公开(公告)号：US20170210761A1

公开(公告)日：2017-07-27

申请号：US15443336

申请日：2017-02-27

申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

发明人： Shaomeng Wang ,  Yujun Zhao ,  Bing Zhou ,  Angelo Aguilar ,  Liu Liu ,  Longchuan Bai ,  Donna McEachern ,  Duxin Sun ,  Bo Wen ,  Ruijuan Luo ,  Ting Zhao ,  Arul Chinnaiyan ,  Irfan A. Asangani ,  Jeanne Stuckey ,  Jennifer Lynn Meagher ,  Xu Ran ,  Yang Hu

IPC分类号： C07D519/00 ,  A61K31/519 ,  C07D487/14 ,  A61K31/538 ,  A61K31/437 ,  C07D487/04 ,  A61K31/5377

CPC分类号： C07D519/00 ,  A61K31/437 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  C07D487/04 ,  C07D487/14

摘要： The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, A, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains. Compounds of the present disclosure are especially useful for treating cancer.

公开(公告)号：US20190119289A1

公开(公告)日：2019-04-25

申请号：US16091544

申请日：2017-04-06

申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

发明人： Shaomeng Wang ,  Yangbing Li ,  Angelo Aguilar ,  Bing Zhou ,  Jiantao Hu ,  Fuming Xu ,  Chong Qin ,  Yang Hu ,  Weiguo Xiang ,  Rohan Rej ,  Jiuling Yang ,  Xin Han ,  Longchuan Bai ,  Chao-Yie Yang

IPC分类号： C07D487/10 ,  C07D401/04 ,  C07D401/14 ,  C07D495/14 ,  C07D487/04

摘要： The present disclosure provides compounds represented by Formula I: and the salts or solvates thereof, wherein X, L, Y, and B are as defined in the specification. Compounds having Formula I are immunomodulators and/or monofunctional synthetic intermediates that can be used to prepare small-molecule drug conjugates.

公开(公告)号：US10253044B2

公开(公告)日：2019-04-09

申请号：US15443336

申请日：2017-02-27

申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

发明人： Shaomeng Wang ,  Yujun Zhao ,  Bing Zhou ,  Angelo Aguilar ,  Liu Liu ,  Longchuan Bai ,  Donna McEachern ,  Duxin Sun ,  Bo Wen ,  Ruijuan Luo ,  Ting Zhao ,  Arul Chinnaiyan ,  Irfan A. Asangani ,  Jeanne Stuckey ,  Jennifer Lynn Meagher ,  Xu Ran ,  Yang Hu

IPC分类号： A61K31/519 ,  C07D519/00 ,  C07D487/04 ,  C07D487/14 ,  A61K31/437 ,  A61K31/5377 ,  A61K31/538

摘要： The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, A, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains. Compounds of the present disclosure are especially useful for treating cancer.

公开(公告)号：US09096625B2

公开(公告)日：2015-08-04

申请号：US14155809

申请日：2014-01-15

申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

发明人： Shaomeng Wang ,  Jianfang Chen ,  Donna McEachern ,  Longchuan Bai ,  Liu Liu ,  Duxin Sun ,  Xiaoqin Li ,  Angelo Aguilar

IPC分类号： A61K31/675 ,  C07F9/6558 ,  A61K45/06 ,  A61K33/30

CPC分类号： C07F9/65583 ,  A61K31/675 ,  A61K33/30 ,  A61K45/06 ,  A61N5/10 ,  A61K2300/00

摘要： Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.

摘要翻译： 公开了Bcl-2 / Bcl-xL的抑制剂及其组合物。 还公开了使用Bcl-2 / Bcl-xL抑制剂治疗其中Bcl-2 / Bcl-xL的抑制提供益处的疾病和病症的方法，如癌症。

公开(公告)号：US11466028B2

公开(公告)日：2022-10-11

申请号：US16332533

申请日：2017-09-13

申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

发明人： Shaomeng Wang ,  Yang Hu ,  Chong Qin ,  Fuming Xu ,  Jiantao Hu ,  Bing Zhou ,  Zhuo Chen ,  Ester Fernandez-Salas ,  Longchuan Bai ,  Donna McEachern

IPC分类号： C07D498/14 ,  A61P35/02 ,  A61P35/04

摘要： The present disclosure provides compounds represented by Formula I and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, Ar, L, X, Y, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a condition or disorder responsive to degradation of BET bromodomains such as cancer.

