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    Triazolopyridazine derivatives, their production and use
    1.
    发明授权
    Triazolopyridazine derivatives, their production and use 失效
    三唑并哒嗪衍生物，其生产和使用

    公开(公告)号：US5492909A

    公开(公告)日：1996-02-20

    申请号：US225981

    申请日：1994-04-12

    申请人： Akio Miyake ,  Masahiro Kajino ,  Yasuko Ashida

    发明人： Akio Miyake ,  Masahiro Kajino ,  Yasuko Ashida

    IPC分类号： C07D487/04 ,  A61K31/50 ,  A61K31/535 ,  C07D487/14

    CPC分类号： C07D487/04

    摘要： 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.

    摘要翻译： 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。

    Imidazopyridazines, their production and use
    2.
    发明授权
    Imidazopyridazines, their production and use 失效
    咪达唑德他们的生产和使用

    公开(公告)号：US5145850A

    公开(公告)日：1992-09-08

    申请号：US659704

    申请日：1991-02-25

    申请人： Akio Miyake ,  Yasuko Ashida

    发明人： Akio Miyake ,  Yasuko Ashida

    IPC分类号： A61K31/50 ,  A61K31/5025 ,  A61P11/00 ,  A61P11/06 ,  A61P11/08 ,  A61P29/00 ,  A61P37/08 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： An imidazo [1,2-b]pyridazine compound of the formula (I): ##STR1## wherein R.sub.1 is a halogen atom or a lower alkyl group optionally having substituent(s), R.sub.2 and R.sub.3 are, independently, a hydrogen atom, a lower alkyl group optionally having substituent(s), a cycloalkyl group or a phenyl group optionally having substituent(s) or R.sub.2 and R.sub.3 together with the adjacent nitrogen atom to which they bond may form a heterolcyclic ring optionally having substituent(s), X is an oxygen atom or S(O).sub.k (k is zero to two), a group --.circle.A-- is a bivalent three to seven membered homocyclic or heterocyclic group optionally having substituent(s), m.sup.1 and m.sup.2 each is an integer of 0 to 4 and n is an integer of 0 or 1; or its salt, which is useful as antiasthmatics.

    Eosinophil chemotaxis inhibitor
    3.
    发明授权
    Eosinophil chemotaxis inhibitor 失效
    嗜酸性粒细胞趋化性抑制剂

    公开(公告)号：US5922712A

    公开(公告)日：1999-07-13

    申请号：US070928

    申请日：1998-05-01

    申请人： Akio Miyake ,  Yasuko Ashida ,  Tatsumi Matsumoto

    发明人： Akio Miyake ,  Yasuko Ashida ,  Tatsumi Matsumoto

    IPC分类号： A61K31/50 ,  A61K31/5025

    CPC分类号： A61K31/5025 ,  A61K31/50

    摘要： A method for inhibiting eosinophil infiltration by administrating to a subject in need thereof an effective amount of a compound of the formula: ##STR1## wherein R.sup.2 and R.sup.3 independently represent a hydrogen atom or a C.sub.1-4 group, and R.sup.4a and R.sup.5a independently represent a hydrogen atom or a C.sub.1-4 alkyl group, or a pharmaceutically acceptable salt thereof.

    摘要翻译： 通过向有需要的受试者施用有效量的下式化合物来抑制嗜酸性粒细胞浸润的方法：其中R2和R3独立地表示氢原子或C1-4基团，并且R4a和R5a独立地表示氢原子或 C 1-4烷基或其药学上可接受的盐。

    Pyridazine compounds, their production and use
    4.
    发明授权
    Pyridazine compounds, their production and use 失效
    哒嗪化合物，其生产和使用

    公开(公告)号：US5369104A

    公开(公告)日：1994-11-29

    申请号：US997538

    申请日：1992-12-28

    申请人： Akio Miyake ,  Yasuhiko Kawano ,  Yasuko Ashida

    发明人： Akio Miyake ,  Yasuhiko Kawano ,  Yasuko Ashida

    IPC分类号： C07D487/04 ,  A61K31/50 ,  A61K31/55 ,  C07D487/14

    CPC分类号： C07D487/04

    摘要： Novel compound represented by the formula: ##STR1## wherein X stands for a methine (i.e. the group --CH.dbd.) group or a nitrogen atom; R.sup.1 stands for a hydrogen atom, an optionally substituted lower alkyl group or a halogen atom; R.sup.2 and R.sup.3 respectively stand for a hydrogen atom or an optionally substituted lower alkyl group, or, taken together, may form a 5- to 7-membered ring combined with the adjacent --C.dbd.C--; R.sup.4 and R.sup.5 respectively stands for a hydrogen atom or an optionally substituted lower alkyl group or, taken together, form a 3- to 7-membered homo- or heterocyclic ring combined with the adjacent carbon atom; A stands for an optionally substituted amino group; m and n denote 1 to 4, respectively, or salts thereof which has an antiallergic, antiinflammatory and anti-PAF activity and is useful as an antiasthmatic agent.

