利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

60 条记录 (耗时 0.032 秒)

    6-fluorobicyclo[3.1.0]hexane derivatives
    42.
    发明授权
    6-fluorobicyclo[3.1.0]hexane derivatives 有权
    6-氟二环[3.1.0]己烷衍生物

    公开(公告)号：US06333428B1

    公开(公告)日：2001-12-25

    申请号：US09763408

    申请日：2001-02-22

    申请人： Atsuro Nakazato ,  Toshihito Kumagai ,  Kazunari Sakagami ,  Kazuyuki Tomisawa

    发明人： Atsuro Nakazato ,  Toshihito Kumagai ,  Kazunari Sakagami ,  Kazuyuki Tomisawa

    IPC分类号： C07C6974

    CPC分类号： C07D317/72 ,  C07C229/50 ,  C07C2602/18 ,  C07D339/06

    摘要： The present invention provides fluorobicyclo[3.1.0]hexane derivatives represented by the formula [wherein R1 and R2 are the same or different and each represents a hydrogen atom, a C1-10 alkyl group, a C3-8 cycloalkyl group or a C3-8 cycloalkyl-C1-5 alkyl group: Y1 and Y2 are the same or different and each represents a hydrogen atom, a C1-10 alkylthio group, a C3-8 cycloalkylthio group, a C3-8 cycloalkyl-C1-5 alkylthio group, a C1-5 alkoxy group, a C3-8 cycloalkoxy group or a C3-8 cycloalkyl-C1-5 alkoxy group; or one represents a hydrogen atom and the other represents a hydroxyl group, a C1-5 alkoxy group, a C3-8 cycloalkoxy group or a C3-8 cycloalkyl-C1-5 alkoxy group; or Y1 and Y2 together represent an oxygen atom or —X(CH2)nX— (X represents an oxygen atom or a sulfur atom: N is 2 or 3)], pharmaceutically acceptable salts thereof, or hydrates thereof. The compounds of the present invention are useful as drugs, in particular group 2 metabotropic glutamate receptor agonists, and useful for treatment or prevention of psychiatric disorders such as, for example, schizophrenia, anxiety and associated diseases, depression, bipolar disorder, and epilepsy, as well as neurological diseases such as, for example, 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： 本发明提供由式[其中R 1和R 2相同或不同，表示氢原子，C 1-10烷基，C 3-8环烷基或C 3-8环烷基]表示的氟双环[3.1.0] 8环烷基-C 1-5烷基：Y1和Y2相同或不同，各自表示氢原子，C1-10烷硫基，C3-8环硫基，C3-8环烷基-C1-5烷硫基， C 1-5烷氧基，C 3-8环烷氧基或C 3-8环烷基-C 1-5烷氧基; 或者一个表示氢原子，另一个表示羟基，C 1-5烷氧基，C 3-8环烷氧基或C 3-8环烷基-C 1-5烷氧基; 或Y1和Y2一起表示氧原子或-X（CH 2）n X-（X表示氧原子或硫原子：N为2或3）]，其药学上可接受的盐或其水合物。本发明化合物 本发明可用作药物，特别是组2代谢型谷氨酸受体激动剂，并且可用于治疗或预防精神病学障碍，例如精神分裂症，焦虑和相关疾病，抑郁症，双相性精神障碍和癫痫以及神经系统疾病 例如药物依赖，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，脊髓损伤和头部创伤。

    2-AMINO-BICYCLO[3.1.0]HEXANE-2, 6-DICARBOXYLIC ESTER DERIVATIVE
    44.
    发明申请
    2-AMINO-BICYCLO[3.1.0]HEXANE-2, 6-DICARBOXYLIC ESTER DERIVATIVE 失效
    2-氨基双环[3.1.0]十六烷-2,6-二羧酸酯衍生物

    公开(公告)号：US20120028982A1

    公开(公告)日：2012-02-02

    申请号：US13269242

    申请日：2011-10-07

    申请人： Akito YASUHARA ,  Kazunari Sakagami ,  Hiroshi Ohta ,  Atsuro Nakazato

    发明人： Akito YASUHARA ,  Kazunari Sakagami ,  Hiroshi Ohta ,  Atsuro Nakazato

    IPC分类号： A61K31/5375 ,  C07C229/46 ,  C07D265/30 ,  C07C261/00 ,  A61K31/27 ,  A61K31/215

    CPC分类号： C07C229/50 ,  C07D307/88

    摘要： A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration. A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.

