公开(公告)号：US10344041B2

公开(公告)日：2019-07-09

申请号：US15966157

申请日：2018-04-30

Applicant: AMGEN, INC.

Inventor： David Bauer ,  Matthew Bio ,  Melanie Cooke ,  Katrina W. Copeland ,  Matthew Peterson ,  Michele Potashman ,  Roman Shimanovich ,  Helming Tan

IPC: C07D519/00 ,  A61K31/52 ,  C07C55/10 ,  C07C55/12 ,  C07C57/10 ,  C07C57/145 ,  C07C275/02

Abstract: Provided herein are novel polymorphic forms and co-crystals of a compound useful in the treatment, prevention, or amelioration of cancer. In particular, the invention provides polymorphs and co-crystals of 6-{(1R)-1-[8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl}-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one, which is an inhibitor of c-Met.

公开(公告)号：US10053452B2

公开(公告)日：2018-08-21

申请号：US15101373

申请日：2014-11-25

Applicant: AMGEN INC.

Inventor： Mary Chaves ,  Matthew Bio ,  Matthew Peterson

IPC: C07D409/14 ,  A61K31/506 ,  C07C309/04 ,  C07C309/30

CPC classification number: C07D409/14 ,  C07B2200/13 ,  C07C309/04 ,  C07C309/30

Abstract: The present invention relates to crystalline forms and co-crystal forms of pharmaceutically acceptable salts of the compound, N-(4-((3-(2-amino-4-pyrimidinyl)-2-pyridinyl)oxy)phenyl)-4-(4-methyl-2-thienyl)-1-phthalazinamine (AMG 900, and pharmaceutical compositions comprising said crystalline and co-crystal forms thereof. The invention further provides uses of the crystalline forms and compositions, to treat cancer, including various types of solid tumors and hematologic cancer including myeloma and leukemia.

公开(公告)号：US09981988B2

公开(公告)日：2018-05-29

申请号：US15293511

申请日：2016-10-14

Applicant: AMGEN, INC.

Inventor： David Bauer ,  Matthew Bio ,  Melanie Cooke ,  Katrina W. Copeland ,  Matthew Peterson ,  Michele Potashman ,  Roman Shimanovich ,  Helming Tan

IPC: C07D519/00 ,  A61K31/52 ,  C07C55/10 ,  C07C55/12 ,  C07C57/10 ,  C07C57/145 ,  C07C275/02

CPC classification number: C07D519/00 ,  A61K31/52 ,  C07B2200/13 ,  C07C55/10 ,  C07C55/12 ,  C07C57/10 ,  C07C57/145 ,  C07C275/02

Abstract: Provided herein are novel polymorphic forms and co-crystals of a compound useful in the treatment, prevention, or amelioration of cancer. In particular, the invention provides polymorphs and co-crystals of 6-{(1R)-1-[8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl}-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one, which is an inhibitor of c-Met.

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：US09643984B2

公开(公告)日：2017-05-09

申请号：US14900976

申请日：2014-06-24

Applicant: AMGEN, INC.

Inventor： Matthew Bio ,  Eric Fang ,  Jacqueline E. Milne ,  Sean Wiedemann ,  Ash Wilsily

IPC: C07D471/04 ,  C07D519/00

CPC classification number: C07D519/00 ,  C07D471/04

Abstract: Disclosed herein are methods for preparing [1,2,4]triazolo[4,3-a]pyridines, particularly (R)-6-(1-(8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one, and precursors thereof, such as a method comprising reacting (R)—N-(3-fluoro-5-(1methyl-1H-pyrazol-4-yl) pyridin-2-yl)-2-(3-(2-methoxyethoxy)-5-oxo-1,6-naphthyridin-6(5H)yl) propanehydrazide (“HYDZ”): (HYDZ) under conditions sufficient to form (R)-6-(1-(8-fluoro-6-(1-methyl-IH-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (“A”): (A)

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.