Genentech, Inc.

Curis, Inc.

The University of Texas System

Sumitomo Chemical Company, Limited

Mark E Reynolds

Mark S Stanley

Daniel P Sutherlin

Scott J Savage

Thomas E Rawson

David A Oare

Georgette M Castanedo

Shumei Wang

Kimberly Malesky

Michael S Dina

Liang Bao

Rebecca L Lalonde

James C Marsters

Dean R Artis

Srinivasan Babu

David Y Jackson

Michael F T Koehler

Qingping Tian

Zhigang Cheng

Robert S McDowell

Thomas Gadek

Joseph L Goldstein

Michael S Brown

Daniel J Burdick

Todd C Somers

Janet Gunzner

Robert L Cohen

Janet L Gunzner-Toste

Craig W Crowley

Herbert Yajima

Edward HyungSuk Ha

Guy L James

Henry Bernard Lowman

Paul Polakis

Gerald R Nakamura

Melissa A Starovasnik

Takashi Miki

Yasuharu Shimasaki

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 present invention relates to antibody-drug conjugate compounds of Formula I:Ab-(L-D)&#x2003;&#x2003;I where one or more nemorubicin metabolite or analog drug moieties (D) are covalently attached by a linker (L) to an antibody (Ab) which binds to one or more tumor-associated antigens or cell-surface receptors. These compounds may be useful in methods of diagnosis or treatment of cancer, and other diseases and disorders.

Nemorubicin metabolite and analog reagents, antibody-drug conjugates and methods

The present invention relates to a method for manufacturing a boronic acid ester compound, characterized by reacting an aryl halide compound and a diboron ester compound in the presence of a nitrogen-containing organic base, a nickel catalyst, a phosphine compound and a solvent. According to the manufacturing method of the present invention, even if a nickel catalyst is used as the catalyst, a desired boronic acid ester compound can be obtained in a sufficiently high yield. Furthermore, even if aryl chloride or aryl bromide having relatively low price and low reactivity, was used as the aryl halide compound, a desired boronic acid ester compound can be obtained in a sufficiently high yield.

Method for manufacturing a boronic acid ester compound

The present invention relates to antibody-drug conjugate compounds of Formula I:Ab-(L-D)&#x2003;&#x2003;I

The invention provides processes of preparing, separating, and purifying PI3K inhibitor, Formula I and II compounds, and novel intermediates for preparing Formula I and II compounds.  

Process for making thienopyrimidine compounds

The invention provides processes of preparing, separating, and purifying PI3K inhibitor, Formula (I) and (II) compounds, and novel intermediates for preparing Formula (I) and (II) compounds. 

Compounds of the disclosure provide compositions, which are effective for prophylaxis and treatment of diseases or disorders, such as cell-proliferation, angiogenesis, or apoptosis mediated diseases. The disclosure encompasses compounds, analogs, prodrugs, metabolites, and pharmaceutically acceptable salts thereof, pharmaceutical compositions, and methods for prophylaxis and treatment of diseases and other maladies or conditions involving cancer, tumors, and like conditions. The disclosure also provides therapeutic methods including the administration of an effective amount of a compound of the disclosure.

Trp-p8 active compounds and therapeutic treatment methods

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 invention provides novel compounds which bind to the high affinity receptor for immunoglobulin E (IgE) designated Fc&#x3b5;RI and methods for identifying and preparing such compounds. In particular aspects, the invention provides to the treatment of disorders mediated by IgE utilizing the novel compounds of the invention. The invention also provides composition, such as pharmaceutical compositions, comprising the novel compounds, as well as for their use in research, diagnostic, therapeutic, and prophylactic methods.

IgE receptor antagonists

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

Growing community of inventors

Millbrae, CA, United States of America

Mark E Reynolds