Entries |
Document | Title | Date |
20080261970 | Sufonamides and Uses Thereof - Compounds of formula (I), including methods of making and methods of using are described in formula (I). | 10-23-2008 |
20080287434 | New amino-alkyl-amide derivatives as CCR3 receptor ligands - The invention relates to a compound of the general formula (I), | 11-20-2008 |
20080293713 | Inhibitors of Diacylglycerol O-acyltransferase Type 1 Enzyme - The present invention relates to compounds of formula (I): | 11-27-2008 |
20080300245 | Pyrazolo[1,5-A]Pyridine-3-Carboxylic Acids as Ephb and Vegfr2 Kinase Inhibitors - The invention relates to novel pyrazolo[1,5a]pyridine-3-carboxylic acid compounds of the formula | 12-04-2008 |
20080312225 | Triazolophthalazines - The compounds of formula (I) | 12-18-2008 |
20090005372 | Triazolophthalazines - The compounds of formula I | 01-01-2009 |
20090005373 | SUBSTITUTED SULFONAMIDO-MACROCYCLES AS TIE2 INHIBITORS AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME - The invention relates to substituted sulfonamido-macrocycles according to the general formula (I): | 01-01-2009 |
20090005374 | IMIDAZOPYRIDINYL THIAZOLYL HISTONE DEACETYLASE INHIBITORS - A compound of general Formula (I) having histone deacetylase (HDAC) and/or CDK inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound. | 01-01-2009 |
20090012078 | Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases - Novel fused pyrazine compounds are disclosed that have a formula represented by the following: | 01-08-2009 |
20090012079 | Triazolopyridine Compounds - A compound of formula (Ia): or a pharmaceutically acceptable salt and/or solvate (including hydrate) thereof, or a compound of formula (Ib): or a pharmaceutically acceptable salt and/or solvate (including hydrate) thereof, and the use of a compound of formula (Ia) or (Ib) in the treatment of a TNF-mediated disease, disorder, or condition, or a p38-mediated disease, disorder, or condition, in particular the allergic and non-allergic airway diseases, more particularly obstructive or inflammatory airways diseases, preferably chronic obstructive pulmonary disease. | 01-08-2009 |
20090012080 | Sirtuin modulating compounds - 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. | 01-08-2009 |
20090018127 | Ergoline Derivatives - Disclosed are ergoline derivatives, Formula (I), wherein either each of R | 01-15-2009 |
20090018128 | Compounds - The present invention relates to novel pyrrolopyrazine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of the cannabinoid receptor. | 01-15-2009 |
20090048244 | PYRROLOTRIAZINE COMPOUNDS AS KINASE INHIBITORS - The present invention provides compounds of formula I | 02-19-2009 |
20090048245 | Imidazolopyridine compounds useful for the treatment of degenerative and inflammatory diseases - Novel imidazolopyridine compounds are disclosed that have a formula represented by the following: | 02-19-2009 |
20090048246 | COMPOUNDS, COMPOSITIONS AND METHODS FOR REDUCING LIPID LEVELS - Compositions comprising extracts or isolated or purified compounds from plants of the genus | 02-19-2009 |
20090069315 | Use of Pyrazolo(1,5A)Pyrimidin-7-YL Amine Derivatives in the Treatment of Neurological Disorders - The invention relates to methods of using the compounds of the invention, including pyrazolo[1,5a]pyrimidin-7-yl amine compounds and salts thereof, as well as pharmaceutical compositions comprising the same, in the treatment of Eph receptor-related (e.g., neurological) injuries and disorders. The invention also relates to modulating the activity of an Eph receptor in a cell, stimulating neural regeneration, and reversing neuronal degeneration, by administering a compound of the invention to a cell or subject in an effective amount. | 03-12-2009 |
20090075999 | OXYGEN LINKED PYRIMIDINE DERIVATIVES - The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases. | 03-19-2009 |
20090093475 | Oxo-substituted imidazo[1,2b]pyridazines, their preparation and use as pharmaceuticals - The invention relates to novel inhibitors of kinases of the general formula (I): | 04-09-2009 |
20090093476 | PYRROLO[1,2-A]QUINOXALINE DERIVATIVES AS ADENOSINE A3 RECEPTOR MODULATORS AND USES THEREOF - The present invention provides new compounds displaying high affinity for adenosine A | 04-09-2009 |
20090099166 | C10-substituted camptothecin analogs - The novel C10-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR/MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW<600). | 04-16-2009 |
20090099167 | Organic compounds - The invention relates to the use of pyrazolo[1,5a]pyrimidin-7-yl amine compounds and salts thereof in the treatment of kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, novel pyrazolo[1,5a]pyrimidin-7-yl amine compounds, and a process for the preparation of the novel pyrazolo[1,5a]pyrimidin-7-yl amine compounds. | 04-16-2009 |
20090099168 | HIV Integrase inhibitors - Pyridopyrazine- and pyrimidopyrazine-dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dihydroxypyridine carboxamides are of Formula I: | 04-16-2009 |
20090105242 | Triazolopyridine compounds useful for the treatment of degenerative & inflammatory diseases - Novel triazolopyridine compounds are disclosed that have a formula represented by the following: | 04-23-2009 |
20090105243 | Pyrrolo-Triazine Aniline Compounds Useful As Kinase Inhibitors - Compounds having the formula (I), | 04-23-2009 |
20090124612 | Fused heterocyclic 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. | 05-14-2009 |
20090131425 | INHIBITORS OF PROTEIN KINASES - Compounds that inhibit Aurora-kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed. | 05-21-2009 |
20090131426 | SOLID FORMS COMPRISING N-(5-TERT-BUTYL-ISOXAZOL-3-YL)-N'-UREA, COMPOSITIONS THEREOF, AND USES THEREWITH - Solid forms comprising N-(5-tert-butyl-isoxazol-3-yl)-N′-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders are disclosed. | 05-21-2009 |
20090143376 | Fused Heterocyclic Compounds and Their Use 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, chemotherapeutic induced neuropathy, neuropathy associated with an ischemic event, polyglutamine diseases, ocular diseases and/or disorders, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 06-04-2009 |
20090149455 | Use of Triazolopyrimidines for Controlling Plant Diseases on Legumes - The triazolopyrimidines of the general formula (I) | 06-11-2009 |
20090149456 | 2-Pyrimidinyl Pyrazolopyridine ErbB Kinase Inhibitors - The present invention provides 2-pyrimidinyl pyrazolopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents. | 06-11-2009 |
20090156594 | HETEROCYCLIC KINASE MODULATORS - The present disclosure provides heterocyclic protein kinase modulators and methods of using these compounds to treat diseases mediated by kinase activity. | 06-18-2009 |
20090163488 | FUSED HETEROCYCLE DERIVATIVES AND USE THEREOF - A compound represented by the formula (I): | 06-25-2009 |
20090163489 | Inhibitors of PI3 kinase - The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof, that inhibit phosphoinositide 3-kinase; | 06-25-2009 |
20090170844 | Spiro Tetracyclic Compound - Disclosed is an anti-coagulant which has extremely excellent inhibitory effect on FXa and an extremely poor inhibitory effect on hERG channel, and can be administered through the oral route. Specifically, disclosed is a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof. | 07-02-2009 |
20090170845 | USE OF IMIDAZO[2,1-b]-1,3,4-THIADIAZOLE-2-SULFONAMIDE COMPOUNDS TO TREAT NEUROPATHIC PAIN - Disclosed herein are methods and compositions for treating and/or prophylaxis of neuropathic pain in a subject. The methods comprise administering to the subject suffering from neuropathic pain, a therapeutically effective amount of a compound, according to Formula I: | 07-02-2009 |
20090176777 | Imidazo (1,2-a)Pyridin-3-YL-Acetic Acid Hydrazides, Proesses for Their Preparation and Pharmaceutical Uses Thereof - The invention provides novel imidazo[1,2-a]pyridin-3-yl-acetic acid hydrazides of formula (I) wherein R | 07-09-2009 |
20090176778 | Certain nitrogen containing bicyclic chemical entities for treating viral infections - Provided are certain chemical entities, pharmaceutical compositions, and methods of treatment of a member of the flaviviradae family of viruses such as hepacivirus (Hepatitis C or HCV). | 07-09-2009 |
20090209531 | Pyrimido-Benzimidazole Derivatives and the Use Thereof in the Form of Agonists and Antagonists of Melanocortin Receptors - The invention relates to novel pyrimido-benzimidazole derivatives. Said products exhibit a good affinity for certain melanocortin receptor sub-types, in particular MC4 receptors. Said products represent a particular interest for treating pathological disorders and diseases associated with one or several melanocortin receptors. Pharmaceutical compositions containing said products and the use thereof for a drug preparation are also disclosed. | 08-20-2009 |
20090221570 | Uses of 2-Phenyl-Substituted Imidazotriazinone Derivatives for Treating Pulmonary Hypertension - The present invention relates to the use of PDE 5 inhibitors generally and in particular of known 2-phenyl-substituted imidazotriazinone derivatives for manufacturing medicaments for the treatment of pathological states which can be treated by raising cGMP levels in certain tissues, such as, for example, of, for example: primary pulmonary hypertension, secondary pulmonary hypertension, pulmonary arterial hypertension, portopulmonary hypertension, hepatopulmonary syndrome, pulmonary hypertension caused by medicaments (amphetamines), interstitial lung disease, pulmonary hypertension occurring with HIV, thromboembolic pulmonary hypertension, pulmonary hypertension in children and neonates, pulmonary hypertension induced by atmospheric hypoxia (altitude sickness), COPD, emphysema, chronic bronchial asthma, mucoviscidosis-related pulmonary hypertension, right heart failure, left heart failure and global failure, and which can be treated by raising cGMP levels in certain tissues, such as, for example, isolated systiolic hypertension (ISH) and hardening of blood vessels, specifically of arterial blood vessels, and combination of PDE 5 inhibitors generally and in particular of known 2-phenyl-substituted imidazotriazinone derivatives with further therapeutic agents in the said indications. | 09-03-2009 |
20090221571 | HIV INTEGRASE INHIBITORS - Pyridopyrimidine carboxamide compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: | 09-03-2009 |
20090247515 | 11 Beta-HSD1 Modulators - A compound according to Formula A: | 10-01-2009 |
20090258872 | USE OF ARYL-SUBSTITUTED POLYCYCLIC AMINES AS MEDICAMENTS - The invention relates to therapeutic use of aryl-substituted polycyclic amines of the formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; | 10-15-2009 |
20090270388 | FUSED AZOLE-PYRIMIDINE DERIVATIVES - The present invention relates to novel fused azolepyriimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity. | 10-29-2009 |
20090275577 | IMIDAZOPYRIDINE AND IMIDAZOPYRIMIDINE DERIVATIVES AS ANTIBACTERIAL AGENTS - Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I as disclosed herein can be used in a variety of applications including use as antibacterial agents. | 11-05-2009 |
