Genentech, Inc.

Auckland Uniservices Limited

Cancer Research Campaign Technology Limited

Warner-lambert Company

Warner Lambert LLC

Moana Tercel

William Alexander Denny

John A Flygare

Brian Salvatore Safina

Thomas Pillow

Gordon William Rewcastle

BinQing Wei

Vishal Verma

Ho Huat Lee

William Robert Wilson

Graham John Atwell

Guiling Zhao

Brian Desmond Palmer

Howard D Showalter

Ellen Myra Dobrusin

Andrew Mark Thompson

Leanna Staben

Binqing Wei

Janet L Gunzner-Toste

Anna Giddens

Muriel Bonnet

Guo-Liang Lu

Christian Miller

Adam Vorn Patterson

Shangjin Yang

Ralph James Stevenson

Frederik Bastlaan Pruijn

Jared Milbank

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 present invention relates generally to nitro-1,2-dihydro-3H-benzo[e]indoles and 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.

Nitrobenzindoles and their use in cancer therapy

A compound which is a 6-substituted seco indoline of the formula (I):

Seco precursors of cyclopropylindolines and their use as prodrugs

The invention provides compounds of general formula (I), wherein: X is halogen or OSO.sub.2 R, where R represents H or is unsubstituted or hydroxy-or amino-substituted lower alkyl; Y is a nitro or amine group or a substituted derivative thereof; W is selected from the structures of formulae (Ia, Ib or Ic), where E is --N.dbd. or --CH.dbd., G is O, S, or NH, and Q is either up to three of R, OR, NRR, NO.sub.2, CONHR, NHCOR or NHCONHR, or is an additional group of formulae (Ia, Ib or Ic) and HET represents a 5- or 6-membered carbocycle or heterocycle; and A and B collectively represent a fused benzene or 2-CO.sub.2 R pyrrole ring. In one embodiment, the group Y is an amine derivative substituted by a group which is a substrate for a nitroreductase or carboxypeptidase enzyme such that one of said enzymes is able to bring about removal of that group. ##STR1##

Condensed N-aclyindoles as antitumor agents

Cyclopropylindoles and their seco precursors, and their use as prodrugs

##STR1## Nitrobenzyl mustard quaternary salts of formula (I), and the pharmaceutically acceptable salts thereof, process for their manufacture and their chemotherapeutic use as hypoxia selective cytotoxic agents. Wherein, X represents a linker chain --CR.sub.1 R.sub.3 -- or CR.sub.1 .dbd.CR.sub.2 -- (where R.sub.1 and R.sub.2 are separately H, lower alkyl, phenyl or nitrophenyl; Y is halogen or OSO.sub.2 R; Q is lower alkyl (optionally substituted with alkyl and/or ether groups and containing up to 6 carbons) or nitrophenyl; Ar represents a mono- or bicyclic aromatic unit, R is lower alkyl optionally substituted with alkyl and/or ether groups, and may contain up to eight carbon atoms. Z represents one or more of the groups NO.sub.2, SO.sub.2 R, CONHR, R, OR, SR, CF.sub.3 and aza (ring --CH-- replared by --N.dbd.); with the proviso that when Y=Cl or Br, Q=Me, and X=--CH.sub.2 -- then Ar.noteq.2-nitrophanyl or 4-nitrophenyl.

Nitrobenzyl mustard quaternary salts and their use as hypoxia-selective

2-Thioindoles (2-selenoindoles) and analogous 2-indolinethione (2-indolineselenone) and polysulfide (selenide) compounds, salts thereof, methods of production, intermediates in their production, pharmaceutical compositions containing said compounds, and methods for inhibiting protein kinase dependent disease in a mammal or treating aberrant cell growth in a mammal, using said compositions, are disclosed.

2-thioindoles (selenoindoles) and related disulfides (selenides) which

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Auckland, New Zealand

Moana Tercel