| 摘要 |
<p>72222-138 This invention relates to certain benzoxazolinones which inhibit lipoxygenase and/or cyclooxygenase enzymes. Such compounds are useful in inhibiting such enzymes, per se, and are useful in treating allergic and inflammatory conditions in a mammal. This invention also relates to methods of inhibiting lipoxygenase and/or cyclooxygenase in a mammal with such benzoxazolinones; methods of treating an allergic condition in a mammal with such compounds; methods of treating an inflammatory condition in a mammal with such compounds; and pharmaceutical compositions comprising the benzoxazolinones hereof. The benzoxazolinones have the formula: (I) wherein Alk is a Cn straight or branched chain divalent alkyl group; n is 0, 1, 2, 3, 4, or 5; R1 is (C1-C3)alkyl, (C1-C3)alkoxy, (C1-C3)alkylthio, hydrogen, halo, phenoxy, phenylthio or trifluoromethyl; and R is selected from the group consisting of: (a) wherein R2 and R3 are each, independently, H, (C1-C4)alkyl, (C1-C4)-alkoxy, (C1-C4)alkylthio or halo, X is methylene which is unsub72222-138 stituted or substituted with one methyl group, nitrogen which is unsubstituted or substituted with a protecting group, oxygen, sulfur, sulfoxide or sulfone, and the dotted line between the 2- and 4-positions represents an optional bond between positions 2 and 3 or positions 3 and 4; (b) , or wherein A and B are each, independently, O or S; (c) , , , , or , (d) , , , , , , or wherein R4 and R5 are each, independently, H or (C1-C4)alkyl, p is 0, 1 or 2 and t is 0, 1 or 2 provided that the sum of p plus t equals 1 or 2; and the wavy line indicates that the moiety 72222-138 containing such wavy line can be endo- or exo-7-oxabicyclo¢2,2,1!-heptan-1-yl; and (e) CH3-(CH2)m-Y-wherein m is an integer from l to 3 and Y is oxygen, sulfur, sulfoxide or sulfone.</p> |
