IP Library Granted Patent US 9,394,303
Granted Patent B2
US 9,394,303 · App. 14/678,267 · Granted Jul 19, 2016

Small molecule inhibitors of MCL-1 and uses thereof

Inventors: Zaneta Nikolovska-Coleska (Ann Arbor, MI); Fardokht Abulwerdi (Frederick, MD); Hollis Showalter (Ann Arbor, MI); Lei Miao (Ann Arbor, MI); Jeanne Stuckey (Fenton, MI); Ahmed Mady (Ann Arbor, MI)
Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
C07D471/04A61K31/437A61K31/5377A61K45/06A61N5/10A61N2005/1098
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Quick Facts
Patent No.
US 9,394,303
App. No.
14/678,267
Granted
Jul 19, 2016
Kind
B2
Abstract

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having pyrazolopyridine structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.

Claims (11)

1. A compound having Formula I:

including pharmaceutically acceptable salts, solvates, and/or prodrugs thereof;

wherein R1 is selected from the group consisting of from

wherein R2 is selected from the group consisting of

and

wherein R3 is selected from the group consisting of hydrogen, OH, OCH 3 OCH 2 CH 3 COOH, COOCH 3 COOCH 2 CH 3 ,

wherein X, Y, Z are independently N, C or CO.

2. The compound of claim 1 , wherein the compound is able to bind the BH3 binding pocket of an Mcl-1 protein.

3. The compound of claim 1 , wherein said compound is selected from the group consisting of

pharmaceutically acceptable carrier.

4. A pharmaceutical composition comprising a compound of claim 1 .

Assignments (2)
CONFIRMATORY LICENSE Recorded Jul 12, 2016
From: UNIVERSITY OF MICHIGAN
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 039309/0163 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 26, 2016
From: NIKOLOVSKA-COLESKA, ZANETA; ABULWERDI, FARDOKHT A; SHOWALTER, HOLLIS; MIAO, LEI; STUCKEY, JEANNE; MADY, AHMED
To: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
Reel/Frame 038729/0055 →
Continuity (2)
Provisional Application 61975297 · Apr 4, 2014
Related Publication 20150284387A1 · Oct 8, 2015