|Title:||Substituted pyrazolyl benzenesulfonamide compounds for the treatment of inflammation|
|Abstract:||A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: ##STR1## or a pharmaceutically-acceptable salt thereof.|
|Inventor(s):||Talley; John J. (St. Louis, MO), Penning; Thomas D. (Elmhurst, IL), Collins; Paul W. (Deerfield, IL), Rogier, Jr.; Donald J. (St. Louis, MO), Malecha; James W. (Libertyville, IL), Miyashiro; Julie M. (Chicago, IL), Bertenshaw; Stephen R. (Brentwood, MO), Khanna; Ish K. (Vernon Hills, IL), Graneto; Matthew J. (St. Louis, MO), Rogers; Roland S. (Richmond Heights, MO), Carter; Jeffery S. (Chesterfield, MO)|
|Assignee:||G. D. Searle & Co. (Skokie, IL)|
|Filing Date:||Jun 01, 1995|
|Claims:||1. A compound of Formula I ##STR44## wherein R.sup.1 is selected from halo, alkyl, alkoxy, hydroxyl and haloalkyl; |
wherein R.sup.2 is selected from hydrido, halo, haloalkyl, cyano, nitro, formyl, carboxyl, alkoxycarbonyl, carboxyalkyl, alkoxycarbonylalkyl, amidino, cyanoamidino, amido, alkoxy, amidoalkyl, N-monoalkylamido, N-monoarylamido, N,N-dialkylamido, N-alkyl-N-arylamido, alkylcarbonyl, alkylcarbonylalkyl, hydroxyalkyl, alkylthio, alkylsulfinyl, alkylsulfonyl, N-alkylsulfamyl, N-arylsulfamyl, arylsulfonyl, N,N-dialkylsulfamyl, N-alkyl-N-arylsulfamyl and heterocyclic;
wherein R.sup.3 is hydrido; and
wherein R.sup.4 is selected from aryl substituted at a substitutable position with sulfamyl;
or a pharmaceutically-acceptable salt thereof.
2. Compound of claim 1 wherein R.sup.1 is selected from halo, alkyl, alkoxy, hydroxyl and haloalkyl; wherein R.sup.2 is selected from haloalkyl; wherein R.sup.3 is hydrido; and wherein R.sup.4 is phenyl substituted at a substitutable position with sulfamyl; or a pharmaceutically-acceptable salt thereof.
3. Compound of claim 2 wherein R.sup.1 is selected from fluoro, chloro, bromo, fluoromethyl, difluoromethyl, trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, pentafluoroethyl, heptafluoropropyl, difluorochloromethyl, dichlorofluoromethyl, difluoroethyl, difluoropropyl, dichlorethyl, dichloropropyl, methyl, ethyl, propyl, hydroxyl, methoxy, ethoxy, propoxy and n-butoxy; wherein R.sup.2 is selected from fluoromethyl, difluoromethyl, trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, pentafluoroethyl, heptafluoroproply, difluoroethyl, difluorochloromethyl, dichlorofluoromethyl, difluoropropyl, dichloroethyl and dichloropropyl; wherein R.sup.3 is hydrido; and wherein R.sup.4 is phenyl substituted at a substitutable position with sulfamyl; or a pharamaceutically-acceptable salt thereof.
4. Compound of claim 3 which is 4-[1-(4-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]benzenesulfonami de, or a pharmaceutically-acceptable salt thereof.
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