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US 2018/0148468 A1Published application
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
Life of this patent
Estimating the term…
Abstract
Disclosed are UAP inhibitors to inhibit glucose flux in the hexosamine biosynthetic pathway and methods of treating a disease using the inhibitors.
Claims28
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 selected from the group consisting of
- wherein V, W, X, Y, Z are, each independently, C, N, S, or O,
- R1, R2, R3, R4, R5 are, each independently, absent, —H, —(CH2)mCH3 where m=0-6 including branched alkyls, —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, R′ is substituted or unsubstituted alkyl, which includes heteroatoms NH, O, or S, i is 0 to 16, k is 0 to 10.
3 more elements
4-8. (canceled)
(canceled)
A pharmaceutical composition comprising 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 selected from the group consisting of
- wherein V, W, X, Y, Z are, each independently, C, N, S, or O,
- R1, R2, R3, R4, R5 are, each independently, absent, —H, —(CH2)mCH3 where m=0-6 including branched alkyls, —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, R′ is substituted or unsubstituted alkyl, which includes heteroatoms NH, O, or S, i is 0 to 16, k is 0 to 10, and
- a pharmaceutically acceptable carrier.
4 more elements
13-21. (canceled)
24-31. (canceled)
35-42. (canceled)
45-50. (canceled)
53-54. (canceled)
60-61. (canceled)
Dependencies are inferred from the claim text.