公开(公告)号：EP0567767A1

公开(公告)日：1993-11-03

申请号：EP93104564.5

申请日：1993-03-19

申请人： BOEHRINGER INGELHEIM ITALIA S.p.A.

发明人： Cereda, Enzo ,  Dubini, Enrica ,  Ezhaya, Antoine ,  Maffione, Grazia ,  Turconi, Marco

IPC分类号： C07D451/04 ,  A61K31/46

CPC分类号： C07D451/04

摘要： Crystalline monohydrates of endo-2,3-dihydro-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2-oxo-1H-benzimidazole-1-carboxamide hydrochloride and of endo-3-ethyl-2,3-dihydro-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2-oxo-1H-benzimidazole-1-carboxamide hydrochloride of formula

(Compound 2a : R = H)
(Compound 2b : R = C₂H₅)
the processes for their preparation and pharmaceutical compositions containing them.

摘要翻译： 内-2,3-二氢-N-（8-甲基-8-氮杂双环[3.2.1]辛-3-基）-2-氧代-1H-苯并咪唑-1-甲酰胺盐酸盐的结晶一水合物， 3-乙基-2,3-二氢-N-（8-甲基-8-氮杂双环[3.2.1]辛-3-基）-2-氧代-1H-苯并咪唑-1-甲酰胺盐酸盐 （化合物2a：R = H>（化合物2b：R = C2H5）其制备方法和含有它们的药物组合物。

公开(公告)号：EP0404737A2

公开(公告)日：1990-12-27

申请号：EP90830281.3

申请日：1990-06-19

申请人： BOEHRINGER INGELHEIM ITALIA S.p.A.

发明人： Bietti, Giuseppe ,  Doods, Henri Nico ,  Cereda, Enzo ,  Schiavone, Antonio ,  Donetti, Arturo ,  Schiavi, Giovanni Battista

IPC分类号： C07D453/02 ,  A61K31/435

CPC分类号： C07D453/02

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.

摘要翻译： 描述了药用活性R（ - ）3-奎宁醇衍生物，它们是可用于治疗下式（I）的胃肠道和呼吸道障碍的毒蕈碱受体阻断剂，其中R表示直链或支链低级烷基，环烷基-C 1 烷基或芳烷基，或不存在; X代表有机或无机酸的阴离子，或当R不存在时它不存在; R 1代表H，直链或支链低级烷基或R 2 -CO型酰基，其中R 2是H或直链或支链低级烷基; A代表环烷基，芳香环或5-或6-元杂环; Y和Z可以同时或者可选地存在或不存在; 当它们同时存在时，它们代表氧气; 当其中只有一个存在时，它是氧气或硫磺; n是1,2或3; A和3-奎宁环基酯基团同时插入到环的相同碳原子上以产生孪位取代。 还描述了制备式（I）化合物的方法以及含有它们的药物组合物。

公开(公告)号：EP0567767B1

公开(公告)日：1998-07-29

申请号：EP93104564.5

申请日：1993-03-19

申请人： BOEHRINGER INGELHEIM ITALIA S.p.A.

发明人： Cereda, Enzo ,  Dubini, Enrica ,  Ezhaya, Antoine ,  Maffione, Grazia ,  Turconi, Marco

IPC分类号： C07D451/04 ,  A61K31/46

CPC分类号： C07D451/04

公开(公告)号：EP0404737A3

公开(公告)日：1992-03-11

申请号：EP90830281.3

申请日：1990-06-19

申请人： BOEHRINGER INGELHEIM ITALIA S.p.A.

发明人： Bietti, Giuseppe ,  Doods, Henri Nico ,  Cereda, Enzo ,  Schiavone, Antonio ,  Donetti, Arturo ,  Schiavi, Giovanni Battista

IPC分类号： C07D453/02 ,  A61K31/435

CPC分类号： C07D453/02

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.