Astrazeneca Ab

Other

Zeneca Limited

Astra Zeneca U.k. Limited

Genzyme Corporation

Zeneca Pharma S. A.

Laurent Francois Andre Hennequin

Andrew Peter Thomas

Elaine Sophie Elizabeth Stokes

Jean-Jacques Marcel Lohmann

Craig Johnstone

Patrick Ple

Christopher Thomas Halsall

Robert Hugh Bradbury

Jason Grant Kettle

Edward Clayton

Kevin Michael Foote

Keith Hopkinson Gibson

Christine Marie Paul Lambert

Graham C Crawley

Robert I Dowell

Bernard Christophe Barlaam

David Huw Davies

James Francis McCabe

Peter R Marsham

Darren Mckerrecher

David Charles Blakey

Alleyn Thomas Plowright

Jeffrey Philip Poyser

Janet Elizabeth Pease

Kieran James Lennon

Benedicte Delouvrie

Andrew Turner

Craig Steven Harris

Richard Storey

Anthony Michael Slater

John Frederick Hennam

Alleyn Plowright

Peter Mark Smith

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

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 concerns quinazoline derivatives of the Formula I, or pharmaceutically acceptable salts thereof: wherein each of R, R, R, Rand m are as defined in the description; processes for their preparation; pharmaceutical compositions containing them and their use in the manufacture of a medicament for providing an anti-proliferative effect. The quinazoline derivatives of Formula I are expected to be useful in the treatment of diseases such as certain cancers mediated by erbB receptor tyrosine kinases, and, for example, EGFR tyrosine kinase.

Quinazoline derivatives as tyrosine kinase inhibitors

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. 

The invention concerns quinazoline derivatives of Formula (I) wherein each of Q, Z, Rand Qhave any of the 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 antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosine kinases. 

4-anilino quinazoline derivatives as antiproliferative agents

The invention relates to compounds of the formula (I) wherein ring C, Z, m, n, Rand Rare defined herein and salts thereof; their use in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals; processes for the preparation of such compounds; intermediates used in such processes; processes for making such intermediates; pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof and methods of treating disease states involving angiogenesis by administering a compound of formula I or a pharmaceutically acceptable salt thereof.

Quinazoline compounds

The present invention relates to compounds of the formula I: wherein: ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which moiety may be saturated or unsaturated, which may be aromatic or non-aromatic, and which optionally may contain 1-3 heteroatoms selected independently from O, N and S; is &#x2014;O&#x2014; &#x2014;NH&#x2014; or &#x2014;S&#x2014;; is 0, 1, 2, 3, 4 or 5; is 0, 1, 2 or 3; and Rand Rare as defined herein; and salts thereof; their use in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals; processes for the preparation of such compounds; pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof and methods of treating disease states involving angiogenesis by administering a compound of formula I or a pharmaceutically acceptable salt thereof. The compounds of formula I 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 angiogenesis inhibitors

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

The invention concerns quinazoline derivatives of Formula (I), wherein each of R, R, R, Rand a have any of the 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 antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosine kinases. 

Quinazoline derivatives as antiproliferative agents

The invention concerns quinazoline derivatives of the formula: (I); wherein X, Q, Z, R, R, Y, a and m are as defined in the description, which are erbB tyrosine kinase inhibitors, particularly EGFR tyrosine kinase inhibitors. Also claimed are processes for their preparation; pharmaceutical compositions containing them; and their use as therapeutic agents in the treatment of erbB tyrosine kinase mediated diseases such as cancer. 

Quinazoline derivatives and their use in the treatment of cancer

A quinazoline derivative of the formula I: wherein: R, R, R, R, R, R, RR, R, a, m and p are as defined in the description. Also claimed are pharmaceutical compositions containing the quinazoline derivative, the use of the quinazoline derivatives as medicaments and processes for the preparation of the quinazoline derivative. The quinazoline derivatives of formula I, are useful in the treatment of hyperproliferative disorders such as a cancer.

Quinazoline compounds for the treatment of hyperproliferative disorders

A quinazoline derivative of the Formula (I): wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm-blooded animal such as man. 

Quinazoline derivatives

The invention concerns quinazoline derivatives of the Formula (I); wherein each of R, R, W, X, X, Z, a and b are as defined in the description; processes for their preparation; pharmaceutical compositions containing them and their use in the manufacture of a medicament for providing an anti-proliferative effect. The quinazoline derivatives of Formula (I) are expected to be useful in the treatment of diseases such as certain cancers mediated by erbB receptor tyrosine kinases, particularly EGFR tyrosine kinase. 

The invention concerns quinazoline derivatives of Formula (I) wherein each of Z, m, R, n, R, Zand Rhave any of the meanings defined hereinbefore 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-invasive or anti-proliferative agent in the containment and/or treatment of solid tumour disease.

Quinzoline derivatives for use in the treatment of cancer

The invention concerns quinoline derivatives of Formula (I) wherein each of Z, m, R, n and Rhave any of the 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-invasive agent in the containment and/or treatment of solid tumour disease. 

Growing community of inventors

Reims, France

Laurent Francois Andre Hennequin