Patent · US Expired

Arylalkylether and arylalkylthioether inhibitors of lipoxygenase enzyme activity

US5183818A · kind A · utility

17Cited by
2References
7Claims
0Family size

Assignee

Inventors

Key dates

Filing dateAug 27, 1991
Grant dateFeb 2, 1993
Priority date
Expiry dateAug 27, 2011

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D495/04
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

The present invention provides compounds having the structure EQU Y-Het-[Q.sub.1 ]-X-[Q.sub.2 ]-Z which inhibit the catalytic action of lipoxygenase enzymes, particularly 5-lipoxygenase, and thereby reduce the biosynthesis of leukotrienes B.sub.4, C.sub.4, D.sub.4, and E.sub.4. In the generic formula given above, X is oxygen or sulfur and Het is a heteroaryl group selected from the group consisting of furyl, thienyl, 2-, 3-, and 4-pyridyl, 2- and 3-benzo[b]furyl, 2- and 3-benzo[b]thienyl and thienothienyl. Y is one or two substituents independently selected from hydrogen, hydroxy, halogen, cyano, alkyl, haloalkyl, alkoxy, alkylthio, alkoxyaryl), alkylthioaryl, arylalkoxy, arylalkylthio, aryloxy, arylthio, alkylamido, cycloalkyl, alkanoyl, alkoxycarbonyl, amino, alkylamino, dialkylamino, and the following groups wherein R, at each occurrence, is independently selected from hydrogen and alkyl of from one to six carbon atoms: --CRROR, --NRC(O)R, --NRC(O)OR, and --C(O)NRR. The group Q.sub.1 is absent or is divalent alkylene of from one to six carbon atoms, and Q.sub.2 is divalent alkylene from from two to ten carbon atoms. The group Z is N(OR.sub.1)COR.sub.2 where R.sub.1 is selected f…

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.