20090286777 | 5,6,Fused Pyrrolidine Compounds Useful as Tachykinin Receptor Antagonists - The present invention is directed to certain 5,6-fused pyrrolidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety. | 11-19-2009 |
20090286778 | MACROCYCLIC COMPOUNDS AND THEIR USE AS KINASE INHIBITORS - The present invention relates to macrocyclic compounds of Formula I: | 11-19-2009 |
20090286779 | PYRAZOLOPYRIMIDINES AS LIPID KINASE INHIBITORS - The invention relates to novel—at least 3,5-disubstituted-pyrazolo[1,5-a]pyrimidines of the formula I, | 11-19-2009 |
20090318436 | Fused heterocyclic 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. | 12-24-2009 |
20090318437 | SUBSTITUTED PYRAZOLO[1,5-a] PYRIDINE COMPOUNDS AND THEIR METHODS OF USE - The present invention is directed to substituted pyrazolo[1,5-a]pyridines and related methods for their synthesis and use. | 12-24-2009 |
20100009985 | THERAPEUTICALLY USEFUL SUBSTITUTED HYDROPYRIDO [3,2,1-ij] QUINOLINE COMPOUNDS - Disclosed herein are compounds represented by the structural formula: | 01-14-2010 |
20100016300 | Imidazoacridine Compounds for Treating FLT3-Mediated Disorders - A method of treating a FLT3-mediated condition in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof: (I), The conditions that can be treated by the compounds of the present invention and the definitions for the variables in formula (I) are provided herein. | 01-21-2010 |
20100016301 | Inhibitors of bruton's tyrosine kinase - This application discloses 6-Phenyl-imidazo[1,2-a]pyridine and 6-Phenyl-imidazo[1,2-b]pyridazine derivatives according to generic Formulae I-V: | 01-21-2010 |
20100016302 | Inhibitors of bruton's tyrosine kinase - This application discloses 6-Phenyl-imidazo[1,2-a]pyrazine derivatives according to generic Formulae I-V: | 01-21-2010 |
20100016303 | NOVEL PHENYLIMIDAZOLE DERIVATIVES AS PDE10A ENZYME INHIBITORS - This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. | 01-21-2010 |
20100029636 | Lck inhibitors - The invention relates to novel pyrazolo[1,5-A]pyrimidine compounds of Formula I | 02-04-2010 |
20100029637 | Chymase Inhibitors - Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving chymase. | 02-04-2010 |
20100029638 | FUSED HETEROCYCLYC INHIBITOR COMPOUNDS - The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin-dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound. | 02-04-2010 |
20100035874 | Organic compounds - There are described pyrazolo[5.1-b]oxazole derivatives useful as corticotropin releasing factor (CRF | 02-11-2010 |
20100035875 | TRIAZOLOPYRIDINE JAK INHIBITOR COMPOUNDS AND METHODS - A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R | 02-11-2010 |
20100048555 | IMIDAZOTHIAZOLE DERIVATIVES AS MARK INHIBITORS - Compounds of formula (I): are inhibitors of MARK, and hence useful for treatment of disorders involving 10 hyperphosphorylation of tau. | 02-25-2010 |
20100048556 | QUINOXALINE DERIVATIVES - The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I) | 02-25-2010 |
20100048557 | Triazolopyridine JAK Inhibitor Compounds and Methods - A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R | 02-25-2010 |
20100056511 | 2- [ (2-SUBSTITUTED) -IND0LIZIN-3-YL] -2-OXO-ACETAMIDE DERIVATIVES AS ANTIFUNGAL AGENTS - The invention provides compounds of formula (I), and pharmaceutically acceptable salts thereof wherein: R1, R2, R3, R4, R5, R6, R7, X and X | 03-04-2010 |
20100063046 | TETRACYCLIC IMIDAZOLE ANALOGS - The present invention provides tetracyclic imidazole analogs which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing these compounds, and methods of using the same. | 03-11-2010 |
20100075958 | PYRROLOTRIAZINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS - This invention relates to pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis. | 03-25-2010 |
20100093718 | Compounds - The invention relates to new bicyclic heterocyclic derivative compounds of Formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer The compounds of Formula (I) are inhibitors of FGFR, VEGFR or PDGFR. | 04-15-2010 |
20100093719 | PHARMACOKINETICALLY IMPROVED COMPOUNDS - A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided: | 04-15-2010 |
20100105675 | 11 BETA-HSD1 MODULATORS -
A compound according to Formula I:
| 04-29-2010 |
20100105676 | FUSED HETEROCYCLIC COMPOUNDS USEFUL AS KINASE MODULATORS - Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, [PLEASE INSERT CHEMICAL STRUCTURE HERE] (I) are useful as kinase modulators, including Btk modulation, wherein R1, R2, R4, Q, Y, A and D are as defined herein. | 04-29-2010 |
20100105677 | INDAZOLES, BENZOTHIAZOLES, BENZOISOTHIAZOLES, BENZISOXAZOLES, AND PREPARATION AND USES THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof. | 04-29-2010 |
20100113441 | SUBSTITUTED IMIDAZOPYRIMIDINES AND TRIAZOLOPYRIMIDINES - The invention relates to substituted imidazopyrimidines and triazolopyrimidines, to methods for the production thereof, and to the use of same for producing medicaments for the treatment and/or prophylaxis of diseases, especially haematological diseases, preferably leucopenia and neutropenia. | 05-06-2010 |
20100113442 | TRIAZOLOPYRIDINES AS PHOSPHODIESTERASE INHIBITORS FOR TREATMENT OF DERMAL DISEASES - The present invention relates to a compound according to formula (I), wherein X and Y are either C and N or N and C; Z is CH | 05-06-2010 |
20100120761 | Bicyclic Heterocyclic Compounds as FGFR Inhibitors - The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. | 05-13-2010 |
20100120762 | Triazine derivatives as inhibitors of phosphodiesterases - The invention relates to triazine derivatives of formula (I): | 05-13-2010 |
20100120763 | IMIDAZO[5,1-C][1,2,4]BENZOTRIAZINE DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASES - The invention relates to imidazo[5,1-c][1,2,4]benzotriazine derivatives of formula I: | 05-13-2010 |
20100130488 | Pyrazolo-Pyrimidines as Casein Kinase II (CK2) Modulators - A compound according to Formula (I) or a pharmaceutically acceptable salt thereof, wherein R | 05-27-2010 |
20100130489 | IMIDAZOLO-HETEROARYL DERIVATIVES WITH ANTIBACTERIAL PROPERTIES - The invention relates to Imidazolo-heteroaryl derivatives of formula (I). The compounds inhibit the activity of the Dlta enzyme of Gram-positive bacteria and are useful to treat Gram-positive bacterial infections. Furthermore the application discloses method for assessing the Dlta inhibitory activity of tested molecules and a method for measuring the efficacy of molecules in inhibiting bacteria proliferation in vitro. | 05-27-2010 |
20100137300 | Indolizine Acetic Acid Derivatives as CRTH2 Antagonists - The specific compounds of this list: {7-cyano-2-methyl-1-[4-(morpholine-4-sutfonyl)benzyl]indolizin-3-yl}acetic acid, {1-(3-chloro-4-ethanesulfonylbenzyl)-7-cyano-2-methylindolizin-3-yl}acetic acid, {1-[3-chloro4-(morpholine-4-sulfonyl)benzyl]-7-cyano-2-methylindolizin-3-yl}acetic acid, {1-(3-chloro-4-ethanesulfonylphenylsulfanyl)-7-cyano-2-methylindolizin-3-yl}acetic acid, {1-[3-chloro-4-(morpholine-4-sutfonyl)phenylsutfanyl]-7-cyano-2-methylindolizin-3-yl}acetic acid, {7-cyano-1-(6-fluoroquinolin-2-ylmethyl)-2-methylindolizin-3-yl}acetic acid are ligands of the CRTH2 receptor and are useful in the treatment of respiratory diseases. | 06-03-2010 |
20100152180 | 4-oxo-4,5-dihydropyrrolo[1,2-A)quinoxaline derivatives as inhibitors of poly(ADP-ribose) polymerase (PARP) - The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment. | 06-17-2010 |
20100152181 | AMINO PYRAZOLE COMPOUND - The present invention provides amino pyrazole compounds useful in the treatment of chronic myeloproliferative disorders and various cancers, e.g., glioblastoma, breast cancer, multiple myeloma, prostate cancer, and leukemias. | 06-17-2010 |
20100160310 | 2,4 (4,6) PYRIMIDINE DERIVATIVES - The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z | 06-24-2010 |
20100160311 | Fungicidal Azolopyrimidines, Process for Their Preparation and Their Use For Controlling Harmful Fungi, and Also Compositions Comprising Them - The present invention relates to azolopyrimidines of the formula I | 06-24-2010 |
20100173906 | Substituted 3,4,6,7-Tetrahydro-5H-1,2a,4a,8-Tetraazacyclopenta[cd]Phenalenes and Methods - Substituted 3,4,6,7-tetrahydro-5H-1,2a,4a,8-tetraazacyclopenta[cd]phenalene-9-amines, pharmaceutical compositions containing the compounds or salts thereof, intermediates, methods of making the compounds or salts thereof, and methods of use of these compounds or salts thereof or pharmaceutical compositions as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed. | 07-08-2010 |
20100197681 | Triazolopyridine Compounds and Their Use as Ask Inhibitors - The present invention relates to triazolopyridine compounds according to Formula (I), their use as medicament, for treating autoimmune disorders, inflammatory diseases, cardiovascular diseases and/or neurodegenerative diseases and a process for their preparation. | 08-05-2010 |
20100197682 | Organic Compounds - Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases. | 08-05-2010 |
20100197683 | FUSED RING COMPOUND AND USE THEREOF - Provided is a novel compound represented by the following formula | 08-05-2010 |
20100197684 | SUBSTITUTED HETEROCYCLIC COMPOUNDS - The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): | 08-05-2010 |
20100210640 | BENZAMIDE DERIVATIVES, THEIR PREPARATION AND USES IN MEDICINE THEREOF - The present invention discloses novel benzamide derivatives represented by general formula (I), their preparation, pharmaceutical compositions containing the derivatives and their use as medicament, especially as a 5-HT | 08-19-2010 |
20100210641 | Organic Compounds - Compounds of formula I: in free or salt or solvate form, where R | 08-19-2010 |
20100210642 | ACETYLENYL-PYRAZOLO-PYRIMIDINE DERIVATIVES - The present invention relates to compounds of formula (I): | 08-19-2010 |
20100216786 | NEW COMPOUNDS - The present invention relates to the adenosine A | 08-26-2010 |
20100222339 | Thiazole pyrazolopyrimidines CRF1 receptor antagonists - The present invention relates to compounds of Formula (I), pharmaceutical compositions thereof, and use thereof as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric and neuroendocrine disorders, neurological diseases, and metabolic syndrome. | 09-02-2010 |
20100222340 | SUBSTITUTED PYRIDO [1,2-a] ISOQUINOLINE DERIVATIVES - The present invention relates to compounds of formula (I) | 09-02-2010 |
20100227860 | DISALT INHIBITORS OF IL-12 PRODUCTION - This invention relates to disalt nitrogen-heteroaryl inhibitors of IL-12 production, and related methods and pharmaceutical compositions. | 09-09-2010 |
20100227861 | IMIDAZO[1,2-beta]PYRIDAZINE AND PYRAZOLO[1,5-alpha]PYRIMIDINE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS - The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II): | 09-09-2010 |
20100240647 | Treatment of Alzheimer's Disease and Related Conditions - Compounds of formula (I) inhibit microtubule affinity regulating kinase (MARK), and hence are suitable for treating diseases associated with abnormal phosphorylation of tau. | 09-23-2010 |
20100240648 | HEXAHYDRO-PYRROLO-ISOQUINOLINE COMPOUNDS - Certain hexahydro-pyrrolo-isoquinoline compounds are histamine H | 09-23-2010 |
