公开(公告)号：US20250059179A1

公开(公告)日：2025-02-20

申请号：US18696948

申请日：2022-04-28

Applicant: AMGEN INC.

Inventor： Brian Alan Lanman ,  Ryan Paul Wurz ,  Wei Zhao ,  Xiaofen Li ,  Michael M. Yamano ,  Yunxiao Li ,  Ning Chen ,  Sebastian Leth-Petersen ,  Kexue Li ,  Liping Pettus ,  Rene Rahimoff ,  Primali Vasundera Navaratne ,  Huan Rui

IPC: C07D417/14 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/55 ,  A61K31/551 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D487/20 ,  C07D498/04 ,  C07D498/10 ,  C07D519/00

Abstract: The present disclosure provides compounds useful for the inhibition of KRAS G12D. The compounds have a general Formula I: (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：US20180289720A1

公开(公告)日：2018-10-11

申请号：US15938001

申请日：2018-03-28

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 ,  A61P35/00

CPC classification number: A61K31/553 ,  A61P35/00 ,  A61P35/02 ,  C07D498/08

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, 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：US08980903B2

公开(公告)日：2015-03-17

申请号：US14453842

申请日：2014-08-07

Applicant: Amgen Inc.

Inventor： Richard V. Connors ,  Kang Dai ,  John Eksterowicz ,  Pingchen Fan ,  Benjamin Fisher ,  Jiasheng Fu ,  Kexue Li ,  Zhihong Li ,  Lawrence R. McGee ,  Rajiv Sharma ,  Xiaodong Wang ,  Dustin L. McMinn ,  Jeffrey T. Mihalic ,  Jeffrey Deignan

IPC: C07D498/04 ,  C07D491/147 ,  C07D471/14 ,  C07D471/04 ,  C07D487/14 ,  C07D491/107 ,  C07D498/10

CPC classification number: C07D471/14 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5386 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/14 ,  C07D491/107 ,  C07D491/147 ,  C07D498/04 ,  C07D498/10 ,  C07D513/14

Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.

Abstract translation: 提供了可用于治疗CDK4介导的疾病如癌症的化合物，药物组合物和方法。 本发明化合物是吡啶，吡嗪酰亚胺和三嗪衍生物。

公开(公告)号：US12091425B2

公开(公告)日：2024-09-17

申请号：US17501075

申请日：2021-10-14

Applicant: AMGEN INC.

Inventor： David Karl Bedke ,  Michael W. Gribble, Jr. ,  Michael G. Johnson ,  Todd J. Kohn ,  Kexue Li

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

CPC classification number: 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.

公开(公告)号：US12054476B2

公开(公告)日：2024-08-06

申请号：US17551105

申请日：2021-12-14

Applicant: AMGEN INC.

Inventor： Nuria A. Tamayo ,  Abhisek Banerjee ,  James Alexander Brown ,  Michael J Frohn ,  Jian Jeffrey Chen ,  Kexue Li ,  Qingyian Liu ,  Jonathan Dante Low ,  Vu Ma ,  Liping H. Pettus ,  Mary Catherine Walton ,  Ana Elena Minatti ,  Matthew Paul Bourbeau ,  Lei Jia

IPC: C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  C07D413/14 ,  C07D419/14 ,  C07D491/107

CPC classification number: C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  C07D413/14 ,  C07D419/14 ,  C07D491/107

Abstract: Compounds of formula (I):




as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

公开(公告)号：US20190201412A1

公开(公告)日：2019-07-04

申请号：US16297904

申请日：2019-03-11

Applicant: AMGEN INC.

Inventor： Sean P. Brown ,  Kexue Li ,  Yunxiao Li ,  Markian M. Stec

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

CPC classification number: A61K31/553 ,  A61P35/00 ,  A61P35/02 ,  C07D498/08

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, 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：US20250059205A1

公开(公告)日：2025-02-20

申请号：US18696946

申请日：2022-04-28

Applicant: AMGEN INC.

Inventor： Brian Alan Lanman ,  Ryan Paul Wurz ,  Wei Zhao ,  Xiaofen Li ,  Michael M. Yamano ,  Yunxiao Li ,  Ning Chen ,  Birgitte Weinreich Husemoen ,  Sebastian Leth-Petersen ,  Jose M. Medina ,  Kexue Li ,  Liping Pettus ,  Rene Rahimoff ,  Primali Vasundera Navaratne ,  Huan Rui ,  Christopher P. Mohr

IPC: C07D519/00 ,  A61K31/4995 ,  A61K31/517 ,  C07D487/08

Abstract: The present disclosure provides compounds useful for the inhibition of KRAS G12D. The compounds have a general Formula I: (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：US11306107B2

公开(公告)日：2022-04-19

申请号：US16078152

申请日：2017-02-24

Applicant: AMGEN INC.

Inventor： Sean P. Brown ,  David Karl Bedke ,  Michael R. Degraffenreid ,  Jiasheng Fu ,  Zhihong 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.

公开(公告)号：US10300075B2

公开(公告)日：2019-05-28

申请号：US15938001

申请日：2018-03-28

Applicant: AMGEN INC.

Inventor： Sean P. Brown ,  Kexue Li ,  Yunxiao Li ,  Markian M. Stec

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：US11364248B2

公开(公告)日：2022-06-21

申请号：US16638503

申请日：2018-08-17

Applicant: AMGEN INC.

Inventor： Sean P. Brown ,  Kexue Li ,  Yunxiao Li ,  Anthony B. Reed ,  Brian Alan Lanman

IPC: A61K31/553 ,  A61K31/496 ,  A61K31/7068 ,  A61K38/07 ,  C07D513/10

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, 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.