公开(公告)号：US20250115622A1

公开(公告)日：2025-04-10

申请号：US18730357

申请日：2023-02-03

Applicant: AMGEN INC.

Inventor： Ron C. Kelly ,  Mary Chaves ,  Jing Teng ,  Stephan Parent ,  Markian Stec ,  Van Luu ,  Robert P. Farrell ,  James E. Huckle ,  Michal Achmatowicz ,  Tian Wu ,  Darren Leonard Reid ,  Lingyun Xiao

IPC: C07D519/00 ,  A61K31/553

Abstract: Disclosed herein are crystalline forms of (4S,7aR,9aR,10R,11E,14S,15R)-6′-chloro-10-methoxy-14,15-dimethyl-10-{[(9aR)-octahydro-2H-pyrido[1,2-a]pyrazin-2-yl]methyl}-3′,4′,7a,8,9,9a,10,13,14,15-decahydro-2′H,3H,5H-spiro[1,19-etheno-1616-cyclobuta[i] [1,4]oxazepino[3,4-f][1,2,7]thiadiazacyclohexadecine-4,1′-naphthalene]-16,16,18(7H,17H)-trione (AMG 397): (AMG 397), hydrates, and solvates thereof. Also disclosed are methods of making the crystalline forms, and methods of treating diseases and disorders with the crystalline forms.

公开(公告)号：US11236091B2

公开(公告)日：2022-02-01

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：US20240013869A1

公开(公告)日：2024-01-11

申请号：US18025311

申请日：2021-08-30

Applicant: AMGEN INC.

Inventor： Ron Christopher Kelly ,  Mary Chaves ,  Marc A. Caporini ,  Fabrice Schlegel

IPC: G16C60/00 ,  G16C20/70 ,  G16C20/80

CPC classification number: G16C60/00 ,  G16C20/70 ,  G16C20/80

Abstract: A method of computational modeling to predict stability of a lyophilized drug product includes receiving model parameters describing a virtual cake, a virtual vial, a virtual stopper, and a virtual ambient environment. The method also includes computing, by implementing a computational model and at each of a plurality of virtual time steps, a change in water amount or concentration in the virtual cake, virtual air within the virtual vial, and the virtual stopper, in part by applying the model parameters to the computational model. The method also includes generating information for display to a user via a user interface.

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：US20250122224A1

公开(公告)日：2025-04-17

申请号：US18730353

申请日：2023-02-03

Applicant: AMGEN INC.

Inventor： Ron C. Kelly ,  Mary Chaves ,  Jing Teng ,  Stephan Parent ,  Van Luu ,  Robert P. Farrell ,  James E. Huckle ,  Michal Achmatowicz ,  Tian Wu ,  Darren Leonard Reid ,  Lingyun Xiao

IPC: C07D519/00 ,  A61K31/553

Abstract: Disclosed herein are salt and solvate forms of (4S,7aR,9aR,10R,11E,14S,15R)-6′-chloro-10-methoxy-14,15-dimethyl-10-{[(9aR)-octahydro-2H-pyrido[1,2-a]pyrazin-2-yl]methyl}-3′,4′,7a,8,9,9a,10,13,14,15-decahydro-2′H,3H,5H-spiro[1,19-etheno-16,16-cyclobuta[i][1,4]oxazepino[3,4-f][1,2,7]thiadlazacyclohexadecine-4,1 naphthalene]-16,16,18 (7H,17H)-trione (AMG 397): (AMG 397), such as crystalline salt and solvate forms thereof. Also disclosed are methods of making the salt and solvate forms, and methods of treating diseases and disorders with the salt and solvate forms.

公开(公告)号：US12187700B2

公开(公告)日：2025-01-07

申请号：US17593110

申请日：2020-03-12

Applicant: Amgen Inc. ,  Cytokinetics, Inc.

Inventor： Stephanie Azali ,  Mary Chaves ,  Ron C. Kelly ,  Steven M. Mennen ,  Darren L Reid ,  Osama Suleiman ,  Ashraf Wilsily ,  Mark Wright

IPC: C07D401/06

Abstract: Provided herein are free base crystalline forms, crystalline salts, solvates, amorphous free base, and cocrystals of Compound A.

公开(公告)号：US12252486B2

公开(公告)日：2025-03-18

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：US20240140966A1

公开(公告)日：2024-05-02

申请号：US18296211

申请日：2023-04-05

Applicant: AMGEN INC.

Inventor： Yosup Rew ,  Van Luu ,  Manuel Zancanella ,  Mary Chaves

IPC: C07D513/10

CPC classification number: C07D513/10

Abstract: Disclosed herein are crystalline and amorphous forms of (1S,3′R,6′R,7′S,8′E,11′S,12′R)-6-chloro-7′-methoxy-11′,12′-dimethyl-3,4-dihydro-2H, 15′H-spiro[naphthalene-1,22′-[20]oxa[13]thia[1,14]diazatetracyclo[14.7.2.03,6,019,24]pentacosa[8,16,18,24]tetraen]-15′-one 13′,13′-dioxide (AMG 176):




and salts and hydrates thereof. Also disclosed are methods of making the crystalline and amorphous forms, and methods of treating diseases and disorders with the crystalline and amorphous forms.

公开(公告)号：US11827635B2

公开(公告)日：2023-11-28

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

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.