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    2-AMINOBICYCLO 3.1.0 HEXANE-2,6-DICARBOXYLIC ESTER DERIVATIVE
    3.
    发明授权
    2-AMINOBICYCLO 3.1.0 HEXANE-2,6-DICARBOXYLIC ESTER DERIVATIVE 有权
    2-AMINOBICYCLO 3.1.0己烷-2,6-二羧酸酯衍生物

    公开(公告)号：EP1637517B1

    公开(公告)日：2010-11-10

    申请号：EP04746867.3

    申请日：2004-06-25

    申请人： Taisho Pharmaceutical Co., Ltd.

    发明人： YASUHARA, Akito ,  SAKAGAMI, Kazunari ,  OHTA, Hiroshi ,  NAKAZATO, Atsuro

    IPC分类号： C07C229/50 ,  C07C235/06 ,  C07C247/04 ,  C07C323/61 ,  A61K31/216 ,  A61K31/365 ,  A61K31/357 ,  C07D307/88 ,  C07D317/34 ,  A61P9/10 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00

    CPC分类号： C07C229/50 ,  C07D307/88

    摘要： A drug which is effective in treatments for and prevention of schizophrenia, anxiety, and diseases related to these, i.e., psychiatrical disorders such as depression, bipolar disorder, and epilepsy. The drug has high activity in oral administration and has an antagonistic effect on a Group II metabotropic glutamate receptor. It is a 2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by the formula [I]: [I] [wherein R1 and R2 are the same or different and each represents hydrogen, C1-10 alkyl, etc.; X represents hydrogen or fluorine; and Y represents, e.g., -OCHR3R4 (wherein R3 and R4 are the same or different and each represents hydrogen, C1-10 alkyl, etc. and n is an integer of 1 or 2)], a pharmaceutically acceptable salt of the derivative, or a hydrate of either.

    摘要翻译： 对治疗和预防精神分裂症，焦虑症和与这些有关的疾病，即抑郁症，双相性精神障碍和癫痫等精神病症有效的药物。 该药在口服给药中具有高活性，并对II组代谢型谷氨酸受体具有拮抗作用。 它是由式[I]表示的2-氨基二环[3.1.0]己烷-2,6-二羧酸酯衍生物：[I] [其中R1和R2相同或不同，各代表氢，C1-10烷基 等; X代表氢或氟; Y表示例如-OCHR 3 R 4（其中R 3和R 4相同或不同，并且各自表示氢，C 1-10烷基等，并且n是1或2的整数）]，衍生物的药学上可接受的盐， 或任一种的水合物。

    PROCESS FOR PRODUCING BICYCLOCARBOXYLIC ACID DERIVATIVE
    5.
    发明公开
    PROCESS FOR PRODUCING BICYCLOCARBOXYLIC ACID DERIVATIVE 审中-公开
    生产双环羧酸衍生物的方法

    公开(公告)号：EP1369408A1

    公开(公告)日：2003-12-10

    申请号：EP02702875.2

    申请日：2002-03-11

    申请人： TAISHO PHARMACEUTICAL CO., LTD

    发明人： NAKAZATO, Atsuro ,  KUMAGAI, Toshihito ,  SAKAGAMI, Kazunari

    IPC分类号： C07C51/377 ,  C07C62/24 ,  C07C67/327 ,  C07C69/757

    CPC分类号： C07C51/377 ,  C07C67/327 ,  C07C2602/18 ,  Y02P20/55 ,  C07C62/24 ,  C07C69/757

    摘要： A process for producing a 2-oxobicyclo[3.1.0]hex-3-ene-6-carboxylic acid derivative represented by a formula:
    (wherein R 1 represents a hydrogen atom, a C 1-6 alkyl group, a C 3-6 cycloalkyl group, a C 3-6 cycloalkyl C 1-6 alkyl group, a C 1-6 alkyl group substituted with a substituted or unsubstituted phenyl group, a C 1-6 alkoxy C 1-6 alkyl group, a C 1-6 hydroxyalkyl group, a C 1-6 alkylthio C 1-6 alkyl group, a C 1-6 mercaptoalkyl group, or a substituted or unsubstituted phenyl group)
    characterized by reacting a 4-hydroxy-2-oxobicyclo[3.1.0]hexane-6-carboxylic acid derivative represented by a formula:
    (wherein R 1 has the same meaning as described above, and R 2 represents a hydrogen atom or a protective group of a hydroxyl group)
    in the presence of an acid or a base.
    A process for producing the compounds which are useful for efficient syntheses of 2-amino-3-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acids is provided.

