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    Pyrrolopyrimidine Derivatives
    1.
    发明申请
    Pyrrolopyrimidine Derivatives 审中-公开
    吡咯并嘧啶衍生物

    公开(公告)号：US20070270588A1

    公开(公告)日：2007-11-22

    申请号：US10591765

    申请日：2005-03-04

    申请人： Francois Bischoff ,  Ludo Kennis ,  Mirielle Braeken ,  Gaston Diels ,  Atsuro Nakazato

    发明人： Francois Bischoff ,  Ludo Kennis ,  Mirielle Braeken ,  Gaston Diels ,  Atsuro Nakazato

    IPC分类号： C07D487/04

    CPC分类号： C07D487/04

    摘要： According to the present invention, there is provided an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastro-intestinal diseases, drug dependence, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alpecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, pain, etc. A pyrrolopyrimidine derivative represented by the following formula [I]: has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.

    摘要翻译： 根据本发明，提供了一种抗CRF受体的拮抗剂，其作为治疗或预防药物是有效的，其涉及CRF被认为涉及的疾病，例如抑郁症，焦虑症，阿尔茨海默氏病，帕金森病，亨廷顿氏舞蹈病，进食 疾病，高血压，胃肠疾病，药物依赖，脑梗塞，脑缺血，脑水肿，头部外伤，炎症，免疫相关疾病，特异性，肠易激综合征，睡眠障碍，癫痫，皮肤病，精神分裂症，疼痛等 由下式[I]表示的吡咯并嘧啶衍生物对CRF受体具有高亲和力，并且对于涉及CRF的疾病有效。

    Pyrrolopyrimidine and Pyrrolopyridine Derivatives Substituted with Tetrahydropyridine as Crf Antagonists
    3.
    发明申请
    Pyrrolopyrimidine and Pyrrolopyridine Derivatives Substituted with Tetrahydropyridine as Crf Antagonists 审中-公开
    用四氢吡啶取代的吡咯并嘧啶和吡咯并吡啶衍生物作为Crf拮抗剂

    公开(公告)号：US20070293670A1

    公开(公告)日：2007-12-20

    申请号：US11630041

    申请日：2005-06-24

    申请人： Atsuro Nakazato ,  Taketoshi Okubo ,  Dai Nozawa ,  Ludo Kennis ,  Marcel De Bruyn

    发明人： Atsuro Nakazato ,  Taketoshi Okubo ,  Dai Nozawa ,  Ludo Kennis ,  Marcel De Bruyn

    IPC分类号： C07D487/04

    CPC分类号： C07D487/04 ,  C07D471/04

    摘要： [PROBLEM TO BE SOLVED]An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal diseases, drug dependence, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, pain, etc. [SOLUTION]A pyrrolopyrimidine or pyrrolopyridine derivative substituted with tetrahydropyridine represented by the following formula [I]: has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.

    摘要翻译： [待解决的问题]本发明的目的是提供一种抗CRF受体的拮抗剂，其作为治疗或预防药物是有效的，其涉及CRF被认为涉及的疾病，例如抑郁症，焦虑症，阿尔茨海默病，帕金森病 疾病，亨廷顿氏舞蹈病，饮食失调，高血压，胃肠道疾病，药物依赖，脑梗死，脑缺血，脑水肿，头部外伤，炎症，免疫相关疾病，脱发，肠易激综合征，睡眠障碍，癫痫，皮肤病，精神分裂症 ，疼痛等。[解决方案]由下式[I]表示的用四氢吡啶取代的吡咯并嘧啶或吡咯并吡啶衍生物对CRF受体具有高亲和力，并且对于被认为涉及CRF的疾病是有效的。

    Thienopyrimidine and Thienopyridine Derivatives Substituted with Cyclic Amino Group
    4.
    发明申请
    Thienopyrimidine and Thienopyridine Derivatives Substituted with Cyclic Amino Group 失效
    用环氨基取代的噻吩并嘧啶和噻吩并吡啶衍生物

    公开(公告)号：US20070254898A1

    公开(公告)日：2007-11-01

    申请号：US10584951

    申请日：2005-01-06

    申请人： Atsuro Nakazato ,  Taketoshi Okubo ,  Dai Nozawa ,  Tomoko Tamita ,  Ludo Kennis

    发明人： Atsuro Nakazato ,  Taketoshi Okubo ,  Dai Nozawa ,  Tomoko Tamita ,  Ludo Kennis

    IPC分类号： A61K31/519 ,  A61K31/435 ,  C07D471/02 ,  C07D487/00

    CPC分类号： C07D495/04

    摘要： [Problem to be Solved] An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastral diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alpecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, etc. [Solution] A thienopyrimidine or thienopyridine derivative substituted with a cyclic amino group represented by the following formula [I]: has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.