20100249127 | SUBSTITUTED INDOLO-PYRIDINONE COMPOUNDS - The present invention relates to substituted indolo-pyridinone compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted indolo-pyridinone compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof. | 09-30-2010 |
20100273792 | MACROCYCLIC INDOLES AS HEPATITIS C VIRUS INHIBITORS - The present invention relates to inhibitors of HCV replication of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, | 10-28-2010 |
20100286139 | AMINO PYRAZOLE COMPOUND - The present invention provides amino pyrazole compounds useful in the treatment of chronic myeloproliferative disorders and various cancers, e.g., glioblastoma, breast cancer, multiple myeloma, prostate cancer, and leukemias. | 11-11-2010 |
20100286140 | TRIAZOLOPHTHALAZINES - The compounds of formula I | 11-11-2010 |
20100292231 | Indazole Compounds for Treating Inflammatory Disorders, Demyelinating Disorders and Cancers - Compounds of formula (I) or formula (Ia) and a method of treating a patient suffering from certain inflammatory disorders, demyelinating disorders, FLT3-mediated disorders, CSF-1R-mediated disorders, cancers and leukemias, comprising administering to said patient a therapeutically effective amount of a compound of formula (I) or formula (Ia) or a pharmaceutically acceptable salt thereof. | 11-18-2010 |
20100292232 | NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS - Disclosed herein are antiviral agents, in particular non-nucleoside reverse transcriptase inhibitors (NNRTIs) of the formula | 11-18-2010 |
20100292233 | DIHYDRO-1H-PYRROLO[1,2-A]INDOL-1-YL CARBOXYLIC ACID DERIVATIVES WHICH ACT AS S1P1 AGONISTS - The present invention relates to certain (1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl carboxylic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, sepsis, myocardial infarction, ischemic stroke, acne, microbial infections or diseases and viral infections or diseases. | 11-18-2010 |
20100298314 | NOVEL JNK INHIBITORS - Disclosed are substituted imidazo[1,2-a]pyridines, imidazo[1,2-a]pyrazines, imidazo[1,2-c]pyrimidines and imidazo[1,2-d]triazines compounds of the formula: (1.0) Also disclosed are methods for treating JNK1 and ERK mediated diseases using the compounds of formula 1.0. | 11-25-2010 |
20100298315 | NOVEL 6-TRIAZOLOPYRIDAZINESULFANYL BENZOTHIAZOLE AND BENZIMIDAZOLE DERIVATIVES, METHOD FOR PRODUCTION THEREOF AND APPLICATION AS MEDICAMENTS AND PHARMNACEUTICAL COMPOSITIONS AND NOVEL USE AS MET INHIBITORS - The disclosure relates to compounds of formula (I): | 11-25-2010 |
20100305118 | PYRIMIDINE INHIBITORS OF KINASE ACTIVITY - Described herein are compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof, | 12-02-2010 |
20100311740 | IMIDAZOPYRIDINE DERIVATIVES AS ACID PUMP ANTAGONISTS - This invention relates to newly identified imidazopyridine compounds of formula (I), to the use of such compounds in treating GERD and the like. | 12-09-2010 |
20100324037 | PHARMACOKINETICALLY IMPROVED COMPOUNDS - A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided: | 12-23-2010 |
20110003806 | Heteroaryls and uses thereof - This invention provides compounds of formula IA or IB: | 01-06-2011 |
20110003807 | Thiazole derivatives - The present invention relates to a compound represented by the formula (I) or (I′): | 01-06-2011 |
20110003808 | OCTAHYDROQUINOLIZINES FOR ANTIDIABETIC TREATMENT - This invention relates to novel octahydroquinolizines for treatment or prevention of diabetes mellitus and its complications, for treatment or prevention of hyperlipidemia, for treatment of diabetic dyslipidemia, for treatment or prevention of the metabolic syndrome, for treatment of diseases related to metabolic dysfunction, for treatment of obesity or obesity-related diseases. The invention also includes pharmaceutical compositions and kits comprising these compounds alone or in combination with other drugs or compounds aiming towards an improved treatment or prevention of the aforementioned diseases or syndromes in humans or animals. | 01-06-2011 |
20110009404 | 4-ARYL-2-ANILINO-PYRIMIDINES - The present invention relates to compounds of Formula (Ia) or (Ib), the N-oxide forms, pharmaceutically acceptable addition salts, quaternary amines, stereoisomers, tautomers, racemics, metabolites, prodrugs, hydrates, or solvates thereof, | 01-13-2011 |
20110015192 | SIRTUIN MODULATING COMPOUNDS - 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 benfit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 01-20-2011 |
20110021518 | PYRROLOTRIAZINE DERIVATIVES USEFUL FOR TREATING CANCER THROUGH INHIBITION OF AURORA KINASE - This invention relates to novel compounds 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. | 01-27-2011 |
20110021519 | TETRAHYDROPTERIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 01-27-2011 |
20110021520 | OXAZINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS - The invention relates to novel heterocyclic compounds of the formula | 01-27-2011 |
20110021521 | FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS - The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: | 01-27-2011 |
20110034456 | IMIDAZOPYRIDAZINES AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS - The invention relates to novel compounds of formula I | 02-10-2011 |
20110039842 | COMPOUNDS HAVING ANTIVIRAL PROPERTIES - The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided. | 02-17-2011 |
20110046130 | TETRAHYDRONAPHTHYRIDINES AND AZA DERIVATIVES THEREOF AS HISTAMINE H3 RECEPTOR ANTAGONISTS - The invention relates to compounds of formula (I), wherein X | 02-24-2011 |
20110053929 | IMIDAZO-, PYRAZOLOPYRAZINES AND IMIDAZOTRIAZINES AND THEIR USE - The invention relates to substituted imidazo-, pyrazolopyrazines and imidazotriazines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of hematological disorders, preferably of leukopenias and neutropenias. | 03-03-2011 |
20110053930 | INHIBITORS OF THE BMP SIGNALING PATHWAY - The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. | 03-03-2011 |
20110065699 | POLYSUBSTITUTED DERIVATIVES OF 2-ARYL-6-PHENYL-IMIDAZO[1,2-a]PYRIDINES, AND PREPARATION AND THERAPEUTIC USE THEREOF - Compounds of formula (I): | 03-17-2011 |
20110065700 | POLYSUBSTITUTED DERIVATIVES OF 6-HETEROARYLIMIDAZO[1,2-a]PYRIDINES, AND PREPARATION AND THERAPEUTIC USE THEREOF - Compounds of formula (I): | 03-17-2011 |
20110077243 | Triazolopyridine Compounds Useful As Kinase Inhibitors - A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula (I), and methods of treating conditions associated with the activity of p38 kinase. | 03-31-2011 |
20110082135 | INHIBITORS OF AKT ACTIVITY - The instant invention provides for substituted [1,2,4]triazolo[4,3-a]-1,5-naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity, especially Akt1 by administering the compound to a patient in need of treatment of cancer. | 04-07-2011 |
20110082136 | INHIBITORS OF JANUS KINASES - The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer. | 04-07-2011 |
20110086850 | RADIOSENSITIZATION OF TUMORS WITH INDAZOLPYRROLOTRIAZINES FOR RADIOTHERAPY - Provided herein is a method of radiosensitizing a tumor in a subject, which comprises administering to the subject a radiosensitizing amount of an indazolpyrrolotriazine of Formula I. Also provided herein is a method of treating a tumor in a subject, which comprises the steps of administering to the subject a radiosensitizing amount of an indazolpyrrolotriazine of Formula I, and a therapeutically effective fraction of radiation. | 04-14-2011 |
20110086851 | SUBSTITUTED QUINAZOLINES AND THEIR USES FOR MYEOLOPROLIFIC AND THROMBOTIC DISEASES - This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim | 04-14-2011 |
20110092497 | IMIDAZOLOPYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following: | 04-21-2011 |
20110092498 | 3-(3-PYRIMIDIN-2-YLBENZYL)-1,2,4-TRIAZOLO[4,3-B]PYRIDAZINE DERIVATIVES AS MET KINASE INHIBITORS - Compounds of the formula (I), in which R | 04-21-2011 |
20110098291 | ANTAGONIST OF SMOOTHENED - Described herein are compounds, pharmaceutical compositions and methods for the inhibition of Hedgehog signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human and veterinary diseases and disorders. | 04-28-2011 |
20110118255 | PYRAZOLO[1,5-a]PYRIMIDINES USEFUL AS JAK2 INHIBITORS - The present invention relates to compounds of formula (I) useful as selective inhibitors of JAK2 kinase. The invention also provides pharmaceutical acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various diseases, conditions or disorders. The invention also provides processes for preparing the compounds of the invention. | 05-19-2011 |
20110118256 | IMIDAZO [1,2-A] PYRIDIN-3-YL-ACETIC ACID HYDRAZIDES, PROCESSES, USES AND COMPOSITIONS - The invention provides novel imidazo[1,2-a]pyridin-3-yl-acetic acid hydrazides of formula (I) wherein R | 05-19-2011 |
20110124640 | FUSED HETEROCYCLIC COMPOUNDS USEFUL AS KINASE MODULATORS - Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation, wherein R | 05-26-2011 |
20110130396 | IMIDAZOTHIADIAZOLE DERIVATIVES - Novel imidazo[2,1-b][1,3,4]thiadiazole derivatives of formula (I) | 06-02-2011 |
20110136803 | Triazolophthalazines - The compounds of formula (I) | 06-09-2011 |
20110144100 | TRIAZOLOPYRIDINE COMPOUNDS AS PIM KINASE INHIBITORS - Compounds of Formula (I): I in which B, R | 06-16-2011 |
20110152256 | 1,2,4-TRIAZOLO[4,3-c]PYRIMIDIN-3-ONE AND PYRAZOLO[4,3-e]-1,2,4-TRIAZOLO[4,3-c]PYRIMIDIN-3-ONE COMPOUNDS FOR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS - Compounds of the Formula I wherein R | 06-23-2011 |
20110152257 | ETHYNYL COMPOUNDS USEFUL FOR TREATMENT OF CNS DISORDERS - The present invention relates to ethynyl compounds of formula | 06-23-2011 |
20110166133 | FUSED NITROGEN CONTAINING HETEROCYCLES AND COMPOSITIONS THEREOF AS KINASE INHIBITORS - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Ros, KDR, FMS, C-FMS, FLT3, c-Kit, JAK2, JAK3, Aurora, PDGFR, Lck, TrkA, TrkB, TrkC, IGF-IR, ALK4, ALK5 and ALK or combinations thereof. | 07-07-2011 |
20110172227 | ALKYL 3-((2-AMIDOETHYL)AMINO)-8-AZABICYCLO[3.2.1]OCTANE-8-CARBOXYLATE ANALOGS AS SELECTIVE M1 AGONISTS AND METHODS OF MAKING AND USING SAME - In one aspect, the invention relates to compounds having a general structure: | 07-14-2011 |
20110178077 | Anti-infective compounds - The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis. | 07-21-2011 |
20110178078 | SUBSTITUTED 3-ARYLSULFONYL-PYRAZOLO[1,5-A]PYRIMIDINES, SEROTONIN 5-HT6 RECEPTOR ANTAGONISTS AND METHODS FOR THE PRODUCTION AND USE THEREOF - The invention relates to the novel substituted 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines of the general formula 1, pharmaceutically acceptable salts and/or hydrates thereof, serotonin 5-HT | 07-21-2011 |
20110183971 | 3,4-DIHYDRO-2H-PYRAZINO[1,2-A]INDOL-1-ONE DERIVATIVES ACTIVE AS KINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM - Compounds which are 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them. | 07-28-2011 |
20110190289 | Imidazolothiadiazoles for Use as Protein Kinase Inhibitors - There is provided compounds of formula (I), wherein Z, M, R | 08-04-2011 |
20110207728 | COMPOUNDS FOR TREATING RESPIRATORY SYNCYTIAL VIRUS INFECTIONS - The present invention relates to compounds of formula (I) | 08-25-2011 |
