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    NOVEL PROCESS FOR THE MANUFACTURE OF DRONEDARONE
    5.
    发明申请
    NOVEL PROCESS FOR THE MANUFACTURE OF DRONEDARONE 失效
    DRONEDARONE制造的新工艺

    公开(公告)号：US20120330037A1

    公开(公告)日：2012-12-27

    申请号：US13580005

    申请日：2011-01-26

    申请人： Mara Sada ,  Antonio Nardi ,  Stefano Maiorana

    发明人： Mara Sada ,  Antonio Nardi ,  Stefano Maiorana

    IPC分类号： C07D307/80

    CPC分类号： C07D307/82

    摘要： The invention relates to a new process for the preparation of dronedarone and its salts, in particular a synthesis process which allows said compound and its salts to be obtained with good yields, high purity and in an industrially expedient manner; the invention also concerns a new synthesis intermediate.

    摘要翻译： 本发明涉及制备决奈达隆及其盐的新方法，特别是允许以高产率，高纯度和工业上方便的方式获得所述化合物及其盐的合成方法; 本发明还涉及一种新的合成中间体。

    Process for the manufacture of dronedarone
    6.
    发明授权
    Process for the manufacture of dronedarone 失效
    制备决奈达隆的方法

    公开(公告)号：US08536350B2

    公开(公告)日：2013-09-17

    申请号：US13580005

    申请日：2011-01-26

    申请人： Mara Sada ,  Antonio Nardi ,  Stefano Maiorana

    发明人： Mara Sada ,  Antonio Nardi ,  Stefano Maiorana

    IPC分类号： A61K31/34 ,  C07D307/00

    CPC分类号： C07D307/82

    摘要： The invention relates to a new process for the preparation of dronedarone and its salts, in particular a synthesis process which allows said compound and its salts to be obtained with good yields, high purity and in an industrially expedient manner; the invention also concerns a new synthesis intermediate.

    摘要翻译： 本发明涉及制备决奈达隆及其盐的新方法，特别是允许以高产率，高纯度和工业上方便的方式获得所述化合物及其盐的合成方法; 本发明还涉及一种新的合成中间体。

    Process for the production of a racemic thioctic acid
    7.
    发明授权
    Process for the production of a racemic thioctic acid 有权
    制备外消旋硫辛酸的方法

    公开(公告)号：US06844450B2

    公开(公告)日：2005-01-18

    申请号：US10398891

    申请日：2001-10-08

    申请人： Annibale Salvi ,  Stefano Maiorana ,  Francesco Corcella

    发明人： Annibale Salvi ,  Stefano Maiorana ,  Francesco Corcella

    IPC分类号： C07D339/04 ,  C07D341/00

    CPC分类号： C07D339/04

    摘要： Process for the synthesis of racemic thioctic acid comprising the following stages: a) reaction of the alkyl ester of 6,8-di-halo-octanoic acid in an organic solvent with an aqueous solution of alkali disulfide in presence of a compound for phase transfer catalysis selected from the group consisting of quaternary ammonium or phosphonium salts having the following general formula: where: A is nitrogen of phosphorus, X is selected from the group consisting of Cl, Br, I, HSO4, and H2PO4 and the substitutents R1, R2, R3 and R4 are selection from the group consisting of linear or branched alkyl radicals having one to twenty carbon atoms (C1-C20), said substituents being identical or different one from the other, or only one of said substituents is selected from the group consisting of arylalkyl radicals having the following formula —(CH2)nC6H5 in which n=1-16; b) followed by the hydrolysis of the ester of racemic thiotic acid.

    摘要翻译： 包括以下步骤合成外消旋硫辛酸的方法：a）在相转移化合物存在下，6,8-二卤代辛酸的烷基酯在有机溶剂中与碱性二硫化物水溶液的反应 选自具有以下通式的季铵或鏻盐的催化剂：其中：A是磷的氮，X选自Cl，Br，I，HSO 4和H 2 PO 4，取代基R1，R2 ，R3和R4选自具有1-20个碳原子的直链或支链烷基（C1-C20），所述取代基彼此相同或不同，或者只有一个所述取代基选自基团 由具有下式的芳基烷基 - （CH 2）n C 6 H 5，其中n = 1-16; b）然后水解外消旋硫酸的酯。

    1,5-Benzothiazepines with cardiovascular utility, and pharmaceutical compositions containing them
    10.
    发明授权
    1,5-Benzothiazepines with cardiovascular utility, and pharmaceutical compositions containing them 失效
    具有心血管功能的1,5-苯并硫氮嗪和含有它们的药物组合物

    公开(公告)号：US4547495A

    公开(公告)日：1985-10-15

    申请号：US628730

    申请日：1984-07-09

    申请人： Stefano Maiorana ,  Diego G. Brocchetti ,  Giuseppe Piacenza

    发明人： Stefano Maiorana ,  Diego G. Brocchetti ,  Giuseppe Piacenza

    IPC分类号： A61K31/55 ,  A61K31/554 ,  A61P9/08 ,  A61P9/10 ,  C07D281/10 ,  C07D417/12

    CPC分类号： C07D281/10

    摘要： New 1,5-benzothiazepines of the following general formula ##STR1## wherein: R.sub.1 represents (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy or a halogen atom;R.sub.2 is selected from: benzoyl independently substituted with 1 to 3 (C.sub.1-4)alkyl or (C.sub.1-4)alkoxy groups, or with halogen atoms; phenylcarbamoyl; phenylcarbamoyl independently substituted with 1 to 3 (C.sub.1-4) alkyl or (C.sub.1-4) alkoxy groups or with halogen atoms; the groups R.sub.5 -CO, in which R.sub.5 is the radical deriving from a heterocyclic ring optionally substituted by a (C.sub.1-4)alkyl or a (C.sub.1-4)alkoxy radical, or by a halogen atom;R.sub.3 and R.sub.4 independently represent (C.sub.1-4)alkyl groups; and salts therewith of pharmaceutically acceptable acids.The compounds of the invention possess cardiovascular utility.

    摘要翻译： 新的具有下列通式的1,5-苯并硫氮杂formula：其中：R 1表示（C 1-4）烷基，（C 1-4）烷氧基或卤素原子; R2选自：独立地被1至3（C 1-4）烷基或（C 1-4）烷氧基或与卤素原子取代的苯甲酰基; 苯基氨基甲酰基; 独立地被1至3个（C 1-4）烷基或（C 1-4）烷氧基或与卤素原子取代的苯基氨基甲酰基; 基团R5-CO，其中R5是由任选被（C 1-4）烷基或（C 1-4）烷氧基取代的杂环或由卤素原子取代的基团; R3和R4独立地表示（C1-4）烷基; 以及其与药学上可接受的酸的盐。 本发明的化合物具有心血管效用。