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    4-TETRAHYDROPYRIDYLPYRIMIDINE DERIVATIVES
    3.
    发明公开
    4-TETRAHYDROPYRIDYLPYRIMIDINE DERIVATIVES 失效
    4- TETRAHYDROPYRIDYLPYRIMIDIN衍

    公开(公告)号：EP0976745A1

    公开(公告)日：2000-02-02

    申请号：EP98911002.8

    申请日：1998-03-25

    申请人： TAISHO PHARMACEUTICAL CO. LTD

    发明人： NAKAZATO, Atsuro, Taisho Pharmaceutical Co., Ltd ,  KUMAGAI, Toshihito, Taisho Pharmaceutical Co., Ltd ,  OKUBO, Taketoshi, Taisho Pharmaceutical Co., Ltd ,  AIBE, Izumi, Taisho Pharmaceutical Co., Ltd ,  TANAKA, Hideo, Taisho Pharmaceutical Co., Ltd ,  CHAKI, Shigeyuki, Taisho Pharmaceutical Co., Ltd ,  OKUYAMA, Shigeru, Taisho Pharmaceutical Co., Ltd ,  TOMISAWA, Kazuyuki, Taisho Pharmaceutical Co., Ltd

    IPC分类号： C07D401/04 ,  A61K31/505

    CPC分类号： C07D401/04 ,  C07D405/14 ,  C07D409/14

    摘要： A 4-tetrahydropyridylpyrimidine derivative represented by formula (I):
    wherein Ar represents a phenyl group substituted with 1 to 3 substituents selected from a halogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, and a trifluoromethyl group, a phenyl group, a thienyl group or a furanyl group; R 1 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an amino group or an amino group substituted with 1 or 2 alkyl groups having 1 to 5 carbon atoms; R 2 represents an alkyl group having 1 to 5 carbon atoms, a cycloalkylalkyl group having 4 to 7 carbon atoms, an alkenyl group having 2 to 5 carbon atoms or an alkynyl group having 2 to 5 carbon atoms; and X 1 , X 2 , and X 3 , which may be the same or different, each represent a hydrogen atom, a halogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, an alkylthio group having 1 to 5 carbon atoms, an amino group or an amino group substituted with 1 or 2 alkyl groups having 1 to 5 carbon atoms, or a pharmaceutically acceptable salt thereof.
    The invention provides a compound effective on diseases which CRF is considered to participate in, such as depression, anxiety, Alzheimer's disease, Parkinson's syndrome, Huntington's chorea, eating disorders, hypertension, digestive diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head wounds, inflammation, and immunity-associated diseases.

    摘要翻译： 由式（I）表示的4-四氢吡啶基嘧啶衍生物：其中Ar表示被1至3个选自卤素原子，具有1至5个碳原子的烷基，1至5个碳原子的烷氧基取代的苯基 碳原子和三氟甲基，苯基，噻吩基或呋喃基; R 1表示氢原子，碳原子数1〜5的烷基，氨基或被1或2个碳原子数1〜5的烷基取代的氨基。 R 2表示碳原子数1〜5的烷基，碳原子数4〜7的环烷基烷基，碳原子数2〜5的烯基或碳原子数2〜5的炔基。 X 1，X 2和X 3可以相同或不同，分别表示氢原子，卤原子，碳原子数为1〜5的烷基，烷氧基为1 至5个碳原子，具有1至5个碳原子的烷硫基，氨基或被1或2个具有1至5个碳原子的烷基取代的氨基或其药学上可接受的盐。 本发明提供了一种对CRF被认为参与抑郁，焦虑，阿尔茨海默病，帕金森综合征，亨廷顿氏舞蹈病，进食障碍，高血压，消化系统疾病，药物依赖，癫痫，脑梗塞，脑缺血， 脑水肿，头部创伤，炎症和免疫相关疾病。

    OPTICALLY ACTIVE SUBSTITUTED PHENYLALKYLAMINE DERIVATIVES
    5.
    发明公开
    OPTICALLY ACTIVE SUBSTITUTED PHENYLALKYLAMINE DERIVATIVES 失效
    OPTISCH AKTIVE SUBSTITUIERTE PHENYLALKYLAMIN-DERIVATE

