公开(公告)号：US20190127387A1

公开(公告)日：2019-05-02

申请号：US16091541

申请日：2017-04-06

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Yangbing Li ,  Jiuling Yang ,  Angelo Aguilar ,  Bing Zhou ,  Jiantao Hu ,  Fuming Xu ,  Rohan Rej ,  Xin Han

IPC: C07D487/10 ,  C07D401/04 ,  C07D401/14 ,  C07D417/14 ,  A61P35/00

Abstract: The present disclosure provides compounds represented by Formula I-A: A1-L1-B1 I-A and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein A1, B1, and L1 are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I-A for use to treat a condition or disorder responsive to degradation of MDM2 protein such as cancer.

公开(公告)号：US20170210761A1

公开(公告)日：2017-07-27

申请号：US15443336

申请日：2017-02-27

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： 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: C07D519/00 ,  A61K31/519 ,  C07D487/14 ,  A61K31/538 ,  A61K31/437 ,  C07D487/04 ,  A61K31/5377

CPC classification number: C07D519/00 ,  A61K31/437 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  C07D487/04 ,  C07D487/14

Abstract: 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：US20220356192A1

公开(公告)日：2022-11-10

申请号：US17227641

申请日：2021-04-12

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Yang Hu ,  Chong Qin ,  Fuming Xu ,  Jiantao Hu ,  Weiguo Xiang ,  Bing Zhou

IPC: C07D495/14 ,  A61P35/00 ,  C07K5/06 ,  A61K45/06

Abstract: The present disclosure provides compounds represented by Formula I: I, and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2a, R2b, R3, 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：US10975093B2

公开(公告)日：2021-04-13

申请号：US16332544

申请日：2017-09-13

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Yang Hu ,  Chong Qin ,  Fuming Xu ,  Jiantao Hu ,  Weiguo Xiang ,  Bing Zhou

IPC: C07D495/14 ,  C07K5/06 ,  A61K45/06 ,  A61P35/00

Abstract: The present disclosure provides compounds represented by Formula I: I, and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2a, R2b, R3, 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：US20210002289A1

公开(公告)日：2021-01-07

申请号：US17007191

申请日：2020-08-31

Applicant: The Regents of the University of Michigan

Inventor： 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: C07D487/10 ,  C07D401/04 ,  C07D401/14 ,  C07D487/04 ,  C07D495/14

Abstract: 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：US10391175B2

公开(公告)日：2019-08-27

申请号：US15619671

申请日：2017-06-12

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Xu Ran ,  Yujun Zhao ,  Chao-Yie Yang ,  Liu Liu ,  Longchuan Bai ,  Donna McEachern ,  Jeanne Stuckey ,  Jennifer Lynn Meagher ,  Duxin Sun ,  Xiaoqin Li ,  Bing Zhou ,  Hacer Karatas ,  Ruijuan Luo ,  Arul Chinnaiyan ,  Irfan A. Asangani

IPC: A61K31/519 ,  C07D471/04 ,  A61K45/06 ,  C07D487/04 ,  C07D491/056

Abstract: Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.

公开(公告)号：US20150246923A1

公开(公告)日：2015-09-03

申请号：US14633360

申请日：2015-02-27

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： 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

IPC: C07D487/04 ,  C07D487/14 ,  C07D519/00

CPC classification number: C07D519/00 ,  A61K31/437 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  C07D487/04 ,  C07D487/14

Abstract: 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.

Abstract translation: 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：US10759808B2

公开(公告)日：2020-09-01

申请号：US16091544

申请日：2017-04-06

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： 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: C07D401/04 ,  C07D487/10 ,  C07D401/14 ,  C07D487/04 ,  C07D495/14

Abstract: 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：US20190169195A1

公开(公告)日：2019-06-06

申请号：US16093160

申请日：2017-04-06

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Bing Zhou ,  Fuming Xu ,  Jiantao Hu ,  Longchuan Bai ,  Chao-Yie Yang

IPC: C07D487/04 ,  A61P35/00 ,  C07K5/083

Abstract: The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein B, R1, R5, Q1, Q″, L, X, Y, and Z are as defined as set forth in the specification. The present disclosure also provids 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：US20170281773A1

公开(公告)日：2017-10-05

申请号：US15619671

申请日：2017-06-12

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Xu Ran ,  Yujun Zhao ,  Chao-Yie Yang ,  Liu Liu ,  Longchuan Bai ,  Donna McEachern ,  Jeanne Stuckey ,  Jennifer Lynn Meagher ,  Duxin Sun ,  Xiaoqin Li ,  Bing Zhou ,  Hacer Karatas ,  Ruijuan Luo ,  Arul Chinnaiyan ,  Irfan A. Asangani

IPC: A61K45/06 ,  C07D487/04 ,  C07D471/04 ,  C07D491/056

CPC classification number: A61K45/06 ,  C07D471/04 ,  C07D487/04 ,  C07D491/056

Abstract: Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.