Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1991-07-18
1993-04-13
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546177, 546332, 546336, 549 49, 549 77, 549441, 514311, 514337, 514443, 514464, 514466, A61K 3138, C07D30752
Patent
active
052023494
ABSTRACT:
Substituted phenylacetylenes of the formula ##STR1## wherein one of the groups R.sub.1 is a hydrogen atom and the other represents the group of the formula ##STR2## in which R.sub.3 is hydrogen, methyl or ethyl and R.sub.4 is a methyl or an amino group and wherein R.sub.2 represents mono- or binuclear aromatic or heterocyclic residues containing sulfur, nitrogen or oxygen as hetero atoms and optionally being substituted by 1 to 3 substituents as defined, which specifically inhibit 5-lipoxygenase and are useful in pharmaceutical compositions for prophylaxis and treatment of diseases due to the action of leukotrienes.
The compounds may be prepared by reacting a compound of the formula ##STR3## wherein R.sub.2 has the same meaning as above and one of the groups R.sub.7 is a hydrogen atom and the other represents the group of the formula --COR.sub.3, with hydroxylamine to form the oxime which then is reduced to the corresponding hydroxylamine compound into which the group of the formula --COR.sub.4 is introduced.
REFERENCES:
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Summers et al., J. Med. Chem., 30:2121-26 (1987).
Bosman Brigitte J.
Englberger Werner
Haurand Michael
Schneider Johannes
Seipp Ulrich
Gruenenthal GmbH
Raymond Richard L.
Russell Mark W.
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