首页> 外国专利> ORPHANIN FQ (OFQ) RECEPTOR AGONIST AND/OR ANTAGONIST DIAZA-SPIRO3,5NONANE DERIVATIVES, PREPARATION AND USE THEREOF

ORPHANIN FQ (OFQ) RECEPTOR AGONIST AND/OR ANTAGONIST DIAZA-SPIRO3,5NONANE DERIVATIVES, PREPARATION AND USE THEREOF

机译:ORPHANIN FQ(OFQ)受体激动剂和/或拮抗剂重氮-螺[3,5]壬烷衍生物,制备及其用途

摘要

The invention relates to compounds of the general formula CHEM wherein R1 is C6-12-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; bicycloÄ3.3.1Ünon-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; bicycloÄ6.2.0Üdec-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; R2 is =O or hydrogen, R3 is hydrogen, isoindolyl-1,3-dione, lower alkoxy, lower alkyl, amino, benzyloxy, -CH2OR5 or -CH2N(R5)2; R4 is hydrogen or -CH2OR5; R5 is hydrogen or lower alkyl; A &cir& 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 and/or antagonists of the orphamin FQ (OFQ) receptor and therefore useful in the treatment of diseases, related to this receptor.
机译:本发明涉及通式的化合物,其中R 1是C6-12-环烷基,其任选地被低级烷基或C(O)O低级烷基,茚满-1-基或茚满-2-基取代,任选地被低级烷基取代; acenaphthen-1-yl;双环3.3.1非9基,八氢茚基-2-基; 2,3-二氢-1H-苯-1-基; 2,3,3a,4,5,6-六氢-1H-苯-1-基,十氢-azulen-2-基; bicycloÄ6.2.0Üdec-9-yl;十氢萘-2-基;十氢萘-2-基;四氢萘-1-基,四氢萘-2-基或2-氧代1,2-二苯基乙基; R 2为= O或氢,R 3为氢,异吲哚基-1,3-二酮,低级烷氧基,低级烷基,氨基,苄氧基,-CH 2 OR 5或-CH 2 N(R 5)2 ; R 4为氢或-CH 2 OR 5; R 5为氢或低级烷基; A cir是环己基或苯基,任选地被低级烷基,卤素或烷氧基取代;外消旋混合物及其相应的对映异构体和/或其药学上可接受的酸加成盐。本发明的化合物是Orphamin FQ(OFQ)受体的激动剂和/或拮抗剂,因此可用于治疗与该受体有关的疾病。

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