2-thio-4h-3, 1-benzoxazin-4-one derivatives for use as...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C544S092000, C544S091000

Reexamination Certificate

active

06916808

ABSTRACT:
The use of a compound, comprising formula (I) or a salt, ester, amide of prodrug thereof in the inhibition of an enzyme whose preferred mode of action is to catalyse the hydrolysis of an ester functionality e.g. in the control and inhibition of unwanted enzymes in products and processes. The compounds are also useful in medicine e.g. in the treatment of obesity and related conditions. The invention also relates to novel compounds within formula (I), to processes for preparing them and pharmaceutical compositions containing them. In formula (I) A is an optionally substituted 6-membered aromatic or heteroaromatic ring; and R1is a branched or unbranched alkyl (optionally interrupted by one or more oxygen atoms), alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, reduced aryl, reduced heteroaryl, reduced heteroarylalkyl or a substituted derivative of any of the foregoing groups

REFERENCES:
patent: WO 00/40247 (2000-07-01), None
patent: WO 00/40569 (2000-07-01), None
NIDDK Weight—control Information Network at <http://www.niddk.nih.gov/health
utri/pubs/health.htm>, downloaded on Jun. 3, 2004 (9 pages).
Chalmers (TIPS vol. 17, pp. 166-172 Apr. 1996).
Thomas A. Godwin (Gastrointestinal Diseases, <http://edcenter.med.cornell.edu/CUMC_PathNotes/Gastrointestinal/Gastrointestinal.html>downloaded on Jun. 4, 2004, (51 pages).
Krantz et al., “Design and synthesis of 4H-3, 1-benzoxazin-4-ones as potent alternate inhibitors of human leukocyte elastase”,J. Med. Chem.33:464-479, 1990.
Robinson et al., “13-C nuclear magnetic resonance and reactivity of 4H-3, 1-benzoxazin-4-ones”,Can. J. Chem.66:416-419, 1988.
Copy of International Search Report for PCT/GB01/00171.

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