Anticholinergic compounds, composititons and methods of treatment
First Claim
Patent Images
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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Abstract
Compounds of the formula ##STR1## wherein the variables are defined in the specification. The compounds and their salts are soft anticholinergic/antisecretory agents especially useful as mydriatics and as antiperspirants.
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Citations
45 Claims
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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. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45)
- R1 is C1 -C8 straight or branched alkyl;
Specification