公开(公告)号：US09873701B2

公开(公告)日：2018-01-23

申请号：US14520899

申请日：2014-10-22

Applicant: AMGEN INC.

Inventor： Yi Chen ,  Timothy D. Cushing ,  Jason A. Duquette ,  Felix Gonzalez Lopez De Turiso ,  Xiaolin Hao ,  Xiao He ,  Brian S. Lucas ,  Lawrence R. McGee ,  Andreas Reichelt ,  Robert M. Rzasa ,  Jennifer L. Seganish ,  Youngsook Shin ,  Dawei Zhang

IPC: C07D487/04 ,  C07D473/30 ,  C07D473/34 ,  C07D471/04

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D473/30 ,  C07D473/34

Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

公开(公告)号：US20140315895A1

公开(公告)日：2014-10-23

申请号：US14316586

申请日：2014-06-26

Applicant: AMGEN INC.

Inventor： Michael D. Bartberger ,  Ana Gonzalez Buenrostro ,  Hilary Plake Beck ,  Xiaoqi Chen ,  Richard Victor Connors ,  Jeffrey Deignan ,  Jason A. Duquette ,  John Eksterowicz ,  Benjamin Fisher ,  Brian M. Fox ,  Jiasheng Fu ,  Zice Fu ,  Felix Gonzalez Lopez de Turiso ,  Michael W. Gribble ,  Darin J. Gustin ,  Julie A. Heath ,  Xin Huang ,  XianYun Jiao ,  Michael G. Johnson ,  Frank Kayser ,  David John Kopecky ,  SuJen Lai ,  Yihong Li ,  Zhihong Li ,  Jiwen Liu ,  Jonathan D. Low ,  Brian S. Lucas ,  Zhihua MA ,  Lawrence R. McGee ,  Joel Mcintosh ,  Dustin L. McMinn ,  Julio C. Medina ,  Jeffrey Thomas Mihalic ,  Steven H. Olson ,  Yosup Rew ,  Philip M. Roveto ,  Daqing Sun ,  Xiaodong Wang ,  Yingcai Wang ,  Xuelei Yan ,  Ming Yu ,  Jiang Zhu

IPC: C07D279/02

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: 本发明提供了式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：US20240300892A1

公开(公告)日：2024-09-12

申请号：US18484675

申请日：2023-10-11

Applicant: Amgen Inc.

Inventor： Michael D. Bartberger ,  Ana Gonzalez Buenrostro ,  Hilary Plake Beck ,  Xiaoqi Chen ,  Richard Victor Connors ,  Jeffrey Deignan ,  Jason A. Duquette, I ,  John Eksterowicz ,  Benjamin Fisher ,  Brian M. Fox ,  Jiasheng Fu ,  Zice Fu ,  Felix Gonzalez Lopez De Turiso ,  Michael W. Gribble ,  Darin J. Gustin ,  Julie A. Heath ,  Xin Huang ,  XianYun Jiao ,  Michael G. Johnson ,  Frank Kayser ,  David John Kopecky ,  SuJen Lai ,  Yihong Li ,  Zhihong Li ,  Jiwen Liu ,  Jonathan D. Low ,  Brian S. Lucas ,  Zhihua MA ,  Lawrence R. McGee ,  Joel McIntosh ,  Dustin L. McMinn ,  Julio C. Medina ,  Jeffrey Thomas Mihalic ,  Steven H. Olson ,  Yossup Rew ,  Philip M. Roveto ,  Daqing Sun ,  Xiaodong Wang ,  Yingcai Wang ,  Xuelei Yan ,  Ming Yu ,  Jiang Zhu

IPC: 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

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.

公开(公告)号：US11001598B2

公开(公告)日：2021-05-11

申请号：US16569927

申请日：2019-09-13

Applicant: AMGEN INC.

