公开(公告)号：WO2009094168A1

公开(公告)日：2009-07-30

申请号：PCT/US2009/000418

申请日：2009-01-21

Applicant: AMGEN INC. ,  CHEN, Xiaoqi ,  HENNE, Kirk ,  MEDINA, Julio C.

Inventor： CHEN, Xiaoqi ,  HENNE, Kirk ,  MEDINA, Julio C.

IPC: C07D471/04 ,  A61K31/519 ,  A61P29/00 ,  A61P37/00

CPC classification number: C07D471/04

Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of a chemokine receptor. The subject methods are useful for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis, transplant rejection and type I diabetes.

Abstract translation: 本文提供了可用于治疗炎症和免疫疾病和疾病的化合物，组合物和方法。 特别地，本发明提供调节趋化因子受体的表达和/或功能的化合物。 本发明的方法可用于治疗炎性和免疫调节性疾病和疾病，例如多发性硬化，类风湿性关节炎，移植排斥和I型糖尿病。

公开(公告)号：WO2006127503A2

公开(公告)日：2006-11-30

申请号：PCT/US2006/019545

申请日：2006-05-18

Applicant: AMGEN INC ,  HOUZE, Jonathan ,  LIU, Jiwen ,  MA, Zhihua ,  MEDINA, Julio C. ,  SCHMITT, Michael J. ,  SHARMA, Rajiv ,  SUN, Ying ,  WANG, Yingcai ,  ZHU, Liusheng

Inventor： HOUZE, Jonathan ,  LIU, Jiwen ,  MA, Zhihua ,  MEDINA, Julio C. ,  SCHMITT, Michael J. ,  SHARMA, Rajiv ,  SUN, Ying ,  WANG, Yingcai ,  ZHU, Liusheng

CPC classification number: C07D277/24 ,  C07B2200/07 ,  C07C235/34 ,  C07D233/64 ,  C07D249/08 ,  C07D257/04 ,  C07D263/32 ,  C07D417/12

Abstract: The present invention provides compounds useful, for example, for modulating insulin levels in a subject, having the general formula I: wherein Q is an optionally substituted phenyl; L is a bond or O; P is a benzene or an optionally substituted thiazole ring; and R 1 has the values provided herein. The present invention also provides compositions, uses, and methods for use of the compounds, for instance, for treatment of type II diabetes.

Abstract translation: 本发明提供了可用于例如用于调节受试者中具有通式I的胰岛素水平的化合物：其中Q是任选取代的苯基; L是一个键或O; P是苯或任选取代的噻唑环; 且R 1具有本文提供的值。 本发明还提供了用于治疗II型糖尿病的化合物的组合物，用途和方法。

公开(公告)号：WO2019173181A1

公开(公告)日：2019-09-12

申请号：PCT/US2019/020492

申请日：2019-03-04

Applicant: AMGEN INC.

Inventor： RESCOURIO, Gwenaella ,  GONZALEZ BUENROSTRO, Ana ,  BROWN, Sean P. ,  LIZARZABURU, Mike ,  MEDINA, Julio C. ,  JABRI, Salman Yojiro ,  SUN, Daqing ,  SIMONOVICH, Scott Preston ,  YAN, Xuelei ,  LI, Yihong ,  REW, Yosup

IPC: C07D498/10 ,  C07D498/20 ,  A61P35/00 ,  A61K31/553 ,  C07D498/22

Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

公开(公告)号：WO2010045258A2

公开(公告)日：2010-04-22

申请号：PCT/US2009/060549

申请日：2009-10-13

Applicant: AMGEN INC. ,  BROWN, Sean P. ,  DRANSFIELD, Paul ,  DU, Xiaohui ,  FU, Zice ,  HOUZE, Jonathan ,  JIAO, XianYun ,  LAI, SuJen ,  LI, An-Rong ,  LIU, Jiwen ,  MA, Zhihua ,  MEDINA, Julio C. ,  PATTAROPONG, Vatee ,  SHEN, Wang ,  VIMOLRATANA, Marc ,  WANG, Yingcai ,  WANG, Zhongyu ,  YU, Ming ,  ZHU, Liusheng

