公开(公告)号：US20180289720A1

公开(公告)日：2018-10-11

申请号：US15938001

申请日：2018-03-28

申请人： AMGEN INC.

发明人： Paul E. Harrington ,  Kate Ashton ,  Sean P. Brown ,  Matthew R. Kaller ,  Todd J. Kohn ,  Brian Alan Lanman ,  Kexue Li ,  Yunxiao Li ,  Jonathan D. Low ,  Ana Elena Minatti ,  Alexander J. Pickrell ,  Markian M. Stec ,  Joshua Taygerly

IPC分类号： A61K31/553 ,  A61P35/00

CPC分类号： A61K31/553 ,  A61P35/00 ,  A61P35/02 ,  C07D498/08

摘要： Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

公开(公告)号：US10300075B2

公开(公告)日：2019-05-28

申请号：US15938001

申请日：2018-03-28

申请人： AMGEN INC.

发明人： Sean P. Brown ,  Kexue Li ,  Yunxiao Li ,  Markian M. Stec

IPC分类号： A61K31/553 ,  C07D498/08 ,  A61P35/00 ,  A61P35/02

摘要： Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

公开(公告)号：US09550762B2

公开(公告)日：2017-01-24

申请号：US14819256

申请日：2015-08-05

申请人： AMGEN INC.

发明人： Jennifer R. Allen ,  Albert Amegadzie ,  Matthew P. Bourbeau ,  James A. Brown ,  Jian J. Chen ,  Yuan Cheng ,  Michael J. Frohn ,  Angel Guzman-Perez ,  Paul E. Harrington ,  Longbin Liu ,  Qingyian Liu ,  Jonathan D. Low ,  Vu Van Ma ,  James Manning ,  Ana Elena Minatti ,  Thomas T. Nguyen ,  Nobuko Nishimura ,  Mark H. Norman ,  Liping H. Pettus ,  Alexander J. Pickrell ,  Wenyuan Qian ,  Shannon Rumfelt ,  Robert M. Rzasa ,  Aaron C. Siegmund ,  Markian M. Stec ,  Ryan D. White ,  Qiufen Xue

IPC分类号： C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D513/10 ,  C07D417/04 ,  C07D279/08

CPC分类号： C07D417/12 ,  C07D279/08 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D513/10

摘要： 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, and 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.

摘要翻译： 本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。 所述化合物具有通式I：其中式I中的变量A4，A5，A6，A8以及R 1，R b，R 1，R 2，R 3和R 7各自独立地定义。 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：US20190201412A1

公开(公告)日：2019-07-04

申请号：US16297904

申请日：2019-03-11

申请人： AMGEN INC.

发明人： Sean P. Brown ,  Kexue Li ,  Yunxiao Li ,  Markian M. Stec

IPC分类号： A61K31/553 ,  A61P35/02 ,  C07D498/08 ,  A61P35/00

CPC分类号： A61K31/553 ,  A61P35/00 ,  A61P35/02 ,  C07D498/08

摘要： Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

公开(公告)号：US11224601B1

公开(公告)日：2022-01-18

申请号：US17029249

申请日：2020-09-23

申请人： AMGEN INC.

发明人： Paul E. Harrington ,  Kate Ashton ,  Sean P. Brown ,  Matthew R. Kaller ,  Todd J. Kohn ,  Brian Alan Lanman ,  Kexue Li ,  Yunxiao Li ,  Jonathan D. Low ,  Ana Elena Minatti ,  Alexander J. Pickrell ,  Markian M. Stec ,  Joshua Taygerly

IPC分类号： A61K31/553 ,  A61P35/02 ,  A61P35/00 ,  C07D498/08

摘要： Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

公开(公告)号：US10821115B2

公开(公告)日：2020-11-03

申请号：US16783269

申请日：2020-02-06

申请人： AMGEN INC.

发明人： Paul E. Harrington ,  Kate Ashton ,  Sean P. Brown ,  Matthew R. Kaller ,  Todd J. Kohn ,  Brian Alan Lanman ,  Kexue Li ,  Yunxiao Li ,  Jonathan D. Low ,  Ana Elena Minatti ,  Alexander J. Pickrell ,  Markian M. Stec ,  Joshua Taygerly

IPC分类号： A61K31/553 ,  A61P35/02 ,  A61P35/00 ,  C07D498/08

摘要： Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.