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41 条记录 (耗时 0.021 秒)

    Stereoselective synthesis of leukotriene antagonists
    3.
    发明公开
    Stereoselective synthesis of leukotriene antagonists 失效
    Stereoselektive Synthese von Leukotrienantagonisten。

    公开(公告)号：EP0244164A1

    公开(公告)日：1987-11-04

    申请号：EP87303613.1

    申请日：1987-04-24

    申请人： MERCK FROSST CANADA INC.

    发明人： Frenette, Richard ,  Gauthier, Jacques-Yves ,  Young, Robert N. ,  Zamboni, Robert ,  Kakushima, Masatoshi ,  Verhoeven, Thomas R.

    IPC分类号： C07C149/40 ,  C07C59/68 ,  C07C59/90 ,  C07C51/00 ,  C07D307/32

    CPC分类号： C07D307/33 ,  C07C51/09 ,  C07C59/68

    摘要： The present invention relates to a stereo­selective synthesis of leukotriene antagonists. More particularly, this invention relates to the stereo­selective synthesis of (βS,γR) and (βR,γS)-­4-((3-(4-acetyl-3-hydroxy-2-propyl(phenoxy)propyl)­thio)-γ-hydroxy-β-methylbenzenebutanoic acid, and related compounds. These compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation and pain in mammals, especially humans. The compounds are also useful for inducing cytoprotection in mammals, especially humans.

    摘要翻译： 本发明涉及白三烯拮抗剂的立体选择性合成。 更具体地说，本发明涉及（βS，γR）和（βR，γS）-4 - （（3-（4-乙酰基-3-羟基-2-丙基（苯氧基）丙基）的立体选择性合成） 硫代）-γ-羟基-β-甲基苯丁酸和相关化合物，这些化合物是用于治疗哺乳动物，特别是人类的过敏性疾病，哮喘，心血管疾病，炎症和疼痛的有用治疗剂，该化合物也可用于诱导细胞保护 在哺乳动物，特别是人类。

    2-Substituted quinolines
    4.
    发明公开
    2-Substituted quinolines 失效
    2-取代基喹啉。

    公开(公告)号：EP0219307A2

    公开(公告)日：1987-04-22

    申请号：EP86307779.8

    申请日：1986-10-08

    申请人： MERCK FROSST CANADA INC.

    发明人： Young, Robert N. ,  Zamboni, Robert ,  Leger, Serge

    IPC分类号： C07D215/14 ,  C07D215/18 ,  A61K31/47

    CPC分类号： C07D215/14 ,  C07D215/18

    摘要： Novel compounds have the formula:
    or are pharmaceutically acceptable salts thereof. In the formula,
    Y is -(CR²=CR²) n -or -(C≡C) n -;
    R¹ is H, halogen, C₁-C₈ alkyl, C₂-C₈ alkenyl, C₂-C₈ alkynyl, -CF₃, OR², -SR², -SOR², -SO₂R², -NR²R², -CHO, -COOR², -(C=O)R², -C(OH)R²R², -CN, -NO₂, substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, or substituted or unsubstituted phenethyl;
    R² is H, C₁ -C₈ alkyl, C₂-C₈ alkenyl, C₂-C₈ alkynyl, -CF₃, substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, or substituted or unsubstituted phenethyl;
    R³ is -(A) m -(CR²R²) m -(CR²R⁴) m -CR²R, with the proviso that R³ is not CHO when it is para to Y;
    R⁴ is H, halogen, -NO₂, -OR², -SR², NR²R², or C₁-C₈ alkyl, or (R⁴)₂ is O=;
    A is =C=O or CR²(OR⁶);
    R⁶ is H, C₁-C₆ alkyl, -(C=O)R⁷, unsubstituted phenyl or unsubstituted benzyl;
    R⁷ is H, C₁-C₈ alkyl, C₂-C₈ alkenyl, C₂-C₈ alkynyl, -CF₃, or unsubstituted phenyl, benzyl, or phenethyl;
    each m is 0 or integer of from 1 to 8, provided that at least one m is not 0;
    and n is 1 or 2. The compounds are antagonists of leukotrienes and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.

