BILLEDEAU, Roland J.,KONDRU, Rama K.,LOPEZ-TAPIA, Francisco Javier,LOU, Yan,OWENS, Timothy D.,QIAN, Yimin,SO, Sung-Sau,THAKKAR, Kshitij Chhabilbhai,WANNER, Jutta,MORALES, Omar Jose
申请号：
ES12721812
公开号：
ES2590491T3
申请日:
2012.05.14
申请国别(地区):
ES
年份:
2016
代理人:
摘要：
A compound of Formula I: ** Formula ** in which: ---- is a double bond； A is pyrazole substituted with one or more A '； A 'is -NHR or R4； R is H, -R1, -R1-R2-R3, -R1-R3 or -R2-R3； R1 is aryl, heteroaryl, cycloalkyl, heterocycloalkyl or heteroaryl fused with a heterocycloalkyl, each of which is optionally substituted with one or more R1 'or R1' '； each R1 'is independently halo, nitro, cyano, C1-6 alkyl sulfonamido, -S (O) 2 or oxo； each R1 "is independently C1-6 alkyl, cycloalkyl, heterocycloalkyl, C1-6 alkoxy, amino or amido, each optionally substituted with one or more R1"； each R1 '' 'is independently hydroxy, halo, amino, alkylamino, dialkylamino or heterocycloalkyl； R2 is -C (>； = O), -C (>； = O) O, -C (>； = O) NR2 ', -NHC (>； = O) O, -C (R2') 2, -O, - C (>； = NH) NR2 'or -S (>； = O) 2； each R2 'is independently H or C1-6 alkyl； R3 is H or R4； R 4 is C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 alkoxy, amino, C 1-6 alkyl, amino C 1-6 dialkyl, aryl, arylalkyl, alkylaryl, heteroaryl, alkylheteroaryl, heteroarylalkyl, cycloalkyl, alkylcycloalkyl, cycloalkylalkyl , heterocycloalkyl, alkylheterocycloalkyl, heterocycloalkylalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, spirocycloalkyl or spiroheterocycloalkyl, each of which is optionally substituted with one or more C1-6 alkyl, halo, C1-6-amino alkyl, dialkyl C1-6-amino, dialkyl hydroxy, C1-6 hydroxyalkyl, C1-6 alkoxy, halo, nitro, amino, amido, acyl, cyano, oxo, guanidino, hydroxylamino, carboxy, carbamoyl, carbamate, C1-6 haloalkoxy or C1-6 haloalkyl, in which two C1-6 alkyl groups together can form a ring； Q is CH or N； X is N； Y0 is H, halogen or C1-6 alkyl； Y1 is Y1b； Y1b is tert-butyl or iso-propyl； Y2 is H, halogen or C1-6 alkyl； Y3 is H or F； and Y4 is H, C1-6 alkyl or C1-6 hydroxyalkyl； or a pharmaceutically acceptable salt thereof.Un compuesto de Fórmula I:**Fórmula** en la que: ---- es un doble enlace； A es pirazol sustituido con uno o más A'； A' es -NHR o R4； R es H, -R1, -R1-R2-R3, -R1-R3 o -R
