发明公开
- 专利标题: New R(-) 3-quinuclidinol derivatives
- 专利标题(中): 新的R( - )3-奎宁环醇衍生物
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申请号: EP90830281.3申请日: 1990-06-19
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公开(公告)号: EP0404737A2公开(公告)日: 1990-12-27
- 发明人: Bietti, Giuseppe , Doods, Henri Nico , Cereda, Enzo , Schiavone, Antonio , Donetti, Arturo , Schiavi, Giovanni Battista
- 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: IT2092989 19890620
- 主分类号: C07D453/02
- IPC分类号: C07D453/02 ; A61K31/435
摘要:
Pharmacologically active R(-) 3-quinuclidinol derivatives are described which are muscarinic receptor blocking agents useful for the treatment of gastrointestinal and respiratory tract disorders of the following formula (I)
wherein
R represents a linear or branched lower alkyl group, a cycloalkyl-C₁₋₂alkyl or an aralkyl group, or it is absent;
X represents the anion of an organic or inorganic acid, or it is absent, when R is absent;
R₁ represents H, a linear or branched lower alkyl group or an acyl group of the type R₂-CO, in which R₂ is H or a linear or branched lower alkyl group;
A represents a cycloalkyl, an aromatic ring or a 5- or 6-membered heterocyclic ring;
Y and Z may be simultaneously or alternatively present or absent; when they are simultaneously present, they represent oxygen; when only one of them is present, it is oxygen or sulphur;
n is 1, 2 or 3;
A and the 3-quinuclidinyl ester groups are inserted simultaneously on the same carbon atom of the ring to give rise to a geminal substitution.
The process of the preparation of the compounds of formula (I) as well as pharmaceutical compositions containing them are also described.
wherein
R represents a linear or branched lower alkyl group, a cycloalkyl-C₁₋₂alkyl or an aralkyl group, or it is absent;
X represents the anion of an organic or inorganic acid, or it is absent, when R is absent;
R₁ represents H, a linear or branched lower alkyl group or an acyl group of the type R₂-CO, in which R₂ is H or a linear or branched lower alkyl group;
A represents a cycloalkyl, an aromatic ring or a 5- or 6-membered heterocyclic ring;
Y and Z may be simultaneously or alternatively present or absent; when they are simultaneously present, they represent oxygen; when only one of them is present, it is oxygen or sulphur;
n is 1, 2 or 3;
A and the 3-quinuclidinyl ester groups are inserted simultaneously on the same carbon atom of the ring to give rise to a geminal substitution.
The process of the preparation of the compounds of formula (I) as well as pharmaceutical compositions containing them are also described.
公开/授权文献
- EP0404737A3 New R(-) 3-quinuclidinol derivatives 公开/授权日:1992-03-11
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