Patent application number | Description | Published |
20080293704 | FACTOR Xa INHIBITORS - The present invention is directed to compounds represented by Formula (I) or a pharmaceutically acceptable salt, ester, or prodrug thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat certain conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample. | 11-27-2008 |
20090030045 | FACTOR XA INHIBITORS - The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample. | 01-29-2009 |
20090042916 | [4-(6-FLUORO-7-METHYLAMINO-2,4-DIOXO-1,4-DIHYDRO-2H-QUINAZOLIN-3-YL)-PHENY- L]-5-CHLORO-THIOPHEN-2-YL-SULFONYLUREA SALTS, FORMS AND METHODS RELATED THERETO - The present invention provides novel sulfonylurea salts of a salt of formula (I) | 02-12-2009 |
20090048216 | INTRAVENOUS AND ORAL DOSING OF A DIRECT-ACTING AND REVERSIBLE P2Y12 INHIBITOR - The invention provides methods and compositions for rapid and reversible inhibition of platelet aggregation in human subjects in need thereof by administering compounds of the formula: | 02-19-2009 |
20090054425 | PROTEIN KINASE INHIBITORS - Compounds, particularly compounds having spleen tyrosine kinase (Syk) inhibition activity, having the following structure: | 02-26-2009 |
20090156620 | [4-(6-FLUORO-7-METHYLAMINO-2,4-DIOXO-1,4-DIHYDRO-2H-QUINAZOLIN-3-YL)-PHENY- L]-5-CHLORO-THIOPHEN-2-YL-SULFONYLUREA SALTS, FORMS AND METHODS RELATED THERETO - The present invention provides novel sulfonylurea salts of a salt of formula (I) | 06-18-2009 |
20090176780 | NITROGENOUS HETEROCYCLIC COMPOUNDS - The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis. | 07-09-2009 |
20090298823 | Inhibitors of protein kinases - The present invention is directed to compounds of formula I-II and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 12-03-2009 |
20090318407 | Inhibitors of protein kinases - The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 12-24-2009 |
20100048567 | Inhibitors of syk and JAK protein kinases - The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 02-25-2010 |
20100113468 | QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS - The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis. | 05-06-2010 |
20100240893 | NITROGENOUS HETEROCYCLIC COMPOUNDS AND PROCESS FOR MAKING NITROGENOUS HETEROCYCLIC COMPOUNDS AND INTERMEDIATES THEREOF - The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention further provides a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases comprising administering an effective amount of a compound according to the invention to a patient in need thereof. | 09-23-2010 |
20100249117 | FACTOR XA INHIBITORS - The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample. | 09-30-2010 |
20110005947 | INHIBITORS OF JAK - The present invention is directed to compounds of formula I and tautomers and pharmaceutically acceptable salts thereof which are selective inhibitors of JAK. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK activity, and methods to prevent or treat a number of conditions mediated at least in part by JAK activity. | 01-13-2011 |
20110098247 | Substituted Dihydroquinazolines as Platelet ADP Receptor Inhibitors - Compounds of formula I are provided: | 04-28-2011 |
20110118244 | FACTOR XA INHIBITORS - The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample. | 05-19-2011 |
20110152530 | METHODS OF PREPARING FACTOR XA INHIBITORS AND SALTS THEREOF - The present invention provides for methods of preparing compounds of Formula I or a salt of the compound or a hydrate of the compound or salt thereof that are factor Xa inhibitors. | 06-23-2011 |
20110160196 | FACTOR XA INHIBITORS - The present invention is directed to compounds represented by Formula (I) or a pharmaceutically acceptable salt, ester, or prodrug thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat certain conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample. | 06-30-2011 |
20110160250 | CRYSTALLINE FORMS OF A FACTOR XA INHIBITOR - The present invention provides crystalline forms of a mesylate salt of the compound 5-chloro-N-((1-(4-(2-oxopyridin-1(2H)-yl)phenyl)-1H-imidazol-4-yl)methyl)thiophene-2-carboxamide and pharmaceutical compositions and methods thereof. | 06-30-2011 |
