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21. 发明授权

US08501944B2 Inhibitors of protein kinases 有权
标题翻译：蛋白激酶抑制剂
公开(公告)号：US08501944B2
公开(公告)日：2013-08-06
申请号：US13360862
申请日：2012-01-30
申请人： Shawn M. Bauer , Zhaozhong J. Jia , Mukund Mehrotra , Yonghong Song , Qing Xu , Wolin Huang , Chandrasekar Venkataramani , Jack W. Rose , Anjali Pandey
发明人： Shawn M. Bauer , Zhaozhong J. Jia , Mukund Mehrotra , Yonghong Song , Qing Xu , Wolin Huang , Chandrasekar Venkataramani , Jack W. Rose , Anjali Pandey
IPC分类号： C07D239/02 , A61K31/497
CPC分类号： C07D417/12 , A61K31/4985 , A61K31/505 , A61K31/506 , A61K31/5355 , A61K31/5377 , A61K31/551 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/12 , C07D413/14
摘要： The present invention is directed to a compound of the formula: and pharmaceutically acceptable tautomers, or salts thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to pharmaceutical compositions containing such a compound.
摘要翻译：本发明涉及下式的化合物及其药学上可接受的互变异构体或其盐，它们是syk和/或JAK激酶的抑制剂。本发明还涉及含有这种化合物的药物组合物。

22. 发明申请

US20120130073A1 INHIBITORS OF SYK AND JAK PROTEIN KINASES 有权
公开(公告)号：US20120130073A1
公开(公告)日：2012-05-24
申请号：US13269523
申请日：2011-10-07
申请人： Zhaozhong Jia , Chandrasekar Venkataramani , Wolin Huang , Mukund Mehrotra , Yonghong Song , Qing Xu , Shawn M. Bauer , Jack W. Rose , Brian Kane , Anjali Pandey
发明人： Zhaozhong Jia , Chandrasekar Venkataramani , Wolin Huang , Mukund Mehrotra , Yonghong Song , Qing Xu , Shawn M. Bauer , Jack W. Rose , Brian Kane , Anjali Pandey
IPC分类号： C07D403/12
CPC分类号： A61K31/506 , C07D239/48 , C07D401/12 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要： 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.

23. 发明申请

US20120129867A1 INHIBITORS OF PROTEIN KINASES 有权
标题翻译：蛋白激酶抑制剂
公开(公告)号：US20120129867A1
公开(公告)日：2012-05-24
申请号：US13360862
申请日：2012-01-30
申请人： Shawn M. Bauer , Zhaozhong J. Jia , Yonghong Song , Qing Xu , Mukund Mehrotra , Jack W. Rose , Wolin Huang , Chandrasekar Venkataramani , Anjali Pandey
发明人： Shawn M. Bauer , Zhaozhong J. Jia , Yonghong Song , Qing Xu , Mukund Mehrotra , Jack W. Rose , Wolin Huang , Chandrasekar Venkataramani , Anjali Pandey
IPC分类号： A61K31/506 , C12N9/99 , A61P9/00 , A61P9/10 , A61P37/08 , A61P37/06 , A61P29/00 , A61P17/06 , A61P13/12 , A61P35/00 , A61P7/06 , C07D403/12 , A61P11/06
CPC分类号： C07D417/12 , A61K31/4985 , A61K31/505 , A61K31/506 , A61K31/5355 , A61K31/5377 , A61K31/551 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/12 , C07D413/14
摘要： 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.
摘要翻译：本发明涉及式I-II化合物及其药学上可接受的互变异构体，其盐或其立体异构体，其是syk和/或JAK激酶的抑制剂。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，抑制性syk和/或JAK激酶活性的方法，抑制血小板聚集的方法以及预防方法或治疗至少部分通过syk和/或JAK激酶活性介导的许多病症，例如不期望的血栓形成和非霍奇金淋巴瘤。

