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1. 发明申请

WO2004108137A1 A METHOD OF TREATING AN ANXIETY DISORDER 审中-公开
标题翻译：一种治疗恶心病的方法
公开(公告)号：WO2004108137A1
公开(公告)日：2004-12-16
申请号：PCT/JP2004/008486
申请日：2004-06-10
申请人： KYOWA HAKKO KOGYO CO., LTD. , KASE, Hiroshi , SENO, Naoki , SHIOZAKI, Shizuo , KOBAYASHI, Minoru , KASE, Junya
发明人： KASE, Hiroshi , SENO, Naoki , SHIOZAKI, Shizuo , KOBAYASHI, Minoru , KASE, Junya
IPC分类号： A61K31/522
CPC分类号： A61K45/06 , A61K31/00 , A61K31/519 , A61K31/522 , A61K2300/00
摘要： Anxiety disorders, such as panic disorder, agoraphobia, obsessive-compulsive disorder, social phobia, post-traumatic stress disorder, generalized anxiety disorder, specific phobia, or the like, are treated by administering an effective amount of at least one adenosine A 2A receptor antagonist to a patient in need thereof, optionally in combination with an anxiolytic(s) other than the adenosine A 2A receptor antagonist.
摘要翻译：通过施用有效量的至少一种腺苷A2A受体拮抗剂来治疗焦虑症，例如恐慌症，广场恐怖症，强迫症，社交恐惧症，创伤后应激障碍，广泛性焦虑症，特异性恐惧症等。任选地与除了腺苷A2A受体拮抗剂之外的抗焦虑药组合。

2. 发明申请

WO2004058139A2 A METHOD OF TREATING BEHAVIORAL DISORDERS 审中-公开
标题翻译：治疗行为障碍的方法
公开(公告)号：WO2004058139A2
公开(公告)日：2004-07-15
申请号：PCT/IB2003/006455
申请日：2003-12-24
申请人： KYOWA HAKKO KOGYO CO., LTD. , SHIOZAKI, Shizuo , SHIMADA, Junichi , KASE, Hiroshi , SHINDO, Mayumi
发明人： SHIOZAKI, Shizuo , SHIMADA, Junichi , KASE, Hiroshi , SHINDO, Mayumi
IPC分类号： A61K
CPC分类号： A61K31/52 , A61K31/522
摘要： The present invention provides a method of treating behavioral disorders such as attention deficit hyperactivity disorder, comprising administering an effective amount of (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methylxanthine or a pharmaceutically acceptable salt thereof to a patient in need thereof and the like.
摘要翻译：本发明提供治疗诸如注意缺陷多动障碍的行为障碍的方法，其包括给予有效量的（E）-8-（3,4-二甲氧基苯乙烯基）-1,3-二乙基-7-甲基黄嘌呤或其药学上可接受的其盐给有需要的患者等。

3. 发明申请

WO2004019949A1 ADENOSINE A2A RECEPTOR ANTAGONISTS FOR TREATING RESTLESS LEGS SYNDROME OR RELATED DISORDERS 审中-公开
标题翻译：腺苷A2A受体拮抗剂治疗无症状综合症或相关疾病
公开(公告)号：WO2004019949A1
公开(公告)日：2004-03-11
申请号：PCT/US2003/026644
申请日：2003-08-27
申请人： KYOWA HAKKO KOGYO CO. LTD. , KASE, Hiroshi , SENO, Naoki , MORI, Akihisa , ZHAO, Dayao
发明人： KASE, Hiroshi , SENO, Naoki , MORI, Akihisa , ZHAO, Dayao
IPC分类号： A61K31/522
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 A 2A receptor antagonist to a patient in need thereof. More preferably the adenosine A 2A 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。

