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41 条记录 (耗时 0.039 秒)

    Process for chiral 3-(1-amino-1,1-bisalkylmethyl)-1-substituted-pyrrolidines
    31.
    发明授权
    Process for chiral 3-(1-amino-1,1-bisalkylmethyl)-1-substituted-pyrrolidines 失效
    手性3-（1-氨基-1,1-双烷基甲基）-1-取代吡咯烷的方法

    公开(公告)号：US5347017A

    公开(公告)日：1994-09-13

    申请号：US88464

    申请日：1993-07-07

    申请人： Victor Fedij ,  Mark J. Suto ,  James N. Wemple ,  James R. Zeller

    发明人： Victor Fedij ,  Mark J. Suto ,  James N. Wemple ,  James R. Zeller

    IPC分类号： C07D207/09 ,  C07D207/50

    CPC分类号： C07D207/09

    摘要： The process for the preparation of chiral 3-(1-amino-1,1-bisalkylmethyl)-1-substituted-pyrrolidines used as key intermediates for the preparation of naphthyridine and quinolone antibacterial agents which comprises reacting readily available chiral 1-substituted-3-pyrrolidinols to their corresponding chiral sulfonate esters; converting the sulfonate esters to chiral 1-substituted-3-cyanopyrrolidines having an inverse configuration, and then dialkylating the chiral cyanopyrrolidines with alkyl lithium in the presence of a Lewis acid without racemization at the asymmetric carbon atom is described.

    摘要翻译： 用作制备萘啶和喹诺酮抗菌剂的关键中间体的手性3-（1-氨基-1,1-双烷基甲基）-1-取代吡咯烷的制备方法，其包括使容易获得的手性1-取代-3 - 吡咯烷醇与其相应的手性磺酸酯; 将磺酸酯转化成具有相反构型的手性1-取代-3-氰基吡咯烷酮，然后在不对称碳原子下进行外消旋化的路易斯酸存在下，用烷基锂二烷基化手性氰基吡咯烷。

    Process for the synthesis of novel and known nitroimidazoles which are useful as sensitizing agents
    33.
    发明授权
    Process for the synthesis of novel and known nitroimidazoles which are useful as sensitizing agents 失效
    用于合成可用作敏化剂的新型和已知的硝基咪唑的方法

    公开(公告)号：US5073639A

    公开(公告)日：1991-12-17

    申请号：US532428

    申请日：1990-06-04

    申请人： Mark J. Suto

    发明人： Mark J. Suto

    IPC分类号： C07D233/91 ,  C07D403/06 ,  C07D413/06

    CPC分类号： C07D403/06 ,  C07D233/91 ,  C07D413/06

    摘要： The present invention is a novel process for preparing both known and novel nitroimidazoles having novel intermediates. The process advantageously reduces the number of process steps, provides increased yield with both greater safety and greater control of stereoisomerism in the products.

    摘要翻译： 本发明是制备具有新型中间体的已知和新型硝基咪唑的新方法。 该方法有利地减少了工艺步骤的数量，提供了增加的产率，同时具有更高的安全性和更好地控制产品中的立体异构性。

    Certain optically active substituted 3-pyrraidine acetic acid derivatives useful as intermediates
    34.
    发明授权
    Certain optically active substituted 3-pyrraidine acetic acid derivatives useful as intermediates 失效
    某些用作中间体的光学活性取代的3-吡咯烷酸乙酸衍生物

    公开(公告)号：US5072001A

    公开(公告)日：1991-12-10

    申请号：US621101

    申请日：1990-11-30

    申请人： Susan E. Hagen ,  Mark J. Suto

    发明人： Susan E. Hagen ,  Mark J. Suto

    IPC分类号： C07D207/08 ,  C07D207/09 ,  C07D401/04 ,  C07D471/04

    CPC分类号： C07D207/08 ,  C07D207/09 ,  C07D401/04 ,  C07D471/04

    摘要： Optically pure isomers of 7-[3-(1,1-dialkylmethyl-1-amino)-1-pyrrolidinyl]quinolones and naphthyridones as therapeutically active and safe antibacterial agents are described, as well as pharmaceutical compositions thereof, and a method of treating bacterial infections therewith. Also described is a method of manufacture of the quinolones and naphthyridones as well as the starting materials, the optically pure pyrrolidine moieties for attachment at the 7-position.

