Entries |
Document | Title | Date |
20080214578 | Novel 5-Substituted 7-Amino-[1,3]Thiazolo[4,5-D]Pyrimidine Derivatives 793 - There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives of formula (I) wherein R | 09-04-2008 |
20080214579 | THIENOPYRIMIDINEDIONES AND THEIR USE IN THE MODULATION OF AUTOIMMUNE DISEASE - The invention relates to thienopyrimidinediones of formula (1): | 09-04-2008 |
20080221131 | THIENOPYRIMIDINEDIONES AND THEIR USE IN MODULATION OF AUTOIMMUNE DISEASE - The invention relates to thienopyrimidinediones of formula (I): | 09-11-2008 |
20080249114 | ARYLOXYPROPANOLAMINES, METHODS OF PREPARATION THEROF AND USE OF ARYLOXYPROPANOLAMINES AS MEDICAMENTS - This invention relates to novel aryloxypropanolamines. The invention also relates to the pharmaceutically acceptable salts and solvates containing said compounds, methods for the preparation thereof and to respective synthetic intermediates. Said compounds have agonistic activity at β3 adrenergic receptors and are useful for treatment of ailments influenced by activation of β3 adrenergic receptors. | 10-09-2008 |
20080275066 | Condensed Thiophene Derivatives and Their Use as Cyclic Glp-1 Agonists - The invention provides compounds of formula (I) for use as GLP-1 receptor agonists. | 11-06-2008 |
20080287465 | Cyclic N-Hydroxy Imides as Inhibitors of Flap Endonuclease and Uses Thereof - Acrylic n-hydroxy imides and their use in pharmaceutical compositions and in the inhibition of flap endonuclease are disclosed. | 11-20-2008 |
20080287466 | 4-AMINO-2,3-DISUBSTITUTED THIENO [2,3,D]PYRIMIDINES AND PHARMACEUTICAL COMPOSITIONS THEREOF - Furo- and thienopyrimidine derivatives, which are useful as TIE-2 and/or VEGFR-2 inhibitors are described herein. The described invention also includes methods of making such furo- and thienopyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases. | 11-20-2008 |
20080293745 | New amino-alkyl-amide derivatives as CCR3 receptor ligands - The invention relates to a compound of the general formula (I), | 11-27-2008 |
20080306093 | MODULATION OF CHEMOSENSORY RECEPTORS AND LIGANDS ASSOCIATED THEREWITH - The present invention provides screening methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors as well as modifiers capable of modulating chemosensory receptors and their ligands. | 12-11-2008 |
20080312256 | Organic Compounds - The present invention provides compounds of the formula | 12-18-2008 |
20080318981 | Novel Compounds 480 - There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) | 12-25-2008 |
20090042913 | Indolylalkylthienopyrimidylamines as modulators of the EP2 receptor - The present invention relates to indolylalkylthienopyrimidylamines of the general formula I, to processes for their preparation and to their use for production of pharmaceutical compositions for treatment of disorders and indications connected to the EP | 02-12-2009 |
20090048273 | PREMATURE OVULATION PREVENTIVE AGENT - The present invention provides a premature ovulation inhibitor for use in in vitro fertilization or embryo transfer process, which contains a nonpeptidic compound having a gonadotropin releasing hormone antagonistic action. The premature ovulation inhibitor for use in in vitro fertilization or embryo transfer process of the present invention is low toxic, permits oral administration, and has a superior inhibitory effect on premature ovulation in in vitro fertilization or embryo transfer process. | 02-19-2009 |
20090069347 | 2-phenoxy pyrimidinone analogues - 2-Phenoxy pyrimidinone analogues are provided, of the Formula: | 03-12-2009 |
20090099210 | ENANTIOMERS OF SELECTED FUSED HETEROCYCLICS AND USES THEREOF - This invention relates to novel compounds having the structural formula (I) | 04-16-2009 |
20090111835 | THIENOPYRIMIDINE AND THIENOPYRIDINE DERIVATIVES SUBSTITUTED WITH CYCLIC AMINO GROUP - An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastral diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alpecia, irritable bowel syndrome, sleep disorders, dermatitides, schizophrenia, pain, etc. A thienopyrimidine or thienopyridine derivative substituted with a cyclic amino group represented by the following formula [I]: has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved. | 04-30-2009 |
20090124637 | Novel 5,7-Disubstituted [1,3]Thiazolo[4,5-D]Pyrimidin-2(3H)-One Derivatives 794 - There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) [Chemical formula should be inserted here. Please see paper copy] wherein R | 05-14-2009 |
20090131455 | HETEROCYCLIC DERIVATIVES - The present invention relates to a heterocyclic derivative according to formula I | 05-21-2009 |
20090131456 | CASPASE INHIBITORS AND USES THEREOF - This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors. These compounds have the general formula I: | 05-21-2009 |
20090143412 | FUROPYRIDINE AND FUROPYRIMIDINE DERIVATIVES FOR THE TREATMENT OF HYPER-PROLIFERATIVE DISORDERS - This invention relates to a compound of Formula I | 06-04-2009 |
