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：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：WO2007111921A1

公开(公告)日：2007-10-04

申请号：PCT/US2007/007077

申请日：2007-03-22

Applicant: AMGEN INC. ,  POWERS, Jay, P. ,  SUN, Daqing ,  YAN, Xuelei

Inventor： POWERS, Jay, P. ,  SUN, Daqing ,  YAN, Xuelei

IPC: C07D295/22 ,  C07D333/22 ,  C07D213/46 ,  A61K31/495 ,  A61K31/496 ,  A61P3/06 ,  A61P3/10 ,  A61P5/24 ,  A61P5/46 ,  A61P9/10 ,  C07D261/08 ,  C07D307/46 ,  C07D231/12 ,  C07D401/04

CPC classification number: C07D243/08 ,  C07D213/56 ,  C07D231/12 ,  C07D241/04 ,  C07D295/26 ,  C07D333/38

Abstract: Diaza heterocyclic amide derivatives according to Formula (I) have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: (I) where R 5 ,R 6 ,R 7 ,R 8 ,R 9 ,R 10 , m, Q, X, and Y are set forth in the description.

Abstract translation: 式（I）的二氮杂环酰胺衍生物具有治疗效用，特别是治疗糖尿病，肥胖症及相关病症和病症：（I）其中R 5，R 6， R 7，R 8，R 9，R 10，m，Q，X和Y 在说明书中阐述。

公开(公告)号：WO2005118538A3

公开(公告)日：2005-12-15

申请号：PCT/US2005/013358

申请日：2005-04-20

Applicant: AMGEN, INC. ,  DEGRAFFENREID, Michael R. ,  POWERS, Jay P. ,  SUN, Daqing ,  YAN, Xuelei

Inventor： DEGRAFFENREID, Michael R. ,  POWERS, Jay P. ,  SUN, Daqing ,  YAN, Xuelei

IPC: A61K31/401 ,  C07D207/48 ,  C07D295/26 ,  C07D209/08 ,  C07D215/58 ,  C07D403/04 ,  C07D401/04 ,  C07D401/06 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/4453 ,  A61K31/47 ,  A61P3/10

Abstract: Arylsulfonamide compounds of formula (I) are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders.

公开(公告)号：WO2008156601A1

公开(公告)日：2008-12-24

申请号：PCT/US2008/007269

申请日：2008-06-11

Applicant: AMGEN INC. ,  POWERS, Jay P. ,  SUN, Daqing ,  YAN, Xuelei ,  JULIAN, Lisa ,  GONZALEZ LOPEZ DE TURISO, Felix

Inventor： POWERS, Jay P. ,  SUN, Daqing ,  YAN, Xuelei ,  JULIAN, Lisa ,  GONZALEZ LOPEZ DE TURISO, Felix

IPC: C07D231/10 ,  C07D261/06 ,  C07D263/30 ,  C07D277/20 ,  A61K31/41 ,  A61P3/10

CPC classification number: C07D231/10 ,  C07D261/06 ,  C07D263/30 ,  C07D277/20

Abstract: The present invention provides tricyclic compounds according to formula (I): (I) where R 1 , R 2 , R 3 , W, X, Y, Z, m, n, and p are as defined in the description; as well as pharmaceutical compositions comprising the same, methods of use of the compounds and compositions of the invention for the treatment of conditions associated with hydroxysteroid dehydrogenases (e.g., 11 -HSD1), and the use of the compounds of the invention in the preparation of medicaments for the treatment of hydroxysteroid dehydrogenase-associated conditions.

Abstract translation: 本发明提供式（I）的三环化合物：（I）其中R 1，R 2，R 3，W，X，Y，Z，m，n和p如说明书中所定义; 以及包含其的药物组合物，本发明化合物和组合物用于治疗与羟基类固醇脱氢酶（例如11-HSD1）相关的病症的方法，以及本发明化合物在制备 用于治疗羟基类固醇脱氢酶相关病症的药物。

公开(公告)号：WO2007070506A2

公开(公告)日：2007-06-21

申请号：PCT/US2006/047353

申请日：2006-12-13

Applicant: AMGEN INC. ,  POWERS, Jay, P. ,  SUN, Daqing ,  TU, Hua ,  YAN, Xuelei

Inventor： POWERS, Jay, P. ,  SUN, Daqing ,  TU, Hua ,  YAN, Xuelei

IPC: C07D295/22 ,  C07D401/04 ,  C07D403/06 ,  A61P3/06 ,  A61K31/496

CPC classification number: C07D295/26 ,  C07D213/74 ,  C07D241/04 ,  C07D243/08 ,  C07D243/10 ,  C07D401/04 ,  C07D403/06

Abstract: Diaza heterocyclic sulfonamide derivatives according to formula I have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: I where R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , X, Y 1 , Y 2 , m, and n are set forth in the description.