4. 发明公开

EP1738766A1 PREVENTIVE AND/OR THERAPEUTIC AGENT FOR DISEASE ACCOMPANIED BY CHRONIC MUSCLE/SKELETON PAIN 审中-公开
标题翻译：剂预防和/或治疗慢性/骨痛病杂志
公开(公告)号：EP1738766A1
公开(公告)日：2007-01-03
申请号：EP05727903.6
申请日：2005-03-30
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： KASE, Hiroshi , TAKAHASHI, Isami , KUNORI, Shunji , KOBAYASHI, Minoru , SHIOZAKI, Shizuo , SHIRAKURA, Shiro
IPC分类号： A61K45/00 , A61K31/522 , A61P3/00 , A61P19/02 , A61P19/04 , A61P21/00 , A61P29/00 , A61P43/00 , C07D473/06 , C07D473/12
CPC分类号： A61K31/522 , C07D473/06 , Y02A50/401
摘要： A prophylactic and/or therapeutic agent for diseases accompanied by chronic musculoskeletal pain comprising as an active ingredient a compound having an adenosine A 2A receptor antagonistic action, for example, represented by the following formula (I) (wherein R 1 , R 2 and R 3 are the same or different, each representing a hydrogen atom, lower alkyl, lower alkenyl or lower alkynyl; R 4 represents cycloalkyl, -(CH 2 ) n -R 5 or the following formula (II); and X 1 and X 2 are the same or different, each representing an oxygen atom or a sulfur atom) or a pharmaceutically acceptable salt thereof.
摘要翻译：对于疾病的预防和/或治疗剂由慢性肌肉骨骼疼痛，包括如上活性成分的陪同具有腺苷A 2A受体拮抗作用，对于实施例的化合物，由下式（I）（其中，R 1，R 2和R所表示 3相同或不同，各自表示氢原子，低级烷基，低级烯基或低级炔基; R 4 darstellt环烷基， - （CH 2）n的-R 5或下述通式（II）;和X 1和X 2 是相同的或不同的，各自为氧原子或硫原子）的化合物或其药学上可接受的盐表示。

5. 发明公开

EP1655029A1 MEDICINAL COMPOSITIONS 有权
标题翻译： MEDIZINISCHE ZUSAMMENSETZUNGEN
公开(公告)号：EP1655029A1
公开(公告)日：2006-05-10
申请号：EP04748023.1
申请日：2004-07-22
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： KASE, Hiroshi , KOBAYASHI, Minoru c/oPharm. Research Center , SHIOZAKI, Shizuo c/o Pharm, Research Center , MORI, Akihisa c/o Head Office , SENO, Naoki c/o Pharm. Research Center
IPC分类号： A61K31/52 , A61K31/137 , A61K31/335 , A61K31/343 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/435 , A61K31/496 , A61K31/5375 , A61K31/55 , A61K31/553 , 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 A 2A 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-HT 2 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）-1,3 - 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-HT 2拮抗剂等）等。

6. 发明公开

EP1709966A1 PREVENTIVE AND/OR THERAPEUTIC AGENT FOR HIGHER BRAIN DYSFUNCTION 审中-公开
标题翻译： PROPHYLAKTISCHES UND / ODER THERAPEUTISCHES MITTELFÜRHÖHEREGEHIRNFUNKTIONSSTÖRUNGEN
公开(公告)号：EP1709966A1
公开(公告)日：2006-10-11
申请号：EP04807124.5
申请日：2004-12-09
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： KASE, Hiroshi , NAKAGAWA, Yutaka , SHIOZAKI, Shizuo KYOWA HAKKO KOGYO CO.,LTD , KOBAYASHI, Minoru KYOWA HAKKO KOGYO CO.,LTD , TOKI, Shinichiro KYOWA HAKKO KOGYO CO.,LTD , SENO, Naoki KYOWA HAKKO KOGYO CO.,LTD , IKEDA, Ken
IPC分类号： A61K31/522 , A61P25/28 , C07D473/12 , C07D473/06
CPC分类号： C07D473/06 , A61K31/522
摘要： (wherein R 1 , R 2 and R 3 are the same or different, and represent a hydrogen atom, lower alkyl, lower alkenyl or lower alkynyl; R 4 represents cycloalkyl, -(CH 2 ) n -R 5 or a group represented by the above formula (II) ; and X 1 and X 2 are the same or different, and represent an oxygen atom or a sulfur atom)
The present invention provides, for example, agents for preventing and/or treating higher brain dysfunction comprising, as an active ingredient, a xanthine derivative represented by the above formula (I) or a pharmaceutically acceptable salt thereof.
摘要翻译：（其中R 1，R 2和R 3相同或不同，表示氢原子，低级烷基，低级烯基或低级炔基; R 4表示环烷基， - （CH 2）n -R 5或由上述式（II）; X 1和X 2相同或不同，表示氧原子或硫原子）本发明提供例如用于预防和/或治疗较高脑功能障碍的药剂，其包含：作为活性成分，上述式（I）表示的黄嘌呤衍生物或其药学上可接受的盐。

