4-(isoxazolyl)-thiazole-2- oxamic acids and derivatives thereof

C - Chemistry – Metallurgy – 07 – D

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C07D 413/04 (2006.01) A61K 31/425 (2006.01) C07D 261/08 (2006.01) C07D 261/10 (2006.01) C07D 261/12 (2006.01) C07D 261/18 (2006.01) C07D 417/04 (2006.01)

Patent

CA 1246583

ABSTRACT OF THE DISCLOSURE This invention discloses novel 4- (isoxazolyl)-thiazole-2-oxamic acids and derivatives thereof, of the general formula (I): Image (I) wherein Z is a group of the formula: Image in which R and R1, which may be the same or different, are a hydrogen atom, or a halogen atom, a hydroxy group, a C1-3 alkoxy carbonyl group, a C1-3 alkyl group optionally substituted by hydroxy, C1-3 alkoxy or alkoxy (C1-3)oxalyloxy, a C1-3 alkoxy groups optionally substituted by phenyl, or a phenyl group optionally substituted by halogen; and R2 is a hydroxy group or OR3 wherein R3 is a C3-6 cycloalkyl group or a C1-3 alkyl group optionally substituted by phenyl or C1-3 alkoxy; and R4 is a hydrogen atom or a C1-3 alkyl group; and when R2 is a hydroxy group, their pharmaceutically acceptable salts with organic and inorganic bases. These compounds exhibit improved anti-allergic and anti-anaphylactic activity and are useful in the production of such pharmaceutical products.

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