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249 条记录 (耗时 0.038 秒)

    Stable salts of novel derivatives of 3,3-diphenylpropylamines
    74.
    发明授权
    Stable salts of novel derivatives of 3,3-diphenylpropylamines 有权
    3,3-二苯基丙胺新衍生物的稳定盐

    公开(公告)号：US06858650B1

    公开(公告)日：2005-02-22

    申请号：US10130214

    申请日：2000-11-15

    申请人： Claus Meese

    发明人： Claus Meese

    IPC分类号： A61P13/00 ,  A61K31/24 ,  A61P13/06 ,  C07B61/00 ,  C07C213/06 ,  C07C215/54 ,  C07C219/28 ,  C07C229/38 ,  A01N37/08 ,  A01N37/12 ,  A01N37/44 ,  A61K31/215 ,  A61N31/24

    CPC分类号： C07C215/54 ,  C07B2200/07 ,  C07C219/28 ,  C07C229/38

    摘要： The present invention concerns highly pure, crystalline, stable compounds of novel derivatives of 3,3-diphenylpropylamines in the form of their salts, a method for the manufacture and highly pure, stable intermediate products.The method is in particular characterized by regio- and chemoselectivity and high yield. Salts of phenolic monoesters of 3,3-diphenylpropylamines are provided, that are particularly well-suited for use in pharmaceutical formulations. Preferred compounds are R-(+)-2-(3-diisopropylamino-1-phenyl-propyl)-4-hydroxymethylphenylisobutyrate ester hydrogen fumarate and R-(+)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenylisobutyrate ester hydrochloride hydrate. Furthermore, stable, crystalline intermediate products that are essential for obtaining the abovementioned salts are provided. A preferred intermediate product is R-(−)-3-(3-diisopropylamino-phenyl-propyl)-4-hydroxy-benzoic acid methyl ester.

    摘要翻译： 本发明涉及其盐形式的3,3-二苯基丙胺的新衍生物的高纯度，结晶，稳定的化合物，制备方法和高纯度，稳定的中间产物。该方法的特征在于区域和 化学选择性高，产量高。 提供了3,3-二苯基丙胺的酚单酯的盐，特别适用于药物制剂。 优选的化合物是R - （+） - 2-（3-二异丙基氨基-1-苯基 - 丙基）-4-羟甲基苯基异丁酸酯氢富马酸酯和R - （+） - 2-（3-二异丙基氨基-1-苯基丙基） 羟甲基苯基异丁酸酯盐酸盐水合物。 此外，提供了获得上述盐所必需的稳定的结晶中间产物。 优选的中间产物是R - （ - ） - 3-（3-二异丙基氨基 - 苯基 - 丙基）-4-羟基 - 苯甲酸甲酯。

    Nmda receptor channel blocker with neuroprotective activity
    76.
    发明申请
    Nmda receptor channel blocker with neuroprotective activity 失效
    具有神经保护活性的Nmda受体通道阻滞剂

    公开(公告)号：US20040054013A1

    公开(公告)日：2004-03-18

    申请号：US10381956

    申请日：2003-09-25

    发明人： Kwok-Keung Tai ,  Sylvie E. Blondelle ,  Richard A. Houghten ,  Mauricio Montal

    IPC分类号： A61K031/137

    CPC分类号： C07C215/54 ,  A61K31/00 ,  A61K31/137 ,  C07B2200/07 ,  C07C211/27 ,  C40B40/00

    摘要： Neuroprotectant agents are provided which do not contain peptides and are protected from the degradation that limits the use of peptide-based drugs in systemic circulation. With great selectivity for NMDA receptors, the agents exert an open channel block on NMDA receptors, and protect neuronal cells containing such receptors from excitotoxic cell death.

    摘要翻译： 提供的神经保护剂不含有肽并被保护免受限制基于肽的药物在全身循环中的使用的降解。 对NMDA受体具有极大的选择性，该药物在NMDA受体上发挥开放通道阻断，并保护含有此类受体的神经细胞免受兴奋性毒性细胞死亡。

    Phenyl propenone compounds
    78.
    发明申请
    Phenyl propenone compounds 失效
    苯基丙烯酮化合物

    公开(公告)号：US20030204114A1

    公开(公告)日：2003-10-30

    申请号：US10401361

    申请日：2003-03-28

    发明人： Pher G. Andersson ,  Christian Hedberg

    IPC分类号： C07C213/02

    CPC分类号： C07D311/20 ,  C07B2200/07 ,  C07C29/143 ,  C07C35/32 ,  C07C45/512 ,  C07C45/65 ,  C07C45/74 ,  C07C49/835 ,  C07C213/00 ,  C07C213/02 ,  C07C215/54 ,  C07C2602/24 ,  C07C49/67 ,  C07C49/813