24. 发明授权

US08138339B2 Inhibitors of protein kinases 有权
标题翻译：蛋白激酶抑制剂
公开(公告)号：US08138339B2
公开(公告)日：2012-03-20
申请号：US12386509
申请日：2009-04-16
申请人： Shawn M. Bauer , Zhaozhong J. Jia , Yonghong Song , Qing Xu , Mukund Mehrotra , Jack W. Rose , Wolin Huang , Chandrasekar Venkataramani , Anjali Pandey
发明人： Shawn M. Bauer , Zhaozhong J. Jia , Yonghong Song , Qing Xu , Mukund Mehrotra , Jack W. Rose , Wolin Huang , Chandrasekar Venkataramani , Anjali Pandey
IPC分类号： C07D239/28 , C07D403/02 , C07D413/02 , C07D279/12 , A61K31/506 , A61K31/501 , A61K31/5377 , A61K31/551 , A61K31/541
CPC分类号： C07D417/12 , A61K31/4985 , A61K31/505 , A61K31/506 , A61K31/5355 , A61K31/5377 , A61K31/551 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/12 , C07D413/14
摘要： The present invention is directed to 2-cycloalkylamino-4-arylamino-benzamide compounds of formula I pharmaceutically acceptable salts 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, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as cardiovascular disease, inflammatory disease, autoimmune disease and cell proliferative disorder.
摘要翻译：本发明涉及作为syk和/或JAK激酶抑制剂的式I的药学上可接受的盐的2-环烷基氨基-4-芳基氨基 - 苯甲酰胺化合物。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，抑制性syk和/或JAK激酶活性的方法，以及预防或治疗多种病症介导的方法至少部分地由syk和/或JAK激酶活性，例如心血管疾病，炎性疾病，自身免疫疾病和细胞增殖性疾病。

25. 发明申请

US20100234350A1 PLATELET ADP RECEPTOR INHIBITORS 有权
标题翻译： PLATELET ADP受体抑制剂
公开(公告)号：US20100234350A1
公开(公告)日：2010-09-16
申请号：US12559389
申请日：2009-09-14
申请人： Robert M. Scarborough , Wolin Huang , Charles K. Marlowe , Kim A. Kane-McGuire , Hans-Michael Jantzen , David M. Sedlock
发明人： Robert M. Scarborough , Wolin Huang , Charles K. Marlowe , Kim A. Kane-McGuire , Hans-Michael Jantzen , David M. Sedlock
IPC分类号： A61K31/55 , C07D209/44 , A61K31/4035 , C07D401/04 , A61K31/4439 , C07D239/02 , A61K31/505 , C07D277/20 , A61K31/426 , C07D243/24 , A61K31/5513 , C07D223/14 , C07D239/72 , A61K31/517 , C07D215/00 , A61K31/47 , C07D413/14 , A61K31/5377 , C07D471/02 , A61K31/437 , C07D513/02 , C07D285/18 , A61K31/542 , C07D237/26 , A61K31/502 , C07D333/34 , A61K31/381 , A61P9/00 , A61P9/10 , A61P7/02
CPC分类号： C07D487/04 , C07D209/48 , C07D239/22 , C07D239/48 , C07D239/50 , C07D239/96 , C07D333/34 , C07D333/62 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D495/04 , C07D521/00
摘要： Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives 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 relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
摘要翻译：式（I）至（VIII）的新型化合物，其更具体地包括作为有效的血小板ADP受体抑制剂的磺酰脲衍生物，磺酰基硫脲衍生物，磺酰基胍衍生物，磺酰氰基胍衍生物，硫代酰基磺酰胺衍生物和酰基磺酰胺衍生物。这些衍生物可用于各种药物组合物中，并且对于预防和/或治疗心血管疾病，特别是与血栓形成有关的疾病特别有效。本发明还涉及一种用于预防或治疗哺乳动物血栓形成的方法，包括施用治疗有效量的式（I）至（VIII）化合物或其药学上可接受的盐的步骤。

26. 发明申请

US20080194597A1 PLATELET ADP RECEPTOR INHIBITORS 有权
标题翻译： PLATELET ADP受体抑制剂
公开(公告)号：US20080194597A1
公开(公告)日：2008-08-14
申请号：US11841711
申请日：2007-08-20
申请人： ROBERT M. SCARBOROUGH , Wolin Huang , Charles K. Marlowe , Kim A. Kane-Maguire
发明人： ROBERT M. SCARBOROUGH , Wolin Huang , Charles K. Marlowe , Kim A. Kane-Maguire
IPC分类号： A61K31/517 , C07D333/34 , A61K31/381 , A61P9/00 , C07D403/12
CPC分类号： C07D487/04 , C07D209/48 , C07D239/22 , C07D239/48 , C07D239/50 , C07D239/96 , C07D333/34 , C07D333/62 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D495/04 , C07D521/00
摘要： Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives 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 relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
摘要翻译：式（I）至（VIII）的新型化合物，其更具体地包括作为有效的血小板ADP受体抑制剂的磺酰脲衍生物，磺酰基硫脲衍生物，磺酰基胍衍生物，磺酰氰基胍衍生物，硫代酰基磺酰胺衍生物和酰基磺酰胺衍生物。这些衍生物可用于各种药物组合物中，并且对于预防和/或治疗心血管疾病，特别是与血栓形成有关的疾病特别有效。本发明还涉及一种用于预防或治疗哺乳动物血栓形成的方法，包括施用治疗有效量的式（I）至（VIII）化合物或其药学上可接受的盐的步骤。

