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：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：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：US20240327384A1

公开(公告)日：2024-10-03

申请号：US18580564

申请日：2022-07-21

Applicant: Amgen Inc.

Inventor： Tian WU ,  Prashant AGARWAL ,  Andreas R. ROTHELI ,  Hyunsoo PARK ,  Michael J. FROHN

IPC: C07D401/14 ,  A61K31/506 ,  C07C15/06 ,  C07C31/02 ,  C07C31/04 ,  C07C31/08 ,  C07C43/04 ,  C07C43/18 ,  C07C49/08 ,  C07C55/02 ,  C07C55/22 ,  C07C69/003 ,  C07C233/05 ,  C07C255/03 ,  C07C275/06 ,  C07C309/04 ,  C07C309/65 ,  C07C309/73 ,  C07D211/90 ,  C07D275/06 ,  C07D307/06 ,  C07D319/12 ,  C07D487/04

CPC classification number: C07D401/14 ,  A61K31/506 ,  C07C15/06 ,  C07C31/02 ,  C07C31/04 ,  C07C31/08 ,  C07C43/046 ,  C07C43/18 ,  C07C49/08 ,  C07C55/02 ,  C07C55/22 ,  C07C69/003 ,  C07C233/05 ,  C07C255/03 ,  C07C275/06 ,  C07C309/04 ,  C07C309/65 ,  C07C309/73 ,  C07D211/90 ,  C07D275/06 ,  C07D307/06 ,  C07D319/12 ,  C07D487/04 ,  C07B2200/13 ,  C07C2601/08

Abstract: Disclosed herein is a salt, a crystalline anhydrous form, a hydrate, a solvate, or a co-crystal of a free base compound 2-(6-azaspiro[2.5]octan-6-yl)-N-[2-(4,4-difluoropiperidin-1-yl)-6-methylpyrimidin-4-yl]-4-[(2-hydroxyethanesulfonyl)amino]benzamide (Compound A); method of preparation, pharmaceutical compositions, and method of treating a disease mediated by a motor protein kinesin family member 18A (KIF18A) inhibition, wherein said disease is a neoplastic disease, including a cancer or a tumor.