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：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.

公开(公告)号：US20190381064A1

公开(公告)日：2019-12-19

申请号：US16547747

申请日：2019-08-22

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 ,  A61P35/02 ,  A61P35/00 ,  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：US20240101570A1

公开(公告)日：2024-03-28

申请号：US18255575

申请日：2021-11-22

Applicant: AMGEN INC.

Inventor： Albert AMEGADZIE ,  Diane Jennifer BEYLKIN ,  Shon BOOKER ,  Matthew Paul BOURBEAU ,  John R. BUTLER ,  Sanne Ormholt Schroder GLAD ,  Todd J. KOHN ,  Brian Alan LANMAN ,  Kexue LI ,  Qingyian LIU ,  Patricia LOPEZ ,  Francesco MANONI ,  Primali Vasundera NAVARATNE ,  Liping H. PETTUS ,  Rene RAHIMOFF ,  Nuria A. TAMAYO ,  Mikkel VESTERGAARD ,  Hui-Ling WANG ,  Nicholas Anthony WEIRES

IPC: C07D491/048 ,  A61K35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/147 ,  C07D495/04 ,  C07D498/04 ,  C07D519/00

CPC classification number: C07D491/048 ,  A61K35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/147 ,  C07D495/04 ,  C07D498/04 ,  C07D519/00

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

公开(公告)号：US20230159510A1

公开(公告)日：2023-05-25

申请号：US17799077

申请日：2021-02-11

Applicant: AMGEN INC.

Inventor： Jennifer Rebecca ALLEN ,  Albert AMEGADZIE ,  Diane Jennifer BEYLKIN ,  Shon BOOKER ,  Matthew Paul BOURBEAU ,  John R. BUTLER ,  Michael J. FROHN ,  Sanne Ormholt Schroder GLAD ,  Birgitte Weinreich HUSEMOEN ,  Matthew R. KALLER ,  Todd J. KOHN ,  Brian Alan LANMAN ,  Kexue LI ,  Qingyian LIU ,  Patricia LOPEZ ,  Vu Van MA ,  Francesco MANONI ,  Jose MEDINA ,  Ana Elena MINATTI ,  Jorge PEIRO CADAHIA ,  Liping PETTUS ,  Alexander J. PICKRELL ,  Ian SARVARY ,  Nuria A. TAMAYO ,  Mikkel VESTERGAARD

IPC: C07D413/14 ,  C07D471/04 ,  C07D401/14 ,  C07D401/12 ,  C07D405/14

CPC classification number: C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04

Abstract: Described herein are compounds of Formula I and pharmaceutically acceptable salt thereof, stereoisomers, tautomers as well as 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: (I)

公开(公告)号：US20240409557A1

公开(公告)日：2024-12-12

申请号：US18657114

申请日：2024-05-07

Applicant: AMGEN INC.

Inventor： Kevin Lloyd GREENMAN ,  Alexander J. Pickrell ,  Kexue LI ,  Albert K. AMEGADZIE ,  Hui-Ling WANG ,  Nicholas Anthony WEIRES ,  John G. ALLEN ,  Matthew P. BOURBEAU

IPC: C07D519/00 ,  A61K31/437 ,  A61K31/519 ,  A61P1/04

Abstract: The present disclosure provides novel 15-hydroxy-prostaglandin dehydrogenase inhibitors, pharmaceutical compositions comprising such compounds, and methods of using such compounds and compositions in treating 15-hydroxy-prostaglandin dehydrogenase-mediated disease. Also provided are methods of making such compounds and intermediates thereof. The compounds have a general Formula (A). Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (A).

公开(公告)号：US20220106293A1

公开(公告)日：2022-04-07

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

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：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：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.