BURGEY, Christopher S.,CROWLEY, Brendan M.,DENG, Zhengwu J.,PAONE, Daniel V.,POTTEIGER, Craig M.
申请号：
ES10756588
公开号：
ES2660892T3
申请日:
2010.03.15
申请国别(地区):
ES
年份:
2018
代理人:
摘要：
A compound of structural formula I: ** (See formula) ** or pharmaceutically acceptable salts and individual enantiomers and diastereomers thereof； for use in the treatment or prevention of chronic or acute pain, the treatment or control of epilepsy, or the improvement of sleep quality in a mammalian patient who needs it； wherein: A represents thienopyrazolyl, indazolyl or indolyl； B represents a bond, C1-6 alkyl, C2-6 alkenyl, C3-10 cycloalkyl, C5-10 heterocyclyl or C6-10 aryl； R1 represents H, C1-6 alkyl, halogen, (CH2) nCF3, C3-10 cycloalkyl, C (R2) 2OH, -O-, CN, (CH2) nOR2, NHC (O) R2, (CH2) C5- nheterocyclyl 10, (CH2) C6-10 naryl or C1-6 alkoxy； said alkyl, cycloalkyl, heterocyclyl and aryl optionally substituted with 1 to 3 C1-6 alkyl groups, halogen, hydroxyl, (CH2) nCF3 or CN； R2 represents H； R3 is selected from the group consisting of (CHRy) npyridyl, (CHRy) nooxyrpyridyl, (CHRy) npyrimidinyl, (CHRy) ntriazolyl, (CHRy) nphenyl, (CHRy) npyrazinyl, (CHRy) npyrazolyl, (CHRy) noxadiazol CHRy) nthiazolyl, (CHRy) nthiadiazolyl, (CHRy) nindazopyridyl ,, C1-6 alkyl and (CHRy) C3-6 cycloalkyl, all of which are optionally substituted with 1 to 3 groups of Ra, and in which Ry represents H, CF3, OH or C1-6 alkyl which is optionally substituted with 1 to 3 groups of Ra； or R2 and R3 can be combined with the nitrogen to which they are attached to form a C5-10 heterocyclyl optionally substituted with 1 to 3 groups of Ra； R4 and R5 independently represent H, (CH2) nOR2, CHF2, (CH2) C5-10 nheterocyclyl, (CH2) C6-10 naryl, C3-10 cycloalkyl, C1-6 alkoxy, C2-6 alkenyl, CF3, CF2, C (O) 1-2R2 or C1-6 alkyl； said alkyl, cycloalkyl, heterocyclyl and aryl optionally substituted with 1 to 3 groups of Ra； R6 represents hydrogen, OR2, (CH2) nCF3, halogen, C (R2) 2OR2, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, (CH2) C6-10 naryl, (CH2) C5-10 n-heterocyclyl, said alkyl, cycloalkyl, aryl and heterocyclyl optionally substituted with 1 to 3 groups of Ra； Ra represents C1-6 a
