Troponyl-oxamic acid derivatives and process therefor

C - Chemistry – Metallurgy – 07 – C

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260/541, 260/479

C07C 62/38 (2006.01) A61K 31/12 (2006.01) A61K 31/135 (2006.01) A61K 31/16 (2006.01) A61K 31/165 (2006.01) A61K 31/18 (2006.01) A61K 31/19 (2006.01) A61K 31/195 (2006.01) A61K 31/215 (2006.01) A61K 31/22 (2006.01) A61K 31/225 (2006.01) A61K 31/325 (2006.01)

Patent

CA 1116629

Abstract of the Disclosure Tropone derivatives represented by formula I Image (I) in which R1 and R4 are the same or different selected from the group consisting of hydrogen, halo, trifluoromethyl, tower alkoxy, lower alkyl, phenyl, hydroxy, phenoxy, mercapto, (2-carboxyphenyl)thio, NR7R8 wherein R7 and R8 each is hydrogen or lower alkyl or R7 is alkyl and R8 is p-toluenesulfonyl, and a radical of formula NR9COR10 wherein R9 is hydrogen or lower alkyl and R10 is carboxy, lower alkoxycarbonyl, hydrazinocarbonyl or a radical of formula COO(CH2)nCOR17 wherein n is an integer from one to six and R17 is hydroxy or lower alkoxy; and R2, R3, R5 and R6 are the same or different selected from the group consisting of hydrogen, halo, trifluoromethyl, lower alkoxy, lower alkyl, phenyl, hydroxy, phenoxy, mercapto, (2-carboxyphenyl)thio, and NR7R8 wherein R7 and R8 each is hydrogen or lower alkylor R7 is lower alkyl and R8 is p-toluenesulfonyl; with the proviso that at least one of R1 and R4 must be a radical of formula NR9COR10 wherein R9 and R10 are as defined herein; or a therapeutically acceptable salt thereof; are useful for preventing or treating allergic conditions in a mammal. Methods for the preparation and use of said compounds are disclosed. -1-

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