LINZ, KLAUS,KOEGEL, BABETTE-YVONNE,SCHROEDER, WOLFGANG,CHRISTOPH, THOMAS,DE VRY, JEAN,FRIDERICHS, ELMAR
申请号：
ES10003202
公开号：
ES2377482T3
申请日:
2007.09.26
申请国别(地区):
ES
年份:
2012
代理人:
摘要：
Compounds that have an affinity for the opioid-μ receptor of at least 100 nM (human Ki value) and an affinity for the ORL-1 receptor, oscillating the ratio between ORL1 / μ affinities, defined as 1 / [Ki (ORL1 ) / Ki (μ)], between 0, 1 and 30, and which consist of spirocyclic cyclohexane derivatives of general formula (I) where R1 and R2 represent, independently of each other, H or CH3, R1 and R2 not being equal to H at the same time； R3 represents phenyl, benzyl or heteroaryl, in each case unsubstituted or mono- or polysubstituted with F, Cl, OH, CN or OCH3； W represents NR4, O or S； R4 H being (C1-5) alkyl, phenyl, phenyl linked through a (C1-3) alkyl group, COR12； SO2R12； where R12 means H, linear or branched (C1-7) alkyl, saturated or unsaturated, unsubstituted or mono- or polysubstituted with OH, F or COO (C1-4) alkyl； cycloalkyl (C4-6)； aryl or heteroaryl, unsubstituted or mono- or polysubstituted with F, Cl, Br, CF3, OCH3, linear or branched (C1-4) alkyl, unsubstituted or substituted with F, Cl, CN, CF3, OCH3 or OH； or phenyl or heteroaryl linked through a saturated or unsaturated (C1-3) alkyl, unsubstituted or mono- or polysubstituted with F, Cl, Br, CF3, OCH3, linear or branched (C1-4) alkyl, unsubstituted or substituted with F, Cl, CN, CF3, OCH3 or OH； or (C5-6) cycloalkyl linked through a saturated or unsaturated (C1-3) alkyl； OR13； NR14R15； R5 represents H； COOR13, CONR13, OR13, saturated or unsaturated (C1-5) alkyl, linear or branched, unsubstituted or mono- or polysubstituted with OH, F, CF3 or CN； R6 represents H； or R5 and R6 mean together (CH2) n, with n = 2, 3, 4, 5 or 6, some individual hydrogen atoms can also be substituted by F, Cl, NO2, CF3, OR13, CN or (C1-5) alkyl )； R7, R8, R9 and R10 independently represent H, F, Cl, Br, NO2, CF3, OH, OCH3, CN, COOR13, NR14R15； (C1-5) alkyl, heteroaryl, unsubstituted or mono- or polysubstituted with benzyl, CH3, Cl, F, OCH3 or OH； R13 being equal to H or (C1-5) alkyl； meaning R14 and R15, independently of e
