申请人:Hoffmann-La Roche Inc.
公开号:US06075034A1
公开(公告)日:2000-06-13
The present invention relates to compounds of the general formula wherein R.sup.1 is C.sub.5-12 -cycloalkyl, optionally substituted by lower alkyl; decahydro-naphthalen-1-yl; decahydro-naphthalen-2-yl; indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; decahydro-azulen-2-yl; bicyclo[6.2.0]dec-9-yl; acenaphthen-1-yl; bicyclo[3.3.1]non-9-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl; octahydro-inden-2-yl; 1,2,3,4-tetrahydro-naphthalen-1-yl; 1,2,3,4-tetrahydro-naphthalen-2-yl; naphthalen-lower alkyl-1-yl; naphthalen-lower alkyl-2-yl; acenaphthen-1-yl; and 5-isopropyl-2-methyl-bicyclo[3.1.0]hex-3-yl; R.sup.2, R.sup.3 are hydrogen; hydroxy; lower alkyl; .dbd.O; or phenyl, optionally substituted by lower allyl, halogen or alkoxy; R.sup.4 is hydrogen; lower alkyl; --(CH.sub.2).sub.n CH(OH)CF.sub.3 ; --(CH.sub.2).sub.n C.sub.3-6 -cycloalkyl; phenyl; benzyl; tetrahydrofuran-3-yl; --(CH.sub.2).sub.n OCH.sub.2 C.sub.6 H.sub.5 ; --(CH.sub.2).sub.n morpholinyl; 3-methyl-oxetan-3-yl-methyl; --(CH.sub.2).sub.n CH.sub.2 OH; --S(O).sub.2 -lower alkyl; --C(O)-lower alkyl; --C(O)CF.sub.3 ; --C(O)(CH.sub.2).sub.n OCH.sub.3 ; --(CH.sub.2).sub.n C(O)N(lower alkyl).sub.2 ; --S(O).sub.2 heteroaryl; --C(O)heteroaryl; --S(O).sub.2 -phenyl; --S(O).sub.2 --N(lower alkyl).sub.2 ; --C(O)--C.sub.3-6 -cycloalkyl; --C(O)O-phenyl; or --C(O)O-lower alkyl: R.sup.5 is hydrogen; halogen; lower alkyl; trifluoromethyl or lower alkoxy; n is 0-3; and to pharmaceutically acceptable acid addition salts thereof The compounds of formula I and their salts are useful as in the treatment of psychiatric, neurological and physiological disorders.
本发明涉及一般式化合物,其中R.sup.1为C.sub.5-12-环烷基,可选地被低碳烷基取代;十氢萘-1-基;十氢萘-2-基;茚-1-基或茚-2-基,可选地被低碳烷基取代;十氢萜烯-2-基;双环[6.2.0]癸-9-基;芴-1-基;双环[3.3.1]壬-9-基;2,3-二氢-1H-苯并-1-基;2,3,3a,4,5,6-六氢-1H-苯并-1-基;八氢茚-2-基;1,2,3,4-四氢萘-1-基;1,2,3,4-四氢萘-2-基;萘-低碳烷基-1-基;萘-低碳烷基-2-基;芴-1-基;和5-异丙基-2-甲基-双环[3.1.0]己-3-基; R.sup.2,R.sup.3为氢;羟基;低碳烷基; .dbd.O;或苯基,可选地被低烯丙基,卤素或烷氧基取代;R.sup.4为氢;低碳烷基;--(CH.sub.2).sub.n CH(OH)CF.sub.3;--(CH.sub.2).sub.n C.sub.3-6-环烷基;苯基;苄基;四氢呋喃-3-基;--(CH.sub.2).sub.n OCH.sub.2 C.sub.6 H.sub.5;--(CH.sub.2).sub.n 嘧啶基;3-甲基-噁唑-3-基-甲基;--(CH.sub.2).sub.n CH.sub.2 OH;--S(O).sub.2-低碳烷基;--C(O)-低碳烷基;--C(O)CF.sub.3;--C(O)(CH.sub.2).sub.n OCH.sub.3;--(CH.sub.2).sub.n C(O)N(低碳烷基).sub.2;--S(O).sub.2杂环芳基;--C(O)杂环芳基;--S(O).sub.2-苯基;--S(O).sub.2--N(低碳烷基).sub.2;--C(O)--C.sub.3-6-环烷基;--C(O)O-苯基;或--C(O)O-低碳烷基: R.sup.5为氢;卤素;低碳烷基;三氟甲基或低碳基氧基; n为0-3;以及其药学上可接受的酸加盐。公式I的化合物及其盐在治疗精神病学、神经学和生理学疾病中有用。