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：US20240417412A1

公开(公告)日：2024-12-19

申请号：US18695688

申请日：2022-08-10

Applicant: AMGEN INC.

Inventor： Brian Alan Lanman ,  Wei Zhao ,  Ryan Paul Wurz ,  Primali Vasundera NAVARATNE ,  Liping PETTUS ,  Michael M. YAMANO ,  Ning Chen ,  Rene RAHIMOFF ,  Francesco MANONI ,  John STELLWAGEN

IPC: C07D519/00 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/553

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：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.