20110178135 | SALTS AND CRYSTALLINE FORMS OF A FACTOR XA INHIBITOR - The present invention provides salts and crystalline forms of the compound 5-chloro-N-((1-(4-(2-oxopyridin-1(2H)-yl)phenyl)-1H-imidazol-4-yl)methyl)thiophene-2-carboxamide, and pharmaceutical compositions and method of use thereof. | 07-21-2011 |
20110319627 | METHODS OF SYNTHESIZING FACTOR Xa INHIBITORS - Described herein are novel methods of preparing a compound of Formula II or a pharmaceutically acceptable salt thereof. In some embodiments, the method is for preparing betrixaban or a pharmaceutically acceptable salt thereof. Also described are compositions comprising substantially pure betrixaban free base or salt thereof. | 12-29-2011 |
20120009172 | INTRAVENOUS AND ORAL DOSING OF A DIRECT-ACTING AND REVERSIBLE P2Y12 INHIBITOR - The invention provides methods and compositions for rapid and reversible inhibition of platelet aggregation in human subjects in need thereof by administering compounds of the formula: | 01-12-2012 |
20120071519 | CRYSTALLINE FORMS OF A FACTOR Xa INHIBITOR - Provided herein are crystalline forms of a maleate salt of betrixaban, compositions and methods of preparation or use thereof. | 03-22-2012 |
20120088795 | FACTOR XA INHIBITORS - The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample. | 04-12-2012 |
20120095019 | METHODS AND FORMULATIONS OF TREATING THROMBOSIS WITH BETRIXABAN AND A P-GLYCOPROTEIN INHIBITOR - This invention is directed to methods of inhibiting coagulation or treating thrombosis using a factor Xa inhibitor and a P-glycoprotein (Pgp) inhibitor. The invention is also directed to formulations used in the methods. | 04-19-2012 |
20120101275 | INHIBITORS OF SYK AND JAK PROTEIN KINASES - The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 04-26-2012 |
20120108566 | NICOTINAMIDES AS JAK KINASE MODULATORS - The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 05-03-2012 |
20120129867 | INHIBITORS OF PROTEIN KINASES - The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 05-24-2012 |
20120129876 | [4-(6-FLUORO-7-METHYLAMINO-2,4-DIOXO-1,4-DIHYDRO-2H-QUINAZOLIN-3-YL)-PHENY- L]-5-CHLORO-THIOPHEN-2-YL-SULFONYLUREA SALTS, FORMS AND METHODS RELATED THERETO - The present invention provides novel sulfonylurea salts of a salt of formula (I) | 05-24-2012 |
20120130073 | INHIBITORS OF SYK AND JAK PROTEIN KINASES - The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 05-24-2012 |
20120142671 | BENZAMIDES AND NICOTINAMIDES AS SYK MODULATORS - The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma. | 06-07-2012 |
20130029944 | INHIBITORS OF PROTEIN KINASES - The present invention is directed to compounds of formula I-II and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 01-31-2013 |
20130131040 | PYRAZINE KINASE INHIBITORS - Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity. | 05-23-2013 |
20130137673 | INHIBITORS OF JAK - The present invention is directed to compounds of formula I and tautomers and pharmaceutically acceptable salts thereof which are selective inhibitors of JAK. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK activity, and methods to prevent or treat a number of conditions mediated at least in part by JAK activity. | 05-30-2013 |
20130165431 | INHIBITORS OF SYK AND JAK PROTEIN KINASES - The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 06-27-2013 |
20130211094 | METHODS OF SYNTHESIZING FACTOR Xa INHIBITORS - Described herein are novel methods of preparing a compound of Formula II or a pharmaceutically acceptable salt thereof. In some embodiments, the method is for preparing betrixaban or a pharmaceutically acceptable salt thereof. Also described are compositions comprising substantially pure betrixaban free base or salt thereof. | 08-15-2013 |
