Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1993-02-03
1995-02-21
Daus, Donald G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514256, 514275, 514340, 514367, 514370, 514376, 544326, 544330, 546275, 546280, 548161, 548193, 548222, 548226, C07D41312
Patent
active
053915658
DESCRIPTION:
BRIEF SUMMARY
OXAZOLIDINE DIONE DERIVATIVES
This invention relates to certain substituted oxazolidinedione derivatives, to a process for preparing such compounds, to pharmaceutical compositions containing such compounds and to the use of such compounds and compositions in medicine.
European Patent Applications, Publication Numbers 0008203, 0139421, 0155845, 0177353, 0193256, 0207581, 0208420 and 0306228 relate to thiazolidinedione derivatives which are disclosed as having hypoglycaemic and hypolipidaemic activity. Chem. Pharm. Bull 30 (10) 3580-3600 also relates to certain thiazolidinedione derivatives having hypoglycaemic and hypolipidaemic activities.
It has now surprisingly been discovered that certain novel substituted-oxazolidinedione derivatives show improved blood-glucose lowering activity and they are therefore of potential use in the treatment and/or prophylaxis of hyperglycaemia and are of particular use in the treatment of Type II diabetes.
These compounds are also indicated to be of potential use for the treatment and/or prophylaxis of other diseases including hyperlipidaemia, hypertension, cardiovascular disease and certain eating disorders.
Accordingly, the present invention provides a compound of formula (I): ##STR2## or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof, and/or a pharmaceutically acceptable solvate thereof, wherein: group; aralkyl group, wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group; and
Suitable aromatic heterocyclyl groups include substituted or unsubstituted, single or fused ring aromatic heterocyclyl groups comprising up to 4 hetero atoms in each ring selected from oxygen, sulphur or nitrogen.
Favoured aromatic heterocyclyl groups include substituted or unsubstituted single ring aromatic heterocyclyl groups having 4 to 7 ring atoms, preferably 5 or 6 ring atoms.
In particular, the aromatic heterocyclyl group comprises 1, 2 or 3 heteroatoms, especially 1 or 2, selected from oxygen, sulphur or nitrogen.
Suitable values for A.sup.1 when it represents a 5- membered aromatic heterocyclyl group include thiazolyl and oxazolyl, especially oxazolyl.
Suitable values for A.sup.1 when it represents a 6- membered aromatic heterocyclyl group include pyridyl or pyrimidinyl.
Preferably, A.sup.1 represents a moiety of formula (a), (b) or (c): ##STR3## wherein: R.sup.4 and R.sup.5 each independently represents a hydrogen atom, an alkyl group or a substituted or unsubstituted aryl group or when R.sup.4 and R.sup.5 are each attached to adjacent carbon atoms, then R.sup.4 and R.sup.5 together with the carbon atoms to which they are attached form a benzene ring wherein each carbon atom represented by R.sup.4 and R.sup.5 together may be substituted or unsubstituted; and in the moiety of formula (a) X represents oxygen or sulphur.
Aptly, A.sup.1 represents a moiety of the abovedefined formula (a).
Aptly, A.sup.1 represents a moiety of the abovedefined formula (b).
Aptly, A.sup.1 represents a moiety of the abovedefined formula (c).
In one favoured aspect R.sup.4 and R.sup.5 together represent a moiety of formula (d): ##STR4## wherein R.sup.6 and R.sup.7 each independently represent hydrogen, halogen, substituted or unsubstituted alkyl or alkoxy.
Suitably, R.sup.6 and R.sup.7 each independently represent hydrogen, halogen, alkyl or alkoxy.
Favourably, R.sup.6 represents hydrogen. Favourably, R.sup.7 represents hydrogen.
Preferably, R.sup.6 and R.sup.7 both represent hydrogen.
In a further favoured aspect R.sup.4 and R.sup.5 each independently represent hydrogen, alkyl or a substituted or unsubstituted phenyl group and more favourably, R.sup.4 and R.sup.5 each independently represent hydrogen, alkyl or phenyl.
Preferably, for the moiety of formula (a), R.sup.4 and R.sup.5 together represent the moiety of formula (d).
Preferably, for the moieties of formula (b) or (c), R.sup.4 and R.sup.5 both represent hydrogen.
Suitable substituents for the moiety A.sup.2 include halogen, substituted or unsubstituted alkyl or alkoxy.
Favoura
REFERENCES:
patent: 4367234 (1983-01-01), Schnur
patent: 5002953 (1991-03-01), Hindley
patent: 5037842 (1991-08-01), Goldstein
Chem.+Pharma. Bulletin vol. 30 No. 10. Oct. 1982. Tokyo, JP: T. Sohda et al. pp. 3563-3573.
Beechan Group p.l.c.
Daus Donald G.
Kinzig Charles M.
Lentz Edward T.
Venetianer Stephen
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