公开(公告)号：US20060178379A1

公开(公告)日：2006-08-10

申请号：US11326414

申请日：2006-01-06

申请人： Hiroshi Kase ,  Akihisa Mori ,  Yutaka Waki ,  Yutaka Ohsawa ,  Akira Karasawa ,  Yoshihisa Kuwana

发明人： Hiroshi Kase ,  Akihisa Mori ,  Yutaka Waki ,  Yutaka Ohsawa ,  Akira Karasawa ,  Yoshihisa Kuwana

IPC分类号： A61K31/522 ,  A61K31/198 ,  A61K31/137

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 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.

公开(公告)号：US07727994B2

公开(公告)日：2010-06-01

申请号：US11326516

申请日：2006-01-06

申请人： Hiroshi Kase ,  Akihisa Mori ,  Yutaka Waki ,  Yutaka Ohsawa ,  Akira Karasawa ,  Yoshihisa Kuwana

发明人： Hiroshi Kase ,  Akihisa Mori ,  Yutaka Waki ,  Yutaka Ohsawa ,  Akira Karasawa ,  Yoshihisa Kuwana

IPC分类号： A61K31/522 ,  A61K31/505

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 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.

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。

公开(公告)号：US20120122897A1

公开(公告)日：2012-05-17

申请号：US13297341

申请日：2011-11-16

申请人： Hiroshi Kase ,  Akihisa Mori ,  Yutaka Waki ,  Yutaka Ohsawa ,  Akira Karasawa ,  Yoshihisa Kuwana

发明人： Hiroshi Kase ,  Akihisa Mori ,  Yutaka Waki ,  Yutaka Ohsawa ,  Akira Karasawa ,  Yoshihisa Kuwana

IPC分类号： A61K31/522 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16

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

摘要： Methods of treating movement disorders by administering an effective amount of one or more adenosine A2A receptor antagonists to a patient in need thereof and methods of decreasing the adverse effects of L-DOPA in patients receiving L-DOPA therapy in the treatment of Parkinson's disease. Also, methods and compositions for treating Parkinson's disease patients with sub-clinically effective doses of L-DOPA with an effective amount of one or more adenosine A2A receptor antagonists, optionally with a dopamine agonist and/or a COMT inhibitor and/or a MAO inhibitor.

摘要翻译： 通过向有需要的患者施用有效量的一种或多种腺苷A2A受体拮抗剂和降低L-DOPA在接受L-DOPA治疗帕金森病的患者中的不利影响的方法来治疗运动障碍的方法。 此外，用有效量的一种或多种腺苷A2A受体拮抗剂，任选地与多巴胺激动剂和/或COMT抑制剂和/或MAO抑制剂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 。

公开(公告)号：US07727993B2

公开(公告)日：2010-06-01

申请号：US11326414

申请日：2006-01-06

申请人： Hiroshi Kase ,  Akihisa Mori ,  Yutaka Waki ,  Yutaka Ohsawa ,  Akira Karasawa ,  Yoshihisa Kuwana

发明人： Hiroshi Kase ,  Akihisa Mori ,  Yutaka Waki ,  Yutaka Ohsawa ,  Akira Karasawa ,  Yoshihisa Kuwana

IPC分类号： A61K31/522 ,  A61K31/505

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 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.

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。

公开(公告)号：US20060148827A1

公开(公告)日：2006-07-06

申请号：US11326516

申请日：2006-01-06

申请人： Hiroshi Kase ,  Akihisa Mori ,  Yutaka Waki ,  Yutaka Ohsawa ,  Akira Karasawa ,  Yoshihisa Kuwana

发明人： Hiroshi Kase ,  Akihisa Mori ,  Yutaka Waki ,  Yutaka Ohsawa ,  Akira Karasawa ,  Yoshihisa Kuwana

IPC分类号： A61K31/522 ,  A61K31/198 ,  A61K31/137

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 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.

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 2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（用于治疗患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 即L-DOPA保护作用）。 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来有效治疗帕金森病的方法 抑制剂。 本发明还提供了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A 2A受体拮抗剂而延长帕金森病有效治疗的方法，而没有 之前或之后的L-DOPA给药，延迟或去除L-DOPA运动并发症。

公开(公告)号：US20120010225A1

公开(公告)日：2012-01-12

申请号：US13234355

申请日：2011-09-16

申请人： Hiroshi Kase ,  Minoru Kobayashi ,  Shizuo Shiozaki ,  Akihisa Mori ,  Naoki Seno

发明人： Hiroshi Kase ,  Minoru Kobayashi ,  Shizuo Shiozaki ,  Akihisa Mori ,  Naoki Seno