Inventor： Brian S. Lucas

IPC: C07C59/56 ,  C07C59/68 ,  C07D513/10 ,  C07D513/08 ,  C07D498/00

Abstract: Provided herein are compounds that are useful intermediates that may used to synthesize myeloid cell leukemia 1 protein (Mcl-1) inhibitors. Also provided are 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, 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：US09593129B2

公开(公告)日：2017-03-14

申请号：US15008342

申请日：2016-01-27

Applicant: AMGEN INC.

Inventor： Michael D. Bartberger ,  Ana Gonzalez Buenrostro ,  Hilary Plake Beck ,  Xiaoqi Chen ,  Richard Victor Connors ,  Jeffrey Deignan ,  Jason A. Duquette ,  John Eksterowicz ,  Benjamin Fisher ,  Brian M. Fox ,  Jiasheng Fu ,  Zice Fu ,  Felix Gonzalez Lopez De Turiso ,  Michael W. Gribble, Jr. ,  Darin J. Gustin ,  Julie A. Heath ,  Xin Huang ,  XianYun Jiao ,  Michael G. Johnson ,  Frank Kayser ,  David John Kopecky ,  SuJen Lai ,  Yihong Li ,  Zhihong Li ,  Jiwen Liu ,  Jonathan D. Low ,  Brian S. Lucas ,  Zhihua Ma ,  Lawrence R. McGee ,  Joel McIntosh ,  Dustin L. McMinn ,  Julio C. Medina ,  Jeffrey Thomas Mihalic ,  Steven H. Olson ,  Yosup Rew ,  Philip M. Roveto ,  Daqing Sun ,  Xiaodong Wang ,  Yingcai Wang ,  Xuelei Yan ,  Ming Yu ,  Jiang Zhu

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

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IE的MDM2抑制剂化合物，该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：US09296736B2

公开(公告)日：2016-03-29

申请号：US14316586

申请日：2014-06-26

Applicant: AMGEN INC.

Inventor： Michael D. Bartberger ,  Ana Gonzalez Buenrostro ,  Hilary Plake Beck ,  Xiaoqi Chen ,  Richard Victor Connors ,  Jeffrey Deignan ,  Jason A. Duquette ,  John Eksterowicz ,  Benjamin Fisher ,  Brian M. Fox ,  Jiasheng Fu ,  Zice Fu ,  Felix Gonzalez Lopez De Turiso ,  Michael W. Gribble ,  Darin J. Gustin ,  Julie A. Heath ,  Xin Huang ,  XianYun Jiao ,  Michael G. Johnson ,  Frank Kayser ,  David John Kopecky ,  SuJen Lai ,  Yihong Li ,  Zhihong Li ,  Jiwen Liu ,  Jonathan D. Low ,  Brian S. Lucas ,  Zhihua Ma ,  Lawrence R. McGee ,  Joel McIntosh ,  Dustin L. McMinn ,  Julio C. Medina ,  Jeffrey Thomas Mihalic ,  Steven H. Olson ,  Yosup Rew ,  Philip M. Roveto ,  Daqing Sun ,  Xiaodong Wang ,  Yingcai Wang ,  Xuelei Yan ,  Ming Yu ,  Jiang Zhu

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

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.

公开(公告)号：US20220169611A1

公开(公告)日：2022-06-02

申请号：US17672660

申请日：2022-02-15

Applicant: Amgen Inc.

Inventor： Michael D. Bartberger ,  Ana Gonzalez Buenrostro ,  Hilary Plake Beck ,  Xiaoqi Chen ,  Richard Victor Connors ,  Jeffrey Deignan ,  Jason A. Dequette, I ,  John Eksterowicz ,  Benjamin Fisher ,  Brian M. Fox ,  Jiasheng Fu ,  Zice Fu ,  Felix Gonzalez Lopez De Turiso ,  Michael W. Gribble ,  Darin J. Gustin ,  Julie A. Heath ,  Xin Huang ,  XianYun Jiao ,  Michael G. Johnson ,  Frank Kayser ,  David John Kopecky ,  SuJen Lai ,  Yihong Li ,  Zhihong Li ,  Jiwen Liu ,  Jonathan D. Low ,  Brian S. Lucas ,  Zhihua Ma ,  Lawrence R. McGee ,  Josel McIntosh ,  Dustin L. McMinn ,  Julio C. Medina ,  Jeffrey Thomas Mihalic ,  Steven H. Olson ,  Yossup Rew ,  Philip M. Roveto ,  Daqing Sun ,  Xiaodong Wang ,  Yingcai Wang ,  Xuelei Yan ,  Ming Yu ,  Jiang Zhu

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

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.

