公开(公告)号：US5106851A

公开(公告)日：1992-04-21

申请号：US474187

申请日：1990-02-02

申请人： Marco Turconi ,  Rosamarie Micheletti ,  Giovanni B. Schiavi ,  Arturo Donetti ,  Angelo Sagrada ,  Henri N. Doods

发明人： Marco Turconi ,  Rosamarie Micheletti ,  Giovanni B. Schiavi ,  Arturo Donetti ,  Angelo Sagrada ,  Henri N. Doods

IPC分类号： C07D209/48 ,  A61K31/435 ,  A61K31/46 ,  A61K31/47 ,  A61K31/496 ,  A61K31/505 ,  A61K31/517 ,  A61K31/54 ,  A61K31/55 ,  A61K31/5513 ,  A61P1/00 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  C07D207/06 ,  C07D211/62 ,  C07D215/54 ,  C07D239/78 ,  C07D239/80 ,  C07D243/10 ,  C07D279/02 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D451/02 ,  C07D451/04 ,  C07D451/12 ,  C07D451/14 ,  C07D453/02 ,  C07D471/06 ,  C07D471/08 ,  C07D487/08

CPC分类号： C07D451/04 ,  C07D215/54 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D451/12 ,  C07D451/14 ,  C07D453/02 ,  C07D471/08 ,  C07D487/08

摘要： Compounds of the formula (I) ##STR1## wherein R represents H or C.sub.1-6 alkyl;R.sub.1 and R.sub.2 represent H, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkythio, C.sub.1-6 alkoxycarbonyl, carboxyl, hydroxy, nitro, cyano, optionally C.sub.1-4 alkyl mono- or disubstituted carbamoyl, optionally C.sub.1-4 alkyl mono- or disubstituted amino, C.sub.1-6 acylamino, C.sub.1-4 alkoxy carbonylamino, C.sub.1-6 alkylsulphynyl, C.sub.1-6 alkylsulphonyl or C.sub.1-6 acyl;R.sub.3 represents H, C.sub.1-6 alkyl, aryl or aralkyl, or it may be absent;A represents CO or C.dbd.S;E represents nitrogen;D represents CO or CR.sub.4 R.sub.5 when the E--D bond is single, or D is C--R when the D--E bond is double, in which R.sub.4 represents H, C.sub.1-6 alkyl, aryl, aralkyl, hydroxy or C.sub.1-4 alkoxy and R.sub.5 represents H;X represents oxygen or N--R, or it is absent;Y represents a basic group selected from: ##STR2## in which n is 2 or 3; p is 0 or 1 at the same time or not; q is 0,2 or 3; R.sub.6 and R.sub.7 may be at the same time or not, H, C.sub.1-4 alkyl, aralkyl or, when R.sub.7 is H or C.sub.1-4 alkyl, R.sub.6 may be --CR.sub.8 .dbd.N--R in which R.sub.8 represents H, C.sub.1-4 alkyl or amino.

公开(公告)号：US5164386A

公开(公告)日：1992-11-17

申请号：US541106

申请日：1990-06-20

申请人： Enzo Cereda ,  Giuseppe Bietti ,  Giovanni B. Schiavi ,  Arturo Donetti ,  Antonio Schiavone ,  Henri N. Doods

发明人： Enzo Cereda ,  Giuseppe Bietti ,  Giovanni B. Schiavi ,  Arturo Donetti ,  Antonio Schiavone ,  Henri N. Doods

IPC分类号： C07D401/12 ,  A61K31/435 ,  A61K31/439 ,  A61K31/445 ,  A61K31/55 ,  A61P1/00 ,  A61P1/04 ,  A61P11/00 ,  A61P11/08 ,  A61P13/02 ,  A61P15/00 ,  A61P25/02 ,  C07D401/14 ,  C07D403/14 ,  C07D409/14 ,  C07D453/00 ,  C07D453/02

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) ##STR1## wherein R represents a linear or branched lower alkyl group, a cycloalkyl-C.sub.1-2 alkyl 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;R.sub.1 represents H, a linear or branched lower alkyl group or an acyl group of the type R.sub.2 --CO, in which R.sub.2 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 for the preparation of the compounds of formula (I) as well as pharmaceutical compositions containing them are also described.