公开(公告)号：US20190023720A1

公开(公告)日：2019-01-24

申请号：US16121750

申请日：2018-09-05

申请人： AMGEN INC.

发明人： Sean P. BROWN ,  Yunxiao LI ,  Mike Elias LIZARZABURU ,  Brian S, LUCAS ,  Nick A. PARAS ,  Joshua TAYGERLY ,  Marc VIMOLRATANA ,  Xianghong WANG ,  Ming YU ,  Manuel ZANCANELLA ,  Liusheng ZHU ,  Ana GONZALEZ BUENROSTRO ,  Zhihong LI

IPC分类号： C07D513/10 ,  C07D513/08

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, 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：US20190016736A1

公开(公告)日：2019-01-17

申请号：US16123030

申请日：2018-09-06

申请人： AMGEN INC.

发明人： Sean P. BROWN ,  Yunxiao LI ,  Mike Elias LIZARZABURU ,  Brian S. LUCAS ,  Nick A. PARAS ,  Joshua TAYGERLY ,  Marc VIMOLRATANA ,  Xianghong WANG ,  Ming YU ,  Manuel ZANCANELLA ,  Liusheng ZHU ,  Ana GONZALEZ BUENROSTRO ,  Zhihong LI

IPC分类号： C07D513/10 ,  C07D513/08

摘要： Provided herein are compounds that are useful intermediates that may used to synthesize myeloid cell leukemia 1 protein (Mcl-1) inhibitors. Also provided are 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, 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：US20140045828A1

公开(公告)日：2014-02-13

申请号：US13929483

申请日：2013-06-27

申请人： AMGEN INC.

发明人： Jian CHEN ,  Wenge ZHONG ,  Bryant YANG ,  Wenyuan QIAN ,  Patricia LOPEZ ,  Ryan WHITE ,  Matthew WEISS ,  Tedd JUDD ,  Timothy POWERS ,  Yuan CHENG ,  Thomas DINEEN ,  Oleg EPSTEIN ,  Jason HUMAN ,  Jonathan D. LOW ,  Isaac E. MARX ,  Ana Elena MINATTI ,  Michele POTASHMAN ,  Nick A. PARAS ,  Qingyian LIU

IPC分类号： C07D513/10 ,  C07D498/20

CPC分类号： C07D513/10 ,  C07D498/10 ,  C07D498/20 ,  C07D513/20

摘要： 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, 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.

摘要翻译： 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，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：US20210040120A1

公开(公告)日：2021-02-11

申请号：US17075864

申请日：2020-10-21

申请人： AMGEN INC.

发明人： Brian S. LUCAS ,  Nick A. PARAS

IPC分类号： C07D513/10 ,  C07D513/08 ,  C07D498/00

摘要： Provided herein are compounds that are useful intermediates that may used to synthesize myeloid cell leukemia 1 protein (Mcl-1) inhibitors. Also provided are 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, 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：US20200062780A1

公开(公告)日：2020-02-27

申请号：US16569927

申请日：2019-09-13

申请人： AMGEN INC.

发明人： Sean P. BROWN ,  Yunxiao LI ,  Mike Elias LIZARZABURU ,  Brian S. LUCAS ,  Nick A. PARAS ,  Joshua TAYGERLY ,  Marc VIMOLRATANA ,  Xianghong WANG ,  Ming YU ,  Manuel ZANCANELLA ,  Liusheng ZHU ,  Ana GONZALEZ BUENROSTRO ,  Zhihong LI

IPC分类号： C07D513/10 ,  C07D498/00 ,  C07D513/08

摘要： Provided herein are compounds that are useful intermediates that may used to synthesize myeloid cell leukemia 1 protein (Mcl-1) inhibitors. Also provided are 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, 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：US20170088560A1

公开(公告)日：2017-03-30

申请号：US15376456

申请日：2016-12-12

申请人： AMGEN INC.

发明人： Sean P. BROWN ,  Yunxiao LI ,  Mike Elias LIZARZABURU ,  Brian S. LUCAS ,  Nick A. PARAS ,  Joshua TAYGERLY ,  Marc VIMOLRATANA ,  Xianghong WANG ,  Ming YU ,  Manuel ZANCANELLA ,  Liusheng ZHU ,  Ana GONZALEZ BUENROSTRO ,  Zhihong LI

IPC分类号： C07D513/10

CPC分类号： C07D513/10 ,  C07D513/08

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, 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.