申请人:Hoffmann-La Roche Inc.
公开号:US06113527A1
公开(公告)日:2000-09-05
The invention relates to compounds of the general formula ##STR1## wherein R.sup.1 is C.sub.6-12 -cycloalkyl, optionally substituted by lower alkyl or C(O)O lower alkyl, indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; acenaphthen-1-yl; bicyclo[3.3.1]non-9-yl, octahydro-inden-2-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl, decahydro-azulen-2-yl; bicyclo[6.2.0]dec-9-yl; decahydro-naphthalen-1-yl, decahydro-naphthalen-2-yl; tetrahydro-naphthalen-1-yl, tetrahydro-naphthalen-2-yl or 2-oxo-1,2-diphenyl-ethyl; R.sup.2 is .dbd.O or hydrogen, R.sup.3 is hydrogen, isoindolyl-1,3-dione, lower alkoxy, lower alkyl, amino, benzyloxy, --CH.sub.2 OR.sup.5 or --CH.sub.2 N(R.sup.5).sub.2 ; R.sup.4 is hydrogen or --CH.sub.2 OR.sup.5 ; R.sup.5 is hydrogen or lower alkyl; ##STR2## is cyclohexyl or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; to racemic mixtures and their corresponding enantiomers and or pharmaceutically acceptable acid addition salts thereof. The compounds of the present invention are agonists of the orphamin FQ (OFQ) receptor and therefore useful in the treatment of diseases, related to this receptor.
该发明涉及一般式##STR1##的化合物,其中R.sup.1是C.sub.6-12-环烷基,可以选择性地被较低的烷基或C(O)O较低的烷基取代,或者是indan-1-yl或indan-2-yl,可以选择性地被较低的烷基取代;acenaphthen-1-yl;bicyclo[3.3.1]non-9-yl;八氢基-茚-2-yl;2,3-二氢-1H-苯莰-1-yl;2,3,3a,4,5,6-六氢-1H-苯莰-1-yl;十氢基-茚-2-yl;bicyclo[6.2.0]庚-9-yl;十氢基-萘-1-yl;十氢基-萘-2-yl;四氢基-萘-1-yl;四氢基-萘-2-yl或2-氧代-1,2-二苯基-乙基;R.sup.2是.dbd.O或氢,R.sup.3是氢,异吲哚基-1,3-二酮,较低的烷氧基,较低的烷基,氨基,苄氧基,--CH.sub.2OR.sup.5或--CH.sub.2N(R.sup.5).sub.2;R.sup.4是氢或--CH.sub.2OR.sup.5;R.sup.5是氢或较低的烷基;##STR2##是环己基或苯基,可以选择性地被较低的烷基,卤素或烷氧基取代;对于该发明的化合物的外消旋混合物及其相应的对映体和/或药学上可接受的酸盐。本发明的化合物是orphamin FQ(OFQ)受体的激动剂,因此在与该受体相关的疾病的治疗中非常有用。