IPC分类号： A61K31/522 ,  A61P25/24

CPC分类号： A61K31/522 ,  A61K31/137 ,  A61K31/138 ,  A61K31/16 ,  A61K31/335 ,  A61K31/343 ,  A61K31/36 ,  A61K31/38 ,  A61K31/381 ,  A61K31/435 ,  A61K31/4525 ,  A61K31/496 ,  A61K31/52 ,  A61K31/5375 ,  A61K31/55 ,  A61K31/553 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention provides pharmaceutical compositions, which are useful for treatment of depression and the like, and which comprises a compound having an adenosine A2A receptor antagonistic activity such as (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione or a pharmaceutically acceptable salt thereof and an antidepressant drug (for example, a tricyclic antidepressant, a tetracyclic antidepressant, a selective serotonin reuptake inhibitor, a selective noradrenalin reuptake inhibitor, a dopamine reuptake inhibitor, a serotonin-noradrenalin reuptake inhibitor, monoamine oxidase inhibitor, a 5-HT2 antagonist or the like), and the like.

摘要翻译： 本发明提供了可用于治疗抑郁症等的药物组合物，其包含具有腺苷A 2A受体拮抗活性的化合物，例如（E）-8-（3,4-二甲氧基苯乙烯基） 二乙基-7-甲基-3,7-二氢-1H-嘌呤-2,6-二酮或其药学上可接受的盐和抗抑郁药（例如，三环抗抑郁药，四环抗抑郁药，选择性5-羟色胺再摄取抑制剂， 选择性去甲肾上腺素再摄取抑制剂，多巴胺再摄取抑制剂，5-羟色胺去甲肾上腺素再摄取抑制剂，单胺氧化酶抑制剂，5-HT2拮抗剂等）等。

公开(公告)号：US20050245545A1

公开(公告)日：2005-11-03

申请号：US10523603

申请日：2003-08-27

申请人： Hiroshi Kase ,  Naoki Seno ,  Akihisa Mori ,  Dayao Zhao

发明人： Hiroshi Kase ,  Naoki Seno ,  Akihisa Mori ,  Dayao Zhao

IPC分类号： C07D473/06 ,  A61K31/00 ,  A61K31/522 ,  A61K45/00 ,  A61P1/14 ,  A61P1/16 ,  A61P3/02 ,  A61P3/10 ,  A61P3/12 ,  A61P5/14 ,  A61P7/02 ,  A61P7/06 ,  A61P7/08 ,  A61P11/00 ,  A61P11/16 ,  A61P13/02 ,  A61P15/00 ,  A61P19/02 ,  A61P25/00 ,  A61P25/02 ,  A61P25/14 ,  A61P25/20 ,  A61P25/28 ,  A61P25/32 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00

CPC分类号： A61K31/00 ,  A61K31/522

摘要： The present invention provides methods of treating restless legs syndrome or related disorders, comprising administering an effective amount of at least one adenosine A2A receptor antagonist to a patient in need thereof. More preferably the adenosine A2A receptor antagonist is a xanthine derivative or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明提供了治疗不宁腿症状或相关疾病的方法，包括向有需要的患者施用有效量的至少一种腺苷A 2A受体拮抗剂。 更优选地，腺苷A 2A受体拮抗剂是黄嘌呤衍生物或其药学上可接受的盐。

公开(公告)号：US08440678B2

公开(公告)日：2013-05-14

申请号：US13234355

申请日：2011-09-16

申请人： Hiroshi Kase ,  Minoru Kobayashi ,  Shizuo Shiozaki ,  Akihisa Mori ,  Naoki Seno

发明人： Hiroshi Kase ,  Minoru Kobayashi ,  Shizuo Shiozaki ,  Akihisa Mori ,  Naoki Seno

IPC分类号： A01N43/90 ,  A01N33/02 ,  A61K31/522 ,  A61K31/13 ,  C07D473/00 ,  C07D403/02 ,  C07C211/00

CPC分类号： A61K31/522 ,  A61K31/137 ,  A61K31/138 ,  A61K31/16 ,  A61K31/335 ,  A61K31/343 ,  A61K31/36 ,  A61K31/38 ,  A61K31/381 ,  A61K31/435 ,  A61K31/4525 ,  A61K31/496 ,  A61K31/52 ,  A61K31/5375 ,  A61K31/55 ,  A61K31/553 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention provides pharmaceutical compositions, which are useful for treatment of depression and the like, and which comprises a compound having an adenosine A2A receptor antagonistic activity such as (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione or a pharmaceutically acceptable salt thereof and an antidepressant drug (for example, a tricyclic antidepressant, a tetracyclic antidepressant, a selective serotonin reuptake inhibitor, a selective noradrenalin reuptake inhibitor, a dopamine reuptake inhibitor, a serotonin-noradrenalin reuptake inhibitor, monoamine oxidase inhibitor, a 5-HT2 antagonist or the like), and the like.