7. 发明公开

EP0303697A1 DERIVATIVES OF PHYSIOLOGICALLY ACTIVE SUBSTANCE K-252 失效
标题翻译： DERIVATE DES PHYSIOLOGISCH AKTIVEN MITTELS K-252。
公开(公告)号：EP0303697A1
公开(公告)日：1989-02-22
申请号：EP87901672.3
申请日：1987-03-09
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： MURAKATA, Chikara , SATO, Akira , TAKAHASHI, Mitsuru , KOBAYASHI, Eiji , MORIMOTO, Makoto , AKINAGA, Shiro , HIRATA, Tadashi , MOCHIDA, Kenichi , KASE, Hiroshi , YAMADA, Koji , IWAHASHI, Kazuyuki
IPC分类号： C07D498/22 , A61K31/55
CPC分类号： C07D498/22
摘要： Novel derivatives of K-252 ((8R', 9S*, 11S')-(-)-9-hydroxy-9-methoxycarbonyl-8-methyl-2,3,9,10-tetrahydro-8,11-epoxy-1H,8H,11H-2,7b,11a-triazadibenzo[a,g]cycloocta[cde]trinden-1-one) represented by formula (l) (wherein W 1 , W 2 , R 1 , R 2 , R 3 , R 4 , X, and Y represent various substituents) are disclosed. These compounds are physiologically active substances having a protein kinase C-inhibiting activity and an oncostatic activity, thus being useful as medicines.
摘要翻译：抗生素K-252衍生物。式（I）的化合物是新的：在（I）中，R 1和R 3是OH，低级烷氧基或氨基，或R 3是H，R 1是H，Me，OH，Br，Cl，羟甲基，NR 5 R 6等; R2是H或氨基; 一个或R 5 / R 6是H，另一个是H，氨基甲酰基或低级烷基氨基羰基，或者R 5和R 6都是低级烷基; R4是H，C1，氨基甲酰基，低级烷基，氨基或-CH2CH2R7; R7是Br，氨基，羟基，二（低级烷基）氨基或羟基。低级烷基氨基; W1和W2为H或一起为= O; X是H，甲酰基，低级烷氧基羰基，-CONR 8 R 9，-CH 2 A或-CH = NR 12; R8和R9是H，低级烷基，羟基。低级烷基或R8是H，R9是OH; A是OH，叠氮基，低级烷硫基，低级烷基磺酰基，-NR10R11，-N = CHNMe2，-OCOCH2CH2COOH或2-四氢吡喃基氧基; R10和R11都是H或一个是H，低级烷基，芳基，羧基 - 低级烷基等，xycar，另一个是低级烷基（选择C1-substd）。或R 10和R 11一起为-CH 2 CH 2 -B-CH 2 CH 2 - ; B是亚甲基，-NH-，S或O; R 12是OH，氨基，胍基或2-咪唑基氨基; Y是OH或氨基甲酰氧基; X和Y可以是（-XY-）-O-，-CH2O-，-CH2OCOO-，-CH2-O-CS-O-，-CH2-NR13-COO-，-CH2-N = CR14-O- 或-CH 2 -NH-CS-O-CH 2 -O-SO-O-; R 13是H，低级烷基，芳基，甲酰基甲基，-CH 2 CHOH-CH 2 OH或-CH 2 CH = N-NH-C（= NH）-NH 2; R 14是低级烷基或低级烷硫基。当W1 / W2 = 0时，R1 = R2 = R3 = H; 当R 4为低级烷基时，氨基或-CH 2 CH 2 R 7，则W1 / W2为= O。当Y是氨基甲酰氧基时，R1 = R2 = R3 = W1 = W2 = H，R4是氨基甲酰基，X是低级烷氧基羰基。当R4为C1时，R1 = R2 = R3 = W1 = W2 = H，X为低级烷氧基羰基。当X是H，甲酰基，-CONR 8 R 9，-CH 2 A或-CH = NR 12时，则R1 = R2 = R3 = W1 = W2 = R4 = H。当X是-CONHOH时，则R1 = R2 = R3 = R4 = H。 = R4 = H。

