Entries |
Document | Title | Date |
20080200472 | Therapeutic agents useful for treating pain - A compound of formula: | 08-21-2008 |
20080207629 | LIQUID PREPARATION COMPRISING PIMOBENDAN - The invention relates to novel liquid preparation comprising a substituted benzimidazol, preferably pimobendan as pharmaceutically active compound. In particular, the present invention relates to liquid preparation comprising an etherified cyclodextrin derivative, preferably in a concentration of about 20 to 70% (w/v) and said substituted benzimidazol, preferably in a concentration of about 0.005 to 0.15% (w/w). | 08-28-2008 |
20080214553 | 2-(4-Oxo-4H-Quinazolin-3-Yl) Acetamides and Their Use as Vasopressin V3 Antagonists - The present invention relates to 2-(4-oxo4H-quinazolin-3-yl)acetamicle derivatives of formula (I), and to their use as vasopressin V3 antagonists, particularly for the treatment of depression. | 09-04-2008 |
20080255133 | Inhibitors of MEK - This invention concerns to N-(2-aylamino)aryl sulfonamides, which are inhibitors of MEK, methods of using such compounds in the treatment of hyperproliferative diseases, and to pharmaceutical compositions containing such compounds. | 10-16-2008 |
20080269232 | Pyridazinyl Amine Derivatives, the Use Thereof in the Preparation of Picorna Virus Inhibitors - The present invention relates to substituted pyridazinylamine derivatives of the formula I or pharmaceutically acceptable salts or hydrates thereof, wherein the substituents are defined as in the description, their preparation process, pharmaceutical compositions comprising them, and uses of the said compounds as picorna virus inhibitors for prevention and/or treatment of diseases caused by picorna viruses. | 10-30-2008 |
20080280916 | PYRIDAZINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS - Methods of treating an SCD-mediated skin disorder or condition in a mammal, preferably a human include administering to a mammal in need thereof a compound of formula (I): | 11-13-2008 |
20080287452 | HETEROARYL/ARYL PYRIMIDINE ANALOGS AND THEIR USE AS AGONISTS OF THE WNT-BETA-CATENIN CELLULAR MESSAGING SYSTEM - The present invention relates to heteroaryl/aryl pyrimidine analogs, methods of making aryl/heteroaryl pyrimidine analogs, compositions comprising a aryl/heteroaryl pyrimidine analog, and methods for treating canonical Wnt-β-catenin cellular messaging system-related disorders comprising administering to a subject in need thereof an effective amount of a heteroaryl/aryl pyrimidine analog. | 11-20-2008 |
20090048263 | Brain/neuronal cell-protecting agent and therapeutic agent for sleep disorder - A compound represented by the formula (I) or a salt thereof; and an agent for protecting a brain/neuronal cell or a therapeutic agent for sleep disorder comprising the compound or salt: wherein Z represents an oxygen or sulfur; R | 02-19-2009 |
20090062293 | 1,4-Substituted Piperazine Derivatives - A compound represented by the formula (I): | 03-05-2009 |
20090062294 | HETEROARYL-SUBSTITUTED UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE - Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis). | 03-05-2009 |
20090069334 | Pyridazine based alpha-helix mimetics - The synthesis of new α-helix scaffolds mimicking i, i+3 or i+4, i+7 residues, was accomplished. The common pyridazine heterocycle originates from the easily available building block, 6. These scaffolds may be thought of as synthetic counterparts of amphiphilic α-helices having a “wet face” along one side and a hydrophobic face along the other side of the helix. | 03-12-2009 |
20090118296 | Heteroaromatic Compounds As Inhibitors Of Stearoyl-Coenzyme A Delta-9 Desaturase - Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; lipid disorders; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and fatty liver disease. | 05-07-2009 |
20090131447 | COMBINATION THERAPY - This invention is directed to the use of SCD-1 inhibitors of the formula (I): where x, y, V, W, G, J, L, M, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein, in combination with other drug therapies to treat adverse weight gain. | 05-21-2009 |