20090192176 | 1H-PYRAZOLO[3,4-D]PYRIMIDINE, PURINE, 7H-PURIN-8(9H)-ONE, 3H-[1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE, AND THIENO[3,2-D]PYRIMIDINE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES - The invention relates to 1H-pyrazolo[3,4-d]pyrimidine, purine, 7H-purin-8(9H)-one, 3H-[1,2,3]triazolo[4,5-d]pyrimidine, and thieno[3,2-d]pyrimidine compounds, compositions comprising the compounds, and methods for making and using the compounds. | 07-30-2009 |
20090203716 | Pyrimidine low molecular weight ligands for modulating hormone receptors - Disclosed herein are small molecule modulators hormone receptors, including agonists and antagonists of luteinizing hormone/choriogonadotropin, follicle stimulating hormone and thyroid stimulating hormone receptors. Exemplary disclosed compounds include those of the formula | 08-13-2009 |
20090209559 | PHARMACEUTICAL COMPOUNDS - Fused pyrimidines of formula (I): | 08-20-2009 |
20090239882 | Thiazolopyramidine Compounds for the Modulation of Chemokine Receptor Activity - A compound of formula (I), or a pharmaceutically acceptable salt, or solvate thereof; and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders. | 09-24-2009 |
20090247554 | KINASE INHIBITORS - Compounds are provided for use with kinases that comprise (I), (II), (III), (IV): wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds. | 10-01-2009 |
20090247555 | 5,7-Disubstituted[1,3]Thiazolo[4,5-D]Pyrimidin-2(3H)-One Derivatives 258 - There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) | 10-01-2009 |
20090270424 | Crystalline N-(4-(4-aminothieno[2,3-d]pyrimidin-5-yl)phenyl)-N'-(2-fluoro-5-(trifluor- omethyl)phenyl)urea hydrochloride - A crystalline N-(4-(4-aminothieno[2,3-d]pyrimidin-5-yl)phenyl)-N′-[2-fluoro-5-(trifluoromethyl)phenyl)urea hydrochloride, ways to make it, compositions comprising it, and methods of treatment using it are disclosed. | 10-29-2009 |
20090281123 | NOVEL THIAZOLO (4,5-D) PYRIMIDINE COMPOUNDS NOVEL COMPOUNDS - The invention provides certain thiazolopyrimidine compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy. | 11-12-2009 |
20090281124 | 4-CYANOPHENYLAMINO-SUBSTITUTED BICYCLIC HETEROCYCLIC COMPOUNDS AS HIV INHIBITORS - This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula I | 11-12-2009 |
20090291971 | HETEROARYL ETHERS AND PROCESSES FOR THEIR PREPARATION - The present invention relates to processes for the preparation of heteroaryl ethers. In some embodiments, the processes relate to cross coupling reactions between triazol-1-yloxy and triazol-1-yl heterocycles with aryl boronic acids. In a further aspect, this invention also relates to compounds that are useful for the treatment of oncological diseases or disorders, and for the treatment of inflammation. | 11-26-2009 |
20090298856 | 2,3 Substituted fused bicyclic pyrimidin-4(3H)-ones modulating the function of the vanilliod-1receptor (VR1) - The use of a compound of formula (I): for the manufacture of a medicament for the treatment of conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1, also known as TRPV1). | 12-03-2009 |
20090318475 | Novel, Acyclically Substituted Furopyrimidine Derivatives and Use Thereof - The present application relates to novel, acyclically substituted furopyrimidine derivatives, methods for their production, their use for the treatment and/or prophylaxis of diseases and their use for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases. | 12-24-2009 |
20100010016 | BICYCLIC COMPOUNDS HAVING ANTIMITOTIC AND/OR ANTITUMOR ACTIVITY AND METHODS OF USE THEREOF - The present invention provides bicyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells. | 01-14-2010 |
20100010017 | CERTAIN THIENOPYRIMIDINE DERIVATIVES AS PHOSPHODIESTERASE 10 INHIBITORS - Certain thienopyrimidine derivatives are useful for the inhibition of PDE10 enzymes, and thus are useful for treating psychiatric or neurological syndromes, e.g., psychoses, obsessive-compulsive disorder and/or Parkinson's disease, as well as, for example, treating a disease state modulated by PDE10 activity. | 01-14-2010 |
20100035899 | 5,7-DISUBSTITUTED[1.3]THIAZOLO[4,5-d]PYRIMIDIN-2(3H)-AMINE DERIVATIVES AND THEIR USE IN THERAPY - There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives of formula (I) wherein R | 02-11-2010 |
20100041676 | Kinase inhibitors - The present application is directed to compounds of the formula (I) | 02-18-2010 |
20100048591 | CHEMICAL COMPOUNDS AND PROCESSES - The present invention relates generally to chemical compounds and methods for their use and preparation. In particular, the invention relates to chemical compounds which may possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds. | 02-25-2010 |
20100056548 | THIENOPYRIMIDINES HAVING MNK1/MNK2 INHIBITING ACTIVITY FOR PHARMACEUTICAL COMPOSITIONS - The present invention relates to novel pharmaceutical compositions comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof. | 03-04-2010 |
20100081675 | FUSED MULTICYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS - Fused multicyclic compounds of formula (I): | 04-01-2010 |
