JOSEPH MARIA GERARDUS BARBARA CALS,SANDER BERNARDUS NABUURS,VERA DE KIMPE,VERA D
申请号:
BR112017026231
公开号:
BR112017026231A2
申请日:
2016.06.03
申请国别(地区):
BR
年份:
2018
代理人:
摘要:
ror gamma modulators (rory)? The present invention relates to compounds according to formula I: (formula i) or a pharmaceutically acceptable salt thereof, wherein - a1-a8 are n or cr1-cr8, respectively, with the provision that not more than two of four positions a at a1-a4 can be simultaneously n and no more than two of the four positions a at a5-a8 can be simultaneously n; R1 -8 is independently h, halogen, amino, c (1-3) alkoxy, (di) c (13) alkylamino or c (16) alkyl; R9 is c (1-6) alkyl; R10 and R11 are independently h, f, methyl, ethyl, hydroxy or methoxy or R10 and R11 together are carbonyl, all alkyl groups, if present, optionally substituted by one or more f; R12 is h or c (1-6) alkyl; R13 is c (3-6) cycloalkyl, c (36) cycloalkyl (13) alkyl, c (2-5) heterocycloalkyl, c (25) heterocycloalkyl (1-3) alkyl, c (6-10) aryl, c (6-10) aryl (1-3) alkyl, c (19) heteroaryl or c (1-9) heteroaryl (1-3) alkyl; R14 is h, c (1-6) alkyl, c (2-6) alkenyl, c (3-6) cycloalkyl, c (36) cycloalkyl (13) alkyl, c (25) heterocycloalkyl, c ( 2-5) heterocycloalkyl (1-3) alkyl, c (6-10) aryl, c (6 10) aryl (1-3) alkyl, c (1-9) heteroaryl or c (1-9) heteroaryl (1 -3) alkyl; - or r13 and r14 are fused to form a ring having 5 to 7 atoms joining r13 which is c (1-6) alkyl or c (2-6) alkenyl with an independent substitutable within the definition of r14, all groups optionally substituted by one or more halogen, amino, hydroxy, cyano, c (13) alkoxy, c (13) alkoxycarbonyl, (di) and (13) alkylamino or c (13) alkyl. The compounds may be used as rory inhibitors and are useful for the treatment of rory mediated diseases.?moduladores de ror gama (rory)? a presente invenção se refere a compostos de acordo com a fórmula i: (fórmula i) ou um sal farmaceuticamente aceitável deste, em que - a1-a8 são n ou cr1-cr8, respectivamente, com a provisão de que não mais de duas das quatro posições a em a1-a4 possam ser simultaneamente n e que não mais que duas das quatro posições a em a5-a8 possa ser simultaneame