申请人:ISTITUTO DE ANGELI S.p.A.
公开号:EP0309425A3
公开(公告)日:1990-06-27
New pharmacologically active heterocyclic derivatives as muscarinic receptor blocking agents, useful for the treatment of gastrointestinal disorders of the following formula
wherein
R is hydrogen atom or C₁₋₉ alkyl optionally substituted by 2 or 3 radicals, which may be identical or different from each other, selected from aryl, cycloalkyl, hydroxy and carboxamide;
R₁ may be any group indicated for R, or NHR₄, in which R₄ is hydrogen atom, C₁₋₄ alkyl substituted by -OOCR₅, in which R₅ is methyl substituted by 2 or 3 radicals, which may be identical or different from each other, selected from aryl, cycloalkyl and hydroxy, or a cycloalkyl substituted by another cycloalkyl;
R₂ is hydrogen atom, C₁₋₄ alkyl, a radical -OOCR₅, in which R₅ is as hereinbefore defined;
R₃ is hydrogen atom or C₁₋₄ alkyl;
n is 0, 1 or 2
provided that at least one among R, R₁, R₂ and R₃ is different from hydrogen atom.The tautomers of the compounds of formula (I) and acid addition salts thereof, as well as the processes for their preparation and pharmaceutical compositions containing them are also described
新的药理活性杂环衍生物作为肌氨酸受体阻断剂,用于治疗以下化学式中的消化系统疾病,其中R是氢原子或C₁₋₉烷基,可由2或3个基团取代,这些基团可以相同或不同,从芳基、环烷基、羟基和羧酰胺中选择;R₁可以是任何R指示的基团,或NHR₄,在其中R₄是氢原子,C₁₋₄烷基,被-OOCR₅取代,其中R₅是甲基取代的2或3个基团,这些基团可以相同或不同,从芳基、环烷基和羟基中选择,或被另一个环烷基取代的环烷基;R₂是氢原子,C₁₋₄烷基,一个基团-OOCR₅,在其中R₅如前所定义;R₃是氢原子或C₁₋₄烷基;n为0、1或2,前提是R、R₁、R₂和R₃中至少有一个不同于氢原子。该化合物的互变异构体及其酸盐,以及其制备方法和含有它们的药物组合物也被描述。