利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

145 条记录 (耗时 0.031 秒)

    Synthesis of 2-alkylcysteine via phase transfer catalysis
    61.
    发明申请
    Synthesis of 2-alkylcysteine via phase transfer catalysis 审中-公开

    公开(公告)号：US20060281926A1

    公开(公告)日：2006-12-14

    申请号：US11508679

    申请日：2006-08-23

    申请人： Rayomand Gimi ,  Mukund Chorghade

    发明人： Rayomand Gimi ,  Mukund Chorghade

    IPC分类号： C07D277/10

    CPC分类号： C07C227/18 ,  C07B2200/07 ,  C07C229/36 ,  C07C255/53 ,  C07C255/54 ,  C07C257/08 ,  C07C319/02 ,  C07C319/06 ,  C07C319/12 ,  C07C319/20 ,  C07D277/12 ,  C07D303/24 ,  C07C323/58

    摘要： Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. In one embodiment, the present invention provides methods of preparing 2-alkylcysteine derivatives. In another embodiment, the method comprises forming a 2-alkylcysteine derivative from a cysteine derivative in the presence of a phase transfer catalyst. In particular, the present invention provides methods for preparing 2-methylcysteine derivatives. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In one aspect, an aryl nitrile or imidate is condensed with cysteine or a 2-alkyl cysteine. The present invention also relates to the preparation of 4,5-dihydro-2-(2,4-dihydroxyphenyl)-4-alkyl-thiazole-4-carboxylic acids, such as 4,5-dihydro-2-(2,4-dihydroxyphenyl)-4-methyl-thiazole-4-carboxylic acid.

    Synthesis of substituted thiazoline carboxylic acids
    62.
    发明授权
    Synthesis of substituted thiazoline carboxylic acids 有权
    取代噻唑啉羧酸的合成

    公开(公告)号：US06982335B2

    公开(公告)日：2006-01-03

    申请号：US10439263

    申请日：2003-05-15

    申请人： Mukund S. Chorghade ,  Rayomand H. Gimi ,  Peter D. McDonnell ,  Paul Wolstenholme-Hogg

    发明人： Mukund S. Chorghade ,  Rayomand H. Gimi ,  Peter D. McDonnell ,  Paul Wolstenholme-Hogg

    IPC分类号： C07D277/56

    CPC分类号： C07C227/18 ,  C07B2200/07 ,  C07C229/36 ,  C07C255/53 ,  C07C255/54 ,  C07C257/08 ,  C07C319/02 ,  C07C319/06 ,  C07C319/12 ,  C07C319/20 ,  C07D277/12 ,  C07D303/24 ,  C07C323/58

    摘要： A useful and efficient method of preparing an alkylated thiazoline carboxylic acid, or a derivative thereof, comprises coupling a substituted aryl nitrile such as, for example, 2,4-dimethoxybenzonitrile or 4-methoxybenzonitrile, with a cysteine ester to form a substituted thiazoline carboxylic acid ester; optionally hydrolyzing the substituted thiazoline carboxylic acid ester to form a substituted thiazoline carboxylic acid; optionally, protecting the carboxyl group; alkylating the thiazoline ring at the 4-carbon position, as indicated in Structural Formula (I), with a compound of the formula R1-L, wherein R1 is as defined above and L is a leaving group, in the presence of a phase transfer catalyst; and, optionally, deprotecting the carboxyl group.In one embodiment of the present invention, a cinchona-alkaloid derived phase transfer catalyst is used to alkylate a protected substituted thiazoline carboxylic acid.

    摘要翻译： 制备烷基化噻唑啉羧酸或其衍生物的有效和有效的方法包括将取代的芳基腈例如2,4-二甲氧基苄腈或4-甲氧基苄腈与半胱氨酸酯偶合以形成取代的噻唑啉羧酸 酸酯; 任选地水解取代的噻唑啉羧酸酯以形成取代的噻唑啉羧酸; 任选地，保护羧基; 如结构式（I）所示，在4-碳位置上使噻唑啉环与式R 1 -L的化合物烷基化，其中R 1为 在相转移催化剂存在下，L是离去基团; 并任选地使羧基脱保护。 在本发明的一个实施方案中，使用致cin生物碱衍生的相转移催化剂烷基化受保护的取代噻唑啉羧酸。

    Novel thiazoline derivatives as selective androgen receptor modulators (SARMS)
    67.
    发明申请
    Novel thiazoline derivatives as selective androgen receptor modulators (SARMS) 审中-公开
    新型噻唑啉衍生物作为选择性雄激素受体调节剂（SARMS）

    公开(公告)号：US20050014952A1

    公开(公告)日：2005-01-20

    申请号：US10866591

    申请日：2004-06-12

    申请人： Raymond Ng ,  Zhihua Sui

    发明人： Raymond Ng ,  Zhihua Sui

    IPC分类号： A61P5/26 ,  C07D277/12 ,  C07D417/02 ,  C07D277/18

    CPC分类号： C07D277/12

    摘要： The present invention is directed to novel thiazoline derivatives of the general formula (I) wherein all variables are as herein defined, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.

    摘要翻译： 本发明涉及通式（I）的新型噻唑啉衍生物，其中所有变量如本文所定义，含有它们的药物组合物及其用于治疗由雄激素受体调节的病症和状况。