公开(公告)号：US11897864B2

公开(公告)日：2024-02-13

申请号：US17938835

申请日：2022-10-07

申请人： AbbVie Inc. ,  Genentech, Inc. ,  The Walter and Eliza Hall Institute of Medical Research

发明人： Milan Bruncko ,  Hong Ding ,  George A. Doherty ,  Steven W. Elmore ,  Lisa A. Hasvold ,  Laura Hexamer ,  Aaron R. Kunzer ,  Xiaohong Song ,  Andrew J. Souers ,  Gerard M. Sullivan ,  Zhi-Fu Tao ,  Gary T. Wang ,  Le Wang ,  Xilu Wang ,  Michael D. Wendt ,  Robert Mantei ,  Todd M. Hansen

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D519/00 ,  C07D471/04 ,  C07D209/82 ,  C07D403/12 ,  A61K31/496

CPC分类号： C07D401/12 ,  A61K31/496 ,  C07D209/82 ,  C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D519/00 ,  Y02A50/30

摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

公开(公告)号：US20230143532A1

公开(公告)日：2023-05-11

申请号：US17938835

申请日：2022-10-07

申请人： AbbVie Inc. ,  Genentech, Inc. ,  The Walter and Eliza Hall Institute of Medical Research

发明人： Milan Bruncko ,  Hong Ding ,  George A. Doherty ,  Steven W. Elmore ,  Lisa A. Hasvold ,  Laura Hexamer ,  Aaron R. Kunzer ,  Xiaohong Song ,  Andrew J. Souers ,  Gerard M. Sullivan ,  Zhi-Fu Tao ,  Gary T. Wang ,  Le Wang ,  Xilu Wang ,  Michael D. Wendt ,  Robert Mantei ,  Todd M. Hansen

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D519/00 ,  C07D471/04 ,  C07D209/82 ,  C07D403/12 ,  A61K31/496

CPC分类号： C07D401/12 ,  A61K31/496 ,  C07D209/82 ,  C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D519/00 ,  Y02A50/30

摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

公开(公告)号：US20140113910A1

公开(公告)日：2014-04-24

申请号：US14038409

申请日：2013-09-26

申请人： AbbVie Inc. ,  The Walter and Eliza Hall Institute of Medical Research ,  Genentech, Inc.

发明人： Milan Bruncko ,  Hong Ding ,  George A. Doherty ,  Steven W. Elmore ,  Lisa A. Hasvold ,  Laura Hexamer ,  Aaron R. Kunzer ,  Xiaohong Song ,  Andrew J. Souers ,  Gerard M. Sullivan ,  Zhi-Fu Tao ,  Gary T. Wang ,  Le Wang ,  Xilu Wang ,  Michael D. Wendt ,  Robert A. Mantei ,  Todd M. Hansen

IPC分类号： C07D471/04 ,  A61K31/496

CPC分类号： C07D401/12 ,  A61K31/496 ,  C07D209/82 ,  C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D519/00 ,  Y02A50/463

摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

公开(公告)号：US20170158666A1

公开(公告)日：2017-06-08

申请号：US15219208

申请日：2016-07-25

申请人： AbbVie Inc. ,  Genentech, Inc. ,  The Walter and Eliza Hall Institute of Medical Research

发明人： Milan Bruncko ,  Hong Ding ,  George A. Doherty ,  Steven W. Elmore ,  Lisa A. Hasvold ,  Laura Hexamer ,  Aaron R. Kunzer ,  Xiaohong Song ,  Andrew J. Souers ,  Gerard M. Sullivan ,  Zhi-Fu Tao ,  Gary T. Wang ,  Le Wang ,  Xilu Wang ,  Michael D. Wendt ,  Robert Mantei ,  Todd M. Hansen

IPC分类号： C07D401/12

CPC分类号： C07D401/12 ,  A61K31/496 ,  C07D209/82 ,  C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D519/00 ,  Y02A50/463

摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

公开(公告)号：US20210221789A1

公开(公告)日：2021-07-22

申请号：US17004841

申请日：2020-08-27

申请人： AbbVie Inc. ,  Genentech, Inc. ,  The Walter and Eliza Hall Institute of Medical Research

发明人： Milan Bruncko ,  Hong Ding ,  George A. Doherty ,  Steven W. Elmore ,  Lisa A. Hasvold ,  Laura Hexamer ,  Aaron R. Kunzer ,  Xiaohong Song ,  Andrew J. Souers ,  Gerard M. Sullivan ,  Zhi-Fu Tao ,  Gary T. Wang ,  Le Wang ,  Xilu Wang ,  Michael D. Wendt ,  Robert Mantei ,  Todd M. Hansen

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D519/00 ,  C07D471/04 ,  C07D209/82 ,  C07D403/12 ,  A61K31/496

摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

公开(公告)号：US20200231566A1

公开(公告)日：2020-07-23

申请号：US16557819

申请日：2019-08-30

申请人： AbbVie Inc. ,  Genentech, Inc. ,  The Walter and Eliza Hall Institute of Medical Research

