Invention Grant
- Patent Title: 1 H-pyrazol-1-yl-thiazoles as inhibitors of lactate dehydrogenase and methods of use thereof
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Application No.: US16313727Application Date: 2017-06-29
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Publication No.: US10954228B2Publication Date: 2021-03-23
- Inventor: David J. Maloney , Alex Gregory Waterson , Ganesha Rai Bantukallu , Kyle Ryan Brimacombe , Plamen Christov , Chi V. Dang , Victor M. Darley-Usmar , Matthew Hall , Xin Hu , Ajit Jadhav , Somnath Jana , Kwangho Kim , William J. Moore , Bryan T. Mott , Leonard M. Neckers , Anton Simeonov , Gary Allen Sulikowski , Daniel Jason Urban , Shyh Ming Yang
- Applicant: NATIONAL INSTITUTES OF HEALTH, UNITED STATES DEPARTMENT OF HEALTH AND HUMAN SERVICES , Vanderbilt University , The UAB Research Foundation , The Trustees of the University of Pennsylvania
- Applicant Address: US MD Bethesda; US TN Nashville; US AL Birmingham; US PA Philadelphia
- Assignee: NATIONAL INSTITUTES OF HEALTH, UNITED STATES DEPARTMENT OF HEALTH AND HUMAN SERVICES,Vanderbilt University,The UAB Research Foundation,The Trustees of the University of Pennsylvania
- Current Assignee: NATIONAL INSTITUTES OF HEALTH, UNITED STATES DEPARTMENT OF HEALTH AND HUMAN SERVICES,Vanderbilt University,The UAB Research Foundation,The Trustees of the University of Pennsylvania
- Current Assignee Address: US MD Bethesda; US TN Nashville; US AL Birmingham; US PA Philadelphia
- Agency: Cantor Colburn LLP
- International Application: PCT/US2017/040021 WO 20170629
- International Announcement: WO2018/005807 WO 20180104
- Main IPC: C07D417/04
- IPC: C07D417/04 ; C07D417/14 ; A61P11/00 ; A61P35/00

Abstract:
The disclosure provides a compound of the formula (II) and pharmaceutically acceptable salts thereof. The variables, e.g. n, R, R3, R10, X, Y, and Z are defined herein. These compounds act as lactate dehydrogenase inhibitors and are useful for treating cancer and fibrosis. The compounds may be particularly useful for treating forms of cancer in which a metabolic switch from oxidative phosphorylation to glycolysis has occurred. The disclosure also provides pharmaceutical compositions containing a compound of this formula and method for treating patients having cancer, fibrosis, or other conditions in which a metabolic switch from oxidative phosphorylation to glycolysis has occurred.
Public/Granted literature
- US20190276448A1 1 H-PYRAZOL-1-YL-THIAZOLES AS INHIBITORS OF LACTATE DEHYDROGENASE AND METHODS OF USE THEREOF Public/Granted day:2019-09-12
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