G.d. Searle & Company

Pharmacia Corporation

Stephen Hermann Docter

Stella S Yu

Thomas Dale Penning

Julie M Miyashiro

Stevan Wakefield Djuric

Ish K Khanna

James W Malecha

John Jeffrey Talley

Matthew James Graneto

Paul Waddell Collins

Stephen R Bertenshaw

Jeffery S Carter

Donald J Rogier, Jr

Roland S Rogers

Michael John Clare

Barbara B Chen

Richard A Haack

Mark Andrew Russell

Nizal S Chandrakumar

Alan Frank Gasiecki

Bipinchandra N Desai

Chi-Dean Liang

Richard M Weier

Joseph Gerace Rico

Francis J Koszyk

Peter Gerrard Ruminski

Helen Y Chen

Xiangdong Xu

Yi Yu

Stella Siu-tzyy Yu

Mark A, Russell

Stella Siu-Tzyy Yu

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 Ris selected from hydrido, alkyl, haloalkyl, alkoxycaronyl, cyano, cyanoalkyl, carboxyl, aminocaronyl, alkylaminocarbonyl, cycloalklaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, amioncarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein Ris selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein Ris selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein Ris 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 Rand Rare not both hydrido; further provided that Ris not carboxyl or methyl when Ris hydrido and when Ris phenyl; further provided that Ris not triazolyl when Ris methyl; further provided that Ris not arakenyl when Ris carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that Ris not phenyl when Ris methyl and Ris carboxyl; and further provided that Ris not unsubstituted thienyl when Ris trifluoromethyl; or a pharmaceutically-acceptable salt thereof.

Substituted pyrazolyl benzenesulfonamides for the treatment of inflammation

The present invention provides compounds of the formula Ar &mdash;Q&mdash;Ar &mdash;Y&mdash;R&mdash;Z and pharmaceutically acceptable salts thereof wherein Ar and Ar are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety which may be an acyclic, cyclic or bicyclic amine or an optionally substituted monocyclic or bicyclic nitrogen-containing heteroaromatic moiety; Q is a linking group capable of linking two aryl groups; R is an alkylene moiety; Y is a linking moiety capable of linking an aryl group to an alkylene moiety and wherein Z is bonded to R through a nitrogen atom. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of inflammatory diseases which are mediated by LTB production, such as psoriasis, ulcerative colitis, IBD and asthma.

LTA4 hydrolase inhibitor pharmaceutical compositions and methods of use

Substituted pyrazolyl benzenesulfonamides for the treatment of asthma

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: ##STR1## wherein R.sup.2 is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R.sup.3 is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R.sup.4 is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R.sup.4 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 R.sup.2 and R.sup.3 are not both hydrido; further provided that R.sup.2 is not carboxyl or methyl when R.sup.3 is hydrido and when R.sup.4 is phenyl; further provided that R.sup.4 is not triazolyl when R.sup.2 is methyl; further provided that R.sup.4 is not aralkenyl when R.sup.2 is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R.sup.4 is not phenyl when R.sup.2 is methyl and R.sup.3 is carboxyl; and further provided that R.sup.4 is not unsubstituted thienyl when R.sup.2 is trifluoromethyl; or a pharmaceutically-acceptable salt thereof.

Substituted pyrazolyl benzenesulfonamides for the treatment of

The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.

Cinnamic acid derivatives

The present invention provides compounds of the formula Ar.sup.1 --Q--Ar.sup.2 --Y--R--Z and pharmaceutically acceptable salts thereof wherein Ar.sup.1 and Ar.sup.2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety which may be an acyclic, cyclic or bicyclic amine or an optionally substituted monocyclic or bicyclic nitrogen-containing heteroaromatic moiety; Q is a linking group capable of linking two aryl groups; R is an alkylene moiety; Y is a linking moiety capable of linking an aryl group to an alkylene moiety and wherein Z is bonded to R through a nitrogen atom. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD and asthma.

LTA.sub.4 hydrolase inhibitors

LTA.sub.4 Hydrolase inhibitors

This invention relates to compounds of Formula I and the stereoisomers and pharmaceutically acceptable salts thereof ##STR1## wherein R is alkyl, alkenyl, alkynyl, or cycloalkylalkyl;

Leukotriene B.sub.4 antagonists

Growing community of inventors

Mt. Prospect, IL, United States of America

Stephen Hermann Docter