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    Use of leukotriene antagonists for producing cytoprotective pharmaceutical compositions and process for producing cytoprotective pharmaceutical compositions
    3.
    发明公开
    Use of leukotriene antagonists for producing cytoprotective pharmaceutical compositions and process for producing cytoprotective pharmaceutical compositions 失效
    用于生产CYPOPROTECTIVE PHARMACEUTICAL组合物的白蛋白拮抗剂的使用和生产CYPOPROTECTIVE PHARMACEUTICAL COMPOSITIONS的方法

    公开(公告)号：EP0156233A3

    公开(公告)日：1986-02-19

    申请号：EP85102787

    申请日：1985-03-12

    申请人： MERCK & CO. INC.

    发明人： Goldenberg, Marvin M.

    IPC分类号： A61K31/35

    CPC分类号： A61K31/40 ,  A61K31/12 ,  A61K31/165 ,  A61K31/19 ,  A61K31/215 ,  A61K31/275 ,  A61K31/335 ,  A61K31/35 ,  A61K31/365 ,  A61K31/41 ,  A61K31/415

    摘要： Leukotriene antagonists have been found to be useful for inducing cytoprotection via an unspecified mechanism. Specific therapeutic utilities include, erosive gastritis, erosive esophagitis, inflammatory bowel disease, and induced hemorrhagic gastric erosions such as those caused by indomethacin or ethanol. The leukotriene antagonists are used to produce cytoprotective pharmaceutical compositions. In a process for producing cytoprotective pharmaceutical compositions the leukotriene antagonists are incorporated into a corresponding composition in a cytoprotective effective amount.

    摘要翻译： 已经发现白细胞三烯拮抗剂可用于通过未指定的机制诱导细胞保护作用。 具体的治疗用途包括侵蚀性胃炎，侵蚀性食管炎，炎症性肠病和诱导的出血性胃糜烂，例如由吲哚美辛或乙醇引起的。 白细胞三烯拮抗剂用于制备细胞保护性药物组合物。 在制备细胞保护性药物组合物的方法中，将白三烯拮抗剂以细胞保护有效量掺入相应的组合物中。

    Benzothiophenes, their production and use, and compositions containing them
    5.
    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。

    Use of lipoxygenase inhibitors for the preparations of cytoprotective pharmaceutical compostions and process for the preparation of a cytoprotective pharmaceutical composition
    7.
    发明公开
    Use of lipoxygenase inhibitors for the preparations of cytoprotective pharmaceutical compostions and process for the preparation of a cytoprotective pharmaceutical composition 失效
    对于cytoschützenden药物制剂和用于制备药物制剂的方法cytoschützenden的制备中使用脂氧合酶抑制剂。

    公开(公告)号：EP0155623A2

    公开(公告)日：1985-09-25

    申请号：EP85102786.2

    申请日：1985-03-12

    申请人： Merck & Co., Inc.

    发明人： Goldenberg, Marvin M.

    IPC分类号： A61K31/535 ,  A61K31/54 ,  A61K31/495

    CPC分类号： C07D279/36 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54 ,  C07C46/06 ,  C07D279/20 ,  C07D279/32 ,  C07D279/34 ,  C07C50/28

    摘要： Lipoxygenase inhibitors are used as cytoprotective active ingredient in producing cytoprotective pharmaceutical compositions. Corresponding cytoprotective pharmaceutical compositions are prepared by incorporating into a pharmaceutical composition a lipoxygenase inhibitor in a cytoprotective active amount. The prepared cytoprotective therapeutic composition may be used to treat or prevent disease states such as erosive gastritis, erosive esophagitis, inflammatory bowel disease, and induced hemorrhagic gastric erosions such as those caused by indomethacin or ethanol. The lipoxygenase inhibitors induce cytoprotection via an unspecified mechanism.

