(Aminopropyl)methylphosphinic acids
    1.
    发明授权
    (Aminopropyl)methylphosphinic acids 失效
    (氨基丙基)甲基次膦酸

    公开(公告)号:US06596711B1

    公开(公告)日:2003-07-22

    申请号:US09786220

    申请日:2001-03-01

    IPC分类号: A61K3166

    摘要: Novel compounds of formula I, with the exception of i) the racemate of (3-amino-2-hydroxypropyl)methylphosphinic acid; ii) (S)-(3-amino-2-hydroxypropyl)methylphosphinic acid; iii) (R)-(3-amino-2-hydroxypropyl)methylphosphinic acid; iv) (3-amino-2-hydroxypropyl)difluoromethylphosphinic acid; and v) (3-amino-2-oxopropyl)methylphosphinic acid, having affinity to one or more GABAB receptors, their pharmaceutically acceptable salts, solvates and stereoisomers, as well as a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and the use of said active compounds in therapy.

    摘要翻译: (3-氨基-2-羟丙基)甲基次膦酸的外消旋物; ii)(S) - (3-氨基-2-羟丙基)甲基次膦酸; iii)(R) - (3-氨基-2-羟丙基)甲基次膦酸; iv)(3-氨基-2-羟丙基)二氟甲基次膦酸; 对于一种或多种GABA B受体具有亲和性,它们的药学上可接受的盐,溶剂合物和立体异构体,以及它们的制备方法,含有所述治疗活性化合物的药物组合物和 所述活性化合物在治疗中的用途。

    Aminopropylphosphinic acids
    2.
    发明授权
    Aminopropylphosphinic acids 失效
    氨基丙基次膦酸

    公开(公告)号:US06576626B2

    公开(公告)日:2003-06-10

    申请号:US09786219

    申请日:2001-03-01

    IPC分类号: A61K31662

    CPC分类号: C07F9/4816 A61K31/66

    摘要: Novel compounds of formula I, with the exception of i) the racemate of (3-amino-2-hydroxypropyl)phosphinic acid; and ii) (2R/S, 3R)-(3-amino-2-hydroxybutyl)phosphinic acid, having affinity to one or more GABAB receptors, their pharmaceutically acceptable salts, solvates and stereoisomers, as well as processes for their preparation, pharmaceutical compositions containing said therapeutically active compounds and the use of said active compounds in therapy

    摘要翻译: 新的式I化合物,除了(i)(3-氨基-2-羟丙基)次膦酸的外消旋物; 对于一种或多种GABA B受体具有亲和性,其药学上可接受的盐,溶剂合物和立体异构体,以及它们的制备方法,药物组合物 含有所述治疗活性化合物和所述活性化合物在治疗中的用途

    New Aminopropylphosphinic acids
    3.
    发明申请
    New Aminopropylphosphinic acids 审中-公开
    新的氨基丙基次膦酸

    公开(公告)号:US20080146836A1

    公开(公告)日:2008-06-19

    申请号:US11776648

    申请日:2007-07-12

    IPC分类号: C07F9/22

    CPC分类号: C07F9/4816 A61K31/66

    摘要: Novel compounds of formula I, with the exception of i) the racemate of (3-amino-2-hydroxypropyl)phosphinic acid; and ii) (2R/S,3R)-(3-amino-2-hydroxybutyl)phosphinic acid, having affinity to one or more GABAB receptors, their pharmaceutically acceptable salts, solvates and stereoisomers, as well as processes for their preparation, pharmaceutical compositions containing said therapeutically active compounds and the use of said active compounds in therapy.

    摘要翻译: 新的式I化合物,除了i)(3-氨基-2-羟丙基)次膦酸的外消旋物; 和ii)对一种或多种GABA B受体具有亲和力的(2R / S,3R) - (3-氨基-2-羟基丁基)次膦酸,其药学上可接受的盐,溶剂合物和立体异构体,作为 以及其制备方法,含有所述治疗活性化合物的药物组合物和所述活性化合物在治疗中的用途。

    New Compounds
    6.
    发明申请
    New Compounds 审中-公开
    新化合物

    公开(公告)号:US20080312449A1

    公开(公告)日:2008-12-18

    申请号:US11679264

    申请日:2007-02-27

    IPC分类号: C07D401/12

    CPC分类号: C07D401/12

    摘要: The novel optically pure compounds Na+, Mg2+, Li+, K+, Ca2+ and N+(R)4 salts of (+)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole or (−)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole, in particular sodium and magnesium salt form thereof, where R is an alkyl with 1-4 carbon atoms, processes for the preparation thereof and pharmaceutical preparations containing the compounds as active ingredients, as well as the use of the compounds in pharmaceutical preparations and intermediates obtained by preparing the compounds.

