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    Process for producing cyclic nitrile sulfites
    31.
    发明授权
    Process for producing cyclic nitrile sulfites 失效
    生产循环硫酸钠的方法

    公开(公告)号：US3649636A

    公开(公告)日：1972-03-14

    申请号：US3649636D

    申请日：1969-11-13

    申请人： ATLANTIC RICHFIELD CO

    发明人： BURK EMMETT H JR ,  CARLOS DONALD D

    IPC分类号： C07D291/04 ,  C07D95/00

    CPC分类号： C07D291/04

    摘要： A CYCLIC NITRILE SULFITE COMPOUND OF THE GENERAL FORMULA:

    5-(((2-(O=)-1,3,2,4-DIOXATHIAZOL-5-YL)N)-A-),2-(O=)-

    1,3,2,4-DIOXATHIAZOLE

    WHEREIN N IS 0 TO 2 AND A IS AROMATIC HYDROCARBON HAVING 1 TO 3 AROMATIC RINGS, UP TO 30 CARBON ATOMS, AND NO ACETYLENE OR ETHYLENIC UNSATURATION, THE CYCLIC NITRILE SULFITE GROUPS BEING DIRECTLY ATTACHED TO AROMATIC RING ATOMS OF A, IS PREPARED BY ADDITION REACTING SULFUR DIOXIDE WITH A NITRILE OXIDE COMPOUND OF THE GENERAL FORMULA:

    O O)N

    WHEREIN A AND N ARE AS DEFINED ABOVE. THE CYCLIC NITRILE SULFITE COMPOUND IS USEFUL AS FOR EXAMPLE, AN ISOCYANATE GENERATOR. THUS IT CAN BE THERMALLY DECOMPOSED TO AN ISOCYANATE OF THE GENERAL FORMULA:

    O=C=N-AEN=C=O)N

    WHEREIN A AND N ARE AS DEFINED ABOVE.

    IMAGING AGENTS
    37.
    发明申请
    IMAGING AGENTS 有权
    成像代理

    公开(公告)号：US20110144483A1

    公开(公告)日：2011-06-16

    申请号：US12946027

    申请日：2010-11-15

    申请人： Mark M. GOODMAN

    发明人： Mark M. GOODMAN

    IPC分类号： A61B5/00 ,  C07C229/48 ,  C07F13/00 ,  C07C227/18 ,  A61K51/04 ,  A61P43/00

    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- [18 F]氟甲基环丁基-1-羧酸（2- [18 F] 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。

    Process for Preparing Optically Active Aminopentane Derivative, Intermediate and Process for Preparing Intermediate
    38.
    发明申请
    Process for Preparing Optically Active Aminopentane Derivative, Intermediate and Process for Preparing Intermediate 有权
    准备光学活性氨基戊烷衍生物，中间体和制备中间体的方法

    公开(公告)号：US20090124813A1

    公开(公告)日：2009-05-14

    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： C07D291/04 ,  C07C209/66

    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）表示的新的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 。