1-hydroxy-4(3-cyclopentyloxy-4-methoxyphenyl)-2-pyrrolidone and

Details 1-hydroxy-4(3-cyclopentyloxy-4-methoxyphenyl)-2-pyrrolidone and 1-hydroxy-4(3-cyclopentyloxy-4-methoxyphenyl)-2-pyrrolidone and

1992-10-22

1994-10-18

Springer, David B.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

548542, C07D20746, A61K 3140

Patent

active

053569237

ABSTRACT:
##STR1## Substituted cyclic hydroxamic acids of general formula (I) in which R.sub.1, R.sub.2 and R.sub.3 are independently hydrogen, halogen, lower alkyl, lower alkoxy, cycloalkoxy, aryloxy which is optionally substituted by 1 to 3 halogen, or aralkyloxy, which is optionally substituted by 1 to 3 halogen, or R.sub.1 and R.sub.2 together form a --O--CH.sub.2 --O-- group; with the proviso that R.sub.3 is not hydrogen when R.sub.1 and R.sub.2 are both hydrogen; R.sub.4 and R.sub.5 are independently hydrogen or lower alkyl, R.sub.6 is hydrogen or lower alkyl and physiologically acceptable salts and esters thereof are selective inhibitors of phosphodiesterase IV activity and leukotriene B.sub.4 and C.sub.4 synthesis without showing any significant effect on phosphodiesterase III activity, and are therefore useful in the treatment of hypersensitivity and inflammatory diseases.

REFERENCES:
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patent: 4738986 (1988-04-01), Kneen et al.
patent: 4977188 (1990-12-01), Kneen et al.
Michel Cariou et al, J. Electroanal. Chem., "Mechanism of the Electroreduction of Aliphatic Nitro Compounds", vol. 182, 1985, pp. 345-354.
H. Singer et al, Synthesis, "Tetramethylguanidine-Catalyzed Addition of Nitromethane to .alpha., .beta.-Unsaturated Carboxylic Acid Esters", vol. 265, 1971, pp. 44-45.

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