公开(公告)号：US10899738B2

公开(公告)日：2021-01-26

申请号：US16098147

申请日：2017-05-02

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Angelo Aguilar ,  Ke Zheng ,  Shilin Xu ,  Tianfeng Xu ,  Denzil Bernard ,  Liyue Huang

IPC: C07D401/14 ,  C07D401/04 ,  C07D405/04 ,  C07D211/34 ,  A61P35/00

Abstract: The present disclosure provides compounds by Formula (I): (Formula (I)) and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R2, R3a, R3b, A, G, X, and Y 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 menin inhibition such as cancer.

公开(公告)号：US20200330464A1

公开(公告)日：2020-10-22

申请号：US16914518

申请日：2020-06-29

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Jianyong Chen

IPC: A61K31/506 ,  C07D405/14 ,  C07D401/12 ,  A61P35/00

Abstract: The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, and R7 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 inhibition of ALK such as cancer.

公开(公告)号：US10781208B2

公开(公告)日：2020-09-22

申请号：US16347630

申请日：2017-11-17

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Jianyong Chen ,  Liu Liu ,  Xuyuan Dong ,  Chao-Yie Yang ,  Donna McEachern ,  Shaomeng Wang

IPC: C07D471/04 ,  A61P35/00

Abstract: The present disclosure provides compounds represented by Formula (I), and the pharmaceutically acceptable salts and solvates thereof wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7, E 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 inhibition of ALK such as cancer. and ®

公开(公告)号：US20190382415A1

公开(公告)日：2019-12-19

申请号：US16481501

申请日：2018-02-02

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Jiantao Hu ,  Fuming Xu

IPC: C07D498/12 ,  C07D495/14 ,  C07D498/04 ,  C07D487/04

Abstract: The present disclosure provides fused 1,4-diazepines represented by Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A. E, R1, R2, R3, R4, R5, and Ar are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds having Formula (I) to treat diseases, conditions, or disorders responsive to inhibition of BET bromodomain proteins such as cancer.

公开(公告)号：US20190315739A1

公开(公告)日：2019-10-17

申请号：US16317056

申请日：2017-08-04

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Jianyong Chen

IPC: C07D471/04 ,  A61P35/02

Abstract: The present disclosure provides compounds having Formula I-A: and the pharmaceutically acceptable salts and solvates thereof, wherein A, X1, X2, X3 R1a, R1b E, and = are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I-A for use to treat a disease, disorder, or condition responsive to Bcl-2 protein inhibition such as cancer.

公开(公告)号：US10307407B2

公开(公告)日：2019-06-04

申请号：US15553593

申请日：2016-02-26

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Yujun Zhao ,  Bing Zhou ,  Angelo Aguilar

IPC: C07D487/04 ,  C07D487/14 ,  A61K31/437 ,  A61K31/519 ,  C07D231/38 ,  C07D261/06 ,  C07D471/04

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, W, 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 such as cancer. The present disclosure is also directed to the use of compound of Formula I as synthetic intermediates.

公开(公告)号：US20190119289A1

公开(公告)日：2019-04-25

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

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：US10253044B2

公开(公告)日：2019-04-09

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

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：US09096625B2

公开(公告)日：2015-08-04

申请号：US14155809

申请日：2014-01-15

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

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

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

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

Abstract: 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.

Abstract translation: 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：US08980838B2

公开(公告)日：2015-03-17

申请号：US13686475

申请日：2012-11-27

Applicant: The Regents of the University of Michigan

Inventor： Shaomeng Wang ,  Hacer Karatas ,  Yali Dou ,  Elizabeth Townsend ,  Denzil Bernard ,  Fang Cao

IPC: A61K38/12 ,  A61P35/00 ,  C07K5/12 ,  A61K45/00 ,  A61N5/10 ,  C07D255/02 ,  C07K5/02 ,  C07K5/09 ,  C07K5/103 ,  C07K5/11 ,  C07K5/062 ,  A61K45/06

CPC classification number: C07K5/126 ,  A61K38/12 ,  A61K45/00 ,  A61K45/06 ,  A61N5/10 ,  A61N2005/1098 ,  C07D255/02 ,  C07K5/0207 ,  C07K5/021 ,  C07K5/0215 ,  C07K5/06034 ,  C07K5/0815 ,  C07K5/101 ,  C07K5/1019 ,  C07K5/123 ,  A61K2300/00

Abstract: Cyclic peptidomimetics that inhibit the interaction between MLL1 and WDR5 are disclosed. Methods of inhibiting MLL1 activity and methods of treating cancers also are disclosed.

Abstract translation: 公开了抑制MLL1和WDR5之间相互作用的循环肽模拟物。 还公开了抑制MLL1活性的方法和治疗癌症的方法。