首页> 外国专利> SUBSTITUTED IMIDAZO1,2A AZINES ASSELECTIVE INHIBITORS OF COX-2

SUBSTITUTED IMIDAZO1,2A AZINES ASSELECTIVE INHIBITORS OF COX-2

机译:取代的咪唑并[1,2A]嗪类COX-2选择性抑制剂

摘要

The present invention relates to new products of formula (I) wherein A and B are selected amongst N and CH, with the condition that when A is N, B is N; R1 is selected amongst CH¿3? and NH2; R?2 and R3¿ are selected amongst H, CH¿3?, Br, Cl, COCH3 and OCH3; R?4, R5 and R6¿, which are similar or different, are selected in the group comprised of H, F, Cl, Br, (C1-C3)-alkyl, trifluoromethyl, (C1-C3)-alkoxyl and trifluoromethoxyl. The products of formula (I) are prepared by condensation between a substituted aminoazine and a substituted 2-bromo-2-(4-R1-sulfonylphenyl)-1-phenyltanone in a polar solvant. These new compounds have an activity which inhibits COX-2, with high selectivity in relation to COX-1. They are useful for the treatment of inflammation and/or diseases mediated by cyclo-oxigenases, with the additional advantage that they have a reduced ulcerogenic potential.
机译:本发明涉及式(Ⅰ)的新产物,其中A和B选自N和CH,条件是当A为N时,B为N; R1是从CH¿3中选择的吗?和NH 2; R 2和R 3选自H,CH 3,Br,Cl,COCH 3和OCH 3;相似或不同的R 4,R 5和R 6选自H,F,Cl,Br,(C 1 -C 3)-烷基,三氟甲基,(C 1 -C 3)-烷氧基和三氟甲氧基。式(I)的产物是通过在极性溶剂中使取代的氨基嗪与取代的2-溴-2-(4-R1-磺酰基苯基)-1-苯基tanone缩合制备的。这些新化合物具有抑制COX-2的活性,相对于COX-1具有高选择性。它们可用于治疗由环氧化酶引起的炎症和/或疾病,其另外的优点是它们具有降低的致溃疡潜力。

著录项

  • 公开/公告号IL141242A

    专利类型

  • 公开/公告日2002-03-10

    原文格式PDF

  • 申请/专利权人 LABORATORIOS S.A.L.V.A.T. S.A.;

    申请/专利号IL141242

  • 发明设计人

    申请日2001-02-01

  • 分类号

  • 国家 IL

  • 入库时间 2022-08-22 00:44:56

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