Use of UAP inhibitors to inhibit flux through the hexosamine biosynthetic pathway
AssigneeThe Johns Hopkins University
InventorsKevin J. Yarema, Christopher T. Saeui, Alfredo Quinones-Hinojosa, Sagar Ramesh Shah
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Abstract
Disclosed are UAP inhibitors to inhibit glucose flux in the hexosamine biosynthetic pathway and methods of treating a disease using the inhibitors.
Claims20
A method of treating a disease comprising administering to a subject an effective amount of a compound or pharmaceutically acceptable salt, solvate, anomers or hydrate thereof:
- wherein X is CO, SO2 or CH2;
- R6, R7, R8, R9, are each independently H or CO(CH2)nCH3;
- n is 0-16;
- R is
- wherein V, W, X, Y, Z are, each independently C or N,
- R1, R2, R3, R4, R5 are, each independently, absent, —H, —(CH2)mCH3 where m=0-6, —Br, —Cl, —F, —I, —NH2, —SH, —NO2, —NHSO2Ra where Rc is alkyl or branched alkyl, —SO2NHRb where Rb is alkyl or branched alkyl, —OH, —ORc where Rc is alkyl or branched alkyl or alkyl ester, —NHRd where Rd is alkyl or branched alkyl or amide, —OCF3, —COOH, or —COORe where Re is alkyl or branched alkyl, i is 0, and k is 1 to 10,
- wherein the disease is selected from cancer, diabetes, neurodegenerative disease, metabolic disorder, cardiovascular disease, ageing, autoimmunity, metabolic syndrome, eye disease and kidney disease.
A method of controlling a glycan production in a cell related to a disease, comprising using a compound or pharmaceutically acceptable salt, solvate, anomers or hydrate thereof:
- wherein X is CO, SO2 or CH2;
- R6, R7, R8, R9, are each independently H or CO(CH2)nCH3;
- n is 0-16;
- R is
- wherein V, W, X, Y, Z are, each independently C or N,
- R1, R2, R3, R4, R5 are, each independently, absent, —H, —(CH2)mCH3 where m=0-6, —Br, —Cl, —F, —I, —NH2, —SH, —NO2, —NHSO2Ra where IV is alkyl or branched alkyl, —SO2NHRb where Rb is alkyl or branched alkyl, —OH, —ORc where Rc is alkyl or branched alkyl or alkyl ester, —NHRd where Rd is alkyl or branched alkyl or amide, —OCF3, —COOH, or —COORe where Re is alkyl or branched alkyl, i is 0, and k is 1 to 10.
A method of treating a brain tumor in a subject comprising administering to the subject an effective amount of a compound or pharmaceutically acceptable salt, solvate, anomers or hydrate thereof:
- wherein X is CO, SO2 or CH2;
- R6, R7, R8, R9, are each independently H or CO(CH2)nCH3;
- n is 0-16;
- R is
- wherein V, W, X, Y, Z are, each independently C or N,
- R1, R2, R3, R4, R5 are, each independently, absent, —H, —(CH2)mCH3 where m=0-6, —Br, —Cl, —F, —I, —NH2, —SH, —NO2, —NHSO2Ra where Ra is alkyl or branched alkyl, —SO2NHRb where Rb is alkyl or branched alkyl, —OH, —ORc where Rc is alkyl or branched alkyl or alkyl ester, —NHRd where Rd is alkyl or branched alkyl or amide, —OCF3, —COOH, or —COORe where Re is alkyl or branched alkyl, i is 0, and k is 1 to 10.
Dependencies are inferred from the claim text.