LEWIS, Jason G.,LEADBETTER, Michael Robert,CALDWELL, Jeremy,DRAGOLI, Dean,BELL, Noah,JACOBS, Jeffrey W.,FINN, Patricia,JAIN, Rakesh,CHEN, Tao,SIEGEL, Matthew
申请号：
PE0011172018
公开号：
PE14922018A1
申请日:
2016.12.19
申请国别(地区):
PE
年份:
2018
代理人:
摘要：
Refers to a compound of formula (i\u00b4), where q = C (o) - CH2 -, - or - or - - NR5 x1 or x2 is Cr6 is CR7 o n n n or X4 X3 is CR8 is few or N and CRB or N and ra RB are each, independently, h,Alkyl, alkoxy (C1 - C6) (C1 - C6), among others, among others r1 is H, alkyl, alkoxy (C1 - C6) (C1 - C6), among others R2 and r2\u00b4son each independently, h, alkyl, alkoxy (C1 - C6) (C1 - C6)Between each other R3 is, so Regardless, alkyl, alkoxy (C1 - C6) (C1 - C6), haloalquilo (C1 - C6), among others R4 is H, alkyl, alkoxy (C1 - C6) (C1 - C6), among others R5 is (H -- C (o) alkyl (C1 - C6) or - C (o) oalquilo (C1 - C6), among others each R6 and R9 is, so Regardless, h, alkyl, alkoxy (C1 - C6) (C1 - C6), among others each R7 and R8 is, so Regardless, h,Alquenilo (C1, C8) alquinilo (C1 - C6), among others n is 0, 1 or 2. These are compounds substituted 4 - fenilpiridina agonist TGR5 not systemic.It also relates to methods for preparing these compounds and their use in the treatment of chemotherapy-induced diarrhea, Diabetes and other diseases and disorders associated with TGR5.Referido a un compuesto de formula(I´), en donde Q es C=(O), -CH2-, -NR5- u -O- X1 es CR6 o N X2 es CR7 o N X3 es CR8 o N X4 es CR9 o N Y es CRb o N Ra y Rb son cada uno, independientemente, H, alquilo(C1-C6), alcoxi(C1-C6), entre otros, entre otros R1 es H, alquilo(C1-C6), alcoxi(C1-C6), entre otros R2 y R2´son cada uno independientemente, H, alquilo(C1-C6), alcoxi(C1-C6), entre otros cada R3 es, de modo independientemente, alquilo(C1-C6), alcoxi(C1-C6), haloalquilo(C1-C6), entre otros R4 es H, alquilo(C1-C6), alcoxi(C1-C6), entre otros R5 es H-, -C(O)alquilo(C1-C6) o -C(O)Oalquilo(C1-C6), entre otros cada R6 y R9 es, de modo independientemente, H, alquilo(C1-C6), alcoxi(C1-C6), entre otros cada R7 y R8 es, de modo independientemente, H, alquenilo(C1-C8), alquinilo(C1-C6), entre otros n es 0, 1 o 2. Estos, son compuestos sustituidos de 4-fenilpiridina, agonista de TGR5 no sistemico. Tambien se refie