    摘要： The invention relates to a process for the enantioselective preparation of tolterodiine and analogues and salts thereof comprises the steps of: a) enantioselectively reducing the carbonyl function in a compound of formula (II): 1 wherein R1, R2 and R3 independently of each other are hydrogen, methyl, methoxy, hydroxy, hydroxymethyl, carbamoyl, sulphamoyl or halogen, to form an enantiomerically enriched compound of formula (IIIa) or (IIIb): 2 wherein R1, R2 and R3 are as defined above; b) subjecting the compound of formula (IIIa) or (IIIb) to a sigmatropic rearrangement to form a corresponding enantiomerically enriched compound of formula (IVa) or (IVb): 3 wherein R1, R2 and R3 are as defined above; c) subjecting the compound of formula (IVa) or (IVb) to a Baeyer-Villiger oxidation to form a corresponding enantiomerically enriched compound of the general formula (Va) or (Vb): 4 wherein R1, R2 and R3 are as defined above; d) converting the compound of formula (Va) or (Vb) to form the corresponding enantiometrically enriched compound of tolterodine or analogue, and e) optionally converting a compound obtained in base form to a salt thereof, or converting a salt form to the free base. The invention also relates to novel starting materials and intermediates used in the process.

    摘要翻译： 本发明涉及一种对映选择性制备托特罗定及其类似物及其盐的方法，包括以下步骤：a）在式（II）化合物中对映体选择性还原羰基官能团：其中R1，R2和R3彼此独立地为氢 ，甲基，甲氧基，羟基，羟甲基，氨基甲酰基，氨磺酰基或卤素，以形成对映异构体富集的式（IIIa）或（IIIb）化合物：其中R1，R2和R3如上定义; b）使式（IIIa）或（IIIb）化合物进行sigmatropic重排以形成相应的对映体富集的式（Ⅳa）或（Ⅳb）化合物：其中R 1，R 2和R 3如上所定义; c）使式（Ⅳa）或（Ⅳb）化合物经Baeyer-Villiger氧化反应形成通式（Ⅴa）或（Ⅴb）的相应对映体富集的化合物：其中R 1，R 2和R 3如上定义; d）转化式（Va）或（Vb）的化合物以形成托特罗定或类似物的相应对映体富集的化合物，和e）任选地将以碱形式获得的化合物转化成其盐，或将盐形式转化为游离的 基础。 本发明还涉及在该方法中使用的新起始材料和中间体。

    Phenyl inden-1-one compounds
    79.
    发明申请
    Phenyl inden-1-one compounds 失效
    苯基茚-1-酮化合物

    公开(公告)号：US20030191348A1

    公开(公告)日：2003-10-09

    申请号：US10402671

    申请日：2003-03-28

    发明人： Pher G. Andersson ,  Christian Hedberg

    IPC分类号： C07C211/27

    CPC分类号： C07D311/20 ,  C07B2200/07 ,  C07C29/143 ,  C07C35/32 ,  C07C45/512 ,  C07C45/65 ,  C07C45/74 ,  C07C49/835 ,  C07C213/00 ,  C07C213/02 ,  C07C215/54 ,  C07C2602/24 ,  C07C49/67 ,  C07C49/813

    摘要： The invention relates to a process for the enantioselective preparation of tolterodine and analogues and salts thereof comprises the steps of: a) enantioselectively reducing the carbonyl function in a compound of formula (II): 1 wherein R1; R2 and R3 independently of each other are hydrogen, methyl, methoxy, hydroxy, hydroxymethyl, carbamoyl, sulphamoyl or halogen, to form an enantiomerically enriched compound of formula (IIIa) or (IIIb): 2 wherein R1, R2 and R3 are as defined above; b) subjecting the compound of formula (IIIa) or (IIIb) to a sigmatropic rearrangement to form a corresponding enantiomerically enriched compound of formula (IVa) or (IVb): 3 wherein R1, R2 and R3 are as defined above; c) subjecting the compound of formula (IVa) or (IVb) to a Baeyer-Villiger oxidation to form a corresponding enantiomerically enriched compound of the general formula (Va) or (Vb). 4 wherein R1, R2 and R3 are as defined above; d) converting the compound of formula (Va) or (Vb) to form the corresponding enantiometrically enriched compound of tolterodine or analogue, and e) optionally converting a compound obtained in base form to a salt thereof, or converting a salt form to the free base. The invention also relates to novel starting materials and intermediates used in the process.

