公开(公告)号：US08063058B2

公开(公告)日：2011-11-22

申请号：US12386525

申请日：2009-04-16

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 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00

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，酯和前体药物。 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。

公开(公告)号：US08367689B2

公开(公告)日：2013-02-05

申请号：US12775358

申请日：2010-05-06

申请人： Shawn M. Bauer ,  Jack W. Rose ,  Yonghong Song ,  Qing Xu ,  Mukund Mehrotra ,  Wolin Huang ,  Anjali Pandey

发明人： Shawn M. Bauer ,  Jack W. Rose ,  Yonghong Song ,  Qing Xu ,  Mukund Mehrotra ,  Wolin Huang ,  Anjali Pandey

IPC分类号： A01N43/54 ,  A61K31/505

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。

公开(公告)号：US20120101275A1

公开(公告)日：2012-04-26

申请号：US13275253

申请日：2011-10-17

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.

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。

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。

公开(公告)号：US09102625B2

公开(公告)日：2015-08-11

申请号：US13286984

申请日：2011-11-01

申请人： Shawn M. Bauer ,  Yonghong Song ,  Qing Xu ,  Jack W. Rose ,  Zhaozhong J. Jia ,  Brian Kane ,  Wolin Huang ,  Anjali Pandey ,  Mukund Mehrotra

发明人： Shawn M. Bauer ,  Yonghong Song ,  Qing Xu ,  Jack W. Rose ,  Zhaozhong J. Jia ,  Brian Kane ,  Wolin Huang ,  Anjali Pandey ,  Mukund Mehrotra

IPC分类号： C07D213/82 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  A61K31/455 ,  A61P35/00 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

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 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.

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，以及预防或治疗数字的方法 至少部分通过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。

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。

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.

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。

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。

公开(公告)号：US08349860B2

公开(公告)日：2013-01-08

申请号：US13275253

申请日：2011-10-17

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 ,  A01N43/64 ,  A61K31/505 ,  A61K31/41 ,  C07D239/02 ,  C07D403/00 ,  C07D487/00 ,  C07D249/04

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.