20100087453 | COMPOUNDS, SCREENS, AND METHODS OF TREATMENT - The present invention features compounds of Formula (I), pharmaceutical compositions, methods of synthesis, and methods for treating diseases and conditions associated with cellular necrosis. Screening assays for identifying compounds useful for treating these conditions are also described. | 04-08-2010 |
20100093763 | PHENYL SUBSTITUTED THIENO[2,3-d]PYRIMIDINES AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS - This invention relates to a novel thieno[2,3-d]pyrimidine, Z, and its therapeutic and prophylactic uses, wherein R | 04-15-2010 |
20100093764 | AMINES AND SULFOXIDES OF THIENO[2,3-d]PYRIMIDINE AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS - This invention relates to a novel thieno[2,3-d]pyrimidine, A, and its therapeutic and prophylactic uses, wherein R | 04-15-2010 |
20100113485 | Piperidinylamino-thieno[2,3-D] Pyrimidine Compounds - The invention relates to 5-HT receptor modulators, particularly 5-HT | 05-06-2010 |
20100130514 | FUSED HETEROCYCLIC DERIVATIVE, PHARMACEUTICAL COMPOSITION COMPRISING THE DERIVATIVE, AND USE OF THE COMPOSITION FOR MEDICAL PURPOSES - The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides fused heterocyclic derivatives represented by the following general formula (I), pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A is 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; R | 05-27-2010 |
20100152206 | Bicyclic Dihydropyrimidines and Uses Thereof - The present invention provides compounds having formula (I): (I) and pharmaceutically acceptable derivatives thereof; as described generally and in subclasses herein, which compounds are useful as kinesin inhibitors (e.g., Eg5 inhibitors), and thus are useful, for example, for the treatment of proliferative disorders e.g., cancer. The invention additionally provides methods for preparing compounds of the invention, compositions comprising them, and methods for the use thereof in the treatment of various disorders where Eg5 is involved. In certain embodiments, the present invention provides for compounds, compositions, methods and systems for inhibiting cell growth. More specifically, the present invention provides for methods, compounds and compositions which are capable of inhibiting mitosis in metabolically active cells. Compounds, compositions and methods of the present invention inhibit the activity of a protein involved in the assembly and maintenance of the mitotic spindle. One class of proteins which acts on the mitotic spindle is the family of mitotic kinesins, a subset of the kinesin superfamily. | 06-17-2010 |
20100152207 | GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO - GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure, wherein R | 06-17-2010 |
20100152208 | BICYCLIC HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE - Bicyclic heteroaromatic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). 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, such as atherosclerosis; obesity; Type 2 diabetes; insulin resistance; hyperglycemia; Metabolic Syndrome; neurological disease; cancer; and liver steatosis. Formula (I). | 06-17-2010 |
20100160348 | MATERIALS AND METHODS FOR DETECTING AND TREATING PERITONEAL OVARIAN TUMOR DISSEMINATION INVOLVING TISSUE TRANSGLUTAMINASE - Tissue transglutaminase-2 (TG2) is involved in Ca | 06-24-2010 |
20100216820 | THIENOPYRIMIDIONES FOR TREATMENT OF INFLAMMATORY DISORDERS AND CANCERS - The current invention provides compounds of formula (1): wherein: one of Q | 08-26-2010 |
20100227873 | NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF - The present invention provides compounds of Formula (I): | 09-09-2010 |
20100234399 | AGENT FOR OVERCOMING RESISTANCE TO ANTI-CANCER AGENT - An agent comprising, as an active ingredient, a xanthine oxidase inhibitor such as 2-[3-cyano-4-(4-fluorophenoxy)phenyl]-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-[3-cyano-4-(4-fluorophenoxy)phenyl]thiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-(3-cyano-4-phenoxyphenyl)thiazolo[5,4-d]pyrimidine, TMX-67, and FYX-051, which can be used as an agent for overcoming anti-cancer agent resistance. | 09-16-2010 |
20100261736 | SUBSTITUTED BICYCLIC HETEROARYL COMPOUNDS FOR THE TREATMENT OF CARDIOVASCULAR DISEASE - The present application relates to novel substituted bicyclic heteroaryl compounds, to processes for their preparation, to their use 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 diseases. | 10-14-2010 |
20100267749 | TRISUBSTITUTED FUROPYRIMIDINES AND USE THEREOF - The invention relates to the novel 4,5,6-trisubstituted furo[2,3-d]pyrimidine derivatives of formula (I), to methods for their production, their use in the treatment and/or prophylaxis of diseases and their use in the production of drugs for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular diseases. | 10-21-2010 |
20100273815 | THIENO[2,3-D]-PYRIMIDIN-4(3H)-ONE COMPOUNDS WITH ANTIFUNGAL PROPERTIES AND PROCESS THEREOF - The present invention discloses novel compounds of the Formula (1), containing thieno-[2,3-d]pyrimidin-4(3H)-one moieties and pharmaceutically acceptable salts thereof, methods for preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds. | 10-28-2010 |
