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1. 发明申请

WO2012061428A3 NICOTINAMIDES AS JAK KINASE MODULATORS 审中-公开
标题翻译： NICOTINAMIDES作为JAK激酶调节剂
公开(公告)号：WO2012061428A3
公开(公告)日：2012-10-11
申请号：PCT/US2011058838
申请日：2011-11-01
申请人： PORTOLA PHARM INC , BAUER SHAWN M , SONG YONGHONG , XU QING , ROSE JACK W , JIA ZHAOZHONG J , KANE BRIAN , HUANG WOLIN , PANDEY ANJALI , MEHROTRA MUKUND
发明人： BAUER SHAWN M , SONG YONGHONG , XU QING , ROSE JACK W , JIA ZHAOZHONG J , KANE BRIAN , HUANG WOLIN , PANDEY ANJALI , MEHROTRA MUKUND
IPC分类号： C07D213/82 , A61K31/455 , A61P35/00 , C07D401/04 , C07D401/12 , C07D405/12 , C07D405/14 , C07D417/12 , C07D417/14 , C07D471/04
CPC分类号： C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： 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 ofinhibition 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.
摘要翻译：本发明涉及作为JAK激酶抑制剂的式I化合物及其药学上可接受的盐，酯和前药。本发明还涉及用于制备这种化合物的中间体，这种化合物的制备，含有这种化合物的药物组合物，抑制JAK激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗多种至少部分由JAK激酶活性介导的病症，例如不期望的血栓形成和非霍奇金淋巴瘤。

2. 发明申请

WO2005032488A2 2,4-DIOXO-3-QUINAZOLINYLARYL SULFONYLUREAS 审中-公开
标题翻译： 2,4-DIOXO-3-QuINAZOLINYLARYL SULFONYLUREAS
公开(公告)号：WO2005032488A2
公开(公告)日：2005-04-14
申请号：PCT/US2004/032921
申请日：2004-09-29
申请人： PORTOLA PHARMACEUTICALS, INC. , SCARBOROUGH, Robert, M. , HUANG, Wolin , PANDEY, Anjali , BAUER, Shawn, M. , ZHANG, Xiaoming , JIA, Zhaozhong, J.
发明人： SCARBOROUGH, Robert, M. , HUANG, Wolin , PANDEY, Anjali , BAUER, Shawn, M. , ZHANG, Xiaoming , JIA, Zhaozhong, J.
IPC分类号： A61K
CPC分类号： C07D409/12 , C07D409/14
摘要： 2,4-Dioxo-3-quinazolinylaryl sulfonylurea compounds are provided that are useful for the inhibition of ADP-platelet aggregation, particularly in the treatment of thrombosis and thrombosis related conditions or disorders.
摘要翻译：提供2,4-二氧代-3-喹唑啉基芳基磺酰脲化合物，其可用于抑制ADP-血小板聚集，特别是在治疗血栓形成和血栓形成相关病症或病症中。

3. 发明申请

WO9924075A3 AFFINITY MARKERS FOR HUMAN SERUM ALBUMIN 审中-公开
标题翻译：人类血清白蛋白的亲和标记
公开(公告)号：WO9924075A3
公开(公告)日：1999-09-02
申请号：PCT/US9823705
申请日：1998-11-06
申请人： CONJUCHEM INC , KRANTZ ALEXANDER , HUANG WOLIN , HANEL ARTHUR M , HOLMES DARREN L , BRIDON DOMINIQUE P
发明人： KRANTZ ALEXANDER , HUANG WOLIN , HANEL ARTHUR M , HOLMES DARREN L , BRIDON DOMINIQUE P
IPC分类号： A61K38/00 , A61K47/48 , A61K49/00 , C07K14/665 , G01N33/68
CPC分类号： A61K49/0021 , A61K38/00 , A61K47/62 , A61K47/6901 , A61K49/0043 , A61K49/0056 , C07K14/665
摘要： Methods and compositions are provided for identifying compounds having affinity or complementarity to a target molecule. Compounds according to the invention may be described by the formula E-Ca-R-Cb-A, wherein E is a therapeutic or diagnostic agent, R is a reactive group, Ca and Cb are connector groups between E and R and between R and A, respectively, and A is a group having an affinity for human serum albumin, wherein affinity group A comprises a sequence of amino acid residues -O1-O2-X1-X2-B in which the amino acid residues are independently selected from the group of all twenty naturally occurring amino acids. Compounds according to the invention may be used for labeling the target molecule, particularly where the target molecule is naturally found in a complex mixture, such as a physiological fluid, like blood. By affinity labeling in vivo, the lifetime of physiologically active entities can be greatly enhanced by becoming bound to long-lived blood components. The covalently bound entity may also serve as an antagonist or agonist of a particular binding protein or as an enzyme inhibitor.
摘要翻译：提供了用于鉴定具有与靶分子具有亲和力或互补性的化合物的方法和组合物。根据本发明的化合物可以由式E-Ca-R-Cb-A描述，其中E是治疗或诊断剂，R是反应性基团，Ca和Cb是E和R之间的连接基团，R和 A，A是对人血清白蛋白具有亲和性的基团，其中亲和基团A包含氨基酸残基-O1-O2-X1-X2-B的序列，其中氨基酸残基独立地选自的二十种天然存在的氨基酸。根据本发明的化合物可用于标记靶分子，特别是当目标分子天然存在于复杂混合物如生理液体如血液中时。通过在体内的亲和标记，生理活性物质的寿命可以通过与长寿命的血液成分结合而大大提高。共价结合的实体还可以用作特异性结合蛋白的拮抗剂或激动剂或作为酶抑制剂。

