135810-05-8Relevant articles and documents
Dibenzoxepinone hydroxylamines and hydroxamic acids: Dual inhibitors of cyclooxygenase and 5-lipoxygenase with potent topical antiinflammatory activity
Hamer, R. Richard L.,Tegeler, John J.,Kurtz, Ellen S.,Allen, Richard C.,Bailey, Steven C.,Elliott, Mary Ellen,Hellyer, Luther,Helsley, Grover C.,Przekop, Penelope,Freed, Brian S.,White, John,Martin, Lawrence L.
, p. 246 - 252 (1996)
Hydroxylamine and hydroxamic acid derivatives of a known nonsteroidal antiinflammatory dibenzoxepine series display both cyclooxygenase (CO) and 5- lipoxygenase (5-LO) inhibitory properties. Many of these new dual CO/5-LO inhibitors also exhibit potent topical antiinflammatory activity in the arachidonic acid-induced murine ear edema model. On the basis of their promising profile of in vitro and in vivo activities, hydroxamic acids 24h, 3-(6,11-dihydro-11-oxodibenz[b,e]oxepin-2-yl)-N-hydroxy-N-methylpropanamide (HP 977), and 25, 3-(6,11-dihydrodibenz[b,e]oxepin-2-yl)-N-hydroxy-N- methylpropanamide (P10294), were selected as developmental candidates for the topical treatment of inflammatory skin disorders.
N-hydroxy-dibenz ?b,e!oxepinalkylamines, N-hydroxy-dibenz ?b,e!oxepinalkanoic acid amides and related heterocyclic analogues
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, (2008/06/13)
This invention relates to N-hydroxy-dibenz?b,e!oxepinalkylamines, N-hydroxy-dibenz?b,e!oxepinalkanoic acid amides and related heterocyclic analogues of the formula STR1 where X together with the carbon atoms to which it is attached forms a benzene or thiophene ring; W and Z are independently hydrogen, halogen, loweralkyl, or trifluoromethyl; R1 is hydrogen, arylloweralkyl, loweralkoxycarbonyl, loweralkylcarbonyl, arylcarbonyl or arylloweralkylcarbonyl; R2 is loweralkyl, cycloalkyl, arylloweralkyl, loweralkoxycarbonyl, loweralkylcarbonyl, arylcarbonyl or arylloweralkylcarbonyl; m is 0 or 1 and n is an integer of 0 to 4 or the pharmaceutically acceptable salts thereof. The compounds of this invention are useful as analgesics and topical antiinflammatory agents for the treatment of various dermatoses and agents for the treatment of conditions where accumulation of cyclooxygenase and/or lipoxygenase metabolites is a causative factor.