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Anticholinergic compounds, composititons and methods of treatment

  • US 5,223,528 A
  • Filed: 07/27/1990
  • Issued: 06/29/1993
  • Est. Priority Date: 03/17/1986
  • Status: Expired due to Term
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First Claim
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1. A compound of the formula ##STR264## wherein:

  • R1 is C1 -C8 straight or branched alkyl;

    C2 -C8 straight or branched alkenyl;

    (C3 -C8 cycloalkyl)-Cp H2p - wherein p is an integer from 0 to 4, and wherein the 3- to 8- membered ring portion may optionally bear 1 to 4 C1 -C4 straight or branched alkyl substituents;

    (C3 -C8 cycloalkenyl)-Cp H2p - wherein p is an integer from 0 to 4 and wherein the 3- to 8- membered ring portion may optionally bear 1 to 4 C1 -C4 straight or branched alkyl substituents;

    C6 H5 -Cq H2q - wherein q is an integer from 1 to 4;

    or (C6 -C18 polycarbocyclic)-Cp H2p - wherein p is an integer from 0 to 4, the 6- to 18-membered ring portion consisting of 2 to 4 rings which may be bridged or fused, which may be saturated or unsaturated and which may optionally bear one or more C1 -C8 straight or branched alkyl substituents, the total carbon atom content of all such optional alkyl substituents being from 1 to 10;

    R2 is phenyl optionally bearing 1 to 3 C1 -C4 straight or branched alkyl substituents;

    C3 -C8 branched alkyl;

    C3 -C8 branched alkenyl;

    (C3 -C8 cycloalkyl)-Cp H2p - wherein p is an integer from 0 to 4, and wherein the 3- to 8- membered ring portion may optionally bear 1 to 4 C1 -C4 straight or branched alkyl substituents;

    (C3 -C8 cycloalkenyl)-Cp H2p - wherein p is an integer from 0 to 4 and wherein the 3- to 8-membered ring portion may optionally bear 1 to 4 C1 -C4 straight or branched alkyl substituents;

    C6 H5 -Cq H2q - wherein q is an integer from 1 to 4;

    or (C6 -C18 polycarbocyclic)-Cp H2p - wherein p is an integer from 0 to 4, the 6- to 18-membered ring portion consisting of 2 to 4 rings which may be bridged or fused, which may be saturated or unsaturated and which may optionally bear one or more C1 -C8 straight or branched alkyl substituents, the total carbon atom content of all such optional alkyl substituents being from 1 to 10;

    R3 is H, phenyl optionally bearing 1 to 3 C1 -C4 straight or branched alkyl substituents, C1 -C4 straight or branched. alkyl or (C3 -C8 cycloalkyl)-Cp H2p - wherein p is an integer from 0 to 4 and wherein the 3- to 8-measured ring portion may optionally bear 1 to 4 C1 -C4 straight or branched alkyl substituents;

    n is an integer from 0 to 4;

    ##STR265## wherein R8 is H or C1 -C5 straight or branched alkyl, ##STR266## wherein each of R9 and R10, which may be the same or different, is H or C1 -C5 straight or branched alkyl;

    --S(CH2)x -- wherein x is 0 or 1;

    --O(CH2)x -- wherein x is 0 or 1;

    or ##STR267## wherein x is 0 or 1 and R11 is H or C1 -C5 straight or branched alkyl;

    m is an integer from 0 to 4; and

    R5 is C1 -C5 straight or branched alkyl;

    or a pharmaceutically acceptable acid addition salt of a compound of formula (I) with an acid of the formula HY wherein Y is a pharmaceutically acceptable anion;

    or a pharmaceutically acceptable quaternary ammonium salt of a compound of formula (I) with a compound of the formula R12 Y wherein Y is defined as above and R12 is C1 -C4 straight or branched alkyl or benzyl.

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