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61 条记录 (耗时 0.033 秒)

    Process for the preparation of entacapone
    22.
    发明授权
    Process for the preparation of entacapone 失效
    恩他卡朋的制备方法

    公开(公告)号：US07750177B2

    公开(公告)日：2010-07-06

    申请号：US11958778

    申请日：2007-12-18

    申请人： Simone Mantegazza ,  Pietro Allegrini ,  Gabriele Razzetti

    发明人： Simone Mantegazza ,  Pietro Allegrini ,  Gabriele Razzetti

    IPC分类号： C07C255/23

    CPC分类号： C07C253/30 ,  C07C255/41

    摘要： A process for the preparation of entacapone, in particular as the polymorphic form A, comprising the preparation of a compound of formula (V), wherein R is C1-C6 alkyl, by condensation of N,N-diethyl-cyano-acetamide with a compound of formula (IV), wherein R is C1-C6 alkyl, in the presence of a strong basic agent; the dealkylation of the compound of formula (V) to obtain entacapone, and the crystallization thereof from methyl ethyl ketone is performed to yield the polymorphic form A. The polymorphic form A of entacapone may be used to treat Parkinson's disease and/or to enhance effectiveness of muscle control.

    摘要翻译： 恩替卡宾的制备方法，特别是多晶型A，其包括通过N，N-二乙基 - 氰基 - 乙酰胺与一种或多种式I化合物的缩合制备其中R为C1-C6烷基的式（Ⅴ）化合物 式（Ⅳ）化合物，其中R为C1-C6烷基，在强碱性试剂存在下; 进行式（V）化合物的脱烷基化以获得恩他卡朋，并从甲基乙基酮中进行结晶，得到多晶型A.恩他卡朋的多晶型A可用于治疗帕金森病和/或增强有效性 的肌肉控制。

    PROCESS FOR THE PREPARATION OF ZILEUTON
    23.
    发明申请
    PROCESS FOR THE PREPARATION OF ZILEUTON 审中-公开
    制备ZILEUTON的方法

    公开(公告)号：US20090286996A1

    公开(公告)日：2009-11-19

    申请号：US12423122

    申请日：2009-04-14

    申请人： Emanuele ATTOLINA ,  Gianmaria Dell'Anna ,  Roberto Rossi ,  Pietro Allegrini ,  Gabriele Razzetti

    发明人： Emanuele ATTOLINA ,  Gianmaria Dell'Anna ,  Roberto Rossi ,  Pietro Allegrini ,  Gabriele Razzetti

    IPC分类号： C07D333/58 ,  C07D333/60 ,  C07F7/10

    CPC分类号： C07D333/56 ,  C07D333/58 ,  C07F7/1804 ,  Y02P20/55

    摘要： Process for preparing a compound of formula (I), or a salt thereof, comprising reacting of a compound of formula (II) wherein X and R are as herein defined; with a compound of formula (III) NH2OZ  (III) wherein Z is a hydroxy protecting group, in presence of a catalyst, to obtain a compound of formula (IV), or a salt thereof, removing the hydroxyl protecting group to obtain a compound of formula (V), or a salt thereof; converting a compound of formula (V), or a salt thereof, into a compound of formula (I), or a salt thereof; and, if desired, converting a compound of formula (I) into a salt thereof, or vice versa.

    摘要翻译： 制备式（I）化合物或其盐的方法，包括其中X和R如本文所定义的式（II）化合物的反应; 与式（III）化合物（其中Z为羟基保护基）在催化剂存在下反应，得到式（Ⅳ）化合物或其盐，除去羟基保护基，得到化合物 式（Ⅴ）化合物或其盐; 将式（Ⅴ）化合物或其盐转化为式（I）化合物或其盐; 如果需要，将式（I）化合物转化为其盐，反之亦然。

    PROCESS FOR THE PREPARATION OF PYRIDINE COMPOUNDS
    25.
    发明申请
    PROCESS FOR THE PREPARATION OF PYRIDINE COMPOUNDS 失效
    制备吡啶化合物的方法

