公开(公告)号：US11285156B2

公开(公告)日：2022-03-29

申请号：US16438349

申请日：2019-06-11

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: A61K31/497 ,  C07D241/04 ,  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：US10532042B2

公开(公告)日：2020-01-14

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

Abstract: Provided herein are KRAS G12C inhibitors, compounds of formula (II), or a pharmaceutically acceptable salt thereof: compositions 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：US09296759B2

公开(公告)日：2016-03-29

申请号：US14346252

申请日：2012-09-21

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: C07D498/20 ,  C07D513/20 ,  A61K31/537 ,  A61K31/547 ,  C07D513/10 ,  C07D498/10

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, 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，A4，A5，A6，L，R2，R7，X，Y和Z如本文所定义。 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：US20150266824A1

公开(公告)日：2015-09-24

申请号：US14633936

申请日：2015-02-27

Applicant: AMGEN INC. ,  Teijin Pharma Limited

Inventor： Hilary Plake Beck ,  Shon Keith Booker ,  Howard Bregman ,  Victor J. Cee ,  Nagasree Chakka ,  Timothy D. Cushing ,  Oleg Epstein ,  Brian M. Fox ,  Stephanie Geuns-Meyer ,  Xiaolin Hao ,  Kenta Hibiya ,  Jun Kirata ,  Zihao Hua ,  Jason Human ,  Shinji Kakuda ,  Patricia Lopez ,  Ryota Nakajima ,  Kazuhisa Okada ,  Steven H. Olson ,  Hiroyuki Oono ,  Lewis D. Pennington ,  Kosuke Sasaki ,  Keiko Shimada ,  Youngsook Shin ,  Ryan D. White ,  Ryan P. Wurz ,  Shuyan Yi ,  Xiao Mei Zheng

IPC: C07D231/14 ,  C07D409/12 ,  C07D413/12 ,  C07D405/14 ,  C07D401/14 ,  C07D493/08 ,  C07D401/12 ,  C07D403/12

CPC classification number: C07D231/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/14 ,  C07D493/08

Abstract: The present invention relates to a novel compound having a function of inhibiting RORγ activity. The present invention also relates to pharmaceutical composition comprising the compound, a use of the compound in treating or preventing autoimmune diseases, inflammatory diseases, metabolic diseases, or cancer diseases.

Abstract translation: 本发明涉及具有抑制RORγ活性的新型化合物。 本发明还涉及包含该化合物的药物组合物，该化合物在治疗或预防自身免疫疾病，炎性疾病，代谢疾病或癌症疾病中的用途。