Abstract translation: 根据式I的二氮杂杂环磺酰胺衍生物具有治疗用途，特别是在治疗糖尿病，肥胖症和相关病症和病症中：其中R 7，R 5， 8，R 9，R 10，R 11，R 12，R 8，R 12， 13，X，Y 1，Y 2，m和n在说明书中阐述。

公开(公告)号：WO2011153509A1

公开(公告)日：2011-12-08

申请号：PCT/US2011/039184

申请日：2011-06-03

Applicant: AMGEN INC. ,  BARTBERGER, Michael David ,  GONZALEZ BUENROSTRO, Ana ,  BECK, Hilary Plake ,  CHEN, Xiaoqi ,  CONNORS, Richard Victor ,  DEIGNAN, Jeffery ,  DUQUETTE, Jason ,  EKSTEROWICZ, John ,  FISHER, Benjamin ,  FOX, Brian Matthew ,  FU, Jiasheng ,  FU, Zice ,  GONZALEZ LOPEZ DE TURISO, Felix ,  GRIBBLE, JR., Michael William ,  GUSTIN, Darin James ,  HEATH, Julie Anne ,  HUANG, Xin ,  JIAO, Xianyun ,  JOHNSON, Michael ,  KAYSER, Frank ,  KOPECKY, David John ,  LAI, Sujen ,  LI, Yihong ,  LI, Zhihong ,  LIU, Jiwen ,  LOW, Jonathan Dante ,  LUCAS, Brian Stuart ,  MA, Zhihua ,  MCGEE, Lawrence ,  MCINTOSH, Joel ,  MCMINN, Dustin ,  MEDINA, Julio Cesar ,  MIHALIC, Jeffrey Thomas ,  OLSON, Steven Howard ,  REW, Yosup ,  ROVETO, Philip Marley ,  SUN, Daqing ,  WANG, Xiaodong ,  WANG, Yingcai ,  YAN, Xuelei ,  YU, Ming ,  ZHU, Jiang

Inventor： BARTBERGER, Michael David ,  GONZALEZ BUENROSTRO, Ana ,  BECK, Hilary Plake ,  CHEN, Xiaoqi ,  CONNORS, Richard Victor ,  DEIGNAN, Jeffery ,  DUQUETTE, Jason ,  EKSTEROWICZ, John ,  FISHER, Benjamin ,  FOX, Brian Matthew ,  FU, Jiasheng ,  FU, Zice ,  GONZALEZ LOPEZ DE TURISO, Felix ,  GRIBBLE, JR., Michael William ,  GUSTIN, Darin James ,  HEATH, Julie Anne ,  HUANG, Xin ,  JIAO, Xianyun ,  JOHNSON, Michael ,  KAYSER, Frank ,  KOPECKY, David John ,  LAI, Sujen ,  LI, Yihong ,  LI, Zhihong ,  LIU, Jiwen ,  LOW, Jonathan Dante ,  LUCAS, Brian Stuart ,  MA, Zhihua ,  MCGEE, Lawrence ,  MCINTOSH, Joel ,  MCMINN, Dustin ,  MEDINA, Julio Cesar ,  MIHALIC, Jeffrey Thomas ,  OLSON, Steven Howard ,  REW, Yosup ,  ROVETO, Philip Marley ,  SUN, Daqing ,  WANG, Xiaodong ,  WANG, Yingcai ,  YAN, Xuelei ,  YU, Ming ,  ZHU, Jiang

IPC: C07D211/40 ,  C07D401/04 ,  C07D401/06 ,  C07D407/04 ,  C07D407/06 ,  C07D409/04 ,  C07D413/06 ,  C07D417/06 ,  C07D471/20 ,  C07D279/02 ,  C07D401/12 ,  C07D498/08 ,  C07D498/20 ,  A61K31/4412 ,  A61P35/00

CPC classification number: C07D211/76 ,  C07D221/20 ,  C07D279/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D407/04 ,  C07D407/06 ,  C07D409/04 ,  C07D409/12 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D491/08 ,  C07D491/153 ,  C07D498/08 ,  C07D498/14 ,  C07D498/20

Abstract: The present invention provides MDM2 inhibitor compounds of Formula (I), 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）的MDM2抑制剂化合物，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：WO2014130470A1

公开(公告)日：2014-08-28

申请号：PCT/US2014/016971

申请日：2014-02-18

Applicant: AMGEN INC.

