Crystalline forms of the anti-cancer compound ZD1839

Details Crystalline forms of the anti-cancer compound ZD1839 Crystalline forms of the anti-cancer compound ZD1839

2003-02-24

2009-11-03

McKane, Joseph K (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C544S253000

Reexamination Certificate

active

07612077

ABSTRACT:
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.

REFERENCES:
patent: 5457105 (1995-10-01), Barker
patent: 5616582 (1997-04-01), Barker
patent: 5770599 (1998-06-01), Gibson
patent: 96/33980 (1996-10-01), None
patent: 96/33980 (1996-10-01), None
patent: WO-96/33980 (1996-10-01), None
patent: 01/76586 (2001-10-01), None
patent: 03/072139 (2003-09-01), None

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