Aminosulfonylphenyl compounds for treating urinary incontinence

A pharmaceutical composition comprising a compound of formula I:

• ##STR3## wherein either R.sup.1 and R.sup.2 are each selected independently from hydrogen, (1-3C)alkyl and phenyl which is unsubstituted or substituted by one or two substituents selected independently from (1-4C)alkyl, (1-4C)alkoxy, (2-4C)alkenyloxy, hydroxy, halo and cyano,
• A-B is selected from NHCO, OCH.sub.2, SCH.sub.2, NHCH.sub.2, trans-vinylene, and ethynylene;
• R.sup.3 and R.sup.4 are independently (1-3C)alkyl substituted by from 0 to 2k+1 atoms selected from fluoro and chloro wherein k is the number of carbon atoms in the said (1-3C)alkyl, provided that R.sup.3 and R.sup.4 are not both methyl;
• or
• R.sup.3 and R.sup.4, together with the carbon atom to which they are attached, form a 3-5 membered cycloalkyl ring optionally substituted by from 0 to 2m-2 fluorine atoms wherein m is the number of carbon atoms in said ring;
• and
• R.sup.5 is hydrogen, (1-4C)alkyl, (1-4C)haloalkyl, (1-4C)alkoxy, (1-4)haloalkoxy, cyano, nitro, (2-4C)alkenyloxy or trifluoromethylthio;
• or a pharmaceutically acceptable in vivo hydrolyzable ester of said compound of formula I;
• or a pharmaceutically acceptable salt of said compound or said ester;
• and a pharmaceutically acceptable diluent or carrier;
• provided the compound is not 3-hydroxy-3-methyl-1-(4-morpholinosulfonylphenyl)-4,4,4-trifluorobut-1-yne .

A method for the treatment of urinary incontinence, comprising administering to a mammal (including man) in need of such treatment an effective amount of a compound of formula I:

• ##STR4## wherein, either R.sup.1 and R.sup.2 are each selected independently from hydrogen, (1-3C)alkyl and phenyl which is unsubstituted or substituted by one or two substituents selected independently from (1-4C)alkyl, (1-4C)alkoxy, (2-4C)alkenyloxy, hydroxy, halo and cyano,
• A-B is selected from NHCO, OCH.sub.2, SCH.sub.2, NHCH.sub.2, trans-vinylene, and ethynylene;
• R.sup.3 and R.sup.4 are independently (1-3C)alkyl substituted by from 0 to 2k+1 atoms selected from fluoro and chloro wherein k is the number of carbon atoms in the said (1-3C)alkyl, provided that R.sup.3 and R.sup.4 are not both methyl;
• or
• R.sup.3 and R.sup.4, together with the carbon atom to which they are attached, form a 3-5 membered cycloalkyl ring optionally substituted by from 0 to 2m-2 fluorine atoms wherein m is the number of carbon atoms in said ring;
• and
• R.sup.5 is hydrogen, (1-4C)alkyl, (1-4C)haloalkyl, (1-4C)alkoxy, (1-4)haloalkoxy, cyano, nitro, (2-4C)alkenyloxy or trifluoromethylthio;
• or a pharmaceutically acceptable in vivo hydrolyzable ester of said compound of formula I;
• or a pharmaceutically acceptable salt of said compound or said ester;
• provided the compound is not 3-hydroxy-3-methyl-1(4-morpholinosulfonylphenyl)-4,4,4-trifluorobut-1-yne.

A method for relaxing bladder smooth muscle, comprising administering to a mammal (including man) in need of such treatment an effective amount of a compound of formula I:

• ##STR5## wherein, either R.sup.1 and R.sup.2 are each selected independently from hydrogen, (1-3C)alkyl and phenyl which is unsubstituted or substituted by one or two substituents selected independently from (1-4C)alkyl, (1-4C)alkoxy, (2-4C)alkenyloxy, hydroxy, halo and cyano,
• A-B is selected from NHCO, OCH.sub.2, SCH.sub.2, NHCH.sub.2, trans-vinylene, and ethynylene;
• R.sup.3 and R.sup.4 are independently (1-3C)alkyl substituted by from 0 to 2k+1 atoms selected from fluoro and chloro wherein k is the number of carbon atoms in the said (1-3C)alkyl, provided that R.sup.3 and R.sup.4 are not both methyl;
• or
• R.sup.3 and R.sup.4, together with the carbon atom to which they are attached, form a 3-5 membered cycloalkyl ring optionally substituted by from 0 to 2m-2 fluorine atoms wherein m is the number of carbon atoms in said ring;
• and
• R.sup.5 is hydrogen, (1-4C)alkyl, (1-4C)haloalkyl, (1-4C)alkoxy, (1-4)haloalkoxy, cyano, nitro, (2-4C)alkenyloxy or trifluoromethylthio;
• or a pharmaceutically acceptable in vivo hydrolyzable ester of said compound of formula I;
• or a pharmaceutically acceptable salt of said compound or said ester;
• provided the compound is not 3-hydroxy-3-methyl-1(4-morpholinosulfonylphenyl)-4,4,4-trifluorobut-1-yne.