4. 发明申请

WO2008137809A2 [4-(6-FLUORO-7-METHYLAMINO-2,4-DIOXO-1,4-DIHYDRO-2H-QUINAZOLIN-3-YL)-PHENYL]-5-CHLORO-THIOPHEN-2-YL-SULFONYLUREA SALTS, FORMS AND METHODS RELATED THERETO 审中-公开
标题翻译： [4-（6-氟-7-甲基氨基-2,4-二氧代-1,4-二氢-2H-喹喔啉-3-基） - 苯基] -5-氯代噻吩-2-基] - 噻唑鎓盐，形式及其相关方法
公开(公告)号：WO2008137809A2
公开(公告)日：2008-11-13
申请号：PCT/US2008/062584
申请日：2008-05-02
申请人： PORTOLA PHARMACEUTICALS, INC. , SHARP, Emma , QUEGAN, Loisa Jane , PANDEY, Anjali , WANG, Juan , NIEDER, Matthew , HUANG, Wolin
发明人： SHARP, Emma , QUEGAN, Loisa Jane , PANDEY, Anjali , WANG, Juan , NIEDER, Matthew , HUANG, Wolin
IPC分类号： C07D409/12
CPC分类号： C07D409/12
摘要： The present invention provides novel sulfonylurea salts of a salt of formula (I) and polymorph forms thereof. The compounds in their various forms are effective platelet ADP receptor inhibitors and may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also provides a method for preparing such compounds and forms and for preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a salt of formula (I) or a pharmaceutically acceptable form thereof.
摘要翻译：本发明提供式（I）的盐的新型磺酰脲盐及其多晶型形式。各种形式的化合物是有效的血小板ADP受体抑制剂，可用于各种药物组合物中，并且特别有效预防和/或治疗心血管疾病，特别是与血栓形成有关的疾病。本发明还提供了一种制备此类化合物和形式并用于预防或治疗哺乳动物血栓形成和血栓形成相关病症的方法，包括施用治疗有效量的式（I）的盐或其药学上可接受的形式的步骤。

5. 发明申请

WO2005032488A3 2,4-DIOXO-3-QUINAZOLINYLARYL SULFONYLUREAS 审中-公开
标题翻译： 2,4-DIOXO-3-喹唑啉基磺酰基脲
公开(公告)号：WO2005032488A3
公开(公告)日：2005-05-12
申请号：PCT/US2004032921
申请日：2004-09-29
申请人： PORTOLA PHARM INC , SCARBOROUGH ROBERT M , HUANG WOLIN , PANDEY ANJALI , BAUER SHAWN M , ZHANG XIAOMING , JIA ZHAOZHONG J
发明人： SCARBOROUGH ROBERT M , HUANG WOLIN , PANDEY ANJALI , BAUER SHAWN M , ZHANG XIAOMING , JIA ZHAOZHONG J
IPC分类号： A61K20060101 , A61K31/517 , A61P7/02 , C07D409/12 , C07D409/14
CPC分类号： C07D409/12 , C07D409/14
摘要： 2,4-Dioxo-3-quinazolinylaryl sulfonylurea compounds are provided that are useful for the inhibition of ADP-platelet aggregation, particularly in the treatment of thrombosis and thrombosis related conditions or disorders.
摘要翻译：提供了2,4-二氧代-3-喹唑啉基芳基磺酰脲化合物，其用于抑制ADP-血小板聚集，特别是在治疗血栓形成和血栓形成相关病症或病症中。