    公开(公告)号：US20070249662A1

    公开(公告)日：2007-10-25

    申请号：US11737852

    申请日：2007-04-20

    申请人： Pietro ALLEGRINI ,  Marcello Rasparini ,  Gabriele Razzetti ,  Roberto Rossi ,  Gianpiero Ventimiglia

    发明人： Pietro ALLEGRINI ,  Marcello Rasparini ,  Gabriele Razzetti ,  Roberto Rossi ,  Gianpiero Ventimiglia

    IPC分类号： A61K31/4439 ,  A61K31/4745 ,  C07D471/02 ,  C07D403/02

    CPC分类号： C07D471/04 ,  C07D401/12

    摘要： A process for preparation of a compound of formula (I), both as the isomeric mixture and individual isomers, wherein Q is ═CR8— or ═N—; each R1, R2, R3, R4 is independently selected from hydrogen, halogen, hydroxy; nitro; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen or C1-C6 alkoxy; phenyl-C1-C6 alkyl; phenyl-C1-C6 alkoxy; and —N(RaRb) wherein each Ra and Rb is independently hydrogen or C1-C6 alkyl or Ra and Rb, taken together with the nitrogen atom they are linked to, form a saturated heterocyclic ring; andeach R5, R6, R7, R8 is independently selected from hydrogen, halogen, hydroxy; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen; C1-C6 alkyl-carbonyl, C1-C6 alkoxy-carbonyl, and oxazol-2-yl; comprising converting a compound of formula (IV), to said compound of formula (I), in the presence of a catalyst, if necessary in an organic solvent.

    摘要翻译： 制备式（I）化合物的方法，均为异构体混合物和各异构体，其中Q为-CR 8 - 或-N-; 每个R 1，R 2，R 3，R 4，R 4独立地选自氢，卤素，羟基; 硝基 任选被羟基取代的C 1 -C 6烷基; 烷硫基C 1 -C 6烷基; 任选被卤素或C 1 -C 6烷氧基取代的C 1 -C 6烷氧基; 苯基-C 1 -C 6烷基; 苯基-C 1 -C 6烷氧基; 和-N（RaRb），其中每个R a和R b独立地是氢或C 1 -C 6烷基或R a和R b与它们所连接的氮原子一起 形成饱和杂环; 并且每个R 5，R 6，R 7，R 8和R 8独立地选自氢，卤素，羟基 ; 任选被羟基取代的C 1 -C 6烷基; 烷硫基C 1 -C 6烷基; 任选被卤素取代的C 1 -C 6烷氧基; C 1 -C 6烷基 - 羰基，C 1 -C 6烷氧基 - 羰基和恶唑-2（C 1 -C 6） - 基; 包括在催化剂存在下，如果需要在有机溶剂中将式（Ⅳ）化合物转化为所述式（Ⅳ）化合物。

    Process for the purification of rufinamide
    30.
    发明授权
    Process for the purification of rufinamide 有权
    Rufinamide净化方法

    公开(公告)号：US08461190B2

    公开(公告)日：2013-06-11

    申请号：US13451651

    申请日：2012-04-20

    申请人： Pietro Allegrini ,  Dario Pastorello ,  Gabriele Razzetti

    发明人： Pietro Allegrini ,  Dario Pastorello ,  Gabriele Razzetti

    IPC分类号： A61K31/41 ,  C07D249/00

    CPC分类号： C07D249/04

    摘要： A process for purifying Rufinamide, comprising: a) providing a dispersion of crude 1-[(2,6-difluorophenyl)methyl]-1H-1,2,3-triazole-4-carboxamide in a solvent mixture containing at least a carboxylic acid, and dissolving it; b) slowly cooling the solution to precipitate Rufinamide crystalline form A; and c) recovering the solid.

    摘要翻译： 一种用于纯化Rufinamide的方法，包括：a）提供粗制的1 - [（2,6-二氟苯基）甲基] -1H-1,2,3-三唑-4-甲酰胺在含有至少一种羧酸 酸，并溶解; b）缓慢冷却溶液以沉淀Ruformamide结晶形式A; 和c）回收固体。