DERIVATIVES OF 6-METHOXY-1H-BENZOTRIAZOLE-5-CARBOXAMIDE, METHOD OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION CONTAINING THEREOF

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes new derivatives of 6-methoxy- -1H-benzotriazole-5-carboxamide of the formula (I) where R means ethyl or cyclopropylmethyl; R means hydrogen atom, methyl or ethyl; n = 1, 2 or 3 and wavy line means that configuration of substituents a...

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Hauptverfasser: ESIMI KHIROKAVA, TOSIJA MORI, KHIROSI JAMAZAKI, NAOJUKI ESIDA, SIRO KATO
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes new derivatives of 6-methoxy- -1H-benzotriazole-5-carboxamide of the formula (I) where R means ethyl or cyclopropylmethyl; R means hydrogen atom, methyl or ethyl; n = 1, 2 or 3 and wavy line means that configuration of substituents at carbon atom bound with N-atom in amide group is (RS), (R) or (S), or pharmaceutically acceptable acid-additive salts. Invention describes also methods of their synthesis, pharmaceutical compositions containing the compound of the formula (I) or its pharmaceutically acceptable acid-additive salt and new intermediate compounds. Compounds show the simultaneous an antivomiting activity and activity enhancing the contractile capability of gastroenteric tract. Except for, they show the low depressant activity with respect to the central nervous system and therefore are useful for prophylaxis and treatment of functional disorders of gastroenteric tract associated with different diseases and therapeutic treatment as an agent enhancing the contractile capability of gastroenteric tract. EFFECT: improved method of synthesis of new compounds, valuable curative properties. 11 cl, 7 tbl, 4 dwg, 38 ex