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    Methods of treating patients suffering from movement disorders
    1.
    发明公开
    Methods of treating patients suffering from movement disorders 审中-公开
    Verfahren zur Behandlung von Patienten mitBewegungsstörungen

    公开(公告)号：EP2044940A2

    公开(公告)日：2009-04-08

    申请号：EP09150929.9

    申请日：2003-01-28

    申请人： Kyowa Hakko Kogyo Co., Ltd

    发明人： Kase, Hiroshi

    IPC分类号： A61K31/522 ,  A61P25/16

    CPC分类号： A61K31/522 ,  A61K9/0019 ,  A61K9/20 ,  A61K9/48 ,  A61K31/198 ,  A61K45/06

    摘要： The present invention is directed to methods of treating movement disorders by administering an effective amount of one or more adenosine A 2A receptor antagonists to a patient in need thereof. The present invention also provides methods of decreasing the adverse effects of L-DOPA in patients receiving L-DOPA therapy in the treatment of Parkinson's disease. The present invention further provides methods and compositions for treating Parkinson's disease patients with sub-clinically effective doses of L-DOPA by combining L-DOPA treatment with an effective amount of one or more adenosine A 2A receptor antagonists (i.e., L-DOPA sparing effect). The present invention further provides methods of effective treatment of Parkinson's disease by co-administering at least one adenosine A 2A receptor antagonist, L-DOPA and a dopamine agonist and/or a COMT inhibitor and/or a MAO inhibitor. The present invention further provides methods of prolonging effective treatment of Parkinson's disease by administering an adenosine A 2A receptor antagonist singly or together with a dopamine agonist, and/or a COMT inhibitor, and/or a MAO inhibitor without prior or subsequent administration of L-DOPA, delaying or removing on-set of L-DOPA motor complication.

    摘要翻译： 本发明涉及通过向有需要的患者施用有效量的一种或多种腺苷A 2A受体拮抗剂来治疗运动障碍的方法。 本发明还提供减少L-DOPA在接受L-DOPA治疗的帕金森病治疗中的不良反应的方法。 本发明还提供了通过将L-DOPA治疗与有效量的一种或多种腺苷A 2A受体拮抗剂组合（即，L-DOPA备用效应）来治疗帕金森病患者的亚临床有效剂量的L-DOPA的方法和组合物 ）。 本发明还提供了通过共同施用至少一种腺苷A 2A受体拮抗剂，L-DOPA和多巴胺激动剂和/或COMT抑制剂和/或MAO抑制剂来有效治疗帕金森病的方法。 本发明还提供了延长帕金森病有效治疗的方法，其通过单独给予腺苷A 2A受体拮抗剂或与多巴胺激动剂和/或COMT抑制剂和/或MAO抑制剂一起施用， DOPA，延迟或去除L-DOPA电机并发症。

    Xanthine derivatives
    5.
    发明公开
    Xanthine derivatives 失效
    黄嘌呤衍生物。

    公开(公告)号：EP0607607A1

    公开(公告)日：1994-07-27

    申请号：EP93120842.5

    申请日：1993-12-23

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： Suzuki, Fumio ,  Shimada, Junichi ,  Koike, Nobuaki ,  Kase, Hiroshi ,  Nakamura, Joji ,  Shiozaki, Shizuo ,  Nonaka, Hiromi

    IPC分类号： C07D473/06 ,  A61K31/52

    CPC分类号： C07D473/06

    摘要： Disclosed are xanthine derivatives represented by the following Formula (I):

    in which R¹, R², and R³ independently represent hydrogen or lower alkyl;
    Q¹, Q², and Q³ independently represent hydrogen, lower alkyl, lower alkoxy, or halogen;
    and X represents -COR⁴ (in which R⁴ represents hydrogen, hydroxy, lower alkyl, or lower alkoxy) or -SO₂R⁵ {in which R⁵ represents hydroxy, lower alkoxy, trifluoromethyl,

    in which R⁶ and R⁷ independently represent hydrogen, hydroxy-substituted or unsubstituted lower alkyl, aryl, or

    (in which m represents an integer of 1 to 3; and R⁸ and R⁹ independently represent hydrogen or lower alkyl), or

    (in which Y represents a single bond, oxygen, or N-R¹⁰ in which R¹⁰ represents hydrogen or lower alkyl; and n1 and n2 independently represent an integer of 1 to 3 )}, and pharmaceutically acceptable salts thereof.

    摘要翻译： 公开了由下式（I）表示的黄嘌呤衍生物：其中R 1，R 2和R 3独立地表示氢或低级烷基的 Q 1，Q 2和Q 3独立地表示氢，低级烷基，低级烷氧基或卤素; 并且X表示-COR 4（其中R 4表示氢，羟基，低级烷基或低级烷氧基）或-SO 2 R 5（其中R 5表示羟基，低级烷氧基，三氟甲基，CHEM 其中R 6和R 7独立地表示氢，羟基取代或未取代的低级烷基，芳基或（其中m表示1至3的整数;并且R 8和R 8' 或其中Y表示单键，氧或NR 1，其中R 1表示氢或低级烷基;和n1 和n2独立地表示1〜3的整数）}及其药学上可接受的盐。

    Quinoline-n-oxide derivative and pharmaceutical composition
    8.
    发明公开
    Quinoline-n-oxide derivative and pharmaceutical composition 失效
    喹啉N-氧化物衍生物和药物制剂。

    公开(公告)号：EP0177764A1

    公开(公告)日：1986-04-16

    申请号：EP85111243.3

    申请日：1985-09-05

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： Teranishi, Masayuki ,  Suzuki, Koji ,  Kase, Hiroshi ,  Kitamura, Shigeto ,  Shuto, Katsuichi ,  Omori, Kenji

    IPC分类号： C07D215/60 ,  C07D405/12 ,  A61K31/47

    CPC分类号： C07D405/12 ,  C07D215/60

    摘要： A quinoline-N-oxide derivative represented by the formula:
    [wherein X is hydroxy, lower alkoxy, lower alkylthio, unsubstituted or substituted aralkyloxy, or unsubstituted or substituted aralkylthio; Y is a hydrogen atom or halogen atom; R, is alkylene or alkenylene having 3 to 15 carbon atoms; Z is hydroxymethyl, lower alkoxymethyl, unsubstituted or substituted aryloxymethyl, tetrahydropyranyloxymethyl, tetrahydrofuranyloxymethyl, unsubstituted or substituted arylsulfonyloxymethyl, lower alkylthiomethyl, unsubstituted or substituted arylthiomethyl, lower alkylsulfinylmethyl, unsubstituted or substituted arylsulfinylmethyl, lower alkylsulfonylmethyl, unsubstituted or substituted arylsulfonylmethyl, aminomethyl, -CH 2 NHR 2 (wherein R 2 is lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), -CH 2 NR 3 R 4 , (wherein R 3 and R 4 are lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), -CH 2 N + R 5 R 6 R 7 (wherein R 5 , R 6 , and R 7 are lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl, where the counterion is an anion of acid or a hydroxyl ion), -COR 8 (wherein R. is a hydrogen atom, lower alkyl or hydroxy), -CH(OR 9 ) 2 (wherein R. is lower alkyl), iminomethyl, hydroxyiminomethyl, or a halogen atom] and its salts, can very strongly inhibit the lipoxygenase and considerably suppress production and release of its metabolites, and thus are useful as preventive and healing agents for the diseases caused by the lipoxygenase metabolites.