Thiazolybenzofuran derivatives and their use as SRS-A and leukotiene antagonists
    3.
    发明公开
    Thiazolybenzofuran derivatives and their use as SRS-A and leukotiene antagonists 失效
    噻唑基苯并呋喃衍生物及其作为SRS-A和白三烯拮抗剂的用途

    公开(公告)号:EP1170009A2

    公开(公告)日:2002-01-09

    申请号:EP01123263.4

    申请日:1997-01-17

    CPC分类号: C07D417/04 C07D417/14

    摘要: This invention relates to novel thiazolylbenzofuran derivatives of formula (I) wherein R 1 is lower alkyl, L is single bond or lower alkylene optionally substituted with aryl, oxo or hydroxy, and Q is a heterocyclix group optionally substituted with one or more suitable substituent(s); or lower alkoxy substituted with aryl which is substituted with one or more suitable substituent(s) and at least one of which is lower alkoxy optionally substituted with cyano, protected carboxy, carboxy, lower alkylene, a heterocyclic group optionally substituted with oxo, or amidino optionally substituted with hydroxy or lower alkoxy, or its salt, which possess activities as leukotriene and SRS-A antagonists or inhibitors.

    摘要翻译: 本发明涉及式(I)的新型噻唑基苯并呋喃衍生物,其中R1是低级烷基,L是单键或任选被芳基,氧代或羟基取代的低级亚烷基,Q是任选被一个或多个合适的取代基取代的杂环基 ); 或被一个或多个合适的取代基取代并且其中至少一个是用氰基,被保护的羧基,羧基,低级亚烷基,任选被氧代取代的杂环基或脒基取代的低碳烷氧基取代的低碳烷氧基 任选地被羟基或低级烷氧基或其盐所取代,它们具有白三烯和SRS-A拮抗剂或抑制剂的活性。

    Piperazine derivatives as Tachykinin antagonists
    7.
    发明公开
    Piperazine derivatives as Tachykinin antagonists 失效
    Piperazinderivate als速激肽拮抗剂。

    公开(公告)号:EP0655442A1

    公开(公告)日:1995-05-31

    申请号:EP94118542.3

    申请日:1994-11-25

    摘要: A compound of the following general formula :

    wherein

    X is carbonyl or sulfonyl;
    Y is bond or lower alkylene;
    R¹ is halogen, lower alkyl, halo(lower)alkyl, aryloxy, nitro or amino which may have 1 or 2 and same or different substituent(s) selected from lower alkyl, acyl and lower alkanesulfonyl;
    R² is aryl or an aromatic hetero(mono- or bi-)cyclic group, and each of which may have 1, 2 or 3 suitable substituent(s);
    R³ is hydrogen or lower alkyl;
    R⁴ is

    (i) a group of the formula -SO₂-R⁵ in which R⁵ is lower alkyl or aryl optionally substituted with lower alkyl or lower alkoxy,
    (ii) a group of the formula
    in which R⁶ is aryl optionally substituted with lower alkyl or lower alkoxy, or
    (iii) a group of the formula -A-(Z) p in which
    A  is bond, lower alkylene, lower alkenylene or lower alkynylene,
    Z  is hydrogen, halogen, hydroxy, nitrile, amino, cyclo(lower)alkyl, aryl, aryloxy, acyl, acylamino, lower alkanesulfonylamino, arylsulfonylamino or an aromatic hetero(mono- or bi-)cyclic group, and each of the cyclic group may have 1, 2 or 3 suitable substituent(s), and
    p  is 1, 2 or 3; and

    n is 0, 1 or 2;

    provided that when n or p is more than 1, these R¹ and Z may be the same or different group respectively; or its pharmaceutically acceptable salt, processes for their preparation and pharmaceutical compositions comprising them.

    摘要翻译: 下列通式的化合物:其中X为羰基或磺酰基; Y是键或低级亚烷基; R 1是卤素,低级烷基,卤代(低级)烷基,芳氧基,硝基或氨基,其可以具有1或2个相同或不同的选自低级烷基,酰基和低级链烷磺酰基的取代基; R 2是芳基或芳族杂环(单或双)环基团,并且各自可以具有1,2或3个合适的取代基; R 3是氢或低级烷基; R 4是(i)式-SO 2 -R 5的基团,其中R 5是任选被低级烷基或低级烷氧基取代的低级烷基或芳基,(ii)式其中R 6为任选被低级烷基或低级烷氧基取代的芳基,或(iii)其中A为键的式-A(Z)p基团,低级亚烷基,低级亚烯基或低级亚烷基,Z 芳基,芳氧基,酰基,酰氨基,低级链烷磺酰氨基,芳基磺酰基氨基或芳族杂环(单 - 或双) - 环基团,并且每个环状基团可以是氢,卤素,羟基,腈, 具有1,2或3个合适的取代基,p是1,2或3; 并且n为0,1或2; 条件是当n或p大于1时,这些R 1和Z可以分别相同或不同; 或其药学上可接受的盐,其制备方法和包含它们的药物组合物。