公开(公告)号：US20240317715A1

公开(公告)日：2024-09-26

申请号：US18680558

申请日：2024-05-31

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：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：US20240124442A1

公开(公告)日：2024-04-18

申请号：US18264216

申请日：2022-02-03

Applicant: AMGEN INC.

Inventor： Albert AMEGADZIE ,  Diane Jennifer BEYLKIN ,  Shon BOOKER ,  Matthew Paul BOURBEAU ,  John R. BUTLER ,  Kevin Lloyd GREENMAN ,  Todd J. KOHN ,  Kexue LI ,  Qingyian LIU ,  Ana Elena MINATTI ,  Primali Vasundera NAVARATNE ,  Liping H. PETTUS ,  Rene RAHIMOFF ,  Hui-Ling WANG ,  Nicholas Anthony WEIRES

IPC: C07D471/04 ,  A61P35/00 ,  C07D471/14 ,  C07D491/048 ,  C07D491/147 ,  C07D495/04 ,  C07D498/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61P35/00 ,  C07D471/14 ,  C07D491/048 ,  C07D491/147 ,  C07D495/04 ,  C07D498/04 ,  C07D519/00

Abstract: Described herein are novel PRMT5 inhibitors of Formula I and pharmaceutically acceptable salts thereof, as well as the pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, metabolic and blood disorders. Compounds of Formula I have the following structure:

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：US20200239441A1

公开(公告)日：2020-07-30

申请号：US16724119

申请日：2019-12-20

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

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：US20140350244A1

公开(公告)日：2014-11-27

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

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。