Certain N(4-benzoyl-2-phenyl)-3- trifluoro-2-hydroxy-propanamide derivatives
First Claim
Patent Images
1. A compound formula Ib:
- whereinAr is phenyl, optionally substituted with a substituent selected from (1-4C)alkyl;
Y is carbonyl;
A-B is --NHC(═
O)--;
R9 is selected from the group consisting of (1-4C)haloalkyl, (1-4C)alkoxy, (2-4C)alkenyloxy, cyano, nitro, halo, trifluoromethyl, trifluoromethylthio, trifluoromethoxy, and hydroxy;
R10 is hydrogen;
R11 is selected from hydrogen, halo, methyl, hydroxy, methoxy, and cyano; and
R2 and R3 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 R2 and R3 are not both methyl;
orR2 and R3, 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;
or a pharmaceutically acceptable salt of said compound;
provided said compound is not N-(4-Benzoyl-2,6-dimethylphenyl)-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide.
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Abstract
Compounds of formula I: ##STR1## wherein, ring C, A-B, R1, n, R2, and R3 have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinary incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
9 Citations
8 Claims
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1. A compound formula Ib:
wherein Ar is phenyl, optionally substituted with a substituent selected from (1-4C)alkyl; Y is carbonyl; A-B is --NHC(═
O)--;R9 is selected from the group consisting of (1-4C)haloalkyl, (1-4C)alkoxy, (2-4C)alkenyloxy, cyano, nitro, halo, trifluoromethyl, trifluoromethylthio, trifluoromethoxy, and hydroxy; R10 is hydrogen; R11 is selected from hydrogen, halo, methyl, hydroxy, methoxy, and cyano; and R2 and R3 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 R2 and R3 are not both methyl;
orR2 and R3, 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;
or a pharmaceutically acceptable salt of said compound;
provided said compound is not N-(4-Benzoyl-2,6-dimethylphenyl)-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide.- View Dependent Claims (2, 3, 4, 5)
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6. A pharmaceutical composition comprising a compound of formula Ib:
- ##STR3## wherein Ar is phenyl, optionally substituted with a substituent selected from (1-4C)alkyl;
Y is carbonyl; A-B is --NHC(═
O)--;R9 is selected from the group consisting of (1-4C)haloalkyl, (1-4C)alkoxy, (2-4C)alkenyloxy, cyano, nitro, halo, trifluoromethyl, trifluoromethylthio, trifluoromethoxy, and hydroxy; R10 is hydrogen; R11 is selected from hydrogen, halo, methyl, hydroxy, methoxy, and cyano; and R2 and R3 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 R2 and R3 are not both methyl;
orR2 and R3, 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; or a pharmaceutically acceptable salt of said compound; and
a pharmaceutically acceptable diluent or carrier.
- ##STR3## wherein Ar is phenyl, optionally substituted with a substituent selected from (1-4C)alkyl;
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7. 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 Ib:
- ##STR4## wherein Ar is phenyl, optionally substituted with a substituent selected from (1-4C)alkyl;
Y is carbonyl; A-B is --NHC(═
O)--;R9 is selected from the group consisting of (1-4C)haloalkyl, (1-4C)alkoxy, (2-4C)alkenyloxy, cyano, nitro, halo, trifluoromethyl, trifluoromethylthio, trifluoromethoxy, and hydroxy; R10 is hydrogen; R11 is selected from hydrogen, halo, methyl, hydroxy, methoxy, and cyano; and R2 and R3 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 R2 and R3 are not both methyl;
orR2 and R3, 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; or a pharmaceutically acceptable salt of said compound.
- ##STR4## wherein Ar is phenyl, optionally substituted with a substituent selected from (1-4C)alkyl;
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8. 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 Ib:
- ##STR5## wherein Ar is phenyl, optionally substituted with a substituent selected from (1-4C)alkyl;
Y is carbonyl; A-B is --NHC(═
O)--;R9 is selected from the group consisting of (1-4C)haloalkyl, (1-4C)alkoxy, (2-4C)alkenyloxy, cyano, nitro, halo, trifluoromethyl, trifluoromethylthio, trifluoromethoxy, and hydroxy; R10 is hydrogen; R11 is selected from hydrogen, halo, methyl, hydroxy, methoxy, and cyano; and R2 and R3 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 R2 and R3 are not both methyl;
orR2 and R3, 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; or a pharmaceutically acceptable salt of said compound.
- ##STR5## wherein Ar is phenyl, optionally substituted with a substituent selected from (1-4C)alkyl;
Specification