7-oxabicyclo(2.2.1)heptane analogs useful as inhibitors of...

C - Chemistry – Metallurgy – 07 – D

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C07D 493/08 (2006.01) A61K 31/34 (2006.01)

Patent

CA 1296344

QA197 Abstract 7-OXABICYCLO(2.2.1)HEPTANE ANALOGS USEFUL AS INHIBITORS OF 5-LIPOXYGENASE AND CYCLOOXYGENASE A compound of the formula Image wherein R1 is hydrogen, hydroxy, alkoxy or aryloxy; R2 is hydrogen, hydroxy, alkoxy or aryloxy; or wherein R1 and R2 taken together is an aromatic ring; R3 is hydrogen or lower alkyl; R4 is lower alkyl, substituted alkyl, alkenyl or alkynyl; X is CH2, amino, alkylamino, alkanoylamino, oxygen or a single bond; A is CH2?CH?CH or a single bond; and n is an integer from 0 to 9, with the proviso that when A is a single bond, n is an integer from 1 to 9; including all stereoisomers thereof. These new compounds have been found to simultaneously inhibit the arachidonic acid enzymes 5-lipoxygenase and cyclooxygenase and as such are useful, for example, as antiinflammatory agents.

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