申请人:American Home Products Corporation
公开号:US04970316A1
公开(公告)日:1990-11-13
There are disclosed compounds of the formula ##STR1## wherein X is O, S, SO, SO.sub.2 or CR.sup.1 R.sup.2 ; R.sup.1 and R.sup.2 are each independently hydrogen, lower alkyl, carboxyl, lower alkoxy carbonyl, lower cycloalkyl, phenyl, anphthyl, pyridyl, quinolinyl, pyrazinyl, pyridinyl, pyridazinyl, pyrimidinyl, quinoxalinyl, quinazolinyl or any of the foregoing aryl or hetaryl substituents substituted with halo, lower alkyl, lower alkyl carbonyl, benzoyl, COOR.sup.3, OR.sup.3, N(R.sup.3).sub.2, CON(R.sup.3).sub.2, SO.sub.3 R.sup.3, SO.sub.2 N(R.sup.3).sub.2, phenylsulfonyl, lower alkyl sulfonyl, cyano, nitro or trifluoromethyl; R.sup.3 is hydrogen, lower alkyl or phenyl; R.sup.4 is halo, morpholino, 4-methylpiperazino, R.sup.5 NNHR.sup.6, R.sup.5 NCH.sub.2 CH.sub.2 OCH.sub.3, or ##STR2## R.sup.5 is hydrogen or lower alkyl; R.sup.6 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkyl or phenyl; and R.sup.7 and R.sup.8 are each independently, hydrogen, halo, nitro, lower alkoxy, lower alkyl, cyano, trifluoromethyl, phenyl, carboxy or lower alkoxycarbonyl, with the proviso that when R.sup.1 and R.sup.2 are hydrogen or lower alkyl, R.sup.4 is other than halo. and, by virtue of their ability to inhibit interleukin 1, their use as antiinflammatory agents and in treatment of disease states involving enzymatic tissue destruction.
公开了化合物的式子 ##STR1## 其中X是O,S,SO,SO.sub.2或CR.sup.1 R.sup.2; R.sup.1和R.sup.2分别独立地是氢,低烷基,羧基,低烷氧基羰基,低环烷基,苯基,
萘基,
吡啶基,
喹啉基,
吡嗪基,
吡啶嗪基,
嘧啶基,喹噁啉基,
喹唑啉基或任何上述芳基或杂芳基取代的卤素,低烷基,低烷基羰基,苯甲酰基,COOR.sup.3,OR.sup.3,N(R.sup.3).sub.2,CON(R.sup.3).sub.2,SO.sub.3R.sup.3,SO.sub.2N(R.sup.3).sub.2,苯基磺酰基,低烷基磺酰基,
氰基,硝基或三
氟甲基; R.sup.3是氢,低烷基或苯基; R.sup.4是卤素,吗啉基,4-甲基
哌嗪基,R.sup.5 NNHR.sup.6,R.sup.5 NCH.sub.2 CH.sub.2 OCH.sub.3或 ##STR2## R.sup.5是氢或低烷基; R.sup.6是氢,低烷基,低烷酰基,低环烷基或苯基; R.sup.7和R.sup.8各自独立地是氢,卤素,硝基,低烷氧基,低烷基,
氰基,三
氟甲基,苯基,羧基或低烷氧羰基,但当R.sup.1和R.sup.2是氢或低烷基时,R.sup.4除了卤素之外。由于它们能够抑制白细胞介素1,因此可用作抗炎药物和治疗涉及酶组织破坏的疾病状态的药物。