20110212956 | Pyrazolopyrimidines for treating CNS disorders - Substituted pyrazolopyrimidine derivatives of formula (I) | 09-01-2011 |
20110212957 | INDAZOLES, BENZOTHIAZOLES, AND BENZOISOTHIAZOLES, AND PREPARATION AND USES THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof. | 09-01-2011 |
20110218196 | COMPOUNDS OF ESTROGEN-RELATED RECEPTOR MODULATORS AND THE USES THEREOF - The compounds according to formula (VIII), their pharmaceutically acceptable acid or base addition salts, and the uses thereof. These compounds and their pharmaceutically acceptable acid or base addition salts can be used for preparing medicaments for modulating estrogen related receptors (ERR), and treating metabolic diseases, such as high blood fat, fatty liver, hyperglycemia, diabetes, obesity. The substituents of the formula are defined in the description. | 09-08-2011 |
20110237582 | PYRIDO[3,4-B]INDOLES AND METHODS OF USE - This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 09-29-2011 |
20110251191 | USE OF SUBSTITUTED 2, 3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINES FOR THE TREATMENT OF MYELOMA - The present invention relates to the use of 2,3-dihydroimidazo[1,2-c]quinazoline compounds, and of pharmaceutical compositions containing such compounds, for the treatment or prophylaxis of multiple myeloma, as a sole agent or in combination with other one or more other active ingredients. | 10-13-2011 |
20110251192 | AMIDE COMPOUNDS, THEIR PHARMACEUTICAL COMPOSITIONS, THEIR PREPARATION METHOD AND THEIR USES - The present invention pertains to the field of pharmaceutical chemistry and discloses 8-(3-aminopropyl)-3-exo-8-azabicyclo[3.2.1]octane-3-amino amide compounds represented by formula I, the pharmaceutical compositions, the preparation method and the use thereof. Such compounds or pharmaceutically acceptable salts thereof can be used as an antagonist of CCR5 in preparing medicaments for treating diseases mediated by CCR5, particularly HIV infection, asthma, rheumatoid arthritis, autoimmune diseases and chronic obstructive pulmonary diseases (COPD). | 10-13-2011 |
20110257171 | NOVEL IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, METHOD FOR THE PREPARATION THEREOF, USE THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE IN PARTICULAR AS MET INHIBITORS - The invention relates to the novel products of formula (I): in which: Ra is H, Hal, aryl or heteroaryl, which are optionally substituted; Rb is H, Rc, —COORc-CO-Rc or —CO—NRcRd; where Rc is alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd is H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors. | 10-20-2011 |
20110257172 | 3-(3-Pyrimidine-2-yl-benzyl)-[1,2,4] triazolo[4,3-b]pyrimidine derivatives - Compounds of the formula I, in which R | 10-20-2011 |
20110257173 | 3 (3-Pyrimidin-2-ylbenzyl)-1,2,4-triazolo[4,3-b]pyridazine derivatives - Compounds of the formula (I), in which R | 10-20-2011 |
20110263592 | IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - Imidazo[1,2-α]pyridine derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT | 10-27-2011 |
20110263593 | NOVEL IMIDAZO[1,2-a]PYRIMIDINE DERIVATIVES, METHOD FOR THE PREPARATION THEREOF, USE THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE, IN PARTICULAR AS MET INHIBITORS - The disclosure concerns imidazo[1,2-a]pyrimidine derivatives of formula (I) and isomers and pharmaceutically acceptable salts thereof. Methods for preparing the compounds, pharmaceutical compositions, and methods of treatment also are disclosed. | 10-27-2011 |
20110263594 | NOVEL TRIAZOLO(4,3-A)PYRIDINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF, USE THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE, IN PARTICULAR AS MET INHIBITORS - The invention relates to the novel products of formula (I): in which: Ra represents H, Hal, aryl or heteroaryl, which is optionally substituted; Rb represents H, Rc, —COORc-CO-Rc or —CO—NRcRd; where Rc represents alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd represents H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors. | 10-27-2011 |
20110269754 | COMPOUNDS AND COMPOSITIONS FOR REDUCING LIPID LEVELS - Compositions comprising extracts or isolated or purified compounds from plants of the genus | 11-03-2011 |
20110275627 | INDOLIZINE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I): | 11-10-2011 |
20110275628 | NOVEL PYRAZOLE-3-CARBOXAMIDE DERIVATIVE HAVING 5-HT2B RECEPTOR ANTAGONIST ACTIVITY - Disclosed is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, which is useful as a selective antagonist of a 5-HT | 11-10-2011 |
20110281863 | IMIDAZO[1,2-B]PYRIDAZINE AND PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS - The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II): | 11-17-2011 |
20110288085 | IMIDAZOPYRIDINE AND IMIDAZOPYRAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS - A compound of Formula (I) or Formula (II) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) or Formula (II), and methods of treating conditions associated with the activity of p38 kinase. | 11-24-2011 |
20110288086 | POLYCYCLIC QUINAZOLINES, PREPARATION THEREOF, AND USE THEREOF - At least one active pharmaceutical ingredient is chosen from polycyclic quinazolines of formula V, | 11-24-2011 |
20110288087 | FUSED RING COMPOUND AND USE THEREOF - Provided is a novel compound represented by the following formula | 11-24-2011 |
20110294800 | HYPOGLYCEMIC DIHYDROPYRIDONES - The present invention provides, inter alia, a compound of formula I: wherein the substituent designations are indicated in the Specification. The present invention also provides pharmaceutical compositions comprising a compound of formula I, and methods of treatment or prevention of diabetes or hyperglycemia in a patient, and of normalizing blood glucose levels in a subject, by administering an effective amount of a compound of formula I. | 12-01-2011 |
20110294801 | MACROCYCLICS PYRIMIDINES AS AURORA KINASE INHIBITORS - Macrocyclic derivative compounds that inhibit protein kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed kinase activity such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases. | 12-01-2011 |
20110301160 | Inhibitors of P38 and Methods of Using the Same - In general, the present invention relates to compounds capable of inhibiting p38 in vivo or in vitro, and methods for treating conditions associated with p38 activity or cytokine activity. | 12-08-2011 |
20110312957 | IMIDAZOPYRIDINES AND IMIDAZOPYRIMIDINES AS HIV-I REVERSE TRANSCRIPTASE INHIBITORS - The invention provides compounds of formula A or B which are useful in the treatment of a subject infected with HIV. | 12-22-2011 |
20110319406 | 2-PYRIDYL SUBSTITUTED IMIDAZOLES AS THERAPEUTIC ALK5 AND/OR ALK4 INHIBITORS - This invention relates to 2-pyridyl substituted imidazoles which are inhibitors of the transforming growth factor-β (TGF-β) type I receptor (ALK5) and/or the activin type I receptor (ALK4), methods for their preparation, and their use in medicine, specifically in the treatment and prevention of a disease state mediated by these receptors. | 12-29-2011 |
20110319407 | INDAZOLES, BENZOTHIAZOLES, BENZOISOTHIAZOLES, BENZISOXAZOLES, AND PREPARATION AND USE THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof. | 12-29-2011 |
20110319408 | Methods of Treating Fibrosis, Cancer and Vascular Injuries - This invention relates to use of inhibitors of the transforming growth factor-β (TGF-β) type I receptor (ALK5) and/or the activin type I receptor (ALK4) in treating, preventing, or reducing fibrosis, cancer, and vascular injuries. | 12-29-2011 |
20120004222 | CB2 RECEPTOR LIGANDS FOR THE TREATMENT OF PAIN - The present invention relates to compounds represented by Formula (I) and Formula (II): | 01-05-2012 |
20120004223 | COMPOUNDS, COMPOSITIONS AND METHODS FOR REDUCING LIPID LEVELS - The present technology relates to compounds of Formulas (V) and (VI) and methods of making and using such compounds. Methods of use include prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Compounds disclosed herein also lower total cholesterol, LDL-cholesterol, and triglycerides and increase hepatic LDL receptor expression, inhibit PCSK9 expression, and activate AMP-activated protein kinase. | 01-05-2012 |
20120028974 | TRIAZOLOPYRIDINES AS PHOSPHODIESTERASE INHIBITORS FOR TREATMENT OF DERMAL DISEASES - The present invention relates to a compound according to formula I, wherein R | 02-02-2012 |
20120028975 | SUBSTITUTED TRIAZOLOPYRIDINES AND ANALOGS THEREOF - The present invention relates to substituted triazolopyridines and analogs thereof, the use of the compounds as phosphodiesterase 10 (PDE10) inhibitors for the treatment of PDE10-modulated disorders, to pharmaceutical compositions comprising the compounds. | 02-02-2012 |
20120035171 | BICYCLIC HETEROCYCLYL DERIVATIVES AS FGFR KINASE INHIBITORS FOR THERAPEUTIC USE - The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. | 02-09-2012 |
20120035172 | Purinone Derivatives as HM74A Agonists - The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease. | 02-09-2012 |
20120040979 | IMIDAZO[1,2-B]PYRIDAZINES, PROCESSES, USES, INTERMEDIATES AND COMPOSITIONS - The invention provides novel imidazo[1,2-b]pyridazines of formula (I) and pharmaceutically acceptable salts, polymorphs, hydrates, tautomers, solvates and stereoisomers thereof. | 02-16-2012 |
20120046282 | METHODS AND COMPOUNDS FOR ANTIMICROBIAL INTERVENTION - The present invention provides Wall Teichoic Acid biosynthesis inhibitors such as compound 1835F03 (targocil) and related synthetic analogs. The invention also provides pharmaceutical compositions thereof and methods for treating bacterial infection and the suppression of growth of bacterial cells by administering a Wall Teichoic Acid biosynthesis inhibitor. The invention is particularly useful for the treatment of Methicillin-resistant | 02-23-2012 |
20120058999 | Substituted Tetrahydropyrrolopyrazine Compounds - Tetrahydropyrrolopyrazine compounds, methods for their preparation, pharmaceutical compositions containing such compounds, and a method of using such compounds for the treatment of pain and other conditions mediated at least partially by Bradykinin 1 receptors (B1R). | 03-08-2012 |
20120071474 | INHIBITORS OF PI3 KINASE - The present invention relates to compounds of Formula I, II or III or a pharmaceutically acceptable salt thereof; | 03-22-2012 |
20120077809 | PYRIMIDOPYRIDAZINE DERIVATIVES USEFUL AS P38 MAPK INHIBITORS - A compound formula (IA) or (IB), or a pharmaceutically acceptable thereof; wherein the substituents are defined as in the claims, and their use as P38 MAP kinase. | 03-29-2012 |
20120077810 | Inhibitors Of AKT Activity - The instant invention provides for substituted fused pyrimidine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer. | 03-29-2012 |
20120083492 | IMIDAZOPYRAZINES FOR USE AS KINASE INHIBITORS - There is provided compounds of formula (I), wherein R | 04-05-2012 |
20120094995 | 2-AZA-BICYCLO[2.2.1]HEPTANE COMPOUNDS AND USES THEREOF - This invention relates to 2-aza-bicyclo[2.2.1]heptane compounds (and salts thereof), the process for making such a compound and pharmaceutical compositions comprising such a compound. The invention also relates to the use of the compounds for modulating the glycine transporter 1 (GlyT1) and for the treatment of psychosis, cognitive disorders, bipolar disorders, depression disorders, anxiety disorders, post-traumatic stress disorders and pain. | 04-19-2012 |