    摘要翻译： 新型化合物具有下式：或其药学上可接受的盐。 在该式中，Y是 - （CR 2）= CR 2）n - 或 - （C IDENTICAL C）n-; R 1是H，卤素，C 1 -C 8烷基，C 2 -C 8烯基，C 2 -C 8炔基，-CF 3，OR 2，-SR 2，-SOR 2，-SO 2 R 2， -NR 2 R 2，-CHO，-COOR 2， - （C = O）R 2，-C（OH）R 2 R 2，-CN，-NO 2， 取代或未取代的苯基，取代或未取代的苄基或取代或未取代的苯乙基; R 2是H，C 1 -C 8烷基，C 2 -C 8烯基，C 2 -C 8炔基，-CF 3，取代或未取代的苯基，取代或未取代的苄基或取代或未取代的苯乙基; R 3是 - （A）m - （CR 2 R 2）m - （CR 2 R 4）m -R CR 2，条件是R 3， 当它是Y的对数时不是CHO; R 4是H，卤素，-NO 2，-OR 2，-SR 2，NR 2 R 2或C 1 -C 8烷基，或（R 4）2是O = ; A = C = O或CR 2（OR 6）; R 6是H，C 1 -C 6烷基， - （C = O）R 7，未取代的苯基或未取代的苄基; R 7是H，C 1 -C 8烷基，C 2 -C 8烯基，C 2 -C 8炔基，-CF 3或未取代的苯基，苄基或苯乙基; 每个m为0或1至8的整数，条件是至少一个m不为0; 并且n为1或2.化合物为白细胞三烯的拮抗剂和白三烯生物合成的抑制剂。 这些化合物可用作抗哮喘，抗过敏，抗炎和细胞保护剂。

    Conjugates of leukotrienes with proteins
    5.
    发明公开
    Conjugates of leukotrienes with proteins 失效
    枸橼酸钠。

    公开(公告)号：EP0179959A1

    公开(公告)日：1986-05-07

    申请号：EP84307569.8

    申请日：1984-11-02

    申请人： MERCK FROSST CANADA INC. ,  Merck & Co., Inc.

    发明人： Hayes, Edward C. ,  Rokach, Joshua ,  Young, Robert N.

    IPC分类号： C07K15/00 ,  C07K5/02 ,  C07C109/093 ,  A61K37/02 ,  C07C103/173 ,  G01N33/531

    CPC分类号： C07K5/0606 ,  A61K38/00 ,  A61K47/62 ,  A61K47/643 ,  C07C243/00 ,  C07D207/416 ,  C07D207/456 ,  C07D309/30 ,  C07K1/1077 ,  C07K14/00 ,  C07K16/18 ,  C07K17/06 ,  G01N33/531 ,  G01N33/60 ,  G01N33/88

    摘要： Leukotrienes B 4 , C 4 , D 4 and E 4 are conjugated with various proteins, viz. Bovine Serum Albumin, Hemocyanin from Giant Keyhole Limpets, human serum albumin, tetanus antigen, diphtheriae toxoid and CRM 197 using 1,5-difluoro-2,4-dinitrobenzene or 6-N-maleimido(C 2-8 alkanoic acid)-chloride as coupling agent.
    These conjugates are useful as reagents in a newly developed immunoassay for leukotrienes, as well as having potential utility as chemical immunotherapeutic agents in the treatment of various allergic and chronic inflammatory diseases of the skin, lung, and airways, including asthma, allergic rhinitis, rheumatoid arthritis, and skin diseases such as psoriasis and eczema. They may be made into pharmaceutical compositions.
    Certain novel intermediate compounds are also provided.

    摘要翻译： 白三烯B4，C4，D4和E4与各种蛋白质缀合， 使用1,5-二氟-2,4-二硝基苯或6-N-马来酰亚胺（C 2-8链烷酸）氯化物的牛血清白蛋白，来自巨孔锁孔的血蓝蛋白，人血清白蛋白，破伤风抗原，白喉类毒素和CRM 197 偶联剂。 这些缀合物可用作新开发的白三烯免疫测定中的试剂，以及作为化学免疫治疗剂用于治疗皮肤，肺和气道的各种过敏性和慢性炎性疾病，包括哮喘，过敏性鼻炎，类风湿病 关节炎和皮肤疾病如牛皮癣和湿疹。 它们可以制成药物组合物。 还提供某些新的中间体化合物。