20090131448 | 2-(Piperidin-4-yl)-4,5-dihydro-2h-pyridazin-3-one derivatives as pde4 inhibitors - The compounds of a certain formula (1), | 05-21-2009 |
20090137600 | Antiplatelet agent and process for producing the same - A compound having an action of suppressing platelet aggregation is provided. This compound also exhibits excellent physical properties and oral absorbability. This compound is represented by formula (Ib): Its production method is also provided. | 05-28-2009 |
20090163508 | AMIDE COMPOUND - An object of the present invention is to provide a novel fused-ring compound which has a FAAH inhibitory effect and is useful as an analgesic. | 06-25-2009 |
20090170861 | Pyridazinone Derivatives Useful as Glucan Synthase Inhibitors - In its many embodiments, the present invention provides -substituted pyridazinone compounds as glucan synthase inhibitors, methods of preparing such compounds, pharmaceutical including one or more of such compounds, methods of preparing pharmaceutical formulations including one or more such compounds or one or more such compounds along with other antifungal agents, and methods of treatment, prevention, inhibition, or amelioration of one or more fungal infections associated with glucan synthase using such compounds or pharmaceutical compositions. | 07-02-2009 |
20090170862 | USE OF C-KIT INHIBITORS FOR THE TREATMENT OF MYELOMA - The present invention relates to the use of a c-kit inhibitor, especially a c-kit inhibitor of formula I, | 07-02-2009 |
20090176793 | 3-(l,3-BENZODIOXOL-5-YL)-6-(4-CYCLOPROPYLPIPERAZIN-l-YL)-PYRIDAZINE, ITS SALTS AND SOLVATES AND ITS USE AS HISTAMINE H3 RECEPTOR ANTAGONIST - 3-(1,3-Benzodioxol-5-yl)-6-(4-cyclopropylpiperazin-1-yl)pyridazine and salts and solvates thereof, (I) having histamine H3 antagonistic activity can be used in pharmaceutical compositions. | 07-09-2009 |
20090197890 | PYRIDAZINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS - A method of treating an SCD-mediated disease or condition in a mammal, preferably a human, includes administering to a mammal a compound of formula (I): | 08-06-2009 |
20090203705 | Spiro Compounds As NPY Y5 Receptor Antagonists - The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt thereof, | 08-13-2009 |
20090215789 | CYCLIC HEXADEPSIPEPTIDES, PROCESSES FOR THEIR PRODUCTION AND THEIR USE AS PHARMACEUTICALS - The present invention provides cyclic hexadepsipeptides and their pharmaceutically acceptable salts, solvates and prodrugs, and methods for obtaining the compounds, by fermentation, optionally followed by post-biosynthesis chemical modification. The present invention further provides uses of cyclic hexadepsipeptides, and their pharmaceutically acceptable salts, solvates and prodrugs as pharmaceuticals, in particular to their use as antibacterial, antifungal or antineoplastic agents, and to pharmaceutical compositions comprising a cyclic hexadepsipeptide, or a pharmaceutically acceptable salt, solvate or prodrug thereof, together with a carrier. | 08-27-2009 |
20090239876 | Substituted 4-Hydroxypyrimidine-5-Carboxamides - The present invention relates to substituted 4-hydroxypyrimidine-5-carboxamides useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions. | 09-24-2009 |
20090253708 | 2-ALKYNYL-6-PYRIDIN-2-YL-PYRIDAZINONES, 2-ALKYNYL-6-PYRIDIN-2-YL-DIHYDROPYRIDAZINONES, 2-ALKYNYL-6-PYRIMIDIN-2-YL-PYRIDAZINONES AND 2-ALKYNYL-6-PYRIMIDIN-2-YL-DIHYDROPYRIDAZINONES AND THEIR USE AS FUNGICIDES - This invention relates to certain novel 2-alkynyl-6-pyridin-2-yl-pyridazinones, 2-alkynyl-6-pyridin-2-yl-dihydropyridazinones, 2-alkynyl-6-pyrimidin-2-yl-pyridazinones and 2-alkynyl-6-pyrimidin-2-yl-dihydropyridazinones and to the use of these compounds for control of fungal pathogens of plants and mammals. | 10-08-2009 |
20090275589 | Pyridazine Compound and Use Thereof - A pyridazine compound of the formula: | 11-05-2009 |