    摘要翻译： 本发明涉及托特罗定及其类似物及其盐的对映选择性制备方法，其包括以下步骤：a）在式（II）化合物中对映体选择性还原羰基官能团：其中R1; R2和R3彼此独立地是氢，甲基，甲氧基，羟基，羟甲基，氨基甲酰基，氨磺酰基或卤素，以形成对映体富集的式（IIIa）或（IIIb）化合物：其中R1，R2和R3如上定义 ; b）使式（IIIa）或（IIIb）化合物进行sigmatropic重排以形成相应的对映体富集的式（Ⅳa）或（Ⅳb）化合物：其中R 1，R 2和R 3如上所定义; c）使式（Ⅳa）或（Ⅳb）化合物进行Baeyer-Villiger氧化，形成通式（Ⅴa）或（Ⅴb）的相应对映体富集的化合物。 其中R1，R2和R3如上定义; d）转化式（Va）或（Vb）的化合物以形成托特罗定或类似物的相应对映体富集的化合物，和e）任选地将以碱形式获得的化合物转化成其盐，或将盐形式转化为游离的 基础。 本发明还涉及在该方法中使用的新起始材料和中间体。

    Process and intermediates
    80.
    发明授权
    Process and intermediates 失效
    工艺和中间体

    公开(公告)号：US06566537B2

    公开(公告)日：2003-05-20

    申请号：US09919401

    申请日：2001-07-31

    申请人： Pher G. Andersson ,  Christian Hedberg

    发明人： Pher G. Andersson ,  Christian Hedberg

    IPC分类号： C07D31102

    CPC分类号： C07D311/20 ,  C07B2200/07 ,  C07C29/143 ,  C07C35/32 ,  C07C45/512 ,  C07C45/65 ,  C07C45/74 ,  C07C49/835 ,  C07C213/00 ,  C07C213/02 ,  C07C215/54 ,  C07C2602/24 ,  C07C49/67 ,  C07C49/813

    摘要： The invention relates to a process for the enantioselective preparation of tolterodine and analogues and salts thereof comprises the steps of: a) enantioselectively reducing the carbonyl function in a compound of formula (II): wherein R1, R2 and R3 independently of each other are hydrogen, methyl, methoxy, hydroxy, hydroxymethyl, carbamoyl, sulphamoyl or halogen, to form an enantiomerically enriched compound of formula (IIIa) or (IIIb): wherein R1, R2 and R3 are as defined above; b) subjecting the compound of formula (IIIa) or (IIb) to a sigmatropic rearrangement to form a corresponding enantiomerically enriched compound of formula (IVa) or (IVb): wherein R1, R2 and R3 are as defined above; c) subjecting the compound of formula (IVa) or (IVb) to a Baeyer-Villiger oxidation to form a corresponding enantiomerically enriched compound of the general formula (Va) or (Vb): wherein R1, R2 and R3 are as defined above; d) converting the compound of formula (Va) or (Vb) to form the corresponding enantiometrically enriched compound of tolterodine or analogue, and e) optionally converting a compound obtained in base form to a salt thereof, or converting a salt form to the free base. The invention also relates to novel starting materials and intermediates used in the process.

    摘要翻译： 本发明涉及一种用于对映选择性制备托特罗定及其类似物及其盐的方法，包括以下步骤：a）对式（II）化合物中对映体选择性还原羰基官能团：其中R1，R2和R3彼此独立地为氢 ，甲基，甲氧基，羟基，羟甲基，氨基甲酰基，氨磺酰基或卤素，以形成对映体富集的式（IIIa）或（IIIb）化合物：其中R1，R2和R3如上定义; b） IIIa）或（IIb）化合物以形成相应的对映异构体富集的式（IVa）或（IVb）化合物：其中R 1，R 2和R 3如上所定义; c）使式（Ⅳa）化合物或（ IVb）至Baeyer-Villiger氧化反应形成通式（Ⅴa）或（Ⅴb）的相应对映异构体富集的化合物：其中R 1，R 2和R 3如上定义; d）将式（Ⅴa）化合物或（ Vb）形成相应的对应 富马酸或其类似物的富集的化合物，和）任选地将以碱形式获得的化合物转化为其盐，或将盐形式转化为游离碱。本发明还涉及在该方法中使用的新的起始原料和中间体。