMBOTIC EVENTS - A novel method of treating and preventing a vascular disease in an individual, comprising: selecting an individual having an elevated level of glycoprotein Ib, glycoprotein IIb/IIIa, PECAM-1, vitronectin receptor or thrombospondin receptor, or formation of platelet-neutrophil aggregates; and administering a therapeutically effective amount of a protease activated receptor-1 (PAR-1) antagonist, a pharmaceutical salt thereof, or a solvate thereof to the individual; and also, composition for treating cardiovascular diseases.03-04-2010
20100056520FORMULATIONS OF PHOSPHOLIPASE ENZYME INHIBITORS - The present invention is directed to formulations of inhibitors of phospholipase enzymes, such as cytosolic PLA03-04-2010
20100056521(AZA)INDOLE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES - The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro or cyano and the like; ring J represents aryl or heteroaryl and the like; Q represents carboxy or 5-tetazolyl and the like; Y represents H, OH, NH03-04-2010
20090215774USES OF INDANE COMPOUNDS - The invention provides methods of treating obesity and eating disorders, which comprise administering indane compounds of Formula (I):08-27-2009
20090215773DIHYDROPYRIDINE DERIVATIVES - The present invention relates to dihydropyridine derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R08-27-2009
20090215772Hydroxybenzamide derivatives and their use as inhibitors of HSP90 - The invention provides compounds of the formula (I):08-27-2009
20110082144N-HETEROARYL INDOLE CARBOXAMIDES AND ANALOGUES THEREOF, FOR USE AS GLUCOKINASE ACTIVATORS IN THE TREATMENT OF DIABETES - This invention relates to compounds that are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial. The compounds are of the general formula (I)04-07-2011
20100069385LIQUID FORMULATIONS OF PHOSPHOLIPASE ENZYME INHIBITORS - The present invention is directed to liquid formulations of inhibitors of phospholipase enzymes, such as cytosolic PLA2, compositions containing the same and processes for manufacture thereof.03-18-2010
20110098296Thiazole And Oxazole Kinase Inhibitors - The present invention provides thiazole and oxazole compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.04-28-2011
20110082145OLOPATADINE COMPOSITIONS AND USES THEREOF - The invention provides solution compositions comprising olopatadine and a PDE4 inhibitor compound of Formula I:04-07-2011
20080249092Novel Quinoline Compounds Capable Of Binding At The Cb2 Receptor - The present invention relates to novel quinoline derivatives such as compounds of the formula (I) which possess are capable of selectively modulating the cannabinoid 2 receptor:10-09-2008
20110160208DIARYL-SUBSTITUTED FIVE-MEMBERED HETEROCYCLE DERIVATIVE - The present invention provides the compounds represented by formula (I):06-30-2011
20090118281Amino Alcohol Derivatives And Their Use As Renin Inhibitor - The application relates to novel amino alcohols of the general formula (I) where R, R05-07-2009
20090118282Compounds and methods for treatment of amyloid-beta-peptide related disorders - The present invention relates to compounds, preparation and uses thereof, particularly in the pharmaceutical industry. The present invention discloses novel compounds more particularly useful for the treatment of Alzheimer's disease and other similar diseases, and more specifically the inventive compounds modulate (in particular, inhibit) the level of amyloid-β peptide (Aβ) exhibited by cells or tissues; Aβ peptide is a major component of the amyloid plaques found in the brains of Alzheimer's sufferers. This invention also relates the use of these inhibitors to prevent, treat or ameliorate the symptoms of Alzheimer's disease or any Amyloid-β-Peptide Related Disorder.05-07-2009
20110288091SOLUBLE MTOR COMPLEXES AND MODULATORS THEREOF - The present invention relates to small molecule modulators of mTORC1 and mTORC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, autoimmune diseases, diabetic retinopathy) and metabolic diseases. Novel small molecules are provided that inhibit one or more of mTORC1, mTORC2, and PI3K-related proteins. Novel methods of providing soluble mTORC1 and mTORC2 complexes are discussed, as well as methods of using the soluble complexes in a high-throughput manner to screen for inhibitory compounds.11-24-2011
20080214542Arylpiperazine Derivatives and their Use as Selective Dopamine D3 Receptor Ligands - The invention concerns compounds of general formula (I), a method for preparing same, as well as their use as therapeutic agent.09-04-2008
20080255113Quinolonecarboxylic Acid Compounds Having 5-Ht4 Receptor Agonistic Activity - This invention provides a compound of the formula (I): wherein Het represents a heterocyclic group having one nitrogen atom, to which B binds directly, and from 4 to 7 carbon atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 4 substituents independently selected from the group consisting of substituents α10-16-2008
