Imperial Chemical Industries Limited

Astrazeneca Ab

Zeneca Limited

British Technology Group Limited

Cancer Research Campaign Technology Limited

Other

National Research Development Corporation

Angiogene Pharmaceuticals Limited

Astrzenca Ab

Francis Thomas Boyle

James Michael Wardleworth

Keith Hopkinson Gibson

Zbigniew S Matusiak

David Huw Davies

Zbigniew Stanley Matusiak

Jean-Claude Arnould

Bernard Thomas Golding

Kevin Michael Foote

David Richard Newell

David Charles Blakey

Alan H Calvert

Roger J Griffin

Nicola J Curtin

Martin E M Noble

Zbigniew Stanely Matusiak

Jane A Endicott

Philip J Jewsbury

Peter Wedderburn Kenny

Peter Beverley Scholes

Andrew John Barker

Gareth Morse Davies

Peter David Davis

Robert Anthony Davies

Vassilios Bavetsias

Peter R Marsham

Michael B Gravestock

Brian S Tait

Marianne Bernice Ashford

Richard W Bayles

David William Tonge

David William Heaton

Anthony Michael Slater

Laurent Francois Hennequin

Michael Wardleworth

Thomas Geoffrey Bird

John Frederick Hennam

James M Wapdleworth

Robert G Andrew

Sian Tomiko Taylor

James William Crook

Jonathan Hugh Marriott

Andrew Mark Hughes

Brian Robert Rabin

Antonio Tarragona-Fiol

Hendrikus Johannes Eggelte

Christopher John Taylorson

Donna Johnstone

Alan Davies

Michael A Taylor

Nigel Charles Barrass

The use of N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide, or a pharmaceutically acceptable salt thereof, in the treatment of cancer and/or pain in a warm blooded animal such as man is described.

N-(-3-methoxy-5-methylpyrazin-2-yl)-2-(4-'1,3,4-oxadiazol-2-yl-phenyl)pyridine-3 sulphonamide as an anticancer agent

The invention concerns compounds of formula (I), wherein each of R, R, R, R, R, R, R, R, Rm, n, p, X, Y and Z have any meanings defined in the description, processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-proliferative agent in the treatment of solid tumor disease.

4-substituted quinolines as antitumor agents

The invention relates to a group of novel indole compounds of Formula (I): wherein: R, R, R, R, R, R, R, R, R, and A are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds. 

Indolylalkylamino-methylidenecarbamate derivatives useful as GnRH antagonists

The invention provides a compound of Formula (Ia), or a pharmaceutically acceptable salt thereof, a process for t he preparation of a compound of Formula (1) and pharmaceutical compositions of a compound of Formula (1).

Substituted quinolines as antitumor agents

The invention concerns compounds of formula (I), wherein each of R, R, R, R, R, R, R, R, Rm, n, p, X, Y and Z have any meanings defined in the description, processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-proliferative agent in the treatment of solid tumour disease.

4-Substituted quinolines as antitumor agents

The invention relates to the use of compounds of formula (I): wherein X is &#x2014;C(O)&#x2014;, &#x2014;C(S)&#x2014;, &#x2014;C&#x2550;NOH, or &#x2014;CH(R)&#x2014; wherein Ris hydrogen, hydroxy, Calkoxy, &#x2014;ORor &#x2014;NRR(wherein Ris a group &#x2014;YR(wherein Yis a direct bond, &#x2014;C(O)&#x2014;, &#x2014;C(S)&#x2014;, &#x2014;S&#x2014;, &#x2014;C(O)O, &#x2014;C(O)NR&#x2014;, &#x2014;SO&#x2014; or &#x2014;SONR&#x2014; (wherein Rand R, which may be the same or different, each independently represents hydrogen, Calkyl or CalkoxyCalkyl) and Ris as defined herein, and Rincludes hydrogen; R, Rand Rare as defined herein and are preferably methyl; R, Rand Rare as defined herein with the proviso that Ris not hydroxy, alkoxy, substituted alkoxy, &#x2014;OPOH, &#x2014;O&#x2014;Calkanoyl or benzyloxy; and salts thereof in the manufacture of a medicament for use in the production of a vascular damaging effect in warm-blooded animals such as humans. The present invention further relates to compounds of the formula (I), pharmaceutical compositions containing them, processes for their preparation and to a method of treatment using the compounds to produce a vascular damaging effect in a warm-blooded animal such as a human. The compounds of formula (I) and the pharmaceutically acceptable salts thereof may be useful in the treatment of a number of disease states including cancer and rheumatoid arthritis. 

Colchinol derivatives as vascular damaging agents

This invention relates to compounds of formula (I) that inhibit farnesylation of gene products through inhibition of the enzyme farnesyl-protein transferase (FPTase). The invention also relates to methods of manufacturing the compounds, pharmaceutical compositions and methods of treating diseases, especially cancer, which are mediated through farnesylation.

