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    • 3. 发明授权
    • Substituted 1,2-dihydro-4h-3,1-benzoxazin-4-one derivatives inhibitors
of interleukin 1
    • 取代的1,2-二氢-4h-3,1-苯并恶嗪-4-酮衍生物白细胞介素1抑制剂
    • US4894374A
    • 1990-01-16
    • US233186
    • 1988-08-17
    • Jerauld S. SkotnickiAhmed F. Abdel-Magid
    • Jerauld S. SkotnickiAhmed F. Abdel-Magid
    • A61K31/535C07D498/10
    • C07D498/10A61K31/535
    • There are disclosed compounds of the formula: ##STR1## wherein X is CHR, NR.sup.1, 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;R.sup.1 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; andR.sup.2 and R.sup.3 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.
    • 公开了下式的化合物:其中X是CHR,NR1,S或O; 吡啶基,喹喔啉基或喹唑啉基,或取代的苯基,萘基,吡啶基,喹啉基,吡嗪基,嘧啶基,喹喔啉基或喹唑啉基,其中取代基选自卤素,羧基,低级烷氧基羰基, 低级烷基磺酰基,氰基,硝基和三氟甲基; R 1是低级烯基,吡啶基,吡嗪基,嘧啶基,喹喔啉基或喹唑啉基,或取代的苯基,萘基,吡啶基,喹啉基,吡嗪基,嘧啶基,喹喔啉基或喹唑啉基,其中取代基选自卤素,羧基,低级烷氧基羰基,低级烷基磺酰基, ,硝基和三氟甲基; 卤素,低级烷基,低级烯基,低级烷氧基,羟基,氨基,单 - 或二 - 低级烷基氨基,羧基,低级烷氧羰基,硝基或氰基; 由于其抑制白细胞介素1的能力,可用作抗炎剂和治疗涉及酶组织破坏的疾病状态,并且还公开了使用这些化合物治疗免疫炎症,炎症/增殖和酶促的方法 组织破坏条件。