首页> 外国专利> ARYLCYCLOALKYLAMINES DERIVATIVES NEUROPROTECTOR (VERSIONS), SUBSTANCES WITH COMBINED NEUROPROTECTOR, ANALGETIC AND ANTIDEPRESSIVE ACTION, PHARMACEUTICAL COMPOSITIONS BASED THEREON

ARYLCYCLOALKYLAMINES DERIVATIVES NEUROPROTECTOR (VERSIONS), SUBSTANCES WITH COMBINED NEUROPROTECTOR, ANALGETIC AND ANTIDEPRESSIVE ACTION, PHARMACEUTICAL COMPOSITIONS BASED THEREON

机译:芳基神经酰胺衍生物(版本),具有神经保护剂组合的物质,镇痛和抗抑郁作用,基于其的药物成分

摘要

FIELD: pharmacology.;SUBSTANCE: invention relates to new arylcycloalkylamines of the general formula ; . In the general formula (I), R1, R2 are H, linear or branched alkyl (C1-C4), linear or branched alkoxy (C1-C4), halogen; Y is -CH2-O-CH2-, - (CH2)n-, where n: 1-3; X is -CO-NH-(CH2)6-, -CO-(CH2)k-, -CH2-NH-(CH2)6-, -CH(CH3)-NH-(CH2)6-, -(CO)p-(CHR5)m, where p, m-: 0, 1, k: 2, 4-7, R5: H, linear alkyl C1-C5; R3, R4 are H, linear alkyl C1-C4, -CH2-C≡CH, -(CH2)2-O-(CH2)2-NH2, cyclopropyl, cyclopropylmethyl; 4-pyridinyl, an amino acid residue of a proteinogenic acyclic or aromatic α-amino acids, γ-aminobutyric acid, ε-aminocaproic acid, β-alanine; -CHR6-CH2-OR7, where R6: H or a linear or branched alkyl C1-C4, benzyl, R7: H, linear alkyl C1-C4, or R3, R4 together with the nitrogen to which they are attached, form a pyrrolidine, 2-(hydroxymethyl) pyrolidine, 4-aminopyridinium ring; G is (C1-C4) carboxylic acid, methanesulfonic acid or a mineral acid or water. As an acyclic or aromatic α-amino acid residue, they contain a proteinogenic α-amino acid residue. As (C1-C4) carboxylic acid, they contain at least one compound from the group consisting of acetic, fumaric, succinic, tartaric, malic and maleic acids. As a mineral acid, they contain at least one compound from the group consisting of hydrochloric, phosphoric, sulfuric acids. The preferred compounds are arylcycloalkylamine derivatives of the general formula , wherein Y: -CH2-O-CH2-, -(CH2)2-. The invention also relates to a pharmaceutical composition which can be a combination of arylcycloalkylamine derivatives and at least one substance from the group comprising levodopa, palmitoyle ethanolamide, N-(2-aminoethyl) palmitamide hydrochloride, rasagiline, risperidone, toloxaton, quetiapine, gamma-aminobutyric acid, sodium valproate, amitriptyline, clomepramine, fluoxetine, paroxetine, sertraline, phenylephrine, dexamethasone, prednisolone. The composition may be in the form of a tablet, capsule, pellet, powder for preparation of a solution for enteral administration, a solution for parenteral administration, a powder for preparation of a solution for parenteral administration.;EFFECT: neuroprotective, analgesic and antidepressant action.;11 cl, 13 tbl, 96 ex
机译:发明领域本发明涉及具有通式的新的芳基环烷基胺。 。通式(I)中,R 1 ,R 2 为H,直链或支链烷基(C 1 -C 4 ),直链或支链烷氧基(C 1 -C 4 ),卤素; Y是-CH 2 -O-CH 2 -,-(CH 2 n -,其中n :1-3; X是-CO-NH-(CH 2 6 -,-CO-(CH 2 k -,-CH 2 -NH-(CH 2 6 -,-CH(CH 3 )- NH-(CH 2 6 -,-(CO) p -(CHR 5 m ,其中p,m-:0,1,k:2,4-7,R 5 :H,直链烷基C 1 -C < Sub> 5 ; R 3 ,R 4 是H,直链烷基C 1 -C 4 ,-CH 2 -C≡CH,-(CH 2 2 -O-(CH 2 2 -NH 2 ,环丙基,环丙基甲基; 4-吡啶基,蛋白原性无环或芳族α-氨基酸,γ-氨基丁酸,ε-氨基己酸,β-丙氨酸的氨基酸残基; -CHR 6 -CH 2 -OR 7 ,其中R 6 :H或直链或支链烷基C 1 -C 4 ,苄基,R 7 :H,直链烷基C 1 -C 4 或R 3 ,R 4 与它们所连接的氮一起形成吡咯烷,2-(羟甲基)吡咯烷,4-氨基吡啶环; G是(C 1 -C 4 )羧酸,甲磺酸或无机酸或水。作为无环或芳族α-氨基酸残基,它们包含蛋白原性α-氨基酸残基。作为(C 1 -C 4 )羧酸,它们包含至少一种选自乙酸,富马酸,琥珀酸,酒石酸,苹果酸和马来酸的化合物。作为无机酸,它们含有至少一种选自盐酸,磷酸,硫酸的化合物。优选的化合物是通式为<图像文件=“ 00000167.JPG” he =“ 30” imgContent =“ undefined” imgFormat =“ JPEG” wi =“ 59” />的芳基环烷基胺衍生物,其中Y:-CH 2 -O-CH 2 -,-(CH 2 2 -。本发明还涉及一种药物组合物,其可以是芳基环烷基胺衍生物和至少一种选自左旋多巴,棕榈酰乙醇酰胺,N-(2-氨基乙基)棕榈酰胺盐酸盐,雷沙吉兰,利培酮,托洛沙酮,喹硫平,γ-氨基丁酸,丙戊酸钠,阿米替林,氯米帕明,氟西汀,帕罗西汀,舍曲林,去氧肾上腺素,地塞米松,泼尼松龙。该组合物可以是片剂,胶囊剂,丸剂,用于制备肠内给药溶液的粉末,用于肠胃外给药的溶液,用于制备用于肠胃外给药的溶液的粉末的形式;效果:神经保护,镇痛药和抗抑郁药动作。; 11 cl,13 tbl,96前

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