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：US11096939B2

公开(公告)日：2021-08-24

申请号：US16428163

申请日：2019-05-31

Applicant: Amgen Inc.

Inventor： Shon Booker ,  John Gordon Allen ,  Brian Alan Lanman ,  Ryan Paul Wurz ,  Ning Chen ,  Victor J. Cee ,  Patricia Lopez ,  Aaron C. Siegmund ,  Michael D. Bartberger

IPC: C07D471/04 ,  A61K31/497 ,  C07K16/28

Abstract: Provided herein are KRAS G12C inhibitors, such as composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

公开(公告)号：US11905281B2

公开(公告)日：2024-02-20

申请号：US17031607

申请日：2020-09-24

Applicant: Amgen Inc.

Inventor： Brian Alan Lanman ,  Jian Chen ,  Anthony B. Reed ,  Victor J. Cee ,  Longbin Liu ,  David John Kopecky ,  Patricia Lopez ,  Ryan Paul Wurz ,  Thomas T. Nguyen ,  Shon Booker ,  Nobuko Nishimura ,  Youngsook Shin ,  Nuria A. Tamayo ,  John Gordon Allen ,  Jennifer Rebecca Allen

IPC: C07D471/04 ,  C07D213/82 ,  C07D417/04 ,  A61K38/07 ,  C07D487/08 ,  C07D417/12 ,  C07D513/04 ,  C07D487/10 ,  C07D487/04 ,  C07D401/04 ,  C07D239/80 ,  C07D401/14 ,  C07D237/34 ,  C07D403/04 ,  A61K31/496 ,  A61K31/416 ,  A61K31/55 ,  A61K31/454 ,  A61K31/519 ,  A61K31/502 ,  A61K31/517 ,  A61K31/5025 ,  A61P35/00 ,  A61K31/7068 ,  C07D275/04 ,  C07D475/00

CPC classification number: C07D417/04 ,  A61K31/416 ,  A61K31/454 ,  A61K31/496 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/517 ,  A61K31/519 ,  A61K31/55 ,  A61K31/7068 ,  A61K38/07 ,  A61P35/00 ,  C07D237/34 ,  C07D239/80 ,  C07D275/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D417/12 ,  C07D471/04 ,  C07D475/00 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D513/04

Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

公开(公告)号：US11045484B2

公开(公告)日：2021-06-29

申请号：US16402589

申请日：2019-05-03

Applicant: Amgen Inc.

Inventor： Ryan Paul Wurz ,  Victor J. Cee ,  Albert Amegadzie ,  Ning Chen ,  Brian Alan Lanman ,  Michael D. Bartberger

IPC: A61K31/675 ,  A61P35/00 ,  A61K31/167 ,  A61K31/553 ,  C07K16/30 ,  A61K45/06

Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

公开(公告)号：US20250163064A1

公开(公告)日：2025-05-22

申请号：US18838954

申请日：2023-02-15

Applicant: AMGEN INC.

Inventor： Brian Alan Lanman ,  Ryan Paul Wurz ,  Wei Zhao ,  Xiaofen LI ,  Michael YAMANO ,  Imelda HOT ,  Rene RAHIMOFF ,  Liping Pettus ,  Jose Medina

IPC: C07D487/04 ,  A61K31/517 ,  A61K31/519 ,  A61K31/55 ,  A61K31/553 ,  A61K31/554 ,  C07D519/00

Abstract: The present disclosure provides compounds useful for the inhibition of KRAS G12D, G12V, G12A, G12S or G12C. 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：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：US12083121B2

公开(公告)日：2024-09-10

申请号：US17579359

申请日：2022-01-19

Applicant: AMGEN INC.

Inventor： John Gordon Allen ,  Brian Alan Lanman ,  Jian Chen ,  Anthony B. Reed ,  Victor J. Cee ,  Longbin Liu ,  Patricia Lopez ,  Ryan Paul Wurz ,  Thomas T. Nguyen ,  Shon Booker ,  Jennifer Rebecca Allen ,  Margaret Chu-Moyer ,  Albert Amegadzie ,  Ning Chen ,  Clifford Goodman ,  Jonathan D. Low ,  Vu Van Ma ,  Ana Elena Minatti ,  Nobuko Nishimura ,  Alexander J. Pickrell ,  Hui-Ling Wang ,  Youngsook Shin ,  Aaron C. Siegmund ,  Kevin C. Yang ,  Nuria A. Tamayo ,  Mary Walton ,  Qiufen Xue

IPC: C07D241/04 ,  A61K31/519 ,  A61K31/551 ,  A61K39/395 ,  A61P35/00

CPC classification number: A61K31/519 ,  A61K31/551 ,  A61K39/39558 ,  A61P35/00

Abstract: Provided herein are KRAS G12C inhibitors, such as




composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

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：US11766436B2

公开(公告)日：2023-09-26

申请号：US17363878

申请日：2021-06-30

Applicant: Amgen Inc.

Inventor： John Gordon Allen ,  Jennifer Rebecca Allen ,  Ana Elena Minatti ,  Qiufen Xue ,  Ryan Paul Wurz ,  Christopher M. Tegley ,  Alexander J. Pickrell ,  Thomas T. Nguyen ,  Vu Van Ma ,  Patricia Lopez ,  Longbin Liu ,  David John Kopecky ,  Michael J. Frohn ,  Ning Chen ,  Jian Jeffrey Chen ,  Aaron C. Siegmund ,  Albert Amegadzie ,  Nuria A. Tamayo ,  Shon Booker ,  Clifford Goodman ,  Mary Walton ,  Nobuko Nishimura ,  Youngsook Shin ,  Jonathan D. Low ,  Victor J. Cee ,  Anthony B. Reed ,  Hui-Ling Wang ,  Brian Alan Lanman

IPC: A61K31/517 ,  A61P35/00 ,  A61K31/4985 ,  A61K39/395 ,  C07D403/04 ,  C07D471/04

CPC classification number: A61K31/517 ,  A61K31/4985 ,  A61K39/39558 ,  A61P35/00 ,  C07D403/04 ,  C07D471/04

Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.