20080255117SULFONYLTRYPTOPHANOLS - The present invention relates to sulfonyltryptophanols of the general formula I,10-16-2008
200802551142-AMINOBENZOXAZOLE CARBOXAMIDES AS 5HT3 MODULATORS - Compounds of formulae I, II and III:10-16-2008
20080255116Quinoline Derivatives as Antibacterial Agents - Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of Formula (Ia) or (Ib)10-16-2008
20110053937Inhibitors of the Interaction Between MDM2 and P53 - The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I)03-03-2011
20110053936 SUBSTITUTED SPIRO[CYCLOALKYL-1,3'-INDOL]-2'(1'H)-ONE DERIVATIVES AND THEIR USE AS P38 MITOGEN-ACTIVATED KINASE INHIBITORS - The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.03-03-2011
20110053935FUSED PYRIDINES ACTIVE AS INHIBITORS OF C-MET - Fused pyridines of formula (I) and the pharmaceutically acceptable salts thereof have activity as inhibitors of c-Met and may thus be used to treat various diseases and disorders including cancer. Processes for synthesizing the compounds are also described.03-03-2011
20110053934COMPOUNDS AND METHODS OF TREATMENT - A derivative, which is useful as a ret kinase inhibitor is described herein. The described invention also includes methods of using the same in the treatment of diseases mediated by inappropriate ret kinase activity.03-03-2011
20110028475TETRAHYDROISOQUINOLINE SULFONAMIDE DERIVATIVES, THE PREPARATION THEREOF, AND THE USE OF THE SAME IN THERAPEUTICS - The disclosure relates to tetrahydroisoquinoline sulfonamide compounds of formula I:02-03-2011
20100286144HETEROARYL DERIVATIVES - A compound of the following formula (1), or its prodrug or pharmaceutically acceptable salt thereof, being useful as a diabetic medicine or preventive, or blood sugar regulator, or therapeutic agent for hyperlipemia, etc.11-11-2010
20110112092AMINOQUINOLINE DERIVATIVES AND THEIR USE AS ADENOSINE A3 LIGANDS - The present invention relates to an adenosine A05-12-2011
20110263600Method for preventing or treating a disease related to the glucocorticoid receptor - A method for preventing or treating a disease related to the glucocorticoid receptor involving administering a pharmacologically effective amount of a 1,2-dihydroquinoline compound or a pharmaceutically acceptable salt thereof.10-27-2011
201102635997-NONSUBSTITUTED INDOLE MCL-1 INHIBITORS - Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.10-27-2011
20100298323APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.11-25-2010
201101368083',6-SUBSTITUTED INDIRUBINS AND THEIR BIOLOGICAL APPLICATIONS - Indirubin derivatives of formula (I) wherein R represents -(A)06-09-2011
20100184763QUINOLONE BASED COMPOUNDS EXHIBITING, PROLYL HYDROXYLASE INHIBITORY ACTIVITY, AND COMPOSITIONS, AND USES THEREOF - This invention relates to new quinolone based compounds that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one quinolone based compound. This invention further involves assays for the detection of a hydroxyproline residue in a HW molecule.07-22-2010
20100324044METABOTROPIC GLUTAMATE RECEPTOR ISOXAZOLE LIGANDS AND THEIR USE AS POTENTIATORS - Compounds in accord with Formula I:12-23-2010
20100324042HETEROCYCLIC COMPOUNDS AND THEIR USE AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS - The present invention relates to a heterocyclic compound of the general formula (I)12-23-2010
20100099674METHOD AND MEANS FOR PREVENTING AND INHIBITING TYPE III SECRETION IN INFECTIONS CAUSED BY GRAM-NEGATIVE BACTERIA - A means for decreasing bacterial virulence in a mammal including man or in a plant by inhibition of the Type III secretion system at concentrations that do not prevent or substantially reduce bacterial growth comprises an N-substituted 7-quinolylmethyl amine, in particular one that is further substituted in 5- and 8-position on the quinoline ring. A corresponding therapeutic method and a pharmaceutical composition are also disclosed.04-22-2010
20120309759Screening Method and Compounds for Modulating Telomerase Activity - The present invention embraces methods for identifying compounds that modulate the activity of telomerase. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the TRBD, “thumb,” “finger,” and/or “palm” domain; or FP-pocket, PT-pocket or Th-pocket of telomerase and testing the compound for its ability to modulate the activity of telomerase. Compounds selected for interacting with the T-pocket or Fingers-Palm pocket of telomerase are also provided.12-06-2012
20110190294NOVEL ESTROGEN RECEPTOR LIGANDS - The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R08-04-2011
20110136807Bicyclic compositions and methods for modulating a kinase cascade - The invention relates to compounds and methods for modulating one or more components of a kinase cascade.06-09-2011
