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US 11,945,827 B2Granted
Rapafucin derivative compounds and methods of use thereof
AssigneeThe Johns Hopkins University
InventorsJun Liu, Sam Hong, Brett R. Ullman, Joseph E. Semple, Kana Yamamoto, Puneet Kumar, Magesh Sadagopan, Jennifer C. Schmitt
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Abstract
The present disclosure provides macrocyclic compounds inspired by the immunophilin ligand family of natural products FK506 and rapamycin. The generation of a Rapafucin library of macrocyles that contain FK506 and rapamycin binding domains should have great potential as new leads for developing drugs to be used for treating diseases.
Claims4
A compound of Formula (V)
- or an optically pure stereoisomer or pharmaceutically acceptable salt thereof,
- wherein L is optionally substituted (CH2)nNR20C1-6 alkylene;
- A is NH, NMe, O, S(O)2 or S;
- each X is O;
- E is CH or N;
- R1 is H;
- R2 is C1-20alkoxy;
- R3 is C1-20alkyl;
- R4 is independently selected from the group consisting of H;
- or R4 forms a cyclic structure formed with R3, the cyclic structure is C2-10 heterocyclyl R20 is H;
- n is 0;
- m is an integer selected from 2;
- p is 2;
- and
- q is 4.
12 more elements
Dependencies are inferred from the claim text.