IP Library Granted Patent US 10,087,173
Granted Patent B2
US 10,087,173 · App. 15/258,393 · Granted Oct 2, 2018

Substituted aminothiazoles as inhibitors of cancers, including hepatocellular carcinoma, and as inhibitors of hepatitis virus replication

Inventors: Andrea Cuconati (Oreland, PA); Xiaodong Xu (Doylestown, PA); Timothy M. Block (Doylestown, PA)
C07D417/14A61K31/425A61K31/426C07D277/42C07D417/04C07D417/12C07D487/04C07D495/04Y02A50/463
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Quick Facts
Patent No.
US 10,087,173
App. No.
15/258,393
Granted
Oct 2, 2018
Kind
B2
Abstract

Pharmaceutical compositions of the invention comprise substituted aminothiazoles derivatives having a disease-modifying action in the treatment of diseases associated with unregulated cell growth that include hepatocellular carcinoma, and infection with a hepatitis virus.

Claims (17)

1. A compound selected from:

(4-(pyridin-2-yl)-2-(pyrimidin-2-ylamino)thiazol-5-yl)methyl acetate;

(4-(pyridin-2-yl)-2-(pyrimidin-2-ylamino)thiazol-5-yl)methyl butyrate;

Ethyl 4-(pyridin-2-yl)-2-(pyrimidin-2-ylamino)thiazole-5-carboxylate;

Tert-butyl 2-(tert-butyl(pyrimidin-2-yl)amino)-4-(pyridine-2-yl)thiazole-5-carboxylate;

Ethyl 2-((4-methylpyrimidin-2-yl)amino)-4-(pyridin-2-yl)thiazole-5-carboxylate;

4-(pyridin-2-yl)-2-(pyrimidin-2-ylamino)thiazole-5-carboxylic acid;

Methyl 4-(pyridin-2-yl)-2-(pyrimidin-2-ylamino)thiazole-5-carboxylate;

and pharmaceutically acceptable salts thereof.

2. The compound of claim 1 , wherein the compound is selected from:

Ethyl 4-(pyridin-2-yl)-2-(pyrimidin-2-ylamino)thiazole-5-carboxylate;

Ethyl 2-((4-methylpyrimidin-2-yl)amino)-4-(pyridin-2-yl)thiazole-5-carboxylate;

Methyl 4-(pyridin-2-yl)-2-(pyrimidin-2-ylamino)thiazole-5-carboxylate;

and pharmaceutically acceptable salts thereof.

3. 4-Pyridin-2-yl-2-(pyrimidin-2-ylamino)-thiazole-5-carbonitrile or a pharmaceutically acceptable salt thereof.

4. 4-Pyridin-2-yl-2-(pyrimidin-2-ylamino)-thiazole-5-carbonitrile hydrochloride.

5. A composition comprising a compound according to claim 1 , and a pharmaceutically acceptable carrier.

Assignments (4)
CHANGE OF NAME Recorded Oct 7, 2016
From: INSTITUTE FOR HEPATITIS AND VIRUS RESEARCH
To: BARUCH S. BLUMBERG INSTITUTE
Reel/Frame 040290/0387 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 7, 2016
From: CUCONATI, ANDREA; XU, XIAODONG
To: INSTITUTE FOR HEPATITIS AND VIRUS RESEARCH
Reel/Frame 039964/0456 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 7, 2016
From: BLOCK, TIMOTHY
To: PHILADELPHIA HEALTH & EDUCATION CORPORATION D/B/A DREXEL UNIVERSITY COLLEGE OF MEDICINE
Reel/Frame 039965/0223 →
MERGER Recorded Oct 7, 2016
From: PHILADELPHIA HEALTH & EDUCATION CORPORATION D/B/A DREXEL UNIVERSITY COLLEGE OF MEDICINE
To: DREXEL UNIVERSITY
Reel/Frame 039965/0632 →
Continuity (3)
Continuation 14349014
Provisional Application 61542907 · Oct 4, 2011
Related Publication 20170066758A1 · Mar 9, 2017