20090306090 | HETEROCYCLIC DERIVATIVES AND THEIR USE AS STEAROYL-COA DESATURASE INHIBITORS - Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): | 12-10-2009 |
20090325973 | FORMULATIONS CONTAINING PYRIDAZINE COMPOUNDS - The invention relates to chemical compounds, compositions and methods of making and using the same. In particular, the invention provides selected pyridazine compounds of the formula I | 12-31-2009 |
20100004254 | THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN - A compound of formula: | 01-07-2010 |
20100022549 | ALPHA-HELIX MIMETIC WITH FUNCTIONALIZED PYRIDAZINE - The synthesis of new α-helix scaffolds mimicking i, i+3 or i+4, i+7 residues, was accomplished. The common pyridazine heterocycle originates from the easily available dimethyl pyridazine-3,6-dicarboxylate building block. These scaffolds may be thought of as synthetic counterparts of amphiphilic α-helices having a hydrophilic face along one side and a hydrophobic face along the other side of the helix. | 01-28-2010 |
20100069394 | FAST-DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS - The present invention relates to 4-aryl-6-piperazin-1-yl-3-substituted-pyridazines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects. | 03-18-2010 |
20100105693 | Modulators of Muscarinic Receptors - The present invention relates to substituted piperazine compounds that are useful modulators of muscarinic receptors. The present invention also provides compositions comprising such compounds, and methods for treating muscarinic receptor mediated diseases. | 04-29-2010 |
20100113464 | NOVEL PYRIDAZINE DERIVATIVES - The present invention relates to novel pyridazine derivatives of formula I as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R | 05-06-2010 |
20100120783 | MELANOCORTIN RECEPTOR AGONISTS - The present invention relates to a compound having a good agonistic activity to melanocortin receptor, or pharmaceutically acceptable salt or isomer thereof, and an agonistic composition for melanocortin receptor comprising the same as an active ingredient. | 05-13-2010 |
20100137329 | DERIVATIVES OF 1-PIPERAZINE- AND 1-HOMOPIPERAZINE-CARBOXYLATES, PREPARATION METHOD THEREOF AND USE OF SAME AS INHIBITORS OF THE FAAH ENZYME - The invention relates to a compound having general formula (I): | 06-03-2010 |
20100144747 | 1H-QUINAZ0LINE-2,4-DIONES - The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) | 06-10-2010 |
20100168120 | SALTS OF PYRIDAZINE COMPOUNDS - The invention relates to stable and substantially purified synthetic pharmaceutically acceptable acid addition salts of pyridazine compounds of the formula I wherein R10 is hydrogen, hydroxyl, alkyl, alkoxy, alkenyl, alkynyl, alkylene, aryl, heteroaryl, sulfonyl, sulfinyl, sulfenyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, =0, ═S, carboxyl, carbonyl, carbamoyl, carboxamide, or phosphonate, and R11 is alkyl, alkoxy, alkenyl, alkynyl, alkylene, alkenylene, alkenyloxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, sulfonyl, sulfinyl, sulfenyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, =0, ═S, phosphonate, carboxyl, carbonyl, carbamoyl, carboxamide, or ureido. The invention also relates to formulations, dosage forms and compositions comprising the salts, and methods of using the salts, formulations, dosage forms and compositions. | 07-01-2010 |
20100210659 | PYRROLIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS - The present invention relates to a compounds of formula I | 08-19-2010 |
20100234389 | AMIDE COMPOUND - An object of the present invention is to provide a novel fused-ring compound which has a FAAH inhibitory effect and is useful as an analgesic. | 09-16-2010 |
20100240668 | Myosin Light Chain Kinase Inhibitor Compounds, Compositions and Related Methods of Use - Pyridazinyl compounds, compositions and related methods of use. | 09-23-2010 |
20100273804 | PYRIDAZINE DERIVATIVES USEFUL AS FUNGICIDES AND FOR THE TREATMENT OF CANCER - The present invention relates to novel pyridazine derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: formula (I) wherein R | 10-28-2010 |