6. 发明申请

WO2012061428A2 NICOTINAMIDES AS JAK KINASE MODULATORS 审中-公开
标题翻译： NICOTINAMIDES作为JAK激酶调节剂
公开(公告)号：WO2012061428A2
公开(公告)日：2012-05-10
申请号：PCT/US2011/058838
申请日：2011-11-01
申请人： PORTOLA PHARMACEUTICALS, INC. , BAUER, Shawn M. , SONG, Yonghong , XU, Qing , ROSE, Jack W. , JIA, Zhaozhong J. , KANE, Brian , HUANG, Wolin , PANDEY, Anjali , MEHROTRA, Mukund
发明人： BAUER, Shawn M. , SONG, Yonghong , XU, Qing , ROSE, Jack W. , JIA, Zhaozhong J. , KANE, Brian , HUANG, Wolin , PANDEY, Anjali , MEHROTRA, Mukund
IPC分类号： C07D213/82 , C07D401/04 , C07D401/12 , C07D405/12 , C07D405/14 , C07D417/12 , C07D417/14 , C07D471/04 , A61K31/455 , A61P35/00
CPC分类号： C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： 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 ofinhibition 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.
摘要翻译：本发明涉及作为JAK激酶抑制剂的式I化合物及其药学上可接受的盐，酯和前药。本发明还涉及用于制备这样的化合物的中间体，制备这样的化合物，含有这种化合物的药物组合物，抑制JAK激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗一些至少部分由JAK激酶活性介导的病症，例如不希望的血栓形成和非何杰金氏淋巴瘤。

7. 发明申请

WO2010054020A1 [4-(6-FLUORO-7-METHYLAMINO-2,4-DIOXO-1,4-DIHYDRO-2H-QUINAZOLIN-3-YL)-PHENYL]-5-CHLORO-THIOPHEN-2-YL-SULFONYLUREA SALTS, FORMS AND METHODS RELATED THERETO 审中-公开
标题翻译： [4-（6-氟-7-甲基氨基-2,4-二氧代-1,4-二氢-2H-喹喔啉-3-基） - 苯基] -5-氯代噻吩-2-基] - 噻唑鎓盐，形式及其相关方法
公开(公告)号：WO2010054020A1
公开(公告)日：2010-05-14
申请号：PCT/US2009/063313
申请日：2009-11-04
申请人： PORTOLA PHARMACEUTICALS, INC. , SHARP, Emma , QUEGAN, Louisa Jane , PANDEY, Anjali , WANG, Juan , NIEDER, Matthew , HUANG, Wolin
发明人： SHARP, Emma , QUEGAN, Louisa Jane , PANDEY, Anjali , WANG, Juan , NIEDER, Matthew , HUANG, Wolin
IPC分类号： C07D409/12 , A61K31/517 , A61P7/02
CPC分类号： C07D409/12
摘要： The present invention provides novel sulfonylurea salts of a salt of formula (I) \ and polymorph forms thereof. The compounds in their various forms are effective platelet ADP receptor inhibitors and may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also provides a method for preparing such compounds and forms and for preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a salt of formula (I) or a pharmaceutically acceptable form thereof.
摘要翻译：本发明提供新的式（I）盐的磺酰脲盐及其多晶型物。各种形式的化合物是有效的血小板ADP受体抑制剂，可用于各种药物组合物中，并且特别有效预防和/或治疗心血管疾病，特别是与血栓形成有关的疾病。本发明还提供了一种制备此类化合物和形式并用于预防或治疗哺乳动物血栓形成和血栓形成相关病症的方法，包括施用治疗有效量的式（I）的盐或其药学上可接受的形式的步骤。

