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    5-methylthio-3-hydroxybenzo [b]thiophene-2-carboxamide derivatives as cyclooxygenase and lipoxygenase inhibitors
    1.
    发明授权
    5-methylthio-3-hydroxybenzo [b]thiophene-2-carboxamide derivatives as cyclooxygenase and lipoxygenase inhibitors 失效
    5-甲硫基-3-羟基苯并[b]噻吩-2-甲酰胺衍生物作为环加氧酶和脂氧合酶抑制剂

    公开(公告)号：US4800211A

    公开(公告)日：1989-01-24

    申请号：US897576

    申请日：1986-08-18

    申请人： Allan N. Tischler ,  Philippe L. Durette ,  Bruce E. Witzel ,  Thomas J. Lanza, Jr.

    发明人： Allan N. Tischler ,  Philippe L. Durette ,  Bruce E. Witzel ,  Thomas J. Lanza, Jr.

    IPC分类号： C07D333/70 ,  A61K31/38

    CPC分类号： C07D333/70

    摘要： 3-Hydroxybenzo[b]thiophene-2-carboxamide derivatives have been prepared by:(1) treating a substituted 2-halobenzoate with a thioacetamide.(2) treating a substituted thiosalicylate with an appropriately substituted haloacetamide; and(3) further synthetic modification of compounds prepared above.These compounds have been found to be effective inhibitors of both cyclooxygenase and lipoxygenase and thereby useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases, cardiovascular disorders, psoriasis, inflammatory bowel disease, glaucoma or other prostaglandins and/or leukotriene mediated diseases.

    摘要翻译： 通过以下方法制备了3-羟基苯并[b]噻吩-2-甲酰胺衍生物：（1）用硫代乙酰胺处理取代的2-卤代苯甲酸酯。 （2）用适当取代的卤代乙酰胺处理取代的硫代水杨酸酯; 和（3）进一步合成上述制备的化合物。 已经发现这些化合物是环加氧酶和脂氧合酶的有效抑制剂，从而可用于治疗疼痛，发热，炎症，关节炎状况，哮喘，过敏性疾病，皮肤疾病，心血管疾病，牛皮癣，炎性肠病，青光眼或其他 前列腺素和/或白三烯介导的疾病。

    3-hydroxybenzo[b]thiophene-2-sulfide derivatives compositions, and method of use therefor
    6.
    发明授权
    3-hydroxybenzo[b]thiophene-2-sulfide derivatives compositions, and method of use therefor 失效
    3-羟基苯并[b]噻吩-2-硫化物衍生物组合物及其用途

    公开(公告)号：US4621091A

    公开(公告)日：1986-11-04

    申请号：US658859

    申请日：1984-10-09

    申请人： Allan N. Tischler ,  Thomas J. Lanza, Jr.

    发明人： Allan N. Tischler ,  Thomas J. Lanza, Jr.

    IPC分类号： C07D521/00 ,  A61K31/38 ,  A61K31/381 ,  A61P1/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D333/64 ,  C07D333/66 ,  C07D333/68 ,  A61K31/34 ,  C07D401/12

    CPC分类号： C07D333/64 ,  C07C323/00

    摘要： 3-hydroxybenzo[b]thiophene-2-sulfide derivatives have been prepared by ring closure of an appropriately substituted 2--R.sup.1 SCH.sub.2 S-- benzoic acid ester in the presence of a strong base. These compounds have been found to be specific inhibitors of 5-lipoxygenase and thereby useful in the treatment of inflammation, pain and fever associated with inflammation, arthritic conditions, asthma, allergic disorders such as allergic rhinitis and chronic bronchitis, skin diseases like psoriasis and atopic exzema, cardiovascular or vascular disorders, and other leukotriene mediated diseases. Furthermore, these compounds have been found to exhibit cytoprotective activity which does not involve the inhibition of gastric acid secretion but can be used at relatively low dosages for increasing the resistance of gastro-intestinal mucosa to strong irritants.

    摘要翻译： 3-羟基苯并[b]噻吩-2-硫化物衍生物已经通过在强碱存在下闭合适当取代的2-R 1 CH 2 S-苯甲酸酯来制备。 已经发现这些化合物是5-脂氧合酶的特异性抑制剂，从而可用于治疗与炎症，关节炎状况，哮喘，过敏性鼻炎和慢性支气管炎等过敏性疾病，牛皮癣和特应性皮肤病有关的炎症，疼痛和发热 心血管或血管疾病，以及其他白细胞三烯介导的疾病。 此外，已经发现这些化合物具有不涉及抑制胃酸分泌的细胞保护活性，但可以以相对低的剂量使用以增加胃肠粘膜对强烈刺激物的抵抗力。