首页> 外国专利> 1.3 - diaminopropane substituted Derivatives, Process for their preparation, medicinal and Pharmaceutical compositions containing them and Use thereof for the preparation of medicaments for the prophylaxis and / or treatment of urinary incontinence, Pain, pruritus, tinnitus, diarrhea and / or AURIUM

1.3 - diaminopropane substituted Derivatives, Process for their preparation, medicinal and Pharmaceutical compositions containing them and Use thereof for the preparation of medicaments for the prophylaxis and / or treatment of urinary incontinence, Pain, pruritus, tinnitus, diarrhea and / or AURIUM

机译:1.3-二氨基丙烷取代的衍生物,其制备方法,含有它们的药物和药物组合物及其在制备用于预防和/或治疗尿失禁,疼痛,瘙痒,耳鸣,腹泻和/或AURIUM的药物中的用途

摘要

1. The derivatives of propane-1,3-diamond were replaced by No.1 total structure;R1 represents C1-12, cycloquilo C3-8, (c1-6-tar) - cycloquilo C3-8 or arilo; R2 represents C1-12, cycloquilo C3-8, arilo, (c1-6-tar) - cyclo-8, (C1-6) - arilo, isopropene, isopropyl or - (c1-6-tar) - isopropene, provided that R1 and 2 are both asymmetric or asymmetric. R2 together forms the radical - (CH2) m -.6) - C1-6) - c1c1-6 - (c1c1-6) - C1-6) - R7; R4 represents h, C1-12, C1-12, cycloquilo C3-8, arilo, - (c1-6-tar) - cycloquilo C3-8, - (c1-6-tar) - arilo, isopropene or - (c1-6-tar) - isopropene; or R3 and R4 combine to form radical - (CH2) n -,N = 3, 4, 5, 6 or 7, or radical - (CH2) 2-x - (CH2) 2,where X = O, S or NR8, and in which - (CH2) n- or - (CH2) 2-X- (CH2) 2- can be unsubstituted or substituted with C1-6 alkyl, R5 and R6 independently represent between yes C1-12 alkyl, C3-8 cycloalkyl, aryl, - (C1-6 alkyl) -C3-8 cycloalkyl, (C1-6 alkyl) -aryl, or together form the radical - (CH2) or-,If o = 3, 4, 5, 6 or 7, or radical - (CH2) 2 - (CH2) 2,where Y = O, S or NR9, being able to - (CH2) or- or - (CH2) 2-Y- (CH2) 2 be unsubstituted or substituted with C1-6 alkyl; A represents aryl, heteroaryl, C (= O) OR10 or 2-propyl; R 7 represents C 1-6 alkyl, C 3-8 cycloalkyl, aryl, heterocyclyl, - (C 1-6 alkyl) -C 3-8 cycloalkyl, - (C 1-6 alkyl) -aryl or - (C 1-6 alkyl) -heterocyclyl; R 8 and R 9 independently represent each other H, C 1-6 alkyl, C 3-8 cycloalkyl, aryl, - (C 1-6 alkyl) -C 3-8 cycloalkyl, - (C 1-6 alkyl) -aryl, or heterocyclyl; R 10 represents C 1-6 alkyl, C 3-8 cycloalkyl, aryl, - (C 1-6 alkyl) -C 3-8 cycloalkyl, or - (C 1-6 