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US 10,112,948 B2Granted
Benzamide or benzamine compounds useful as anticancer agents for the treatment of human cancers
AssigneeBoard of Regents, The University of Texas System
InventorsJef DeBrabander, Luis Parada
Life of this patent
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Abstract
The described invention provides small molecule anti-cancer compounds for treating tumors that respond to cholesterol biosynthesis inhibition. The compounds selectively inhibit the cholesterol biosynthetic pathway in tumor-derived cancer cells, but do not affect normally dividing cells.
Claims7
A compound according to Formula I-g
- wherein
- R1 is selected from the group consisting of
- n=0, 1, or 2;
- m=0 or 1;
- R2 and R3 can be attached at any available position on the aromatic ring and are independently selected from the group consisting of H, D, F, Cl, CF3, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 hydroxyalkyl, cycloalkyl, OR, N(R)2, NO2, N3, NH—C(O)—R, CN, C(O)R, C(O)OR, C(O)N(R)2, SR, alkylacyl, and arylacyl;
- Each R is independently selected from the group consisting of H, C1-3 alkyl, propargyl, and phenyl;
- R4 and R5 are independently selected from the group consisting of H, C1-6 alkyl optionally substituted with N(R)2, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 hydroxyalkyl, phenyl optionally substituted with R3, and CH2OC(O)-phenyl optionally substituted with R3;
- R6 and R7 are independently selected from the group consisting of H, C1-3 alkyl, and C(O)OMe3;
- such that all possible stereoisomers, including optically active isomers, are included whenever stereogenic centers are present;
- or a pharmaceutically acceptable salt, prodrug, active metabolite, or solvate thereof.
7 more elements
A compound selected from the group consisting of:
- such that all possible stereoisomers, including optically active isomers, are included whenever stereogenic centers are present;
- or a pharmaceutically acceptable salt, prodrug, active metabolite, or solvate thereof.
A compound selected from the group consisting of
- such that all possible stereoisomers, including optically active isomers, are included whenever stereogenic centers are present;
- or a pharmaceutically acceptable salt, prodrug, active metabolite, or solvate thereof.
A compound selected from the group consisting of:
- such that all possible stereoisomers, including optically active isomers, are included whenever stereogenic centers are present;
- or a pharmaceutically acceptable salt, prodrug, active metabolite, or solvate thereof.
Dependencies are inferred from the claim text.