Hoffmann-la Roche Inc.

Brian P Tong

Peter J Machin

Carey Ernest Smithen

Noel A Roberts

John M Osbond

Christopher R Self

Colin H Cashin

Oxazole and isoxazole derivatives of the formula ##STR1## wherein A is C.sub.1-6 -alkylene, Het is a 2-R-oxazol-5-yl, 5-R-oxazol-2-yl, 4-R-oxazol-2-yl, 2-R-oxazol-4-yl, 3-R-isoxazol-5-yl or 5-R-isoxazol-3-yl group which is optionally substituted on the heterocyclic ring by a C.sub.1-6 -alkyl group, R is phenyl or thienyl monosubstituted or disubstituted by halogen, trifluoromethyl or C.sub.1-6 -alkylthio, R.sup.1 and R.sup.2 each is a C.sub.1-6 -alkyl group and R.sup.3 is a hydroxy or C.sub.1-6 -alkoxy group or a group of the formula --NR.sup.4 R.sup.5 in which R.sup.4 and R.sup.5 each is a hydrogen atom or a C.sub.1-6 -alkyl group or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached is a 5-membered or 6-membered saturated heteromonocyclic ring which may contain an oxygen or sulphur atom or an additional nitrogen atom, and pharmaceutically acceptable salts of the compounds of formula I in which R.sup.3 is a hydroxy group with bases, have anti-arthritic activity.

Oxazole and isoxazole derivatives having anti-arthritic activity

Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each individually is hydrogen, or lower alkyl and R.sup.4 is hydroxy, lower alkoxy, aryl-(lower alkoxy), amino, mono(lower alkyl)amino or di(lower alkyl) amino, and pharmaceutically acceptable salts thereof which are useful in the treatment of degenerative joint diseases and of Wilson's disease are described.

Imidazole derivatives for treating joint diseases and Wilson's disease

Growing community of inventors

Harpenden, United Kingdom

Brian P Tong