G.d. Searle & Company

Pharmacia Corporation

Monsanto Company

Other

Monsanto Company of St. Louis

Mosanto Company

Donald J Rogier, Jr

John Jeffrey Talley

Jeffery S Carter

Thomas Dale Penning

Matthew James Graneto

Stephen R Bertenshaw

Ish K Khanna

James W Malecha

Paul Waddell Collins

Roland S Rogers

Julie M Miyashiro

Daniel P Getman

John Nicholas Freskos

Ko-Chung Lin

Robert M Heintz

Stella S Yu

Gary A DeCrescenzo

Stephen Hermann Docter

Richard A Mueller

Michael L Vazquez

Michael John Clare

Kathryn L Reed

Deborah E Bertenshaw

David Louis Brown

Srinivasan Raj Nagarajan

Richard M Weier

Xiangdong Xu

Jinglin J Li

Balekudru Devadas

Suzanne S Metz

Cindy L Ludwig

Steven W Kramer

Mark G Obukowicz

Cathleen Elizabeth Hanau

Donald E Korte

Susan J Hartman

Stephen H Doctor

Prodrugs of COX-2 inhibitors are described as being useful in treating inflammation and inflammation-related disorders.

Process for preparing prodrugs of benzenesulfonamide-containing COX-2 inhibitors

N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Retroviral protease inhibitors

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

A class of dihydrobenzopyrans, dihydrobenzothiopyrans, tetrahydroquinolines, tetrahydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula (I) wherein X, A , A , A , A , R, R&Prime;, R and R are as described in the specification

Dihydrobenzopyrans, dihydrobenzothiopyrans, and tetrahydroquinolines for the treatment of COX-2 mediated disorders

Prodrugs of COX-2 inhibitors and methods of their preparation are described. The prodrugs of COX-2 inhibitors are described as being useful in treating inflammation and inflammation-related disorders.

Process for preparing prodrugs of benzenesulfonamide-containing cox-2 inhibitors

Substituted benzopyran derivatives for the treatment

Process for preparing a substituted pyrazolyl benzenesulfonamide for the treatment of inflammation

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

1,3,5 trisubstituted pyrazole compounds for treatment of inflammation

N-heterocyclic moiety containing hydroxyethylamine compounds of the formula: ##STR1## such as 3-isoquinolinecarboxamide,N-(,1-dimethylethyl)decahydro-2-�2-hydroxy-3-��2 -methyl-3-(methysulfonyl)-1-oxopropyl!amino!-4-phenylbutyl!-, �3S-�2�2S*,3R*(R*)!,3.alpha.,4a.beta., 8 a.beta.!!- are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Growing community of inventors

St. Louis, MO, United States of America

Donald J Rogier, Jr