20120094996 | Imidazo [2, 1-B] [1, 3, 4] Thiadiazole Derivatives - There is provided compounds of formula (I): wherein R | 04-19-2012 |
20120101093 | SUBSTITUTED IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS BETA-SECRETASE INHIBITORS - The present invention is directed to substituted imidazo[1,2-a]pyridine derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which BACE is involved. | 04-26-2012 |
20120101094 | INDAZOLES, BENZOTHIAZOLES, AND BENZOISOTHIAZOLES, AND PREPARATION AND USES THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof. | 04-26-2012 |
20120129850 | IMIDAZOLOTHIAZOLE COMPOUNDS FOR THE TREATMENT OF DISEASE - Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases. | 05-24-2012 |
20120135986 | Bicyclic Heteroaryl Compounds - This invention relates to compounds of the general formula: | 05-31-2012 |
20120135987 | NOVEL PHENYLIMIDAZOLE DERIVATIVES AS PDE10A ENZYME INHIBITORS - This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. | 05-31-2012 |
20120142680 | HETEROALKYL LINKED PYRIMIDINE DERIVATIVES - The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to heteroalkyl linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other conditions or disorders associated with kinases. | 06-07-2012 |
20120142681 | HETEROCYCLIC HYDRAZONE COMPOUNDS - The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I). | 06-07-2012 |
20120149699 | IMIDAZO[1,2-a]PYRIDINE SULFONAMIDES AS TRPM8 MODULATORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: | 06-14-2012 |
20120157451 | RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF - Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 06-21-2012 |
20120165326 | DERIVATIVES OF 6-(6-SUBSTITUTED-TRIAZOLOPYRIDAZINE-SULFANYL) 5-FLUORO BENZOTHIAZOLES AND 5-FLUORO BENZIMIDAZOLES, PREPARATION THEREOF, USE THEREOF AS DRUGS, AND USE THEREOF AS MET INHIBITORS - The invention relates to novel products of the formula (I) where: (II) is a single or double bond; F is a fluorine atom, Ra is H, HaI, alkoxy, O-cycloalkyl, —O— heterocycloalkyl; —NH-heterocycloalkyl, heteroaryl, phenyl, NHCOalk NHCOcycloalk or NR1 R2; X is S, SO or SO2, A is NH or S; W is H, alkyl, or COR with R being cycloalkyl; alkyl optionally substituted by NR3R4, alkoxy, hydroxy, phenyl, heteroaryl or heterocycloalkyl; alkoxy optionally substituted by NR3R4, i.e. a O—(CH2)n-NR3R4 radical, an O-phenyl or an O—(CH2)n-phenyl radical, with phenyl optionally substituted and n=1 to 4; or the NR1 R2 radical; R1 is H or alk and R2 is H, cycloalkyl or alkyl; R3 and R4 are H, alk, cycloalkyl, heteroaryl or phenyl; R1, R2 and/or R3, R4 form a cycle together with N optionally containing O, S, N and/or NH; heterocycloalkyl, heteroaryl and phenyl and cycles all being optionally substituted; wherein said products can be in any isomer or salt form, and can be used as drugs, in particular as MET inhibitors. | 06-28-2012 |
20120178751 | 2-ARYLIMIDAZO[1,2-B]PYRIDAZINE, 2-PHENYLIMIDAZO[1,2-A]PYRIDINE, AND 2-PHENYLIMIDAZO[1,2-A]PYRAZINE DERIVATIVES - Disclosed are compounds of formula (I): | 07-12-2012 |
20120184546 | [1,2,4]TRIAZOLO [1,5-C]PYRIMIDINE DERIVATIVES AS HSP90 MODULATORS - The present invention relates to [1,2,4]triazolo[1,5-c]pyrimidine derivatives of formula (I) which inhibit the activity of Heat Shock Protein Hsp90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, methods of treating diseases and the pharmaceutical compositions comprising these compounds. | 07-19-2012 |
20120196855 | OXYGEN LINKED PYRIMIDINE DERIVATIVES - The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases. | 08-02-2012 |
20120202807 | AZABICYCLOALKANE DERIVATIVES, PREPARATION THEREOF AND USE THEREOF IN THERAPY - The invention relates to compounds of the general formula (I): | 08-09-2012 |
20120208810 | NOVEL 1,2,3,4-TETRAHYDRO-PYRIMIDO(1,2-A)PYRIMIDIN-6-ONE DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL USE THEREOF - The invention relates to the novel materials of formula (I), where: R | 08-16-2012 |
20120220582 | IMIDAZOPYRAZINE SYK INHIBITORS - Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample. | 08-30-2012 |
20120232075 | Fused Pyrazine Compounds Useful for the Treatment of Degenerative and Inflammatory Diseases - Novel fused pyrazine compounds are disclosed that have a formula represented by the following: | 09-13-2012 |
20120232076 | QUINOLIZIDINONE CARBOXAMIDE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to 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. | 09-13-2012 |
20120238564 | IMIDAZO PYRAZINES - Compounds of formula | 09-20-2012 |
20120238565 | TRIAZOLOPYRIDINE COMPOUNDS AND THEIR USE AS ASK INHIBITORS - The present invention relates to triazolopyridine compounds according to Formula (I), their use as medicament, for treating autoimmune disorders, inflammatory diseases, cardiovascular diseases and/or neurodegenerative diseases and a process for their preparation. | 09-20-2012 |
20120245164 | DIPHENYL-PYRAZOLOPYRIDINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF AS NUCLEAR RECEPTOR NOT MODULATORS - The invention relates to a formula (I), in which R is a hydrogen or halogen atom or a (C1-C6)alkyl group; X is one or more substituents selected from a hydrogen or halogen atom, a (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkoxy, cyano, hydroxy, or hydroxy(C1-C6)alkyl group; Y is a hydrogen or halogen atom or a (C1-C6)alkyl group; R1 is an NR2R3 or OR4 group; R2 and R3 independently are a hydrogen atom, a (C1-C6)alkyl, hydroxy(C1-C6)alkyl or oxo(C1-C6)alkyl group or R2 and R3, together with the nitrogen atom supporting the same, form a heterocycle optionally substituted by a (C1-C6)alkyl, hydroxy or oxo group; and R4 is a (C1-C6)alkyl, hydroxy(C1-C6)alkyl, or oxo(C1-C6)alkyl group, in the base or acid addition salt state. Said formula can be used therapeutically for treating or preventing diseases linked to the nuclear receptors Nurr-1, also known as NR4A2, NOT, TINUR, RNR-1, and HZF3. | 09-27-2012 |
20120277224 | HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK - Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus. | 11-01-2012 |
20120277225 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase. | 11-01-2012 |
20120289503 | AQUEOUS SOLUTION COMPRISING 3 - QUINUCLIDINONES FOR THE TREATMENT HYPERPROLIFERATIVE, AUTOIMMUNE AND HEART DISEASE - A liquid composition that is an aqueous solution of a compound of formula (I), wherein the aqueous solution has a pH from about 3.0 to about 5.0. The liquid composition may be used in the treatment of a disorder selected from hyperproliferative diseases, autoimmune diseases and heart diseases. | 11-15-2012 |
20120302564 | (1,2,4)TRIAZOLO[4,3-A]QUINOXALINE DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASES - The invention relates to (1,2,4)triazolo[4,3-a]quinoxaline derivatives which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases. | 11-29-2012 |
20120302565 | KINASE INHIBITORS FOR PREVENTING OR TREATING PATHOGEN INFECTION AND METHOD OF USE THEREOF - The present invention provides compositions and methods of use thereof to prevent and/or treat pathogenic infection. In particular, the present invention provides the use of kinase inhibitors to inhibit kinases that involve in pathogen-host cell interactions that are associated with or cause pathogenic infections, therefore, to effectively prevent and/or treat pathogenic infections with far less likely to engender resistance as compared to conventional antibiotics and anti-viral drugs. The present invention further provides the use of kinase inhibitors for the treatment of acute pathogenic infections for a short period of time to avoid toxicities that may caused by long term use of these kinase inhibitors. | 11-29-2012 |
20120309754 | PYRAZOLOPYRIMIDINE COMPOUNDS AND THEIR USE AS PDE10 INHIBITORS - The present invention relates to a compound represented by formula [I]: wherein: R | 12-06-2012 |
20130005721 | INDOLIZINE INHIBITORS OF 5-LIPOXYGENASE - Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of 5-lipoxygenase (5-LO). Also described herein are methods of using such 5-LO inhibitors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions, diseases, or disorders. | 01-03-2013 |
20130012506 | ANTI-INFECTIVE PYRIDO (1,2-A) PYRIMIDINES - The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis. | 01-10-2013 |
20130023530 | NOVEL NK-3 RECEPTOR SELECTIVE ANTAGONIST COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN NK-3 RECEPTORS MEDIATED DISORDERS - The present invention is directed to novel compounds of formula I | 01-24-2013 |
20130029981 | COMPOUNDS, COMPOSITIONS, AND METHODS FOR CONTROLLING BIOFILMS - The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2- | 01-31-2013 |
20130029982 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. | 01-31-2013 |
20130040946 | SUBSTITUTED IMIDAZOPYRIMIDINES AND TRIAZOLOPYRIMIDINES - The invention relates to substituted imidazo- and triazolopyrimidines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of haematological disorders, preferably of leucopenias and neutropenias. | 02-14-2013 |
20130053379 | 4-ARYL-2-ANILINO-PYRIMIDINES - The present invention relates to compounds of Formula (Ia) or (Ib), the N-oxide forms, pharmaceutically acceptable addition salts, quaternary amines, stereoisomers, tautomers, racemics, metabolites, prodrugs, hydrates, or solvates thereof, | 02-28-2013 |
20130059844 | 2-PHENYL SUBSTITUTED IMIDAZOTRIAZINONES AS PHOSPHODIESTERASE INHIBITORS - The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction. | 03-07-2013 |
20130059845 | BICYCLIC AGONISTS OF GPR131 AND USES THEREOF - The present disclosure relates to compounds that act as agonists of, or otherwise modulate the activity of, GPR131 and to their use in the treatment of various diseases. In particular embodiments, the structure of the compounds is given by Formula I: | 03-07-2013 |
20130059846 | COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS - The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFRα, PDGFRβ) kinases. | 03-07-2013 |
20130065893 | IMIDAZOLE DERIVATIVES AS ALDOSTERONE SYNTHASE INHIBITORS - The present invention provides a compound of formula (I) or pharmaceutically acceptable salt thereof, wherein the variables R | 03-14-2013 |
20130085141 | SUBSTITUTED OCTAHYDROPYRROLO[1,2-a]PYRAZINE SULFONAMIDES AS CALCIUM CHANNEL BLOCKERS - The present application relates to: (a) compounds of Formula (I): | 04-04-2013 |
20130085142 | SUBSTITUTED OCTAHYDROPYRROLO[1,2-a]PYRAZINES AS CALCIUM CHANNEL BLOCKERS - The present application relates to: (a) compounds of Formula (I): | 04-04-2013 |
20130085143 | AMINOACID DERIVATIVES, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTICAL USES AS INHIBITORS OF ONCOGENIC SIGNALS BY THE MET FAMILY - Novel amino acids derivatives, in particular some amino acid amides derivatives, their process of preparation and their use for inhibiting Met-triggered disorders, in particular cancer. | 04-04-2013 |
20130096113 | HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF - Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFRβ kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions. | 04-18-2013 |
