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41 条记录 (耗时 0.02 秒)

    Leukotriene antagonists
    23.
    发明公开
    Leukotriene antagonists 失效
    白三烯，Antagonisten。

    公开(公告)号：EP0140684A2

    公开(公告)日：1985-05-08

    申请号：EP84307390.9

    申请日：1984-10-26

    申请人： MERCK FROSST CANADA INC.

    发明人： Frenette, Richard ,  Rokach, Joshua ,  Young, Robert N. ,  Kakushima, Masatoshi

    IPC分类号： C07C69/738 ,  C07C59/90 ,  C07D307/93 ,  C07C321/28 ,  C07C381/10 ,  C07C317/00 ,  A61K31/34 ,  A61K31/35 ,  A61K31/215

    CPC分类号： C07D307/93 ,  C07C59/90 ,  C07C317/00 ,  C07C323/00

    摘要： Compounds having the formula:
    and their salts, including acid-addition salts, are novel. These compounds are antagonists of leukotrienes of C 4 , D 4 and E 4 , the slow reacting substance of anaphylaxis. The compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents and are made into suitable pharmaceutical compositions.

    In the formula, each R, independently of the other(s), is H, OH or OR 2 , or C(R) 2 represents C=C(R 4 ) 2 ;
    R 1 is H, OH, acyl, formyl, R 5 CO; or R 5 OCO; each of R 2 and R 3 , independently of the others, is H, OH,
    C 1-6 alkyl, C 2-6 alkenyl, trifluoromethyl, C 1-6 alkoxy, SH, C 1-6 thioalkyl, phenyl, phenyl having C 1-3 alkyl halogen substitution, benzyl, phenethyl, halogen, amino, N(R 4 ) 2 , COOR 4 , CH 2 0R 4 , formyl, CN, trifluoromethylthio or nitro;
    .each of X 1 and X 2 , independently of the other, is oxygen, sulfur, sulfoxide, sulfone, -SO=NR 5 , NR e , N-CO-R 7 , N-CN or NCONHR 6 ;
    each of R 4 and R 6 , independently of the other(s), is H or C 1-6 alkyl;
    each R 5 is C 1-6 alkyl; each R 7 , independently of the other, if any, is C 1-6 alkyl or C 1-6 alkoxy;
    W is H or C 1-6 alkyl or is combined with Y to form an unsaturated bond;
    Z is H, OH or C 1-6 alkoxy, or is combined with Y to form an oxo residue;
    Y, of not combined with Z or W, is hydrogen;
    A is -[C(R 4 ) 2]s- R 8 where S is 0,1, 2, or 3 and R 8 isCOOR 4 , CH 2 0H, CHO, tetrazolyl, NHSO 2 R 9 , CONHSO 2 R 9 , hydroxymethylketone, CN, CON(R 7 ) 2 , a monocyclic heterocyclic ring containing an acidic hydroxyl group, or
    where each s, independently, of the others, is 0, 1, 2 or 3 and R 10 is (A) a monocyclic or bicyclic radical containing from 3 to 12 nuclear carbon atoms and, as nuclear heteroatoms, two Ns or one N and one S, and with each ring in the heterocyclic radical being formed of 5 or 6 atoms, or (B) the radical X'-R 11 where X' is O, S or NH and R 11 contains up to 21 carbon atoms and is a hydrocarbon radical or an acryl radical of an organic acyclic or monocyclic carboxylic acid containing not more than 1 heteroatom in the ring;
    each n, independently of the others, is 0,1, or 3;
    R 9 is OH, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 perfluoroalkyl, phenyl, or phenyl having one or more R 2 substituents.