Inventor： BROWN, Sean P. ,  DRANSFIELD, Paul ,  DU, Xiaohui ,  FU, Zice ,  HOUZE, Jonathan ,  JIAO, XianYun ,  LAI, SuJen ,  LI, An-Rong ,  LIU, Jiwen ,  MA, Zhihua ,  MEDINA, Julio C. ,  PATTAROPONG, Vatee ,  SHEN, Wang ,  VIMOLRATANA, Marc ,  WANG, Yingcai ,  WANG, Zhongyu ,  YU, Ming ,  ZHU, Liusheng

IPC: C07C62/34 ,  C07D249/00 ,  C07D277/00 ,  C07D311/00 ,  C07D231/00 ,  C07D271/00 ,  C07D221/00

CPC classification number: C07C62/34 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07D213/643 ,  C07D217/24 ,  C07D253/065 ,  C07D277/22 ,  C07D311/04 ,  C07D401/12

Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula IA, IB, I'A or I'B, where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.

Abstract translation: 本发明提供了可用于例如治疗受试者的代谢紊乱的化合物。 这些化合物具有通式IA，IB，I'A或I'B，其中本文提供变量的定义。 本发明还提供了组合物，其包括化合物在制备药物和用于治疗代谢性疾病例如II型糖尿病中的使用方法。

公开(公告)号：WO2018097945A1

公开(公告)日：2018-05-31

申请号：PCT/US2017/059824

申请日：2017-11-03

Applicant: AMGEN INC.

Inventor： CHEN, Ning ,  CHEN, Xiaoqi ,  CHEN, Yinhong ,  CHENG, Alan C. ,  CONNORS, Richard V. ,  DEIGNAN, Jeffrey ,  DRANSFIELD, Paul John ,  DU, Xiaohui ,  FU, Zice ,  HARVEY, James S. ,  HEATH, Julie Anne ,  HEUMANN, Lars V. ,  HORNE, Daniel B. ,  HOUZE, Jonathan ,  KALLER, Matthew R. ,  KAYSER, Frank ,  KHAKOO, Aarif Yusuf ,  KOPECKY, David J. ,  LAI, Su-Jen ,  MA, Zhihua ,  MEDINA, Julio C. ,  MIHALIC, Jeffrey T. ,  NISHIMURA, Nobuko ,  OLSON, Steven H. ,  PATTAROPONG, Vatee ,  SWAMINATH, Gayathri ,  WANG, Xiaodong ,  WANSKA, Malgorzata ,  YANG, Kevin ,  YEH, Wen-Chen

IPC: C07D401/14 ,  C07D409/14 ,  C07D417/14 ,  C07D487/04 ,  A61K31/341 ,  A61K31/4196 ,  A61P9/00 ,  A61P9/02

Abstract: Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.

公开(公告)号：WO2018097944A1

公开(公告)日：2018-05-31

申请号：PCT/US2017/059822

申请日：2017-11-03

Applicant: AMGEN INC.

Inventor： BROWN, Matthew ,  CHEN, Ning ,  CHEN, Xiaoqi ,  CHEN, Yinhong ,  CHENG, Alan C. ,  CONNORS, Richard V. ,  DEIGNAN, Jeffrey ,  DRANSFIELD, Paul John ,  DU, Xiaohui ,  FU, Zice ,  HARVEY, James S. ,  HEATH, Julie Anne ,  HEUMANN, Lars V. ,  HOUZE, Jonathan ,  KAYSER, Frank ,  KHAKOO, Aarif Yusuf ,  KOPECKY, David J. ,  LAI, Su-Jen ,  MA, Zhihua ,  MEDINA, Julio C. ,  MIHALIC, Jeffrey T. ,  OLSON, Steven H. ,  PATTAROPONG, Vatee ,  SWAMINATH, Gayathri ,  WANG, Xiaodong ,  WANSKA, Malgorzata ,  YEH, Wen-Chen

IPC: C07D307/54 ,  C07D405/04 ,  C07D405/14 ,  A61K31/341 ,  A61K31/4196 ,  A61P9/02 ,  A61P9/00

Abstract: Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula (I) and Formula (II) have the following structures: (I); (II). Intermediates (V) are also claimed.

公开(公告)号：WO2016187308A1

公开(公告)日：2016-11-24

申请号：PCT/US2016/033088

申请日：2016-05-18

Applicant: AMGEN INC.

