公开(公告)号：US20210221771A1

公开(公告)日：2021-07-22

申请号：US17263224

申请日：2019-08-16

申请人： AMGEN INC. ,  CYTOKINETICS, INC.

发明人： 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分类号： C07D213/75

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

公开(公告)号：US11827635B2

公开(公告)日：2023-11-28

申请号：US17553598

申请日：2021-12-16

申请人： AMGEN INC.

发明人： Mary Chaves ,  Patricia Lopez ,  Prashant Agarwal ,  Albert Amegadzie ,  Stephanie Azali ,  Roman Shimanovich ,  Ron C. Kelly ,  Darren Leonard Reid

IPC分类号： C07D471/04

CPC分类号： C07D471/04 ,  C07B2200/13

摘要： 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：US12000915B2

公开(公告)日：2024-06-04

申请号：US17766055

申请日：2020-10-02

申请人： AMGEN INC.

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

IPC分类号： G01R33/44 ,  G01N24/08

CPC分类号： G01R33/448 ,  G01N24/08

摘要： 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

申请人： AMGEN INC. ,  CYTOKINETICS, INC.

发明人： 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分类号： C07D213/75

摘要： 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

申请人： AMGEN INC.

发明人： Mary Chaves ,  Patricia Lopez ,  Prashant Agarwal ,  Albert Amegadzie ,  Stephanie Azali ,  Roman Shimanovich ,  Ron C. Kelly ,  Darren Leonard Reid

IPC分类号： C07D471/04

摘要： 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

申请人： AMGEN INC.

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

IPC分类号： 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分类号： 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

摘要： 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

申请人： AMGEN INC.

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

IPC分类号： 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分类号： 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

摘要： 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：US11926592B2

公开(公告)日：2024-03-12

申请号：US17929645

申请日：2022-09-02

申请人： Amgen Inc.

发明人： Henry Morrison ,  Sheng Cui ,  Kyle Quasdorf ,  Evelyn Yanez ,  Bin Peter Quan ,  Ron C. Kelly ,  Sebastien Caille ,  Lingyun Xiao ,  David Pearson ,  Jaclyn Raeburn ,  Alisa Golightly

IPC分类号： C07D213/75

CPC分类号： C07D213/75 ,  C07B2200/13

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

公开(公告)号：US20220365156A1

公开(公告)日：2022-11-17

申请号：US17766055

申请日：2020-10-02

申请人： AMGEN INC.

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

IPC分类号： G01R33/44 ,  G01N24/08

摘要： 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：US20200157141A1

公开(公告)日：2020-05-21

申请号：US16494165

申请日：2018-03-14

申请人： AMGEN INC.

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

IPC分类号： C07K1/30 ,  A61K39/395 ,  G01N24/08

摘要： 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.