Therapeutic amides

Claim 1

An amide of formula I: wherein: E is nitrogen; R 2 and R 3 are independently selected from the group consisting of (1-3C)alkyl substituted by from 0 to 2 k+1 groups selected from fluoro and chloro wherein k is the number of carbon atoms in the said (1-3C)alkyl, provided that R 2 and R 3 are not both methyl; or together, with the carbon atom to which both R 2 and R 3 are attached, form a 3-5 membered cycloalkyl ring optionally substituted by from 0 to 2m-2 fluoro groups wherein m is the number of carbon atoms in said ring; X is ArY; Y is a linking group selected from carbonyl, sulfinyl, and sulfonyl; and Ar is phenyl substituted with 0-2 substituents selected from halo, hydroxy, cyano, (1-4C)alkyl, and (1-4C)alkoxy; provided that the 4-position of said phenyl may be substituted by fluoro only, and that the said phenyl may not be 3,5-disubstituted; and provided that Ar is not 3-chlorophenyl, 3-bromophenyl, 3-iodophenyl, or 3-(1-4C)alkylphenyl when Y is carbonyl; or a pharmaceutically acceptable in vivo hydrolyzable ester of said amide; or a pharmaceutically acceptable salt of said amide or said ester.

Claim 9

A method of treating urinary incontinence, comprising administering to a mammal in need of such treatment an effective amount of an amide of formula I: ##STR4## wherein: E is nitrogen; R 2 and R 3 are independently selected from the group consisting of (1-3C)alkyl substituted by from 0 to 2k+1 groups selected from fluoro and chloro wherein k is the number of carbon atoms in the said (1-3C)alkyl, provided that R 2 and R 3 are not both methyl; or together, with the carbon atom to which both R 2 and R 3 are attached, form a 3-5 membered cycloalkyl ring optionally substituted by from 0 to 2m-2 fluoro groups wherein m is the number of carbon atoms in said ring; X is ArY; Y is a linking group selected from carbonyl, sulfinyl, and sulfonyl; and Ar is phenyl substituted with 0-2 substituents selected from halo, hydroxy, cyano, (1-4C)alkyl, and (1-4C)alkoxy; provided that the 4-position of said phenyl may be substituted by fluoro only, and that the said phenyl may not be 3,5-disubstituted; and provided that Ar is not 3-chlorophenyl, 3-bromophenyl, 3-iodophenyl, or 3-(1-4C)alkylphenyl when Y is carbonyl; or a pharmaceutically acceptable in vivo hydrolyzable ester of said amide; or a pharmaceutically acceptable salt of said amide or said ester.

Claim 10

A method of treating urinary incontinence, comprising administering to a mammal in need of such treatment an effective amount of an amide of formula I: ##STR4## wherein: E is nitrogen; R 2 and R 3 are independently selected from the group consisting of (1-3C)alkyl substituted by from 0 to 2k+1 groups selected from fluoro and chloro wherein k is the number of carbon atoms in the said (1-3C)alkyl, provided that R 2 and R 3 are not both methyl; or together, with the carbon atom to which both R 2 and R 3 are attached, form a 3-5 membered cycloalkyl ring optionally substituted by from 0 to 2m-2 fluoro groups wherein m is the number of carbon atoms in said ring; X is ArY; Y is a linking group selected from carbonyl, sulfinyl, and sulfonyl; and Ar is phenyl substituted with 0-2 substituents selected from halo, hydroxy, cyano, (1-4C)alkyl, and (1-4C)alkoxy; provided that the 4-position of said phenyl may be substituted by fluoro only, and that the said phenyl may not be 3,5-disubstituted; and provided that Ar is not 3-chlorophenyl, 3-bromophenyl, 3-iodophenyl, or 3-(1-4C)alkylphenyl when Y is carbonyl; or a pharmaceutically acceptable in vivo hydrolyzable ester of said amide; or a pharmaceutically acceptable salt of said amide or said ester.