Abbott Laboratories Corporation

Chemocentryx, Inc.

Medarex Inc.

Other

Ligand Pharmaceuticals, Inc.

Jimmie L Moore

Dee W Brooks

Wei Yu Chen

Sreenivas Punna

Yibin Zeng

Andrew M K Pennell

Solomon Ungashe

Daniel J Dairaghi

Joseph F Dellaria, Jr

Zheng Wei

Trevor T Charvat

John Jessen Wright

Jeff Jin

Derek Hansen

Arindrajit Basak

Howard P Ng

Sanjeev Gangwar

Guoxian Wu

Irina Astafieva

Danny P C McGee

Qiang Wang

Antoni Krasinski

Oliver L Saunders

Zhi-Hong Li

James Patrick Edwards

Todd Kevin Jones

Philip R Kym

John K Pratt

Michael E Kort

James B Summers, Jr

Karen E Rodriques

Michael J Coghlan

Alan X Wang

Kevin J Sallin

William A Carroll

Steven Elmore

David J King

Andrew O Stewart

Irene I Drizin

Thomas Jay Lobl

James H Holms

Zhihong Li

Clint D Brooks

Richard A Craig

James F Kerwin

Valeri Martichonok

Sharon Elaine Boyd

Robert G Maki

Yiyuan Chen

Steven W Elmore

Oliver L Saunder

Teodozyji Kolasa

Danny P Mcgee

Geoffrey Thomas Yarranton

Andrew MK Pennell

Arindrajit Badak

Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.

Heteroaryl sulfonamides and CCR2/CCR9

Heteroaryl sulfonamides and CCR2

The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.

Peptidyl prodrugs and linkers and stabilizers useful therefor

Compounds having Formula Iare useful for partially or fully antagonizing, repressing, agonizing, or modulating the glucocorticoid receptor and treating immune, autoimmune and inflammatory diseases in a mammal. Also disclosed are pharmaceutical compositions comprising compounds of Formula I and methods of inhibiting immune or autoimmune diseases in a mammal.

Glucocorticoid-selective anti-inflammatory agents

Cyclopentanone dihydropyridine compounds useful as potassium channel openers

Glucocortiocoid-selective antinflammatory agents

The present invention provides a class of substituted indole and indene iminoxy derivatives of the formula ##STR1## which inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states.

Iminoxy derivatives of indole and indene compounds as inhibitors of

Arylamidoalkyl-N-hydroxyurea compounds having lipoxygenase inhibitory

Compounds of the structure ##STR1## where Ar is optionally substituted carbocyclic aryl, 5- or 6-membered heterocyclic aryl, 10-membered bicyclic heterocyclic aryl containing one or two nitrogen atoms, 9- or 10-membered heterocyclic containing one or two nitrogen atoms and optionally containing a further nitrogen or oxygen atom and one oxo or thioxo substituent, benzo[b]furyl, or benzo[b]thienyl, A.sub.1 is propynyl, methylene, or a direct link to X, X is oxy, thio, sulfonyl, or NR.sub.4, A.sub.2 is selected from ##STR2## where Y is hydrogen, halogen, or nitrile; Z is hydrogen, R.sub.1 is alkyl, and R.sub.2 is hydrogen or alkyl are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.

Ether-containing inhibitors of 5-lipoxygenase

Growing community of inventors

Gurnee, IL, United States of America

Jimmie L Moore