公开(公告)号：US20230357137A1

公开(公告)日：2023-11-09

申请号：US17923015

申请日：2021-04-28

Applicant: AMGEN INC.

Inventor： Neil Fred LANGILLE ,  Jason S. TEDROW ,  Jonathan Vinh-Phu TRUONG ,  Robert Ronald MILBURN ,  Alessandro ARENA

IPC: C07C303/36 ,  C07D513/06 ,  C07D519/00 ,  C07C67/08 ,  C07D301/24 ,  C07C29/62 ,  C07C303/28 ,  C07D213/70 ,  C07D213/71

CPC classification number: C07C303/36 ,  C07D513/06 ,  C07D519/00 ,  C07C67/08 ,  C07D301/24 ,  C07C29/62 ,  C07C303/28 ,  C07D213/70 ,  C07D213/71 ,  C07B2200/13

Abstract: Provided herein are processes for synthesizing mcl-1 inhibitors and intermediates such as compound Z that can be used to prepare them. In particular, provided herein are processes for synthesizing compound A1, and salts or solvates thereof and compound A2, and salts and solvates thereof.

公开(公告)号：US20230183164A1

公开(公告)日：2023-06-15

申请号：US17920084

申请日：2021-05-04

Applicant: AMGEN INC.

Inventor： Austin G. SMITH ,  Michael T. CORBETT ,  Neil Fred LANGILLE ,  Kyle D. BAUCOM ,  Peter K. DORNAN ,  Gabrielle ST- PIERRE ,  Philipp C. ROOSEN ,  Sheng CUI ,  Roberto PROFETA

IPC: C07C67/62 ,  C07D249/18 ,  C07D519/00 ,  C07D513/08

CPC classification number: C07C67/62 ,  C07D249/18 ,  C07D519/00 ,  C07D513/08 ,  C07B2200/13

Abstract: Provided herein are processes for synthesizing intermediates useful in preparing Mcl-1 inhibitors. In particular, provided herein are processes for synthesizing compound F, or a salt thereof, wherein R1 and OPG2 are described herein. Compound F can be useful in synthesizing compound A1, or a salt of solvate thereof, and compound A2, or a salt of solvate thereof.

公开(公告)号：US20230117777A1

公开(公告)日：2023-04-20

申请号：US17910042

申请日：2021-03-30

Applicant: Amgen Inc.

Inventor： Michal ACHMATOWICZ ,  Sheng CUI ,  Tsang-Lin HWANG ,  Neil Fred LANGILLE ,  Janine K. TOM ,  James E. HUCKLE ,  Markian STEC ,  Tian WU ,  Sean P. BROWN

IPC: C07D519/00

Abstract: Disclosed herein is an improved process for the synthesis of compound (A): (A), or a salt or solvate thereof via methylation of compound (B): (B), or a salt or solvate thereof, a crystalline hydrate of compound A, and pharmaceutical formulations comprising a crystalline hydrate of compound (A).