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    1,4-DI-SUSTITUTED PIPERIDINES AS MUSCARINIC ANTAGONISTS
    78.
    发明专利
    1,4-DI-SUSTITUTED PIPERIDINES AS MUSCARINIC ANTAGONISTS 未知

    公开(公告)号：CA2259655C

    公开(公告)日：2003-05-13

    申请号：CA2259655

    申请日：1997-07-08

    Applicant: SCHERING CORP

    Inventor： GREEN MICHAEL J ,  ASBEROM THEODROS ,  LOWE DEREK B

    IPC: A61K31/00 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/4468 ,  A61K31/4545 ,  A61K45/06 ,  A61P25/28 ,  C07D211/58 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07F7/10 ,  C07D401/12 ,  A61K31/47 ,  A61K31/495 ,  A61K31/535 ,  A61K31/695

    Abstract: 1,4-Di-substituted piperidine muscarinic antagonists of formula (I) or a pharmaceutically acceptable salt, ester, or solvate thereof, wherein X is a bond, -O-, -S-, -SO-, -SO2-, -CO-, -C(OR7)2-, -CH2-O-, -O-CH2-, -CH=CH-, -CH 2- , -CH(C1-C6 alkyl)-, -C(C1-C6 alkyl)2-, -CONR17-, -NR17CO-, -SO2NR17- or - NR17SO2-; R is C3-C6 cycloalkyl, (a), (b), (c), (d), (e), optionally substituted phenyl or optionally substituted pyridyl; R1 is H, -CN, -CF3, alkyl, cycloalkyl, cycloalkenyl, alkenyl, -COR15, -COO(alkyl, aryl, heteroaryl, alkylaryl or alkylheteroaryl), alkylaryl, alkylheteroaryl or - CON(R13)2; R2 is cycloalkyl, cycloalkenyl, t-butoxycarbonyl or optionally substituted 4-piperidinyl; R3 and R4 are H, halo, -CF3, alkyl, alkoxy or -OH ; R5 and R6 are H, alkyl, -CF3, alkoxy, -OH, alkylcarbonyl, alkoxycarbonyl, R13CONH-, R14OCONH-, R13NHCONH- or NH2CONR13-; R7 is H or alkyl, or the two R7 groups may form -(CH2)2-4; R13 is H, alkyl, cycloalkyl, -(alkyl)COOR15, aryl , heteroaryl, alkylaryl, alkylheteroaryl and adamantyl; R14 is H or alkyl; R15 is H, C1-C20 alkyl, C1-C6 cycloalkyl, aryl or heteroaryl; and R17 is H, C1-C 6 alkyl, aryl or heteroaryl; useful for treating cognitive disorders such as Alzheimer's disease are disclosed, as well as pharmaceutical compositions an d methods of preparation. Also disclosed are combinations of compounds of formula (I) capable of enhancing ACh release with ACh'ase inhibitors.

    79.
    发明专利
    未知

    公开(公告)号：PT912515E

    公开(公告)日：2003-03-31

    申请号：PT97932321

    申请日：1997-07-08

    Applicant: SCHERING CORP

    Inventor： ASBEROM THEODROS ,  LOWE DEREK B ,  GREEN MICHAEL J

    IPC: A61K31/00 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/4468 ,  A61K31/4545 ,  A61K45/06 ,  A61P25/28 ,  C07D211/58 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14

    Abstract: 1,4-Di-substituted piperidine muscarinic antagonists of formula (I) or a pharmaceutically acceptable salt, ester, or solvate thereof, wherein X is a bond, -O-, -S-, -SO-, -SO2-, -CO-, -C(OR )2-, -CH2-O-, -O-CH2-, -CH=CH-, -CH2-, -CH(C1-C6 alkyl)-, -C(C1-C6 alkyl)2-, -CONR -, -NR CO-, -SO2NR - or -NR SO2-; R is C3-C6 cycloalkyl, (a), (b), (c), (d), (e), optionally substituted phenyl or optionally substituted pyridyl; R is H, -CN, -CF3, alkyl, cycloalkyl, cycloalkenyl, alkenyl, -COR , -COO(alkyl, aryl, heteroaryl, alkylaryl or alkylheteroaryl), alkylaryl, alkylheteroaryl or -CON(R )2; R is cycloalkyl, cycloalkenyl, t-butoxycarbonyl or optionally substituted 4-piperidinyl; R and R are H, halo, -CF3, alkyl, alkoxy or -OH; R and R are H, alkyl, -CF3, alkoxy, -OH, alkylcarbonyl, alkoxycarbonyl, R CONH-, R OCONH-, R NHCONH- or NH2CONR -; R is H or alkyl, or the two R groups may form -(CH2)2-4; R is H, alkyl, cycloalkyl, -(alkyl)COOR , aryl, heteroaryl, alkylaryl, alkylheteroaryl and adamantyl; R is H or alkyl; R is H, C1-C20 alkyl, C1-C6 cycloalkyl, aryl or heteroaryl; and R is H, C1-C6 alkyl, aryl or heteroaryl; useful for treating cognitive disorders such as Alzheimer's disease are disclosed, as well as pharmaceutical compositions and methods of preparation. Also disclosed are combinations of compounds of formula (I) capable of enhancing ACh release with ACh'ase inhibitors.

    80.
    发明专利
    未知

    公开(公告)号：DK0912515T3

    公开(公告)日：2003-03-10

    申请号：DK97932321

    申请日：1997-07-08

    Applicant: SCHERING CORP

    Inventor： ASBEROM THEODROS ,  LOWE DEREK B ,  GREEN MICHAEL J

    IPC: A61K31/00 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/4468 ,  A61K31/4545 ,  A61K45/06 ,  A61P25/28 ,  C07D211/58 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14

    Abstract: 1,4-Di-substituted piperidine muscarinic antagonists of formula (I) or a pharmaceutically acceptable salt, ester, or solvate thereof, wherein X is a bond, -O-, -S-, -SO-, -SO2-, -CO-, -C(OR )2-, -CH2-O-, -O-CH2-, -CH=CH-, -CH2-, -CH(C1-C6 alkyl)-, -C(C1-C6 alkyl)2-, -CONR -, -NR CO-, -SO2NR - or -NR SO2-; R is C3-C6 cycloalkyl, (a), (b), (c), (d), (e), optionally substituted phenyl or optionally substituted pyridyl; R is H, -CN, -CF3, alkyl, cycloalkyl, cycloalkenyl, alkenyl, -COR , -COO(alkyl, aryl, heteroaryl, alkylaryl or alkylheteroaryl), alkylaryl, alkylheteroaryl or -CON(R )2; R is cycloalkyl, cycloalkenyl, t-butoxycarbonyl or optionally substituted 4-piperidinyl; R and R are H, halo, -CF3, alkyl, alkoxy or -OH; R and R are H, alkyl, -CF3, alkoxy, -OH, alkylcarbonyl, alkoxycarbonyl, R CONH-, R OCONH-, R NHCONH- or NH2CONR -; R is H or alkyl, or the two R groups may form -(CH2)2-4; R is H, alkyl, cycloalkyl, -(alkyl)COOR , aryl, heteroaryl, alkylaryl, alkylheteroaryl and adamantyl; R is H or alkyl; R is H, C1-C20 alkyl, C1-C6 cycloalkyl, aryl or heteroaryl; and R is H, C1-C6 alkyl, aryl or heteroaryl; useful for treating cognitive disorders such as Alzheimer's disease are disclosed, as well as pharmaceutical compositions and methods of preparation. Also disclosed are combinations of compounds of formula (I) capable of enhancing ACh release with ACh'ase inhibitors.

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