公开(公告)号：US20240101570A1

公开(公告)日：2024-03-28

申请号：US18255575

申请日：2021-11-22

Applicant: AMGEN INC.

Inventor： Albert AMEGADZIE ,  Diane Jennifer BEYLKIN ,  Shon BOOKER ,  Matthew Paul BOURBEAU ,  John R. BUTLER ,  Sanne Ormholt Schroder GLAD ,  Todd J. KOHN ,  Brian Alan LANMAN ,  Kexue LI ,  Qingyian LIU ,  Patricia LOPEZ ,  Francesco MANONI ,  Primali Vasundera NAVARATNE ,  Liping H. PETTUS ,  Rene RAHIMOFF ,  Nuria A. TAMAYO ,  Mikkel VESTERGAARD ,  Hui-Ling WANG ,  Nicholas Anthony WEIRES

IPC: C07D491/048 ,  A61K35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/147 ,  C07D495/04 ,  C07D498/04 ,  C07D519/00

CPC classification number: C07D491/048 ,  A61K35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/147 ,  C07D495/04 ,  C07D498/04 ,  C07D519/00

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

公开(公告)号：US20230159510A1

公开(公告)日：2023-05-25

申请号：US17799077

申请日：2021-02-11

Applicant: AMGEN INC.

Inventor： Jennifer Rebecca ALLEN ,  Albert AMEGADZIE ,  Diane Jennifer BEYLKIN ,  Shon BOOKER ,  Matthew Paul BOURBEAU ,  John R. BUTLER ,  Michael J. FROHN ,  Sanne Ormholt Schroder GLAD ,  Birgitte Weinreich HUSEMOEN ,  Matthew R. KALLER ,  Todd J. KOHN ,  Brian Alan LANMAN ,  Kexue LI ,  Qingyian LIU ,  Patricia LOPEZ ,  Vu Van MA ,  Francesco MANONI ,  Jose MEDINA ,  Ana Elena MINATTI ,  Jorge PEIRO CADAHIA ,  Liping PETTUS ,  Alexander J. PICKRELL ,  Ian SARVARY ,  Nuria A. TAMAYO ,  Mikkel VESTERGAARD

IPC: C07D413/14 ,  C07D471/04 ,  C07D401/14 ,  C07D401/12 ,  C07D405/14

CPC classification number: C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04

Abstract: Described herein are compounds of Formula I and pharmaceutically acceptable salt thereof, stereoisomers, tautomers as well as 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: (I)

公开(公告)号：US20220395504A1

公开(公告)日：2022-12-15

申请号：US17363878

申请日：2021-06-30

Applicant: Amgen Inc.

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

IPC: A61K31/517 ,  A61P35/00 ,  A61K31/4985 ,  A61K39/395 ,  C07D403/04 ,  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：US20200069657A1

公开(公告)日：2020-03-05

申请号：US16675121

申请日：2019-11-05

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 methods of treating cancer with KRAS G12C inhibitors and compositions of the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

公开(公告)号：US20180177767A1

公开(公告)日：2018-06-28

申请号：US15849905

申请日：2017-12-21

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 ,  A61K31/517 ,  A61K31/5025 ,  A61K31/502 ,  A61P35/00

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：US20160159818A1

公开(公告)日：2016-06-09

申请号：US15041835

申请日：2016-02-11

Applicant: AMGEN INC.

Inventor： Ryan WHITE ,  Yuan CHENG ,  Ana Elena MINATTI ,  Bryant YANG ,  Xiao Mei ZHENG ,  Patricia LOPEZ ,  Jason B. HUMAN ,  Oleg EPSTEIN ,  Ted JUDD ,  Kelvin SHAM ,  Qiufen XUE

IPC: C07D498/10 ,  C07D498/20 ,  C07D513/20 ,  C07D513/10

CPC classification number: C07D498/10 ,  C07D498/20 ,  C07D513/10 ,  C07D513/20

Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A3, A4, A5, A6, L, R2, R7, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.

Abstract translation: 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。 在一个实施方案中，化合物具有通式I，其中式I中的A1，A2，A3，A3，A4，A5，A6，L，R2，R7，X，Y和Z定义如下。 本发明还包括在药物组合物中用于治疗，预防或治疗与β-分泌酶蛋白活性相关的病症和病症的用途。 这种病症包括例如阿尔茨海默氏病，认知缺陷，认知障碍，精神分裂症和与脑上形成和/或沉积斑块相关和/或引起的其他中枢神经系统病症。 本发明还包括式I的其它实施方案，可用于制备式I化合物的中间体和方法。

公开(公告)号：US20140107109A1

公开(公告)日：2014-04-17

申请号：US14051339

申请日：2013-12-18

Applicant: Amgen Inc.

Inventor： Richard T. LEWIS ,  Jennifer R. ALLEN ,  Yuan CHENG ,  Deborah CHOQUETTE ,  Oleg EPSTEIN ,  Angel GUZMAN-PEREZ ,  Paul E. HARRINGTON ,  Zihao HUA ,  Randall W. HUNGATE ,  Jason Brooks HUMAN ,  Ted JUDD ,  Qingyian LIU ,  Patricia LOPEZ ,  Ana Elena MINATTI ,  Philip OLIVIERI ,  Karina ROMERO ,  Shannon RUMFELT ,  Robert M. RZASA ,  Laurie SCHENKEL ,  John STELLWAGEN ,  Ryan WHITE ,  Qiufen XUE ,  Xiao ZHENG ,  Wenge ZHONG

IPC: C07D513/04 ,  C07D513/10 ,  C07D279/12 ,  C07D498/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D279/14 ,  C07D417/04

CPC classification number: C07D279/12 ,  C07D213/79 ,  C07D239/74 ,  C07D241/44 ,  C07D279/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D513/10 ,  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 A4, A5, A6, A8, R1, R2, R3, R7 and n 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, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.

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A4，A5，A6，A8，R1，R2，R3，R7和n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。 本发明还提供式II化合物及其次级实施方案，可用于制备式I-II化合物的中间体和方法和方法。