MONOCYCLIC BENZAMIDES OF DERIVATIVES OF 3- OR 4-SUBSTITUTED 4-(AMINOMETHYL)PIPERIDINE, METHODS FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION, METHOD FOR ITS PREPARING, DERIVATIVE OF CARBOXYLIC ACID Russian patent published in 2003 - IPC

Abstract RU 2213089 C2

FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention describes compound of the formula (I) , its stereochemically isomeric form or its pharmaceutically acceptable additive salt of acid and base wherein R1 is C1-6-alkoxy; R2 is hydrogen atom, C1-6-alkyl, C1-6-alkoxy; R3 is hydrogen, halogen atom; R4 is hydrogen atom, C1-6-alkyl; R5 is hydrogen atom; Z is C3-6-cycloalkyl, C2-6- alkynyl, radical of the formula Alk-R6 (b-1), -Alk-X-R7 (b-2), -Alk-Y-C(=O)- R9 (b-3), -Alk-Y-C(=O)- NR11R12 (b-4) wherein each Alk is C1-12-alkanediyl; R6 is hydrogen atom, cyano-group, C1-6- alkylsulfonylamino-group, C3-6-cycloalkyl, Het'; R7 is C1-6-alkyl, hydroxy-C1-6-alkyl; X is oxygen atom; R9 is C1-6-alkyl, C1-6- alkoxy; Y is a direct bond; R11 and R12 each means independently C1-6-alkyl, or R11 and R12 linked with nitrogen atom carrying R11 and R12 can form pyrrolidinyl ring; Het' is taken among tetrahydrofuran dioxolan, dioxolan substituted with C1-6/ -alkyl, tetrahydropyran, pyridazinyl substituted with two substituents being each of that is taken independently among hydroxy-group, C1-6-alkyl, halogen atom; radical (C-1), (C-3), (C-4); R13 is C1-4-alkyl. Invention describes two methods for its preparing, pharmaceutical composition used for treatment of states associated with retention of stomach evacuation based on compound of the formula (I) and method for preparing the composition. Invention describes also intermediate monocyclic benzamide of derivative of 3- or 4-substituted 4-(aminomethyl)piperidine of the formula (III) and derivative of carboxylic acid of the formula (VI) given in the invention description used for synthesis of compound of the formula (I). Invention provides the usage of compounds of the formula (I) for treatment of states associated with disorders of stomach evacuation. EFFECT: improved preparing methods, valuable medicinal properties of compounds. 13 cl, 6 tbl, 18 ex

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RU 2 213 089 C2

Authors

Bosman Zhan-Pol' Rene Mari Andre

De Klejn Mishel' Anna Jozef

Sjurkin Mishel'

Dates

2003-09-27Published

1998-07-07Filed