发明公开
EP0309423A2 New benzimidazoline-2-oxo-1-carboxylic acid derivatives useful as 5-ht receptor antagonists
失效
苯并咪唑啉-2-氧代-1-羧基 - 衍生物，verwendbar als拮抗剂von 5-HT-Rezeptoren。
- 专利标题： New benzimidazoline-2-oxo-1-carboxylic acid derivatives useful as 5-ht receptor antagonists
- 专利标题（中）： 苯并咪唑啉-2-氧代-1-羧基 - 衍生物，verwendbar als拮抗剂von 5-HT-Rezeptoren。
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申请号： EP88830375.7申请日： 1988-09-19
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公开(公告)号： EP0309423A2公开(公告)日： 1989-03-29
- 发明人: Turconi, Marco , Donetti, Arturo , Micheletti, Rosamaria , Uberti, Annamaria , Nicola, Massimo , Giachetti, Antonio , Montagna, Ernesto
- 申请人： BOEHRINGER INGELHEIM ITALIA S.p.A.
- 申请人地址： Via Pellicceria, 10 I-50123 Firenze IT
- 专利权人： BOEHRINGER INGELHEIM ITALIA S.p.A.
- 当前专利权人： BOEHRINGER INGELHEIM ITALIA S.p.A.
- 当前专利权人地址： Via Pellicceria, 10 I-50123 Firenze IT
- 代理机构： Aimi, Luciano
- 优先权： IT2199787 19870923
- 主分类号： C07D451/12
- IPC分类号： C07D451/12 ; C07D453/02 ; C07D401/12 ; C07D451/14 ; C07D403/12 ; C07D453/06 ; C07D451/04 ; A61K31/46 ; A61K31/445 ; A61K31/435
摘要：
New pharmacologically active benzimidazoline-2-oxo-1-carboxylic acid derivatives which are 5-HT receptor antagonists useful as antiemetic agents and as gastric prokinetic agents of the following formula:
wherein R represents a hydrogen atom, C₁₋₆ alkyl, C₁₋₆ alkenyl or C₁₋₆ alkynil; R₁ and R₂ may be at the same time or not a hydrogen atom, halogen, trifluoromethyl, C₁₋₆ alkyl, C₁₋₆ alkoxy, C₁₋₆ alkylthio, C₁₋₆ acyl, carboxyl, C₁₋₆ alkoxycarbonyl, hydroxy, nitro, amino optionally C₁₋₄ alkyl N-mono or di-substituted, C₁₋₆ acylamino, C₁₋₆ alkoxycarbonylamino, carbamoyl optionally C₁₋₄ alkyl N-mono or di-substituted, cyano, C₁₋₆alkylsulphinyl, C₁₋₆ alkylsulphonyl, amino sulphonyl optionally C₁₋₄ alkyl N-mono or di-substituted, C₁₋₄ alkyl N-mono or di-substituted aminosulphonylamino, aminosulphonylamino; Y is oxygen or is N - R₃ in which R₃ is a hydrogen, a C₁₋₆ alkyl or optionally substituted by one or more C₁₋₆ alkoxy benzyl; A is a group selected from:
wherein p is 0, 1; r is 0, 1, 2, 3; R₄ is hydrogen atom or a C₁₋₄ alkyl; R₅ is a hydrogen atom, C₁₋₆ alkyl, C₃₋₈ cycloalkyl, C₃₋₈ cycloalkyl C₁₋₄ alkyl,substituted phenyl C₁₋₄ alkyl or R₅ is a group of formula
wherein R₆ is hydrogen atom, C₁₋₄ alkyl or an amino group and R₇ is hydrogen atom or C₁₋₆ alkyl, tautomers thereof and acid addition salts of the aforesaid compounds.
The processes for the preparation of the compounds of formula (I) as well as pharmaceutical compositions containing them are also described.
wherein R represents a hydrogen atom, C₁₋₆ alkyl, C₁₋₆ alkenyl or C₁₋₆ alkynil; R₁ and R₂ may be at the same time or not a hydrogen atom, halogen, trifluoromethyl, C₁₋₆ alkyl, C₁₋₆ alkoxy, C₁₋₆ alkylthio, C₁₋₆ acyl, carboxyl, C₁₋₆ alkoxycarbonyl, hydroxy, nitro, amino optionally C₁₋₄ alkyl N-mono or di-substituted, C₁₋₆ acylamino, C₁₋₆ alkoxycarbonylamino, carbamoyl optionally C₁₋₄ alkyl N-mono or di-substituted, cyano, C₁₋₆alkylsulphinyl, C₁₋₆ alkylsulphonyl, amino sulphonyl optionally C₁₋₄ alkyl N-mono or di-substituted, C₁₋₄ alkyl N-mono or di-substituted aminosulphonylamino, aminosulphonylamino; Y is oxygen or is N - R₃ in which R₃ is a hydrogen, a C₁₋₆ alkyl or optionally substituted by one or more C₁₋₆ alkoxy benzyl; A is a group selected from:
wherein p is 0, 1; r is 0, 1, 2, 3; R₄ is hydrogen atom or a C₁₋₄ alkyl; R₅ is a hydrogen atom, C₁₋₆ alkyl, C₃₋₈ cycloalkyl, C₃₋₈ cycloalkyl C₁₋₄ alkyl,substituted phenyl C₁₋₄ alkyl or R₅ is a group of formula
wherein R₆ is hydrogen atom, C₁₋₄ alkyl or an amino group and R₇ is hydrogen atom or C₁₋₆ alkyl, tautomers thereof and acid addition salts of the aforesaid compounds.
The processes for the preparation of the compounds of formula (I) as well as pharmaceutical compositions containing them are also described.
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