Farnesyl transferase inhibitors

The invention provides a compound of Formula (Ia), or a pharmaceutically acceptable salt pro-drug or solvate thereof. The invention also provides a process for the preparation of a compound of Formula (Ia), pharmaceutical compositions of a compound of Formula (Ia) and methods for the treatment or prevention of cancer comprising administering an effective amount of a compound of Formula (Ia).

The invention provides a compound of Formula (I).Wherein R1, R2, R3, R10 and R11 have the meanings given in the description. Such compounds are predicted to cause the selective destruction of tumour vasculature. They may therefore be used to inhibit and/or reverse, and/or alleviate symptoms of angiogenesis and/or any disease state associated with angiogenesis.

Indole derivatives with vascular damaging activity

The present invention relates to inhibitors of ras farnesylation of the Formula Iwherein:

3-mercaptopyrrolidines as farnesyl protein transferase inhibitors

Inhibitors of farnesyl protein transferase

A range is disclosed of pyrimidine derivatives (I) which can act as inhibitors of cyclin dependent kinases (CDK's) and which thereby can provide useful therapeutic compounds for use in treatment of tumours or other cell proliferation disorders. The compounds of this invention bind to CDK molecules in a manner that appears to differ from that of known CDK inhibitors such as olomoucine and roscovitine. In formula (I), X is O, S or CHR where R is H or C alkyl; D is H or NZ Z where Z and Z are each independently H, C alkyl, C hydroxyalkyl, optionally substituted aryl or optionally substituted aralkyl; A is selected from H, C alkyl, C alkoxy, hydroxy, CH (CH ) OH (n&equals;1-4), and NR R where R and R are each independently H or C alkyl; Y is or includes an optionally substituted 4- to 8-membered carbocyclic or heterocyclic ring; D&prime; is H or NZ Z where Z and Z are each independently H, C alkyl, C hydroxyalkyl, optionally substituted aryl or optionally-substituted aralkyl; E is selected from NO, NO , N&boxH;N&mdash;Ar where Ar is an optionally substituted aryl or optionally substituted aralkyl, NR R or Nr Nr R (R , R and R each being independently H, C alkyl, C hydroxyalkyl, an optionally substituted aryl or an optionally substituted aralkyl), C(R )&boxH;U (R being hydrogen, C alkyl or substituted alkyl, e.g. hydroxyalkyl, or an unsubstituted or substituted aryl or aralkyl, e.g. benzyl, and U being selected from O, Nr &prime;, NOR &prime; and N&mdash;NR &prime;R &Prime; where R &prime; and R &Prime; are each independently H, C alkyl or CONH ), T, CH T, CHT and CT , where T is a halide I, Br, Cl or F.

Cyclin dependent kinase inhibitors

Pharmaceutical compositions comprising an inhibitor of ras farnesylation of formula (I) wherein, R is for example H and further values as defined in the specification; R is for example H and further values as defined in the specification; R is for example H or a substituent having values as defined in the specification; p is 0-3 in which R values can be the same or different; L is a linking moiety for example &mdash;CO&mdash;NH &mdash; and further values as defined in the specification; A is selected from phenyl; naphthyl; a 5-10 membered monocyclic or bicyclic heteroaryl ring containing up to 5 heteroatoms where the heteroatoms are independently selected from O, N and S; or a &mdash;S&mdash;S-dimer thereof when R &equals;H; or an enantiomer, diastereoisomer, pharmaceutically acceptable salt, prodrug or solvate thereof together with a pharmaceutically acceptable diluent or carrier. A particular use is cancer therapy.

4-mercaptopyrrolidine derivatives as farnesyl transferase inhibitors

The invention concerns anti-tumor agents of formula (I), wherein each of R , R and R has the meanings defined in the specification including hydrogen, (1-4C)alkyl, (3-4C)alkynyl and (1-4C)alkoxyl; each of R and R is (1-4C) alkyl; each of R and R is hydrogen or (1-4C)alkyl; X is N-(1-4C)alkylimino, N-(3-4C)alkenylimino, or (3-4C)alkynylimino; m is 1 or 2 and each R is as defined in the specification; each Y&prime; and Y is halogen, (1-4C)alkanesulphonyloxy, benzensulphonyloxy or phenyl-(1-4C)alkanesulfonyloxy; or a pharmaceutical acceptable salt thereof; provided that at least one of R , R and R is other than hydrogen; a process for their preparation, pharmaceutical composition containing them and their use for producing an anti-proliferative effect in a warm-blooded animal.

Anti-tumor agents

Imidazolyl compounds as inhibitors of farnesyl-protein tranferase

Growing community of inventors

Macclesfield, United Kingdom

Francis Thomas Boyle