20100029646PRODRUGS OF DIPHENYL OX-INDOL-2-ONE COMPOUNDS - The present application discloses prodrugs of substituted 3,3-diphenyl-1,3-dihydro-indol-2-one compounds having the general formula (I). The 4-position of the phenyl moieties and the N-position of the indole represent useful handles for the introduction of particular prodrug groups, in particular those comprising an amino acid moiety. The prodrug compounds are believed to be useful for the treatment of cancer in a mammal, possibly in combination with one or more other chemotherapeutic agents. The application also discloses the compounds for use in a method of treating a mammal suffering from or being susceptible to cancer02-04-2010
20100029644Compounds Which Modulate The CB2 Receptor - Compounds of formula (I) are disclosed. Compounds according to the invention are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.02-04-2010
201000225352-Pyridyl substituted imidazoles as ALK5 and/or ALK4 Inhibitors - 2-pyridyl-substituted imidazoles which are used advantageously in the treatment of diseases mediated by ALK 5 or ALK 4 inhibitors or both.01-28-2010
20100016312Substituted indolyl and indazolyl derivatives and uses thereof - This application discloses compounds of generic Formula I:01-21-2010
20100016310METHODS OF USING ARYL SULFONYL COMPOUNDS EFFECTIVE AS SOLUBLE EPOXIDE HYDROLASE INHIBITORS - Disclosed are methods of using soluble epoxide hydrolase (sEH) inhibitors for treating diseases related to cardiovascular disease.01-21-2010
20100016308Tetrahydroindole Derivatives for Treatment of Alzheimer's Disease - Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.01-21-2010
20100016313INTESTINAL ALKALINE PHOSPHATASE MODULATORS AND USES THEREOF - Disclosed are modulators, i.e., activators and inhibitors, of Intestinal Alkaline Phosphatase (IAP). Also disclosed are methods for treating bacterial infections of the intestinal tract and methods for maintaining the health of the intestinal tract using IAP activators. Further disclosed are methods to assist in weight gain of emaciated patients and those having reduced or negligible fat absorption using IAP inhibitors.01-21-2010
20100197688EPHA4 RTK INHIBITORS FOR TREATMENT OF NEUROLOGICAL AND NEURODEGENERATIVE DISORDERS AND CANCER - The present invention is directed to compounds of generic formula (I)08-05-2010
20100222349QUINOLINE DERIVATIVES USED TO TREAT INFLAMMATORY AND ALLERGIC DISEASES - The present invention relates to compounds of formula (I)09-02-2010
20100324043Bicyclic And Tricyclic Compounds As KAT II Inhibitors - Compounds of Formula X:12-23-2010
20120178755CYANOISOQUINOLINE COMPOUNDS AND METHODS OF USE THEREOF - The present invention relates to cyanoisoquinoline compounds suitable for use in treating hypoxia inducible factor-mediated and/or erythropoietin-associated conditions. The cyanoisoquinoline compounds of the invention have the following structure:07-12-2012
20120208814Thetrahydroquinolines Derivatives As Bromodomain Inhibitors - Tetrahydroquinoline compounds of formula (I)08-16-2012
200900622813-QUINOLINECARBONITRILE PROTEIN KINASE INHIBITORS - This invention provides a compound of Formula 103-05-2009
20090312325Quinoline Derivatives As Phosphodiesterase Inhibitors - There are provided according to the invention novel compounds of formula (I)12-17-2009
20110071150INDOLE DERIVATIVES AS CRAC MODULATORS - Compounds of the formula I:03-24-2011
20090186893IRE-1alpha INHIBITORS - Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.07-23-2009
20120046287Dihydroindolone compounds, a process for their preparation and pharmaceutical compositions containing them - Compounds of formula (I):02-23-2012
20120065203Methods of Reducing Serum Glucose and Triglyceride Levels and for Inhibiting Angiogenesis Using Substituted Indolealkanoic Acids - Disclosed are methods of reducing serum glucose and triglyceride levels and for inhibiting angiogenesis, the methods comprising administration of substituted indolealkanoic acids to patients in need of such treatment. Also disclosed are such compounds useful in the treatment of angiogenesis, hyperglycemia, hyperlipidemia and chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds.03-15-2012
20120004224Triheterocyclic Compounds and Compositions Thereof - The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus.01-05-2012
201001603183-Pyrrolo[b]Cyclohexylene-2-Dihydroindolinone Derivatives and Uses Thereof - 3-pyrrolo[b]cyclohexylene-2-dihydro-indolinone derivatives of formula (I) or their pharmaceutically acceptable salts and uses thereof. The intermediates of formula (II) for preparing the above compounds. The bioassay shows that the above compounds and their pharmaceutically acceptable salts can modulate the activity of protein kinases (PKs), inhibit the activity of tyrosine kinases (PTKs) and inhibit many kinds of tumor cells as well as.06-24-2010
20110098297FUSED RING COMPOUNDS AND USE THEREOF - The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like. The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein each symbol is defined in the specification, or a salt thereof or a prodrug thereof.04-28-2011
20120010205NOVEL QUINOLINE ESTERS USEFUL FOR TREATING SKIN DISORDERS - Disclosed are quinoline esters of Formula (I):01-12-2012