20130237493 | COMBINATION THERAPY OF 4-(CYCLOPROPYLAMINO)-2-(4-(4-(ETHYLSULFONYL)PIPERAZIN-1-YL)PHENYLAMINO)PY- RIMIDINE-5-CARBOXAMIDE AND FLUDARABINE - The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing 4-(cyclopropylamino)-2-(4-(4-(ethylsulfonyl)piperazin-1-yl)phenylamino)pyrimidine-5-carboxamide, or a pharmaceutically acceptable salt thereof, and fludarabine for the treatment of cell proliferative disorders, such as undesired acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL), non-Hodgkin lymphoma (NHL), including diffuse large B cell lymphoma (DLBCL); mantle cell lymphoma, acute lymphocytic leukemia (ALL), follicular lymphoma, Burkitt's lymphoma, small Lymphocytic Lymphoma (SLL) and multiple myeloma. | 09-12-2013 |
20130244963 | COMBINATION THERAPY WITH 4-(3-(2H-1,2,3-TRIAZOL-2-YL)PHENYLAMINO)-2-((1R,2S)-2-AMINOCYCLOHEXYLAMIN- O)PYRIMIDINE-5-CARBOXAMIDE - The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing a SYK inhibitor, or a pharmaceutically acceptable salt thereof, and a antineoplastic or antiinflammatory agent for the treatment of inflammatory, autoimmune and cell proliferative diseases, such as allergic reaction, transplant rejection, rheumatoid arthritis (RA), lupus, multiple sclerosis (MS) or psoriasis undesired acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL), non-Hodgkin lymphoma (NHL) (including diffuse large B cell lymphoma (DLBCL)), mantle cell lymphoma, acute lymphocytic leukemia (ALL), follicular lymphoma, Burkitt's lymphoma, small Lymphocytic (SLL), Lymphoma, multiple myeloma, asthma, vasculitis, Idiopathic thrombocytopenic purpura (ITP), Heparin Induced Thrombocytopenia (HIT) and hemolytic anemia. | 09-19-2013 |
20130252917 | COMBINATION THERAPY OF 4-(3-(2H-1,2,3-TRIAZO-2-YL)PHENYLAMINO)-2-((1R,2S)-2-AMINOCYCLOHEXYLAMINO- )PYRIMIDINE-5-CARBOXAMIDE AND FLUDARABINE - The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing 4-(3-(2H-1,2,3-triazol-2-yl)phenylamino)-2-(1R,2S)-2-aminocyclohexylamino)pyrimidine-5-carboxamide, or a pharmaceutically acceptable salt thereof, and fludarabine for the treatment of cell proliferative disorders, such as undesired acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL), non-Hodgkin lymphoma (NHL), including diffuse large B cell lymphoma (DLBCL); mantle cell lymphoma, acute lymphocytic leukemia (ALL), follicular lymphoma, Burkitt's lymphoma, small Lymphocytic Lymphoma (SLL) and multiple myeloma. | 09-26-2013 |
20130274252 | QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS - The Present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis. | 10-17-2013 |
20130317029 | OXYPYRIMIDINES AS SYK MODULATORS - The present invention is directed to compounds of formula (I) and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which arc inhibitor of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 11-28-2013 |
20130345191 | 1,2,4-TRIAZINE-6-CARBOXAMIDE KINASE INHIBITORS - Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity. | 12-26-2013 |
20140031361 | INHIBITORS OF PROTEIN KINASES - The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 01-30-2014 |
20140113931 | SUBSTITUTED PICOLINAMIDE KINASE INHIBITORS - Provided are picolinamide compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity. | 04-24-2014 |
20140186923 | COMPOUNDS AND METHODS FOR PURIFICATION OF SERINE PROTEASES - Disclosed herein are compounds, compositions, methods and kits for purifying a serine protease and serine proteases purified with the compounds, compositions and methods. | 07-03-2014 |
20140309209 | Pyrazine Kinase Inhibitors - Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity. | 10-16-2014 |
20140323418 | SELECTIVE KINASE INHIBITORS - Provided are pyrimidine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity. | 10-30-2014 |
20140323497 | METHODS AND FORMULATIONS OF TREATING THROMBOSIS WITH BETRIXABAN AND A P-GLYCOPROTEIN INHIBITOR - This invention is directed to methods of inhibiting coagulation or treating thrombosis using a factor Xa inhibitor and a P-glycoprotein (Pgp) inhibitor. The invention is also directed to formulations used in the methods. | 10-30-2014 |
20140346397 | COMPOUNDS AND METHODS FOR PURIFICATION OF SERINE PROTEASES - Disclosed herein are compounds, compositions, methods and kits for purifying a serine protease and serine proteases purified with the compounds, compositions and methods. | 11-27-2014 |
20150038492 | BENZAMIDES AND NICOTINAMIDES AS SYK MODULATORS - The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma. | 02-05-2015 |