27. 发明授权

US07056926B2 Platelet ADP receptor inhibitors 有权
公开(公告)号：US07056926B2
公开(公告)日：2006-06-06
申请号：US10941053
申请日：2004-09-13
申请人： Robert M. Scarborough , Wolin Huang , Charles K. Marlowe , Kim A. Kane-Maguire
发明人： Robert M. Scarborough , Wolin Huang , Charles K. Marlowe , Kim A. Kane-Maguire
IPC分类号： C07D409/12 , A61K31/517 , A61P7/02
CPC分类号： C07D487/04 , C07D209/48 , C07D239/22 , C07D239/48 , C07D239/50 , C07D239/96 , C07D333/34 , C07D333/62 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D495/04 , C07D521/00
摘要： Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives 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 relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.

28. 发明申请

US20050037974A1 Affinity markers for human serum albumin 失效
标题翻译：人血清白蛋白的亲和标记
公开(公告)号：US20050037974A1
公开(公告)日：2005-02-17
申请号：US10934841
申请日：2004-09-02
申请人： Alexander Krantz , Wolin Huang , Arthur Hanel , Darren Holmes , Dominique Bridon
发明人： Alexander Krantz , Wolin Huang , Arthur Hanel , Darren Holmes , Dominique Bridon
IPC分类号： A61K38/00 , A61K47/48 , A61K49/00 , C07K14/665 , A61K38/08 , C07K7/06
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以用于标记靶分子，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。通过体内亲和标记，生理活性实体的寿命可以通过与长寿命的血液成分结合而大大增强。共价结合的实体也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。

29. 发明授权

US06403324B1 Affinity labeling libraries with tagged leaving group 失效
标题翻译：具有标记离去基团的亲和标记库
公开(公告)号：US06403324B1
公开(公告)日：2002-06-11
申请号：US09042234
申请日：1998-03-13
申请人： Alexander Krantz , Arthur M. Hanel , Wolin Huang
发明人： Alexander Krantz , Arthur M. Hanel , Wolin Huang
IPC分类号： G01N3353
CPC分类号： C40B30/04 , B01J2219/00592 , G01N33/6845
摘要： Methods and compositions are provided for identifying compounds having affinity to a target site. The method provides for the affinity group to be a leaving group from a reactive functionality capable of forming a covalent bond to the target site. One can combine the compound comprising the target site with the library, and assay for the resulting composition of the leaving groups. The leaving groups having the highest concentration can be identified as the groups having the binding highest affinity for the target site. The selected compounds may then 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 proteins or as an enzyme inhibitor.
摘要翻译：提供方法和组合物用于鉴定对靶位点具有亲和性的化合物。该方法提供了亲和基团为能够与靶位点形成共价键的反应性官能团的离去基团。可以将包含靶位点的化合物与文库结合，并测定所得离去基团的组成。具有最高浓度的离去基团可以被鉴定为对靶位点具有最高亲和力的结合基团。然后可以将所选择的化合物用于标记靶分子，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。通过体内的亲和标记，通过与长寿命血液成分结合，可以大大提高生理活性物质的寿命。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。

30. 发明授权

US08318755B2 Inhibitors of SYK and JAK protein kinases 有权
标题翻译： SYK和JAK蛋白激酶抑制剂
公开(公告)号：US08318755B2
公开(公告)日：2012-11-27
申请号：US13269523
申请日：2011-10-07
申请人： Zhaozhong J. Jia , Chandrasekar Venkataramani , Wolin Huang , Mukund Mehrotra , Yonghong Song , Qing Xu , Shawn M. Bauer , Jack W. Rose , Brian Kane , Anjali Pandey
发明人： Zhaozhong J. Jia , Chandrasekar Venkataramani , Wolin Huang , Mukund Mehrotra , Yonghong Song , Qing Xu , Shawn M. Bauer , Jack W. Rose , Brian Kane , Anjali Pandey
IPC分类号： A01N43/54 , A61K31/505 , C07D239/02
CPC分类号： A61K31/506 , C07D239/48 , C07D401/12 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要： 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.
摘要翻译：本发明涉及作为syk激酶抑制剂的式I-V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通过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。

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