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    • 3. 发明申请
    • ADENOSINE INCORPORATION INHIBITOR
    • 腺苷合成抑制剂
    • WO1994019342A1
    • 1994-09-01
    • PCT/JP1994000229
    • 1994-02-16
    • KYOWA HAKKO KOGYO CO., LTD.FUJIWARA, ShigekiMACHII, DaisukeTAKAI, HarukiNONAKA, HiromiKASE, HiroshiYAO, KozoKAWAKAGE, MichiyoKUSAKA, HideakiKARASAWA, Akira
    • KYOWA HAKKO KOGYO CO., LTD.
    • C07D401/14
    • C07D401/14C07D491/04
    • An adenosine incorporation inhibitor and a drug for protecting cardiac muscles or preventing or treating inflammatory edema, each containing as the active ingredient a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, wherein R represents hydrogen, (un)substituted lower alkyl, alkenyl or (un)substituted aralkyl; R , R , R and R represent each independently hydrogen, halogen, amino, mono- or di(lower alkyl) amino, lower alkanoyl amino, nitro, cyano, (un)substituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy or lower alkanoyloxy; R , R , R and R represent each independently hydrogen, hydroxy, (un)substituted lower alkoxy or aralkyloxy, or alternatively the two adjacent groups among them may be combined together to represent methylenedioxy; R represents hydrogen or lower alkyl; and Y and Z represent each independently N or C-R'', wherein R'' represents hydrogen, (un)substituted lower alkyl or halogen.
    • 一种腺苷并入抑制剂和用于保护心肌或预防或治疗炎症性水肿的药物,每种含有作为活性成分的通式(I)表示的1,2,3,4-四氢-2,4-二氧代喹唑啉衍生物或 其中R 1表示氢,(取代的)取代的低级烷基,烯基或(未)取代的芳烷基; R 2,R 3,R 4和R 5各自独立地表示氢,卤素,氨基,一或二(低级烷基)氨基,低级烷酰氨基,硝基,氰基,(取代) 低级烷基,羟基,低级烷氧基,低级烷硫基,羧基,低级烷氧基羰基,低级烷酰基,芳烷氧基或低级烷酰氧基; R 6,R 7,R 8和R 9各自独立地表示氢,羟基,(未)取代的低级烷氧基或芳烷氧基,或者它们中的两个相邻基团可以组合在一起代表亚甲二氧基 ; R 10代表氢或低级烷基; 并且Y和Z各自独立地表示N或C-R“,其中R”表示氢,(un)取代的低级烷基或卤素。
    • 5. 发明申请
    • METHODS OF TREATING PATIENTS SUFFERING FROM MOVEMENT DISORDERS
    • 治疗运动障碍患者的方法
    • WO03063876A2
    • 2003-08-07
    • PCT/US0302658
    • 2003-01-28
    • KASE HIROSHIMORI AKIHISAWAKI YUTAKAOHSAWA YUTAKAKARASAWA AKIRAKUWANA YOSHITOSHI
    • KASE HIROSHIMORI AKIHISAWAKI YUTAKAOHSAWA YUTAKAKARASAWA AKIRAKUWANA YOSHITOSHI
    • C07D473/06A61K31/522A61K45/00A61P25/14A61P25/16
    • 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 antagonist 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 LDOPA 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。 本发明还提供了通过将LDOPA治疗与有效量的一种或多种腺苷A2A受体拮抗剂(即L-DOPA备用效应)组合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,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。
    • 6. 发明申请
    • THERAPEUTIC AGENT FOR KIDNEY DISEASES
    • 用于治疗疾病的治疗剂
    • WO1997029749A1
    • 1997-08-21
    • PCT/JP1997000439
    • 1997-02-19
    • KYOWA HAKKO KOGYO CO., LTD.FUJIWARA, ShigekiOKAMURA, YukoTAKAI, HarukiNONAKA, HiromiMORIYAMA, TakahiroYAO, KozoKARASAWA, Akira
    • KYOWA HAKKO KOGYO CO., LTD.