20100280050 | Piperidinylamino-Thieno[2,3-D] Pyrimidine Compounds for Treating Fibrosis - The invention provides a method of treating or preventing fibrosis in a subject by administering a 5-HT modulator, e.g., a 5-HT | 11-04-2010 |
20100286174 | INHIBITING GSNOR - Treatment of myocardial infarction to reduce infarct size and organogenesis is provided by administration of agents selected from the group consisting of | 11-11-2010 |
20100298349 | THIENOPYRIMIDINE COMPOUNDS AND COMPOSITIONS - Compounds of formula (I) are A | 11-25-2010 |
20100331348 | TROPANE DERIVATIVES USEFUL AS PESTICIDES - Compounds of formula (I) wherein the substituents have the meanings assigned to them in claim | 12-30-2010 |
20110021541 | INHIBITORS OF HUMAN PHOSPHATIDYL-INOSITOL 3-KINASE DELTA - Compounds that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3Kδ plays a role in leukocyte function, using the compounds also are disclosed. | 01-27-2011 |
20110028496 | Deuterium-enriched pyrimidine compounds and derivatives - The present invention is concerned with deuterium-enriched pyrimidine compounds of formula I, their derivatives and pharmaceutically acceptable salts and methods of use thereof | 02-03-2011 |
20110046163 | FURANOPYRIMIDINE CANNABINOID COMPOUNDS AND RELATED METHODS OF USE - Furanopyrimidine cannabinoid analog compounds of the formula I are disclosed. | 02-24-2011 |
20110082157 | Piperidinylamino-Thieno [2,3-D] Pyrimidine Compounds - The invention relates to 5-HT receptor antagonists. Novel piperidinylamino-thieno [2,3-d] pyrimidine compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as pulmonary arterial hypertension, migraine, hypertension, disorders of the gastrointestinal tract, restenosis, asthma, obstructive airway disease, prostatic hyperplasia and priapism, anxiety, depression, schizophrenia, neural injury and stroke. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also provided. | 04-07-2011 |
20110082158 | SELECTIVE PROTON COUPLED FOLATE TRANSPORTER AND FOLATE RECEPTOR, AND GARFTASE AND/OR OTHER FOLATE METABOLIZING ENZYMES INHIBITOR COMPOUNDS AND METHODS OF USING THE SAME - Fused cyclic pyrimidine compounds, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, are disclosed having the general Formula II: | 04-07-2011 |
20110086865 | ANT-LIGANDS MOLECULES AND BIOLOGICAL APPLICATIONS - The invention relates to molecules ANT-ligands having a substituted nitrogeneous heterocycle A wherein —A is a substituted pyrazinone of formula I | 04-14-2011 |
20110092519 | 5,7-DISUBSTITUTED THIAZOLO[4,5-D]PYRIMIDINES AS CHEMOKINE INHIBITORS - There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives of formula (I) wherein R | 04-21-2011 |
20110105537 | 5,7-DISUBSTITUTED THIAZOLO[4,5-D]PYRIMIDINES FOR THE SELECTIVE INHIBITION OF CHEMOKINE RECEPTORS - There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) | 05-05-2011 |
20110118284 | THIENOPYRIMIDINE COMPOUNDS - Compounds of formula (I) are A | 05-19-2011 |
20110124665 | Novel, Cyclically Substituted Furopyrimidine Derivatives and Use Thereof - The present application relates to novel, cyclically substituted furopyrimidine derivatives, methods for their production, their use for the treatment and/or prophylaxis of diseases and their use for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases. | 05-26-2011 |
20110136834 | INHIBITORS OF E1 ACTIVATING ENZYMES - This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia. | 06-09-2011 |
20110166163 | SUBSTITUTED FUROPYRIMIDINES AND USE THEREOF - The present application relates to novel substituted furopyrimidine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular diseases. | 07-07-2011 |
20110166164 | THIAZOLO[5,4-d] PYRIMIDINES AND THEIR USE AS AGROCHEMICALS - The present disclosure relates to thiazolo[5,4-d]pyrimidines and their use as agrochemicals and animal health products. | 07-07-2011 |
20110201628 | HETEROCYCLIC JAK KINASE INHIBITORS - The present invention relates to compounds of Formula (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer. | 08-18-2011 |
20110230502 | MODULATION OF CHEMOSENSORY RECEPTORS AND LIGANDS ASSOCIATED THEREWITH - The present invention provides screening methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors as well as modifiers capable of modulating chemosensory receptors and their ligands. | 09-22-2011 |
20110251216 | COMPOSITIONS AND METHODS FOR INHIBITING EZH2 - The present invention relates to therapeutic targets for cancer. In particular, the present invention relates to small molecules and nucleic acids that target EZH2 expression in cancer (e.g., prostate cancer, breast cancer, other solid tumors, multiple myeloma). | 10-13-2011 |
20110257201 | AGENT FOR OVERCOMING RESISTANCE TO ANTI-CANCER AGENT - An agent comprising, as an active ingredient, a xanthine oxidase inhibitor such as 2-[3-cyano-4-(4-fluorophenoxy)phenyl]-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-[3-cyano-4-(4-fluorophenoxy)phenyl]thiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-(3-cyano-4-phenoxyphenyl)thiazolo[5,4-d]pyrimidine, TMX-67, and FYX-051, which can be used as an agent for overcoming anti-cancer agent resistance. | 10-20-2011 |