20110166136Calcium Ion Channel Modulators & Uses Thereof - Compounds of formula (1), salts and pro-drugs wherein:07-07-2011
20090163493Benzene, Pyridine, and Pyridazine Derivatives - Disclosed are compounds and pharmaceutically acceptable salts of Formula I 06-25-2009
20120115865New Salts of an Indole Derivative and Their Use in Medicine - The present invention relates to new pharmaceutically acceptable salts of 2-hydroxy-3-[5-(morpholin-4-yl-methyl)pyridin-2-yl]1H-indole-5-carbonitrile, processes for their preparations, pharmaceutical formulations containing said salts and to the use of said active salts in therapy, and particularly to GSK3 related disorders.05-10-2012
20120022063Oligomer-Cannabinoid Conjugates - The invention relates to (among other things) oligomer-cannabinoid conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated cannabinoid compounds.01-26-2012
20120022064DIHYDROQUINOLINONE DERIVATIVES - The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.01-26-2012
20120022065C-Met Modulators and Method of Use - The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.01-26-2012
20100267720 Crystalline Forms of 2-Hydroxy-3- [5- (Morpholin- 4- Ylmethyl) Pyridin-2-YL] IH- Indole- 5 -Carbonitrile Citrate - The present invention relates to new crystalline forms of 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]1H-indole-5-carbonitrile citrate, a Form D and a Form E, respectively, a process for their preparations, pharmaceutical formulations containing said compounds and to the use of said active compounds in therapy, and particularly to GSK3 related conditions and disorders.10-21-2010
20090036446Indole derivatives as histamine 3 receptor inhibitors for the treatment of cognitive and sleep disorders, obesity and other CNS disorders - This invention relates to compounds having pharmacological activity, to compositions containing these compounds, and to a method of treatment employing the compounds and compositions. More particularly, this invention concerns certain indole derivatives and their salts and solvates. These compounds have H02-05-2009
20120157454ISOQUINOLIN-1 (2H) -ONE DERIVATIVES AS PARP-1 INHIBITORS - There are provided substituted isoquinolin-1(2H)-one derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds. A screening method for the identification of compounds capable of binding several PARP proteins, as well the probes used in such method, are further objects of the invention.06-21-2012
20110092504INHIBITORS OF PI3 KINASE - The present invention relates to compounds of Formula (I), or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein Q, X04-21-2011
20110092503QUINOLINE DERIVATIVES AS AXL KINASE INHIBITORS - Novel compounds which are inhibitors of receptor tyrosine kinases of the AXL receptor family are described herein. These compounds are suitable for the treatment or prevention of disorders associated with, accompanied by or caused by hyperfunction of a receptor of the AXL family. The compounds are suitable for the treatment of hyperproliferative disorders, such as cancer, particularly cancer metastases.04-21-2011
20120309758MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.12-06-2012
201202088133-CARBAMOYL-2-PYRIDONE DERIVATIVES - The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I):08-16-2012
20110065703NOVEL AGENTS OF CALCIUM ION CHANNEL MODULATORS - The present invention includes a group of chemical compounds useful as modulators of calcium ion (Ca03-17-2011
20110065704COMPOUNDS FOR MODULATING RNA BINDING PROTEINS AND USES THEREFOR - The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders.03-17-2011
20120309757N-BIPHENYLMETHYLINDOLE MODULATORS OF PPARG - The invention provides molecular entities that bind with high affinity to PPARG (PPARγ), 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. In methods of treatment of these conditions using a compound of the invention, the compound can avoid producing side effects of significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, in the patient 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
20110105502TETRAHYDROISOQUINOLINES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY - The present invention relates to tetrahydroisoquinoline of the formula (I)05-05-2011
20110105501PHARMACEUTICAL COMBINATIONS - The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I):05-05-2011
20080287435Active Ingredient Combinations Having Insecticide and Acaricide Properties - The novel active compound combinations of certain cyclic ketoenols and ethiprole have very good insecticidal and acaricidal properties.11-20-2008
20100093725SEMI-SOLID FORMULATIONS OF PHOSPHOLIPASE ENZYME INHIBITORS - The present invention is directed to semi-solid formulations of inhibitors of phospholipase enzymes, such as cytosolic PLA04-15-2010
20100093727COMPOUNDS AND METHODS OF USE - The present invention provides novel compounds useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.04-15-2010
