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    • 46. 发明授权
    • Quinoline-N-oxide derivative and pharmaceutical composition
    • 喹啉-N-氧化物衍生物和药物组合物
    • US4657916A
    • 1987-04-14
    • US772693
    • 1985-09-05
    • Masayuki TeranishiKoji SuzukiHiroshi KaseShigeto KitamuraKatsuichi ShutoKenji Omori
    • Masayuki TeranishiKoji SuzukiHiroshi KaseShigeto KitamuraKatsuichi ShutoKenji Omori
    • A61K31/47A61P43/00C07D215/60C07D405/12C07F7/18
    • C07D405/12C07D215/60
    • A quinoline-N-oxide derivative represented by the formula: ##STR1## 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.sub.1 is alkylene or alkenylene having 3 to 15 carbon atom; 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.sub.2 NHR.sub.2 (wherein R.sub.2 is lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), --CH.sub.2 NR.sub.3 R.sub.4 (wherein R.sub.3 and R.sub.4 are lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), --CH.sub.2 N.sup.+ R.sub.5 R.sub.6 R.sub.7 (wherein R.sub.5, R.sub.6, and R.sub.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.sub.8 (wherein R.sub.8 is a hydrogen atom, lower alkyl or hydroxy), --CH(OR.sub.9).sub.2 (wherein R.sub.9 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.
    • 由下式表示的喹啉-N-氧化物衍生物:其中X为羟基,低级烷氧基,低级烷硫基,未取代或取代的芳烷氧基,或未取代或取代的芳烷硫基; Y是氢原子或卤素原子; R1是具有3至15个碳原子的亚烷基或亚烯基; Z是羟甲基,低级烷氧基甲基,未取代或取代的芳氧基甲基,四氢吡喃氧基甲基,四氢呋喃氧基甲基,未取代或取代的芳基磺酰氧基甲基,低级烷硫基甲基,未取代或取代的芳基硫代甲基,低级烷基亚磺酰基甲基,未取代或取代的芳基亚磺酰基甲基,低级烷基磺酰基甲基,未取代或取代的芳基磺酰基甲基,氨基甲基,-CH2NHR2( 其中R 2是低级烷基,未取代或取代的芳烷基或未取代或取代的芳基),-CH 2 NR 3 R 4(其中R 3和R 4是低级烷基,未取代或取代的芳烷基,或未取代或取代的芳基),-CH 2 N + R 5 R 6 R 7(其中R 5,R 6 ,R 7为低级烷基,未取代或取代的芳烷基或未取代或取代的芳基,其中抗衡离子为酸或羟基离子的阴离子),-COR8(其中R8为氢原子,低级烷基或羟基),-CH (OR 9)2(其中R 9为低级烷基),亚氨基甲基,羟基亚氨基甲基或卤素 原子及其盐可以非常强烈地抑制脂氧合酶,并显着抑制其代谢物的产生和释放,因此可用作由脂氧合酶代谢物引起的疾病的预防和治疗剂。
    • 48. 发明申请
    • APPARATUS REGISTRATION METHOD AND SERVER DEVICE
    • 装置注册方法和服务器设备
    • US20120131649A1
    • 2012-05-24
    • US13388127
    • 2010-10-26
    • Hiroshi Kase
    • Hiroshi Kase
    • G06F21/00
    • H04N5/765H04N21/6334
    • In a method of registering an access permission from a first device to a second device to the second device over a network, when receiving via the network a connection request from the first device of which access permission is not registered, the second device rejects connection from the first device, and shifts to the first mode. In the first mode, the second device detects user's operation on the second device, and judges whether the detected user's operation is an operation regarding viewing of a reproduction signal from the second device. If the user's operation is not the operation regarding viewing, the second device shifts to the second mode for registering an access permission. If the user's operation is the operation regarding viewing, the second device does not shift to the second mode.
    • 在通过网络将从第一设备到第二设备的访问许可登记到第二设备的方法中,当经由网络接收到来自未登记访问许可的第一设备的连接请求时,第二设备拒绝 第一个设备,并转移到第一个模式。 在第一模式中,第二设备检测用户在第二设备上的操作,并且判断检测到的用户的操作是否是关于从第二设备观看再现信号的操作。 如果用户的操作不是关于观看的操作,则第二设备转移到用于注册访问许可的第二模式。 如果用户的操作是关于观看的操作,则第二设备不转移到第二模式。
    • 50. 发明授权
    • Administering adenosine A2A receptor antagonist to reduce or suppress side effects of parkinson's disease therapy
    • 管理腺苷A2A受体拮抗剂以减少或抑制帕金森病治疗的副作用
    • US07727993B2
    • 2010-06-01
    • US11326414
    • 2006-01-06
    • Hiroshi KaseAkihisa MoriYutaka WakiYutaka OhsawaAkira KarasawaYoshihisa Kuwana
    • Hiroshi KaseAkihisa MoriYutaka WakiYutaka OhsawaAkira KarasawaYoshihisa Kuwana
    • A61K31/522A61K31/505
    • A61K31/522A61K9/0019A61K9/20A61K9/48A61K31/198A61K45/06
    • The present invention is directed to methods of treating movement disorders by administering an effective amount of one or more adenosine A2A 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 A2A 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 A2A 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 A2A 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.
    • 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。 本发明还提供降低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。 本发明进一步提供了通过将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)来治疗具有亚临床有效剂量的L-DOPA的帕金森病患者的方法和组合物, 。 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,通过单独或与多巴胺激动剂和/或COMT抑制剂和/或MAO抑制剂一起施用腺苷A2A受体拮抗剂,而无需先前或随后给予L-DOPA ,延迟或消除L-DOPA电机并发症。