20120004245 | COMPOUNDS FOR THE TREATMENT OF POSTERIOR SEGMENT DISORDERS AND DISEASES - The use of certain urea compounds, for the treatment of retinal disorders associated with pathologic ocular angiogenesis and/or neovascularization is disclosed. | 01-05-2012 |
20120010223 | ISOTHIAZOLO-PYRIMIDINEDIONE DERIVATIVES AS TRPAI MODULATORS - The present invention is related to novel isothiazolo[3,4-d]pyrimidinedione and isothiazolo[5,4-d]pyrimidinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. | 01-12-2012 |
20120035191 | Deuterium-enriched pyrimidine compounds and derivatives - The present invention is concerned with deuterium-enriched pyrimidine compounds of formula I, their derivatives and pharmaceutically acceptable salts and methods of use thereof | 02-09-2012 |
20120122889 | SMALL MOLECULE INHIBITORS OF NECROPTOSIS - The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-α) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (I)-(I), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-α induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role. | 05-17-2012 |
20120122890 | Potassium Channel Modulators - Disclosed herein are KCNQ potassium channels modulators of formula (I) | 05-17-2012 |
20120122891 | GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO - GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: | 05-17-2012 |
20120136011 | COMPOUNDS AND METHODS FOR SKIN REPAIR - The disclosure provides compositions and methods for treating a skin blemish. The compositions comprise a therapeutically effective amount of a compound useful for treating skin blemishes such as wounds, scars and wrinkles. | 05-31-2012 |
20120178766 | FUROPYRIMIDINEDIONE DERIVATIVES AS TRPAI MODULATORS - The present invention is related to novel furopyrimidinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. | 07-12-2012 |
20120178767 | TREATMENT OF LIVER DISORDERS WITH P13K INHIBITORS - The invention provides methods to treat certain liver disorders by administering a compound that inhibits PD K isoforms, particularly the delta isoform. It further provides specific compounds useful for these methods and ways to identify subjects who are particularly suitable for receiving these treatments. | 07-12-2012 |
20120208829 | 2-PHENOXY PYRIMIDINONE ANALOGUES - 2-Phenoxy pyrimidinone analogues are provided, of the Formula: | 08-16-2012 |
20120225894 | Substituted Thienol[2,3-d] pyrimidines as HIV Inhibitors - This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula I | 09-06-2012 |
20120264768 | BICYCLIC AND TRICYCLIC PYRIMIDINE TYROSINE KINASE INHIBITORS WITH ANTITUBULIN ACTIVITY AND METHODS OF TREATING A PATIENT - Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed. | 10-18-2012 |
20120270886 | INHIBITORS OF IAP - The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula (I): wherein Q, X | 10-25-2012 |
20120289522 | COMPOUNDS AS LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS - Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases. | 11-15-2012 |
20120295924 | THIENOPYRIMIDINEDIONE DERIVATIVES AS TRPA1 MODULATORS - The present invention is related to novel thienopyrimidinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. | 11-22-2012 |
20120309773 | HETEROCYCLIC COMPOUNDS AS JANUS KINASE INHIBITORS - The invention provides compounds of formula I: | 12-06-2012 |
20120316184 | NOVEL MICROBICIDES - Compounds of formula (I) wherein G | 12-13-2012 |
20130023544 | CARBOXYLIC ACID DERIVATIVES HAVING AN OXAZOLO[5,4-d]PYRIMIDINE RING - The invention therefore relates to compounds of the formula I | 01-24-2013 |
20130023545 | CYCLOALKYLOXYCARBOXYLIC ACID DERIVATIVES - The present invention relates to cycloalkyloxycarboxylic acid derivatives of the formula I | 01-24-2013 |
20130023546 | THIENOPYRIMIDINE DERIVATIVES - This invention provides thienopyrimidine derivatives of the formula, | 01-24-2013 |
20130035347 | AROMATIC BYCYCLIC DERIVATIVES AS CXCR4 RECEPTOR MODULATORS - The present invention relates to novel aromatic bicyclic derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the CXCR4 receptor. | 02-07-2013 |
20130059866 | NOVEL PIPERIDINO-DIHYDROTHIENOPYRIMIDINE SULFOXIDES AND THEIR USE FOR TREATING COPD AND ASTHMA - The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, | 03-07-2013 |
20130059867 | SALT OF FUSED HETEROCYCLIC DERIVATIVE AND CRYSTAL THEREOF - An objective of the present invention is to improve the solubility of 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid. | 03-07-2013 |
20130065914 | HALOGEN OR CYANO SUBSTITUTED THIENO [2,3-D]PYRIMIDINES HAVING MNK1/MNK2 INHIBITING ACTIVITY FOR PHARMACEUTICAL COMPOSITIONS - The present invention relates to novel thienopyhmidine compounds of general formula (I), pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof. | 03-14-2013 |
