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    Process for the manufacture of 3-hydroxy-N-alkyl-1-cycloalky1-6-alkyl-4-oxo-1,4-dihydropyridine-2-carboxamide and its related analogues
    4.
    发明授权
    Process for the manufacture of 3-hydroxy-N-alkyl-1-cycloalky1-6-alkyl-4-oxo-1,4-dihydropyridine-2-carboxamide and its related analogues 有权
    制备3-羟基-N-烷基-1-环烷基-1-6-烷基-4-氧代-1,4-二氢吡啶-2-甲酰胺及其相关类似物的方法

    公开(公告)号：US07893269B2

    公开(公告)日：2011-02-22

    申请号：US11667751

    申请日：2005-11-17

    申请人： Tim Fat Tam ,  Regis Leung-Toung ,  Yanqing Zhao ,  Wanren Li ,  Yingsheng Wang ,  Sandra Vittoria Agostino ,  Birenkumar Hasmukhbhai Shah

    发明人： Tim Fat Tam ,  Regis Leung-Toung ,  Yanqing Zhao ,  Wanren Li ,  Yingsheng Wang ,  Sandra Vittoria Agostino ,  Birenkumar Hasmukhbhai Shah

    IPC分类号： C07D403/02

    CPC分类号： C07D213/81 ,  Y02P20/55

    摘要： The present invention relates to a novel process for the preparation of 1-alkyl or 1-cycloalkyl derivatives of 3-hydroxy-4-oxo-1,4-dihydropyridine-2-carboxamide of formula (I). The process includes reacting an amine R2NH2 with a compound of formula (II) in a solution of metal hydroxide in water to give a compound of formula (III). Subsequent reaction of the compound of formula (III) with an acid chloride formation reagent in an inert solvent gives compounds of formula (I). The acid chloride formation reagent is selected from oxalyl chloride and dimethylformamide, dimethylchloromethylene-ammonium chloride and thionyl chloride and dimethylformamide. If desired, a compound of formula (I) where R5 is hydrogen may be formed when an intermediate substituent is used wherein R5 is an alcohol protective group removable by catalytic hydrogenation.

    摘要翻译： 本发明涉及制备式（I）的3-羟基-4-氧代-1,4-二氢吡啶-2-甲酰胺的1-烷基或1-环烷基衍生物的新方法。 该方法包括使胺R 2 NH 2与式（II）化合物在金属氢氧化物在水中的溶液中反应，得到式（III）化合物。 式（III）化合物与酰氯形成试剂在惰性溶剂中的随后反应得到式（I）化合物。 酰氯形成试剂选自草酰氯和二甲基甲酰胺，二甲基氯亚甲基氯化铵和亚硫酰氯和二甲基甲酰胺。 如果需要，当使用R5是可通过催化氢化除去的醇保护基团的中间取代基时，可以形成其中R 5为氢的式（I）化合物。

    Process For The Manufacture Of 3-Hydroxy-N-Alkyl-1-Cycloalkyl-6-Alkyl-4-Oxo-1,4-Dihydropyridine-2-Carboxamide And Its Related Analogues
    5.
    发明申请
    Process For The Manufacture Of 3-Hydroxy-N-Alkyl-1-Cycloalkyl-6-Alkyl-4-Oxo-1,4-Dihydropyridine-2-Carboxamide And Its Related Analogues 有权
    3-羟基-N-烷基-1-环烷基-6-烷基-4-氧代-1,4-二氢吡啶-2-羧酰胺及其相关类似物的制备方法

    公开(公告)号：US20080096886A1

    公开(公告)日：2008-04-24

    申请号：US11667751

    申请日：2005-11-17

    申请人： Tim Tam ,  Regis Leung-Toung ,  Yanqing Zhao ,  Wanren Li ,  Yingsheng Wang ,  Sandra Agostino ,  Birenkumar Shah