    摘要翻译： 制备方法中。 的细胞保护药物compsn。，脂氧合酶抑制剂（I）被使用。 把选项。 （I）是式（Ia）的。 （X = O，S或NR在1或3 posn处; R = H，1-6C烷基，CN或pH; Y = O，硒，S，SO，SO 2或NR; THR虚线darstellt到选择。 在1和2或2和3之间posn处双键; R1，R2，R3和R4 = H，1-6C烷基，2-6C烯基，（CH 2）nM或任何2可以被连接以形成5-6C 环选择unsatd; N = 0-6; ... M = OR 5，卤素，CF 3，SR 5，选择substd PH，COOR 6，COR14，四唑，NHCOR7，NR8R9，NHSO2R10，COCH 2 OH，SOR11，CONR8R9，SO2NR8R9，SO2R3， NO2，OCOR14，OCONR8R9，OCOOR，CN或NR15R16; R5 = H，低级烷氧基 - 低级烷基，低级酰氧基 - 低级烷基，1-6C烷基苄基或选择substd Ph值; .. pH值substit-这里和R1-R4。 是1-3C烷基，卤素，CN，CF 3，COOR 6，CH2COOR6，（CH2）1-3C mR8R9烷氧基，OH，卤代C 1-6烷基，（CH 2）pCOOR6，CN，甲酰基，全氟烷基或CH2R12; m = 0的 -2; p = 0-6; R 6 = H，1-6C烷基或pH; R12 = 1-5C烷基中，Ph或二甲氨基; R 14 = H，（CH 2）qCOOR6; 1-6C烷基，CF 3或PH选择。 。substd作为R5，q = 0-4; R7 = 1-6C烷基，苄基或Ph值; R8，R9 = H中，Ph选择substd作为R5，1-4C-烷.. 基，1-4C-烷基氨基烷基，或者可以通过N连接形成5-8元杂环烷基; R10 = OH，1-6C烷基，1-6C烷氧基，pH或CF 3; R11 = 1-6C烷基中，Ph选择。 substd。 作为R5，（CH2）5COOR6，CN，甲酰基或全氟1-4C烷基; S = 1-6; R13 = OH，H，1-6C烷基中，Ph选择。 substd。 作为R5; （CH2）5COOR6，CN或全氟1-4C烷基; R15，R16被检查确实NHR15R16是一种必需氨基酸; Ť= H卤素-CF 3的。

    Use of leukotriene antagonists for producing cytoprotective pharmaceutical compositions and process for producing cytoprotective pharmaceutical compositions
    9.
    发明公开
    Use of leukotriene antagonists for producing cytoprotective pharmaceutical compositions and process for producing cytoprotective pharmaceutical compositions 失效
    用于生产细胞保护的药物组合物和用于生产的细胞保护的药物组合物的方法的使用白三烯拮抗剂的。

    公开(公告)号：EP0156233A2

    公开(公告)日：1985-10-02

    申请号：EP85102787.0

    申请日：1985-03-12

    申请人： Merck & Co., Inc.

    发明人： Goldenberg, Marvin M.

    IPC分类号： A61K31/35

    CPC分类号： A61K31/40 ,  A61K31/12 ,  A61K31/165 ,  A61K31/19 ,  A61K31/215 ,  A61K31/275 ,  A61K31/335 ,  A61K31/35 ,  A61K31/365 ,  A61K31/41 ,  A61K31/415

    摘要： Leukotriene antagonists have been found to be useful for inducing cytoprotection via an unspecified mechanism. Specific therapeutic utilities include, erosive gastritis, erosive esophagitis, inflammatory bowel disease, and induced hemorrhagic gastric erosions such as those caused by indomethacin or ethanol.
    The leukotriene antagonists are used to produce cytoprotective pharmaceutical compositions. In a process for producing cytoprotective pharmaceutical compositions the leukotriene antagonists are incorporated into a corresponding composition in a cytoprotective effective amount.

    摘要翻译： 白三烯拮抗剂已经被发现是通过在未指定的机制诱导细胞保护有用。 特定治疗应用包括，糜烂性胃炎，腐蚀性食管炎，炎性肠病，和引起的出血胃黏膜糜烂：例如那些由吲哚美辛或乙醇引起的。 的白三烯拮抗剂被用来产生细胞保护性药物组合物。 在用于生产细胞保护的药物组合物的方法的白三烯拮抗剂结合到相应的组合物在细胞保护有效量。