20100286157 | 4- [3- (4-CYCLOPROPANECARBONYL-PIPERAZINE-I-CARBONYL) -4 -FLUORO-BENZYL] -2H-PHTHALAZ IN-1-ONE - 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form L, methods of obtaining form L, pharmaceutical compositions comprising Form L and methods of using Form L and compositions comprising Form L. | 11-11-2010 |
20100286158 | DIHYDROPYRIMIDINONES - This invention relates to dihydropyrimidinones of the formula | 11-11-2010 |
20110003825 | SUBSTITUTED AMIDE BETA SECRETASE INHIBITORS - Disclosed are novel compounds of the formula | 01-06-2011 |
20110034474 | PYRIDAZINONE DERIVATIVES - Compounds of the formula (I), in which R | 02-10-2011 |
20110059978 | PYRIDAZINYL AMINE DERIVATIVES, THE USE THEREOF IN THE PREPARATION OF PICORNA VIRUS INHIBITORS - The present invention relates to substituted pyridazinylamine derivatives of the formula I or pharmaceutically acceptable salts or hydrates thereof, wherein the substituents are defined as in the description, their preparation process, pharmaceutical compositions comprising them, and uses of the said compounds as picorna virus inhibitors for prevention and/or treatment of diseases caused by picorna viruses. | 03-10-2011 |
20110077252 | PYRIDYL DERIVATIVES, THEIR PREPARATION AND USE - The present invention relates to pyridyl derivatives capable of inhibiting phosphatidylinositol-3-kinase (PI3k), mammalian target of rapamycin (mTOR) and/or hypoxia inducible factor 1α (HIF-1α) mediated signaling. Also disclosed are processes for preparation of the pyridyl derivatives, and their use in the manufacture of pharmaceutical compositions for the treatment of clinical conditions caused by deregulation of signaling pathways selected from one or more of PI3K, mTOR and HIF-1α pathways. The pyridyl derivatives are also useful for the treatment of conditions or disorders mediated by TNF-α. | 03-31-2011 |
20110082152 | THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN - A compound of formula: | 04-07-2011 |
20110112107 | SUBSTITUTED 6-(1-PIPERAZINYL)-PYRIDAZINES AS 5-HT6 RECEPTOR ANTAGONISTS - The present invention is concerned with novel substituted 6-(1-piperazinyl)-pyridazines of Formula (I) | 05-12-2011 |
20110118273 | PYRROLO-PYRIDINE, PYRROLO-PYRIMIDINE AND RELATED HETEROCYCLIC COMPOUNDS - Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: | 05-19-2011 |
20110124652 | Chemical Compounds and Uses - The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds. | 05-26-2011 |
20110136819 | 6-THIOXOPYRIDAZINE DERIVATIVES - Compounds of the formula I, in which R | 06-09-2011 |
20110152281 | COMPOUNDS AND METHOD FOR TREATMENT OF CANCER - The invention relates to a compound of Formula (I) and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, E-isomer, Z-isomer, or combination thereof, wherein X is selected from S or O; R | 06-23-2011 |
20110166153 | Protein Kinase Targeted Therapeutics - The present invention relates to compositions and methods useful in treating diseases and disorders related to protein kinases. In particular, the present invention relates to compositions and methods useful for targeting protein kinases related to mitogen activated protein kinase (MAPK) pathways (e.g., p38 MAPK, JNK, ERK, and upstream and downstream protein kinases) and/or casein kinase (CK) pathways (e.g., CK1δ, and upstream and downstream protein kinases), and diseases and disorders related to MAPK pathways (e.g., p38 MAPK, JNK, ERK, and upstream and downstream protein kinases) and/or CK pathways (e.g., CK1δ, and upstream and downstream protein kinases). | 07-07-2011 |
20110178093 | TETRASUBSTITUTED PYRIDAZINES HEDGEHOG PATHWAY ANTAGONISTS - The present invention provides novel tetrasubstituted pyridazine hedgehog pathway antagonists useful in the treatment of cancer. | 07-21-2011 |
