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US 2022/0177425 A1Published application
Small molecules for cancer therapy that reduce the expression of transcription factors klf5 and egr-1
AssigneesThe Scripps Research Institute, The Research Foundation for The State University of New York
InventorsThomas D. Bannister, Chao Wang, Agnieszka Bialkowska, Vincent Yang
Life of this patent
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Abstract
The present disclosure provides compounds of formula (I), as described herein, their pharmaceutically acceptable salts, and their pharmaceutical compositions, which are effective in reducing the expression level of KLF5 or EGR1 in a living cell, and for the treatment of tumors and colorectal cancer in a human patient.
Claims13
A compound of formula (I), or a pharmaceutically acceptable salt thereof:
- wherein
- X1 is selected from the group consisting of NH, CH2, CH-alkyl, and N-alkyl;
- Y is selected from the group consisting of CH2, CH-alkyl, and a bond;
- R1 is of formula
- wherein
- X1 is selected from the group consisting of H and 1-3 independent instances of Cl, Br, I, F, SO2NH2, SO2N(Me)2, SO2NH-alkyl, SO2Me, (C═O)NH2, (C═O)NMe2, (C═O)NH-alkyl, O-alkyl, and SMe;
- Z is selected from the group consisting of H, CN, CF3, SO2Me, SO2NH2, SO2NH-alkyl, SO2N(alkyl)2 (wherein the alkyl groups and the nitrogen atom to which they are bonded optionally form a ring further comprising 0 or 1 heteroatoms selected from the group consisting of O, S, NH, and N-alkyl), C(O)Me, CO2-alkyl, C(O)—NH-alkyl, and C(O)N(Me)-alkyl;
- R2 is selected from the group consisting of H, alkyl, and a side chain group of a natural amino acid;
- R3 and the nitrogen atoms to which it is attached together comprise a cyclic or acyclic diamine of any one of the following formulae:
- wherein a wavy line indicates a position of bonding;
- and,
- R4 is alkyl.
9 more elements
Dependencies are inferred from the claim text.