20130096114 | PHARMACOKINETICALLY IMPROVED COMPOUNDS - A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided: | 04-18-2013 |
20130116249 | INDOLIZINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to compounds corresponding to formula (I): | 05-09-2013 |
20130116250 | IMIDAZOPYRIDINE DERIVATIVES, PROCESS FOR PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to compounds corresponding to formula (I): | 05-09-2013 |
20130123254 | PHARMACEUTICALLY ACCEPTABLE MGLUR5 POSITIVE ALLOSTERIC MODULATORS AND THEIR METHODS OF IDENTIFICATION - The present invention relates to mGluR5 positive allosteric modulators (PAM) and methods for identifying pharmaceutically acceptable compounds with high tolerability and safety, which method comprises the use of at least one non-competitive mGluR5 allosteric modulator which has a shift factor measured at 10 uM glutamate concentration below 3.0, | 05-16-2013 |
20130131057 | NEW BICYCLIC COMPOUNDS AS PI3-K AND MTOR INHIBITORS - There is provided compounds of formula (I), wherein A | 05-23-2013 |
20130150360 | INHIBITORS OF BRUTON'S TYROSINE KINASE - This application discloses compounds according to generic Formula I: | 06-13-2013 |
20130150361 | KINASE INHIBITORS - Compounds of formula (I): | 06-13-2013 |
20130150362 | NOVEL PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS - The present invention relates to certain pyrazolo[1,5-a]pyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrimidine compounds. | 06-13-2013 |
20130158025 | NOVEL COMPOUND ACTING AS A CANNABINOID RECEPTOR-1 INHIBITOR - Disclosed is a novel compound acting as a cannabinoid receptor 1 inhibitor, a prodrug thereof, an isomer thereof, a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof. The novel compound or the like is useful for preventing or treating diseases mediated by the cannabinoid receptor-1. | 06-20-2013 |
20130165437 | NOVEL DIHYDROPYRIMIDINOISOQUINOLINONES AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS. - A compound according to Formula Ia: | 06-27-2013 |
20130172338 | OXYGEN LINKED PYRIMIDINE DERIVATIVES - The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases. | 07-04-2013 |
20130184273 | BICYCLIC PYRIMIDINES - Compounds of formula (I), which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals. | 07-18-2013 |
20130190308 | PYRIDO[3,4-B]INDOLES AND METHODS OF USE - This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 07-25-2013 |
20130196984 | 3-AMINO-5-PHENYL-56-DIHYDRO-2H-[1,4]OXAZINES - The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I | 08-01-2013 |
20130196985 | HETEROCYCLIC ALKYNYL BENZENE COMPOUNDS AND MEDICAL COMPOSITIONS AND USES THEREOF - The heterocyclic alkynyl benzene compounds of formula (I), their pharmaceutically acceptable salts and stereoisomers thereof, as well as application in preparing drugs for preventing or treating tumors. The compounds can overcome the clinically induced resistance against Gleevec. | 08-01-2013 |
20130196986 | TRIAZOLOPYRAZINONES AS P2X7 RECEPTOR ANTAGONISTS - The invention provides certain 3,7-disubstituted-[1,2,4]triazolo[4,3-a]pyrazin-8(7H)-ones of the Formula (I), and their pharmaceutically acceptable salts, wherein R | 08-01-2013 |
20130203754 | 2-Aryl Imidazo[1,2-a]Pyridine-3-Acetamide Derivatives, Preparation Methods and Uses Thereof - Disclosed are 2-arylimidazo[1,2- | 08-08-2013 |
20130217682 | PYRAZOLOPYRIMIDINYL INHIBITORS OF UBIQUITIN-ACTIVATING ENZYME - Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: | 08-22-2013 |
20130217683 | INDAZOLES, BENZOTHIAZOLES, BENZOISOTHIAZOLES, BENZISOXAZOLES, AND PREPARATION AND USE THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof. | 08-22-2013 |
20130225572 | Substituted Imidazo[1,5-A]Quinoxalines As a PDE9 Inhibitor - The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I) | 08-29-2013 |
20130231337 | Bicyclic Heteroaryl Compounds - This invention relates to compounds of the general formula: | 09-05-2013 |
20130252951 | 7-HYDROXY-PYRAZOLO[1,5-A] PYRIMIDINE COMPOUNDS AND THEIR USE AS CCR2 RECEPTOR ANTAGONISTS - The compounds of formula (I) are antagonists of the CCR2 receptor Wherein R | 09-26-2013 |
20130252952 | 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS - The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) | 09-26-2013 |
20130261114 | COMPOUNDS USEFUL AS INHIBITORS OF CHOLINE KINASE - The present invention relates to compounds useful as inhibitors of choline kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 10-03-2013 |
20130261115 | IMIDAZO-, PYRAZOLOPYRAZINES AND IMIDAZOTRIAZINES AND THEIR USE - The invention relates to substituted imidazo-, pyrazolopyrazines and imidazotriazines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of hematological disorders, preferably of leukopenias and neutropenias. | 10-03-2013 |
20130267511 | Macrocyclic Indoles as Hepatitis C Virus Inhibitors - The present invention relates to inhibitors of HCV replication of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, | 10-10-2013 |
20130289031 | PYRIMIDINONE DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF - The invention relates to novel products of formula (Ia) or (Ib): | 10-31-2013 |
20130303532 | IMIDAZOPYRAZINES FOR USE AS MPS-1 AND TKK INHIBITORS IN THE TREATMENT HYPERPROLIFERATIVE DISORDERS - The present invention relates to substituted imidazopyrazine compounds of general formula (I): in which R | 11-14-2013 |
20130324525 | SUBSTITUTED HETEROCYCLIC COMPOUNDS - The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): | 12-05-2013 |
20130324526 | [1,2,4] TRIAZOLO [4,3-B] PYRIDAZINE COMPOUNDS AS INHIBITORS OF THE C-MET TYROSINE KINASE - The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I). | 12-05-2013 |
20130324527 | IMIDAZOPYRIDINES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS - A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof: | 12-05-2013 |
20130331389 | Methods and Compositions for Cardiomyocyte Replenishment by Endogenous and Progenitor Stem Cells - Disclosed herein are methods and compositions for replenishing injured and/or damaged cardiomyocytes in a subject by inducing, increasing, and/or enhancing the differentiation of endogenous stem and progenitor cells in the subject. | 12-12-2013 |
20140005189 | NOVEL 6-TRIAZOLOPYRIDAZINE SULFANYL BENZOTHIAZOLE DERIVATIVES AS MET INHIBITORS | 01-02-2014 |
20140011805 | INHIBITORS OF THE BMP SIGNALING PATHWAY - The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. | 01-09-2014 |
20140031351 | Macrocyclic Compounds as ALK, FAK and JAK2 Inhibitors - The present invention provides compounds of Formula I | 01-30-2014 |
20140038953 | COMPOSITIONS AND METHODS FOR CARDIOVASCULAR DISEASE - The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to reduce circulating levels of ApoB-100 or LDL. These compounds may also be used to treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia. | 02-06-2014 |
20140038954 | Spiro-Amino-Imidazo-Fused Heterocyclic Compounds as Beta-secretase Modulators and Methods of Use - The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I, wherein variables A | 02-06-2014 |
20140038955 | HETEROARYL AMIDE ANALOGUES AS P2X7 ANTAGONISTS - Heteroaryl amide analogues are provided, of the Formula: | 02-06-2014 |
20140045835 | TRIAZOLOPYRIDINE COMPOUNDS AS PIM KINASE INHIBITORS - Provided herein are methods of treating diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases by administering to a mammal in need thereof a therapeutically effective amount of a compound of Formula I: | 02-13-2014 |
20140045836 | [1,2,4]TRIAZOLO[1,5-C]PYRIMIDINE DERIVATIVES AS HSP90 MODULATORS - The present invention relates to [1,2,4]triazolo[1,5-c]pyrimidine derivatives which inhibit the activity of Heat Shock Protein Hsp90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, methods of treating diseases and the pharmaceutical compositions comprising these compounds. | 02-13-2014 |
20140051696 | THERAPIES FOR TREATING CANCER - Provided herein are methods that relate to a novel therapeutic strategy for treatment of cancer, including hematological malignancies such as leukemia, lymphoma, and multiple myeloma. In particular, the method includes administration of a PI3Kδ inhibitor and a Syk inhibitor. | 02-20-2014 |
20140051697 | COMPOUNDS FOR TREATING RESPIRATORY SYNCYTIAL VIRUS INFECTIONS - The present invention relates to compounds of formula (I) | 02-20-2014 |
20140073638 | ETHYNYL COMPOUNDS USEFUL FOR TREATMENT OF CNS DISORDER - The present invention relates to ethynyl compounds of formula | 03-13-2014 |
20140088096 | PYRAZOLOPYRIMIDINYL INHIBITORS OF UBIQUITIN-ACTIVATING ENZYME - Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: | 03-27-2014 |
20140088097 | HETEROCYCLIC COMPOUNDS, MEDICAMENTS CONTAINING SAID COMPOUNDS, USE THEREOF AND PROCESSES FOR THE PREPARATION THEREOF - The present invention relates to compounds of general formula (I) | 03-27-2014 |
20140088098 | IMIDAZO[1,2-a]PYRIDINE SULFONAMIDES AS TRPM8 MODULATORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: | 03-27-2014 |
20140113896 | ARYLAMINOALCOHOL-SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINOLINES - The present invention relates to substituted phenoxypyridine compounds of general formula (I); in which R | 04-24-2014 |
20140121203 | IMIDAZO[1,2-a]PYRIDINE DERIVATIVES: PREPARATION AND PHARMACEUTICAL APPLICATIONS - The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to imidazo[1,2-a]pyridine containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase activities (HDAC). | 05-01-2014 |
20140121204 | NOVEL DIHYDROPYRIMIDINOISOQUINOLINONES AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS. - A compound according to Formula Ia: | 05-01-2014 |
20140128385 | BACE-2 INHIBITORS FOR THE TREATMENT OF METABOLIC DISORDERS - The present invention relates to the use of BACE-2 inhibitors and pharmaceutical compositions comprising BACE-2 inhibitors for treating metabolic disorders related to decreased β cell mass and/or function. | 05-08-2014 |
20140128386 | Hydroxy-substituted imidazo[1,2-a]pyridinecarboxamides and their use - The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders. | 05-08-2014 |
20140135323 | OXO-SUBSTITUTED IMIDAZO[1,2B]PYRIDAZINES, THEIR PREPARATION AND USE AS PHARMACEUTICALS - The invention relates to novel inhibitors of kinases of the general formula (I): | 05-15-2014 |
20140187548 | 6 SUBSTITUTED IMIDAZOPYRAZINES FOR USE AS MPS-1 AND TKK INHIBITORS IN THE TREATMENT OF HYPERPROLIFERATIVE DISORDERS - The present invention relates to substituted imidazopyrazine compounds of general formula (I) in which R | 07-03-2014 |
20140194418 | BICYCLIC CARBOXAMIDE INHIBITORS OF KINASES - Compounds of formula (I) or pharmaceutical acceptable salts are provided, wherein X | 07-10-2014 |
20140206682 | COMPOUNDS AND COMPOSITIONS AS PDGFR KINASE INHIBITORS - The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of PDGFR (PDGFRα, PDGFRβ) kinases or c-kit and PDGFR (PDGFRα, PDGFRβ) kinases. | 07-24-2014 |
20140206683 | MACROCYCLIC LRRK2 KINASE INHIBITORS - The present invention relates to novel macrocylic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of LRRK2 (Leucine-Rich Repeat Kinase 2). Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine or diagnostic agent, in particular for the treatment and/or diagnosis of diseases characterized by LRRK2 kinase activity such as neurological disorders including Parkinson's disease and Alzheimer's disease. | 07-24-2014 |
