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    • 4. 发明专利
    • DE3763863D1
    • 1990-08-30
    • DE3763863
    • 1987-02-17
    • WARNER LAMBERT CO
    • BUTLER DONALD EMOOS WALTER HDODD JOHN HTECLE HAILE
    • A61K31/445A61K31/4433A61K31/4465A61K31/451A61K31/455A61P25/28C07D211/78C07D333/00C07D401/06C07D409/04C07D413/06C07D413/12
    • 1,2,3,6-Tetrahydro- and 1,2,5,6-tetrahydropyridine-3-car-boxylic acids, esters, and amides having structural formula I … … wherein the dashed lines indicate the presence of only one carbon-carbon double bond either between carbon atoms numbers 3 and 4 or between carbon atoms numbers 4 and 5; R1 = hydrogen: C1-C6-alkyl, C2-C6 alkenyl, alkoxycarbonyl of from 2 to 5 C, C4-C8-cycloalkyl or phenyl-(C1-C6)-alkyl, wherein the phenyl ring may be substituted; R3 = -COOR, wherein R = hydrogen, C1-C6-alkyl, C2-C6-alkenyl; C3-C8-cycloalkyl or phenyl, which may be substituted; -CONR min R sec , wherein R min and R sec are independently hydrogen or cycloalkyl, benzyloxy or phenyl-(C1-C6)-alkyl, wherein the phenyl ring may be substituted, or R min and R sec when taken together with the nitrogen atom to which they are attached from a 5 to 7 membered heterocyclic ring which may contain another heteroatom selected from N,0 or S; R4 = C1-C6-alkyl, C2-C6-alkenyl,C3-C8-cycloalkyl, 2- or 3-thienyl, phenyl, which may be substituted or phenyl-(C1-C6)-alkyl, wherein the phenyl group may be substituted, and the pharmaceutically acceptable salts thereof, possessing muscarinic binding activity, having utility for the treatment of the symptoms of senile cognitive decline are disclosed. Pharmaceutical compositions and pharmaceuticals are also disclosed.
    • 5. 发明专利
    • AT54910T
    • 1990-08-15
    • AT87102216
    • 1987-02-17
    • WARNER LAMBERT CO
    • BUTLER DONALD EMOOS WALTER HDODD JOHN HTECLE HAILE
    • A61K31/445A61K31/4433A61K31/4465A61K31/451A61K31/455A61P25/28C07D211/78C07D333/00C07D401/06C07D409/04C07D413/06C07D413/12
    • 1,2,3,6-Tetrahydro- and 1,2,5,6-tetrahydropyridine-3-car-boxylic acids, esters, and amides having structural formula I … … wherein the dashed lines indicate the presence of only one carbon-carbon double bond either between carbon atoms numbers 3 and 4 or between carbon atoms numbers 4 and 5; R1 = hydrogen: C1-C6-alkyl, C2-C6 alkenyl, alkoxycarbonyl of from 2 to 5 C, C4-C8-cycloalkyl or phenyl-(C1-C6)-alkyl, wherein the phenyl ring may be substituted; R3 = -COOR, wherein R = hydrogen, C1-C6-alkyl, C2-C6-alkenyl; C3-C8-cycloalkyl or phenyl, which may be substituted; -CONR min R sec , wherein R min and R sec are independently hydrogen or cycloalkyl, benzyloxy or phenyl-(C1-C6)-alkyl, wherein the phenyl ring may be substituted, or R min and R sec when taken together with the nitrogen atom to which they are attached from a 5 to 7 membered heterocyclic ring which may contain another heteroatom selected from N,0 or S; R4 = C1-C6-alkyl, C2-C6-alkenyl,C3-C8-cycloalkyl, 2- or 3-thienyl, phenyl, which may be substituted or phenyl-(C1-C6)-alkyl, wherein the phenyl group may be substituted, and the pharmaceutically acceptable salts thereof, possessing muscarinic binding activity, having utility for the treatment of the symptoms of senile cognitive decline are disclosed. Pharmaceutical compositions and pharmaceuticals are also disclosed.
    • 7. 发明专利
    • DE3569926D1
    • 1989-06-08
    • DE3569926
    • 1985-07-15
    • WARNER LAMBERT CO
    • BUTLER DONALD ELEONARD JAMES D
    • A61K31/40C07D487/04
    • A compound having the following general formula I: wherein A is the radical -NR1R2 in which R1 and R2 are independently hydrogen, lower alkyl, or lower alkenyl; or wherein A is the radical -NHR3 in which R3 is phenyl, phenylmethyl, N,N-bis (1-methylethyl)- aminoethyl or 4-pyridyl; or wherein A is the radical -OR4 in which R4 is lower alkyl, phenyl (optionally substituted in the 2-, 3-, or 4-position with one or more of a chlorine, fluorine, lower alkoxy or phenylmethoxy), or phenylmethyl (optionally substituted in the 2-,3-, or 4- position with one or more of a chlorine, fluorine, lower alkoxy or phenyl (methoxy); and the pharmaceutically acceptable salts of those compounds of formula I having a basic nitrogen atom. The compounds are effective as cognition activators for treating senility or for reversing the effects of electroshock induced amnesia. A process for producing the compounds, a useful intermediate in their preparation and pharmaceutical compositions are also disclosed.