    摘要翻译： 由下式表示的新型化合物：其中X表示次甲基（即基团-CH =）基团或氮原子; R1代表氢原子，任选取代的低级烷基或卤素原子; R2和R3分别表示氢原子或任选取代的低级烷基，或者一起可以形成与相邻-C = C-结合的5-至7-元环; R4和R5分别表示氢原子或任选取代的低级烷基，或者一起形成与相邻碳原子结合的3-至7-元同 - 或杂环; A代表任选取代的氨基; m和n分别表示1至4个或其盐，其具有抗过敏，抗炎和抗PAF活性，并且可用作抗哮喘药。

    Triazolopyridazine compounds, their production and use
    5.
    发明授权
    Triazolopyridazine compounds, their production and use 失效
    三唑并哒嗪化合物，其生产和使用

    公开(公告)号：US5482939A

    公开(公告)日：1996-01-09

    申请号：US306423

    申请日：1994-09-16

    申请人： Akio Miyake ,  Yasuhiko Kawano ,  Yasuko Ashida

    发明人： Akio Miyake ,  Yasuhiko Kawano ,  Yasuko Ashida

    IPC分类号： C07D487/04 ,  A61K31/50 ,  A61K31/535 ,  C07D487/12

    CPC分类号： C07D487/04

    摘要： 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.

    摘要翻译： 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。

    Method for treating allergic rhinitis
    6.
    发明授权
    Method for treating allergic rhinitis 失效
    治疗过敏性鼻炎的方法

    公开(公告)号：US5945419A

    公开(公告)日：1999-08-31

    申请号：US250392

    申请日：1999-02-16

    申请人： Akio Miyake ,  Yasuko Ashida ,  Tatsumi Matsumoto

    发明人： Akio Miyake ,  Yasuko Ashida ,  Tatsumi Matsumoto

    IPC分类号： A61K31/50 ,  A61K31/5025

    CPC分类号： A61K31/5025 ,  A61K31/50

    摘要： A method for treating allergic rhinitis by administrating to a subject in need thereof an effective amount of a compound of the formula: ##STR1## wherein R.sup.2 and R.sup.3 independently represent a hydrogen atom or a C.sub.1-4 alkyl group, and R.sup.4a and R.sup.5a independently represent a hydrogen atom or a C.sub.1-4 alkyl group, or a pharmaceutically acceptable salt thereof.

    摘要翻译： 通过向有需要的受试者施用有效量的下式化合物来治疗过敏性鼻炎的方法：其中R2和R3独立地表示氢原子或C1-4烷基，R4a和R5a独立地表示氢原子 或C 1-4烷基，或其药学上可接受的盐。

    Imidazopyridazines, their production and use
    7.
    发明授权
    Imidazopyridazines, their production and use 失效
    咪唑哒嗪，其生产和使用

    公开(公告)号：US5491145A

    公开(公告)日：1996-02-13

    申请号：US345326

    申请日：1994-11-21

    申请人： Akio Miyake ,  Yasuhiko Kawano ,  Yasuko Ashida

    发明人： Akio Miyake ,  Yasuhiko Kawano ,  Yasuko Ashida

    IPC分类号： C07D487/04 ,  A61K31/50

    CPC分类号： C07D487/04

    摘要： Novel compound of the general formula: ##STR1## wherein R.sup.1 stands for a hydrogen atom, an optionally substituted lower alkyl group or a halogen atom; R.sup.2 and R.sup.3 respectively stand for a hydrogen atom or an optionally substituted lower alkyl group, provided that either R.sup.2 or R.sup.3 is a hydrogen atom, the other being an optionally substituted lower alkyl group, or R.sup.2 and R.sup.3 may, taken together with the adjacent --C=C-- group, form a 5- to 7-membered ring; X stands for an oxygen atom or S(O).sub.p (p stands for an integer from 0 to 2; Y stands for a group of the formula: ##STR2## (R.sup.4 and R.sup.5 respectively stand for a hydrogen atom 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 a hydrogen atom, an optionally substituted lower lakyl 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 nitrogen atom, form an optionally substituted nitrogen-containing heterocyclic group; m stands for an integer from 0 to 4; and n stands for an integer from 0 to 4, or a salt thereof, which has excellent anti-PAF activities, and is of value as an antiasthmatic agent, and their production, intermediates and pharmaceutical compositions.

    摘要翻译： 新的通式化合物：其中R1代表氢原子，任选取代的低级烷基或卤素原子; R2和R3分别代表氢原子或任选取代的低级烷基，条件是R2或R3是氢原子，另一个是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，形成5-至7-元环; X表示氧原子或S（O）p（p表示0至2的整数; Y表示下式的基团：R 1和R 5分别代表氢原子或任选取代的低级 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各自表示氢原子，任选取代的低级烷酰基，任选取代的环烷基或任选取代的芳基 或R 6和R 7可以与相邻的氮原子一起形成任选取代的含氮杂环基; m表示0至4的整数; n表示0至4的整数，或表示盐 其具有优异的抗PAF活性，并且作为抗哮喘药物及其生产，中间体和药物组合物具有价值。

    Triazolopyridazine compounds, their production and use
    8.
    发明授权
    Triazolopyridazine compounds, their production and use 失效
    三唑并哒嗪化合物，其生产和使用

    公开(公告)号：US5389633A

    公开(公告)日：1995-02-14

    申请号：US32296

    申请日：1993-03-17

    申请人： Akio Miyake ,  Yasuhiko Kawano ,  Yasuko Ashida

    发明人： Akio Miyake ,  Yasuhiko Kawano ,  Yasuko Ashida

    IPC分类号： A61K20060101 ,  A61K31/50 ,  A61K31/5025 ,  A61P7/02 ,  A61P29/00 ,  A61P37/08 ,  C07D20060101 ,  C07D487/04 ,  A61K31/535 ,  C07D471/14

    CPC分类号： C07D487/04

    摘要： 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 pharmasceutical compositions.

    摘要翻译： 由下式表示的新型化合物：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。