20110224219 | MELANOCORTIN RECEPTOR AGONISTS - The present invention relates to a compound having a good agonistic activity to melanocortin receptor, or pharmaceutically acceptable salt or isomer thereof, and an agonistic composition for melanocortin receptor comprising the same as an active ingredient. | 09-15-2011 |
20110245262 | COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS - Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier. | 10-06-2011 |
20110269765 | Pyridazinone derivatives - Compounds of the formula (I) in which D, R | 11-03-2011 |
20110269766 | Benzimidazole-4-Carboxamide Derivatives, Their Preparation Methods, Pharmaceutical Compositions And Their Uses - The present invention relates to the benzimidazole-4-carboxamide derivatives, their preparation methods, pharmaceutical compositions and their uses; wherein X represents monosubstituted or bissubstituted or polysubstitued C | 11-03-2011 |
20110269767 | Novel Polymorphic Forms of 3-(1--6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile Hydrochloride Salt and Processes of Manufacturing Thereof - The present invention relates to 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer. | 11-03-2011 |
20110269768 | UROTENSIN II RECEPTOR ANTAGONISTS - This invention is directed to a compound of Formula (I): | 11-03-2011 |
20110275647 | PYRIMIDIN-4-(3H)-ONE DERIVATIVES - The present invention relates to a compound represented by a formula (I): or a pharmaceutically acceptable salt thereof, wherein R | 11-10-2011 |
20110294818 | 1H-QUINAZOLINE-2,4-DIONES - The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) | 12-01-2011 |
20120015954 | THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN - A compound of formula: | 01-19-2012 |
20120040991 | 3-AZABICYCLO [4.1.0] HEPTANES USED AS OREXIN ANTAGONISTS - Disclosed are 3-azabicyclo[4.1.0]heptane derivatives of formula (I) and their use as orexin receptor antagonists. | 02-16-2012 |
20120071486 | THIENOPYRIMIDINE COMPOUNDS AND USE THEREOF - The present invention provides a compound represented by the formula: | 03-22-2012 |
20120095011 | NOVEL COMPOUNDS - The invention provides compounds of formula | 04-19-2012 |
20120108600 | SUBSTITUTED 4-HYDROXYPYRIMIDINE-5-CARBOXAMIDES - The present invention relates to substituted 4-hydroxypyrimidine-5-carboxamides useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions. | 05-03-2012 |
20120115876 | N-BENZYL-4-METHYLENEAMINO-3-HYDROXY-2-PYRIDONES - Compounds of Formula (I) | 05-10-2012 |
20120142694 | SUBSTITUTED 4-HYDROXYPYRIMIDINE-5-CARBOXAMIDES - The present invention relates to substituted 4-hydroxypyrimidine-5-carboxamides useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions. | 06-07-2012 |
20120149710 | SORTASE A INHIBITORS - Bacterial infections, including Methicillin resistant | 06-14-2012 |
20120149711 | PIPERIDINE DERIVATIVES USED AS OREXIN ANTAGONISTS - This invention relates to heteroarylamine methyl substituted piperidine derivatives (I) and their use as antagonists of human orexin. | 06-14-2012 |
20120232087 | METHODS AND COMPOSITIONS FOR TREATING SOLID TUMORS AND OTHER MALIGNANCIES - A combination of a kinase inhibitors of mTOR and downstream effector and a hedgehog pathway inhibitor for the treatment of cancer. | 09-13-2012 |
20120245180 | COMBINATION - The present invention relates to a method of treating cancer in a mammal and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a novel combination comprising the MEK inhibitor: N-{3-[3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, and the PI3 kinase inhibitor: 2,4-difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl}benzenesulfonamide, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same, and methods of using such combinations in the treatment of cancer. | 09-27-2012 |
20120264761 | Aminobenzoquinazolinone M1 Receptor Positive Allosteric Modulators - The present invention is directed to aminobenzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 10-18-2012 |