    • A61K31/505
    • C07D401/14A61K31/517A61K31/5377A61K31/541A61K31/55
    • A therapeutic agent for kidney diseases which comprises as the active ingredient a quinazoline derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, wherein R represents hydrogen, lower alkyl, alkenyl, aralkyl, etc.; R , R , R , and R may be the same or different and each represents hydrogen, lower alkyl, lower alkoxy, lower alkanoyl, etc.; R , R , R , and R may be the same or different and each represents hydrogen, lower alkyl, lower alkoxy, aralkyloxy, lower alkanoyloxy, etc., or adjacent two of these may be bonded to each other to thereby form methylenedioxy, etc.; R represents hydrogen, lower alkyl, etc.; R and R may be the same or different and each represents hydrogen, lower alkyl, cycloalkyl, phenyl, aralkyl, etc., or R and R may be bonded to each other to thereby form a heterocycle with the nitrogen atom; and n is 0, 1, or 2. The therapeutic agent is useful for the prevention or treatment of kidney diseases such as nephritis and diabetic nephropathy.
    • 作为肾脏疾病的治疗剂,其含有作为活性成分的通式(I)表示的喹唑啉衍生物或其药理学上可接受的盐,其中R 1表示氢,低级烷基,烯基,芳烷基等; R 2,R 3,R 4和R 5可以相同或不同,各自代表氢,低级烷基,低级烷氧基,低级烷酰基等; R 6,R 7,R 8和R 9可以相同或不同,各自表示氢,低级烷基,低级烷氧基,芳烷氧基,低级烷酰氧基等,或相邻的两个 可以彼此键合从而形成亚甲二氧基等; R 10代表氢,低级烷基等; R 11和R 12可以相同或不同,各自表示氢,低级烷基,环烷基,苯基,芳烷基等,或者R 11和R 12可以彼此键合,从而 与氮原子形成杂环; 并且n为0,1或2.治疗剂可用于预防或治疗肾脏疾病如肾炎和糖尿病性肾病。
    • 8. 发明申请
    • QUINAZOLINE DERIVATIVE
    • 喹诺酮衍生物
    • WO1996006841A1
    • 1996-03-07
    • PCT/JP1995001694
    • 1995-08-25
    • KYOWA HAKKO KOGYO CO., LTD.FUJIWARA, ShigekiOKAMURA, YukoTAKAI, HarukiNONAKA, HiromiMORIYAMA, TakahiroYAO, KozoKARASAWA, Akira
    • KYOWA HAKKO KOGYO CO., LTD.
    • C07D401/14
    • C07D401/14
    • A quinazoline derivative represented by general formula (I) or a pharmacologically acceptable salt thereof (wherein R represents hydrogen, lower alkyl, alkenyl or aralkyl; R , R , R and R represent each hydrogen, lower alkyl, lower alkoxy, lower alkanolyl, etc.; R , R , R and R represent each hydrogen, lower alkyl, lower alkoxy, aralkyloxy, etc., or two adjacent members thereof are combined together to represent methylenedioxy, etc; R represents hydrogen, lower alkyl, etc.; R and R either represent each hydrogen, lower alkyl, cycloalkyl, phenyl or aralkyl, or are combined together with the nitrogen atom to which they are bonded to represent a heterocyclic group; and n represents 0, 1 or 2). The compound has the effect of inhibiting adenosine incorporation and is useful for protecting cardiac muscles and preventing or treating inflammations such as podedema.
    • 由通式(I)表示的喹唑啉衍生物或其药理学上可接受的盐(其中R 1表示氢,低级烷基,烯基或芳烷基; R 2,R 3,R 4和R 5 代表每个氢,低级烷基,低级烷氧基,低级链烷酰基等; R 6,R 7,R 8和R 9分别表示氢,低级烷基,低级烷氧基,芳烷氧基等。 或其两个相邻的成员结合在一起代表亚甲二氧基等; R 10代表氢,低级烷基等; R 11和R 12分别表示氢,低级烷基,环烷基,苯基或芳烷基 ,或与它们所键合的氮原子一起表示杂环基; n表示0,1或2)。 该化合物具有抑制腺苷掺入的作用,并且可用于保护心肌和预防或治疗诸如肝硬化的炎症。