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    • 6. 发明授权
    • Triazolopyridazine derivatives, their production and use
    • 三唑并哒嗪衍生物,其生产和使用
    • US5492909A
    • 1996-02-20
    • US225981
    • 1994-04-12
    • Akio MiyakeMasahiro KajinoYasuko Ashida
    • Akio MiyakeMasahiro KajinoYasuko Ashida
    • C07D487/04A61K31/50A61K31/535C07D487/14
    • C07D487/04
    • A compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group or a halogen atom; R.sup.2 and R.sup.3 are a hydrogen atom, a lower alkyl group or a 5- to 7-membered cyclic group formed together with the adjacent --C.dbd.C--; X is an oxygen atom, a sulfur atom or a methylene group; Y is an optionally substituted methylene group, a divalent 3- to 7-membered homo- or heterocyclic group; R.sup.6 and R.sup.7 are a hydrogen atom, a lower alkyl group, a cycloalkyl group, an aryl group, or a nitrogen-containing heterocyclic group formed together With the adjacent nitrogen atom; m is an integer of 0 to 4; and n is an integer of 0 to 4, or a salt thereof. Said compound has an excellent anti-PAF activity, antiallergic action, etc., thus is useful as an antiasthmatic agent.
    • 下式的化合物:其中R 1是氢原子,低级烷基或卤素原子; R2和R3是与相邻的-C = C-一起形成的氢原子,低级烷基或5-至7-元环基; X是氧原子,硫原子或亚甲基; Y是任选取代的亚甲基,二价3-至7-元同 - 或杂环基; R6和R7是与相邻的氮原子一起形成的氢原子,低级烷基,环烷基,芳基或含氮杂环基; m为0〜4的整数。 n为0〜4的整数,或其盐。 所述化合物具有优异的抗PAF活性,抗过敏作用等,因此可用作抗哮喘药。
    • 10. 发明授权
    • Triazolopyridazine compounds, their production and use
    • 三唑并哒嗪化合物,其生产和使用
    • US5482939A
    • 1996-01-09
    • US306423
    • 1994-09-16
    • Akio MiyakeYasuhiko KawanoYasuko Ashida
    • Akio MiyakeYasuhiko KawanoYasuko Ashida
    • C07D487/04A61K31/50A61K31/535C07D487/12
    • C07D487/04
    • Novel compound represented by the formula: ##STR1## wherein R.sup.1 stands for H, an optionally substituted lower alkyl group or a halogen; R.sup.2 and R.sup.3 respectively stands for a hydrogen or an optionally substituted lower alkyl group, or R.sup.2 and R.sup.3 may, taken together with the adjacent --C.dbd.C-- group, form a 5- to 7-membered ring; X stands for O, SO or SO.sub.2 ; Y stands for a group of the formula: ##STR2## (R.sup.4 and R.sup.5 respectively stand for H or an optionally substituted lower alkyl group) or a divalent group derived from an optionally substituted 3- to 7-membered homocyclic or heterocyclic ring; R.sup.6 and R.sup.7 each stands for H, an optionally substituted lower alkyl group, an optionally substituted cycloalkyl group or an optionally substituted aryl group, or R.sup.6 and R.sup.7 may, taken together with the adjacent N, form an optionally substituted N-containing heterocyclic group; m stands for 0 to 4; n stands for 0 to 4, or a salt thereof, which has excellent anti-PAF activities anti-LTC.sub.4 activities and anti-ET-1 activities, and is of value as an antiasthmatic agent, and their production, intermediates and pharmaceutical compositions.
    • 由下式表示的新化合物:其中R1代表H,任选取代的低级烷基或卤素; R2和R3分别表示氢或任选取代的低级烷基,或者R 2和R 3可以与相邻的C = C-基团一起形成5-至7-元环; X代表O,SO或SO2; Y代表下式的基团:(R 4和R 5分别代表H或任意取代的低级烷基)或衍生自任选取代的3-至7-元级环或杂环的二价基团; R 6和R 7各自代表H,任选取代的低级烷基,任选取代的环烷基或任选取代的芳基,或者R 6和R 7可以与相邻的N一起形成任选取代的含N杂环基; m代表0到4; n代表0至4或其盐,其具有优异的抗PAF活性抗LTC4活性和抗ET-1活性,并且具有价值作为抗哮喘药及其制备,中间体和药物组合物。