Genentech, Inc.

Curis, Inc.

University of California

F. Hoffmann-la Roche Ag

Mark S Stanley

Mark E Reynolds

Daniel P Sutherlin

Thomas E Rawson

Liang Bao

Georgette M Castanedo

Shumei Wang

Scott J Savage

Kimberly Malesky

Michael S Dina

Rebecca L Lalonde

Robert S McDowell

Dean R Artis

John P Burnier

Ross G Clark

Kathleen Ann Elias

David Y Jackson

Karen Williams

Todd C Somers

Michael F T Koehler

John Gary Montana

Thomas Gadek

Stephen Colin Price

David A Oare

Hazel Joan Dyke

Simon Charles Goodacre

Daniel J Burdick

Janet Gunzner

Janet L Gunzner-Toste

James C Marsters

Jun Liang

Steven R Magnuson

Wendy Lee

Vickie Hsiao-Wei Tsui

Birong Zhang

Kirk D Robarge

Aihe Zhou

Carl W Cotman

Yingjie Lai

A Richard Chamberlin

Pascal Savy

Richard J Bridges

Janet L Gunzner

Pascal Pierre Savy

Pierre Pascal Savy

The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R, R, R, R, m and n are as described herein.

Pyridyl inhibitors of hedgehog signalling

The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, B, D, R, R, Rand Rare defined herein, a pharmaceutical composition that includes a compound of Formula I and methods of use thereof. 

Janus kinase inhibitor compounds and methods

The invention relates to azabenzothiophenyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azabenzothiophenyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions. 

Aza-benzothiophenyl compounds and methods of use

The invention relates to azaindolyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azaindolyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

Aza-indolyl compounds and methods of use

Provided are compounds of formula (I) wherein A, Q, W, X, Y, Z, Rto R, m and n are as defined herein. Compounds of the invention bind to &#x3b1;integrin receptors and thereby inhibit binding of ligands for &#x3b1;integrins which is useful for prophylactic and/or therapeutic treatment of diseases and conditions associated with &#x3b1;integrins or their ligands.

Integrin receptor inhibitors

The present invention comprises growth hormone releasing peptides/peptidomimetics (GHRP) capable of causing release of growth hormone from the pituitary. Compositions containing the GHRP's of this invention are used to promote growth in mammals either alone or in combination with other growth promoting compounds, especially IGF-1. In a method of this invention GHRP's in combination with IGF-1 are used to treat Type II diabetes. An exemplary compound of this invention is provided below

Low molecular weight peptidomimetic growth hormone secretagogues

Provided are compounds of formula (I)wherein A, Q, W, X, Y, Z, Rto R, m and n are as defined herein. Compounds of the invention bind to &#x3b1;integrin receptors and thereby inhibit binding of ligands for &#x3b1;integrins which is useful for prophylactic and/or therapeutic treatment of diseases and conditions associated with &#x3b1;integrins or their ligands.

The invention relates to novel compounds having formula (I)wherein Cy, X, Y, L and Rare as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation and autoimmune diseases.

LFA-1 antagonist compounds

The present invention comprises growth hormone releasing peptides/peptidomimetics (GHRP) capable of causing release of growth hormone from the pituitary. Compositions containing the GHRP's of this invention are used to promote growth in mammals either alone or in combination with other growth promoting compounds, especially IGF-1. In a method of this invention GHRP's in combination with IGF-1 are used to treat Type II diabetes. An exemplary compound of this invention is provided below. ##STR1##

A method of inhibiting the transport of a neurotransmitter away from the synapse comprising contacting a neurotransmitter transporter with a compound having the structure ##STR1## wherein ##STR2## or CONHR.sup.3 in any combination and and wherein R.sup.2 =OR.sup.3, NR.sup.3.sub.2, alkyl, or substituted alkyl and R.sup.3 =alkyl or substituted alkyl.

Method of inhibiting the transport of L-glutamate to treat CNS disorders

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Pacifica, CA, United States of America

Mark S Stanley