    摘要翻译： 一种制备下式代表的2-氧代双环[3.1.0]己-3-烯-6-羧酸衍生物的方法：（其中R1代表氢原子，C1-6烷基，C3-6环烷基 ，C3-6环烷基C1-6烷基，被取代或未取代的苯基取代的C1-6烷基，C1-6烷氧基C1-6烷基，C1-6羟烷基，C1-6烷硫基 C 1-6烷基，C 1-6巯基烷基或取代或未取代的苯基），其特征在于使由下式表示的4-羟基-2-氧代双环[3.1.0]己烷-6-羧酸衍生物 其中R1具有与上述相同的含义，并且R2表示氢原子或羟基的保护基团）在酸或碱存在下反应。 提供了用于有效合成2-氨基-3-氟二环[3.1.0]己烷-2,6-二羧酸的化合物的制备方法。

    1-NAPHTHYL ALKYLPIPERIDINE DERIVATIVE
    8.
    发明公开
    1-NAPHTHYL ALKYLPIPERIDINE DERIVATIVE 审中-公开
    1-萘基烷基哌啶衍生物

    公开(公告)号：EP2098509A1

    公开(公告)日：2009-09-09

    申请号：EP07829299.2

    申请日：2007-10-05

    申请人： Taisho Pharmaceutical Co. Ltd.

    发明人： SEKIGUCHI, Yoshinori ,  KANUMA, Kosuke ,  SAKAGAMI, Kazunari ,  HAYASHI, Masato ,  KASHIWA, Shuhei ,  OMODERA, Katsunori

    IPC分类号： C07D211/58 ,  A61K31/4468 ,  A61K31/453 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P9/12 ,  A61P25/08 ,  A61P25/14 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28

    CPC分类号： C07D405/12 ,  C07D211/58 ,  C07D401/10 ,  C07D401/12 ,  C07D405/10 ,  C07D409/12

    摘要： Disclosed is a pharmaceutical composition comprising a compound represented by the formula (I)

    or a pharmaceutically acceptable salt thereof as an active ingredient, which has an antagonistic activity on a melanin-concentrating hormone receptor. The pharmaceutical composition is useful, due to its antagonistic activity on a MCH receptor, for the prevention or treatment of a disease such as depression, anxiety disorders (e.g., generalized anxiety disorder, post traumatic stress disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder), attention deficit disorder, mania, manic-depressive disorder, schizophrenia, mood disorders, stress, sleep disorder, attacks, memory impairment, cognitive impairment, dementia, amnesia, delirium, obesity, eating disorder, appetite disorder, hyperphagia, bulimia, cibophobia, diabetes, a cardiovascular diseases, hypertension, dyslipidemia, cardiac infarction, movement disorder (e.g., Parkinson's disease, epilepsy, convulsion, tremor), drug abuse and drug addiction.

    摘要翻译： 本发明公开了一种药物组合物，其包含式（I）所示的化合物或其药学上可接受的盐作为活性成分，其对黑色素浓集激素受体具有拮抗活性。 由于其对MCH受体的拮抗活性，所述药物组合物用于预防或治疗疾病如抑郁症，焦虑症（例如广泛性焦虑症，创伤后应激障碍，恐慌症，强迫症， 社交焦虑障碍），注意力缺陷障碍，躁狂症，躁狂抑郁症，精神分裂症，情绪障碍，压力，睡眠障碍，发作，记忆障碍，认知障碍，痴呆，遗忘症，deli妄，肥胖症，进食障碍，食欲不振， 贪食症，视力障碍，糖尿病，心血管疾病，高血压，血脂异常，心肌梗塞，运动障碍（例如帕金森病，癫痫，惊厥，震颤），药物滥用和药物成瘾。