Invention Grant
- Patent Title: Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof
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Application No.: US15301188Application Date: 2015-04-01
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Publication No.: US10087175B2Publication Date: 2018-10-02
- Inventor: William Hawkins , Robert Mach , Dirk Spitzer , Suwanna Vangveravong , Brian Van Tine
- Applicant: Washington University
- Applicant Address: US MO St. Louis
- Assignee: Washington University
- Current Assignee: Washington University
- Current Assignee Address: US MO St. Louis
- International Application: PCT/US2015/023954 WO 20150401
- International Announcement: WO2015/153814 WO 20151008
- Main IPC: C07D451/14
- IPC: C07D451/14 ; C07D471/08 ; A61K31/517 ; A61K31/496 ; A61K45/06

Abstract:
Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described. At least one described molecular species exhibits an IC50 value below 5 μM against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo, and led to 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.
Public/Granted literature
- US20170015660A1 SIGMA-2 RECEPTOR LIGAND DRUG CONJUGATES AS ANTITUMOR COMPOUNDS, METHODS OF SYNTHESIS AND USES THEREOF Public/Granted day:2017-01-19
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