    摘要翻译： [待解决的问题]本发明的目的是提供一种抗CRF受体的拮抗剂，其作为治疗或预防药物有效，其中CRF被认为是涉及的疾病，例如抑郁症，焦虑症，阿尔茨海默病，帕金森病 疾病，亨廷顿氏舞蹈病，饮食失调，高血压，胃疾病，药物依赖，癫痫，脑梗死，脑缺血，脑水肿，头部外伤，炎症，免疫相关疾病，特发性，肠易激综合征，睡眠障碍，癫痫，皮肤病 ，精神分裂症等。[溶液]由下式[I]表示的环状氨基取代的噻吩并嘧啶或噻吩并吡啶衍生物对CRF受体具有高亲和力，对于CRF被认为是涉及的疾病有效。

    Triaza-cyclopenta [cd] indene derivatives
    5.
    发明申请
    Triaza-cyclopenta [cd] indene derivatives 失效
    三氮杂 - 环戊二烯并[cd]茚衍生物

    公开(公告)号：US20070060602A1

    公开(公告)日：2007-03-15

    申请号：US10584952

    申请日：2005-01-06

    申请人： Atsuro Nakazato ,  Taketoshi Okubo ,  Dai Nozawa ,  Tomoko Tamita ,  Ludo Kennis

    发明人： Atsuro Nakazato ,  Taketoshi Okubo ,  Dai Nozawa ,  Tomoko Tamita ,  Ludo Kennis

    IPC分类号： A61K31/519 ,  C07D487/14

    CPC分类号： C07D487/16

    摘要： An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastral diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alpecia, irritable bowel syndrome, sleep disorders, dermatitides, schizophrenia, pain, etc. A triaza-cyclopenta[cd]indene derivative represented by the following formula [I]: has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.

    摘要翻译： 本发明的目的是提供一种抗CRF受体的拮抗剂，其作为治疗或预防药物是有效的，其涉及CRF被认为涉及的疾病，例如抑郁症，焦虑症，阿尔茨海默氏病，帕金森病，亨廷顿氏舞蹈病，进食 疾病，高血压，胃疾病，药物依赖，癫痫，脑梗塞，脑缺血，脑水肿，头部外伤，炎症，免疫相关疾病，特异性，肠易激综合征，睡眠障碍，皮肤病，精神分裂症，疼痛等。 由下式[I]表示的三氮杂 - 环戊二烯并[cd]茚衍生物：对CRF受体具有高亲和力，并且对于CRF被认为涉及的疾病有效。

    2-amino-bicyclo[3.1.0]hexane-2, 6-dicarboxylic ester derivative
    6.
    发明授权
    2-amino-bicyclo[3.1.0]hexane-2, 6-dicarboxylic ester derivative 失效
    2-氨基 - 双环[3.1.0]己烷-2,6-二羧酸酯衍生物

    公开(公告)号：US08258133B2

    公开(公告)日：2012-09-04

    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： A61K31/535

    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。

    Phenyloxyaniline derivatives
    8.
    发明授权
    Phenyloxyaniline derivatives 有权
    苯氧基苯胺衍生物

    公开(公告)号：US06870069B2

    公开(公告)日：2005-03-22

    申请号：US10699743

    申请日：2003-11-04

    申请人： Kazutoshi Suzuki ,  Ming-Rong Zhang ,  Tetsuya Suhara ,  Atsuro Nakazato ,  Makoto Goto

    发明人： Kazutoshi Suzuki ,  Ming-Rong Zhang ,  Tetsuya Suhara ,  Atsuro Nakazato ,  Makoto Goto

    IPC分类号： C07C233/15 ,  C07C233/05 ,  A61K31/16

    CPC分类号： C07C233/15

    摘要： A phenyloxyaniline derivative useful as a ligand for peripheral benzodiazepine receptor having a strong affinity and a high selectivity, which is represented by formula (1): wherein X1 and X2 are same or different and each is hydrogen atom or halogen atom; R1 and R2 are same or different and each is hydrogen atom, an alkyl group having 1 to 10 carbon(s) or a halogen-substituted alkyl group having 1 to 10 carbon(s); and R3 is a halogen-substituted alkyl group having 1 to 5 carbon(s), or a radioisotope thereof.

