5-Substituted picolinic acid compounds and their production proc

Details 5-Substituted picolinic acid compounds and their production proc 5-Substituted picolinic acid compounds and their production proc

1998-10-26

2000-03-07

Fan, Jane

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514344, 514354, 514356, 546326, 5462684, 546323, 546286, A61K 3144, C07D40104

Patent

active

060341076

ABSTRACT:
The present invention provides novel 5-substituted picolinic acid compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 and R.sup.2 are independently H, C.sub.2 -C.sub.6 acyl or halo-substituted benzoyl; and R.sup.3 is --C(O)O--C.sub.1 -C.sub.6 alkyl, C(O)OH, CN, CONH.sub.2, CONHCH.sub.3, CON(CH.sub.3).sub.2, 1-methyltetrazole or 2-methyltetrazole, with the proviso that when R.sub.2 is acetyl and R.sup.3 is methoxycarbonyl, R.sup.1 is not H; and that when R.sup.3 is CN, CONH.sub.2, CONHCH.sub.3, CON(CH.sub.3).sub.2, 1-methyltetrazole or 2-methyltetrazole, R.sup.1 and R.sup.2 are H.
The present invention also relates to a pharmaceutical composition comprising compound of the present invention, which is useful in the treatment of IL-1 and TNF mediated diseases or the like.
The present invention further relates to a process for producing the compounds of the formula (I).

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