公开(公告)号：US20250129050A1

公开(公告)日：2025-04-24

申请号：US18832887

申请日：2023-01-26

Applicant: Amgen Inc.

Inventor： Sebastien CAILLE ,  Daniel Gerard GREENE ,  Michael Thomas CORBETT ,  Carolyn WEI

IPC: C07D401/14 ,  C07D221/20 ,  C07F3/00

Abstract: The present invention relates to improved preparation of a KIF18A inhibitor having the chemical structure Compound (1), or a salt thereof Compound (la); wherein HA is as defined herein; and key intermediates thereof, i.e., Compound (2a), Compound (3a), Compound (5) or a salt thereof, and Compound (6a) or a hydrate thereof, of the formulae: Compound (2a); Compound (3a); Compound (5) or a salt thereof; and Compound (6a) or a hydrate thereof, preferably Compound (6a-1). The present invention further relates to solid form of Compound (6a), preferably the crystalline hydrate form of Compound (6a-1).

公开(公告)号：US20220298099A1

公开(公告)日：2022-09-22

申请号：US17690729

申请日：2022-03-09

Applicant: Amgen Inc.

Inventor： Sebastien CAILLE ,  James MURRAY ,  Kyle QUASDORF ,  Hannah NGUYEN ,  Maria Victoria SILVA ELIPE ,  Ari Elizabeth ERICSON

IPC: C07C201/08

Abstract: Provided herein are synthetic methods for the preparation of intermediates that are utilized in the synthesis of omecamtiv mecarbil dihydrochloride.

公开(公告)号：US20200281912A1

公开(公告)日：2020-09-10

申请号：US16664103

申请日：2019-10-25

Applicant: AMGEN INC.

Inventor： Matthew BIO ,  Sebastien CAILLE ,  Brian COCHRAN ,  Yuanqing FANG ,  Brian M. FOX ,  Brian S. LUCAS ,  Lawrence R. MCGEE ,  Filisaty VOUNTSOS ,  Sean H. WIEDEMANN ,  Sarah WORTMAN

IPC: A61K31/451 ,  C07D211/94 ,  C07D491/048 ,  C07C309/25 ,  C07C309/04 ,  C07C313/02 ,  C07C309/35 ,  C07D498/04 ,  C07D211/76

Abstract: The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

公开(公告)号：US20160289243A1

公开(公告)日：2016-10-06

申请号：US15175805

申请日：2016-06-07

Applicant: AMGEN INC.

Inventor： Matthew BIO ,  Sebastien CAILLE ,  Yuanqing FANG ,  Brian M. FOX ,  Brian S. LUCAS ,  Lawrence R. McGEE ,  Sean H. WIEDEMANN

IPC: C07D498/04 ,  C07C309/35

CPC classification number: A61K31/451 ,  C07B2200/13 ,  C07C309/04 ,  C07C309/25 ,  C07C309/35 ,  C07C313/02 ,  C07D211/76 ,  C07D211/94 ,  C07D491/048 ,  C07D498/04

Abstract: The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

公开(公告)号：US20160289178A1

公开(公告)日：2016-10-06

申请号：US15175821

申请日：2016-06-07

Applicant: AMGEN INC.

Inventor： Sebastien CAILLE ,  Filisaty VOUNATSOS

IPC: C07C309/04

CPC classification number: A61K31/451 ,  C07B2200/13 ,  C07C309/04 ,  C07C309/25 ,  C07C309/35 ,  C07C313/02 ,  C07D211/76 ,  C07D211/94 ,  C07D491/048 ,  C07D498/04

Abstract: The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

公开(公告)号：US20140364455A1

公开(公告)日：2014-12-11

申请号：US14301087

申请日：2014-06-10

Applicant: AMGEN INC.

Inventor： Matthew BIO ,  Sebastien CAILLE ,  Brian COCHRAN ,  Yuanqing FANG ,  Brian M. FOX ,  Brian S. LUCAS ,  Lawrence R. McGEE ,  Filisaty VOUNATSOS ,  Sean WIEDEMANN ,  Sarah WORTMAN

IPC: C07D211/94 ,  C07C309/25 ,  C07C309/04 ,  C07D491/048

CPC classification number: A61K31/451 ,  C07B2200/13 ,  C07C309/04 ,  C07C309/25 ,  C07C309/35 ,  C07C313/02 ,  C07D211/76 ,  C07D211/94 ,  C07D491/048 ,  C07D498/04

Abstract: The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

Abstract translation: 本发明提供了制备2 - （（3R，5R，6S）-5-（3-氯苯基）-6-（4-氯苯基）-1 - （（S）-1-（异丙基磺酰基）-3-甲基丁基 -2-基）-3-甲基-2-氧代哌啶-3-基）乙酸，以及制备中间体的中间体和方法。 还提供了化合物和中间体的晶型。