公开(公告)号：US20190062276A1

公开(公告)日：2019-02-28

申请号：US15927426

申请日：2018-03-21

Applicant: Amgen Inc.

Inventor： Michael D. Bartberger ,  Ana Gonzalez Buenrostro ,  Hilary Plake Beck ,  Xiaoqi Chen ,  Richard Victor Connors ,  Jeffrey Deignan ,  Jason A. Duquette ,  John Eksterowicz ,  Benjamin Fisher ,  Brian M. Fox ,  Jiasheng Fu ,  Zice Fu ,  Felix Gonzalez Lopez De Turiso ,  Michael W. Gribble, JR. ,  Darin J. Gustin ,  Julie A. Heath ,  Xin Huang ,  XianYun Jiao ,  Michael G. Johnson ,  Frank Kayser ,  David John Kopecky ,  SuJen Lai ,  Yihong Li ,  Zhihong Li ,  Jiwen Liu ,  Jonathan D. Low ,  Brian S. Lucas ,  Zhihua Ma ,  Lawrence R. McGee ,  Joel McIntosh ,  Dustin L. McMinn ,  Julio C. Medina ,  Jeffrey Thomas Mihalic ,  Steven H. Olson ,  Yosup Rew ,  Philip M. Roveto ,  Daqing Sun ,  Xiaodong Wang ,  Yingcai Wang ,  Xuelei Yan ,  Ming Yu ,  Jiang Zhu

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

公开(公告)号：US20210179560A1

公开(公告)日：2021-06-17

申请号：US16983027

申请日：2020-08-03

Applicant: Amgen Inc.

Inventor： Michael D. Bartberger ,  Ana Gonzalez Buenrostro ,  Hilary Plake Beck ,  Xiaoqi Chen ,  Richard Victor Connors ,  Jeffrey Deignan ,  Jason A. Duquette, I ,  John Eksterowicz ,  Benjamin Fisher ,  Brian M. Fox ,  Jiasheng Fu ,  Zice Fu ,  Felix Gonzalez Lopez De Turiso ,  Michael W. Gribble ,  Darin J. Gustin ,  Julie A. Heath ,  Xin Huang ,  XianYun Jiao ,  Michael G. Johnson ,  Frank Kayser ,  David John Kopecky ,  SuJen Lai ,  Yihong Li ,  Zhihong Li ,  Jiwen Liu ,  Jonathan D. Low ,  Brian S. Lucas ,  Zhihua MA ,  Lawrence R. McGee ,  Joel McIntosh ,  Dustin L. McMinn ,  Julio C. Medina ,  Jeffrey Thomas Mihalic ,  Steven H. Olson ,  Yossup Rew ,  Philip M. Roveto ,  Daqing Sun ,  Xiaodong Wang ,  Yingcai Wang ,  Xuelei Yan ,  Ming Yu ,  Jiang Zhu

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

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.

公开(公告)号：US10100063B2

公开(公告)日：2018-10-16

申请号：US15376456

申请日：2016-12-12

Applicant: AMGEN INC.

Inventor： Sean P. Brown ,  Yunxiao Li ,  Mike Elias Lizarzaburu ,  Brian S. Lucas ,  Nick A. Paras ,  Joshua Taygerly ,  Marc Vimolratana ,  Xianghong Wang ,  Ming Yu ,  Manuel Zancanella ,  Liusheng Zhu ,  Ana Gonzalez Buenrostro ,  Zhihong Li

IPC: C07D513/10 ,  C07D513/08

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, 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.