    摘要翻译： 描述了作为治疗活性和安全的抗菌剂的7- [3-（1,1-二烷基甲基-1-氨基）-1-吡咯烷基]喹诺酮和萘啶酮的光学纯异构体及其药物组合物，以及治疗方法 细菌感染。 还描述了制备喹诺酮和萘啶酮的方法以及起始材料，用于连接在7-位的光学纯的吡咯烷部分。

    Haloalkylaminomethyl-2-nitro-1H-imidazoles
    35.
    发明授权
    Haloalkylaminomethyl-2-nitro-1H-imidazoles 失效
    卤代烷基氨基甲基-2-硝基-1H-咪唑

    公开(公告)号：US4954515A

    公开(公告)日：1990-09-04

    申请号：US274209

    申请日：1988-11-25

    申请人： Mark J. Suto

    发明人： Mark J. Suto

    IPC分类号： A61K31/415 ,  A61K31/42 ,  A61P35/00 ,  C07D233/91 ,  C07D403/06 ,  C07D413/06

    CPC分类号： C07D403/06 ,  C07D233/91 ,  C07D413/06

    摘要： The present invention is novel nitroimidazoles useful as radiosensitizing or chemosensitizing agents in the treatment of hypoxic tumor cells. Also, the present invention is a novel process for preparing both known and novel nitroimidazoles having novel intermediates. The process advantageously reduces the number of process steps, provides increased yield with both greater safety and greater control of stereo-isomerism in the products.

    SODIUM CHANNEL INHIBITORS
    37.
    发明申请
    SODIUM CHANNEL INHIBITORS 有权
    钠通道抑制剂

    公开(公告)号：US20100267782A1

    公开(公告)日：2010-10-21

    申请号：US12669018

    申请日：2008-07-14

    申请人： Serge Beaudoin ,  Matthew Scott Johnson ,  Brain Edward Marron ,  Mark J. Suto

    发明人： Serge Beaudoin ,  Matthew Scott Johnson ,  Brain Edward Marron ,  Mark J. Suto

    IPC分类号： A61K31/425 ,  C07D277/52 ,  A61P25/00

    CPC分类号： C07D277/52

    摘要： Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.

    摘要翻译： 提供了可用于通过电压门控钠通道抑制钠离子通量来治疗疾病的化合物，组合物和方法。 更具体地，本发明提供取代的芳基磺酰胺，包含这些化合物的组合物，以及使用这些化合物或组合物治疗中枢或周围神经系统疾病，特别是疼痛和慢性疼痛的方法，其通过阻断与起始相关的钠通道或 指示条件复发。 本发明的化合物，组合物和方法特别用于通过电压门控钠通道抑制离子通量来治疗神经性或炎性疼痛。

    Inhibitors of ion channels
    38.
    发明授权
    Inhibitors of ion channels 失效
    离子通道抑制剂

    公开(公告)号：US07615569B2

    公开(公告)日：2009-11-10

    申请号：US11464057

    申请日：2006-08-11

    申请人： Alan Fulp ,  Brian Marron ,  Mark J. Suto ,  Xiaodong Wang

    发明人： Alan Fulp ,  Brian Marron ,  Mark J. Suto ,  Xiaodong Wang

    IPC分类号： A61K31/427 ,  A61K31/513 ,  C07D283/02 ,  C07D277/52 ,  C07D277/28 ,  C07D403/10

    CPC分类号： C07D417/12 ,  C07D401/12 ,  C07D417/14

    摘要： Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides heterocyclic aryl sulfonamides, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.

    摘要翻译： 提供了可用于通过电压门控钠通道抑制钠离子通量来治疗疾病的化合物，组合物和方法。 更具体地，本发明提供了可用于治疗中枢或周围神经系统疾病，特别是疼痛和慢性疼痛的杂环芳基磺酰胺，组合物和方法，其通过阻断与所述病症的发作或复发相关的钠通道。 本发明的化合物，组合物和方法特别用于通过电压门控钠通道抑制离子通量来治疗神经性或炎性疼痛。