Single morphic forms of metalloproteinase inhibitors

Details Single morphic forms of metalloproteinase inhibitors Single morphic forms of metalloproteinase inhibitors

1999-10-22

2001-08-21

Powers, Fiona T. (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

C548S319500, C548S546000, C424S451000, C424S464000

Reexamination Certificate

active

06277827

ABSTRACT:

FIELD OF THE INVENTION
This invention relates to new crystalline forms of known compounds, having therapeutic utility, that are metalloproteinase inhibitors.
BACKGROUND OF THE INVENTION
As potential therapeutic agents, in the treatment of inflammatory and other conditions, there is considerable interest in compounds that have the ability to inhibit matrix metalloproteinases and also the release of tumour necrosis factor. Two known compounds of this type are 2S-[4-(2, 5-dioxopyrrolidin-1-yl)-2S-mercaptobutyrylamino]-4-methylpentanoic acid (2,2-dimethyl-1S-methylcarbamoylpropyl)amide (herein Compound A) and 2S-[2S-mercapto-4-(3,4,4-trimethyl-2, 5-dioxoimidazolidin-1-yl)butyrylamino]-4-methylpentanoic acid (2,2-dimethyl-1S-methylcarbamoylpropyl)amide (herein Compound B). Compound A is disclosed in WO-A-96/11209 and WO-A-98/39024. Compound B is disclosed in WO-A-97/12902 (generically) and WO-A-98/39024 (specifically).
SUMMARY OF THE INVENTION
This invention is based on the surprising discovery that Compounds A and B exists in more than one morphic form. Further, it has been found that, by comparison with the products whose preparation has previously been reported, novel compounds can be isolated as a single morphic form (this term is used herein to describe a crystalline form having a single morphology).
A novel morphic form according to the present invention is reproducibly isolable as a single crystalline species. It may be characterised by its crystalline structure, its X-ray powder diffraction (XRPD) pattern, its DSC thermogram, and/or by a different melting point from that previously reported. It may be essentially free of bound solvent, non-hygroscopic, and more thermodynamically stable, i.e. both more chemically and physically stable than the compound as previously reported. This stability makes the novel species particularly suitable for formulation into pharmaceutical formulations, following milling and, if appropriate, compression. It may also provide improved bioavailability.


REFERENCES:
patent: 96/11209 (1996-04-01), None
patent: 97/12902 (1997-04-01), None
patent: 98/39024 (1998-09-01), None

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