20100093726NOVEL 4-AMINO-QUINOLINE DERIVATIVES USEFUL AS ANTI-MALARIA DRUGS - The present invention relates to clotrimazole/quinoline hybrids useful as active ingredients of anti-malaria drugs. The compounds show a remarkable in vitro biological activity especially against the chloroquine-resistant 04-15-2010
20120316168QUINOLONE COMPOUND AND PHARMACEUTICAL COMPOSITION - The present invention provides a quinolone compound represented by General Formula (1)12-13-2012
20120316167SECONDARY 8-HYDROXYQUINOLINE-7-CARBOXAMIDE DERIVATIVES - The present invention provides new secondary 8-hydroxyquinoline-7-carboxamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful as antifungal agents. Specifically, these compounds were tested against 12-13-2012
20120122865ISOINDOLINE COMPOUNDS AND METHODS OF THEIR USE - Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases.05-17-2012
20110183977BENZENE, PYRIDINE, AND PYRIDAZINE DERIVATIVES - Disclosed are compounds and pharmaceutically acceptable salts of Formula I07-28-2011
201101839765- AND 6-MEMBERED HETEROCYCLIC COMPOUNDS - 5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Also described is the treatment of neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.07-28-2011
20090197883Diphenyl Substituted Cycloalkanes, Compositions Containing Such Compounds and Methods Of Use - The instant invention provides compounds of Formula (I) which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.08-06-2009
20120165331Di/tri-aza-spiro-C9-C11alkanes - The invention relates to compounds of the formula I06-28-2012
20130172346USE OF KYNURENIC ACID AMIDE DERIVATIVES FOR THE TREATMENT OF HUNTINGTON'S DISEASE - The invention is directed to kynurenic acid analogues and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing said compounds for treating the symptoms of Huntington's disease and preventing the development of the symptoms.07-04-2013
20120252808QUINOLINE AMIDE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to quinoline amide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.10-04-2012
20100179145PHARMACEUTICAL COMBINATIONS - The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I):07-15-2010
20100048566ANTIBACTERIAL QUINOLINE DERIVATIVES - The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib):02-25-2010
20100292235Bicycloheteroaryl Compounds as P2x7 Modulators and Uses Thereof - Bicycloheteroaryl compounds are disclosed that have a formula represented by the following:11-18-2010
20120083495COMPOUNDS FOR THE TREATMENT OF SPINAL MUSCULAR ATROPHY AND OTHER USES - Compounds useful for the treatment of spinal muscular atrophy or other uses, as well as methods of using such compounds to increase SMN expression, increase EAAT2 expression, or increase the expression of a nucleic acid that encodes a translational stop codon introduced by mutation or frameshift.04-05-2012
20120083494NOVEL TRIAZOLE DERIVATIVES WITH IMPROVED RECEPTOR ACTIVITY AND BIOAVAILABILITY PROPERTIES AS GHRELIN ANTAGONISTS OF GROWTH HORMONE SECRETAGOGUE RECEPTORS - The present invention provides novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular alcohol disorder, drug abuse, growth retardation, cachexia, short-, medium-, and/or long term regulation of energy balance, short-, medium-, and/or long term regulation (stimulation and/or inhibition) of food intake, intake of rewarding food, adipogenesis, adiposity and/or obesity, body weight gain and/or reduction, diabetes, diabetes type I, diabetes type II, tumor cell proliferation, inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and/or gastrectomy (ghrelin replacement therapy).04-05-2012
20120225875HETEROARYLAMINOQUINOLINES AS TGF-BETA RECEPTOR KINASE INHIBITORS - Novel hetarylaminoquinoline derivatives of formula (I)09-06-2012
20120225873COMPOUNDS FOR ALZHEIMER'S DISEASE - The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(═O)OH, -L-CH═CHC(═O)OH, -L-C(═O)NH09-06-2012
20120225874BICYCLIC DERIVATIVES AS CETP INHIBITORS - The present invention relates to novel compounds of formula (I)09-06-2012
201202258768-AZABICYCLO[3.2.1]OCTANE-8-CARBOXAMIDE DERIVATIVE - Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof (In the formula, A represents a group that is represented by formula (A-1); R09-06-2012
20110124645FLUOROALKOXY-SUBSTITUTED 1,3-DIHYDRO-ISOINDOLYL COMPOUNDS AND THEIR PHARMACEUTICAL USES - The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4.05-26-2011
20110124644METHODS OF DIAGNOSING AND CHARACTERIZING CANNABINOID SIGNALING IN CROHN'S DISEASE - Diagnosis of Crohn's Disease by determining the presence or absence of variants at the CNR2 (cannabinoid) genetic locus and serological markers is disclosed Methods of diagnosing a Crohn's Disease sub-type by determining the presence or absence of one or more risk variants at the CNR2 5 locus and the presence or absence of ASCA, OmpC, 12 and/or anti-Cbir1 antibodies are included05-26-2011
20110046133ORGANIC COMPOUNDS - The present invention provides compounds of the following structure;02-24-2011
