Thiazolderivat und Verfahren zu dessen Herstellung

摘要

1,192,701. Anti-inflammatory &c. medicines. IMPERIAL CHEMICAL INDUSTRIES Ltd. 10 Feb., 1969 [22 March, 1968], No. 13989/68. Heading A5B. '[Also in Division C2] Pharmaceutical compositions having antiinflammatory, analgesic and anti-pyretic activity comprise, as active ingredient, at least one α-thiazolyl-malonic acid derivative of the general formula wherein Y or Z is linked to the 2-position of the thiazole nucleus, X is a hydrogen atom or a C 1-3 alkyl group, Y is a phenyl group optionally substituted by 'up to two halogen atoms selected from fluorine, chlorine or bromine, and Z is a group of the formula wherein R1 is a hydrogen or alkali metal atom, a C 1-3 alkyl group, a dialkylaminomethyl group of up to 5 carbon atoms, a piperidinomethyl or morpholinomethyl group, or a chlorine or bromine atom, and R2 and R3 are each a hydrogen atom or a C 1-3 alkyl group, provided that, when R2 and R3 are each a hydrogen atom, R1 is a hydrogen atom or a C 1-3 alkyl group, a tautomer thereof or a non-toxic, pharmaceutically-acceptable salt thereof, togothler with a non-toxic, pharmaceuticallyacceptable diluent or carrier. The compositions may be administered orally, parenterally, topically or rectally in the form of tablets, pills, capsules, suppositories, non-sterile aqueous or non-aqueous solutions or suspensions, sterile injectable aqueous or non-aqueous solutions or suspensions, creams, lotions or ointments. The compositions may additionally contain at least one known anti-inflammatory or analgesic agent, e.g. aspirin, paracetamol, codeine, chloroquine, phenylbutazone, oxyphenbutazone, indomethacin, mefenamic acid, flufenamic acid or ibufenac, or an anti-inflammatory . steroid, such as prednisolone. Compositions intended for oral administration may additionally contain an anti-cholinergic agent, e.g. homatropine methyl bromide, and/or an antacid, e.g. aluminium hydroxide, or a uricosuric agent, e.g. probenecid. Compositions suitable for topical application may additionally contain a vasodilating agent, eg. tolazoline, or a vasoconstricting agent, e.g. adrenaline; a local anaesthetic, e.g. amethocaine, a counter-irritant, e.g. capsicum, and/or at least one agent chosen from 'antibacterial agents, such as sulphonamides and antibiotics having antibacterial action, e.g. neomycin; anti-fungal agents, e.g. hydroxyquinoline; .antihistaminic agents, e.g. promethazine, and rubefacient agents, e.g. methyl nicotinate.