发明名称 Substituted 1,2-dihydro-4h-3,1-benzoxazin-4-one derivatives inhibitors of interleukin 1
摘要 There are disclosed compounds of the formula: <IMAGE> wherein X is CHR, NR1, S or O; R is hydrogen, lower alkenyl, pyridyl, quinolinyl, pyrazinyl, pyrimidinyl, quinoxalinyl or quinazolinyl, or substituted phenyl, naphthyl, pyridyl, quinolinyl, pyrazinyl, pyrimidinyl, quinoxalinyl or quinazolinyl, wherein the substituents are selected from halo, carboxy, lower alkoxycarbonyl, lower alkylsulfonyl, cyano, nitro and trifluoromethyl; R1 is lower alkenyl, pyridyl, pyrazinyl, pyrimidinyl, quinoxalinyl or quinazolinyl, or substituted phenyl, naphthyl, pyridyl, quinolinyl, pyrazinyl, pyrimidinyl, quinoxalinyl or quinazolinyl, wherein the substituents are selected from halo, carboxy, lower alkoxycarbonyl, lower alkylsulfonyl, cyano, nitro and trifluoromethyl; and R2 and R3 are each, independently, hydrogen, halo, lower alkyl, lower alkenyl, lower alkoxy, hydroxy, amino, mono- or diloweralkylamino, carboxy, lower alkoxycarbonyl, nitro or cyano; which, by virtue of their ability to inhibit interleukin 1, are of use as antiinflammatory agents and in treatment of disease states involving enzymatic tissue destruction, and there is also disclosed a method using such compounds in the treatment of immunoinflammatory, inflammatory/proliferative and enzymatic tissue destruction conditions.
申请公布号 US4894374(A) 申请公布日期 1990.01.16
申请号 US19880233186 申请日期 1988.08.17
申请人 AMERICAN HOME PRODUCTS CORPORATION 发明人 SKOTNICKI, JERAULD S.;ABDEL-MAGID, AHMED F.
分类号 A61K31/535;C07D498/10 主分类号 A61K31/535
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