    发明人： Tim Tam ,  Regis Leung-Toung ,  Yanqing Zhao ,  Wanren Li ,  Yingsheng Wang ,  Sandra Agostino ,  Birenkumar Shah

    IPC分类号： A61K31/5377 ,  A61K31/496 ,  A61K31/4439 ,  A61K31/4415 ,  C07D413/02 ,  C07D403/02

    CPC分类号： C07D213/81 ,  Y02P20/55

    摘要： The present invention relates to a novel process for the preparation of 1-alkyl or 1-cycloalkyl derivatives of 3-hydroxy-4-oxo-1,4-dihydropyridine-2-carboxamide of formula I. The process includes reacting an amine R2NH2 with a compound of formula II in a solution of metal hydroxide in water to give a compound of formula III. Subsequent reaction of the compound of formula III with an acid chloride formation reagent in an inert solvent gives compounds of formula I. The acid chloride formation reagent is selected from oxalyl chloride and dimethylformamide, dimethylchloromethylene-ammonium chloride and thionyl chloride and dimethylformamide. If desired, a compound of formula I where R5 is hydrogen may be formed when an intermediate substituent is used wherein R5 is an alcohol protective group removable by catalytic hydrogenation.

    摘要翻译： 本发明涉及制备式I的3-羟基-4-氧代-1,4-二氢吡啶-2-甲酰胺的1-烷基或1-环烷基衍生物的新方法。该方法包括使胺R 1， 将其与式II化合物在金属氢氧化物在水中的溶液中反应，得到式III化合物。 随后将式III化合物与酰氯形成试剂在惰性溶剂中反应，得到式I化合物。酰氯形成试剂选自草酰氯和二甲基甲酰胺，二氯氯甲基氯化铵和亚硫酰氯和二甲基甲酰胺。 如果需要，当使用其中R 5是可通过催化氢化除去的醇保护基团的中间取代基时，可以形成其中R 5为氢的式I化合物。

    Pharmaceutically acceptable salts of thymodepressin and processes for their manufacture
    7.
    发明授权
    Pharmaceutically acceptable salts of thymodepressin and processes for their manufacture 有权
    胸腺抑素的药学上可接受的盐及其制造方法

    公开(公告)号：US08138221B2

    公开(公告)日：2012-03-20

    申请号：US12520337

    申请日：2007-12-13

    申请人： Tim Fat Tam ,  Blaise N'Zemba ,  Regis Leung-Toung ,  Yingsheng Wang ,  Yanqing Zhao ,  Lily Yu

    发明人： Tim Fat Tam ,  Blaise N'Zemba ,  Regis Leung-Toung ,  Yingsheng Wang ,  Yanqing Zhao ,  Lily Yu

    IPC分类号： A61K31/404 ,  C07D209/12

    CPC分类号： C07D209/20 ,  A61K38/05 ,  C07K5/0215

    摘要： The present invention relates to pharmaceutically acceptable crystalline and amorphous salts of D-isoglutamyl-D-tryptophan as well as processes for their manufacture, pharmaceutical compositions comprising them, and their uses in the preparation of pharmaceutical compositions for the treatment of various conditions and/or diseases. In particular, the present invention relates to D-isoglutamyl-D-tryptophan potassium salt (1:1), D-isoglutamyl-D-tryptophan lithium salt (1:1), D-isoglutamyl-D-tryptophan calcium salt (2:1), D-isoglutamyl-D-tryptophan magnesium salt (2:1), and D-isoglutamyl-D-tryptophan organic ammonium salts (1:1).

