Genentech, Inc.

Auckland Uniservices Limited

Pfizer Corporation

Btg International Limited

Ho Huat Lee

William Alexander Denny

John A Flygare

Brian Salvatore Safina

Thomas Pillow

BinQing Wei

Vishal Verma

Moana Tercel

Guo-Liang Lu

Gordon William Rewcastle

William Robert Wilson

Jeffrey Bruce Smaill

Guiling Zhao

Leanna Staben

Adam Vorn Patterson

Janet L Gunzner-Toste

Amir Ashoorzadeh

Michael Patrick Hay

Anna Giddens

Muriel Bonnet

Christian Miller

Robert Forbes Anderson

Joseph Thomas Repine

James S Kaltenbronn

Andrew David White

Brian Desmond Palmer

Ellen Myra Dobrusin

Richard John Booth

Binqing Wei

Andrew Mark Thompson

Douglas Scott Johnson

Daniele Marie Leonard

Alan Kraker

Bronwyn Gae Siim

Alexandra Marie Mowday

Jared Bruce John Milbank

Adrian Blaser

Shangjin Yang

Richard H Hutchings

Frederik Bastiaan Pruijn

Karin Pchalek

Kevin Owen Hicks

Stephen Michael Frazer Jamieson

Kendall Marie Carlin

Lorna Helen Mitchell

Florence Oliver Joseph McCarthy

Andrej Maroz

Huai-Ling Annie Hsu

Janet Gunzner-Toste

Thomas H Pillow

This invention relates to peptidomimetic linkers and anti-body drug conjugates thereof, to pharmaceutical compositions containing them, and to their use in therapy for the prevention or treatment of cancer.

Peptidomimetic compounds and antibody-drug conjugates thereof

The invention provides antibody-drug conjugates comprising an antibody conjugated to a 1-(chloromethyl)-2,3-dihydro-1H-benzo[e]indole (CBI) dimer drug moiety via a linker, and methods of using the antibody-drug conjugates.

1-(Chloromethyl)-2,3-dihydro-1H-benzo[e]indole dimer antibody-drug conjugate compounds, and methods of use and treatment

1-(chloromethyl)-2,3-dihydro-1H-benzo[E]indole dimer antibody-drug conjugate compounds, and methods of use and treatment

The invention provides kinase inhibitors of Formula I:  Also provided are reductive prodrugs, comprising a kinase inhibitor as defined above and a reductive trigger linked directly or indirectly to a nitrogen of the kinase inhibitor. Further provided are pharmaceutical compositions, comprising the kinase inhibitors or the prodrugs, and the use of such compositions in therapy, in particular for treating cancer.

Kinase inhibitors, prodrug forms thereof and their use in therapy

The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a positive charge. In preferred embodiments, the compounds are of Formula I: where: X is any negatively charged counterion; Ris a group of the formula &#x2014;(CH)Tr, where Tr is an aromatic nitroheterocycle or aromatic nitrocarbocycle and &#x2014;(CH)Tr acts as a reductively-activated fragmenting trigger; and n is an integer from 0 to 6; R, Rand Rmay each independently be selected from aliphatic or aromatic groups of a tertiary amine kinase inhibitor (R)(R)(R)N, or two of R, R, and Rmay form an aliphatic or aromatic heterocyclic amine ring of a kinase inhibitor, or one of R, Rand Rmay be absent and two of R, Rand Rform an aromatic heterocyclic amine ring of a kinase inhibitor. The compounds of the invention are useful in treating proliferative diseases such as cancer.

Prodrug forms of kinase inhibitors and their use in therapy

The invention relates to novel tricyclic 1,2,4-triazine-1-oxides and novel tricyclic 1,2,4-triazine-1,4-dioxides of formula I and to related analogues, to their preparation, and to their use as hypoxia-selective drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.

Tricyclic 1,2,4-triazine oxides and compositions for therapeutic use in cancer treatments

This invention relates to pyrrolocarbazole derivatives according formula I wherein R, R, R, R, R, X and Y are as defined in the specification wherein said derivatives specifically inhibit one or both of the checkpoint kinases Wee1 and Chk1 

Inhibitors of checkpoint kinases (Wee1 and Chk1)

The present invention provides novel 5-substituted tetralones of Formulas I, II, III, and IV and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, which are useful for treating and preventing uncontrolled or abnormal proliferation of tissues, such as cancer, atherosclerosis, restenosis, and psoriasis. Specifically, the present invention relates to compounds that inhibit the farnesyl transferase enzyme

5-substituted tetralones as inhibitors of ras farnesyl transferase

A process for the preparation of the compound AQ4 of formula 3:

Synthetic method

Growing community of inventors

Auckland, New Zealand

Ho Huat Lee