DERIVATIVES OF 1-[(1-SUBSTITUTED-4-PIPERIDINYL)- METHYL]-4-PIPERIDINE, METHODS FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND INTERMEDIATE SUBSTANCES

FIELD: organic chemistry, chemical technology, medicine, pharmacy. SUBSTANCE: invention relates to novel derivatives of 1-[(1-substituted-4-piperidinyl)methyl]-4-piperidine of the formula (I) wherein Ar represents group of the formula (Ar-1) or (Ar-2) wherein R1 represents halogen atom; R2 represent...

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Hauptverfasser: TATEISI KHIROTAKA, MORIKAGE KATSUO, KATO SIRO, ESIDA NAOJUKI, TOETOMI ESIKHITO, KHARADA KHIROSI, MORIKAGE JUKIKO
Format: Patent
Sprache:eng
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Zusammenfassung:FIELD: organic chemistry, chemical technology, medicine, pharmacy. SUBSTANCE: invention relates to novel derivatives of 1-[(1-substituted-4-piperidinyl)methyl]-4-piperidine of the formula (I) wherein Ar represents group of the formula (Ar-1) or (Ar-2) wherein R1 represents halogen atom; R2 represents hydrogen atom or lower alkyl; R3 represents hydrogen atom, lower alkyl or lower alkanoyl; R4 represents hydrogen atom or lower alkyl; R5 and R5 are similar or different and represent hydrogen atom or lower alkyl; n = 1, 2 or 3; A represents group of the formula (A-1), (A-2) or (A-3): -Z-N(Q1)(Q2) (A-1) wherein Z represents CO-, CS or ; Q1 and Q2 are similar or different and represent hydrogen atom, lower alkyl, cycloalkyl, unsubstituted or substituted phenyl or phenyl- (lower alkyl); or Q1 and Q2 in common with nitrogen atom form pyrrolidine, piperidine, hexahydroazepine, morpholine, thiomorpholine or piperazine ring; -CO-R7 (A-2) wherein R7 represents hydrogen atom, lower alkyl, lower alkoxy-group, lower alkoxycarbonyl, substituted lower alkyl; (A-3) wherein p = 0, 1, 2, 3, 4, 5; R8 represents hydrogen atom or lower alkyl; R9 represents lower alkyl or alkoxy-group, or to pharmaceutically acceptable salts. Compounds of the formula (I) show agonistic activity with respect to serotonin receptors-4 and can be used for treatment of gastroenteric disorders. EFFECT: improved preparing method, valuable medicinal properties of compounds. 25 cl, 9 tbl, 106 ex