20120322800Sepiapterin Reductase Inhibitors For The Treatment of Pain - Disclosed herein are small molecule heterocyclic inhibitors of sepiapterin reductase (SPR), and prodrugs and pharmaceutically acceptable salts thereof. The Also featured are pharmaceutical compositions of the compounds and uses of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, and neuropathic pain).12-20-2012
20120270872Crystalline Forms of N-[3-fluoro-4-(oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxam- ide - This invention relates to three crystalline forms of N—[3-fluoro-4-((6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl|oxy)phenyl]—N′—(4-fluorophenyl)cyclopropane-1,1-dicarboxamide. Compound (I), designated as Form A, Form B, and Form C. The invention provides methods for treatment of cancer by exploiting the modulation of protein kinase activity. The invention also provides pharmaceutical compositions containing a crystalline form of Compound (I) and a pharmaceutically acceptable excipient.10-25-2012
20100227863SUBSTITUTED 3-(4-HYDROXYPHENYL)-INDOLIN-2-ONE COMPOUNDS - The present application discloses substituted 3-(4-hydroxyphenyl)-indolin-2-one compounds (oxindole compounds) of the formula09-09-2010
20100234373BIS-ARYL AMIDE COMPOUNDS AND METHODS OF USE - The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including autoimmune disease and inflammation. In one embodiment, the compounds have a general Formula I09-16-2010
20100234371Bicyclic heterocycles, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof - The invention relates to bicyclic heterocycles of general formula (I), in which R09-16-2010
20120277231QUINOLINYLOXYPHENYLSULFONAMIDES - The present invention relates to quinolinyloxyphenylsulfonamides and stereoisomeric forms, solvates, hydrates and/or pharmaceutically acceptable salts of these quinolinyloxyphenylsulfonamide compounds as well as pharmaceutical compositions containing at least one of these compounds together with at least one pharmaceutically acceptable carrier, excipient and/or diluent. Said quinolinyloxyphenylsulfonamides are useful for prophylaxsis, treatment and/or after-treatment of hyperproliferative disorders, such as cancer, tumors and particularly cancer metastases.11-01-2012
20090203692NOVEL CHEMICAL COMPOUNDS - This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with hYAK3 activity.08-13-2009
20120277230COMPOUNDS USEFUL FOR TREATING CANCER - The present invention relates to compound (I) wherein: means a pyridazine, a pyrimidine or a pyrazine group, R independently represent a hydrogen atom, a halogen atom or a group chosen among a CN group, a hydroxyl group, a COOR11-01-2012
20100222347PROPHYLACTIC AND/OR THERAPEUTIC AGENT FOR ANEMIA, COMPRISING TETRAHYDROQUINOLINE COMPOUND AS ACTIVE INGREDIENT - Disclosed is a low-molecular-weight compound having an EPO production-promoting activity and/or a hemoglobin expression-enhancing activity. Specifically disclosed is an EPO production promoter and/or a hemoglobin expression enhancer comprising a 1-acyl-4-(phenoxy, benzyloxy or phenylamino)-1,2,3,4-tetrahydroquinoline derivative, more specifically a tetrahydroquinoline compound represented by the general formula (1);09-02-2010
20120329796COMPOUNDS USEFUL FOR TREATING PREMATURE AGING AND IN PARTICULAR PROGERIA - The present invention relates to compound (I) wherein: means a pyridazine, a pyrimidine or a pyrazine group, R independently represent a hydrogen atom, a halogen atom or a group chosen among a —CN group, a hydroxyl group, a —COOR12-27-2012
20120329797SECONDARY 8-HYDROXYQUINOLINE-7-CARBOXAMIDE DERIVATIVES FOR USE AS ANTIFUNGAL AGENTS - The present invention provides secondary 8-hydroxyquinoline-7-carboxamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful as antifungal agents. Specifically, these compounds were tested against 12-27-2012
20110319412PIPERIDINE AND PYRROLIDINE DERIVATIVES HAVING NPY Y5 RECEPTOR ANTAGONISM - The present invention discloses novel piperidine and pyrrolidine derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), a pharmaceutically acceptable salt or a solvate thereof:12-29-2011
20110319411ISOINDOLINONE AND RELATED ANALOGS AS SIRTUIN MODULATORS - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.12-29-2011
20100168100QUINOLINE DERIVATIVES AS P13 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.07-01-2010
201001680991H-QUINOLIN-4-ONE COMPOUNDS, WITH AFFINITY FOR THE GABA RECEPTOR, PROCESSES, USES AND COMPOSITIONS - The invention provides new 1H-quinolin-4-one compounds of formula (I), wherein R07-01-2010
20100168101OXINDOLE HYDRAZIDE MODULATORS OF PROTEIN TYROSINE PHOSPHATASES (PTPS) - The present invention is related to the use of oxindole hydrazide derivatives of formula (I) for the treatment and/or prevention of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, obesity, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of oxindole hydrazide derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs, in particular of PTP1B, TC-PTP, SHP and GLEPP-1. The present invention is furthermore related to novel oxindole hydrazide derivatives and method of preparation thereof.07-01-2010
