Condensed pyridazine derivatives, their production and use
    2.
    发明授权
    Condensed pyridazine derivatives, their production and use 失效
    冷凝哒嗪衍生物,其生产和使用

    公开(公告)号:US06248740B1

    公开(公告)日:2001-06-19

    申请号:US09284362

    申请日:1999-04-14

    IPC分类号: C07D40304

    CPC分类号: C07D487/04

    摘要: The present invention provides a compound represented by the formula: wherein Ar1 and Ar2 are independently an aromatic group which may be substituted, and Ar1 and Ar2 may form a condensed cyclic group with an adjacent carbon atom; ring B is a nitrogen-containing heterocycle which may be substituted; X and Y are the same or different and are independently a bond, an oxygen atom, S(O)p (p is an integer of 0 ot 2), NR4 wherein R4 is a hydrogen atom or a lower alkyl group, or a bivalent linear lower hydrocarbon group which may contain 1 to 3 hetero atoms and the bivalent linear lower hydrocarbon group may be substituted; A is a nitrogen atom or CR7 wherein R7 is a hydrogen atom, a halogen atom, a hydrocarbon which may be substituted, an acyl group or a hydroxy group which may be substituted; R1, R2 and R3 are the same or different and are independently a hydrogen atom, a halogen atom, a hydrocarbon group which may be substituted, an acyl group or a hydroxy group which may be substituted; R8 is a hydrogen atom, a hydroxy group which may be substituted by a lower alkyl or a carboxyl group, or a salt thereof, which exhibits excellent anti-histaminic or eosinophil chemotaxis-inhibiting activities and is useful in treatment or prevention of asthma, allergic conjunctivitis, allergic rhinitis, chronic urticaria or atopic dermatitis.

    摘要翻译: 本发明提供由下式表示的化合物:其中Ar1和Ar2独立地为可被取代的芳基,Ar1和Ar2可以与相邻的碳原子形成稠合的环状基团; 环B是可以被取代的含氮杂环; X和Y相同或不同,独立地为键,氧原子,S(O)p(p为0〜2的整数),NR4,其中R4为氢原子或低级烷基,或二价 可以含有1〜3个杂原子的直链低级烃基,二价直链低级烃基可以被取代; A是氮原子或CR 7,其中R7是氢原子,卤素原子,可被取代的烃基,酰基或可被取代的羟基; R1,R2和R3相同或不同,独立地为氢原子,卤素原子,可被取代的烃基,酰基或可被取代的羟基; R8是氢原子,可以被低级烷基或羧基取代的羟基或其盐,其表现出优异的抗组氨酸或嗜酸性粒细胞趋化性抑制活性,并且可用于治疗或预防哮喘,过敏 结膜炎,过敏性鼻炎,慢性荨麻疹或特应性皮炎。

    Condensed pyridazine compounds, their production and use
    3.
    发明授权
    Condensed pyridazine compounds, their production and use 失效
    缩合哒嗪化合物,其生产和使用

    公开(公告)号:US06610694B1

    公开(公告)日:2003-08-26

    申请号:US09806652

    申请日:2001-04-02

    IPC分类号: A61K3150

    CPC分类号: C07D487/04

    摘要: A condensed pyridazine derivative which exhibits anti-allergic activity, anti-histaminic activity and/or eosinophil chemotaxis-inhibiting activity, anti-inflammatory activity, anti-PAF (platelet-activating factor) activity, and the like, and is useful as an agent for preventing or treating asthma, allergic conjunctivitis, allergic rhinitis, urticaria, atopic dermatitis, and the like.

    摘要翻译: 具有抗过敏活性,抗组氨酸活性和/或嗜酸性粒细胞趋化性抑制活性,抗炎活性,抗PAF(血小板活化因子)活性等的缩合哒嗪衍生物等,可用作试剂 用于预防或治疗哮喘,过敏性结膜炎,过敏性鼻炎,荨麻疹,特应性皮炎等。

    Nitrogenous fused-ring compounds, process for the preparation of the same, and drugs
    5.
    发明授权
    Nitrogenous fused-ring compounds, process for the preparation of the same, and drugs 失效
    含氮稠环化合物,其制备方法和药物

    公开(公告)号:US06407116B1

    公开(公告)日:2002-06-18

    申请号:US09486646

    申请日:2000-02-25

    IPC分类号: C07D23996

    摘要: A compound represented by the formula: [wherein ring A represents a homocycle optionally having substituents or a nitrogen-containing heterocycle optionally having substituents; D and E are O or S; one of R1 and R2 represents a group represented by the formula: (wherein Ar1 and Ar2 represent an aromatic group optionally having substituents; Ar1 and Ar2 may form a condensed cyclic group optionally having substituents together with an adjacent carbon atom; ring B represents a nitrogen-containing heterocycle optionally having substituents; X and Y are a bond, O, S(O)p (p is an integer of 0 to 2), NR4 (R4 is H or a lower alkyl group) or a bivalent straight-chained lower hydrocarbon group, which may contain 1 to 3 hetero atoms, optionally having substituents; and R3 represents H, a hydroxy group optionally having substituents or an optionally esterified carboxyl group); and the other is a hydrogen atom, a cyano group or a hydrocarbon group optionally having substituents], or a salt thereof, has an anti-histaminic action, an anti-inflammatory action, eosinophil chemotaxis-inhibiting action, and is useful for preventing or treating asthma, allergic conjunctivitis, allergic rhinitis, urticaria, atopic dermatitis and so on.

    摘要翻译: 由下式表示的化合物:其中环A表示任选具有取代基的均质环或任选具有取代基的含氮杂环; D和E为O或S; R1和R2中的一个表示由下式表示的基团:其中Ar1和Ar2表示任选具有取代基的芳族基团; Ar1​​和Ar2可以与相邻碳原子一起形成任选具有取代基的稠合环状基团;环B表示氮 任选具有取代基的杂环; X和Y是键,O,S(O)p(p是0-2的整数),NR4(R4是H或低级烷基)或二价直链低级 可以含有1〜3个杂原子的烃基,任选具有取代基; R 3表示H,任选具有取代基的羟基或任选被酯化的羧基); 另一个是氢原子,氰基或任选具有取代基的烃基]或其盐具有抗组胺作用,抗炎作用,嗜酸性粒细胞趋化性抑制作用,并且可用于预防或 治疗哮喘,过敏性结膜炎,过敏性鼻炎,荨麻疹,特应性皮炎等。