G.d. Searle & Company

Pharmacia Corporation

Other

Bristol-myers Squibb Compnay

G.d. Searle LLC

Pharmacia Corporation (of Pfizer, Inc.)

Bristol-meyers Squibb

Stephen R Bertenshaw

John Jeffrey Talley

Matthew James Graneto

Jeffery S Carter

Thomas Dale Penning

Paul Waddell Collins

James W Malecha

Roland S Rogers

Ish K Khanna

Donald J Rogier, Jr

Julie M Miyashiro

Donald J Rogier

David Louis Brown

Srinivasan Raj Nagarajan

Balekudru Devadas

Suzanne S Metz

Stella S Yu

Cindy L Ludwig

Mark G Obukowicz

Cathleen Elizabeth Hanau

Susan J Hartmann

Stephen Hermann Docter

Donald E Korte

Richard M Weier

David B Reitz

Xiangdong Xu

Jinglin J Li

Katherine S Takaki

Graham Johnson

Len F Lee

Li-Qiang Sun

Guanglin Luo

Gene Michael Dubowchik

Jie Chen

Jonathan L Ditta

Derek John Denhart

James R Epperson

Li-Quang Sun

Susan J Hartman

Stephen H Doctor

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: or a pharmaceutically-acceptable salt thereof.A method of treating inflammation or an inflammation-associated disorder in a subject by administering a therapeutically-effective dose of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide, or a pharmaceutically-acceptable salt thereof, to the subject.

4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-YL]benzenesulfonamide for the treatment of inflammation or an inflammation-associated disorder

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

A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, 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&#x2033;, Rand Rare as described in the specification.

Substituted benzopyran derivatives for the treatment of inflammation

A class of benzopyran, derivatives 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&#x2033;, Rand Rare as described in the specification.

A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I:wherein Y is selected from O, S and NR; wherein Ris selected from hydrido and lower alkyl; wherein X is one or two substituent selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein Rand Rare independently aryl or heteroaryl; and wherein Rand Rare optionally substituted at a substitutable position with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.

3,4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents

Substituted furans and furanones for the treatment of inflammation

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 invention encompasses a series of tetrahydroisoquinolines of formula I which are antagonists of the human melatonin MTreceptor and are useful as chronobiotic and sleep agents.

Tetrahydroisoquinoline derivatives as melatonin MT2 antagonists

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

Novel benzoxazole derivatives which have a binding affinity for the human melatonin receptor and, therefore, are useful as melatonergic agents.

Benzoxazole derivatives as novel melatonergic agents

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

3,4-diaryl thiopenes and analogs thereof having use as antiinflammatory agents

Novel benzofuran and dihydrobenzofuran derivatives which have a binding affinity for the human melatonin receptor and, therefore, are useful as melatonergic agents.

Arylalkylbenzofuran derivatives as melatonergic agents

Growing community of inventors

Brentwood, MO, United States of America

Stephen R Bertenshaw