20130072501 | 2,5-SUBSTITUTED OXAZOLOPYRIMIDINE DERIVATIVES - The invention relates to oxazolopyrimidine compounds of formula I, where A, R | 03-21-2013 |
20130072502 | HETEROCYCLIC CARBOXYLIC ACID DERIVATIVES HAVING A 2,5-SUBSTITUTED OXAZOLOPYRIMIDINE RING - Heterocyclic carboxylic acid derivatives comprising a 2,5-substituted oxazolopyrimidine ring as Edg-1 receptor agonists | 03-21-2013 |
20130079357 | CARBOXYLIC ACID DERIVATIVES HAVING A 2,5,7-SUBSTITUTED OXAZOLOPYRIMIDINE RING - The invention relates to oxazolopyrimidine compounds of formula (I), where A, R | 03-28-2013 |
20130079358 | CARBOXYLIC ACID DERIVATIVES HAVING A 2,5-SUBSTITUTED OXAZOLOPYRIMIDINE RING - The present invention relates to oxazolopyrimidine compounds of the formula I, | 03-28-2013 |
20130079359 | NOVEL PIPERIDINO-DIHYDROTHIENOPYRIMIDINE SULFOXIDES AND THEIR USE FOR TREATING COPD AND ASTHMA - The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, | 03-28-2013 |
20130096141 | BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF - Compounds of structural formula I: are GPR119 agonists and are useful for the treatment, control or prevention of disorders responsive to agonism of GPR119, such as metabolic-related disorders such as type I diabetes, type II diabetes, inadequate glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia or syndrome X. The compounds are also reported as being useful for controlling weight gain, controlling food intake, and inducing satiety in mammals. | 04-18-2013 |
20130102621 | NOVEL CONDENSED PYRIDINE OR CONDENSED PYRIMIDINE DERIVATIVE, AND MEDICINAL AGENT COMPRISING SAME - The present invention relates to provision of a novel compound that has an activity of promoting insulin secretion from pancreatic β cells and thus is useful as a prophylaxis and/or therapeutic agent for diseases caused by hyperglycemia such as diabetes mellitus, and | 04-25-2013 |
20130123279 | CRYSTAL OF THIENOPYRIMIDINE DERIVATIVE - Crystals are obtained by heating an aqueous suspension of 2-(3,4-dichlorobenzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylic acid. Novel crystals are obtained by adjusting the heating temperature and/or duration. | 05-16-2013 |
20130158051 | HETEROCYCLIC CARBOXYLIC ACID DERIVATIVES HAVING A 2,5,7-SUBSTITUTED OXAZOLOPYRIMIDINE RING - The invention relates to oxazolopyrimidine compounds of formula (I), where A, R | 06-20-2013 |
20130225609 | COMBINATIONS OF MEDICAMENTS, CONTAINING PDE4-INHIBITORS AND EP4-RECEPTOR-ANTAGONISTS - The present invention relates to new medicament combinations which contain in addition to one or more PDE4-inhibitors (1) at least one EP4 receptor antagonist (2), as well as the use thereof for the treatment of preferably respiratory complaints such as particularly COPD, chronic sinusitis and asthma. | 08-29-2013 |
20130281467 | NOVEL MICROBICIDES - Compounds of formula (I), wherein G represents together with the two carbon atoms of the pyrimidine ring to which it is attached, a 5- to 7-membered aliphatic carbocyclic or heterocyclic ring system which contain 0 to 2 heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur; and wherein said 5- to 7-membered aliphatic carbocyclic or heterocyclic ring system can be mono-, di- or trisubstituted by substituents selected from the group consisting of halogen, keto, C | 10-24-2013 |
20130281468 | BICYCLIC ARYL AND BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS - Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed. | 10-24-2013 |
20130289054 | THIENOPYRIMIDINEDIONE DERIVATIVES AS TRPA1 MODULATORS - The present invention is related to novel thienopyrimidinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. | 10-31-2013 |
20130296344 | CHROMENE DERIVATIVES AND THEIR ANALOGA AS WNT PATHWAY ANTAGONISTS - Compounds according to the general formula (I) wherein X | 11-07-2013 |
20130303550 | CHROMENE DERIVATIVES AND THEIR ANALOGA AS WNT PATHWAY ANTAGONISTS - Compounds of formula (IIc); wherein X | 11-14-2013 |
20130303551 | PYRIMIDINONE DERIVATIVES AS FATTY ACID SYNTHASE INHIBITORS - This invention relates to the use of pyrimidinone derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of pyrimidinones in the treatment of cancer. | 11-14-2013 |
20130317044 | NOVEL CARBOXYLIC ACID DERIVATIVES, THEIR PREPARATION AND USE - Carboxylic acid derivatives | 11-28-2013 |
20130317045 | THIENOPYRIDINE AND THIENOPYRIMIDINE COMPOUNDS AND METHODS OF USE THEREOF - Provided herein are thienopyridine and thienopyrimidine compounds of formula (I) for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions. | 11-28-2013 |
20140011818 | ENANTIOMERS OF FLUCONAZOLE ANALOGUES CONTAINING THIENO-[2,-3-D]PYRIMIDIN-4(3H)-ONE MOIETY AS ANTIFUNGAL AGENTS - The present invention discloses novel enantiomeric antifungal compounds of Formula (1a) and Formula (1b) containing thieno-[2,3-d]Jpyrimidin-4(3H)-one moiety and pharmaceutically acceptable salts thereof, method of preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these compounds. | 01-09-2014 |