20140235631 | EFFLUX INHIBITOR COMPOSITIONS AND METHODS OF TREATMENT USING THE SAME - The present invention relates to efflux inhibitor compositions and methods of using these agents for treating conditions where the activity of efflux transporter proteins (e.g., Breast Cancer Resistance Protein (BCRP) and P-Glycoprotein (P-GP)) inhibit effective delivery of a therapeutic agent to a target tissue (e.g., brain, spinal cord, nerves, cerebrospinal fluid, testis, eyeballs, retina, inner ear, placenta, mammary gland, liver, biliary tract, kidney, intestines, lung, adrenal cortex, endometrium, hematopoietic cells, and/or stem cells). | 08-21-2014 |
20140243328 | IMIDAZOPYRIDINE DERIVATIVES, PROCESS FOR PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to compounds corresponding to formula (I): | 08-28-2014 |
20140249145 | SUBSTITUTED PYRAZOLOPYRIMIDINES AS GLUCOCEREBROSIDASE ACTIVATORS - Substituted pyrazolopyrimidines and dihydropyrazolopyrimidines and related compounds, their methods of manufacture, compositions containing these compounds, and methods of use of these compounds in treating lysosomal storage disorders such as Gaucher disease are described herein. The compounds are of general Formula (I) | 09-04-2014 |
20140249146 | 4-ALKYL SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS - The present invention relates to 4-alkyl substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them. | 09-04-2014 |
20140249147 | Substituted Bicyclic Aza-Heterocycles and Analogues as Sirtuin Modulators - Provided herein are novel substituted bicyclic aza-heterocycle 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. | 09-04-2014 |
20140256718 | HYDROXYMETHYLARYL-SUBSTITUTED PYRROLOTRIAZINES AS ALK1 INHIBITORS - This invention relates to novel 5-[(hydroxymethyl)aryl]-substituted pyrrolo[2,1-f][1,2,4]triazin-4-amines of formula (I), to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating angiogenesis-related disorders, in particular angiogenesis-related ocular disorders. | 09-11-2014 |
20140256719 | PYRROLOTRIAZINES AS POTASSIUM ION CHANNEL INHIBITORS - A compound of formula (I) | 09-11-2014 |
20140256720 | CANCER TREATMENT USING BMP INHIBITOR - Methods for regulating cancer cell growth and survival, inhibiting cancer cell growth, promoting cancer cell death, and/or treating a cancer make use of antagonists of a type I BMP receptor. In some embodiments the cancer is a lung cancer and the cancer cell is a lung cancer cell. | 09-11-2014 |
20140275065 | SUBSTITUTED 7-AZABICYLES AND THEIR USE AS OREXIN RECEPTOR MODULATORS - The present invention is directed to compounds of Formula I: | 09-18-2014 |
20140275066 | Transient Protection of Normal Cells During Chemotherapy - This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders. | 09-18-2014 |
20140275067 | Transient Protection of Normal Cells During Chemotherapy - This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders. | 09-18-2014 |
20140288069 | AMINO-SUBSTITUTED IMIDAZOPYRIDAZINES AS MKNK1 KINASE INHIBITORS - The present invention relates to amino imidazopyridazine compounds of general formula (I): in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said 10 compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients. | 09-25-2014 |
20140296231 | AMINO-SUBSTITUTED IMIDAZOPYRIDAZINES - The present invention relates to amino-substituted imidazopyridazine compounds of general formula (I): in which A, R1, R3 and n are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients. | 10-02-2014 |
20140303158 | FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS - The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: | 10-09-2014 |
20140303159 | MACROCYCLIC FLT3 KINASE INHIBITORS - The present invention relates to macrocylic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of FLT3 (FMS-Related Tyrosine kinase 3). Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine, in particular for the treatment of cell proliferative disorders, such as cancer. | 10-09-2014 |
20140336189 | 3,4-DIHYDROPYRROLO[1,2-A]PYRAZINE-2,8(1H)-DICARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - Compounds corresponding to the general formula (I) | 11-13-2014 |
20140343053 | TRIAZOLOPYRIDINONE PDE10 INHIBITORS - The present invention is directed to triazolopyridinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. | 11-20-2014 |
20140343054 | Therapeutic Use of Imidazopyridine Derivatives - The invention relates to the use of compounds corresponding to formula (I) in which R | 11-20-2014 |
20140343055 | KINASE INHIBITORS - Compounds of formula (I): | 11-20-2014 |
20140350008 | 2-HETEROARYL CARBOXAMIDES - The invention relates to novel 2-heteroaryl carboxamides and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory. | 11-27-2014 |
20140371216 | PURINONE DERIVATIVES AS HM74A AGONISTS - The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease. | 12-18-2014 |
20140371217 | SUBSTITUTED PYRAZOLO[1,5-A] PYRIDINE AS TROPOMYOSIN RECEPTOR KINASE (TRK) INHIBITORS - The present application relates to a series of substituted pyrazolo[1,5-a]pyridine compounds, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compounds. | 12-18-2014 |
20140371218 | NOVEL NK-3 RECEPTOR SELECTIVE ANTAGONIST COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN NK-3 RECEPTORS MEDIATED DISORDERS - The present invention is directed to novel compounds of formula I | 12-18-2014 |
20140378447 | NOVEL PYRAZOLE DERIVATIVE - It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates. | 12-25-2014 |
20140378448 | NOVEL PYRAZOLE DERIVATIVE - It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates. | 12-25-2014 |
20140378449 | TRIAZOLOPYRIDINE JAK INHIBITOR COMPOUNDS AND METHODS - A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R | 12-25-2014 |
20150011544 | COMPOUNDS OF ESTROGEN-RELATED RECEPTOR MODULATORS AND THE USES THEREOF - The compounds according to formula (VIII), their pharmaceutically acceptable acid or base addition salts, and the uses thereof. These compounds and their pharmaceutically acceptable acid or base addition salts can be used for preparing medicaments for modulating estrogen related receptors (ERR), and treating metabolic diseases, such as high blood fat, fatty liver, hyperglycemia, diabetes, obesity. The substituents of the formula are defined in the description. | 01-08-2015 |
20150018348 | Lactam Kinase Inhibitors - Compounds useful as kinase inhibitors are provided herein, as well as salts, pharmaceutical compositions, methods of medical treatment and methods of synthesis thereof. | 01-15-2015 |
20150038503 | DERIVATIVES OF 6-SUBSTITUTED TRIAZOLOPYRIDAZINES AS REV-ERB AGONISTS - The present invention provides novel 6-substituted [1,2,4]triazolo[4,3-b]pyridazines that are agonists of Rev-Erb. These compounds, and pharmaceutical compositions comprising the same, are suitable means for treating any disease wherein the activation of Rev-Erb has therapeutic effects, for instance in inflammatory and circadian rhythm-related disorders or cardiometabolic diseases. | 02-05-2015 |
20150038504 | FORMULATION OF SYK INHIBITORS - Disclosed are pharmaceutical compositions comprising a compound having the formula: | 02-05-2015 |
20150038505 | POLYMORPH OF SYK INHIBITORS - Polymorphs of a bis-mesylate salt of a compound of Formula I: | 02-05-2015 |
20150038506 | BICYCLIC HETEROARYL DERIVATIVES AS MNK1 AND MNK2 MODULATORS AND USES THEREOF - The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), neurodegenerative diseases (e.g., Alzheimer's disease), metabolic diseases (e.g. diabetes), neurodevelopmental disorders (e.g. autism), or psychiatric disorders (e.g. schizophrenia or anxiety)) as well as methods of treating these diseases. | 02-05-2015 |
20150051206 | COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS - The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFRα, PDGFRβ) kinases. | 02-19-2015 |
20150057273 | KINASE INHIBITORS - Disclosed are compounds having [1,2,4]triazolo[4,3-a]pyridine groups and pharmaceutically acceptable salts thereof. The compounds are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract. | 02-26-2015 |
20150057274 | TRIAZOLOTHIENOPYRIMIDINE COMPOUND INHIBITORS OF UREA TRANSPORTERS AND METHODS OF USING INHIBITORS - Provided herein are small molecule triazolothienopyrimidine compounds that inhibit urea transport activity of solute transporters, particularly the UT-B transporter. The compounds described herein are useful for increasing solute clearance in states of fluid overload and for treating refractory edema associated with cardiovascular, renal, and metabolic diseases, disorders, and conditions. | 02-26-2015 |
20150105381 | SUBSTITUTED PYRAZOLOQUINAZOLINONES AND PYRROLOQUINAZOLINONES AS ALLOSTERIC MODULATORS OF GROUP II METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to the pyrazoloquinazolinone and pyrroloquinazolinone derivatives of the general formula (I), as well as pharmaceutical compositions containing them, and their use in the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals, in particular their use in the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders. | 04-16-2015 |
20150111887 | COMPOSITIONS USEFUL FOR TREATING DISORDERS RELATED TO KIT - Compounds and compositions useful for treating disorders related to mutant KIT are described herein. | 04-23-2015 |
20150119390 | IMIDAZOTHIADIAZOLE AND IMIDAZOPYRIDAZINE DERIVATIVES AS PROTEASE ACTIVATED RECEPTOR 4 (PAR4) INHIBITORS FOR TREATING PLATELET AGGREGATION - The present invention provides imidazothiadiazole compounds of Formula (I); Wherein W, Y, R | 04-30-2015 |
20150119391 | ANTI-TUMORAL COMPOSITION COMPRISING THE COMPOUND 1-(6--1,3-BENZOTHIAZOL-2-YL)-3-(2-MORPHOLIN-4-YLETHYL)UREA - The present invention concerns an anti-tumoral composition comprising the compound 1-(6-{[6-(4-fluorophenyl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]sulfanyl}1,3-benzothiazol-2-yl)-3-(2-morpholin-4-ylethyl)urea and its use in the treatment of cancer. | 04-30-2015 |
20150126506 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. | 05-07-2015 |
20150133446 | IMIDAZOTHIADIAZOLE DERIVATIVES AS PROTEASE ACTIVATED RECEPTOR 4 (PAR4) INHIBITORS FOR TREATING PLATELET AGGREGATION - The present invention provides imidazothiadiazole compounds of Formula (I) wherein A, B, D, R | 05-14-2015 |
20150133447 | Triazolopyrazine - The present invention encompasses compounds of general formula (I) | 05-14-2015 |
20150133448 | NOVEL PYRAZOLE DERIVATIVE - It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates. | 05-14-2015 |
20150141419 | DIARYL[A, G]QUINOLIZIDINE COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION, AND USES THEREOF - The present invention relates to a diarylo[a,g]quinolizidine compound of formula (I), enantiomer, diastereoisomer, racemate, mixture, pharmaceutically acceptable salt, crystalline hydrate or solvate thereof; the preparation method thereof, and uses thereof in preparing an experimental model drugs related to dopamine receptors and 5-HT receptors or a medicament for treating or preventing a disease related to dopamine receptors and 5-HT receptors. | 05-21-2015 |
