公开(公告)号：US20220235045A1

公开(公告)日：2022-07-28

申请号：US17612717

申请日：2020-05-20

Applicant: Amgen Inc.

Inventor： Mary CHAVES ,  Ron C. KELLY ,  Prashant AGARWAL ,  Stephan D. PARENT ,  Darren Leonard REID ,  Roman SHIMANOVICH

IPC: C07D471/04 ,  A61P35/00

Abstract: The present invention provides a crystalline form and stable salts of 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(2-propanyl)-3-pyridinyl)-4-((2S)-2-methyl-4-(2-propenoyl)-1- piperazinyl)pyrido[2,3-d]pyrimidin-2(1H)-one, including several hydrochloride salt forms, phosphate salt form, mesylate salt form, and solid state forms thereof, pharmaceutical compositions, and methods of treating a disease mediated by KRAS G12C inhibition.

公开(公告)号：US20170029443A1

公开(公告)日：2017-02-02

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 ,  C07C275/02 ,  C07C57/10 ,  C07C55/12 ,  C07C57/145 ,  C07C55/10

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.

Abstract translation: 本文提供了可用于治疗，预防或改善癌症的化合物的新型多晶型物和共晶体。 特别地，本发明提供了6 - {（1R）-1- [8-氟-6-（1-甲基-1H-吡唑-4-基）[1,2,4]三唑并[ 4,3-a]吡啶-3-基]乙基} -3-（2-甲氧基乙氧基）-1,6-萘啶-5（6H） - 酮，其是c-Met的抑制剂。

公开(公告)号：US20240067647A1

公开(公告)日：2024-02-29

申请号：US18382927

申请日：2023-10-23

Applicant: AMGEN INC.

Inventor： Mary CHAVES ,  Patricia LOPEZ ,  Prashant AGARWAL ,  Albert AMEGADZIE ,  Stephanie AZALI ,  Roman SHIMANOVICH ,  Ron C. KELLY ,  Darren Leonard REID

IPC: C07D471/04

CPC classification number: C07D471/04 ,  C07B2200/13

Abstract: The present disclosure provides crystalline and amorphous forms of 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(2-propanyl)-3-pyridinyl)-4-((2S)-2-methyl-4-(2-propenoyl)-1-piperazinyl)pyrido[2,3-d]pyrimidin-2(1H)-one, including several anhydrous, hydrate and solvate forms, and solid state forms thereof, pharmaceutical compositions, and methods of treating a disease mediated by KRAS G12C inhibition.

公开(公告)号：US20220106313A1

公开(公告)日：2022-04-07

申请号：US17553598

申请日：2021-12-16

Applicant: AMGEN INC.

Inventor： Mary CHAVES ,  Patricia LOPEZ ,  Prashant AGARWAL ,  Albert AMEGADZIE ,  Stephanie AZALI ,  Roman SHIMANOVICH ,  Ron C. KELLY ,  Darren Leonard REID

IPC: C07D471/04

Abstract: The present disclosure provides crystalline and amorphous forms of 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(2-propanyl)-3-pyridinyl)-4-((2S)-2-methyl-4-(2-propenoyl)-1-piperazinyl)pyrido[2,3-d]pyrimidin-2(1H)-one, including several anhydrous, hydrate and solvate forms, and solid state forms thereof, pharmaceutical compositions, and methods of treating a disease mediated by KRAS G12C inhibition.

公开(公告)号：US20200369662A1

公开(公告)日：2020-11-26

申请号：US16878824

申请日：2020-05-20

Applicant: AMGEN INC.

Inventor： Mary CHAVES ,  Patricia LOPEZ ,  Prashant AGARWAL ,  Albert AMEGADZIE ,  Stephanie AZALI ,  Roman SHIMANOVICH ,  Ron C. KELLY ,  Darren Leonard REID

IPC: C07D471/04

Abstract: The present disclosure provides crystalline and amorphous forms of 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(2-propanyl)-3-pyridinyl)-4-((2S)-2-methyl-4-(2-propenoyl)-1-piperazinyl)pyrido[2,3-d]pyrimidin-2(1H)-one, including several anhydrous, hydrate and solvate forms, and solid state forms thereof, pharmaceutical compositions, and methods of treating a disease mediated by KRAS G12C inhibition.

公开(公告)号：US20180244696A1

公开(公告)日：2018-08-30

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 ,  C07C57/145 ,  C07C57/10 ,  C07C55/12 ,  C07C55/10 ,  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.