Desferrithiocin derivatives and methods of use thereof
    42.
    发明授权
    Desferrithiocin derivatives and methods of use thereof 失效
    脱铁硫代衍生物及其使用方法

    公开(公告)号:US08604216B2

    公开(公告)日:2013-12-10

    申请号:US11367042

    申请日:2006-03-02

    IPC分类号: A61K31/425 C07D277/10

    CPC分类号: C07D277/12

    摘要: Compounds represented by structural formulas such as Structural Formula (I): are highly efficient in clearing excess iron from an organism. The invention also discloses methods of treating conditions such as metal overload, oxidative stress, and neoplastic and preneoplastic conditions.

    摘要翻译: 由结构式表示的化合物如结构式(I):在从生物体中清除多余的铁中是高效的。 本发明还公开了治疗诸如金属过载,氧化应激和肿瘤和肿瘤前病症的病症的方法。

    Process for the preparation of substituted thiazolines and their intermediates
    45.
    发明授权
    Process for the preparation of substituted thiazolines and their intermediates 失效
    制备取代噻唑啉及其中间体的方法

    公开(公告)号:US06894170B2

    公开(公告)日:2005-05-17

    申请号:US10270324

    申请日:2002-10-15

    摘要: Process for the preparation of substituted thiazolines of the formula (I) in which Ar is a phenyl, naphthyl, thienyl, pyridyl or quinolinyl radical which can optionally be substituted by one or more substituents from the group consisting of halogen, OH, benzyloxy, C1-C4-alkyl, C1-C4-alkoxy, COOR1 where R1 is H or C1-C4-alkyl, by coupling of (S)-α-methylcysteine hydrochloride of the formula (II) with a nitrile of the formula (III) Ar—CN in which Ar is as defined above, or a corresponding C1-C4-alkyl imidate, in which (S)-α-methylcysteine hydrochloride of the formula (II) is reacted in a suitable solvent with a nitrile of the formula (III) or a corresponding C1-C4-alkyl imidate in the presence of a tertiary base at a pH of 6.5 to 10 at 50° C. up to the reflux temperature to give the corresponding thiazoline of the formula (I), and processes for the preparation of (S)-α-methylcysteine hydrochloride and its use for the preparation of thiazolines of the formula (I).

    摘要翻译: 制备式(I)的取代噻唑啉的方法,其中Ar是苯基,萘基,噻吩基,吡啶基或喹啉基,其可以任选地被一个或多个选自卤素,OH,苄氧基,C C 1 -C 4 - 亚烷基,C 1 -C 4 - 烷氧基,COOR 1 - 其中R 1是H或C 1 -C 4 - 烷基,通过将(S)-α-甲基半胱氨酸盐酸盐与 式(II)与式(III)的腈<?in-line-formula description =“In-line formula”end =“lead”?> Ar-CN <?in-line-formula description =“In- 其中Ar如上所定义,或其相应的C 1 -C 4 - 亚烷基亚氨酸酯,其中(S) - 式(II)的α-甲基半胱氨酸盐酸盐在合适的溶剂中与式(III)的腈或相应的C 1 -C 4 - 亚烷基亚氨基酯反应 在pH为6.5t的叔碱存在下进行 o 10在50℃直到回流温度,得到相应的式(I)噻唑啉,以及制备(S)-α-甲基半胱氨酸盐酸盐的方法及其用于制备式(I)的噻唑啉的用途 一世)。