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：US20220175782A1

公开(公告)日：2022-06-09

申请号：US17579359

申请日：2022-01-19

Applicant: AMGEN INC.

Inventor： John Gordon ALLEN ,  Brian Alan LANMAN ,  Jian CHEN ,  Anthony B. REED ,  Victor J. CEE ,  Longbin LIU ,  Patricia LOPEZ ,  Ryan Paul WURZ ,  Thomas T. NGUYEN ,  Shon BOOKER ,  Jennifer Rebecca ALLEN ,  Margaret CHU-MOYER ,  Albert AMEGADZIE ,  Ning CHEN ,  Clifford GOODMAN ,  Jonathan D. LOW ,  Vu Van MA ,  Ana Elena MINATTI ,  Nobuko NISHIMURA ,  Alexander J. PICKRELL ,  Hui-Ling WANG ,  Youngsook SHIN ,  Aaron C. SIEGMUND ,  Kevin C. YANG ,  Nuria A. TAMAYO ,  Mary WALTON ,  Qiufen XUE

IPC: A61K31/519 ,  A61K31/551 ,  A61K39/395 ,  A61P35/00

Abstract: Provided herein are KRAS G12C inhibitors, such as composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

公开(公告)号：US20220168280A1

公开(公告)日：2022-06-02

申请号：US17589163

申请日：2022-01-31

Applicant: AMGEN INC.

Inventor： Brian Alan LANMAN ,  Victor J. CEE ,  Alexander J. PICKRELL ,  Anthony B. REED ,  Kevin C. YANG ,  David John KOPECKY ,  Hui-Ling WANG ,  Patricia LOPEZ ,  Kate ASHTON ,  Shon BOOKER ,  Christopher M. TEGLEY

IPC: A61K31/428 ,  A61K31/496 ,  A61K31/519 ,  A61P35/00 ,  A61K31/5025 ,  A61K31/502 ,  A61K31/517 ,  C07D275/04 ,  C07D471/08 ,  C07D403/04 ,  C07D401/04 ,  C07D513/04 ,  C07D487/04 ,  C07D417/04 ,  C07D239/80 ,  C07D487/10 ,  C07D471/04

Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

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：US20150252011A1

公开(公告)日：2015-09-10

申请号：US14691715

申请日：2015-04-21

Applicant: AMGEN INC.

Inventor： Ana Elena Minatti ,  Jonathan D. LOW ,  Jennifer R. ALLEN ,  Albert AMEGADZIE ,  James BROWN ,  Michael J. FROHN ,  Angel GUZMAN-PEREZ ,  Paul E. HARRINGTON ,  Patricia LOPEZ ,  Vu Van MA ,  Nobuko NISHIMURA ,  Wenyuan QIAN ,  Shannon RUMFELT ,  Robert M. RZASA ,  Kelvin SHAM ,  Adrian L. SMITH ,  Ryan WHITE ,  Qiufen XUE

IPC: C07D265/12 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D413/12 ,  C07D471/04

CPC classification number: C07D413/12 ,  C07D265/12 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048

Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.

Abstract translation: 本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。 化合物具有通式I：其中式I中的每个R a，R b，R 1，R 2，R 3和R 7各自独立地定义的变量A4，A5，A6，A8在本文中定义。 本发明还提供包含该化合物的药物组合物，以及该化合物和组合物用于治疗由BACE的生物学活性产生的与A-β斑块形成和沉积有关的病症和/或病症的用途。 这种BACE介导的疾病包括例如阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。 本发明还提供式II和III的化合物及其分子式实施方案，用于制备本发明化合物的中间体和方法。

公开(公告)号：US20140275058A1

公开(公告)日：2014-09-18

申请号：US14199844

申请日：2014-03-06

Applicant: AMGEN INC.

