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    • 80. 发明授权
    • Substituted 4,6-di-tertiary-butyl 5-hydroxy-pyrimidines
    • 取代的4,6-二叔丁基5-羟基嘧啶
    • US5356898A
    • 1994-10-18
    • US84188
    • 1993-07-01
    • Thomas R. BelliottiCatherine R. KostlanDavid T. Connor
    • Thomas R. BelliottiCatherine R. KostlanDavid T. Connor
    • A61K31/505A61K31/506A61P1/04A61P9/00A61P9/10A61P11/00A61P29/00A61P43/00C07D239/34C07D239/36C07D401/06C07D413/04C07D413/06C07D417/04C07D417/06C07D239/02
    • C07D239/36C07D239/34C07D413/04C07D413/06C07D417/04C07D417/06Y02P20/55
    • The present invention is novel compounds which are 4,6-di-tertiary-butyl-5-hydroxy-1,3-pyrimidine substituted 1,2,4- and 1,3,4-thiadiazoles and oxadiazoles, and 1,2,4-triazoles, and pharmaceutically acceptable additions and base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are now found to have activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever, and particularly rheumatoid arthritis, osteoarthritis, other inflammatory conditions, psoriasis, allergic diseases, asthma, inflammatory bowel disease, GI ulcers, cardiovascular conditions, including ischemic heart disease and atherosclerosis, and ischemia-induced cell damage, particularly brain damage caused by stroke. They can also be used topically for treating acne, sunburn, psoriasis, and eczema. Also included are leukotriene mediated pulmonary, gastrointestinal, inflammatory, dermatological, and cardiovascular conditions. The disclosed compounds also have potential utility as antioxidants. The preferred use is in treating inflammatory conditions. Thus, the present invention is also a pharmaceutical composition or method of manufacturing a pharmaceutical composition for the use of treating the noted conditions.
    • PCT No.PCT / US92 / 00442 Sec。 371日期:1993年7月1日 102(e)日期1993年7月1日PCT提交1992年1月17日PCT公布。 出版物WO92 / 本发明是4,6-二叔丁基-5-羟基-1,3-嘧啶取代的1,2,4-和1,3,4-噻二唑的新化合物,以及 恶二唑和1,2,4-三唑及其药学上可接受的添加剂和碱盐,药物组合物及其使用方法。 现在发现本发明化合物具有作为5-脂氧合酶和/或环加氧酶的抑制剂的活性,其提供有利地受到包括炎症,关节炎,疼痛,发烧,特别是类风湿性关节炎,骨关节炎,其它炎性病症,牛皮癣, 过敏性疾病,哮喘,炎症性肠病,GI溃疡,心血管疾病,包括缺血性心脏病和动脉粥样硬化,以及缺血诱导的细胞损伤,特别是脑卒中引起的脑损伤。 它们也可以局部用于治疗痤疮,晒伤,牛皮癣和湿疹。 还包括白三烯介导的肺,胃肠道,炎症,皮肤病学和心血管疾病。 所公开的化合物还具有作为抗氧化剂的潜在用途。 优选的用途是治疗炎性病症。 因此,本发明也是制备用于治疗所述病症的药物组合物的药物组合物或方法。