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37 条记录 (耗时 0.03 秒)

    Process for preparing fexofenadine
    11.
    发明申请
    Process for preparing fexofenadine 有权
    非索非那定制备方法

    公开(公告)号：US20110190504A1

    公开(公告)日：2011-08-04

    申请号：US12374539

    申请日：2007-07-25

    申请人： Giorgio Bertolini ,  Maurizio Gallina ,  Giuseppe Motta ,  Domenico Vergani

    发明人： Giorgio Bertolini ,  Maurizio Gallina ,  Giuseppe Motta ,  Domenico Vergani

    IPC分类号： C07D211/34

    CPC分类号： C07D211/22

    摘要： A process for preparing fexofenadine is described, which provides for the hydrolysis of 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-oxobutyl]-α,α-dimethylbenzeneacetic acid-alkyl ester, in a mixture of water and optionally an organic solvent, in the presence of a base; the carboxylate salt of 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-oxobutyl]-α,α-dimethylbenzeneacetic acid is thus obtained, which is then directly reduced as carboxylate in a basic environment with hydrogen in the presence of a suitable hydrogenation catalyst to give the carboxylate of fexofenadine, which is precipitated by neutralisation of the solution.

    摘要翻译： 描述了制备非索非那定的方法，其提供4- [4- [4-（羟基二苯基甲基）-1-哌啶基] -1-氧代丁基]-α，α-二甲基苯乙酸 - 烷基酯在水溶液 水和任选的有机溶剂，在碱的存在下; 由此得到4- [4- [4-（羟基二苯基甲基）-1-哌啶基] -1-氧代丁基]-α，α-二甲基苯乙酸的羧酸盐，然后在碱性环境中用氢气将其直接还原为羧酸盐 存在合适的氢化催化剂以得到通过溶液中和而沉淀的非索非那定的羧酸盐。

    Benzoxazinone and benzothiazinone derivatives having cardiovascular activity
    14.
    发明授权
    Benzoxazinone and benzothiazinone derivatives having cardiovascular activity 失效
    具有心血管活性的苯并嗪酮和苯并噻嗪酮衍生物

    公开(公告)号：US5480882A

    公开(公告)日：1996-01-02

    申请号：US347217

    申请日：1994-11-23

    申请人： Alberto Sala ,  Roberto Barani ,  Francesca Benedini ,  Giorgio Bertolini ,  Giancarlo Dona ,  Gianni Gromo ,  Silvio Levi

    发明人： Alberto Sala ,  Roberto Barani ,  Francesca Benedini ,  Giorgio Bertolini ,  Giancarlo Dona ,  Gianni Gromo ,  Silvio Levi

    IPC分类号： A61K31/535 ,  A61K31/536 ,  A61K31/54 ,  A61K31/5415 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  C07D265/22 ,  C07D279/08 ,  C07D413/04 ,  C07D417/04

    CPC分类号： C07D265/22 ,  C07D279/08

    摘要： Compounds of formula I ##STR1## wherein R represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, methylene-dioxy or phenyl, which may be substituted by one or two groups independently selected from hydroxy, halogen, nitro, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy; R.sub.1 and R.sub.2 independently represent hydrogen, COOR.sub.3, --CONR.sub.4 R.sub.5, ##STR2## --OCONR.sub.4 R.sub.5, --OCOR.sub.3, --NR.sub.4 R.sub.5, --OCOOR.sub.6, --NR.sub.3 COR.sub.7, --NR.sub.CONR.sub.4 R.sub.5, --N.dbd.CH--NR.sub.4 R.sub.5, NO.sub.2, CN, OH, SR.sub.3, wherein R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.4 and R.sub.5 independently are hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.6 is C.sub.1 -C.sub.6 alkyl, and R.sub.7 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy, with the proviso that R.sub.1 and R.sub.2 cannot be hydrogen at the same time; X is oxygen or sulphur; Y represents a C.sub.2 -C.sub.6 alkylene chain or a C.sub.5 -C.sub.7 cycloalkylene group; and their pharmaceutically acceptable salts are provided and their use in pharmaceutical compositions which may be used in the treatment of cardiovascular diseases.

    摘要翻译： 式I的化合物其中R表示氢，C1-C6烷基，C5-C7环烷基，亚甲基 - 二氧基或苯基，其可以被一个或两个独立地选自羟基，卤素，硝基，C1 -C 1-6烷基或C 1 -C 6烷氧基; R1和R2独立地表示氢，COOR3，-CONR4R5，-OCONR4R5，-OCOR3，-NR4R5，-OCOOR6，-NR3COR7，-NRCONR4R5，-N = CH-NR4R5，NO2，CN，OH，SR3，其中R3 是氢或C1-C6烷基，R4和R5独立地是氢或C1-C6烷基，R6是C1-C6烷基，R7是氢，C1-C6烷基或C1-C6烷氧基，条件是R1和R2不能 同时是氢; X是氧或硫; Y表示C2-C6亚烷基链或C5-C7亚环烷基; 及其药学上可接受的盐，并且它们可用于可用于治疗心血管疾病的药物组合物中。

    Process for preparing 2,5-disubstituted 3-alkylthiophenes
    19.
    发明申请
    Process for preparing 2,5-disubstituted 3-alkylthiophenes 审中-公开
    制备2,5-二取代的3-烷基噻吩的方法

    公开(公告)号：US20060069272A1

    公开(公告)日：2006-03-30

    申请号：US10530858

    申请日：2003-10-13

    申请人： Giorgio Bertolini ,  Marco Frigerio

    发明人： Giorgio Bertolini ,  Marco Frigerio

    IPC分类号： C07D333/16

    CPC分类号： C07D333/22 ,  C07D333/08 ,  C07D333/16

    摘要： The present invention relates to a process for preparing 2,5-disubstituted 3-alkyl-thiophenes and more particularly to a process for preparing them that comprises an acylation reaction in position 5 of 2-substituted 3-alkylthiophenes. This process does not need reagents which are difficult to handle and does not need anhydrous conditions or inert atmosphere. The resulting product is obtained in high purity.

    摘要翻译： 本发明涉及一种制备2,5-二取代的3-烷基 - 噻吩的方法，更具体地涉及一种制备它们的方法，其包括2-取代的3-烷基噻吩的5位的酰化反应。 该方法不需要难以处理并且不需要无水条件或惰性气氛的试剂。 得到的产物是高纯度的。