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    2-Substituted quinolines, their preparation and use.
    6.
    发明公开
    2-Substituted quinolines, their preparation and use. 失效
    2-Substituierte Chinoline，ihre Herstellung und Verwendung。

    公开(公告)号：EP0206751A2

    公开(公告)日：1986-12-30

    申请号：EP86304686

    申请日：1986-06-17

    Applicant: MERCK FROSST CANADA INC

    Inventor： YOUNG ROBERT N ,  LEGER SERGE ,  FRENETTE RICHARD ,  ZAMBONI ROBERT ,  WILLIAMS HAYDEN W R

    IPC: A61K31/47 ,  A61P9/00 ,  A61P11/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D215/12 ,  C07D215/14 ,  C07D215/16 ,  C07D215/18 ,  C07D215/36 ,  C07D401/12

    CPC classification number: C07D401/12 ,  C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D215/36

    Abstract: Compounds having the formula: are selective antagonists of leukotrienes of D4. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents and may be made up into pharmaceutical compositions. In the formula R is H, halogen, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, -CF3, -OR , -SR , -NR R , -CHO, -COOR , -(C=0)R , -C(OH)R R , -CN, -NO2, substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, or substituted or unsubstituted phenethyl; R 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; R is -(A)m-(CR =CR )p-(CR R )m-Q; R is H, halogen, -NO2, -CN, -OR , -SR , NR R , or C1-C8 alkyl; R is H or C1-C4 alkyl; R is A) a monocyclic or bicyclic heterocyclic radical containing from 3 to 12 nuclear carbon atoms and 1 or 2 nuclear heteroatoms selected from N and S with at least one being N, and with each ring in the heterocyclic radical being formed of 5 or 6 atoms, or B) the radical W-R ; R contains up to 21 carbon atoms and is (1) a hydrocarbon radical or (2) an acyl radical of an organic acyclic or monocyclic carboxylic acid containing not more than 1 heteroatom in the ring; R is -OR , -SR , or NR R ; R is H, C1-C6 alkyl, -(C=O)R , unsubstituted phenyl or unsubstituted benzyl; R is H, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, -CF3, or unsubstituted phenyl, benzyl, or phenethyl; m is 0-8; n is 1 or 2;

    Abstract translation: 具有下式的化合物：是D4的白三烯的选择性拮抗剂。 这些化合物可用作抗哮喘，抗过敏，抗炎和细胞保护剂，并且可以制成药物组合物。 在式中，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，-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 = CR 2）p - （CR 2 R 2）m -Q; R 4是H，卤素，-NO 2，-CN，-OR 2，-SR 2，NR 2 R 2或C 1 -C 8烷基; R 6是H或C 1 -C 4烷基; R 7是A）含有3至12个核碳原子和1或2个选自N和S的核杂原子，至少一个为N的单环或双环杂环基，杂环基中的每个环由 5或6个原子，或B）基团WR 8; R 8含有最多21个碳原子，并且（1）烃基或（2）环中含有不超过1个杂原子的有机无环或单环羧酸的酰基; R 9是-OR 1，O，R 1，R 2，R 11， R 1是H，C 1 -C 6烷基， - （C = O）R 1，未取代的苯基或未取代的苄基; R 1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; m为0-8; n为1或2;

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