    公开(公告)号：EP0870758A1

    公开(公告)日：1998-10-14

    申请号：EP96917670.0

    申请日：1996-06-13

    申请人： TAISHO PHARMACEUTICAL CO. LTD

    发明人： NAKAZATO, Atsuro, Taisho Pharmaceutical Co., Ltd ,  KUMAGAI, Toshihito, Taisho Pharmaceutical Co., Ltd ,  MIYAZAWA, Tomoki, Taisho Pharmaceutical Co., Ltd ,  OHTA, Koumei, Taisho Pharmaceutical Co., Ltd ,  KAWASHIMA, Yutaka, Taisho Pharmaceutical Co., Ltd ,  HATAYAMA, Katsuo, Taisho Pharmaceutical Co., Ltd

    IPC分类号： C07C217/60 ,  C07D333/16 ,  A61K31/135 ,  A61K31/38 ,  C07C217/62

    CPC分类号： C07C271/16 ,  C07C217/60 ,  C07C217/62 ,  C07D333/16

    摘要： The present invention relates to an optically active, substituted phenylalkylamine derivative represented by Formula [1]:
       wherein A is a substituted or non-substituted phenyl or thienyl; X 1 is hydrogen, halogen, hydroxyl or a substituted or non-substituted C 1-5 alkoxy; R 1 and R 2 are equally or differently hydrogen, C 1-7 alkyl, C 3-7 alkenyl or C 3-7 alkynyl; R 3 is C 1-10 alkyl, C 2-10 alkenyl or C 2-10 alkynyl; n is an integer from 2 to 5; and m is an integer from 1 to 4,
    or a pharmaceutically acceptable salt thereof, and pharmaceutical use of such compound or salt. The compound of the invention is excellent in sigma 1 receptor antagonism and useful for treating schizophrenia, depression, anxiety, cerebrovascular diseases/senile troublesome behaviors, and cognitive dysfunctions and motor dysfunctions such as Alzheimer's disease, Parkinson's disease and Huntington's disease which are neurodegenerative diseases. Further, the compound of the invention is also useful for treating dependence resulted from drug abuse.

    摘要翻译： 本发明涉及由式Ä1Ü表示的光学活性的取代的苯基烷基胺衍生物：其中A是取代或未取代的苯基或噻吩基; X 1是氢，卤素，羟基或取代或未取代的C 1-5烷氧基; R 1和R 2同样或不同的是氢，C 1-7烷基，C 3-7烯基或C 3-7炔基; R 3是C 1-10烷基，C 2-10烯基或C 2-10炔基; n是2至5的整数; 和m为1〜4的整数，或其药学上可接受的盐，以及该化合物或盐的药物用途。 本发明的化合物在σ1受体拮抗作用方面优异，可用于治疗精神分裂症，抑郁症，焦虑症，脑血管疾病/老年麻醉行为，以及认知功能障碍和运动功能障碍如阿尔茨海默氏病，帕金森病和亨廷顿舞蹈病，这些都是神经变性疾病。 此外，本发明的化合物还可用于治疗药物滥用所引起的依赖性。

    NOVEL CARBOXYLIC ACID DERIVATIVES AND PROCESS FOR PRODUCING THE SAME
    6.
    发明授权
    NOVEL CARBOXYLIC ACID DERIVATIVES AND PROCESS FOR PRODUCING THE SAME 有权
    CARBONSÄUREDERIVATEUND VERFAHREN ZU IHRER HERSTELLUNG

    公开(公告)号：EP1164121B1

    公开(公告)日：2008-10-29

    申请号：EP00904066.8

    申请日：2000-02-21

    申请人： TAISHO PHARMACEUTICAL CO., LTD

    发明人： NAKAZATO, Atsuro, Taisho Pharmaceutical Co., Ltd ,  KUMAGAI, Toshihito, Taisho Pharmaceutical Co., Ltd ,  SAKAGAMI, Kazunari, Taisho Pharmaceutical Co., Ltd ,  TOMISAWA, Kazuyuki, Taisho Pharmaceutical Co., Ltd

