利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

39 条记录 (耗时 0.034 秒)

    N-alkenyl-3-hydroxybenzo[b]thiophene-2-carboxamide derivatives as dual cyclooxygenase and lipoxygenase inhibitors
    1.
    发明授权
    N-alkenyl-3-hydroxybenzo[b]thiophene-2-carboxamide derivatives as dual cyclooxygenase and lipoxygenase inhibitors 失效
    N-烯基-3-羟基苯并[b]噻吩-2-甲酰胺衍生物作为双重环加氧酶和脂氧合酶抑制剂

    公开(公告)号：US4760086A

    公开(公告)日：1988-07-26

    申请号：US705115

    申请日：1985-02-27

    申请人： Allan N. Tischler ,  Bruce E. Witzel ,  Philippe L. Durette ,  Kathleen M. Rupprecht ,  Timothy F. Gallagher ,  Debra L. Allison ,  Marvin M. Goldenberg

    发明人： Allan N. Tischler ,  Bruce E. Witzel ,  Philippe L. Durette ,  Kathleen M. Rupprecht ,  Timothy F. Gallagher ,  Debra L. Allison ,  Marvin M. Goldenberg

    IPC分类号： C07C63/70 ,  C07D303/04 ,  C07D333/70 ,  C07D409/12 ,  A61K31/38 ,  C07D333/62

    CPC分类号： C07D409/12 ,  A61K9/0048 ,  A61K9/0051 ,  C07C247/00 ,  C07D303/04 ,  C07D333/70

    摘要： N-Alkenyl-3-hydroxybenzo[b]thiophene-2-carboxamide derivatives have been prepared by:(1) treating a substituted 2-halobenzoate with thioacetamide followed by N-alkenylation with appropriate agents, such as aldehydes, ketones, enol ethers, epoxides, acetals or ketals;(2) treating a substituted thiosalicylate with an appropriately substituted haloacetamide, followed by dehydration; 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. 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： N-烯基-3-羟基苯并[b]噻吩-2-甲酰胺衍生物通过以下方法制备：（1）用硫代乙酰胺处理取代的2-卤代苯甲酸，然后用合适的试剂如醛，酮，烯醇醚， 环氧化物，缩醛或缩酮; （2）用适当取代的卤代乙酰胺处理取代的硫代水杨酸酯，然后脱水; 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。 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。

    Derivatives of 3-hydroxyazabenzo[b]thiophene useful as 5-lipoxygenase inhibitors
    4.
    发明授权
    Derivatives of 3-hydroxyazabenzo[b]thiophene useful as 5-lipoxygenase inhibitors 失效
    可用作5-脂氧合酶抑制剂的3-羟基苯并[b]噻吩的衍生物

    公开(公告)号：US4904672A

    公开(公告)日：1990-02-27

    申请号：US187170

    申请日：1988-04-28

    申请人： Robert K. Baker ,  Kathleen M. Rupprecht ,  Arsenio A. Pessolano ,  Philippe L. Durette

    发明人： Robert K. Baker ,  Kathleen M. Rupprecht ,  Arsenio A. Pessolano ,  Philippe L. Durette

    IPC分类号： C07D495/04

    CPC分类号： C07D495/04

    摘要： 3-Hydroxyazabenzo[b]thiophene derivatives having optionally 2-aryl, 2-aralkyl, 2-alkyl or 2-alkenyl substituents were prepared by, among other methods, ring closure of an appropriately substituted benzylthioalkoxycarbonyl-pyridine. These compounds are found to be useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases such as psoriasis and atopic eczema, cardiovascular disorders, inflammatory disease and other leukotriene mediated diseases.

    摘要翻译： 具有任选2-芳基，2-芳烷基，2-烷基或2-烯基取代基的3-羟基氮杂苯并[b]噻吩衍生物通过其它方法闭合适当取代的苄基硫代烷氧基羰基 - 吡啶来制备。 发现这些化合物可用于治疗疼痛，发热，炎症，关节炎病症，哮喘，过敏性疾病，皮肤疾病如牛皮癣和特应性湿疹，心血管疾病，炎性疾病和其他白三烯介导的疾病。

    Derivatives of 3-hydroxyazabenzo(B)thiophene useful as 5-lipoxygenase inhibitors
    6.
    发明授权
    Derivatives of 3-hydroxyazabenzo(B)thiophene useful as 5-lipoxygenase inhibitors 失效
    可用作5-脂氧合酶抑制剂的3-羟基苯并苯并（B）噻吩的衍生物

    公开(公告)号：US4767766A

    公开(公告)日：1988-08-30

    申请号：US8881

    申请日：1987-01-30

    申请人： Robert K. Baker ,  Kathleen M. Rupprecht ,  Arsenio A. Pessolano ,  Philippe L. Durette

    发明人： Robert K. Baker ,  Kathleen M. Rupprecht ,  Arsenio A. Pessolano ,  Philippe L. Durette

    IPC分类号： C07D495/04 ,  A61K31/435

    CPC分类号： C07D495/04

    摘要： 3-Hydroxyazabenzo[b]thiophene derivatives having optionally 2-aryl, 2-aralkyl, 2-alkyl or 2-alkenyl substituents were prepared by, among other methods, ring closure of an appropriately substituted benzylthio-alkoxycarbonyl-pyridine. These compounds are found to be useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases such as psoriasis and atopic eczema, cardiovascular disorders, inflammatory diseases and other leukotriene mediated diseases.

    摘要翻译： 具有任选2-芳基，2-芳烷基，2-烷基或2-烯基取代基的3-羟基氮杂苯并[b]噻吩衍生物通过其它方法闭环合适取代的苄硫基 - 烷氧基羰基 - 吡啶来制备。 发现这些化合物可用于治疗疼痛，发烧，炎症，关节炎病症，哮喘，过敏性疾病，皮肤疾病如牛皮癣和特应性湿疹，心血管疾病，炎性疾病和其他白三烯介导的疾病。