Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2000-12-15
2002-08-13
Rotman, Alan L. (Department: 1625)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
Reexamination Certificate
active
06432987
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The invention relates to novel N-substituted indole-3-glyoxylamides, processes for their preparation and pharmaceutical uses. The compounds according to the invention have antitumor properties.
Indole-3-glyoxylamides have a variety of uses as pharmacodynamically active compounds and as synthetic building blocks in pharmaceutical chemistry.
In the patent application Neth. Appl. 6502481, compounds are described which have an antiinflammatory and antipyretic activity profile and analgesic activity.
In the British Application GB-B 1 028 812, derivatives of indolyl-3-glyoxylic acid and their amides are mentioned as analgesic, anticonvulsant and &bgr;-adrenergic compounds.
G. Domschke et al. (Ber. 94, 2353 (1961)) describes [sic] 3-indolylglyoxylamides which are not characterized pharmacologically.
E. Walton reports in J. Med. Chem., 11, 1252 (1968) on indolyl-3-glyoxylic acid derivatives which have an inhibitory action on glycerophosphate dehydrogenase and lactate dehydrogenase.
In the European Patent Specification EP 675110, 1H-indole-3-glyoxylamides are described which are profiled as sPLA2 inhibitors and are used in the treatment of septic shock, in pancreatitis and in the treatment of allergic rhinitis and rheumatoid arthritis.
It has already been proposed in the German Patent Application having the file reference 19814838.0 to employ the compounds according to DE-A 196 36 150 A1 as antitumor agents.
REFERENCES:
patent: 6008231 (1999-12-01), Lebaut et al.
patent: 6251923 (2001-06-01), Hofgen et al.
patent: 99/55696 (1999-11-01), None
Bacher Gerald
Emig Peter
Gunther Eckhard
Le Baut Guillaume
Nickel Bernd
Rotman Alan L.
Zentaris AG
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