KUDUK, SCOTT D.,CHANG, RONALD K.,GRESHOCK, THOMAS J.
申请号:
ES10812601
公开号:
ES2537979T3
申请日:
2010.08.26
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A compound of formula (I): ** Formula ** or a pharmaceutically acceptable salt thereof, in which XY is selected from the group consisting of (1) -O-CRARB-, (2) -CRARB-O-, (3) -CRARB-SRC-, (4) -CRARB-NRC-, and (5) -NRC-CRARB-; wherein each of RA and RB is independently selected from the group consisting of, (a) hydrogen, and (b) -C1-6 alkyl, and RC is selected from the group consisting of, (a) hydrogen, ( b) -C (>; = O) -C1-6 alkyl, (c) C1-6 alkyl, (d) -C (>; = O) -CH2-C6H5, (e) -S (>; = O) 2- C1-6 alkyl; R1 is selected from the group consisting of (1) hydrogen, and (2) hydroxy, provided that when XY is -O-CRARB-, -CRARB-O- or -CRARB-SRC-, then R1 is hydroxy in the position trans isomeric as graphically represented: ** Formula ** R2 is selected from the group consisting of (1) -C6-10 aryl, or (2) heteroaryl, which is an aromatic cyclic group, having five to twelve ring atoms, the ring atoms being selected from C, O, N, N → O or S, at least one of which is O, N, N → O or S, wherein the aryl or heteroaryl group R2 is optionally substituted with one or more (a) halogen, (b) hydroxy, (c) -NR3R4, (d) -C 1-6 alkyl, (e) -O-C 1-6 alkyl, (f) C2-8 alkenyl, (g ) -C (>; = O) - (O) m-R5, (h) -C (>; = O) -NR5, (i) -S (>; = O) 2-R5, (j) -SR5, ( k) -CN; (l) -C6-10 aryl.Un compuesto de fórmula (I):**Fórmula** o una de sus sales farmacéuticamente aceptables, en el que X-Y se selecciona del grupo que consiste en (1) -O-CRARB-, (2) -CRARB-O-, (3) -CRARB-SRC-, (4) -CRARB-NRC-, y (5) -NRC-CRARB-; en donde cada uno de RA y RB se selecciona independientemente entre el grupo que consiste en, (a) hidrógeno, y (b) -alquilo C1-6, y RC se selecciona entre el grupo que consiste en, (a) hidrógeno, (b) -C(>;=O)-alquilo C1-6, (c) alquilo C1-6, (d) -C(>;=O)-CH2-C6H5, (e) -S(>;=O)2-alquilo C1-6; R1 se selecciona entre el grupo que consiste en (1) hidrógeno, y (2) hidroxi, siempre que cuando X-Y es-O-CRARB-, -CRARB-O- o -CRARB-SRC-, entonces R1 es hidroxi en la posición isomérica tran