Inventor： Ana Elena MINATTI ,  Jonathan D. LOW ,  Jennifer R. ALLEN ,  Albert AMEGADZIE ,  James BROWN ,  Michael J. FROHN ,  Angel GUZMAN-PEREZ ,  Paul E. HARRINGTON ,  Patricia LOPEZ ,  Vu Van MA ,  Nobuko NISHIMURA ,  Wenyuan QIAN ,  Shannon RUMFELT ,  Robert M. RZASA ,  Kelvin SHAM ,  Adrian L. SMITH ,  Ryan WHITE ,  Qiufen XUE

IPC: C07D471/04 ,  C07D265/12 ,  C07D417/12 ,  C07D417/14 ,  C07D413/12 ,  C07D413/14

CPC classification number: C07D413/12 ,  C07D265/12 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048

Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.

Abstract translation: 本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。 化合物具有通式I：其中式I中的每个R a，R b，R 1，R 2，R 3和R 7各自独立地定义的变量A4，A5，A6，A8在本文中定义。 本发明还提供包含该化合物的药物组合物，以及该化合物和组合物用于治疗由BACE的生物学活性产生的与A-β斑块形成和沉积有关的病症和/或病症的用途。 这种BACE介导的疾病包括例如阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。 本发明还提供式II和III的化合物及其分子式实施方案，用于制备本发明化合物的中间体和方法。

公开(公告)号：US20250057817A1

公开(公告)日：2025-02-20

申请号：US18443925

申请日：2024-02-16

Applicant: AMGEN INC.

Inventor： Brian Alan LANMAN ,  Victor J. CEE ,  Alexander J. PICKRELL ,  Anthony B. REED ,  Kevin C. YANG ,  David John KOPECKY ,  Hui-Ling WANG ,  Patricia LOPEZ ,  Kate ASHTON ,  Shon BOOKER ,  Christopher M. TEGLEY

IPC: A61K31/428 ,  A61K31/496 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/517 ,  A61K31/519 ,  A61P35/00 ,  C07D239/80 ,  C07D275/04 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D513/04

Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

公开(公告)号：US20240092794A1

公开(公告)日：2024-03-21

申请号：US18502780

申请日：2023-11-06

Applicant: AMGEN INC.

Inventor： Shon BOOKER ,  Matthew Paul BOURBEAU ,  John R. BUTLER ,  Sanne Ormholt Schroder GLAD ,  Brian Alan LANMAN ,  Patricia LOPEZ ,  Francesco MANONI ,  Liping H. PETTUS ,  Ian SARVARY ,  Nuria A. TAMAYO ,  Mikkel VESTERGAARD ,  Nicholas Anthony WEIRES

IPC: C07D491/06 ,  A61P35/00 ,  C07D471/06 ,  C07D471/16 ,  C07D491/16

CPC classification number: C07D491/06 ,  A61P35/00 ,  C07D471/06 ,  C07D471/16 ,  C07D491/16

Abstract: Described herein are novel PRMT5 inhibitors of Formula I and pharmaceutically acceptable salts thereof, as well as the pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, metabolic and blood disorders. Compounds of Formula I have the following structure:

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：US20140213581A1

公开(公告)日：2014-07-31

申请号：US14166012

申请日：2014-01-28

Applicant: AMGEN INC.

Inventor： Ryan WHITE ,  Jennifer R. ALLEN ,  Oleg EPSTEIN ,  Fang-Tsao HONG ,  Zihao HUA ,  Jason Brooks HUMAN ,  Patricia LOPEZ ,  Philip R. OLIVIERI ,  Karina ROMERO ,  Laurie SCHENKEL ,  John STELLWAGEN ,  Nuria A. TAMAYO ,  Xiao Mei ZHENG

IPC: C07D513/04 ,  C07D513/14

CPC classification number: C07D513/04 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/10 ,  C07D513/14 ,  C07D513/20 ,  C07D519/00

Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A5, A6, A8, R1, R2, R3, R7, X, Y, n and o of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.

Abstract translation: 本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。 化合物具有通式I：其中式I的变量A5，A6，A8，R1，R2，R3，R7，X，Y，n和o独立地在本文中定义。 本发明还提供包含该化合物的药物组合物，以及用于治疗由BACE的生物学活性产生的A-β斑块形成和沉积相关的病症和/或病症的化合物和组合物的相应用途。 这种BACE介导的疾病包括例如阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。 本发明进一步提供式II化合物及其次式实施方案，式III化合物，可用于制备式I-III化合物的中间体和方法和方法及其分式。