    摘要翻译: (+) - 5-甲氧基-2 - [[(4-甲氧基-3,5-二甲基-2-吡啶基)甲基)的新型光学纯化合物Na +,Mg2 +,Li +,K +,Ca2 +和N +(R) ]亚磺酰基] -1H-苯并咪唑或( - ) - 5-甲氧基-2 - [[(4-甲氧基-3,5-二甲基-2-吡啶基)甲基]亚磺酰基] -1H-苯并咪唑,特别是钠盐和镁盐 其形式,其中R是具有1-4个碳原子的烷基,其制备方法和含有化合物作为活性成分的药物制剂,以及该化合物在药物制剂中的用途以及通过制备化合物获得的中间体。

    Compounds Useful for the Synthesis of S- and R-Omeprazole and a Process for Their Preparation
    7.
    发明申请
    Compounds Useful for the Synthesis of S- and R-Omeprazole and a Process for Their Preparation 审中-公开
    用于合成S-和R-奥美拉唑的化合物及其制备方法

    公开(公告)号:US20080255199A1

    公开(公告)日:2008-10-16

    申请号:US10588056

    申请日:2005-02-17

    CPC分类号: C07D401/12

    摘要: The present invention relates to an improved method for the synthesis of the (S)- or (R)-enantiomer of omeprazole, characterized in that 2-[[(4-X-3,5-dimethylpyridin-2-yl)methyl]thio]-5-methoxy-1H-benzimidazole or 2-[[(4-X-3,5-dimethyl-1-ox-idopyridin-2-yl) methyl]thio]-5-methoxy-1H-benzimidazole, wherein X is a leaving group, is oxidized into the corresponding sulphoxide which is obtained as a crystalline compound. Recrystallisation of the thus obtained sulphoxide results in a compound of enhanced chemical and optical purity, which is subsequently transformed into the (S)- or (R)-enantiomer of omeprazole.

    摘要翻译: 本发明涉及一种用于合成奥美拉唑的(S) - 或(R) - 对映异构体的改进方法,其特征在于2 - [[(4-X-3,5-二甲基吡啶-2-基)甲基] 硫代] -5-甲氧基-1H-苯并咪唑或2 - [[(4-X-3,5-二甲基-1-氧代 - 吡啶-2-基)甲基]硫代] -5-甲氧基-1H-苯并咪唑,其中 X是离去基团,被氧化成作为结晶化合物获得的相应的亚砜。 由此获得的亚砜的重结晶产生增强的化学和光学纯度的化合物,其随后转化成奥美拉唑的(S) - 或(R) - 对映异构体。

    Compounds
    8.
    发明授权
    Compounds 有权
    化合物

    公开(公告)号:US06875872B1

    公开(公告)日:2005-04-05

    申请号:US09690044

    申请日:2000-10-16

    IPC分类号: C07D401/12

    CPC分类号: C07D401/12

    摘要: The novel optically pure compounds Na+, Mg2+, Li+, K+, Ca2+ and N+(R)4 salts of (+)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole or (−)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole, in particular sodium and magnesium salt form thereof, where R is an alkyl with 1-4 carbon atoms, processes for the preparation thereof and pharmaceutical preparations containing the compounds as active ingredients, as well as the use of the compounds in pharmaceutical preparations and intermediates obtained by preparing the compounds.

    摘要翻译: (+) - 5-甲氧基 - 苯甲酸的新型光学纯化合物Na +,Mg 2+,Li +,K +,Ca 2+和N + 2 - [[(4-甲氧基-3,5-二甲基-2-吡啶基)甲基]亚磺酰基] -1H-苯并咪唑或( - ) - 5-甲氧基-2 - [[(4-甲氧基-3,5-二甲基 -2-吡啶基)甲基]亚磺酰基] -1H-苯并咪唑,特别是其钠盐和镁盐形式,其中R是具有1-4个碳原子的烷基,其制备方法和含有该化合物作为活性成分的药物制剂, 以及化合物在通过制备化合物获得的药物制剂和中间体中的用途。

    Process for the optical purification of enantiomerically enriched
benzimidazole derivatives
    9.
    发明授权
    Process for the optical purification of enantiomerically enriched benzimidazole derivatives 失效
    对映异构体富集的苯并咪唑衍生物的光学纯化方法

    公开(公告)号:US5929244A

    公开(公告)日:1999-07-27

    申请号:US676215

    申请日:1996-07-19

    申请人: Sverker Von Unge

    发明人: Sverker Von Unge

    IPC分类号: C07D235/28 C07D401/12

    CPC分类号: C07D401/12 C07D235/28

    摘要: Process for the optical purification of the single enantiomers of some 2-sulphinyl-1H-benzimidazole derivatives and another structurally related sulphoxide from the respective enantiomerically enriched preparation thereof.

    摘要翻译: PCT No.PCT / SE96 / 00841 Sec。 371日期:1996年7月19日 102(e)1996年7月19日PCT PCT 1996年6月26日PCT公布。 出版物WO97 / 02261 日期1997年1月23日从相应的对映异构体富集的制剂中光学纯化一些2-亚磺酰基-1H-苯并咪唑衍生物和另一结构相关的亚砜的单一对映异构体的方法。