发明名称 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
摘要 <p>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</p>
申请公布号 RU2213089(C2) 申请公布日期 2003.09.27
申请号 RU20000103212 申请日期 1998.07.07
申请人 JANSSEN FARMATSEVTIKA N.V. 发明人 BOSMAN ZHAN-POL' RENE MARI ANDRE;DE KLEJN MISHEL' ANNA JOZEF;SJURKIN MISHEL'
分类号 A61K31/4427;A61K31/443;A61K31/445;A61K31/4523;A61K31/4525;A61K31/453;A61K31/454;A61K31/4545;A61K31/497;A61K31/501;A61K31/502;A61P1/00;A61P1/10;A61P1/14;A61P43/00;C07C229/60;C07D211/42;C07D211/44;C07D401/06;C07D405/06;C07D405/12;C07D405/14;C07D417/14;C07D513/04;(IPC1-7):C07D211/42;A61K31/452 主分类号 A61K31/4427
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