    摘要翻译： 一种有效治疗和预防精神疾病如精神分裂症，焦虑及其相关疾病，抑郁症，双相情感障碍和癫痫的药物。 该药物拮抗II型代谢型谷氨酸受体的作用，并且在口服给药中显示高活性。 由式[I]表示的2-氨基 - 双环[3.1.0]己烷-2,6-二羧酸酯衍生物[其中R 1和R 2相同或不同，各自表示氢原子，C 1-10烷基或 喜欢; X表示氢原子或氟原子; Y表示-OCHR 3 R 4等（其中R 3和R 4相同或不同，并且各自表示氢原子，C 1-10烷基等; n表示1或2的整数）]，其药学上可接受的盐或 水合物。

    2-AMINO-BICYCLO(3.1.0) HEXANE-2, 6-DICARBOXYLIC ESTER DERIVATIVE
    45.
    发明申请
    2-AMINO-BICYCLO(3.1.0) HEXANE-2, 6-DICARBOXYLIC ESTER DERIVATIVE 失效
    2-氨基双酚（3.1.0）HEXANE-2，6-二甲氧基硅烷衍生物

    公开(公告)号：US20100298561A1

    公开(公告)日：2010-11-25

    申请号：US12847392

    申请日：2010-07-30

    申请人： Akito YASUHARA ,  Kazunari Sakagami ,  Hiroshi Ohta ,  Atsuro Nakazato

    发明人： Akito YASUHARA ,  Kazunari Sakagami ,  Hiroshi Ohta ,  Atsuro Nakazato

    IPC分类号： C07C69/757 ,  C07C321/22 ,  C07D295/088 ,  C07C69/96 ,  C07D317/24 ,  C07D307/88

    CPC分类号： C07C229/50 ,  C07D307/88

    摘要： A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.

    摘要翻译： 一种有效治疗和预防精神疾病如精神分裂症，焦虑及其相关疾病，抑郁症，双相情感障碍和癫痫的药物。 该药物拮抗II型代谢型谷氨酸受体的作用，并且在口服给药中表现出高活性。由式[I]表示的2-氨基 - 双环[3.1.0]己烷-2,6-二羧酸酯衍生物[其中R1和R2为 相同或不同，并且各自表示氢原子，C 1-10烷基等; X表示氢原子或氟原子; Y表示-OCHR 3 R 4等（其中R 3和R 4相同或不同，各自表示氢原子，C 1-10烷基等; n表示1或2的整数）]，其药学上可接受的盐或 水合物。

    Radioactive Halogen-Labeled Phenyloxyaniline Derivatives
    46.
    发明申请
    Radioactive Halogen-Labeled Phenyloxyaniline Derivatives 审中-公开
    放射性卤素标记苯氧基苯胺衍生物

    公开(公告)号：US20090234162A1

    公开(公告)日：2009-09-17

    申请号：US11884763

    申请日：2005-12-28

    申请人： Kazutoshi Suzuki ,  Tetsuya Suhara ,  Christer Halldin ,  Ming-Rong Zhang ,  Atsuro Nakazato

    发明人： Kazutoshi Suzuki ,  Tetsuya Suhara ,  Christer Halldin ,  Ming-Rong Zhang ,  Atsuro Nakazato

    IPC分类号： C07C233/25

    CPC分类号： A61K51/04 ,  C07B59/001 ,  C07B2200/05 ,  C07C233/88

    摘要： A radioactive halogen-labeled phenyoxyaniline derivative represented by the following formula: wherein R1 represents a group such as an alkyl group; X1, X2, X3 and X4 represent each a hydrogen atom, an alkyl group, an alkoxy group, an alkoxy group carrying 11C introduced thereinto or a radioactive halogen atom, provided that at least one of X1, X2, X3 and X4 represents an alkoxy group carrying 11C introduced thereinto or a radioactive halogen atom; which is a compound useful as a PBR ligand having a high affinity and a high selectivity. In in vitro measurement of PBR, a PBR ligand having a high affinity and a high selectivity is labeled with a radioactive halogen nuclear species so as to enable the measurement of PBR in vivo with the use of means including not only PET but also SPECT. Thus, a compound which is useful in early diagnosing, preventing and treating diseases such as Alzheimer type dementia can be obtained.

    摘要翻译： 由下式表示的放射性卤素标记的苯氧基苯胺衍生物：其中R1表示烷基等基团; X 1，X 2，X 3和X 4各自表示氢原子，烷基，烷氧基，带有11C的烷氧基或放射性卤素原子，条件是X 1，X 2，X 3和X 4中的至少一个表示烷氧基 携带11C的基团或放射性卤素原子; 其是可用作具有高亲和力和高选择性的PBR配体的化合物。 在PBR的体外测量中，具有高亲和力和高选择性的PBR配体用放射性卤素核物种进行标记，以便能够使用不仅包括PET而且还包括SPECT的方法在体内测量PBR。 因此，可以获得可用于早期诊断，预防和治疗诸如阿尔茨海默氏型痴呆症的疾病的化合物。

    Dicarboxylic acid derivatives
    48.
    发明授权
    Dicarboxylic acid derivatives 失效
    二羧酸衍生物

    公开(公告)号：US06770676B2

    公开(公告)日：2004-08-03

    申请号：US10297479

    申请日：2002-12-06

    申请人： Atsuro Nakazato ,  Toshihito Kumagai ,  Kosuke Kanuma ,  Kazunari Sakagami

    发明人： Atsuro Nakazato ,  Toshihito Kumagai ,  Kosuke Kanuma ,  Kazunari Sakagami

    IPC分类号： C07C6113

    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[3.1.0]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组2代谢型谷氨酸受体的调节剂，具有治疗和/或预防精神病学障碍如精神分裂症，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。