ARYLCYCLOALKYLAMINES DERIVATIVES NEUROPROTECTOR (VERSIONS), SUBSTANCES WITH COMBINED NEUROPROTECTOR, ANALGETIC AND ANTIDEPRESSIVE ACTION, PHARMACEUTICAL COMPOSITIONS BASED THEREON Russian patent published in 2017 - IPC C07C225/10 C07C225/20 C07C225/18 C07C225/22 C07C235/50 C07C235/54 C07C237/20 C07C237/34 C07C237/42 C07D309/14 C07D309/04 C07D207/277 C07D209/14 A61K31/16 A61K31/13 A61K31/351 A61K31/4453 A61K31/40 A61K31/4045 A61K31/5377 A61P29/00 A61P25/24 A61P25/28 

Abstract RU 2637928 C2

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

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RU 2 637 928 C2

Authors

Veselkina Olga Sergeevna

Borovitov Maksim Evgenevich

Kobelev Sergej Mikhajlovich

Sofronov Artem Vladimirovich

Dates

2017-12-08Published

2016-02-08Filed