Chiron Corporation

Novartis Ag

Novartis Vaccines & Diagnostics, Gmbh

Arris Pharmaceutical Corporation

Robert L Warne

Simon C Ng

Kevin R Shoemaker

Mark J Selby

Ronald N Zuckermann

David Y Chien

Eric J Martin

Reyna J Simon

Weibo Wang

Savithri Ramurthy

Keith Bruce Pfister

Allan S Wagman

Sharadha Subramanian

Yasheen Zhou

Xiaodong Lin

Rama Jain

Alice C Rico

James M Clark

Payman Amiri

Mina E Aikawa

Jeffrey H Dove

Johanna M Jansen

Wei Shu

Xiaojong M Wang

Jeremy M Murray

Stephen E Basham

The invention provides quinazoline compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions. 

Quinazolines for PDK1 inhibition

A polypeptide containing an anchor region, a protease recognition site, and a detectable signal region can be produced recombinantly and directly attached to a solid support. The polypeptide is useful for screening protease regulators, especially protease inhibitors.

Protease regulator screening assay

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

Opiate receptor ligands

The instant invention is directed to recombinant production of functionally active chymase. 'Functionally active' as used herein refers to the ability to exhibit one or more functional activities of a full-length wild-type chymase protein. In a preferred aspect, a proteolytically inactive chymase fusion protein comprising a functionally active portion of a non-chymase protein joined to the amino-terminus of the chymase protein is produced, which, upon cleavage away of the non-chymase fusion protein portion, becomes proteolytically active. A refolding procedure for increasing yields of proteolytically active recombinant chymase is provided. The invention is further directed to use of the recombinant chymase thus produced for preparing chymase-specific antibodies.

Recombinant production of chymase

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;

Growing community of inventors

San Leandro, CA, United States of America

Robert L Warne