发明人： Milan Bruncko ,  Hong Ding ,  George A. Doherty ,  Steven W. Elmore ,  Lisa A. Hasvold ,  Laura Hexamer ,  Aaron R. Kunzer ,  Xiaohong Song ,  Andrew J. Souers ,  Gerard M. Sullivan ,  Zhi-Fu Tao ,  Gary T. Wang ,  Le Wang ,  Xilu Wang ,  Michael D. Wendt ,  Robert Mantei ,  Todd M. Hansen

IPC分类号： C07D401/12 ,  A61K31/496 ,  C07D403/12 ,  C07D209/82 ,  C07D471/04 ,  C07D519/00 ,  C07D401/14

摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

公开(公告)号：US20240043404A1

公开(公告)日：2024-02-08

申请号：US18462355

申请日：2023-09-06

申请人： AbbVie Inc. ,  Genentech, Inc. ,  The Walter and Eliza Hall Institute of Medical Research

发明人： Milan Bruncko ,  Hong Ding ,  George A. Doherty ,  Steven W. Elmore ,  Lisa A. Hasvold ,  Laura Hexamer ,  Aaron R. Kunzer ,  Xiaohong Song ,  Andrew J. Souers ,  Gerard M. Sullivan ,  Zhi-Fu Tao ,  Gary T. Wang ,  Le Wang ,  Xilu Wang ,  Michael D. Wendt ,  Robert Mantei ,  Todd M. Hansen

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D519/00 ,  C07D471/04 ,  C07D209/82 ,  C07D403/12 ,  A61K31/496

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D519/00 ,  C07D471/04 ,  C07D209/82 ,  C07D403/12 ,  A61K31/496 ,  Y02A50/30

摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

公开(公告)号：US20150329541A1

公开(公告)日：2015-11-19

申请号：US14694965

申请日：2015-04-23

申请人： AbbVie Inc. ,  Genentech, Inc. ,  The Walter and Eliza Hall Institute of Medical Research

发明人： Milan Bruncko ,  Hong Ding ,  George A. Doherty ,  Steven W. Elmore ,  Lisa A. Hasvold ,  Laura Hexamer ,  Aaron R. Kunzer ,  Xiaohong Song ,  Andrew J. Souers ,  Gerard M. Sullivan ,  Zhi-Fu Tao ,  Gary T. Wang ,  Le Wang ,  Xilu Wang ,  Michael D. Wendt ,  Robert Mantei ,  Todd M. Hansen

IPC分类号： C07D471/04

CPC分类号： C07D401/12 ,  A61K31/496 ,  C07D209/82 ,  C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D519/00 ,  Y02A50/463

摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

摘要翻译： 公开了抑制抗凋亡Bcl-2蛋白活性的化合物，含有化合物的组合物和治疗疾病的方法，其中表达抗凋亡Bcl-2蛋白。

公开(公告)号：US09174982B2

公开(公告)日：2015-11-03

申请号：US14038304

申请日：2013-09-26

申请人： AbbVie Inc. ,  Genentech, Inc. ,  The Walter and Eliza Hall Institute of Medical Research

发明人： Milan Bruncko ,  Hong Ding ,  George A. Doherty ,  Steven W. Elmore ,  Lisa A. Hasvold ,  Laura Hexamer ,  Aaron R. Kunzer ,  Xiaohong Song ,  Andrew J. Souers ,  Gerard M. Sullivan ,  Zhi-Fu Tao ,  Gary T. Wang ,  Le Wang ,  Xilu Wang ,  Michael D. Wendt ,  Robert A. Mantei ,  Todd M. Hansen

IPC分类号： C07D209/82 ,  C07D403/12 ,  C07D401/14 ,  C07D471/04 ,  C07D519/00 ,  A61K31/496

CPC分类号： C07D401/12 ,  A61K31/496 ,  C07D209/82 ,  C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D519/00 ,  Y02A50/463

摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

公开(公告)号：US09067928B2

公开(公告)日：2015-06-30

申请号：US13929701

申请日：2013-06-27

申请人： Genentech, Inc. ,  AbbVie Inc. ,  The Walter and Eliza Hall Institute of Medical Research

发明人： Jonathan Bayldon Baell ,  Chinh Thien Bui ,  Peter Colman ,  Danette A. Dudley ,  Wayne J. Fairbrother ,  John A. Flygare ,  Guillaume Laurent Lessene ,  Chudi Ndubaku ,  George Nikolakopoulos ,  Carl Steven Rye ,  Brad Edmund Sleebs ,  Brian John Smith ,  Keith Geoffrey Watson ,  Steven W. Elmore ,  Andrew M. Petros ,  Andrew J. Souers ,  Peter Czabotar

IPC分类号： C07D417/14 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/496 ,  A61K31/498 ,  A61K31/4709 ,  C07D487/04 ,  C07D417/12

CPC分类号： C07D417/14 ,  C07D417/12 ,  C07D487/04

摘要： In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.

摘要翻译： 一方面，本发明提供式I化合物，其中在式I中，变量X1，X2a，X2b，X2c，R1，B，L，E，A和下标n如本文所定义。 另一方面，本发明提供包含式I化合物的药物组合物以及使用式I化合物治疗以表达或过表达为特征的疾病和病症（例如，癌症，血小板增多症等）的方法 的Bcl-2抗凋亡蛋白，例如抗凋亡Bcl-xL蛋白。