    摘要翻译： 具有下式的化合物：及其盐，包括酸加成盐，是新颖的。 这些化合物是C4，D4和E4的白细胞三烯的拮抗剂，过敏反应的缓慢反应物质。 该化合物可用作抗哮喘，抗过敏，抗炎和细胞保护剂，并制成合适的药物组合物。 在该式中，每个R独立地为H，OH或OR 2，或者C（R）2表示C = C（R 4）2; R1是H，OH，酰基，甲酰基，R5CO; 或R5OCO; R 2和R 3各自独立地为H，OH，C 1-6烷基，C 2-6烯基，三氟甲基，C 1-6烷氧基，SH，C 1-6硫代烷基，苯基，具有C 1-3烷基卤素取代基的苯基 ，苄基，苯乙基，卤素，氨基，N（R4）2，COOR4，CH2OR4，甲酰基，CN，三氟甲硫基或硝基; X1和X2分别独立地为氧，硫，亚砜，砜，-SO = NR5，NR6，N-CO-R7，N-CN或NCONHR6; R 4和R 6各自独立地为H或C 1-6烷基; 每个R 5是C 1-6烷基; 每个R 7，独立于另一个，如果有的话是C 1-6烷基或C 1-6烷氧基; W是H或C 1-6烷基或与Y结合形成不饱和键; Z是H，OH或C 1-6烷氧基，或与Y结合形成氧代残基; Y不与Z或W组合，是氢; A是 - [C（R4）2] s-R8，其中S是0,1,2或3，R8是COOR4，CH2OH，CHO，四唑基，NHSO2R9，CONHSO2R9，羟甲基酮，CN，CON（R7）2， 含有酸性羟基的单环杂环，或，其中各自独立地为0,1,2或3，R 10为（A）含有3至12个核碳原子的单环或双环基团 和作为核杂原子的两个N或一个N和一个S，杂环基中的每个环由5或6个原子形成，或（B）基团X min -R11，其中X min为O，S或NH 并且R 11含有至多21个碳原子，并且是在环中含有不超过1个杂原子的烃基或丙烯基或有机非环或单环羧酸; 每个n独立于其他n是0,1,2或3; R 9是OH，C 1-6烷基，C 1-6烷氧基，C 1-6全氟烷基苯基或具有一个或多个R 2取代基的苯基。

    2-Substituted quinolines, their preparation and use
    30.
    发明公开
    2-Substituted quinolines, their preparation and use 失效
    2-取代的喹啉，其制备和使用

    公开(公告)号：EP0206751A3

    公开(公告)日：1988-05-25

    申请号：EP86304686

    申请日：1986-06-17

    申请人： MERCK FROSST CANADA INC.

    发明人： Young, Robert N. ,  Leger, Serge ,  Frenette, Richard ,  Zamboni, Robert ,  Williams, Hayden W. R.

    IPC分类号： C07D215/18 ,  C07D215/14 ,  C07D215/12 ,  C07D215/36 ,  C07D401/12 ,  A61K31/47

    CPC分类号： C07D401/12 ,  C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D215/36

    摘要： Compounds having the formula:
    are selective antagonists of leukotrienes of D 4 . 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 1 is H, halogen, C 1 -C 8 alkyl, C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, -CF 3 , -OR 2 , -SR 2 , -NR 2 R 2 , -CHO, -COO R 2 , -( C = O ) R 2 , -C(OH)R 2 R 2 , -CN, -N0 2 , substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, or substituted or unsubstituted phenethyl; R 2 is H, C 1 -C 8 alkyl, C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, -CF 3 , substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, or substituted or unsubstituted phenethyl; R 3 is -(A) m -(CR 2 =CR 2 ) p -(CR 2 R 2 ) m - Q; R 4 is H, halogen, -N0 2 , -CN, -OR 2 , -SR 2 , NR 2 R 2 , or C 1 -C 8 alkyl;
    R 5 is -(CH 2 ) s -C-(CH 2 ) s -R 7 ;
    R 6 is H or C 1 -C 4 alkyl; R 7 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 s ; R S 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 9 is -OR 10 , -SR 10 , or NR 10 R 10 ; R 10 is H, C 1 -C 6 alkyl, -(C=O)R 11 , unsubstituted phenyl or unsubstituted benzyl; R 11 is H, C 1 -C 8 alkyl, C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, -CF 3 , or unsubstituted phenyl, benzyl, or phenethyl; m is 0-8; n is 1 or 2; p is 0-2; s is 0-3; A is -CR 2 R 4- , or =C=O; Q is -COOR 2 , tetrazole, -COOR 5 , -COCH 2 OH, -CONHSO 2 R 11 , -CH 2 OH, -CN, -CONR 10 R 10 , -NHSO 2 R 11 (but only when the sum of m and p in R 3 is greater than 0), or if Q is COOH and R 3 contains an R 4 which is -OH, -SH, or -NHR 2 then Q and R 4 and the carbons through which they are attached may form a heterocyclic ring with loss of water; W is O, S, or NH; X is O, S, -SO, -S0 2 , or -NR 2 ; Y is -(CR 2 =CR 2 ) n -, -(C≡C) n -, -CR 2 R 2- X-, or-X-CR 2 R 2 -.