| abstract |
Referring to a compound of formula (I '), where Q is C = (O), -CH2-, -NR5- or -O-; X1 is CR6 or N; X2 is CR7 or N; X3 is CR8 or N; X4 is CR9 or N; Y is CRb or N; Ra and Rb are each, independently, H, (C1-C6) alkyl, (C1-C6) alkoxy, among others, among others; R1 is H, (C1-C6) alkyl, (C1-C6) alkoxy, among others; R2 and R2 are each independently, H, (C1-C6) alkyl, (C1-C6) alkoxy, among others; each R3 is independently (C1-C6) alkyl, (C1-C6) alkoxy, (C1-C6) haloalkyl, among others; R4 is H, (C1-C6) alkyl, (C1-C6) alkoxy, among others; R5 is H-, -C (O) (C1-C6) alkyl or -C (O) O (C1-C6) alkyl, among others; each R6 and R9 is independently H, (C1-C6) alkyl, (C1-C6) alkoxy, among others; each R7 and R8 is independently H, (C1-C8) alkenyl, (C1-C6) alkynyl, among others; n is 0, 1 or 2. These are substituted compounds of 4-phenylpyridine, a non-systemic TGR5 agonist. It also relates to methods for preparing these compounds, and their utility in the treatment of chemotherapy-induced diarrhea, diabetes, among other diseases and disorders associated with TGR5. |