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    Radioactive Halogen-Labeled Phenyloxyaniline Derivatives
    1.
    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。

    Phenyloxyaniline derivatives
    2.
    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。

    2-amino-bicyclo[3.1.0]hexane-2, 6-dicarboxylic ester derivative
    3.
    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。

    Carboxylic acid derivatives and process for producing the same
    6.
    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
    7.
    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]。

    1,2-Dihydro-2-oxoquinoline derivatives
    10.
    发明授权
    1,2-Dihydro-2-oxoquinoline derivatives 失效
    1,2-二氢-2-氧代喹啉衍生物

    公开(公告)号：US06329525B1

    公开(公告)日：2001-12-11

    申请号：US09555568

    申请日：2000-06-01

    申请人： Atsuro Nakazato ,  Taketoshi Okubo ,  Toshihito Kumagai ,  Shigeyuki Chaki ,  Kazuyuki Tomisawa ,  Masashi Nagamine ,  Makoto Gotoh ,  Masanori Yoshida

    发明人： Atsuro Nakazato ,  Taketoshi Okubo ,  Toshihito Kumagai ,  Shigeyuki Chaki ,  Kazuyuki Tomisawa ,  Masashi Nagamine ,  Makoto Gotoh ,  Masanori Yoshida

    IPC分类号： C07D215227

    CPC分类号： C07D401/06 ,  C07D215/54 ,  C07D241/44

    摘要： A 1,2-dihydro-2-oxoquinoline derivative represented by the formula: wherein Ar is a pyridyl group or a group represented by the formula: (wherein X3 and X4 are the same or different, and are each a hydrogen atom, a halogen atom, a C1-5 alkyl group, a C1-5 alkoxy group, a hydroxyl group or a trifluoromethyl group), Y is a nitrogen atom, CH or C(OH), R1 and R2 are the same or different, and are each a hydrogen atom, a C1-10 alkyl group, a C3-15 alkoxyalkyl group or a C3-15 alkylaminoalkyl group, or R1 and R2 taken together with the nitrogen atom to which they are attached form a cyclic amino group, X1 and X2 are the same or different, and are each a hydrogen atom, a C1-5 alkyl group, a C1-5 alkoxy group or a halogen atom, or X1 and X2 taken together form an alkylenedioxy group, and n is an integer of 1 to 3; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 由下式表示的1,2-二氢-2-氧代喹啉衍生物：其中Ar是吡啶基或由下式表示的基团：（其中X 3和X 4相同或不同，并且各自为氢原子，卤素 原子，C 1-5烷基，C 1-5烷氧基，羟基或三氟甲基），Y是氮原子，CH或C（OH），R 1和R 2相同或不同，各自相同或不同 氢原子，C 1-10烷基，C 3-15烷氧基烷基或C 3-15烷基氨基烷基，或者R 1和R 2与它们所连接的氮原子一起形成环状氨基，X 1和X 2是 相同或不同，各自为氢原子，C1-5烷基，C1-5烷氧基或卤素原子，或X1和X2一起形成亚烷基二氧基，n为1〜3的整数 ; 或其药学上可接受的盐。