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US 10,703,761 B2Granted
Bile acid receptor modulators and methods of use thereof
AssigneeCity of Hope
InventorsDonna Yu, Barry Forman
Life of this patent
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Abstract
Disclosed herein, inter alia, compounds and methods of use thereof for the modulation of bile acid receptor activity.
Claims11
A salt composition having the formula:
- wherein
- L2 is a bond, —C(O)—, —C(O)O—, —O—, —S—, —NR2L—, —C(O)NR2L—, —NR2LC(O)—, —S(O)2—, —S(O)NR2L—, —NR2LC(O)NH—, —NHC(O)NR2L—, substituted or unsubstituted alkylene, substituted or unsubstituted heteroalkylene, substituted or unsubstituted cycloalkylene, substituted or unsubstituted heterocycloalkylene, substituted or unsubstituted arylene, or substituted or unsubstituted heteroarylene;
- R25 is —OCH3, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;
- R26 is hydrogen, halogen, —CX263, —CHX262, —CH2X26, —OCX263, —OCH2X26, —OCHX262, —CN, —SOn26R26C, —SOv26NR26AR26B, —NHC(O)NR26AR26B, —(O)m26, —NR26AR26B, —C(O)R26C, —C(O)—OR26C, —C(O)NR26AR26B, —OR26C, —NR26ASO2R26C, —NR26AC(O)R26C, —NR26AC(O)OR26C, —NR26AOR26C, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R2L, R26A, R26B and R26C are independently hydrogen, —CX26A3, —CN, —COOH, —CONH2, —CHX26A2, —CH2X26A, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- X26 and X26A are independently halogen;
- n26 is an integer from 0 to 4;
- m26 and v26 are independently 1 or 2;
- and
- Y2 is an anionic bile acid receptor modulator the formula:
- wherein:
- L1 is a bond, —C(O)—, —C(O)O—, —C(O)NH—, or —CH2—;
- X1 is —CH2—;
- X2 is —C(R14)(R15)—;
- R3 is hydrogen, or unsubstituted alkyl;
- R4 is hydrogen or unsubstituted alkyl;
- R5 is hydrogen, unsubstituted alkyl, or —OR5A;
- R6 is hydrogen, unsubstituted alkyl, or —OR6A;
- R7 is hydrogen, unsubstituted alkyl, or —OR7A;
- R8 is hydrogen, unsubstituted alkyl, or —OR8A;
- R9 is hydrogen, or unsubstituted alkyl;
- R10 is hydrogen, unsubstituted alkyl, or —OR10A;
- R11 is hydrogen, unsubstituted alkyl, or —OR11A;
- R12 is hydrogen, unsubstituted alkyl, or —OR12A;
- R13 is hydrogen, unsubstituted alkyl, or —OR13A;
- R14 is hydrogen, unsubstituted alkyl, or —OR14A;
- R15 is hydrogen, unsubstituted alkyl, or —OR15A;
- R16 is —COO−, —S(O)3−, —SO4− or —NHS(O)3−,
- R1A, R2A, R5A, R6A, R7A, R8A, R10A, R11A, R12A, R13A, R14A, and R15A are independently hydrogen, unsubstituted alkyl, or an alcohol protecting group.
26 more elements
The method of claim above 4, wherein the metabolic disease or disorder is selected from the group consisting of diabetes, obesity, insulin resistance, metabolic syndrome, atherosclerosis and liver disease.
Dependencies are inferred from the claim text.