公开(公告)号：US20190315741A1

公开(公告)日：2019-10-17

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 (R)

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.

公开(公告)号：US09675697B2

公开(公告)日：2017-06-13

申请号：US14204076

申请日：2014-03-11

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

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.

公开(公告)号：US20150299211A1

公开(公告)日：2015-10-22

申请号：US14688553

申请日：2015-04-16

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Angelo Aguilar ,  Liu Liu ,  Jianfeng Lu ,  Donna McEachern

IPC: C07D487/10 ,  A61K45/06 ,  A61N5/10 ,  A61K31/407

CPC classification number: C07D487/10 ,  A61K31/407 ,  A61K45/06 ,  A61N5/10 ,  A61N2005/1098

Abstract: Inhibitors of MDM2 and MDM2-related proteins and compositions containing the same are disclosed. Methods of using the MDM2 inhibitors in the treatment of diseases and conditions wherein inhibition of an interaction between p53 and MDM2 provides a benefit, like cancers, also are disclosed.

Abstract translation: 公开了MDM2和MDM2相关蛋白的抑制剂和含有它们的组合物。 还公开了使用MDM2抑制剂治疗其中抑制p53和MDM2之间的相互作用提供益处的疾病和病症的方法，如癌症。

公开(公告)号：US20180289677A1

公开(公告)日：2018-10-11

申请号：US15949799

申请日：2018-04-10

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Haibin Zhou ,  Jianfeng Lu ,  Liu Liu ,  Jeanne Stuckey ,  Liangyou Rui ,  Yi Sun

IPC: A61K31/428 ,  A61P1/16

Abstract: Small molecule covalent inhibitors of DCN1 and compositions containing the same are disclosed. Methods of using the DCN1 covalent inhibitors in the treatment of diseases and conditions wherein inhibition of DCN1 provides a benefit, like oxidative stress-related diseases and conditions, neurodegenerative diseases and conditions, metabolic disorders, and muscular nerve degeneration, also are disclosed.

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：US08883771B2

公开(公告)日：2014-11-11

申请号：US13969030

申请日：2013-08-16

Applicant: The Regents of the University of Michigan

Inventor： Shaomeng Wang ,  Rong Sheng ,  Haiying Sun ,  Liu Liu ,  Jianfeng Lu ,  Donna McEachern

IPC: C07D225/00 ,  A61K31/545 ,  C07D519/00 ,  A61K31/407 ,  A61K31/496 ,  A61K45/06

CPC classification number: C07D519/00 ,  A61K31/407 ,  A61K31/496 ,  A61K45/06

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

Abstract translation: 公开了IAP蛋白的抑制剂和含有其的组合物。 还公开了使用IAP蛋白抑制剂治疗其中抑制IAP蛋白提供益处的疾病和病症的方法，如癌症。

公开(公告)号：US20140057924A1

公开(公告)日：2014-02-27

申请号：US13969030

申请日：2013-08-16

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Rong Sheng ,  Haiying Sun ,  Liu Liu ,  Jianfeng Lu ,  Donna McEachern

IPC: C07D519/00 ,  A61K31/407 ,  A61K31/496 ,  A61K45/06

CPC classification number: C07D519/00 ,  A61K31/407 ,  A61K31/496 ,  A61K45/06

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

Abstract translation: 公开了IAP蛋白的抑制剂和含有其的组合物。 还公开了使用IAP蛋白抑制剂治疗其中抑制IAP蛋白提供益处的疾病和病症的方法，如癌症。

公开(公告)号：US12012467B2

公开(公告)日：2024-06-18

申请号：US16496974

申请日：2018-03-28

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Haibin Zhou ,  Jianfeng Lu ,  Liu Liu ,  Yi Sun ,  Denzil Bernard

IPC: A61K31/426 ,  A61K31/427 ,  A61K31/428 ,  A61K31/454 ,  A61K31/5377 ,  A61K38/05 ,  A61K38/06 ,  A61K38/07 ,  A61K45/06 ,  C07D277/30 ,  C07D277/64 ,  C07D417/12 ,  C07K5/02 ,  C07K5/062 ,  C07K5/078 ,  C07K5/097 ,  C07K5/113 ,  C07K5/117 ,  C07K7/02

CPC classification number: C07K5/1021 ,  A61K31/426 ,  A61K31/427 ,  A61K31/428 ,  A61K31/454 ,  A61K31/5377 ,  A61K38/05 ,  A61K38/06 ,  A61K38/07 ,  A61K45/06 ,  C07D277/30 ,  C07D277/64 ,  C07D417/12 ,  C07K5/02 ,  C07K5/021 ,  C07K5/06026 ,  C07K5/06139 ,  C07K5/0821 ,  C07K5/1024 ,  C07K7/02

Abstract: Compounds of formula (I) as inhibitors of DCN1 and compositions containing the same are disclosed. Methods of using the DCN1 inhibitors in the treatment of diseases and conditions wherein inhibition of DCN1 provides a benefit, like oxidative stress-related diseases and conditions, neurodegenerative diseases and conditions, metabolic disorders, and muscular nerve degeneration, also are disclosed.

公开(公告)号：US11168082B2

公开(公告)日：2021-11-09

申请号：US16611238

申请日：2018-05-15

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Dengyou Zhang ,  Canhui Zheng ,  Zhuo Chen ,  Liu Liu ,  Liyue Huang ,  Chao-Yie Yang

IPC: C07D471/04 ,  A61P35/00 ,  C07D519/00

Abstract: The present disclosure provides compounds represented by Formula I and II: and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, X, W, Y, and Z are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I and II for use to treat a condition or disorder responsive to LSD1 inhibition such as cancer.