20100168098Viral Polymerase Inhibitors - The present invention relates to compounds represented by formula (I) wherein A, B, D, E, R07-01-2010
20100173907Method of treatment of aggression - The invention comprises a method of treatment of aggression and similar behavioral syndromes, such as impulsivity and irritability, by a pharmaceutical agent exhibiting combined D2 and D5 antagonistic activity.07-08-2010
20100130494DERMATITIS TREATING AGENT (AS AMENDED) - The present invention is to provide a topical dermatitis treating agent which comprises a pyridine compound represented by the following formula [I]:05-27-2010
20120149702INHIBITORS OF CELLULAR NECROSIS - The present invention relates to compounds and pharmaceutical preparations and their use in therapy for preventing or treating trauma, ischemia, stroke and degenerative diseases associated with cell death. Methods and compositions of the invention are particularly useful for treating neurological disorders associated with cellular necrosis.06-14-2012
20110160207HETEROCYCLIC AMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS - A compound of Formula I06-30-2011
201301723444-OXOQUINOLINE COMPOUND AND USE THEREOF AS HIV INTEGRASE INHIBITOR - An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I]07-04-2013
201301723451-ACYL-4-(PHENOXY, BENZYLOXY, OR PHENYLAMINO)-1,2,3,4-TETRAHYDROQUINOLINE DERIVATIVES - Disclosed is a low-molecular-weight compound having an EPO production-promoting activity and/or a hemoglobin expression-enhancing activity. Specifically disclosed is an EPO production promoter and/or a hemoglobin expression enhancer comprising a 1-acyl-4-(phenoxy, benzyloxy or phenylamino)-1,2,3,4-tetrahydroquinoline derivative, more specifically a tetrahydroquinoline compound represented by the general formula (1);07-04-2013
20080234269N-Oxo-Heterocycle and N-Oxo-Alkyl Quinoline-4-Carboxamides as Nk-3 Receptor Ligands - Compounds of Formula I09-25-2008
20080234268Bis-aryl amide derivatives and methods of use - Selected compounds are effective for prophylaxis and treatment of diseases, such as c-Met mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.09-25-2008
20080234267Compounds and Methods of Treatment - A derivative, which is useful as a ret kinase inhibitor is described herein. The described invention also includes methods of using the same in the treatment of diseases mediated by inappropriate ret kinase activity.09-25-2008
20080227779Heterocyclic compounds and methods of use - The present invention comprises a new class of compounds capable of modulating the c-kit protein kinase and, accordingly, useful for treatment of c-kit mediated diseases including, without limitation, autoimmune disease, allergies, mastcytosis, mast cell related tumors and various fibrotic diseases. The compounds have a general Formula I09-18-2008
20080227778Isoquinolinone Potassium Channel Inhibitors - The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.09-18-2008
20120252807ARBOVIRUS INHIBITORS AND USES THEREOF - The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides compounds as inhibitors of arboviruses.10-04-2012
20080214543N-Phenyl-(2R,5S)Dimethylpiperazine Derivative - The present invention relates to a novel N-phenyl-(2R,5S)dimethylpiperazine derivatives useful as antiandrogenic agent which exhibits a sufficient prostate gland reducing effect as compared with conventional compounds and are excellent in oral activity. The compound of the present application is useful in preventing or treating prostate cancer, benign prostatic hyperplasia, and the like. The present invention also provides a novel intermediate useful in producing the compound of the present invention.09-04-2008
20130096119Isoquinolin-3-Ylurea Derivatives - The invention relates to isoquinolin-3-ylurea derivatives of formula (I) wherein R04-18-2013
20130096121APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bc1-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bc1-xL protein.04-18-2013
20130096122FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS - The present invention relates to sodium channel inhibitors of Formula I:04-18-2013
20130096120APOPTOSIS-INDUCED AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.04-18-2013
20130102604NOVEL CYCLOPROPANE INDOLINONE DERIVATIVES - The present invention relates to a compound of formula (I)04-25-2013
20130123259SUBSTITUTED 3-(5-MEMBERED UNSATURATED HETEROCYCLYL-1, 3-DIHYDRO-INDOL-2-ONES AND DERIVATIVES THEREOF AS KINASE INHIBITORS - The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.05-16-2013
201301232584(1H)-Quinolones Having Antimalarial Activity With Reduced Chemical Resistance - Provided are 4(1H)-quinolone derivatives effective in inhibiting or eliminating the viability of at least one of the stages in the life-cycle of the malarial parasite, and to show a reduced propensity to induce resistance to the compound by the target parasite. In particular, the compounds can be derivatives of phenoxyethoxy-quinolones, and including, but not only, 7-(2-phenoxyethoxy)quinolin derivatives. These compounds may be administered by themselves, with at least one other derivative compound, or with other antimalarial compounds, to an animal or human subject. The therapeutic compositions can be and formulated to reduce the extent of a 05-16-2013