    IPC分类号： C07C51/373 ,  C07C62/26 ,  C07D235/02 ,  C07F7/18 ,  C07C65/40 ,  C07C69/757 ,  C07D339/06 ,  C07D495/10

    CPC分类号： C07D235/02 ,  C07C62/26 ,  C07C65/40 ,  C07C69/757 ,  C07C2602/18 ,  C07D339/06 ,  C07D495/10

    摘要： Compounds which are useful in the efficient synthesis of 2-amino-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acid. The compounds are 2-oxobicyclo[3.1.0]hexane-6-carboxylic acid derivatives represented by formula (1) [wherein R1 represents hydrogen, C¿1-6? alkyl, C3-6 cycloalkyl, C1-6 alkyl substituted by C3-6 cycloalkyl, aryl, C1-6 alkyl substituted by aryl, C1-6 alkyl substituted by C1-6 alkoxy, C1-6 hydroxyalkyl, C1-6 alkyl substituted by C1-6 alkylthio, C1-6 mercaptoalkyl, tetrahydrofuranyl, or tetrahydropyranyl; R?2 and R3¿ are the same or different and each represents C¿1-6? alkyl, C3-6 cycloalkyl, C1-6 alkyl substituted by C3-6 cycloalkyl, aryl, or C1-6 alkyl substituted by aryl, or R?2 and R3¿ in combination represent -(CH¿2?)n- (n is 2 or 3); and Y?1 and Y2¿ are the same or different and each represents sulfur, oxygen, or nitrogen].

    摘要翻译： 本发明涉及可用于高效合成2-氨基-4-氧代二环[3.1.0]己烷-2,6-二羧酸的化合物。 根据本发明的化合物包含由下式表示的2-氧代双环[3.1.0]己烷-6-羧酸衍生物：其中R 1表示氢原子，C 1 -C 6烷基，C 3 C 6环烷基，C 3 -C 6环烷基C 1 -C 6烷基，芳基，芳基C 1 -C 6烷基，C 1 -C 6烷氧基C 1 -C 6烷基，C 1 -C 6羟基烷基，C 1 -C 6 烷硫基C1-C6烷基，C1-C6巯基烷基，四氢呋喃基或四氢吡喃基; R 2和R 3相同或不同，各自表示C1-C6烷基，C3-C6环烷基，C3-C6环烷基C1-C6烷基，芳基或芳基C1 -C 6烷基，或者R 2和R 3一起表示 - （CH 2）n - （其中n表示2或3）; Y 1和Y 2相同或不同，各自表示硫原子，氧原子或氮原子。

    NOVEL DICARBOXYLIC ACID DERIVATIVES
    7.
    发明公开
    NOVEL DICARBOXYLIC ACID DERIVATIVES 审中-公开
    使用DICARBONSÄUREDERIVATE

    公开(公告)号：EP1295865A1

    公开(公告)日：2003-03-26

    申请号：EP01945657.3

    申请日：2001-06-28

    申请人： TAISHO PHARMACEUTICAL CO., LTD

    发明人： NAKAZATO, Atsuro, Taisho Pharmaceutical Co., Ltd. ,  KUMAGAI, Toshihito, Taisho Pharmaceutical Co., Ltd ,  KANUMA, Kosuke, Taisho Pharmaceutical Co., Ltd. ,  SAKAGAMI, Kazunari, Taisho Pharmaceutical Co., Ltd

    IPC分类号： C07C229/50 ,  A61K31/198 ,  A61K31/223 ,  A61P9/10 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P43/00

    CPC分类号： C07C229/50 ,  C07C2602/18

    摘要： The present invention relates to 2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives represented by the formula:
    the pharmaceutically acceptable salts thereof, or the hydrates thereof. The compounds of the present invention are useful as a medicament, and in particular, are useful as modulators acting on group 2 metabotropic glutamate receptors, having effects for treating and/or preventing psychiatric disorders such as schizophrenia, anxiety and its associated diseases, depression, bipolar disorder, and epilepsy; and/or neurological diseases such as drug dependence, cognitive disorders, Alzheimer's disease, Huntington's chorea, Parkinson's disease, dyskinesia associated with muscular stiffness, cerebral ischemia, cerebral failure, myelopathy, and head trauma.

    摘要翻译： 本发明涉及由下式表示的2-氨基-6-氟双环[3,3.1,0]己烷-2,6-二羧酸衍生物或其药学上可接受的盐或其水合物。 本发明的化合物可用作药物，特别是可用作作用于第2组代谢型谷氨酸受体的调节剂，具有治疗和/或预防精神疾病如精神分裂症，焦虑及其相关疾病，抑郁症， 双相障碍和癫痫; 和/或神经系统疾病如药物依赖性，认知障碍，阿尔茨海默病，亨廷顿氏舞蹈病，帕金森病，与肌肉僵硬相关的运动障碍，脑缺血，脑衰竭，脊髓病和头部创伤。