Chiron Corporation

Novartis Vaccines & Diagnostics, Gmbh

Eric J Martin

Ronald N Zuckermann

Hong Yang

Weibo Wang

Mark Knapp

Paul Andrew Barsanti

Vincent P Le

Paul A Renhowe

Walter H Moos

Savithri Ramurthy

Sabina Pecchi

Sharadha Subramanian

Simon C Ng

David Duhl

Kenneth Walter Bair

Tinya Abrams

Rama Jain

Annette Olga Walter

Ryan N Constantine

Reyna J Simon

Robert L Warne

Kris Mendenhall

Elisa Jazan

Nathan Brammeier

Elizabeth J Mieuli

Kelly Wayman

Anu Sharma

Rustum Boyce

Megan C Phillips

Kay Huh

David C Spellmeyer

Gregory Stauber

Susan Barnett

Liana Marie Lagniton

Kerry L Spear

Karin Hartog

Yia Xia

Dane A Goff

Steven Rosenberg

Rustum S Boyce

Kevin R Shoemaker

Steve Rosenberg

Dirksen Bussiere

Liana Marie Lagnition

Xia Yia

The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds. The compounds of the invention have the following general formula: 

Substituted imidazole derivates

Substituted imidazole derivatives

The present invention relates to new substituted imidazole compounds have the following Formula (I) and to the pharmaceutically acceptable salts, esters, or prodrugs thereof, to compositions of the compounds together with pharmaceutically acceptable carriers, and to uses of the compounds: 

Cyclized derivatives as Eg-5 inhibitors

This invention provides methods of identifying an Eg5 binding ligand. The ligand is identified by using the atomic coordinates of an Eg5 crystal to generate a three dimensional structure. The three dimensional structure is used in molecular modeling techniques and docking experiments to identify ligands that bind to the binding pocket of Eg5. A novel binding pocket is identified. The invention also provides a crystallized Eg5 and ligand complex.

Eg5 co-crystals

Polynucleotide encoding modified HIV Env polypeptides are disclosed. The Env polypeptides are modified so as to expose at least part of the CD4 binding region. Methods of diagnosis, treatment and prevention using the polynucleotides and polypeptides are also provided.

Modified HIV Env polypeptides

Polynucleotide encoding modified HIV Env polypeptides are disclosed. The Env polypeptides are modified in the region of amino acids 420-436 so as to expose at least part of the CD4 binding region. Methods of diagnosis, treatment and prevention using the polynucleotides and polypeptides are also provided.

Urokinase receptor ligands

Compounds of the invention inhibit urokinase plasminogen activator: ##STR1## where R.sub.1 is lower alkyl, lower alkenyl, lower alkynyl, aryl, aralkyl, aryl-alkenyl, aryl-alkynyl, aryl-cycloalkyl, unsubstituted or substituted with 1-3 halo, OH, NH.sub.2, lower alkyl, halo-lower alkyl, lower alkoxy, lower alkylamino, lower alkylthio, CN or NO.sub.2 ;

Compounds of Formula 1 bind opioid receptors: which binds to the opioid receptor: ##STR1##

Opiate receptor ligands

Compounds of Formula 1 bind opioid receptors: ##STR1## wherein X and Y are each independently ##STR2##

Compounds of Formula 1 bind to the opioid receptors: ##STR1## wherein R.sub.1 is a group of the formula ##STR2## where W is --(CH.sub.2).sub.a -- (where a is 0, 1, or 2), --O--, --NH--, --S--, --SO--, or --SO.sub.2 --, and Ar is phenyl, phenyl-alkyl, phenyl substituted with 1-3 halo, nitro, lower alkyl, hydroxy, amino, alkylamino, dialkylamino, and/or hydroxy-lower alkyl groups, and n is 0, 1, 2, 3, or 4;

Compounds of the formula: ##STR1## are useful for treating conditions modulated by .alpha..sub.1 -adrenergic receptors.

Peptoid .alpha.-1 adrenergic receptor ligands

Peptoid alpha-1 adrenergic receptor ligands

Growing community of inventors

El Cerrito, CA, United States of America

Eric J Martin