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4- (diarylmethyl) -1-piperazinyl derivatives

机译:4-(二芳基甲基)-1-哌嗪基衍生物

摘要

A compound of formula I wherein X, Y, X' & Y' are selected from hydrogen, halogen, substituted or unsubstituted alkyl (linear, branched or cyclo), aryl, alkyloxy and haloalkyl group; RSUB1/SUB, RSUB2/SUB, RSUB3 /SUB& RSUB4 /SUBare selected from hydrogen, substituted or unsubstituted alkyl groups (linear, branched or cyclo), aryl, heteroaryl groups or aralkyl groups, heterocycles containing one or more of hetero atoms (viz., N, S, O), substituted or unsubstituted alkenyl or alkynyl groups of carbon 2 to 6; wherein the substituents RSUB1 /SUB& RSUB2 /SUBon the piperazinyl moiety are either syn or anti to each other and optionally RSUB3 /SUBand RSUB4 /SUBtogether with the carbons to which they are attached form a monocyclic saturated or aryl or substituted aryl or heteroaryl or substituted heteroaryl ring containing one or more hetero atoms selected from N, S and O with a ring size ranging from 3 to 6; with a proviso that when RSUB3 /SUB& RSUB4 /SUBtogether do not form part of a ring they may exist in either E or Z configuration; RSUB5 /SUBis (CHSUB2/SUB)SUBn/SUB-O-CHSUB2/SUB-CO-Z wherein n is 1 to 6; Z is selected from OH, OR, NRR', N(OR)R', N(R)-N(R)R'and wherein R & R' are selected from hydrogen, substituted or unsubstituted alkyl groups (linear, branched or cyclo), aryl, heteroaryl groups or aralkyl groups, heterocycles containing one or more of hetero atoms (viz., N, S, O), substituted or unsubstituted alkenyl or alkynyl groups of carbon 2 to 6; and B is selected from -(CH 2 )n-(n is 1 to 6) and -(CH 2 )x-D-(CH 2 )y where D is O, NR, S or SO 2 , x and y are independently 1 to 6; and m is selected from 1 to 6; and pharmaceutically acceptable salts thereof.
机译:式I化合物,其中X,Y,X′和Y′选自氢,卤素,取代或未取代的烷基(直链,支链或环),芳基,烷氧基和卤代烷基; R 1 ,R 2 ,R 3 和R 4 选自氢,取代或未取代的烷基(直链,支链或环),芳基,杂芳基或芳烷基,含有一个或多个杂原子(即N,S,O),碳原子数2至6的取代或未取代的烯基或炔基的杂环;其中哌嗪基部分上的取代基R 1 和R 2 彼此同位或反位,并且任选地R 3 和R 4 与它们所连接的碳一起形成一个单环饱和或芳基或取代的芳基或杂芳基或取代的杂芳基环,其包含一个或多个选自N,S和O的杂原子,其环尺寸为3至6;附带条件是,当R 3 &R 4 一起不形成环的一部分时,它们可能以E或Z构型存在; R 5 是(CH 2 n -O-CH 2 -CO-Z其中n为1至6; Z选自OH,OR,NRR',N(OR)R',N(R)-N(R)R',其中R和R'选自氢,取代或未取代的烷基(直链,支链或环),芳基,杂芳基或芳烷基,含有一个或多个杂原子(即N,S,O),碳原子数为6至6的取代或未取代的烯基或炔基的杂环;并且B选自-(CH 2)n-(n为1至6)和-(CH 2)xD-(CH 2)y,其中D为O,NR,S或SO 2,x和y独立为1至6; m选自1至6;及其药学上可接受的盐。

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