Inventor： CHEN, Ning ,  CHEN, Xiaoqi ,  CHEN, Yinhong ,  CHENG, Alan C. ,  CONNORS, Richard V. ,  DEIGNAN, Jeffrey ,  DRANSFIELD, Paul John ,  DU, Xiaohui ,  FU, Zice ,  HEATH, Julie Anne ,  HORNE, Daniel B. ,  HOUZE, Jonathan ,  KALLER, Matthew R. ,  KHAKOO, Aarif Yusuf ,  KOPECKY, David John ,  LAI, Su-Jen ,  MA, Zhihua ,  MCGEE, Lawrence R. ,  MEDINA, Julio C. ,  MIHALIC, Jeffrey T. ,  NISHIMURA, Nobuko ,  OLSON, Steven H. ,  PATTAROPONG, Vatee ,  SWAMINATH, Gayathri ,  WANG, Xiaodong ,  YANG, Kevin ,  YEH, Wen-Chen ,  DEBENEDETTO, Mikkel V. ,  FARRELL, Robert P. ,  HEDLEY, Simon J. ,  JUDD, Ted C. ,  KAYSER, Frank

IPC: C07D401/14 ,  C07D401/04 ,  C07D413/04 ,  A61K31/4196 ,  A61K31/4439 ,  A61P9/00

CPC classification number: C07D401/14 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  A61K31/695 ,  A61K45/06 ,  C07B57/00 ,  C07B59/002 ,  C07B2200/05 ,  C07B2200/07 ,  C07C311/13 ,  C07D211/54 ,  C07D213/61 ,  C07D213/71 ,  C07D213/82 ,  C07D239/26 ,  C07D239/30 ,  C07D239/34 ,  C07D241/12 ,  C07D241/18 ,  C07D241/24 ,  C07D249/08 ,  C07D295/16 ,  C07D401/04 ,  C07D401/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07F7/08

Abstract: Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures where the definitions of the variables are provided herein.

Abstract translation: 式I和式II的化合物，其药学上可接受的盐，前述任何一种的立体异构体或其混合物是APJ受体的激动剂，并且可用于治疗心血管和其它病症。 式I和式II的化合物具有以下结构，其中本文提供变量的定义。

公开(公告)号：WO2013049250A1

公开(公告)日：2013-04-04

申请号：PCT/US2012/057389

申请日：2012-09-26

Applicant: AMGEN INC. ,  BARTBERGER, Michael D. ,  BECK, Hilary Plake ,  CHEN, Xiaoqi ,  CONNORS, Richard V. ,  DEIGNAN, Jeffrey ,  DUQUETTE, Jason A. ,  EKSTEROWICZ, John ,  FOX, Brian M. ,  FU, Jiasheng ,  GONZALEZ BUENROSTRO, Ana ,  GONZALEZ LOPEZ DE TURISO, Felix ,  GUSTIN, Darin J. ,  HEATH, Julie A. ,  JOHNSON, Michael G. ,  KAYSER, Frank ,  KOPECKY, David J. ,  LI, Yihong ,  LI, Zhihong ,  MA, Zhihua ,  MCINTOSH, Joel ,  MEDINA, Julio C. ,  MIHALIC, Jeffrey T. ,  OLSON, Steven H. ,  REW, Yosup ,  ROVETO, Philip M. ,  SCHMITT, Michael J. ,  SUN, Daqing ,  WANG, Xiaodong ,  WANSKA, Malgorzata ,  WEATHERS, Christine ,  YAN, Xuelei

Inventor： BARTBERGER, Michael D. ,  BECK, Hilary Plake ,  CHEN, Xiaoqi ,  CONNORS, Richard V. ,  DEIGNAN, Jeffrey ,  DUQUETTE, Jason A. ,  EKSTEROWICZ, John ,  FOX, Brian M. ,  FU, Jiasheng ,  GONZALEZ BUENROSTRO, Ana ,  GONZALEZ LOPEZ DE TURISO, Felix ,  GUSTIN, Darin J. ,  HEATH, Julie A. ,  JOHNSON, Michael G. ,  KAYSER, Frank ,  KOPECKY, David J. ,  LI, Yihong ,  LI, Zhihong ,  MA, Zhihua ,  MCINTOSH, Joel ,  MEDINA, Julio C. ,  MIHALIC, Jeffrey T. ,  OLSON, Steven H. ,  REW, Yosup ,  ROVETO, Philip M. ,  SCHMITT, Michael J. ,  SUN, Daqing ,  WANG, Xiaodong ,  WANSKA, Malgorzata ,  WEATHERS, Christine ,  YAN, Xuelei

IPC: C07D265/06 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D413/12

CPC classification number: C07D413/04 ,  C07D265/06 ,  C07D265/32 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04

Abstract: The present invention provides MDM2 inhibitor compounds of Formula I or II, or the pharmaceutically acceptable salts thereof, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.

