Genentech, Inc.

University of Texas System

Hoffman-laroche, Inc. (us Only)

F. Hoffman-laroche, Ag (ex-us)

F. Hoffmann-la Roche Ag

Thomas E Rawson

Mark S Stanley

Robert S McDowell

Daniel P Sutherlin

Dean R Artis

Mark E Reynolds

Aihe Zhou

Todd C Somers

Richard Pastor

Bing-Yan Zhu

John P Burnier

Ross G Clark

Kathleen Ann Elias

David Y Jackson

Ignacio Aliagas-Martin

Joseph P Lyssikatos

John A Flygare

Alan G Olivero

Steven R Magnuson

Joseph L Goldstein

Michael S Brown

David A Oare

Yan Zhu

Richard A Goldsmith

Kirk D Robarge

Emily J Hanan

Paul Gibbons

Craig W Crowley

Michael S Dina

James C Marsters

Guy L James

Regina A Munroe

Kenneth J Weese

Jun Liang

Brian Salvatore Safina

Lewis J Gazzard

Christopher Hurley

Michael Siu

Birong Zhang

Mark Edward Zak

Matthias Rueth

Rohan V Mendonca

Jun M Li

Jennafer Dotson

Wendy Liu

Jason S Halladay

Michael Prime

Frederick Brookfield

Jeffrey Blaney

Paul A Gibbons

A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R, Rand Rare defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed. 

Pyrazolopyrimidine JAK inhibitor compounds and methods

The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R, R, Rand Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient. 

The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I wherein A, X, Y, Z, Ra, Rb, Rc, R, R, Rand m are defined herein.

Pentacyclic kinase inhibitors

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

Compounds having the general formula I are useful for inhibiting serine protease enzymes, such as Tissue Factor VIIa, factor Xa, thrombin and kallikrein and have improved permeability properties. These compounds may be used in methods of preventing and/or treating clotting disorders 

Acylsulfamide inhibitors of factor VIIa

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.

Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.

Serine protease inhibitors

Compounds having the structure shown below wherein A, B, N , N , X, Y, Q, R , R and R are as defined herein are useful to inhibit serine protease enzymes, such as TF/factor VIIa factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.

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##

Ras farnesyl transferase inhibitors

Benzodiazepine derivatives are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases for which inhibition of the ras farnesyl:protein transferase is indicated. Also disclosed are benzazepines of the following general formula (II) having similar utility as the aforementioned benzodiazepines: ##STR1##

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Mountain View, CA, United States of America

Thomas E Rawson