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    Process for preparing optically active aminopentane derivative, intermediate and process for preparing intermediate
    3.
    发明授权
    Process for preparing optically active aminopentane derivative, intermediate and process for preparing intermediate 有权
    光学活性氨基戊烷衍生物的制备方法，中间体及其制备方法

    公开(公告)号：US07807840B2

    公开(公告)日：2010-10-05

    申请号：US11922925

    申请日：2006-06-28

    申请人： Fumio Yoneda ,  Mayumi Watanabe ,  Takuya Yasusa

    发明人： Fumio Yoneda ,  Mayumi Watanabe ,  Takuya Yasusa

    IPC分类号： C07C209/00 ,  C07D291/04

    CPC分类号： C07B53/00 ,  C07D209/14 ,  C07D291/04 ,  C07D307/81 ,  C07D317/58 ,  C07D333/58

    摘要： There are provided a process for preparing an optically active aminopentane derivative that is promising as a psychotropic agent, an antidepressant agent, an antiparkinsonian agent, an anti-Alzheimer's agent, an apoptosis inhibitor, or the like; a novel optically active intermediate oxathiazolidine derivative very useful in the production of the aminopentane derivative; and process for the production thereof.The optically active aminopentane derivatives can be produced in an industrially advantageous manner from a novel optically active oxathiazolidine derivative represented by formula (5): wherein * indicates the position of an asymmetric carbon atom in the R or S configuration, and n is 0 or 1.

    摘要翻译： 提供了制备作为精神药物有前途的光学活性氨基戊烷衍生物的方法，抗抑郁药，抗帕金森病药，抗阿尔茨海默氏剂，凋亡抑制剂等; 一种在生产氨基戊烷衍生物中非常有用的新型光学活性中间体噻唑烷衍生物; 及其生产方法。 光学活性氨基戊烷衍生物可以以工业上有利的方式从由式（5）表示的新型光学活性氧杂噻唑烷衍生物制备：其中*表示R或S构型中不对称碳原子的位置，n为0或1 。

    Imaging Agents
    7.
    发明申请
    Imaging Agents 有权
    成像剂

    公开(公告)号：US20070082879A1

    公开(公告)日：2007-04-12

    申请号：US11425078

    申请日：2006-06-19

    申请人： Mark Goodman

    发明人： Mark Goodman

    IPC分类号： A61K31/397 ,  A61K31/337 ,  A61K31/38 ,  A61K31/335

    CPC分类号： C07C229/48 ,  A61K51/0402 ,  A61K51/0406 ,  C07B59/001 ,  C07C2601/04 ,  C07D291/04 ,  C07D345/00 ,  C07F13/005

    摘要： The present invention provides novel amino acid compounds useful in detecting and evaluating brain and body tumors. These compounds have the advantageous properties of rapid uptake and prolonged retention in tumors and can be labeled with halogen isotopes such as fluorine-18, iodine-123, iodine-124, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77, bromine-82, astatine-210, astatine-211, and other astatine isotopes. These compounds can also be labeled with technetium and rhenium isotopes using known chelation complexes. The compounds disclosed herein bind tumor tissues in vivo with high specificity and selectivity when administered to a subject. Preferred compounds show a target to non-target ratio of at least 2:1, are stable in vivo and substantially localized to target within 1 hour after administration. Preferred compounds include 1-amino-2-[18F]fluorocyclobutyl-1-carboxylic acid (2-[18F]FACBC) and 1-amino-2-[18F]fluoromethylcyclobutyl-1-carboxylic acid (2-[18F]FMACBC). The labeled amino acid compounds of the invention are useful as imaging agents in detecting and/or monitoring tumors in a subject by PET or SPECT.

    摘要翻译： 本发明提供了可用于检测和评估脑和体肿瘤的新型氨基酸化合物。 这些化合物具有在肿瘤中快速吸收和延长保留的有利特性，并可用卤素同位素如氟-18，碘-123，碘-124，碘-125，碘-131，溴-75，溴-76 ，溴-77，溴-82，ast ine -21，ast ine -211和其他ast同位素。 这些化合物也可以使用已知的螯合络合物用锝和铼同位素标记。 当给予受试者时，本文所公开的化合物以高特异性和选择性在体内结合肿瘤组织。 优选的化合物显示至少2:1的目标与非目标比例，在给药后1小时内在体内是稳定的并且基本上定位于靶标上。 优选的化合物包括1-氨基-2 - [[18 F]氟代环丁基-1-羧酸（2 - [（18 F）FACBC））和1-氨基-2- [ F]氟甲基环丁基-1-羧酸（2- [叔丁基] FMACBC））。 本发明的标记氨基酸化合物可用作通过PET或SPECT检测和/或监测受试者的肿瘤的成像剂。

    Method of producing a quinolonecarboxylic acid derivative
    10.
    发明授权
    Method of producing a quinolonecarboxylic acid derivative 失效
    制备喹诺酮羧酸衍生物的方法

    公开(公告)号：US5869661A

    公开(公告)日：1999-02-09

    申请号：US339404

    申请日：1994-11-17

    申请人： Kiyoshige Ochi ,  Hirohito Shimizu

    发明人： Kiyoshige Ochi ,  Hirohito Shimizu

    IPC分类号： C07D215/56 ,  C07D265/28 ,  C07D291/04 ,  C07D295/155

    CPC分类号： C07D215/56 ,  C07D265/28 ,  C07D291/04 ,  C07D295/155

    摘要： The present invention is a method of producing a 6-fluoro-7-substituted quinolonecarboxylic acid derivative represented by the general formula (4): ##STR1## wherein the variables are defined in the specification, which is characterized by adding an alkylboric acid ester represented by the general formula (3):B (OR.sub.5).sub.3 (3)wherein R.sub.5 represents a lower alkyl group, an aryl group, a substituted aryl group or a substituted aralkyl group to a 6-fluoroquinolonecarboxylic acid derivative represented by the general formula (1): ##STR2## wherein R.sub.1 and R.sub.2 are as defined in the specification; and R.sub.3 represents an optional, functional residue capable of participating in a nucleophilic substitution reaction, and a substituted saturated heterocyclic amine represented by the general formula (2): ##STR3## wherein X, Y and n are as defined in the specification, and condensing the reaction mixture with heating.

    摘要翻译： 本发明是由通式（4）表示的6-氟-7-取代喹诺酮羧酸衍生物的制造方法，其特征在于，加入通式（3）表示的烷基硼酸酯： B（OR 5）3（3）其中R 5表示通式（1）表示的6-氟喹诺酮羧酸衍生物的低级烷基，芳基，取代的芳基或取代的芳烷基： ）其中R1和R2如说明书中所定义; 和R3表示任选的能够参与亲核取代反应的官能残基，以及由通式（2）表示的取代的饱和杂环胺：其中X，Y和n如说明书中所定义。 ，并加热反应混合物。