20140024661 | FUSED PYRIMIDINES AND SUBSTITUTED QUINAZOLINES AS INHIBITORS OF P97 - A group of fused two ring pyrimidine compounds having a heterocycles substituent at the 2 position and a substituted amine at the 4 position as well as optional aliphatic, functional and/or aromatic components substituted at other positions of the pyrimidine and other ring are disclosed. In addition a group of quinazoline compounds having similar substituents at the 2 and 4 positions as well as at other positions are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity. | 01-23-2014 |
20140024662 | COMPOUNDS, SCREENS, AND METHODS OF TREATMENT - The present invention features compounds of Formula (I), pharmaceutical compositions, methods of synthesis, and methods for treating diseases and conditions associate with cellular necrosis. Screening assays for identifying compounds useful for treating these conditions are also described. | 01-23-2014 |
20140045865 | 2-AMINO-4-ARYLTHIAZOLE COMPOUNDS AS TRPA1 ANTAGONISTS - The present invention is related to 2-amino-4-arylthiazole derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. | 02-13-2014 |
20140206703 | THIENO [2, 3-D] PYRIMIDINE DERIVATIVES AND THEIR USE TO TREAT ARRHYTHMIA - The present invention relates to thienopyrimidine compounds which are potassium channel inhibitors. Pharmaceutical compositions comprising the compounds and their use in the treatment of arrhythmia are also described. | 07-24-2014 |
20140235655 | CRYSTAL OF THIENOPYRIMIDINE DERIVATIVE - The invention provides a crystal of 2-(3,4-dichlorobenzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylic acid (which has the chemical structure shown below) and a mixed crystal comprising such a crystal. | 08-21-2014 |
20140323503 | INHIBITORS OF PHOSPODIESTERASES 11 (PDE11) AND METHODS OF USE TO ELEVATE CORTISOL PRODUCTION - The present intervention generally relates to compositions comprising a PDE11 inhibitor for increasing cortisol levels in a subject, or for increasing the production of cortisol from adenocortical cells in a subject. Aspects of the invention relate to the use of a PDE11 inhibitor in a method of treatment of low cortisol levels and/or adrenal insufficiency in a subject, or a method of treating a disease or disorders associated with adrenal insufficiency. Aspects of the invention relate to PDE11 inhibitors belonging to compounds of formula (I)-(VI), and their use alone or in combination with long-term corticosteroid treatment to elevate cortisol levels in a subject, and/or to treat adrenal insufficiency. Another aspect relates to kits comprising PDE11 inhibitors for administration to a subject, pharmaceutical compositions comprising compounds of formula (I)-(VI) for use in methods to increase cortisol levels and/or treat adrenal insufficiency, and their use as an adjuvant for treatment of cancer or other disorders such as psychiatric diseases where elevating cortisol levels would be beneficial to the subject. | 10-30-2014 |
20140350033 | ANT-LIGANDS MOLECULES AND BIOLOGICAL APPLICATIONS - ANT-ligands having a substituted nitrogeneous heterocycle A wherein
| 11-27-2014 |
20140350034 | Aminopyridine derivatives as plasma kallikrein inhibitors - The invention relates to compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it. | 11-27-2014 |
20140350035 | COMBINATIONS OF MEDICAMENTS, CONTAINING PDE4-INHIBITORS AND EP4-RECEPTOR- ANTAGONISTS - The present invention relates to new medicament combinations which contain in addition to one or more PDE4-inhibitors ( | 11-27-2014 |
20140364445 | PHARMACEUTICAL COMPOSITION COMPRISING A TRPA1 ANTAGONIST AND AN ANTICHOLINERGIC AGENT - The present invention relates to a pharmaceutical composition comprising a transient receptor potential ankyrin-1 receptor (“TRPA1”) antagonist and an anticholinergic agent. Particularly, the present invention provides a pharmaceutical composition comprising a TRPA1 antagonist having IC | 12-11-2014 |
20140378477 | MCT PROTEIN INHIBITOR-RELATED PROGNOSTIC AND THERAPEUTIC METHODS - This invention provides a method of identifying one or more subgroups of cancer patients that are likely to benefit from treatment with a monocarboxylate transporter (MCT) protein inhibitor comprising: (a) obtaining a sample of a cancer/tumor tissue from each of said cancer patients; (b) determining the expression level of stromal MCT4 protein in each of said samples of cancer/tumor tissue to obtain a first dataset; and (c) using the expression level of the stromal MCT4 protein from said first dataset to classify each of said sets of one or more cancer patients as stromal MCT4-positive or stromal MCT4-negative, wherein the cancer patients classified as stromal MCT4-positive are patients that are more likely to benefit from treatment with said MCT protein inhibitor. This invention also provides related methods for treating a cancer/tumor whose stromal component expresses the MCT4 protein in a patient. | 12-25-2014 |
