- Patent Title: First-in-class of SHMT2 and MTHFD2 inhibitors as antitumor agents
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Application No.: US16118007Application Date: 2018-08-30
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Publication No.: US10793573B2Publication Date: 2020-10-06
- Inventor: Aleem Gangjee , Larry H. Matherly
- Applicant: Duquesne University of the Holy Spirit , Wayne State University
- Applicant Address: US PA Pittsburgh US MI Detroit
- Assignee: Duquesne University of The Holy Spirit,Wayne State University
- Current Assignee: Duquesne University of The Holy Spirit,Wayne State University
- Current Assignee Address: US PA Pittsburgh US MI Detroit
- Agency: Buchanan Ingersoll & Rooney PC
- Agent Craig G. Cocheour, Esq.
- Main IPC: A61K31/519
- IPC: A61K31/519 ; C07D487/04 ; A61P35/00

Abstract:
A compound of the Formula I and optionally a pharmaceutically acceptable salt thereof is provided: Formula I, wherein, R is one selected from the group consisting of H and CH3; n is an integer ranging from 1 to 4; X is one selected from the group consisting of —CH2—, O, S, —NH—, —NHCHO—, —NHCOCH3—, and —NHCOCF3—; and Ar is one selected from the group consisting of (a) 1,4-phenyl, (b) 2′-fluoro-1,4-phenyl, and (c) 2,5-thienyl. Methods of treating a patient having cancer, targeting mitochondrial metabolism, and targeting SHMT2 and MTHFD2 using the compounds of this invention are disclosed.
Public/Granted literature
- US20190100524A1 FIRST-IN-CLASS OF SHMT2 AND MTHFD2 INHIBITORS AS ANTITUMOR AGENTS Public/Granted day:2019-04-04
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