20120316176 | DERIVATIVES OF 7,8-DIHYDRO-1H-IMIDAZO[2,1-b] PURIN-4(5H)-ONE and METHODS OF USE THEREOF - The present invention relates to derivatives of 7,8-dihydro-1H-imidazo[2,1-b]purin-4(5H)-one, compositions thereof and methods of use thereof for treating or preventing pain or an inflammatory disease. | 12-13-2012 |
20130018053 | SUBSTITUTED PYRIMIDINES - The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions. | 01-17-2013 |
20130029999 | MYOSIN LIGHT CHAIN KINASE INHIBITOR COMPOUNDS, COMPOSITIONS AND RELATED METHODS OF USE - Pyridazinyl compounds, compositions and related methods of use. | 01-31-2013 |
20130072496 | FORMULATIONS CONTAINING PYRIDAZINE COMPOUNDS - The invention relates to chemical compounds, compositions and methods of making and using the same. In particular, the invention provides selected pyridazine compounds of the formula I wherein R1, R4, R5, R6, R7, R8, R9, R12, R13 ET R14 are independently hydrogen, hydroxyl, alkyl, alkenyl, alkynyl, alkylene, alkenylene, alkoxy, alkenyloxy, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloalkoxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, amino, imino, azido, thiol, thioallyl, thioalkoxy, thioaryl, nitro, cyano, halo, sulfate, sulfonyl, sulfinyl, sulfonyl, sultanate, sulfoxide, silyl, silyloxy, silylalkyl, silylthio, =0, ═S, phosphonate, ureido, carboxyl, carbonyl, carbamoyl, or carboxamide; and X is optionally substituted pyrimidinyl or pyridazinyl, an isomer, a pharmaceutically acceptable salt, or derivative thereof. The invention additional relates to compositions comprising the compounds, and methods of using the compounds and compositions for modulation of cellular pathways, for treatment or prevention of inflammatory diseases, for research, drug screening, and therapeutic applications. | 03-21-2013 |
20130116263 | PAK INHIBITORS FOR THE TREATMENT OF CELL PROLIFERATIVE DISORDERS - Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of cell proliferative disorders and/or CNS disorders. | 05-09-2013 |
20130116264 | Novel Hetaryl (thio)carboxamide Compounds for Controlling Invertebrate Pests - The present invention relates to hetaryl (thio)carboxamide compounds of formula I, to the tautomers and N-oxides thereof and to the salts thereof: | 05-09-2013 |
20130131074 | PYRIDONE AND PYRIDAZONE ANALOGUES AS GPR119 MODULATORS - Novel compounds of structure Formula I: | 05-23-2013 |
20130143892 | NEW COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF - The present invention relates to compounds of general formula I, | 06-06-2013 |
20130190319 | PYRIDAZINE DERIVATIVES AND USE THEREOF AS MEDICAMENTS FOR TREATING MICRORNA VIRAL INFECTION - Disclosed are pyridazine derivatives represented by Formula I or pharmaceutically acceptable salts or hydrates thereof, pharmaceutical compositions comprising the compounds, methods of treating and/or preventing diseases or disorders associated with viral infections in patients using the compounds, and the use of the compounds in preparing the medicaments for treating and/or preventing diseases or disorders associated with viral infections. The compounds represented by Formula I have antiviral activity, especially anti-microRNA viral activity. Symbols in the compounds represented are described in the specification. | 07-25-2013 |
20130210831 | PYRROLOPYRIMIDINE COMPOUNDS AND USES THEREOF - The present disclosure provides pyrrolopyrimidine compounds and methods of use therefor. For example, the disclosure provides certain pyrrolopyrimidine compounds capable of inhibiting JAK kinases. The disclosure further provides the pharmaceutical compositions containing these pyrrolopyrimidine compounds, and use of these pyrrolopyrimidine compounds in the treatment of disorders or diseases, such as inflammatory diseases and cancer. | 08-15-2013 |
20130231345 | Compounds and Method for Treatment of Cancer - The invention relates to a compound of Formula I: | 09-05-2013 |
20130245033 | AMIDE COMPOUNDS - A compound represented by formula (I) and the pharmaceutical acceptable salt thereof are disclosed, | 09-19-2013 |