摘要翻译： 本发明提供了可用于治疗抑郁症等的药物组合物，其包含具有腺苷A 2A受体拮抗活性的化合物，例如（E）-8-（3,4-二甲氧基苯乙烯基） 二乙基-7-甲基-3,7-二氢-1H-嘌呤-2,6-二酮或其药学上可接受的盐和抗抑郁药（例如，三环抗抑郁药，四环抗抑郁药，选择性5-羟色胺再摄取抑制剂， 选择性去甲肾上腺素再摄取抑制剂，多巴胺再摄取抑制剂，5-羟色胺去甲肾上腺素再摄取抑制剂，单胺氧化酶抑制剂，5-HT2拮抗剂等）等。

公开(公告)号：US07759355B2

公开(公告)日：2010-07-20

申请号：US10523603

申请日：2003-08-27

申请人： Hiroshi Kase ,  Naoki Seno ,  Akihisa Mori ,  Dayao Zhao

发明人： Hiroshi Kase ,  Naoki Seno ,  Akihisa Mori ,  Dayao Zhao

IPC分类号： A61K31/522 ,  A61P25/00 ,  A61P25/14

CPC分类号： A61K31/00 ,  A61K31/522

摘要： The present invention provides methods of treating restless legs syndrome or related disorders, comprising administering an effective amount of at least one adenosine A2A receptor antagonist to a patient in need thereof. More preferably the adenosine A2A receptor antagonist is a xanthine derivative or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明提供了治疗不宁腿症状或相关病症的方法，包括向有需要的患者施用有效量的至少一种腺苷A 2A受体拮抗剂。 更优选地，腺苷A 2A受体拮抗剂是黄嘌呤衍生物或其药学上可接受的盐。

公开(公告)号：US08034820B2

公开(公告)日：2011-10-11

申请号：US10565239

申请日：2004-07-22

申请人： Hiroshi Kase ,  Minoru Kobayashi ,  Shizuo Shiozaki ,  Akihisa Mori ,  Naoki Seno

发明人： Hiroshi Kase ,  Minoru Kobayashi ,  Shizuo Shiozaki ,  Akihisa Mori ,  Naoki Seno

IPC分类号： A01N43/90 ,  A01N43/52 ,  A61K31/522 ,  A61K31/415 ,  C07D473/00 ,  C07D403/02 ,  C07D317/44 ,  C07C211/00 ,  C07C213/00 ,  C07C215/00 ,  C07C217/00

CPC分类号： A61K31/522 ,  A61K31/137 ,  A61K31/138 ,  A61K31/16 ,  A61K31/335 ,  A61K31/343 ,  A61K31/36 ,  A61K31/38 ,  A61K31/381 ,  A61K31/435 ,  A61K31/4525 ,  A61K31/496 ,  A61K31/52 ,  A61K31/5375 ,  A61K31/55 ,  A61K31/553 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention provides pharmaceutical compositions, which are useful for treatment of depression and the like, and which comprises a compound having an adenosine A2A receptor antagonistic activity such as (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione or a pharmaceutically acceptable salt thereof and an antidepressant drug (for example, a tricyclic antidepressant, a tetracyclic antidepressant, a selective serotonin reuptake inhibitor, a selective noradrenalin reuptake inhibitor, a dopamine reuptake inhibitor, a serotonin-noradrenalin reuptake inhibitor, a monoamine oxidase inhibitor, a 5-HT2 antagonist or the like), and the like.

摘要翻译： 本发明提供了可用于治疗抑郁症等的药物组合物，其包含具有腺苷A2A受体拮抗活性的化合物，例如（E）-8-（3,4-二甲氧基苯乙烯基） 二乙基-7-甲基-3,7-二氢-1H-嘌呤-2,6-二酮或其药学上可接受的盐和抗抑郁药（例如，三环抗抑郁药，四环抗抑郁药，选择性5-羟色胺再摄取抑制剂， 选择性去甲肾上腺素再摄取抑制剂，多巴胺再摄取抑制剂，5-羟色胺去甲肾上腺素再摄取抑制剂，单胺氧化酶抑制剂，5-HT2拮抗剂等）等。