Warner-lambert Company

Auckland Uniservices Limited

Global Alliance for Tb Drug Development

Pfizer Corporation

Janssen Pharmaceutica Nv

Cancer Research Campaign Technology Limited

Warner Lambert LLC

Brian Desmond Palmer

William Alexander Denny

Andrew Mark Thompson

Zhenkun Ma

William Robert Wilson

Gordon William Rewcastle

Howard D Showalter

Ellen Myra Dobrusin

Hamish Scott Sutherland

James Bernard Kramer

Diane H Boschelli

Koenraad Jozef Lodewijk Marcel Andries

Annette Marian Doherty

James Marino Hamby

Christopher Blair Cooper

Moana Tercel

Swarnalatha Akuratiya Gamage

Adrian Blaser

David C Ware

Sonya Shah Khatana

Anna Marie Upton

Walter Marcel Mathilde Van Den Broeck

Lai Ming Ching

Iveta Kmentova

Genliang Lu

Charles Z Ding

Graham John Atwell

Jeffrey Bruce Smaill

Richard John Booth

Howard Daniel Hollis Showalter

Ho Huat Lee

Julie Ann Spicer

Keith D Combrink

Alan Kraker

Lai-Ming Ching

Jiancheng Wang

Jeremy Tyson Starr

Richard John Sciotti

William P Wilson

Minsoo Song

Florence Oliver Joseph McCarthy

Lorna Helen Mitchell

Christopher Richardson

Dianjun D Chen

Koenraad Jozel Lodewijk Marcel

Jerome Emile Goerges Guillemont

Andrew M Thompson

Diajun D Chen

Pharmaceutical compositions comprising 3-aminoisoxazolopyridine compounds of the Formula I having IDO1 and/or TDO inhibitory activity are described, where W is CR, N or N-oxide; X is CR, N or N-oxide; Y is CR, N or N-oxide; Z is CR, N or N-oxide; and at least one of W, X, Y, and Z is N or N-oxide; and Rand Rare as defined. Also described are methods of using such compounds in the treatment of various conditions, such as cancer.

Inhibitors of tryptophan dioxygenases (IDO1 and TDO) and their use in therapy

Pharmaceutical compositions comprising 3-aminoisoxazolopyridine compounds of the Formula I having IDO1 and/or TDO inhibitory activity are described, where W is CR1, N or N-oxide; X is CR2, N or N-oxide; Y is CR3, N or N-oxide; Z is CR4, N or N-oxide; and at least one of W, X, Y, and Z is N or N-oxide; and R9 and R10 are as defined. Also described are methods of using such compounds in the treatment of various conditions, such as cancer. 

The present invention relates to compounds of formula (I) including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of tuberculosis. 

Antibacterial compounds and uses thereof

Pharmaceutical compositions comprising 3-aminoisoxazolopyridine compounds of the Formula I having IDO1 and/or TDO inhibitory activity are described, where W is CR, N or N-oxide; X is CR, N or N-oxide; Y is CR, N or N-oxide; Z is CR, N or N-oxide; and at least one of W, X, Y, and Z is N or N-oxide; and Rand Rare as defined. Also described are methods of using such compounds in the treatment of various conditions, such as cancer. 

The present invention relates to novel nitroimidazooxazines, to their preparation, and to their use as drugs for treatingand other microbial infections, either alone or in combination with other anti-infective treatments.

Nitroimidazooxazines and their uses in anti-tubercular therapy

The current invention provides a series of bicyclic nitroimidazole-substituted phenyl oxazolidinones in which a bicyclic nitroimidazole pharmacophore is covalently bonded to a phenyl oxazolidinone, their pharmaceutical compositions, and the method of use of the compositions for prevention and treatment of bacterial infections. The bicyclic nitroimidazole-substituted phenyl oxazolidinones possess surprising antibacterial activity against wild-type and resistant strains of pathogens, and are therefore useful for the prevention, control and treatment of a number of human and veterinary bacterial infections caused by these pathogens, such as

Bicyclic nitroimidazole-substituted phenyl oxazolidinones

Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I as disclosed herein can be used in a variety of applications including use as antibacterial agents. 

Substituted Imidazo[1,2-a]pyridines as Antibacterial Agents

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)

A range of aziridin-1-yl nitrobenzamides are provided for use as prodrugs in conjunction with nitroreductase (NR) enzymes. The amides may have 1 or 2-substituents which may be bulky and polar. For example, 5-(aziridin-1-yl)-N-&lsqb;2-(4-morpholino)ethyl&rsqb;-2,4-dinitrobenzamide of Formula (A) was found to be highly active against all NR&plus; cell lines tested.

Nitrophenylaziridine compounds and their use as prodrugs

Benzimidazoles of Formula I below are inhibitors of protein tyrosine kinases, and are useful in treating cellular proliferation.

Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular proliferation

Benzimidazoles of Formula I below are inhibitors of protein tyrosine kinases, and are useful in treating cellular proliferation. ##STR1## The compounds are especially useful in treating cancer, atherosclerosis, restenosis, and psoriasis.

Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular

The invention provides nitroaniline derivatives represented by general formula (1) where the nitro group is substituted at any one of the available benzene positions 2-6; where R and A separately represent the groups NO.sub.2, CN,COOR.sup.1, CONR.sup.1 R.sup.2, CSNR.sup.1 R.sup.2 or SO.sub.2 NR.sup.1 R.sup.2 and A is substituted at any one of the available benzene positions 2-6; where B represents N(CH.sub.2 CH.sub.2 halogen).sub.2 or N(CH.sub.2 CH.sub.2 OSO.sub.2 R.sup.3).sub.2 substituted at any one of the available benzene positions; and where R.sup.1, R.sup.2 and R.sup.3 separately represent H, or lower alkyl optionally substituted with hydroxyl, ether, carboxy or amino functions, including cyclic structures, or R.sup.1 and R.sup.2 together with the nitrogen form a heterocyclic structure, and pharmaceutical preparations containing them. These compounds have activity as hypoxia-selective cytotoxins, reductively-activated prodrugs for cytotoxins, hypoxic cell radiosensitisers, and anticancer agents. ##STR1##

Nitroaniline derivatives and their use as anti-tumour agents

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

Brian Desmond Palmer