20130252963 | PYRIMIDINONE COMPOUNDS FOR USE IN THE TREATMENT OF DISEASE OR CONDITIONS MEDIATED BY LP-PLA2 - The present invention relates to novel compounds that inhibit Lp-PLA | 09-26-2013 |
20130296332 | 1H-QUINAZOLINE-2,4-DIONES - The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) | 11-07-2013 |
20130338162 | COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS - Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier. | 12-19-2013 |
20140142111 | Pyrazole Compounds for Controlling Invertebrate Pests - The present invention relates to pyrazole compounds of formulae I or II and the salts and N-oxides thereof, | 05-22-2014 |
20140142112 | THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN - A compound of formula: | 05-22-2014 |
20140148463 | PYRIDAZINONE DERIVATIVES - Compounds of the formula (I) in which D, R | 05-29-2014 |
20140163036 | Carbamate/urea derivatives - The invention relates to compound of the formula I | 06-12-2014 |
20140179709 | ANTIVIRAL AGENTS - This invention relates to compounds of formula I | 06-26-2014 |
20140200221 | NOVEL POLYMORPHIC FORMS OF 3-(1--6-OXO-1,6-DIHYDRO-PYRIDAZIN-3-YL)-BENZONITRILE HYDROCHLORIDE SALT AND PROCESSES OF MANUFACTURING THEREOF - The present invention relates to 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer. | 07-17-2014 |
20140221381 | THIENOPYRIMIDINE COMPOUNDS AND USE THEREOF - The present invention provides a compound represented by the formula: | 08-07-2014 |
20140249156 | Treatment Of Blood Lipid Abnormalities And Other Conditions - There is provided a method of treatment of a patient suffering from blood lipid abnormality comprises the administration of a GPR119 agonist. | 09-04-2014 |
20140350025 | COMPOUNDS FOR THE TREATMENT OF CNS DISORDERS - The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones of formula (I), | 11-27-2014 |
20140378464 | PYRIMIDINEDIONE COMPOUNDS - Provided are novel pyrimidine dione compounds and pharmaceutically acceptable salts thereof, that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds and pharmaceutically acceptable salts thereof, are described, as well as methods for treating HCM and other forms of heart disease. | 12-25-2014 |
20150011558 | PYRIDAZINE DERIVATIVES AND USE THEREOF AS MEDICAMENTS FOR TREATING MICRORNA VIRAL INFECTION - Disclosed are pyridazine derivatives represented by Formula I or pharmaceutically acceptable salts or hydrates thereof, pharmaceutical compositions comprising the compounds, methods of treating and/or preventing diseases or disorders associated with viral infections in patients using the compounds, and the use of the compounds in preparing the medicaments for treating and/or preventing diseases or disorders associated with viral infections. The compounds represented by Formula I have antiviral activity, especially anti-microRNA viral activity. Symbols in the compounds represented are described in the specification. | 01-08-2015 |
20150099756 | PYRIMIDINONE COMPOUNDS FOR USE IN THE TREATMENT OF DISEASES OR CONDITIONS MEDIATED BY LP-PLA2 - The present invention relates to novel compounds that inhibit Lp-PLA | 04-09-2015 |
20150105397 | Piperazine derivatives and the use thereof as medicament - The present inventions relate to substituted piperazine derivatives of general formula (I) | 04-16-2015 |
20150148351 | NOVEL POLYMORPHIC FORMS OF 3-(1--6-OXO-1,6-DIHYDRO-PYRIDAZIN-3-YL)-BENZONITRILE HYDROCHLORIDE SALT AND PROCESSES OF MANUFACTURING THEREOF - The present invention relates to 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer. | 05-28-2015 |
20150291561 | SUBSTITUTED PYRIDONE DERIVATIVES AS PDE10 INHIBITORS - The present invention is directed to substituted pyridinone 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. | 10-15-2015 |
20150297594 | Combination of a 6-oxo-1,6-dihydro-pyridazine derivative having anti-cancer activity with a MEK inhibitor - A pharmaceutical composition comprising 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile or a pharmaceutically acceptable salt and/or solvate thereof and N-((S)-2,3-dihydroxy-propyl)-3-(2-fluoro-4-iodo-phenylamino)-isonicotinamide or a pharmaceutically acceptable salt and/or solvate thereof. | 10-22-2015 |