Inventor： BARTBERGER, Michael, D. ,  BECK, Hilary, Plake ,  DEGRAFFENREID, Michael, R. ,  FOX, Brian, M. ,  GONZALEZ LOPEZ DE TURISO, Felix ,  JULIAN, Lisa, D. ,  KAYSER, Frank ,  MEDINA, Julio, C. ,  OLSON, Steven, H. ,  REW, Yosup ,  ROVETO, Philip, M. ,  SUN, Daqing ,  YAN, Xuelei

IPC: C07D265/32 ,  C07D413/04 ,  C07D413/06 ,  C07D279/12 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/54 ,  A61P35/00

CPC classification number: C07D265/32 ,  C07D279/12 ,  C07D413/04 ,  C07D413/06 ,  C07D487/04

Abstract: The present invention provides MDM2 inhibitor compounds of Formula (I), 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）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：WO2007145835A3

公开(公告)日：2007-12-21

申请号：PCT/US2007/012809

申请日：2007-05-31

Applicant: AMGEN INC. ,  POWERS, Jay, P. ,  DEGRAFFENREID, Michael ,  JULIAN, Lisa ,  KAIZERMAN, Jacob ,  MCMINN, Dustin ,  REW, Yosup ,  SUN, Daqing ,  YAN, Xuelei ,  WANG, Zhulun

Inventor： POWERS, Jay, P. ,  DEGRAFFENREID, Michael ,  JULIAN, Lisa ,  KAIZERMAN, Jacob ,  MCMINN, Dustin ,  REW, Yosup ,  SUN, Daqing ,  YAN, Xuelei ,  WANG, Zhulun

IPC: C07C235/54 ,  C07D213/56 ,  C07D213/57 ,  C07D239/26 ,  C07D261/08 ,  C07D273/08 ,  C07D307/94 ,  C07D333/24 ,  C07D333/38 ,  A61K31/166 ,  A61K31/381 ,  A61K31/415 ,  A61K31/4406 ,  A61K31/4409

Abstract: Benzamide derivatives of formula ( I ) are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders, formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , and n are as defined herein.

公开(公告)号：WO2006138508A2

公开(公告)日：2006-12-28

申请号：PCT/US2006/023395

申请日：2006-06-15

Applicant: AMGEN INC. ,  POWERS, Jay P. ,  DEGRAFFENREID, Michael R. ,  HE, Xiao ,  JULIAN, Lisa ,  MCMINN, Dustin L. ,  SUN, Daqing ,  REW, Yosup ,  YAN, Xuelei

Inventor： POWERS, Jay P. ,  DEGRAFFENREID, Michael R. ,  HE, Xiao ,  JULIAN, Lisa ,  MCMINN, Dustin L. ,  SUN, Daqing ,  REW, Yosup ,  YAN, Xuelei

IPC: C07C235/42 ,  C07C237/22 ,  C07C255/24 ,  C07C255/31

CPC classification number: C07D277/28 ,  C07C235/42 ,  C07C235/54 ,  C07C237/42 ,  C07C255/29 ,  C07C255/31 ,  C07C255/44 ,  C07C255/46 ,  C07C255/60 ,  C07C317/36 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/42 ,  C07D211/16 ,  C07D211/18 ,  C07D211/22 ,  C07D211/34 ,  C07D211/38 ,  C07D211/52 ,  C07D211/60 ,  C07D211/64 ,  C07D213/40 ,  C07D213/61 ,  C07D213/74 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D233/64 ,  C07D295/192 ,  C07D307/22 ,  C07D309/14 ,  C07D333/20

Abstract: Benzamide derivatives of formulae I and II, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof, and pharmaceutical compositions comprising the same, are described and have therapeutic utility, particularly in the treatment of diabetes, obesit and related conditions and disorders: wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 9 , R 10 , R ll , and R 12 are defined as provided herein.

Abstract translation: 描述了式I和II的苯甲酰胺衍生物及其药学上可接受的盐，溶剂化物，立体异构体和前药，以及包含其的药物组合物，并且具有治疗用途，特别是在治疗糖尿病，obesit和相关病症和病症中：其中 R 1，R 2，N 2，...，