8. 发明公开

EP1709967A1 AGENTS FOR TREATING MIGRAINE 审中-公开
标题翻译： MITTEL ZUR BEHANDLUNG VONMIGRÄNE
公开(公告)号：EP1709967A1
公开(公告)日：2006-10-11
申请号：EP05704394.5
申请日：2005-01-28
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： TAKEUCHI, Megumi , TAKAYAMA, Makoto, c/o Pharma Research Center , SHIRAKURA, Shiro, Pharma Research Centre , KASE, Hiroshi
IPC分类号： A61K31/522 , A61P25/06 , C07D473/12 , C07D473/06
CPC分类号： A61K31/522 , C07D473/08
摘要： (wherein R 1 , R 2 and R 3 are the same or different, and represent a hydrogen atom, lower alkyl, lower alkenyl or lower alkynyl; R 4 represents cycloalkyl, -(CH 2 ) n -R 5 or a group represented by the above formula (II); and X 1 and X 2 are the same or different, and represent an oxygen atom or a sulfur atom)
The present invention provides, for example, agents for treating migraine comprising, as an active ingredient, a xanthine derivative represented by the above formula (I) or a pharmaceutically acceptable salt thereof.
摘要翻译：（其中R 1，R 2和R 3相同或不同，表示氢原子，低级烷基，低级烯基或低级炔基; R 4表示环烷基， - （CH 2）n -R 5或由上述式（II）; X 1和X 2相同或不同，表示氧原子或硫原子）本发明提供例如用于治疗偏头痛的药剂，其包含作为活性成分的黄嘌呤由上式（I）表示的衍生物或其药学上可接受的盐。

9. 发明公开

EP1631294A1 A METHOD OF TREATING AN ANXIETY DISORDER 有权
标题翻译：方法焦虑状态的方法
公开(公告)号：EP1631294A1
公开(公告)日：2006-03-08
申请号：EP04746014.2
申请日：2004-06-10
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： KASE, Hiroshi , SENO, Naoki , SHIOZAKI,Shizuo Pharma.Res.Center, , KOBAYASHI, Minoru Pharma.Res.Center , KASE, Junya Pharma.Res.Center
IPC分类号： A61K31/522 , A61K31/519 , A61P25/22
CPC分类号： A61K45/06 , A61K31/00 , A61K31/519 , A61K31/522 , A61K2300/00
摘要： Anxiety disorders, such as panic disorder, agoraphobia, obsessive-compulsive disorder, social phobia, post-traumatic stress disorder, generalized anxiety disorder, specific phobia, or the like, are treated by administering an effective amount of at least one adenosine A2A receptor antagonist to a patient in need thereof, optionally in combination with an anxiolytic(s) other than the adenosine A2A receptor antagonist.

10. 发明公开

EP1534289A1 ADENOSINE A2A RECEPTOR ANTAGONISTS FOR TREATING RESTLESS LEGS SYNDROME OR RELATED DISORDERS 有权
标题翻译：腺苷A2A受体拮抗剂不宁腿综合征或夜间肌阵挛的治疗
公开(公告)号：EP1534289A1
公开(公告)日：2005-06-01
申请号：EP03791769.7
申请日：2003-08-27
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： KASE, Hiroshi , SENO, Naoki , MORI, Akihisa , ZHAO, Dayao
IPC分类号： A61K31/522 , 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.

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