20150299121 | MODULATORS OF THE RETINOID-RELATED ORPHAN RECEPTOR GAMMA (ROR-GAMMA) FOR USE IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISEASES - The present invention relates to novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORγ. | 10-22-2015 |
20150307489 | PYRIMIDINE PDE10 INHIBITORS - The present invention is directed to pyrimidine 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. | 10-29-2015 |
20150368240 | DIHYDROPYRIDO PYRIMIDINE COMPOUNDS AS AUTOTAXIN INHIBITORS - The present invention provides compounds of the formula (I) or a pharmaceutically acceptable salt thereof. Compounds of the invention are autotaxin inhibitors useful in the treatment of pain associated with osteoarthritis. | 12-24-2015 |
20150376167 | PYRIDAZINONE-AMIDES DERIVATIVES - The present invention relates to compounds of formula (I) wherein R1, Ra, Rb and Z have the meaning given in claim | 12-31-2015 |
20160016947 | SUBSTITUTED PYRIDIZINONE DERIVATIVES AS PDE10 INHIBITORS - The present invention is directed to substituted pyridizinone compounds of formula I 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. | 01-21-2016 |
20160030428 | PYRIMIDINEDIONE COMPOUNDS - Provided are novel pyrimidine dione compounds and pharmaceutically acceptable salts thereof, that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds and pharmaceutically acceptable salts thereof, are described, as well as methods for treating HCM and other forms of heart disease. | 02-04-2016 |
20160052939 | SUBSTITUTED 2-AZABICYCLES AND THEIR USE AS OREXIN RECEPTOR MODULATORS - The present invention is directed to compounds of Formula I: wherein X is N or CR1; Y is N or CR2; R1 is H, alkoxy, halo, triazolyl, pyrimidinyl, oxazolyl, isoxazole, oxadiazolyl, or pyrazolyl; R2 is H, alkyl, alkoxy, or halo; Z is NH or O; R3 is H, alkyl, alkoxy, halo, or triazolyl; R4 is H or alkyl; or R3 and R4, together with the atoms to which they are attached, form a 6-membered aryl ring or a 5- or 6-membered heteroaryl ring; R5 is pyridyl, pyrazinyl, or pyrimidinyl, wherein the pyridyl, pyrazinyl, or pyrimidinyl is optionally substituted with halo or alkyl; and n is 1 or 2. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention. | 02-25-2016 |
20160082117 | LOW MOLECULAR WEIGHT POLYETHYLENE GLYCOL DRUG CONJUGATES HAVING IMPROVED DRUG BIOLOGICAL ACTIVITY - Provided are polyethylene glycol drug conjugates of general formula (I), (II) or (III) and pharmaceutical compositions and a use thereof. The conjugates are formed by combining low molecular weight polyethylene glycol with 2-4 drug molecules. The conjugates can interact with receptor dimers or polymers, thereby improving the in vivo distribution of the drug, changing the oil and water distribution coefficient, enhancing the pharmacological activity, reducing the blood-brain barrier permeability of the drug, and improving the bioavailability of the drug. | 03-24-2016 |
20160122353 | HETEROCYCLIC COMPOUNDS AS PEST CONTROL AGENTS - The present application relates to the use of known and novel heterocyclic compounds for controlling animal pests, to novel heterocyclic compounds, to processes for preparation thereof and to the use thereof for controlling animal pests. | 05-05-2016 |
20160145236 | 4-(3-CYANOPHENYL)-6-PYRIDINYLPYRIMIDINE MGLU5 MODULATORS - The disclosures herein relate to novel compounds of formula wherein R | 05-26-2016 |
20160151366 | Compositions and Methods for Treating Autism Spectrum Disorders | 06-02-2016 |
20160168130 | HETEROARYL SUBSTITUTED PYRAZOLES | 06-16-2016 |
20160184310 | OXOQUINAZOLINYL-BUTANAMIDE DERIVATIVES - Compounds of the formula I | 06-30-2016 |
20180021442 | LOW MOLECULAR WEIGHT POLYETHYLENE GLYCOL DRUG CONJUGATES HAVING IMPROVED DRUG BIOLOGICAL ACTIVITY | 01-25-2018 |
20180021443 | LOW MOLECULAR WEIGHT POLYETHYLENE GLYCOL DRUG CONJUGATES HAVING IMPROVED DRUG BIOLOGICAL ACTIVITY | 01-25-2018 |