Astrazeneca Ab

Zeneca Limited

Other

Imperial Chemical Industries Limited

Zeneca Pharma S. A.

Astra Zeneca U.k. Limited

Genzyme Corporation

Andrew Peter Thomas

Laurent Francois Andre Hennequin

Jean-Jacques Marcel Lohmann

Elaine Sophie Elizabeth Stokes

Nicholas John Newcombe

Craig Johnstone

Kevin Michael Foote

David Buttar

Maria-Elena Theoclitou

Lyn Powell

Stanley A Lee

David M Martin

Robert Hugh Bradbury

Patrick Ple

Edward Clayton

Gloria Anne Breault

David William Heaton

Laurent Francois Hennequin

David A Roberts

Dearg Sutherland Brown

Bernard Christophe Barlaam

Robert J Pearce

Jeffrey James Morris

Thorsten Nowak

Phillip John Jewsbury

John Franklin Beattie

Andrew Pape

The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R' represents halogeno or Calkyl; Xrepresents &#x2014;O&#x2014;; Ris selected from one of the following three groups: 1) CalkylR(wherein Ris piperidin-4-yl which may bear one or two substituents selected from hydroxy, halogeno, Calkyl, Chydroxyalkyl and Calkoxy; 2) CalkenylR(wherein Ris as defined hereinbefore); 3) CalkynylR(wherein Ris as defined hereinbefore); and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis. 

Quinazoline derivatives as VEGF inhibitors

There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.

Compounds

Methods of treating cancer with a pyrazole derivative

The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; Rrepresents halogeno or Calkyl; Xrepresents &#x2014;O&#x2014;; Ris selected from one of the following three groups: 1) CalkylR, wherein Ris piperidinyl-4-yl which may bear one or two substituents selected from hydroxy, halogeno, Calkyl, Chydroxyalkyl and Calkoxy; 2) CalkenylR, wherein Ris as defined herein; 3) CalkynylR, wherein Ris as defined herein; and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation; pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.

The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; Rrepresents halogeno or Calkyl; Xrepresents &#x2014;O&#x2014;; Ris selected from one of the following three groups: 1) C-5alkylR(wherein Ris piperidinyl-4-yl which may bear one or two substituents selected from hydroxy, halogeno, Calkyl, Chydroxyalkyl and Calkoxy; 2) CalkenylR(wherein Ris as defined hereinbefore); 3) CalkynylR(wherein Ris as defined hereinbefore); and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis. 

N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1h-pyrazol-3-yl]-4-(3,4-dimethylpiperazin-1-yl)benzamide and salts thereof

N-[5-[2-(3,5-Dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-4-(3,4-dimethylpiperazin-1-yl)benzamide and salts thereof

The invention relates to quinazoline derivatives of formula (1) wherein m is an integer from 1 to 2; Rrepresents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, Calkyl, Calkoxy, Calkylthio, or &#x2014;NRR(wherein Rand R, which may be the same or different, each represents hydrogen or Calkyl); Rrepresents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; Rrepresents hydroxy, halogeno, Calkyl, Calkoxy, Calkanoyloxy, trifluoromethyl, cyano, amino or nitro; Xrepresents &#x2014;O&#x2014;, &#x2014;CH&#x2014;, &#x2014;S&#x2014;, &#x2014;SO&#x2014;, &#x2014;SO&#x2014;, &#x2014;NRCO&#x2014;, &#x2014;CONR&#x2014;, &#x2014;SONR&#x2014;, &#x2014;NRSO&#x2014; or &#x2014;NR&#x2014; (wherein R, R, R, Rand Reach independently represents hydrogen, Calkyl or CalkoxyCalkyl); Rrepresents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selected from alkyl and a 5 or 6 membered saturated carbocyclic or heterocyclic group, and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

Quinazoline derivatives and pharmaceutical compositions containing them

N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof

A compound of Formula (I); wherein the substituents are as defined in the text for use in modulating insulin-like growth factor 1 receptor activity in a warm blooded animal such as man. 

4-(pyrazol-3-ylamino) pyrimidine derivatives for use in the treatment of cancer

Compounds of the formula (I), and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti cell proliferation) effect in a warm blooded animal, such as man. 

Pyrimidine derivatives possessing cell-cycle inhibitors activity

The invention provides compounds of formula in which R, R, Rand Rhave the meanings defined in the specification; processes for the preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.

Pyrimidine derivatives as modulators of insulin-like growth factor-1 receptor (IGF-I)

Compounds of the formula (I), wherein R, R, R, R, Rand p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man. 

Pyrimidine compounds

Compounds of the formula (I): wherein R, R, R, R, Rand p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man. 

Derivatives of 4-(imidazol-5-yl)-2-(4-sulfoanilino)pyrimidine with CDK inhibitory activity

Compounds of the formula (I) wherein R, R, R, R, R, Rand p are as defined within and pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man. 

Growing community of inventors

Macclesfield, United Kingdom

Andrew Peter Thomas