Astrazeneca Ab

Georges Rene Pasquet

Frederic H Jung

Andrew Mortlock

Nicola Murdoch Heron

Frederic Henri Jung

Laurent F A Hennequin

Andrew Austen Mortlock

Quinazoline derivatives of formula (I): wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.

Phosphonoxy quinazoline derivatives and their pharmaceutical use

Quinazoline derivatives of formula (I); for use in the treatment of proliferative diseases such as cancer and in the preparation of medicaments for use in the treatment of proliferative diseases, and to process for their preparation, as well as pharmaceutical compositions containing them as active ingredient. 

Chemical compounds

The invention provides quinazoline derivatives of formula (I): in the preparation of a medicament for use in the inhibition of Aurora kinase and also novel quinazoline derivatives, processes for their preparation, pharamceutical compositions containing them and their use in therapy 

Substituted quinazoline derivatives as inhibitors of aurora kinases

The invention relates to the use of compounds of the formula I: wherein: ring C is a 5-6 membered heterocyclic moiety; Z is &#x2014;O&#x2014;, &#x2014;S&#x2014;, or &#x2014;CH&#x2014;; Ris hydrogen, Calkyl, Calkoxymethyl, di(C)alkoxy)methyl, Calkanoyl, trifluoromethyl, cyano, amino, Calkenyl, Calkynyl, carboxy, Ccycloalkyl, C-cycloalkylCalkyl, or an optionally substituted group selected from phenyl, benzyl, phenylCalkyl and a 5-6 membered heterocyclic group; n is an integer from 0 to 5; m is an integer from 0 to 3; Rrepresents hydrogen, hydroxy, halgeno, 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 Xrepresents a direct bond, &#x2014;CH&#x2014;, or a heteroatom linker group and Ris an alkyl, alkenyl or alkynyl chain optionally substituted by for example hydroxy, amino, nitro, alkyl, cycloalkyl, alkoxyalkyl, or an optionally substituted group selected from pyridone, phenyl and a heterocyclic ring, which alkyl, alkenyl or alkynyl chain may have a heteroatom linker group, or Ris an optionally substituted group selected from pyridone, phenyl and a heterocyclic ring, 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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Reims, France

Georges Rene Pasquet