20150011567 | PHOSPHORYLATION OF HISTONES AND USES THEREOF - Phosphorylation of histones was observed at certain tyrosine residues which have not been associated with epigenetic modification. These sites include H2B Tyr37, H4 Tyr88 and Tyr 51 and H3 Tyr99. Kinases responsible for the phosphorylation as well as downstream genes regulated by such phosphorylation were also identified. Antibodies that are specific to such phosphorylated histones have been generated, which are useful for detecting the phosphorylation and related events. With such findings, the present disclosure provides compositions and methods for disease diagnosis, prognosis and therapy selection, in particular for cancer, obesity and diabetes. | 01-08-2015 |
20150031709 | Heteroaryl Compounds and Methods of Use Thereof - Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia. | 01-29-2015 |
20150045376 | NOVEL PIPERIDINO-DIHYDROTHIENOPYRIMIDINE SULFOXIDES AND THEIR USE FOR TREATING COPD AND ASTHMA - Piperidino-dihydrothienopyrimidine sulfoxides of formula I | 02-12-2015 |
20150045377 | PHARMACEUTICAL COMPOUNDS - The present invention relates to compounds that are useful as inhibitors of the activity of one or more isoforms of the serine/threonine kinase, AKT. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in the treatment of cancer and methods of treating cancer. | 02-12-2015 |
20150057295 | New 6-Alkynyl Pyridine - This invention relates to 6-alkynyl-pyridine of general formula (I) | 02-26-2015 |
20150072998 | COMPOSITIONS AND METHODS OF MODULATING 15-PGDH ACTIVITY - Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein. | 03-12-2015 |
20150080416 | Thieno[2,3-d]Pyrimidine Derivatives, Preparation Method and Use Thereof - This invention provides thieno[2,3-d]pyrimidine derivatives containing isoxazole heterocycle represented by formula (I), or pharmaceutically acceptable salts thereof | 03-19-2015 |
20150105406 | PHARMACEUTICAL COMPOSITION COMPRISING A TRPA1 ANTAGONIST AND AN ANALGESIC AGENT - The present patent application relates to a pharmaceutical composition comprising a TRPA1 antagonist and an analgesic agent. Particularly, the present patent application provides a pharmaceutical composition comprising a thienopyrimidinedione compound as a TRPA1 antagonist and an analgesic agent; and use of such composition for treating pain in a subject. | 04-16-2015 |
20150105407 | Substituted Pyrrolo, -Furano, and Cyclopentylpyrimidines Having Antimitotic and/or Antitumor Activity and Methods of Use Thereof - The present invention provides substituted pyrrolo-, furano-, and cyclopentylpyrimidine bicyclic compounds of Formula III, | 04-16-2015 |
20150329502 | COMPOUNDS AS LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS - Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases. | 11-19-2015 |
20150329556 | SUBSTITUTED 2- AMIDOQUINAZOL-4-ONES AS MATRIX METALLOPROTEINASE-13 INHIBITORS - The present invention provides a novel amide derivative having a matrix metalloproteinase inhibitory activity, and useful as a pharmaceutical agent, which is a compound represented by the formula (I) wherein ring A is an optionally substituted, nitrogen containing heterocycle, ring B is an optionally substituted monocyclic homocycle or an optionally substituted monocyclic heterocycle, Z is N or NR | 11-19-2015 |
20150342953 | Thienopyrimidine Compounds - Compounds of formula (I) are A | 12-03-2015 |
20150344496 | NOVEL SUBSTITUTED CONDENSED PYRIMIDINE COMPOUNDS - The invention relates to novel substituted condensed pyrimidine compounds of general formula (I) | 12-03-2015 |
20150361094 | BICYCLIC HETEROARYLAMINOALKYL PHENYL DERIVATIVES AS PI3K INHIBITORS - This application relates to derivatives of Formula I: | 12-17-2015 |
20160009731 | Bicyclic and Tricyclic Pyrimidine Tyrosine Kinase Inhibitors with Antitubulin Activity and Methods of Treating a Patient | 01-14-2016 |
20160031852 | VMAT INHIBITORY COMPOUNDS - Disclosed herein are compounds that bind to the vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions comprising those compounds, and methods of treatment using said compounds and pharmaceutical compositions. | 02-04-2016 |
20160039839 | Tricyclic Proteasome Activity Enhancing Compounds - Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies. | 02-11-2016 |
20160039841 | THIENO- AND FURO[2,3-d]PYRIMIDINE-2,4[1H,3H]-DIONE DERIVATIVES - This invention relates to novel Thieno- and Furo[2,3-d]pyrimidine-2,4[1H,3H]-dione derivatives of formula I | 02-11-2016 |
20160082010 | SALT OF FUSED HETEROCYCLIC DERIVATIVE AND CRYSTAL THEREOF - An objective of the present invention is to improve the solubility of 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid. | 03-24-2016 |
20160108060 | ACC INHIBITORS AND USES THEREOF - The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same. | 04-21-2016 |
20160168164 | THIENO[3,2-d]PYRIMIDINES DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS | 06-16-2016 |
20160176891 | Conformationally Restricted 4-Substituted-2,6-dimethylfuro[2,3-d]pyrimidines as Multi-targeted Receptor Tyrosine Kinase Inhibitors and Microtubule Targeting Antitumor Agents | 06-23-2016 |
20160176899 | CO-CRYSTALS OF 5-AMINO-2-OXOTHIAZOLO[4,5-D]PYRIMIDIN-3(2H)-YL-5-HYDROXYMETHYL TETRAHYDROFURAN-3-YL ACETATE AND METHODS FOR PREPARING AND USING THE SAME | 06-23-2016 |