alkyl) -aryl; the compound of the general structure (1) being in the form of a racemate,1. In the form of one or more non enantiomers or one or more corresponding isomers, but compounds n, N-dimethyl - [phenyl - (2-pirrolidin-1-il-cyclohexyl) - methyl] - amines, N, N-dimethyl - [(2-moroflin-4-il-cyclohexyl) - phenyl methyl] - amines, 4 - [phenyl - (2-pirrolidin-1-il-cyclohexyl) - methyl] - pyrylides - methyl methyl methyl methyl methyl methyl methyl Di Di Di Di Di 1,3-diphenyl-3 - (n; n-diethylmethyl) - propyl) - amine, 4 - (1, 3-diphenyl-3-pirolin-1-il-propylmorphine,N. N, N-dimethyl - (2-methyl-1-phenyl-3 - (morfolin-4-il) - pentachlorobenzene) - amine, benzene - [2 - (dimethyl-phenyl-methyl) - cyclohexane] - amine (2-methyl-1, 3-diphenyl-3-piperididin-1-il-propyl) - propyl amine, its preparation procedure, drug and drug synthesis containing these substances, And drugs for the treatment and / or prevention of pain, incontinence, pruritus, dinitrus aureum and / or diarrhea.
机译:1.将丙烷-1,3-金刚石的衍生物替换为总结构No.1; R 1代表C 1-12,环基C3-8,(c1-6-tar)-环基C3-8或芳基; R2代表C1-12,环基C3-8,芳基,(c1-6-tar)-环8,(C1-6)-芳基,异丙基,异丙基或-(c1-6-tar)-异丙基,条件是R1和2都是不对称或不对称的。 R 2一起形成基团-(CH 2)m -.6)-C1-6)-c1c1-6-(c1c1-6)-C1-6)-R7; R 4代表h,C1-12,C1-12,环基C3-8,芳基--(c1-6-tar)-环基C3-8,-(c1-6-tar)-芳基,异丙烯或-(c1- 6-焦油)-异丙烯;或R3和R4结合形成基团-(CH2)n-,N = 3、4、5、6或7,或基团-(CH2)2-x-(CH2)2,其中X = O,S或NR8且其中-(CH 2)n-或-(CH 2)2 -X-(CH 2)2-可以是未取代的或被C 1-6烷基取代,R 5和R 6独立地表示是C 1-12烷基,C 3-8环烷基,芳基,-(C 1-6烷基)-C 3-8环烷基,(C 1-6烷基)-芳基,或一起形成基团-(CH 2)或-,如果o = 3、4、5、6或7或基团-(CH2)2-(CH2)2,其中Y = O,S或NR9,能够使-(CH2)或-或-(CH2)2-Y-(CH2)2被未取代或取代为C 1-6烷基; A代表芳基,杂芳基,C(= O)OR 10或2-丙基; R 7代表C 1-6烷基,C 3-8环烷基,芳基,杂环基,-(C 1-6烷基)-C 3-8环烷基,-(C 1-6烷基)-芳基或-(C 1- 6烷基)-杂环基; R 8和R 9彼此独立地表示H,C 1-6烷基,C 3-8环烷基,芳基,-(C 1-6烷基)-C 3-8环烷基,-(C 1-6烷基)-芳基或杂环基; R 10代表C 1-6烷基,C 3-8环烷基,芳基,-(C 1-6烷基)-C 3-8环烷基或-(C 1-6烷基)-芳基;通式(1)的化合物为外消旋体形式,1。以一种或多种非对映异构体或一种或多种相应异构体的形式存在,但化合物n,N-二甲基-[苯基-(2-吡咯烷-1--1-环己基)-甲基]-胺,N,N-二甲基- [(2-moroflin-4-il-cyclohexyl)-苯甲基]-胺,4-[苯基-(2-pirrolidin-1-il-cyclohexyl)-甲基]-吡啶盐-甲基甲基甲基甲基甲基甲基甲基Di Di Di Di Di 1,3-diphenyl-3--(n; n-diethylmethyl)-propyl)-胺,4-(1,3-diphenyl-3-pirolin-1-il-propylmorphine,N.N,N-二甲基-(2-甲基-1-苯基-3-(吗啉-4-il)-五氯苯)-胺,苯-[2--(二甲基苯基甲基)-环己烷]-胺(2-甲基-1,3 (-diphenyl-3-piperididin-1-il-propyl)-丙胺,其制备程序,包含这些物质的药物和药物合成,以及用于治疗和/或预防疼痛,尿失禁,瘙痒,金黄色的双耳炎和/或的药物腹泻。

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