8. 发明申请

WO2007056219A2 [4-(6-HALO-7-SUBSTITUTED-2,4-DIOXO-1,4-DIHYDRO-2H-QUINAZOLIN-3-YL)-PHENYL]-5-CHLORO-THIOPHEN-2-YL-SULFONYLUREAS AND FORMS AND METHODS RELATED THERETO 审中-公开
标题翻译： [4-（6-羟基-7-取代-2,4-二氧代-1,4-二氢-2H-喹唑啉-3-基） - 苯基] -5-氯代 - 噻吩-2-基] - 磺酰基和形式方法相关
公开(公告)号：WO2007056219A2
公开(公告)日：2007-05-18
申请号：PCT/US2006/043093
申请日：2006-11-03
申请人： PORTOLA PHARMACEUTICALS, INC. , SCARBOROUGH, Carroll, Anna, Crew , HUANG, Wolin , MEHROTRA, Mukund , ZHANG, Xiaoming , CANNON, Hilary , GRANT, Craig M.
发明人： HUANG, Wolin , MEHROTRA, Mukund , ZHANG, Xiaoming , CANNON, Hilary , GRANT, Craig M.
IPC分类号： A61K31/517 , C07D409/02
CPC分类号： C07D409/12
摘要： The present invention provides novel sulfonylurea compounds of formula (I) and pharmaceutically acceptable derivatives and polymorph and amorphous forms thereof. The compounds in their various forms are effective platelet ADP receptor inhibitors and may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also provides a method for preparing such compounds and forms and for preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt or forms thereof.
摘要翻译：本发明提供式（I）的新型磺酰脲化合物及其药学上可接受的衍生物及其多晶型物和无定形形式。各种形式的化合物是有效的血小板ADP受体抑制剂，可用于各种药物组合物中，并且特别有效预防和/或治疗心血管疾病，特别是与血栓形成有关的疾病。本发明还提供了一种制备此类化合物和形式并用于预防或治疗哺乳动物血栓形成和血栓形成相关病症的方法，包括施用治疗有效量的式（I）化合物或其药学上可接受的盐或其形式的步骤。

9. 发明申请

WO2012061415A1 OXYPYRIMIDINES AS SYK MODULATORS 审中-公开
标题翻译：氧化亚胺作为SYK调节剂
公开(公告)号：WO2012061415A1
公开(公告)日：2012-05-10
申请号：PCT/US2011/058822
申请日：2011-11-01
申请人： PORTOLA PHARMACEUTICALS, INC. , PANDEY, Anjali , XU, Qing , HUANG, Wolin , JIA, Zhaozhong J. , SONG, Yonghong
发明人： PANDEY, Anjali , XU, Qing , HUANG, Wolin , JIA, Zhaozhong J. , SONG, Yonghong
IPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D417/12 , A61K31/505 , A61K31/506 , A61K31/513 , A61P9/00 , A61P29/00 , A61P35/00 , A61P37/00
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D417/12
摘要： 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.
摘要翻译：本发明涉及其抑制Syk激酶的式（I）化合物及其互变异构体或其药学上可接受的盐，酯和前药。本发明还涉及用于制备这些化合物的中间体，这种化合物的制备，含有这种化合物的药物组合物，抑制Syk激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗数字的方法至少部分地由Syk激酶活性介导的病症，例如不期望的血栓形成和非霍奇金淋巴瘤。

10. 发明申请

WO2010129802A1 INHIBITORS OF JAK 审中-公开
标题翻译： JAK的抑制剂
公开(公告)号：WO2010129802A1
公开(公告)日：2010-11-11
申请号：PCT/US2010/033921
申请日：2010-05-06
申请人： PORTOLA PHARMACEUTICALS, INC. , BAUER, Shawn M. , ROSE, Jack W. , SONG, Yonghong , XU, Qing , MEHROTRA, Mukund , HUANG, Wolin , PANDEY, Anjali
发明人： BAUER, Shawn M. , ROSE, Jack W. , SONG, Yonghong , XU, Qing , MEHROTRA, Mukund , HUANG, Wolin , PANDEY, Anjali
IPC分类号： C07D213/82 , C07D239/48 , C07D401/12 , C07D403/12 , C07D403/14 , A61K31/505 , A61P37/00
CPC分类号： C07D417/14 , C07D213/82 , C07D239/48 , C07D401/12 , C07D403/12 , C07D403/14 , C07D417/12
摘要： 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.
摘要翻译：本发明涉及作为JAK的选择性抑制剂的式（I）化合物及其互变异构体及其药学上可接受的盐。本发明还涉及用于制备这种化合物的中间体，这种化合物的制备，含有这种化合物的药物组合物，抑制JAK活性的方法，以及预防或治疗至少部分地由 JAK活动。

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