200802076186- (Heterocyclyl-substituted Benzyl) -4-Oxoquinoline Compound and Use Thereof as HIV Integrase Inhibitor - The present invention relates to a compound represented by the following formula [I]08-28-2008
20080200459TETRAHYDROQUINOLINE CANNABINOID RECEPTOR MODULATORS - The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula I:08-21-2008
20110224207FLAVIVIRUS INHIBITORS AND METHODS FOR THEIR USE - Methods of treating, preventing, and/or ameliorating a Flavivirus infection in a subject are disclosed. The methods comprise administering to the subject a therapeutically effective amount of a Flavivirus inhibitor, e.g., a Flavivirus serine protease inhibitor. These methods are useful in treating, preventing, and/or ameliorating Flavivurs infections such as, for example, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus.09-15-2011
20110275632Method for preventing or treating a disease related to the glucocorticoid receptor - A method for preventing or treating a disease related to the glucocorticoid receptor involving administering a pharmacologically effective amount of a 1,2-dihydroquinoline compound.11-10-2011
20110275631Heteroaryl Substituted Indole Compounds Useful as MMP-13 Inhibitors - Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.11-10-2011
20110275630ISOINDOLINONE KINASE INHIBITORS - Compounds having the formula:11-10-2011
20100317662Metabotropic Glutamate Receptor Isoxazole Ligands and Their Use as Potentiators - 286 - Compounds in accord with Formula I:12-16-2010
20100317661SMALL MOLECULE INHIBITORS OF MDM2 AND THE USES THEREOF - The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).12-16-2010
20130184275HYDRAZONE MODULATORS OF CANNABINOID RECEPTORS - Hydrazone compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.07-18-2013
20130184276MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.07-18-2013
20130158029SIGMA RECEPTOR INHIBITORS - The invention refers to compounds of general formula (I)06-20-2013
20130158030PYRROLYL SUBSTITUTED DIHYDROINDOL-2-ONE DERIVATIVES, PREPARATION METHODS AND USES THEREOF - Provided are pyrrolyl substituted dihydroindol-2-one derivatives represented by formula (I), pharmaceutically acceptable salts or solvates of said derivatives, or solvates of said salts, which are effective tyrosine kinase inhibitors. Also provided are the preparation methods of the above compounds, pharmaceutical compositions containing these compounds, and the use of these compounds in manufacturing drugs useful for the treatment or adjunctive treatment of tumors medicated by tyrosine kinases or proliferation or migration of tumor cells driven by tyrosine kinases in mammals (including human).06-20-2013
20130158031ALKYNE-BRIDGED HETERO-AROMATICS AND USES THEREOF - This invention relates to novel alkyne-bridged hetero-aromatics as described in the specification which are PDE10A inhibitors and useful for the treatment of neurological, psychiatric disorder, metabolic disorders, such as Schizophrenia, Parkinson's disease, Huntington's disease, Alzheimer's disease, learning memory disorder, drug addiction (abuse), sleeping disorder, depression, obesity, non-insulin dependent diabetes, bipolar disorder, obsessive compulsive disorder, or pain; to process for their preparation; to pharmaceutical compositions comprising them; and to methods of using them.06-20-2013
201103129612,5-Disubstituted Morpholine Orexin REceptor Antagonists - The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).12-22-2011
20120028977Subunit Selective NMDA Receptor Potentiators For The Treatment Of Neurological Conditions - Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-J, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.02-02-2012
20120028976PHARMACOKINETICALLY-BASED DOSING REGIMENTS OF A THROMBIN RECEPTOR ANTAGONIST - Dosing regimens based on the pharmacokinetic characteristics of a thrombin receptor antagonist are disclosed. In some embodiments, the dosing regimens result in mean plasma concentrations. Also disclosed are methods of treating acute coronary syndrome and peripheral arterial disease, and of effecting secondary prevention, by orally administering thrombin receptor antagonists according to such dosing regimens.02-02-2012
20130196991SUBSTITUTED INDOLES, ANTIVIRAL ACTIVE COMPONENT, METHOD FOR PREPARATION AND USE THEREOF - The invention relates to novel antiviral active components of the general formula 1, pharmaceutical composition, antiviral medicament, method for prophylaxis and treatment of viral diseases, particularly caused by hepatisis C viruses (HCV). In the general formula 108-01-2013

Patent applications in class Ring nitrogen in the bicyclo ring system