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    Tricyclic derivatives of substituted pyrrole acids as analgesic and anti-inflammatory agents
    1.
    发明公开
    Tricyclic derivatives of substituted pyrrole acids as analgesic and anti-inflammatory agents 失效
    Tricyclische衍生取代器Pyrrolsäurenals analgetische undentzündungshemmendeMittel。

    公开(公告)号：EP0068460A1

    公开(公告)日：1983-01-05

    申请号：EP82105637.1

    申请日：1982-06-25

    申请人： Merck & Co., Inc.

    发明人： Doherty, James B. ,  Dorn, Conrad P. ,  Witzel, Bruce E. ,  Allison, Debra L. ,  Shen, Tsung-Ying ,  Finke, Paul E.

    IPC分类号： C07D491/044 ,  C07D495/04 ,  C07D487/04 ,  C07D209/70 ,  A61K31/55 ,  A61K31/38 ,  A61K31/365 ,  A61K31/385

    CPC分类号： C07D487/04 ,  C07D207/34 ,  C07D209/70 ,  C07D313/08 ,  C07D491/04 ,  C07D495/04

    摘要： Compounds having the structural formula:
    are disclosed wherein
    there are 0-4 R groups and

    R is e.g. hydrogen, lower alkyl, halo-loweralkyl, hydroxy, lower alkoxy, halo, lower alkylthio or lower alkylsulfinyl;
    R 1 is e.g. hydrogen or lower alkyl;


    Z is (a) -(CH 2 ) o-n , n being 0-10;
    (b) -CO(CH 2 ) 1-n -;
    (c) -(CH 2 ) 1-n -CO-; or
    (d)

    R 2 is e.g. hydrogen or lower alkyl;
    R 3 is hydrogen, lower alkyl, hydroxy, loveralkoxy or halo; and
    X-Y is e.g. -O-CH 2 - or -S-CH 2 -.

    Those compounds have been prepared via hydrolysis of a precursor or decarboxylation of a precursor-diacid. These tricyclic compounds are found to have high analgesic and anti-inflammatory activities but low ulcerogenic side effects.

    摘要翻译： 公开了具有结构式：的化合物，其中存在0-4个R基团，并且R为例如。 氢，低级烷基，卤代低级烷基，羟基，低级烷氧基，卤素，低级烷硫基或低级烷基亚磺酰基; R 1是例如。 氢或低级烷基; Z是（a） - （CH 2）0-n，n是0-10; （b）-CO（CH 2）1-n; （c） - （CH 2）1-n -CO-; 或（d） - @@ - （CH 2）0-n; R 2是例如。 氢或低级烷基; R 3是氢，低级烷基，羟基，卤代烷氧基或卤素; 而X-Y是例如。 -O-CH 2 - 或-S-CH 2 - 。 这些化合物是通过前体的水解或前体二酸的脱羧制备的。 发现这些三环化合物具有高的止痛和抗炎活性，但是具有低的溃疡性副作用。

    Process for the preparation of zomepirac and related compounds
    4.
    发明公开
    Process for the preparation of zomepirac and related compounds 失效
    Verfahren zur Herstellung von“Zomepirac”und Derivaten。

    公开(公告)号：EP0067370A2

    公开(公告)日：1982-12-22

    申请号：EP82104852.7

    申请日：1982-06-03

    申请人： Merck & Co., Inc.

    发明人： Doherty, James B. ,  Allison, Debra L.

    IPC分类号： C07D207/337 ,  C07D207/34

    CPC分类号： C07D207/337 ,  C07D207/34

    摘要： Zomepirac and its analogs of the structural formula:
    wherein

    Ar is phenyl or halophenyl;
    R 1 and R 3 independently are H or C 1-6 alkyl and
    R 2 is H, C 1-6 alkyl or halo are prepared from a 5-aroyl-3-hydroxycarbonyl-4-substituted pyrrole-2-acetic acid via acidic decarboxylation.

    摘要翻译： Zomepirac及其类似物的结构式：... 其中Ar是苯基或卤代苯基; R 1和R 3独立地是H或C 1-6烷基，且R 2是H，Cl -6烷基或卤素通过酸性脱羧由5-芳酰基-3-羟基羰基-4-取代的吡咯-2-乙酸制备。

    Benzothiophenes, their production and use, and compositions containing them
    7.
    发明公开
    Benzothiophenes, their production and use, and compositions containing them 失效
    苯并噻吩，我的Herstellung und Verwendung und sie enthaltende Zusammensetzungen。

    公开(公告)号：EP0160408A1

    公开(公告)日：1985-11-06

    申请号：EP85302275.4

    申请日：1985-04-01

    申请人： Merck & Co., Inc.

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

    IPC分类号： C07D333/70 ,  C07D409/12 ,  A61K31/38

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

    摘要： N-Alkenyl-3-hydroxybenzo [b] thiophene-2-carboxamide derivatives of formula)
    and their pharmaceutically acceptable salts, are novel. In the formula, each of R, R 1 , R 2 , R 3 and R 4 is selected from various hydrocarbons (including heteroaryl), acyl, and acyl- substituted hydrocarbon groups and their ring-substituted derivatives; or R 1 , R 2 and R 3 can be halo, or R' and R 2 joined to form certain tricyclic bivalent residues, or R 4 is -CR 1 =CR 2 R 3 , and n is 0, 1, or 2. These compounds are 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 halocetamide, 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 as relatively low dosages for increasing the resistance of gastro-intestinal mucosa to strong irritants. They are included in pharmaceutical compositions.

    摘要翻译： 具有式（Ⅸ）的N-烯基-3-羟基苯并[b]噻吩-2-甲酰胺衍生物及其药学上可接受的盐是新颖的。 在该式中，R 1，R 2，R 2，R 3和R 4各自选自各种烃（包括杂芳基），酰基和酰基取代的烃基及其环取代的 衍生物; 或R 1，R 2和R 3可以是卤素，或R 1和R 2连接形成某些三环二价残基，或R 4是-CR 1 = CR 这些化合物通过以下步骤制备：（1）用硫代乙酰胺处理取代的2-卤代苯甲酸酯，然后用合适的试剂如醛，酮，烯醇处理N-烯基化反应 醚，环氧化物，缩醛或缩酮; （2）用适当取代的卤代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，发烧，炎症，关节炎病症，哮喘，过敏性疾病，皮肤疾病，心血管疾病，牛皮癣，炎性肠病，青光眼等 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，但可以用作相对较低的剂量来增加胃肠粘膜对强刺激物的抵抗力。 它们被包括在药物组合物中。