公开(公告)号：WO2021097212A1

公开(公告)日：2021-05-20

申请号：PCT/US2020/060421

申请日：2020-11-13

Applicant: AMGEN INC.

Inventor： PARSONS, Andrew T. ,  BEAVER, Matthew

IPC: C07D471/04 ,  C07F5/02 ,  C07F5/05

Abstract: The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2,2',2"-(1,3,5,2,4,6-trioxatriborinane-2,4,6-triyl)tris(3-fluorophenol), useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

公开(公告)号：WO2022076623A1

公开(公告)日：2022-04-14

申请号：PCT/US2021/053859

申请日：2021-10-06

Applicant: AMGEN INC.

Inventor： BEAVER, Matthew G. ,  CORBETT, Michael T. ,  FANG, Yuanqing ,  FORD, David D. ,  PARSONS, Andrew T. ,  ST-PIERRE, Gabrielle ,  TELMESANI, Reem

IPC: C07D471/04

Abstract: Provided herein is a process comprising heating a composition comprising (P)-compound A or a salt thereof and a solvent to a temperature of 250°C to 350°C to form racemized compound A. Also provided is a process for isolating (P)-compound A from a composition comprising (P)‑compound A and a tartrate, as described herein. Further provided herein, is a process for isolating a free acid of a tartrate or a hydrate thereof from a composition comprising a tartrate, (P)‑compound A, and an organic solvent. [Insert Structure] (A).

公开(公告)号：WO2022109242A1

公开(公告)日：2022-05-27

申请号：PCT/US2021/060048

申请日：2021-11-19

Applicant: AMGEN INC.

Inventor： ACHMATOWICZ, Michal ,  COYLER, John T. ,  CORBETT, Michael T. ,  GRIFFIN, Daniel J. ,  PARSONS, Andrew T. ,  ROBINSON, Joanna ,  QUASDORF, Kyle

IPC: C07D471/04

Abstract: Provided herein is a process for preparing compound A comprising (a) admixing 2-isopropyl-4-methylpyridin-3-amine (Compound B), or a salt thereof, a first base, and a reactive compound comprising phosgene or a phosgene equivalent in an organic solvent to form 3‑isocyanato-2-isopropyl-4-methylpyridine (Compound C); (b) admixing Compound C and 2,6-dichloro-5-fluoronicotinamide (Compound D) to form 2,6-dichloro-5-fluoro-N-((2-isopropy1-4-methylpyridin-3-yl)carbamoyl)nicotinamide (Compound E); and (c) admixing Compound E and a second base to form a product mixture comprising Compound A and the second base. Also provided herein is a process for synthesizing AMG 510 comprising using Compound A prepared according to the disclosed processes [Insert Structure] (Compound A).

公开(公告)号：EP4247813A1

公开(公告)日：2023-09-27

申请号：EP21827309.2

申请日：2021-11-19

Applicant: Amgen, Inc

Inventor： ACHMATOWICZ, Michal ,  COYLER, John T. ,  CORBETT, Michael T. ,  GRIFFIN, Daniel J. ,  PARSONS, Andrew T. ,  ROBINSON, Joanna ,  QUASDORF, Kyle

IPC: C07D471/04

公开(公告)号：EP4225755A1

公开(公告)日：2023-08-16

申请号：EP21802088.1

申请日：2021-10-06

Applicant: Amgen Inc.

Inventor： BEAVER, Matthew G. ,  CORBETT, Michael T. ,  FANG, Yuanqing ,  FORD, David D. ,  PARSONS, Andrew T. ,  ST-PIERRE, Gabrielle ,  TELMESANI, Reem

IPC: C07D471/04

公开(公告)号：EP4058453A1

公开(公告)日：2022-09-21

申请号：EP20821492.4

申请日：2020-11-13

Applicant: Amgen Inc.

Inventor： PARSONS, Andrew T. ,  BEAVER, Matthew

IPC: C07D471/04 ,  C07F5/02 ,  C07F5/05