公开(公告)号：US11267822B2

公开(公告)日：2022-03-08

申请号：US16645953

申请日：2018-09-12

申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

发明人： Shaomeng Wang ,  Weiguo Xiang ,  Fuming Xu ,  Longchuan Bai ,  Ester Fernandez-Salas ,  Donna McEachern

IPC分类号： C07D495/14 ,  C07D498/14 ,  A61P35/00

摘要： The present disclosure provides compounds represented by Formula (I): Formula (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, Y, ═, Ar, W, L, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I)I for use to treat a condition or disorder responsive to inhibition and/or degradation of BET bromodomains such as cancer.

公开(公告)号：US20210284657A1

公开(公告)日：2021-09-16

申请号：US16332533

申请日：2017-09-13

申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

发明人： Shaomeng Wang ,  Yang Hu ,  Chong Qin ,  Fuming Xu ,  Jiantao Hu ,  Bing Zhou ,  Zhuo Chen ,  Ester Fernandez-Salas ,  Longchuan Bai ,  Donna McEachern

IPC分类号： C07D498/14 ,  A61P35/04 ,  A61P35/02

摘要： The present disclosure provides compounds represented by Formula I and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, Ar, L, X, Y, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a condition or disorder responsive to degradation of BET bromodomains such as cancer.

公开(公告)号：US09580430B2

公开(公告)日：2017-02-28

申请号：US14633360

申请日：2015-02-27

申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

发明人： Shaomeng Wang ,  Yujun Zhao ,  Bing Zhou ,  Angelo Aguilar ,  Liu Liu ,  Longchuan Bai ,  Donna McEachern ,  Duxin Sun ,  Bo Wen ,  Ruijuan Luo ,  Ting Zhao ,  Arul Chinnaiyan ,  Irfan A. Asangani ,  Jeanne Stuckey ,  Jennifer Lynn Meagher ,  Xu Ran ,  Yang Hu

IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D491/00 ,  C07D487/04 ,  A61K31/519 ,  C07D487/14 ,  C07D519/00

CPC分类号： C07D519/00 ,  A61K31/437 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  C07D487/04 ,  C07D487/14

摘要： The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, A, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains. Compounds of the present disclosure are especially useful for treating cancer.

摘要翻译： 本公开提供取代的9H-嘧啶并[4,5-b]吲哚和5H-吡啶并[4,3-b]吲哚和由式I表示的相关类似物及其药学上可接受的盐，水合物和溶剂合物，其中R1a A，B1，B2，G，X1，Y1，Y2和Y3如说明书中所述。 本公开还涉及式I化合物用于治疗对抑制BET溴结构域有反应的病症或病症。 本公开的化合物特别可用于治疗癌症。

公开(公告)号：US09403856B2

公开(公告)日：2016-08-02

申请号：US14816191

申请日：2015-08-03

申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

发明人： Shaomeng Wang ,  Jianfang Chen ,  Donna McEachern ,  Longchuan Bai ,  Liu Liu ,  Duxin Sun ,  Xiaoqin Li ,  Angelo Aguilar

IPC分类号： C07D401/12 ,  C07D403/12 ,  C07F9/6558 ,  A61K31/496 ,  A61K31/675 ,  A61K45/06 ,  A61N5/10 ,  A61K33/30

CPC分类号： C07F9/65583 ,  A61K31/675 ,  A61K33/30 ,  A61K45/06 ,  A61N5/10 ,  A61K2300/00

摘要： Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.

摘要翻译： 公开了Bcl-2 / Bcl-xL的抑制剂及其组合物。 还公开了使用Bcl-2 / Bcl-xL抑制剂治疗其中Bcl-2 / Bcl-xL的抑制提供益处的疾病和病症的方法，如癌症。

公开(公告)号：US20150336994A1

公开(公告)日：2015-11-26

申请号：US14816191

申请日：2015-08-03

申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

发明人： Shaomeng Wang ,  Jianfang Chen ,  Donna McEachern ,  Longchuan Bai ,  Liu Liu ,  Duxin Sun ,  Xiaoqin Li ,  Angelo Aguilar

IPC分类号： C07F9/6558 ,  A61K45/06 ,  A61N5/10 ,  A61K31/675

CPC分类号： C07F9/65583 ,  A61K31/675 ,  A61K33/30 ,  A61K45/06 ,  A61N5/10 ,  A61K2300/00

摘要： Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.

摘要翻译： 公开了Bcl-2 / Bcl-xL的抑制剂及其组合物。 还公开了使用Bcl-2 / Bcl-xL抑制剂治疗其中Bcl-2 / Bcl-xL的抑制提供益处的疾病和病症的方法，如癌症。