Substituted pyrazolyl benzenesulfonamides for the treatment of inflammation - Patent US6156781(A)

Filed: Nov 24, 1999

Published: Dec 05, 2000

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 II: wherein R2 is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R3 is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R4 is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R4 is optionally substituted at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxyl, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided R2 and R3 are not both hydrido; further provided that R2 is not carboxyl or methyl when R3 is hydrido and when R4 is phenyl; further provided that R4 is not triazolyl when R2 is methyl; further provided that R4 is not aralkenyl when R2 is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R4 is not phenyl when R2 is methyl and R3 is carboxyl; and further provided that R4 is not unsubstituted thienyl when R2 is trifluoromethyl; or a pharmaceutically-acceptable salt thereof.

Applicants

SEARLE CO

Inventors

KHANNA ISH K
DOCTER STEPHEN H
BERTENSHAW STEPHEN R
TALLEY JOHN J
ROGERS ROLAND S
YU STELLA S
ROGIER JR DONALD J
COLLINS PAUL W
CARTER JEFFERY S
PENNING THOMAS D
MALECHA JAMES W
MIYASHIRO JULIE M
GRANETO MATTHEW J

Application Number

449076

Priority Claims

US16059493

Family Members

US6156781(A) - Substituted pyrazolyl benzenesulfonamides for the treatment of inflammation

Classification Codes

A61P17/00, C07D409/00, C07D495/00, C07D231/00, C07D403/04, A61P17/06, C07D405/04, C07D231/54, C07D401/00, C07D231/16, C07D231/12, C07D231/14, C07D495/04, C07D409/04, C07D401/04, C07D405/00, C07D403/00