公开(公告)号：US20210221771A1

公开(公告)日：2021-07-22

申请号：US17263224

申请日：2019-08-16

Applicant: AMGEN INC. ,  CYTOKINETICS, INC.

Inventor： Henry Morrison ,  Sheng Cui ,  Kyle Quasdorf ,  Evelyn Yanez ,  Bin Peter Quan ,  Ron C. Kelly ,  Sebastien Caille ,  Lingyun Xiao ,  David Pearson ,  Jaclyn Raeburn ,  Ailsa Golightly ,  Bradley Morgan ,  Matthew Peterson ,  Alex Eberlin ,  Alexander Oblezov

IPC: C07D213/75

Abstract: Provided herein are free base crystalline forms, crystalline salts, and an amorphous salts of omecamtiv mecarbil.

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：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.

公开(公告)号：US20240270788A1

公开(公告)日：2024-08-15

申请号：US18603661

申请日：2024-03-13

Applicant: AMGEN INC.

Inventor： Rizwan SHARNEZ ,  William TRIEU ,  Marc A. CAPORINI ,  Ron C. Kelly ,  Neill Burt ,  Laura Nicholson ,  Twinkle R. Christian

IPC: C07K1/30 ,  A61K39/395 ,  B01J8/20 ,  B01J8/38 ,  C30B7/00 ,  C30B7/10 ,  C30B30/00 ,  C30B30/02 ,  C30B30/04 ,  G01N24/00 ,  G01N24/08 ,  G01R33/20 ,  G01R33/46

CPC classification number: C07K1/306 ,  A61K39/39591 ,  B01J8/20 ,  B01J8/38 ,  C30B7/00 ,  C30B7/10 ,  C30B30/04 ,  G01N24/087 ,  C30B30/00 ,  C30B30/02 ,  G01N24/00 ,  G01N24/008 ,  G01R33/20 ,  G01R33/46

Abstract: Disclosed herein are methods of preparing a composition comprising crystalline biomolecules, for example, crystalline antibodies. In exemplary embodiments, the method comprises forming a fluidized bed of crystalline biomolecules using, for example, a counter-flow centrifuge to exchange buffer and/or to concentrate the crystalline biomolecules in a solution. Also provided are methods of detecting crystalline biomolecules and/or amorphous biomolecules in a sample.

公开(公告)号：US11958882B2

公开(公告)日：2024-04-16

申请号：US16494165

申请日：2018-03-14

Applicant: AMGEN INC.

Inventor： Rizwan Sharnez ,  William Trieu ,  Marc A. Caporini ,  Ron C. Kelly ,  Neill Burt ,  Laura Nicholson ,  Twinkle R. Christian

IPC: C30B7/10 ,  A61K39/395 ,  B01J8/20 ,  B01J8/38 ,  C07K1/30 ,  C30B7/00 ,  C30B30/04 ,  G01N24/08 ,  C30B30/00 ,  C30B30/02 ,  G01N24/00 ,  G01R33/20 ,  G01R33/46

CPC classification number: C07K1/306 ,  A61K39/39591 ,  B01J8/20 ,  B01J8/38 ,  C30B7/00 ,  C30B7/10 ,  C30B30/04 ,  G01N24/087 ,  C30B30/00 ,  C30B30/02 ,  G01N24/00 ,  G01N24/008 ,  G01R33/20 ,  G01R33/46

Abstract: Disclosed herein are methods of preparing a composition comprising crystalline biomolecules, for example, crystalline antibodies. In exemplary embodiments, the method comprises forming a fluidized bed of crystalline biomolecules using, for example, a counter-flow centrifuge to exchange buffer and/or to concentrate the crystalline biomolecules in a solution. Also provided are methods of detecting crystalline biomolecules and/or amorphous biomolecules in a sample.

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：US12000915B2

公开(公告)日：2024-06-04

申请号：US17766055

申请日：2020-10-02

Applicant: AMGEN INC.

Inventor： Marc A. Caporini ,  Ron C. Kelly ,  Mariana De Maillé

IPC: G01R33/44 ,  G01N24/08

CPC classification number: G01R33/448 ,  G01N24/08

Abstract: Disclosed herein is a method of conducting direct detection 1H solid state NMR (“ssNMR”) on a macromolecule-containing solid state formulation. The method includes conducting a 1H spin-lattice relaxation time (“T1”) experiment on the solid state formulation at various temperatures to generate a T1 value at each temperature, converting the T1 values to 1H spin-lattice relaxation rate (“R1”), and plotting R1 versus temperature to generate a relaxation rate curve for the solid state formulation. The relaxation rate curve can be analyzed to determine the molecular mobility of the macromolecule in the solid state formulation, the degree of aggregation in the solid state formulation, and/or the stability of the solid state formulation.

公开(公告)号：US11465969B2

公开(公告)日：2022-10-11

申请号：US17263224

申请日：2019-08-16

Applicant: AMGEN INC. ,  CYTOKINETICS, INC.

Inventor： Henry Morrison ,  Sheng Cui ,  Kyle Quasdorf ,  Evelyn Yanez ,  Bin Peter Quan ,  Ron C. Kelly ,  Sebastien Caille ,  Lingyun Xiao ,  David Pearson ,  Jaclyn Raeburn ,  Ailsa Golightly ,  Bradley Morgan ,  Matthew Peterson ,  Alex Eberlin ,  Alexander Oblezov

IPC: C07D213/75

Abstract: Provided herein are free base crystalline forms, crystalline salts, and an amorphous salts of omecamtiv mecarbil.

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：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.