20150141420 | USE OF SUBSTITUTED 2, 3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINES FOR THE TREATMENT OF MYELOMA - The present invention relates to the use of 2,3-dihydroimidazo[1,2-c]quinazoline compounds, and of pharmaceutical compositions containing such compounds, for the treatment or prophylaxis of multiple myeloma, as a sole agent or in combination with other one or more other active ingredients. | 05-21-2015 |
20150297607 | Tricyclic Lactams for Use in the Protection of Normal Cells During Chemotherapy - This invention is in the area of tricyclic lactam compounds, compositions and methods of protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, protection of healthy cells is disclosed using compounds that act as cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders. | 10-22-2015 |
20150307503 | SMALL MOLECULE BICYCLIC AND TRICYCLIC CFTR CORRECTORS - Novel CFTR corrector compounds that are effective in rescuing halide efflux, delF508-CFTR protein processing, and apical functional chloride ion transport in a cell are provided. Also provided are methods for treating protein folding disorders (e.g., cystic fibrosis). The methods include administering a CFTR corrector compound or pharmaceutically acceptable salt or prodrug thereof. Methods of rescuing halide efflux in a cell, correcting a processing defect of a delF508-CFTR protein in a cell, and correcting functional delF508-CFTR chloride channels in a cell are also provided. | 10-29-2015 |
20150322019 | PYRIMIDINE COMPOUNDS FOR THE TREATMENT OF CANCER - Compounds of Formula I or II: | 11-12-2015 |
20150322075 | COMPOUNDS - The present invention relates to novel 3,4-dihydro-1H-pyrimido[1,6-a]pyrimidin-6(2H)-one compounds that inhibit Lp-PLA | 11-12-2015 |
20150328224 | SUBSTITUTED 7-AZABICYCLES AND THEIR USE AS OREXIN RECEPTOR MODULATORS - The present invention is directed to compounds of Formula I: | 11-19-2015 |
20150344480 | PYRAZOLE SUBSTITUTED IMIDAZOPYRAZINES AS CASEIN KINASE 1 D/E INHIBITORS - The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents. | 12-03-2015 |
20150352087 | PYRIDO[3,4-B]INDOLES AND METHODS OF USE - This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 12-10-2015 |
20150361078 | Imidazopyridine Compounds and Uses Thereof - This invention generally relates to substituted imidazopyridine compounds, particularly substituted 4-(imidazo[1,2-a]pyridin-2-yl)benzamide compounds and salts thereof. This invention also relates to pharmaceutical compositions and kits comprising such a compound, uses of such a compound (including, for example, treatment methods and medicament preparations), processes for making such a compound, and intermediates used in such processes. | 12-17-2015 |
20150366873 | COMBINATIONS COMPRISING PDE 2 INHIBITORS SUCH AS 1-ARYL-4-METHYL-[1,2,4]TRIAZOLO-[4,3-A]]QUINOXALINE COMPOUNDS AND PDE 10 INHIBITORS FOR USE IN THE TREATMENT OF NEUROLOGICAL OF METABOLIC DISORDERS - The present invention relates to combinations of phosphodiesterase 2 (PDE2) inhibitors with inhibitors of phosphodiesterase 10 (PDE10). In particular, the invention relates to combinations of 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives which have been found to inhibit phosphodiesterase 2 (PDE2), with inhibitors of phosphodiesterase 10 (PDE10). Particular PDE10 inhibitors are selected from the group of MP-10, PQ-10, TP-10, papaverine, and the compounds disclosed in WO 2011/051324 and in WO 2011/110545. The invention is also directed to pharmaceutical compositions comprising such combinations, to processes for preparing such compositions, to the use of PDE2 inhibitors, in particular of 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives for the potentiation of said PDE10 inhibitors, and to the use of said PDE10 inhibitors for the potentiation of the effect of said PDE2 inhibitors, in particular, 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives, and to the use of such combinations and compositions for the prevention and treatment of disorders in which PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases. | 12-24-2015 |
20160002265 | MACROCYCLIC COMPOUNDS AS IRAK4 INHIBITORS FOR THE TREATMENT OF INFLAMMATORY DISEASES - Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein i.a. Ring A is phenylene or 5- to 6-membered heteroarylene; Ring B is phenylene, 5- to 6-membered heterocycloalkylene or 5- to 6-membered heteroarylen; R | 01-07-2016 |
20160009718 | MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF | 01-14-2016 |
20160009721 | TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES AS LSD1 INHIBITORS | 01-14-2016 |
20160039807 | NOVEL DIHYDROPYRIMIDINOISOQUINOLINONES AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS (GPR84 ANTAGONISTS) - A compound according to Formula (Ia), | 02-11-2016 |
20160046633 | BMP INHIBITORS AND METHODS OF USE THEREOF - The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds may also be used to reduce circulating levels of ApoB-100 or LDL and treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia. | 02-18-2016 |
20160046640 | SUBSTITUTED 7-AZABICYCLES AND THEIR USE AS OREXIN RECEPTOR MODULATORS - The present invention is directed to compounds of Formula I: wherein ring A is phenyl, naphihalenyl, pyridyl, quinolinyl, isoquinolinyl, imidazopyridyl, furanyi, tlisazolyl, isoxazolvl, pyrazolyl, imidazothiazolyi, benzimidazolyl, or indazolyi; R | 02-18-2016 |
20160046642 | Compounds for Treating Respiratory Syncytial Virus Infections - The present invention relates to compounds of formula (I) | 02-18-2016 |
20160050930 | METHODS OF CONTROLLING NEONICOTINOID RESISTANT PESTS - The present invention relates to a method of controlling insects (in particular insects of the order Hemiptera, especially aphids and whitefly) that are resistant to neonicotinoid insecticides, to methods of controlling insects whereby undesired insects are affected but beneficial arthropods are not affected, using compounds of formula (I) (where A, R1 and R2 are as defined above), and, further, to novel compounds of formula (I) which are useful in the aforementioned methods and/or which possess enhanced insecticidal properties, and to compositions containing said compounds. | 02-25-2016 |
20160051557 | METHODS OF TREATING PROLIFERATIVE DISEASES - Provided herein are methods of administering N-(5-tert-butyl-isoxazol-3-yl)-N′-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea, or a pharmaceutically acceptable salt or solvate thereof, to human patients, including a specific patient population. Specifically, dosing, dosing schedules or dosing regimens are provided herein. Methods of treating proliferative diseases or FLT-3 mediated diseases in humans are also provided. | 02-25-2016 |
20160052909 | GDF-8 Inhibitors - Described are GCF-8 inhibitors of the formula (I), | 02-25-2016 |
20160058758 | SYK INHIBITORS - The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: | 03-03-2016 |
20160067245 | 1,2,4-Triazolo [4,3-A] Pyridine Derivatives and Their Use For The Treatment of Prevention of Neurological and Psychiatric Disorders - The present invention relates to methods of treating various central nervous system disorders using novel triazolo[4,3-a]pyridine derivatives of Formula (I) | 03-10-2016 |
20160068525 | Fused Heterocyclic Compounds as Selective BMP Inhibitors - The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. | 03-10-2016 |
20160095863 | COMBINATION TREATMENT OF ACUTE MYELOID LEUKEMIA and MYELODYSPLASTIC SYNDROME - The present invention relates to the use of Volasertib or a salt thereof or the hydrate thereof in combination with Quizartinib or a salt thereof or the hydrate thereof for treating patients suffering from acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS). | 04-07-2016 |
20160102097 | COMPOSITIONS USEFUL FOR TREATING DISORDERS RELATED TO KIT - Compounds and compositions useful for treating disorders related to mutant KIT are described herein. | 04-14-2016 |
20160108054 | Lactam Kinase Inhibitors - Compounds useful as kinase inhibitors are provided herein, as well as salts, pharmaceutical compositions, methods of medical treatment and methods of synthesis thereof. | 04-21-2016 |
20160115166 | PYRROLO[2, 1-F] [1,2,4]TRIAZINE DERIVATIVE AND USE THEREOF FOR TREATING TUMORS - Disclosed are a pyrrolo[2,1-f][1,2,4]triazine derivative of Formula (I) and use thereof for treating tumors. The compound has remarkable antiproliferative activity for a variety of human tumor cell lines, and is useful for treating cancers, especially solid tumors such gastric cancer, lung cancer, liver cancer, breast cancer, colon cancer, prostatic cancer, and oral cancer. | 04-28-2016 |
20160120863 | SLC2A TRANSPORTER INHIBITORS - Provided is a SLC2A class I transporter inhibitor compound for use in medicine, which compound comprises the following formula: | 05-05-2016 |
20160122344 | Novel 6,7-dihydrobenzo[a]quinolizin-2-one derivatives for the treatment and prophylaxis of hepatitis B virus infection - The invention provides novel compounds having the general formula: | 05-05-2016 |
20160129001 | SUBSTITUTED [1,2,4]TRIAZOLO[4,3-a]PYRAZINES AS BRD4 INHIBITORS - Method for treating AML and MM by administration of a compound of the formula (I) | 05-12-2016 |
20160137640 | FIVE-MEMBER-HETEROCYCLE FUSED PYRIDINE COMPOUNDS, METHOD OF PRODUCING THE SAME, AND USE THEREOF - This invention provides a class of five-member-heterocycle fused pyridine compounds as shown below in Formula (X), pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, a method of producing the same, pharmaceutical compositions containing the compound, and use of the compounds in preparing medicament for preventing and/or treating diseases and tumours associated with abnormal protein tyrosine kinase. | 05-19-2016 |
20160151367 | METHODS OF USING PHTHALAZINONE KETONE DERIVATIVES | 06-02-2016 |
20160166579 | COMBINATION METHODS FOR TREATING CANCERS | 06-16-2016 |
20160166580 | FORMULATION OF SYK INHIBITORS | 06-16-2016 |
20160168152 | N-ALKYL TRYPTANTHRIN DERIVATIVE, PREPARATION METHOD FOR SAME, AND APPLICATION THEREOF | 06-16-2016 |
20160168155 | POLYMORPH OF SYK INHIBITORS | 06-16-2016 |
20160176880 | SUBSTITUTED IMIDAZO[1,2-A]PYRAZINECARBOXAMIDES AND USE THEREOF | 06-23-2016 |
20160185774 | Anti-Infective Compounds - The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis. | 06-30-2016 |
20180022750 | 6-HYDROXYBENZOFURANYL- AND 6-ALKOXYBENZOFURANYL-SUBSTITUTED IMIDAZOPYRIDAZINES | 01-25-2018 |
20190142826 | IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO | 05-16-2019 |
20190144454 | COMPOSITIONS USEFUL FOR TREATING DISORDERS RELATED TO KIT | 05-16-2019 |
20220133679 | EFFLUX INHIBITOR COMPOSITIONS AND METHODS OF TREATMENT USING THE SAME - The present invention relates to efflux inhibitor compositions and methods of using these agents for treating conditions where the activity of efflux transporter proteins (e.g., Breast Cancer Resistance Protein (BCRP) and P-Glycoprotein (P-GP)) inhibit effective delivery of a therapeutic agent to a target tissue (e.g., brain, spinal cord, nerves, cerebrospinal fluid, testis, eyeballs, retina, inner ear, placenta, mammary gland, liver, biliary tract, kidney, intestines, lung, adrenal cortex, endometrium, hematopoietic cells, and/or stem cells). | 05-05-2022 |
20220135561 | IMIDAZOPYRIDINE DERIVATIVES - The present disclosure provides a compound of Formula (I): | 05-05-2022 |