公开(公告)号：US09296735B2

公开(公告)日：2016-03-29

申请号：US14402069

申请日：2013-05-17

Applicant: AMGEN INC.

Inventor： Eric A. Bercot ,  Matthew Bio ,  Johann Chan ,  John Colyer ,  Yuanqing Fang ,  Steven Mennen ,  Robert R. Milburn ,  Jason Tedrow ,  Babak Riahi

IPC: C07D285/08 ,  C07D417/04 ,  C07D317/26

CPC classification number: C07D317/26 ,  C07D317/72 ,  C07D417/04

Abstract: The present invention relates to processes for preparing protected glyceraldehydes, such as (hydroxy)methanesulfonates. In addition, the invention relates to thiadiazoles, particularly 3-diooxolanyl-thiadiazoles.

Abstract translation: 本发明涉及制备受保护的甘油醛，例如（羟基）甲磺酸酯的方法。 此外，本发明涉及噻二唑，特别是3-二氧杂环戊烷基 - 噻二唑。

公开(公告)号：US20150141655A1

公开(公告)日：2015-05-21

申请号：US14402069

申请日：2013-05-17

Applicant: AMGEN INC.

Inventor： Eric A. Bercot ,  Matthew Bio ,  Johann Chan ,  John Colyer ,  Yuanqing Fang ,  Steven Mennen ,  Robert R. Milburn ,  Jason Tedrow ,  Babak Riahi

IPC: C07D417/04 ,  C07D317/26

CPC classification number: C07D317/26 ,  C07D317/72 ,  C07D417/04

Abstract: The present invention relates to processes for preparing protected glyceraldehydes, such as (hydroxy)methanesulfonates. In addition, the invention relates to thiadiazoles, particularly 3-diooxolanyl-thiadiazoles.

Abstract translation: 本发明涉及制备受保护的甘油醛，例如（羟基）甲磺酸盐的方法。 此外，本发明涉及噻二唑，特别是3-二氧杂环戊烷基 - 噻二唑。

公开(公告)号：US09855259B2

公开(公告)日：2018-01-02

申请号：US15163186

申请日：2016-05-24

Applicant: AMGEN INC.

Inventor： Matthew Bio ,  Sebastien Caille ,  Brian Cochran ,  Yuanqing Fang ,  Filisaty Vounatsos ,  Sarah Wortman

IPC: C07D211/76 ,  A61K31/451 ,  C07D211/94 ,  C07D491/048 ,  C07C309/25 ,  C07C309/04 ,  C07C313/02 ,  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：US09376386B2

公开(公告)日：2016-06-28

申请号：US14301087

申请日：2014-06-10

Applicant: AMGEN INC.

Inventor： Matthew Bio ,  Sebastien Caille ,  Brian Cochran ,  Yuanqing Fang ,  Filisaty Vounatsos ,  Sarah Wortman

IPC: C07D211/94 ,  C07D491/048 ,  C07C309/25 ,  C07C309/04 ,  C07D498/04 ,  C07D211/76 ,  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.

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。

公开(公告)号：US09801867B2

公开(公告)日：2017-10-31

申请号：US15175824

申请日：2016-06-07

Applicant: AMGEN INC.

Inventor： Matthew Bio ,  Sebastien Caille ,  Brian Cochran ,  Yuanqing Fang ,  Brian M. Fox ,  Brian S. Lucas ,  Lawrence R. McGee ,  Filisaty Vounatsos ,  Sean H. Wiedemann ,  Sarah Wortman

IPC: C07D211/76 ,  A61K31/451 ,  C07D211/94 ,  C07D491/048 ,  C07C309/25 ,  C07C309/04 ,  C07C313/02 ,  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：US09623018B2

公开(公告)日：2017-04-18

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 ,  A61K31/451 ,  C07D211/94 ,  C07D491/048 ,  C07C309/25 ,  C07C309/04 ,  C07D211/76 ,  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.