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：US20090298823A1

公开(公告)日：2009-12-03

申请号：US12386848

申请日：2009-04-22

申请人： Yonghong Song ,  Qing Xu ,  Shawn M. Bauer ,  Zhaozhong J. Jia ,  Mukund Mehrotra ,  Anjali Pandey

发明人： Yonghong Song ,  Qing Xu ,  Shawn M. Bauer ,  Zhaozhong J. Jia ,  Mukund Mehrotra ,  Anjali Pandey

IPC分类号： A61K31/5377 ,  C07D487/04 ,  C07D239/28 ,  C07D413/14 ,  A61K31/497 ,  A61K31/506 ,  A61P7/02

CPC分类号： C07D471/04 ,  C07D239/48 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D473/16

摘要： 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.

摘要翻译： 本发明涉及式I-II化合物及其药学上可接受的盐，酯和前体药物，它们是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：US20130029944A1

公开(公告)日：2013-01-31

申请号：US13528709

申请日：2012-06-20

申请人： Yonghong Song ,  Qing Xu ,  Shawn M. Bauer ,  Zhaozhong J. Jia ,  Mukund Mehrotra ,  Anjali Pandey

发明人： Yonghong Song ,  Qing Xu ,  Shawn M. Bauer ,  Zhaozhong J. Jia ,  Mukund Mehrotra ,  Anjali Pandey

IPC分类号： C07D471/04 ,  C07D401/04 ,  A61K31/506 ,  C07D403/04 ,  C07D473/16 ,  A61K31/52 ,  A61K31/496 ,  C07D401/14 ,  A61K31/635 ,  C07D487/04 ,  A61K31/5377 ,  C07D403/14 ,  A61K31/551 ,  A61K31/538 ,  A61K31/541 ,  A61P43/00 ,  A61P9/00 ,  A61P29/00 ,  A61P37/00 ,  A61P35/00 ,  C07D498/04 ,  A61K31/519

CPC分类号： C07D471/04 ,  C07D239/48 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D473/16

摘要： 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.

摘要翻译： 本发明涉及式I-II化合物及其药学上可接受的盐，酯和前体药物，它们是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：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：US09139581B2

公开(公告)日：2015-09-22

申请号：US13528709

申请日：2012-06-20

申请人： Yonghong Song ,  Qing Xu ,  Shawn M. Bauer ,  Zhaozhong J. Jia ,  Mukund Mehrotra ,  Anjali Pandey

发明人： Yonghong Song ,  Qing Xu ,  Shawn M. Bauer ,  Zhaozhong J. Jia ,  Mukund Mehrotra ,  Anjali Pandey

IPC分类号： A61K31/497 ,  A61K31/505 ,  C07D403/00 ,  C07D471/04 ,  C07D239/48 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D473/16 ,  C07D403/14

CPC分类号： C07D471/04 ,  C07D239/48 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D473/16

摘要： 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.

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.

公开(公告)号：US08258144B2

公开(公告)日：2012-09-04

申请号：US12386848

申请日：2009-04-22

申请人： Yonghong Song ,  Qing Xu ,  Shawn M. Bauer ,  Zhaozhong J. Jia ,  Mukund Mehrotra ,  Anjali Pandey

发明人： Yonghong Song ,  Qing Xu ,  Shawn M. Bauer ,  Zhaozhong J. Jia ,  Mukund Mehrotra ,  Anjali Pandey

IPC分类号： C07D487/00 ,  A61K31/519

CPC分类号： C07D471/04 ,  C07D239/48 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D473/16

摘要： 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.

摘要翻译： 本发明涉及式I-II化合物及其药学上可接受的盐，酯和前体药物，它们是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：US20120108566A1

公开(公告)日：2012-05-03

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： A61K31/496 ,  A61K31/4545 ,  C07D413/14 ,  A61K31/5377 ,  A61K31/4427 ,  A61P9/00 ,  A61P29/00 ,  A61P37/00 ,  A61P7/06 ,  A61P35/00 ,  A61P37/06 ,  A61P19/02 ,  A61P1/00 ,  A61P11/06 ,  A61P27/02 ,  A61P11/00 ,  A61P19/04 ,  A61P25/00 ,  A61P3/10 ,  A61P17/06 ,  C12N5/071 ,  C07D401/12

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：US20110005947A1

公开(公告)日：2011-01-13

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： B65D85/00 ,  C07D239/48 ,  A61K31/505 ,  C07D403/12 ,  A61K31/506 ,  C07D405/12 ,  C07D413/12 ,  A61K31/5377 ,  C07D403/14 ,  C07D401/12 ,  C07D417/12 ,  C07D401/14 ,  A61K31/444 ,  A61K31/4427 ,  A61K31/4439 ,  A61P29/00 ,  A61P3/10 ,  A61P25/00 ,  A61P37/06 ,  A61P9/00 ,  A61P11/06

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：US20120088736A1

公开(公告)日：2012-04-12

申请号：US13271037

申请日：2011-10-11

申请人： Robert Scarborough ,  Carroll Anna Crew Scarborough ,  Wolin Huang ,  Mukund Mehrotra ,  Xiaoming Zhang ,  Hilary Cannon ,  Craig M. Grant

发明人： Robert Scarborough ,  Carroll Anna Crew Scarborough ,  Wolin Huang ,  Mukund Mehrotra ,  Xiaoming Zhang ,  Hilary Cannon ,  Craig M. Grant

IPC分类号： A61K31/517 ,  A61K31/727 ,  A61P7/02 ,  A61P7/00 ,  A61P9/10 ,  A61P25/00 ,  A61P29/00 ,  A61K31/616 ,  A61P9/00

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 。