Astrazeneca Ab

John Peter Gilday

Anthony Stephen Graham

Martin Hans Bohlin

Jonathan David Moseley

Evan William Snape

Philip Hopes

David Brown

Andrew Wells

David Moody

Bo Ingvar Ymen

Martin Bohlin

Enzymatic and chemical processes for the preparation of certain of 3-phenyl-2-arylalkylthiopropionic acid derivatives which have utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance and other manifestations of the metabolic syndrome are described and also certain novel intermediates used in these processes.

Chemical Process

Chemical processes and intermediates useful in the manufacture of the quinazoline derivative 4-(3'-chloro-4&#x2032;-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline, in particular processes for the manufacture of 7-methoxy-6-(3-morpholinopropoxy)-3,4-dihydroquinazolin-4-one of Formula II and 4-methoxy-5-(3-morpholinopropoxy)-2-nitrobenzonitrile of Formula III and their use in the manufacture of the quinazoline derivative.

Process for the preparation of 4-(3'-chloro-4&#x2032;-fluoroanilino) -7-methoxy-6-(3-morpholinopropoxy) quinazoline

The invention concerns certain crystalline solvates and hydrates of the compound of the Formula (I) which is known inter alia by way of the code number ZD1839. In particular, the invention concerns a first solvate that occurs in the presence of methanol which is designated as Form 2 ZD1839 MeOH solvate, a second solvate that occurs in the presence of dimethyl sulphoxide which is designated as Form 3 ZD1839 DMSO solvate and a trihydrate that occurs in the presence of water which is designated Form 5 ZD1839 trihydrate. The invention further concerns processes for the preparation of these solvates and the trihydrate and for their conversion back to the compound ZD1839, pharmaceutical compositions containing them and their use in the manufacture of medicaments for use the production of an anti-proliferative effect in a warm-blooded animal such as man. 

Crystalline forms of the anti-cancer compound ZD1839

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Bristol, United Kingdom

John Peter Gilday