公开(公告)号：US20250129072A1

公开(公告)日：2025-04-24

申请号：US18987521

申请日：2024-12-19

Applicant: AMGEN INC.

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

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-isopropyl-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

公开(公告)号：US20210346513A1

公开(公告)日：2021-11-11

申请号：US16636325

申请日：2018-08-03

Applicant: AMGEN INC.

Inventor： Michal ACHMATOWICZ ,  Dante ROMANINI ,  James R. FALSEY ,  Bradley J. HERBERICH ,  Oliver R. THIEL

IPC: A61K47/68 ,  C07K16/28 ,  C07K14/605

Abstract: The present disclosure relates to a method of capping, reducing, and oxidizing cys-mAbs in order to provide homogenous material for subsequent conjugation reactions. The present method demonstrates robust ways to manufacture conjugates of cysteine-engineered antibodies that offer high yield and consistent product quality.

公开(公告)号：US20240025896A1

公开(公告)日：2024-01-25

申请号：US18253285

申请日：2021-11-19

Applicant: AMGEN INC.

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

IPC: C07D471/04

CPC classification number: 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-isopropyl-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：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).