Abstract translation: 本发明提供式I或II的MDM2抑制剂化合物或其药学上可接受的盐，其中变量如上所定义，哪些化合物可用作治疗剂，特别是用于治疗癌症。 本发明还涉及含有MDM2抑制剂的药物组合物。

公开(公告)号：WO2008030618A1

公开(公告)日：2008-03-13

申请号：PCT/US2007/019662

申请日：2007-09-06

Applicant: AMGEN INC. ,  BROWN, Sean P. ,  DRANSFIELD, Paul ,  HOUZE, Jonathan B. ,  LIU, Jinqian ,  LIU, Jiwen ,  MA, Zhihua ,  MEDINA, Julio C. ,  PATTAROPONG, Vatee ,  SCHMITT, Michael J. ,  SHARMA, Rajiv ,  WANG, Yingcai

Inventor： BROWN, Sean P. ,  DRANSFIELD, Paul ,  HOUZE, Jonathan B. ,  LIU, Jinqian ,  LIU, Jiwen ,  MA, Zhihua ,  MEDINA, Julio C. ,  PATTAROPONG, Vatee ,  SCHMITT, Michael J. ,  SHARMA, Rajiv ,  WANG, Yingcai

IPC: C07D213/55 ,  C07D231/12 ,  C07D233/64 ,  C07D239/26 ,  C07D249/10 ,  C07D257/04 ,  C07D261/08 ,  C07D263/32 ,  C07D285/12 ,  C07D333/24 ,  C07D207/327 ,  C07D277/587 ,  C07C59/72 ,  C07C233/65 ,  A61K31/192 ,  A61K31/40

CPC classification number: C07D233/64 ,  C07C51/09 ,  C07C51/367 ,  C07C51/47 ,  C07C235/34 ,  C07C2602/10 ,  C07D207/327 ,  C07D213/55 ,  C07D231/12 ,  C07D239/26 ,  C07D249/10 ,  C07D257/04 ,  C07D261/08 ,  C07D263/32 ,  C07D277/587 ,  C07D285/12 ,  C07D333/24 ,  C07C59/72

Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables Q, L 1 , ℗, L 2 , M, X, L 3 , and A are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.

Abstract translation: 本发明提供了可用于例如治疗受试者的代谢紊乱的化合物。 这些化合物具有通式I：其中变量Q，L 1，...，L 2，M，X，L 3，...的定义 >和A。 本发明还提供了组合物，其包括化合物在制备药物和用于治疗代谢性疾病例如II型糖尿病中的使用方法。

公开(公告)号：WO2007062175A2

公开(公告)日：2007-05-31

申请号：PCT/US2006/045298

申请日：2006-11-21

Applicant: AMGEN INC. ,  COLLINS, Tassie L. ,  MEDINA, Julio C. ,  XU, Feng ,  ZHU, Liusheng

Inventor： COLLINS, Tassie L. ,  MEDINA, Julio C. ,  XU, Feng ,  ZHU, Liusheng

IPC: C07D471/20 ,  A61K31/438 ,  A61P3/10 ,  A61P29/00 ,  A61P35/04 ,  A61P37/06

CPC classification number: C07D471/20

Abstract: CXCR3 ANTAGONISTS Compounds, compositions and methods are provided that are useful in the treatment of conditions and diseases mediated by a chemokine receptor. In particular, the compounds of the invention modulate the CXCR3 chemokine receptor. The subject methods are useful for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis and type I diabetes.

Abstract translation: CXCR3拮抗剂提供可用于治疗由趋化因子受体介导的病症和疾病的化合物，组合物和方法。 特别地，本发明的化合物调节CXCR3趋化因子受体。 本发明的方法可用于治疗炎症和免疫调节性疾病和疾病，例如多发性硬化，类风湿性关节炎和I型糖尿病。