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US 12,522,631 B2Granted
Compounds for use in the treatment of liver disease
AssigneeThe Provost, Fellows, Foundation Scholars, and the Other Members of Board, of the College of the Holy and Undivided Trinity of Queen Elizabeth Near Dublin
InventorsJohn Gilmer, Jason Gavin
Life of this patent
Estimating the term…
Abstract
Bile acid derivatives, methods of manufacture thereof, and uses thereof are disclosed herein. The bile acid derivatives have demonstrated potential as therapeutics for treating liver disease.
Claims21
A compound having the formula:
- n is 0 or 1,
- X is —C1-C12 aliphatic optionally substituted with one or more selected from the group consisting of hydroxyl, amino, amido, sulfonyl, sulphonamide, thiol, carboxyl, cyano, nitro, —C1-C6 alkyl, —C1-C6 alkoxy, C1-C6 thioalkyl, oxo, —C(O)O—C1-C6 alkyl, —OC(O)O—C1-C6alkyl, —C(O)NR′R′, —N(R′)C(O)NR′R′, —N(R′)C(O)O—C1-C6alkyl, and —C3-C6 cycloalkyl;
- R1 is selected from the group consisting of carboxylate, —CO2H, —C(O)OR′, —C(O)NR′—RA1, —N(R′)C(O)—RA1, —N(R′)C(O)ORA2, and sulfonate;
- R2 has a formula:
- where:
- Y and Z are each independently selected from N or CH
- R3 is H, or —C1-C12 aliphatic optionally substituted with one or more of hydroxyl, amino, amido, sulfonyl, sulphonamide, thiol, carboxyl, cyano, nitro, —C1-C6 alkyl, —C3-C6 cycloalkyl, —C1-C6 alkoxy, —C1-C6 thioalkyl, oxo, —C(O)O—C1-C6 alkyl, —OC(O)O—C1-C6alkyl, —C(O)NR′R′, —N(R′)C(O)NR′R′, —N(R′)C(O)O—C1-C6alkyl, or —NR′RA2;
- R4 is H, halo, or —C1-C3 alkyl;
- and
- R′ is independently selected, for each occurrence, from the group consisting of hydrogen, and C1-C6 alkyl optionally substituted with RA1;
- RA1 is hydrogen, carboxylate, —CO2H, sulfonate or —C1-C6 alkyl, optionally substituted with one or more of hydroxyl, —C3-C6 cycloalkyl, —C1-C6 alkenyl, —C1-C6 alkoxyl, carboxylate, —CO2H or sulfonate;
- RA2 is RA1, —C(O)RA1, —C6-C12 aryl, —C6-C12 alkaryl, —C6-C12 alkenaryl, —SO2—C1-C6 alkyl, or —SO2—C6-C12 aryl;
- or a pharmaceutically acceptable salt, hydrate, stereoisomer, or prodrug thereof.
10 more elements
A compound having the formula:
- wherein n is 1 and —(X)n—R1 is selected from the group consisting of:
- R2 has a formula:
- where:
- Y and Z are each independently selected from N or CH
- R3 is H, or —C1-C12 aliphatic optionally substituted with one or more of hydroxyl, amino, amido, sulfonyl, sulphonamide, thiol, carboxyl, cyano, nitro, —C1-C6 alkyl, —C3-C6 cycloalkyl, —C1-C6 alkoxy, —C1-C6 thioalkyl, oxo, —C(O)O—C1-C6 alkyl, —OC(O)O—C-C6alkyl, —C(O)NR′R′, —N(R′)C(O)NR′R′, —N(R′)C(O)O—C1-C6alkyl, or —NR′RA2;
- R4 is H, halo, or —C1-C3 alkyl;
- and
- R′ is independently selected, for each occurrence, from the group consisting of hydrogen, and C1-C6 alkyl optionally substituted with RA1;
- RA1 is hydrogen, carboxylate, —CO2H, sulfonate or —C1-C6 alkyl, optionally substituted with one or more of hydroxyl, —C3-C6 cycloalkyl, —C1-C6 alkenyl, —C1-C6 alkoxyl, carboxylate, —CO2H, sulfonate;
- RA2 is RA1, —C(O)RA1, —C6-C12 aryl, —C6-C12 alkaryl, —C6-C12 alkenaryl, —SO2—C1-C6 alkyl, or —SO2—C6-C12 aryl;
- or a pharmaceutically acceptable salt, hydrate, stereoisomer, or prodrug thereof.
8 more elements
A compound having the formula:
- a pharmaceutically acceptable salt, hydrate, stereoisomer, or prodrug thereof.
Dependencies are inferred from the claim text.