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ANALOGUES OF NONICEPTINE AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF

机译:基于其的去甲炔诺酮类药物和药物组成的类似物

摘要

FIELD: organic chemistry, pharmacy.;SUBSTANCE: invention relates to new biologically active compounds that are able to modulate the pharmacological response of one or some opioid receptors taken among ORL-1 and -receptors. Invention describes a compound of the formula (I): wherein W represents hydrogen atom, (C1-C10)-alkyl, (C1-C4)-alkyl-SO2N(V1)2, cyano-(C1-C10)-alkyl, (C1-C4)-alkyl-CON(V1)2, -NH2-SO2-(C1-C4)-alkyl-, (C1-C4)-alkyl-COOV1 wherein all V1 represent (C1-C6)-alkyl; Q represents a 6-membered aromatic group; n represents a whole number from 0 to 3; n' represents a whole number 0 or 1; A, B and C represent hydrogen atom; Z is taken among the group including a bond, linear or branched (C1-C6)-alkylene; R1 is taken among the group including hydrogen atom, (C1-C10)-alkyl, (C3-C12)-cycloalkyl, (C2-C10)-alkylene, (C3-C12)-cycloalkylamino-group, benzyl, (C3-C12)-cycloalkenyl, monocyclic, bicyclic or tricyclic aryl wherein indicated alkyl, cycloalkyl, alkenyl, (C3-C12)-cycloalkylamino-group or benzyl are optionally substituted with substitutes taken among the group including (C1-C10)-alkyl, phenyl, benzyl, benzyloxy-group wherein indicated phenyl, benzyl and benzyloxy-group are substituted optionally with (C1-C10)-alkyl and indicated (C3-C12)-cycloalkyl, (C3-C12)-cycloalkenyl, monocyclic, bicyclic or tricyclic aryl are substituted optionally with 1-3 substitutes taken among the group including (C1-C10)-alkyl and benzyl wherein indicated benzyl is substituted optionally with (C1-C10)-alkyl; R2 represents hydrogen atom and under condition that when n' = 0 then ZR1 doesn't means hydrogen atom (H), or to its pharmaceutically acceptable salt or solvate. Also, the invention describes a pharmaceutical composition based on thereof. Invention provides preparing new compounds possessing the useful biological properties.;EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.;21 cl, 5 tbl, 8 ex
机译:领域:本发明涉及新的生物活性化合物,其能够调节ORL-1和β受体之间的一种或某些阿片受体的药理反应。本发明描述了式(I)的化合物:<图像文件=“ 00000002.GIF” he =“ 71” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 43” />其中W代表氢原子,(C 1 -C 10 )-烷基,(C 1 -C 4 )-烷基-SO 2 N(V 1 2 ,氰基-(C 1 -C 10 )-烷基,(C 1 -C 4 )-烷基-CON(V 1 2 ,-NH < Sub> 2 -SO 2 -(C 1 -C 4 )-烷基-,(C 1 < / Sub> -C 4 )-烷基-COOV 1 ,其中所有V 1 表示(C 1 -C 6 )-烷基; Q代表6元芳族基团; n表示0到3的整数; n'表示整数0或1; A,B和C代表氢原子; Z选自包括直链或支链(C 1 -C 6 )亚烷基的基团; R 1 选自氢原子,(C 1 -C 10 )-烷基,(C 3 -C 12 )-环烷基,(C 2 -C 10 )-亚烷基,(C 3 -C 12 )-环烷基氨基,苄基,(C 3 -C 12 )-环烯基,单环,双环或三环芳基烷基,环烷基,烯基,(C 3 -C 12 )-环烷基氨基或苄基任选被选自(C 1 < / Sub> -C 10 )-烷基,苯基,苄基,苄氧基,其中所示的苯基,苄基和苄氧基可选地被(C 1 -C < Sub> 10 )-烷基并表示(C 3 -C 12 )-环烷基,(C 3 -C 12 )-环烯基,单环,双环或三环芳基被(C 1 -C 10 )组中的1-3个取代基取代-烷基和苄基,其中指示为苯yl任选被(C 1 -C 10 )-烷基取代; R 2 表示氢原子,并且在n'= 0时ZR 1 并不表示氢原子(H)或其可药用盐或溶剂化物。另外,本发明描述了基于其的药物组合物。本发明提供了制备具有有用生物学特性的新化合物。效果:化合物和药物组合物的有价值的医学特性。21 cl,5 tbl,8 ex

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