Process for preparing novel thiazolylguanidine compounds and...

C - Chemistry – Metallurgy – 07 – D

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C07D 215/46 (2006.01) C07D 215/42 (2006.01) C07D 401/12 (2006.01)

Patent

CA 1120929

ABSTRACT OF THE DISCLOSURE The compounds, pharmaceutically acceptable non-toxic salts thereof, non toxic metal complexes thereof, and the produces obtained by acylating such compounds with a carboxylic acid are provided herein. The new compounds have the general Formula I: Image I in which R1 represents hydrogen, alkyl, alkoxy, hydroxy, halogen, trifluoro- methyl, or phenyl; R2 represents hydrogen; alkyl, alkoxy, halogen, trifluoro- methyl, or hydroxy; R3 represents C1-C18-alkyl, C3-C8-cycloalkyl which is un- substituted or is mono- or di-substituted whith methyl or ethyl, or phenyl or phenyl-C1-C3-alkyl which is unsubstituted or is substituted with a methyl, methoxy, halo or trifluoromethyl group; and R4 represents a 5- or 6-membered heterocyclic ring containing from one to four ring nitrogen atoms and from 0 to 1 further hetero atoms selected from the group consisting of oxygen and sulphur atoms, the ring system being unsubstituted or substituted with from 1 to 2 members of the group consisting of C1-C3-alkyl, C1-C3-alkoxy, carboxy, carbalkoxy, halogen, trifluoromethyl, hydroxy and mercapto; or the ring system forms part of a larger fused ring system; and pharmaceutically acceptable, non-toxic salts thereof, non-toxic metal compl?s thereof or the products obtained by acylating such compounds with a carboxylic acid. Such compounds can be used in therapy of rheumatoid arthritis, osteo-arthritis, and allied conditions in humans and domestic animals by enteral, parenteral or topical administration.

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