Medimmune Limited

Spirogen Sarl

Genentech, Inc.

Seattle Genetics, Inc.

Spirogen Limited

Spirogen Developments Sàrl

Luke Masterson

Philip Wilson Howard

Paul Polakis

Arnaud Charles Tiberghien

Stephen John Gregson

John A Flygare

Andrew G Polson

Thomas Pillow

Janet L Gunzner-Toste

Peter Senter

Brian Salvatore Safina

Scott C Jeffrey

Patrick J Burke

Guiling Zhao

Vishal Verma

Binqing Wei

Leanna Staben

Zhizhi Chen

Nazzareno Dimasi

Thais Cailleau

Helga E Raab

Niall Dickinson

Maximillian Taro William Lee

Andreas Lothar Severino Maderna

Akbar Husain Khan

Nicole Danielle Bartolo

William Robert Fraser Goundry

Alla Pryyma

Balakumar Vijayakrishnan

Albano Galan Coca

Mattia Cocco

Jonathan David Beadle

Boliang Deng

Jason White

Elizabeth Dunny

William Goundry

Janet L Gunzner

Arnaud Tiberghien

Janet Gunzner-Toste

Susan D Spencer

The specification relates to conjugates comprising a linker of Formula (IA): and pharmaceutically acceptable salts thereof. The specification also relates the use of the conjugates for the treatment of diseases such as cancer, and intermediates useful for the synthesis of the conjugates.

Conjugates comprising cleavable beta-glucuronide-containing linkers

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

Peptidomimetic compounds and antibody-drug conjugates thereof

A conjugate of formula (I) wherein Ab is a modified antibody having at least one free conjugation site on each heavy chain. 

Pyrrolobenzodiazepine conjugates

A conjugate of formula I:L-(D)&#x2003;&#x2003;(1) wherein L is a Ligand unit, Dis a Drug Linker unit of formula II:  wherein either: (a) Rand Rform a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (b) Ris OH, and Ris:  p is an integer of from 1 to 20.

Pyrrolobenzodiazepine antibody conjugates

A conjugate comprising the following topoisomerase inhibitor derivative (A*): with a linker for connecting to a Ligand Unit, wherein the linker is attached in a cleavable manner to the amino residue. The Ligand Unit is preferably an antibody. Also provided is A* with the linking unit attached, and intermediates for their synthesis, as well as the released warhead.

Compounds and conjugates thereof

A conjugate of formula (A): where Y is selected from a single bond, and a group of formulae A1 or A2: where N shows where the group binds to the N10 of the PBD moiety;

Pyrrolobenzodiazepines and conjugates thereof

A conjugate of formula (I): L-(D)(I) wherein L is a Ligand unit, D is a Drug Linker unit of formula (II) wherein p is an integer of from 1 to 20. 

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

Pyrrolobenzodiazepine dimers having a C2-C3 double bond and an aryl group at the C2 position on one monomer unit, and a C2-C3 double bond and either a conjugated double or triple bond at the C2 position or an alkyl group at the C2 position on the other monomer unit, and conjugates of these compounds.

Pyrrolobenzodiazepines used to treat proliferative diseases

Unsymmetrical pyrrolobenzodiazepine-dimers for treatment of proliferative diseases

The present invention is directed to novel pyrrolobenzodiazepine dimers and methods of using the dimers in the treatment of proliferative diseases.

A compound of formula (I): which is substantially free of any of the corresponding compound of formula (IB): methods of making such compounds, and the further transformation of such compounds. 

Intermediates useful for the synthesis of pyrrolobenzodiazepines

Pyrrolobenzodiazepine dimers I having a C2-C3 double bond and an aryl group at the C2 position on one monomer unit, and a C2-C3 double bond and either a conjugated double or triple bond at the C2 position or an alkyl group at the C2 position on the other monomer unit, and conjugates of these compounds. 

Claimed are unsymmetrical Pyrrolobenzodiazepine-dimers (PBD-dimers) of formula (I), that are unsymmetrical due at least to the values that the variables Rand Rrepresent. Formula (I), wherein: Ris of formula (II), where A is a Caryl group, X is selected from the group comprising: OH, SH, COH, COH, N&#x2550;C&#x2550;O, NHR, wherein Ris selected from the group comprising H and Calkyl, and (OCH)OCH, where m is 1 to 3, and either: (i) Qis a single bond, and Qis selected from a single bond and &#x2014;Z&#x2014;(CH)&#x2014;, where Z is selected from a single bond, O, S and NH and n is from 1 to 3; or (ii) Qis &#x2014;CH&#x2550;CH&#x2014;, and Qis a single bond; Ris a Caryl group, optionally substituted by one or more substituents selected from the group comprising: halo, nitro, cyano, ether, Calkyl, Cheterocyclyl and bis-oxy-Calkylene. The other variables are as defined in the claims. The compounds are useful for the treatment of proliferative diseases. 

Methods of preparing ZC-423 (I) which result in varying enantiomeric ratios. 

Pyrrolobenzodiazepines

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Luke Masterson