公开(公告)号：WO2020050890A2

公开(公告)日：2020-03-12

申请号：PCT/US2019/036626

申请日：2019-06-11

Applicant: AMGEN INC.

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

Abstract: Provided herein are KRAS G12C inhibitors, such as [Insert Compound Here] 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：WO2014134341A1

公开(公告)日：2014-09-04

申请号：PCT/US2014/019100

申请日：2014-02-27

Applicant: AMGEN INC.

Inventor： MINATTI, Ana Elena ,  LOW, Jonathan D. ,  ALLEN, Jenifer R. ,  CHEN, Jian ,  CHEN, Ning ,  CHENG, Yuan ,  JUDD, Ted ,  LIU, Qingyian ,  LOPEZ, Patricia ,  QIAN, Wenyuan ,  RUMFELT, Shannon ,  RZASA, Robert M. ,  TAMAYO, Nuria A. ,  XUE, Qiufen ,  YANG, Bryant ,  ZHONG, Wenge

IPC: C07D413/14 ,  A61K31/535 ,  A61K31/5355 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D471/04 ,  C07D265/08 ,  C07D498/04 ,  C07D513/04 ,  A61P25/00

CPC classification number: C07D413/14 ,  C07D265/08 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  C07F7/0812

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 A 4 , A 5 , A 6 , A 8 , each of R 1 and R 2 , R 3 and R 7 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 Formulas II and III, and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.

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中的各个R 1和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和III的化合物及其分式实施方案，可用于制备式I-III化合物的中间体和方法和方法。

公开(公告)号：WO2020050890A3

公开(公告)日：2020-03-12

申请号：PCT/US2019/036626

申请日：2019-06-11

Applicant: AMGEN INC.

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

IPC: C07D471/04 ,  C07D487/04 ,  A61K31/519 ,  A61K31/551 ,  A61P35/00 ,  A61K45/06

Abstract: Provided herein are KRAS G12C inhibitors, such as [Insert Compound Here] 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：WO2019241157A1

公开(公告)日：2019-12-19

申请号：PCT/US2019/036397

申请日：2019-06-10

Applicant: AMGEN INC.

Inventor： CHEN, Jian ,  TAMAYO, Nuria A. ,  LIU, Longbin ,  WANG, Hui-Ling ,  LANMAN, Brian Alan ,  WURZ, Ryan Paul ,  SHIN, Youngsook ,  CEE, Victor J.

IPC: C07D471/04 ,  A61K31/4375 ,  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：WO2018217651A1

公开(公告)日：2018-11-29

申请号：PCT/US2018/033714

申请日：2018-05-21

Applicant: AMGEN INC.

Inventor： LANMAN, Brian Alan ,  CHEN, Jian ,  REED, Anthony B. ,  CEE, Victor J. ,  LIU, Longbin ,  KOPECKY, David John ,  LOPEZ, Patricia ,  WURZ, Ryan Paul ,  NGUYEN, Thomas T. ,  BOOKER, Shon ,  NISHIMURA, Nobuko ,  SHIN, Youngsook ,  TAMAYO, Nuria A. ,  ALLEN, John Gordon ,  ALLEN, Jennifer Rebecca

IPC: C07D471/04 ,  A61K31/519 ,  A61P35/00 ,  C07D475/00

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.