公开(公告)号：US20190023720A1

公开(公告)日：2019-01-24

申请号：US16121750

申请日：2018-09-05

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.

公开(公告)号：US20200171043A1

公开(公告)日：2020-06-04

申请号：US16783269

申请日：2020-02-06

Applicant: AMGEN INC.

Inventor： Paul E. HARRINGTON ,  Kate ASHTON ,  Sean P. BROWN ,  Matthew R. KALLER ,  Todd J. KOHN ,  Brian Alan LANMAN ,  Kexue LI ,  Yunxiao LI ,  Jonathan D. LOW ,  Ana Elena MINATTI ,  Alexander J. PICKRELL ,  Markian M. STEC ,  Joshua TAYGERLY

IPC: A61K31/553 ,  C07D498/08 ,  A61P35/00 ,  A61P35/02

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：US20190016736A1

公开(公告)日：2019-01-17

申请号：US16123030

申请日：2018-09-06

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 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：US20200247821A1

公开(公告)日：2020-08-06

申请号：US16642441

申请日：2018-08-27

Applicant: AMGEN INC.

Inventor： Sean P. BROWN ,  Yunxiao LI ,  Paul E. HARRINGTON ,  Brian Alan LANMAN ,  Jonathan D. LOW ,  Ana Elena MINATTI ,  Vu Van MA ,  Kexue LI

IPC: C07D513/04 ,  C07D519/00 ,  A61P35/00

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 stenoisomer 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：US20160068545A1

公开(公告)日：2016-03-10

申请号：US14839149

申请日：2015-08-28

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

CPC classification number: 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.

Abstract translation: 本文提供了骨髓细胞白血病1蛋白（Mcl-1）抑制剂，其制备方法，相关药物组合物及其使用方法。 例如，本文提供了式I化合物及其药学上可接受的盐和含有这些化合物的药物组合物。 本文提供的化合物和组合物可用于例如治疗疾病或病症如癌症。

公开(公告)号：US20250122222A1

公开(公告)日：2025-04-17

申请号：US18695673

申请日：2022-08-10

Applicant: AMGEN INC.

Inventor： Michael M. YAMANO ,  Yunxiao LI ,  Primali Vasundera NAVARATNE ,  Jose M. MEDINA ,  Ning CHEN ,  Liping PETTUS ,  Rene RAHIMOFF ,  Xiaofen LI ,  John STELLWAGEN ,  Francesco MANONI ,  Kexue LI ,  Brian Alan LANMAN ,  Ryan Paul Wurz ,  Wei ZHAO ,  Huan RUI ,  Josephine ESHON

IPC: C07D519/00 ,  A61K31/519 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/553 ,  A61K31/554 ,  C07D471/04

Abstract: The present disclosure provides compounds useful for the inhibition of KRAS. The compounds have a general Formula I: wherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, cancer.

公开(公告)号：US20250034167A1

公开(公告)日：2025-01-30

申请号：US18695693

申请日：2022-08-10

Applicant: AMGEN INC.

Inventor： Michael M. YAMANO ,  Yunxiao LI ,  Primali Vasundera NAVARATNE ,  Jose M. MEDINA ,  Ning CHEN ,  Liping PETTUS ,  Rene RAHIMOFF ,  Xiaofen LI ,  John STELLWAGEN ,  Francesco MANONI ,  Kexue LI ,  Brian Alan LANMAN ,  Ryan Paul Wurz ,  Wei ZHAO ,  Huan RUI ,  Josephine ESHON

IPC: C07D519/00 ,  A61K31/519 ,  A61K31/55

Abstract: The present disclosure provides compounds useful for the inhibition of KRAS G12D. The compounds have a general Formula (I): wherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, cancer.

公开(公告)号：US20240294551A1

公开(公告)日：2024-09-05

申请号：US18614911

申请日：2024-03-25

Applicant: AMGEN INC.

Inventor： Ryan Paul Wurz ,  Yunxiao LI ,  Primali Vasundera NAVARATNE ,  Jose M. MEDINA ,  Ning CHEN ,  Liping PETTUS ,  Xiaofen LI ,  John STELLWAGEN ,  Kexue LI ,  Brian Alan LANMAN ,  Michael M. YAMANO ,  Wei ZHAO ,  Benjamin WIGMAN ,  Fabien EMMETIERE ,  Albert K. AMEGADZIE ,  Christopher P. MOHR ,  Aaron C. SIEGMUND ,  Rene RAHIMOFF ,  Zhichen WU ,  Adriano BAUER ,  Andrew SMALIGO ,  Quentin Tercenio ,  Qingyian Liu ,  Shon K. Booker

IPC: C07D519/00 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  C07D471/22 ,  C07D498/22 ,  C07D513/22

CPC classification number: C07D519/00 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  C07D471/22 ,  C07D498/22 ,  C07D513/22

Abstract: The present disclosure provides compounds useful for the inhibition of KRAS G12D, G12V, G12A, G12S, G13D, Q61H, Q61L or G12C. The compounds have a general Formula I′:




wherein the variables of Formula I′ are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, cancer.

公开(公告)号：US20210230189A1

公开(公告)日：2021-07-29

申请号：US16078152

申请日：2017-02-24

Applicant: AMGEN INC.

Inventor： Sean P. BROWN ,  David Karl BEDKE ,  Micheal R. DEGRAFFENREID ,  Jiasheng FU ,  Zhihong LI ,  Felix GONZALEZ LOPEZ TURISO ,  Ana GONZALEZ BUENROSTRO ,  Micheal W. GRIBBLE, JR. ,  Micheal G. JOHNSON ,  Todd J. KOHN ,  Kexue LI ,  Yunxiao LI ,  Mike Elias LIZARZABURU ,  Yosup REW ,  Joshua TAYGERLY ,  Yingcal WANG ,  Xuelei YAN ,  Ming YU ,  Jiang ZHU ,  Manuel ZANCANELLA ,  Xian Yun JIAO ,  Liusheng ZHU ,  Xianghong WANG ,  Julio C. MEDINA ,  Jason A. DUQUETTE ,  Jonathan B. HOUZE ,  Marc VIMOLRATANA ,  Marlo G. CARDOZO ,  Alan C. CHENG

IPC: C07D513/10 ,  C07D515/10 ,  C07D513/20

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.

公开(公告)号：US20230052348A1

公开(公告)日：2023-02-16

申请号：US17501075

申请日：2021-10-14

Applicant: AMGEN INC.

Inventor： Sean P BROWN ,  David Karl BEDKE ,  Michael R. DEGRAFFENREID ,  Jiasheng FU ,  Zhinghong LI ,  Felix GONZALEZ LOPEZ DE TURISO ,  Ana GONZALEZ BUENROSTRO ,  Michael W. GRIBBLE JR. ,  Michael G. JOHNSON ,  Todd J. KOHN ,  Kexue LI ,  Yunxiao LI ,  Mike Elias LIZARZABURU ,  Yosup REW ,  Joshua TAYGERLY ,  Yingcai WANG ,  Xuelei YAN ,  Ming YU ,  Jiang ZHU ,  Manuel ZANCANELLA ,  Xian Yun JIAO ,  Liusheng ZHU ,  Xianghong WANG ,  Julio C. MEDINA ,  Jason A. DUQUETTE ,  Jonathan B. HOUZE ,  Marc VIMOLRATANA ,  Mario G. CARDOZO ,  Alan C. CHENG

IPC: C07D513/10 ,  C07D513/20 ,  C07D515/10

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.