    摘要翻译： 本发明涉及D-异谷氨酰-D-色氨酸的药学上可接受的结晶和无定形盐以及其制备方法，包含它们的药物组合物及其在制备药物组合物中用于治疗各种病症和/或 疾病 特别地，本发明涉及D-异谷氨酰-D-色氨酸钾盐（1：1），D-异谷氨酰基-D-色氨酸锂盐（1:1），D-异谷氨酰-D-色氨酸钙盐（2： 1），D-异谷氨酰-D-色氨酸镁盐（2:1）和D-异谷氨酰-D-色氨酸有机铵盐（1:1）。

    Pharmaceutically acceptable salts of thymodepressin and processes for their manufacture
    8.
    发明授权
    Pharmaceutically acceptable salts of thymodepressin and processes for their manufacture 有权
    胸腺抑素的药学上可接受的盐及其制造方法

    公开(公告)号：US08735602B2

    公开(公告)日：2014-05-27

    申请号：US13424343

    申请日：2012-03-19

    申请人： Tim Fat Tam ,  Blaise N'Zemba ,  Regis Leung-Toung ,  Yingsheng Wang ,  Yanqing Zhao ,  Lily Yu

    发明人： Tim Fat Tam ,  Blaise N'Zemba ,  Regis Leung-Toung ,  Yingsheng Wang ,  Yanqing Zhao ,  Lily Yu

    IPC分类号： C07D209/12

    CPC分类号： C07D209/20 ,  A61K38/05 ,  C07K5/0215

    摘要： The present invention relates to pharmaceutically acceptable crystalline and amorphous salts of D-isoglutamyl-D-tryptophan as well as processes for their manufacture, pharmaceutical compositions comprising them, and their uses in the preparation of pharmaceutical compositions for the treatment of various conditions and/or diseases. In particular, the present invention relates to D-isoglutamyl-D-tryptophan potassium salt (1:1), D-isoglutamyl-D-tryptophan lithium salt (1:1), D-isoglutamyl-D-tryptophan calcium salt (2:1), D-isoglutamyl-D-tryptophan magnesium salt (2:1), and D-isoglutamyl-D-tryptophan organic ammonium salts (1:1).

    摘要翻译： 本发明涉及D-异谷氨酰-D-色氨酸的药学上可接受的结晶和无定形盐以及其制备方法，包含它们的药物组合物及其在制备药物组合物中用于治疗各种病症和/或 疾病 特别地，本发明涉及D-异谷氨酰-D-色氨酸钾盐（1：1），D-异谷氨酰基-D-色氨酸锂盐（1:1），D-异谷氨酰-D-色氨酸钙盐（2： 1），D-异谷氨酰-D-色氨酸镁盐（2:1）和D-异谷氨酰-D-色氨酸有机铵盐（1:1）。

    Fluorinated derivatives of deferiprone
    10.
    发明申请
    Fluorinated derivatives of deferiprone 有权
    去铁酮的氟化衍生物

    公开(公告)号：US20080242706A1

    公开(公告)日：2008-10-02

    申请号：US12078079

    申请日：2008-03-27

    申请人： Tim Fat Tam ,  Regis Leung-Toung ,  Yingsheng Wang ,  Yanqing Zhao

    发明人： Tim Fat Tam ,  Regis Leung-Toung ,  Yingsheng Wang ,  Yanqing Zhao

    IPC分类号： A61K31/44 ,  C07D213/69 ,  C07D309/32 ,  A61K31/35 ,  A61P25/16 ,  A61P25/28

    CPC分类号： C07D309/40 ,  C07D213/69

    摘要： The present invention relates to novel derivatives of deferiprone. In particular, the present invention relates to fluorinated derivatives of deferiprone or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, processes for the manufacture thereof and their use in the treatment of neurodegenerative diseases caused by the presence of free iron or iron accumulation in neural tissues and in diseases wherein excess iron must be removed or redistributed.

    摘要翻译： 本发明涉及去铁酮的新型衍生物。 特别地，本发明涉及去铁酮的氟化衍生物或其药学上可接受的盐，包含其的药物组合物，其制备方法及其用于治疗由神经组织中游离铁或铁积聚引起的神经变性疾病的治疗 以及必须除去或重新分配过量铁的疾病。