Astrazeneca Ab

Elaine S E Stokes

Patrick Ple

Darren Mckerrecher

Laurent F A Hennequin

The invention relates to the use of compounds of formula (I) and salts thereof, 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 as active ingredient and compounds of formula I. 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 angiogenesis inhibitors

The invention relates to the use of compounds of formula (I), wherein ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which optionally may contain 1&#x2013;3 heteroatoms selected independently from O, N and S; Z is &#x2014;O&#x2014;, &#x2014;NH&#x2014;, &#x2014;S&#x2014;, &#x2014;CH&#x2014; or a direct bond; n is 0&#x2013;5; m is 0&#x2013;3; Rrepresents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, Calkyl, Calkoxy, Calkylsulphanyl, &#x2014;NRR(wherein Rand R, which may be the same or different, each represents hydrogen or Calkyl), or RX&#x2014; (wherein Xand Rare as defined herein; Rrepresents hydrogen, oxo, halogeno, hydroxy, Calkoxy, Calkyl, Calkoxymethyl, Calkanoyl, Chaloalkyl, cyano, amino, Calkenyl, Calkynyl, Calkanoyloxy, nitro, Calkanoylamino, Calkoxycarbonyl, Calkylsulphanyl, Calkylsulphinyl, Calkylsulphonyl, carbamoyl, N&#x2014;Calkylcarbamoyl, N,N-di(Calkylcarbamoyl, aminosulphonyl, N&#x2014;Calkylaminosulphonyl, N,N-di(Calkyl)aminosulphonyl, N&#x2014;(Calkylsulphonyl)amino, N&#x2014;(Calkylsulphonyl)-N&#x2014;(Calkyl)amino, N,N-di(Calkylsulphonyl)amino, a Calkylene chain joined to two ring C carbon atoms, CalkanoylaminoCalkyl, carboxy or a group RX(wherein Xand Rare as defined herein); and salts thereof, 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 as active ingredient and compounds of formula (I). 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. 

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Macclesfield, United Kingdom

Elaine S E Stokes