    摘要翻译： 用作具有强亲合力和高选择性的外部苯并二氮杂受体的配体的苯氧基苯胺衍生物，其由式（1）表示：其中X 1和X 2相同或不同，各自为氢原子或卤素 原子; R 1和R 2相同或不同，各自为氢原子，具有1〜10个碳原子的烷基或具有1〜10个碳原子的卤素取代的烷基; R 3是具有1〜5个碳原子的卤素取代的烷基或其放射性同位素。

    Carboxylic acid derivatives and process for producing the same
    9.
    发明授权
    Carboxylic acid derivatives and process for producing the same 失效
    羧酸衍生物及其制备方法

    公开(公告)号：US06500958B2

    公开(公告)日：2002-12-31

    申请号：US10176528

    申请日：2002-06-24

    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： C07D23500

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

    摘要： The present invention relates to compounds which are useful for efficient synthesis of 2-amino-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acids. The compounds according to the present invention comprise 2-oxobicyclo[3.1.0]hexane-6-carboxylic acid derivatives represented by the formula as follows: [wherein, R1 represents a hydrogen atom, a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C3-C6 cycloalkyl C1-C6 alkyl group, an aryl group, an aryl C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C1-C6 hydroxyalkyl group, a C1-C6 alkylthio C1-C6 alkyl group, a C1-C6 mercaptoalkyl group, a tetrahydrofuranyl group, or a tetrahydropyranyl group; R2 and R3 are identical or different, and each represents a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C3-C6 cycloalkyl C1-C6 alkyl group, an aryl group, or an aryl C1-C6 alkyl group, or alternatively, R2 and R3 together represent —(CH2)n— (wherein n represents 2 or 3); and Y1 and Y2 are identical or different, and each represents a sulfur atom, an oxygen atom, or a nitrogen atom].

    摘要翻译： 本发明涉及可用于高效合成2-氨基-4-氧代双环[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2-氧代双环[3.1.0] 由下式表示的己烷-6-羧酸衍生物：[其中，R1表示氢原子，C1-C6烷基，C3-C6环烷基，C3-C6环烷基C1-C6烷基，芳基 基团，芳基C1-C6烷基，C1-C6烷氧基C1-C6烷基，C1-C6羟基烷基，C1-C6烷硫基C1-C6烷基，C1-C6巯基烷基，四氢呋喃基， 或四氢吡喃基; R2和R3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-C6烷基，或 或者，R2和R3一起表示 - （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]。

    Carboxylic acid derivatives and process for producing same
    10.
    发明授权
    Carboxylic acid derivatives and process for producing same 失效
    羧酸衍生物及其制备方法

    公开(公告)号：US06479674B1

    公开(公告)日：2002-11-12

    申请号：US09937212

    申请日：2001-09-24

    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： C07D31500

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

    摘要： The present invention relates to compounds which are useful for efficient synthesis of 2-amino-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acids. The compounds according to the present invention comprise 2-oxobicyclo[3.1.0]hexane-6-carboxylic acid derivatives represented by the formula as follows: [wherein, R1 represents a hydrogen atom, a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C3-C6 cycloalkyl C1-C6 alkyl group, an aryl group, an aryl C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C1-C6 hydroxyalkyl group, a C1-C6 alkylthio C1-C6 alkyl group, a C1-C6 mercaptoalkyl group, a tetrahydrofuranyl group, or a tetrahydropyranyl group; R2 and R3 are identical or different, and each represents a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C3-C6 cycloalkyl C1-C6 alkyl group, an aryl group, or an aryl C1-C6 alkyl group, or alternatively, R2 and R3 together represent —(CH2)n— (wherein n represents 2 or 3); and Y1 and Y2 are identical or different, and each represents a sulfur atom, an oxygen atom, or a nitrogen atom].

    摘要翻译： 本发明涉及可用于高效合成2-氨基-4-氧代双环[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2-氧代双环[3.1.0] 由下式表示的己烷-6-羧酸衍生物：[其中，R1表示氢原子，C1-C6烷基，C3-C6环烷基，C3-C6环烷基C1-C6烷基，芳基 基团，芳基C1-C6烷基，C1-C6烷氧基C1-C6烷基，C1-C6羟基烷基，C1-C6烷硫基C1-C6烷基，C1-C6巯基烷基，四氢呋喃基， 或四氢吡喃基; R2和R3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-C6烷基，或 或者，R2和R3一起表示 - （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]。