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    Methods to manufacture 1,3-dioxolane nucleosides
    1.
    发明授权
    Methods to manufacture 1,3-dioxolane nucleosides 有权
    1,3-二氧戊环核苷的制备方法

    公开(公告)号：US07785839B2

    公开(公告)日：2010-08-31

    申请号：US11051287

    申请日：2005-02-03

    申请人： Marcos Sznaidman ,  George R. Painter ,  Merrick R. Almond ,  Darryl G. Gleary ,  Amir Pesyan

    发明人： Marcos Sznaidman ,  George R. Painter ,  Merrick R. Almond ,  Darryl G. Gleary ,  Amir Pesyan

    IPC分类号： C07D239/00 ,  C07D473/00 ,  C12P19/00 ,  C12P19/38 ,  C12P19/40

    CPC分类号： C07D473/16 ,  C07D317/34 ,  C07D405/04

    摘要： This application provides a process for preparing enantiomerically pure β-D-dioxolane nucleosides. In particular, a new synthesis of (−)-DAPD, suitable for large scale development, is described. In one embodiment the invention provides a process for preparing a substantially pure β-D- or β-L-1,3-dioxolane nucleosides comprising a) preparing or obtaining an esterified 2,2-dialkoxy ethanol; b) cyclizing the esterified 2,2-dialkoxy ethanol with glycolic acid to obtain a 1,3-dioxolane lactone; c) resolving the 1,3-dioxolane lactone to obtain a substantially pure D- or L-lactone; d) selectively reducing and activating the D- or L-chiral lactone to obtain a substantially pure D- or L-1,3-dioxolane; e) coupling the D- or L-1,3-dioxolane to an activated and/or protected purine or pyrimidine base; and f) optionally purifying the nucleoside to obtain a substantially pure protected β-D- or β-L-1,3-dioxolane nucleoside.

    摘要翻译： 本申请提供了制备对映异构体纯的对二氧戊环核苷的方法。 特别地，描述了适用于大规模开发的（ - ） - DAPD的新合成。 在一个实施方案中，本发明提供了制备基本上纯的二 - 或 - bgr--L-1,3-二氧戊环核苷的方法，其包括a）制备或获得酯化的2,2-二烷氧基乙醇; b）用乙醇酸环化酯化的2,2-二烷氧基乙醇得到1,3-二氧戊环内酯; c）拆分1,3-二氧戊环内酯以获得基本上纯的D-或L-内酯; d）选择性还原和活化D-或L-手性内酯，得到基本上纯的D-或L-1,3-二氧戊环; e）将D-或L-1,3-二氧戊环与活化和/或受保护的嘌呤或嘧啶碱基偶联; 和f）任选地纯化所述核苷以获得基本上纯的保护的β-和/或b-l-1,3-二氧戊环核苷。

    Methods to manufacture 1,3-dioxolane nucleosides
    2.
    发明授权
    Methods to manufacture 1,3-dioxolane nucleosides 有权
    1,3-二氧戊环核苷的制备方法

    公开(公告)号：US08420354B2

    公开(公告)日：2013-04-16

    申请号：US12870319

    申请日：2010-08-27

    申请人： Marcos Sznaidman ,  George R. Painter ,  Merrick R. Almond ,  Darryl G. Cleary ,  Amir Pesyan

    发明人： Marcos Sznaidman ,  George R. Painter ,  Merrick R. Almond ,  Darryl G. Cleary ,  Amir Pesyan

    IPC分类号： C12P19/00 ,  C12P19/38 ,  C12P19/40 ,  C07D239/00 ,  C07D239/02 ,  C07D473/00

    CPC分类号： C07D473/16 ,  C07D317/34 ,  C07D405/04

    摘要： This application provides a process for preparing enantiomerically pure β-D-dioxolane nucleosides. In particular, a new synthesis of (−)-DAPD, suitable for large scale development, is described. In one embodiment the invention provides a process for preparing a substantially pure β-D- or β-L-1,3-dioxolane nucleosides comprising a) preparing or obtaining an esterified 2,2-dialkoxy ethanol; b) cyclizing the esterified 2,2-dialkoxy ethanol with glycolic acid to obtain a 1,3-dioxolane lactone; c) resolving the 1,3-dioxolane lactone to obtain a substantially pure D- or L-lactone; d) selectively reducing and activating the D- or L-chiral lactone to obtain a substantially pure D- or L-1,3-dioxolane; e) coupling the D- or L-1,3-dioxolane to an activated and/or protected purine or pyrimidine base; and f) optionally purifying the nucleoside to obtain a substantially pure protected β-D- or β-L-1,3-dioxolane nucleoside.

    摘要翻译： 本申请提供了制备对映异构体纯的对二氧戊环核苷的方法。 特别地，描述了适用于大规模开发的（ - ） - DAPD的新合成。 在一个实施方案中，本发明提供了制备基本上纯的二 - 或 - bgr--L-1,3-二氧戊环核苷的方法，其包括a）制备或获得酯化的2,2-二烷氧基乙醇; b）用乙醇酸环化酯化的2,2-二烷氧基乙醇得到1,3-二氧戊环内酯; c）拆分1,3-二氧戊环内酯以获得基本上纯的D-或L-内酯; d）选择性还原和活化D-或L-手性内酯，得到基本上纯的D-或L-1,3-二氧戊环; e）将D-或L-1,3-二氧戊环与活化和/或受保护的嘌呤或嘧啶碱基偶联; 和f）任选地纯化所述核苷以获得基本上纯的保护的-β-或 - bgr; -L-1,3-二氧戊环核苷。

    Methods to Manufacture 1,3-Dioxolane Nucleosides
    3.
    发明申请
    Methods to Manufacture 1,3-Dioxolane Nucleosides 有权
    1,3-二氧戊环核苷的制备方法

    公开(公告)号：US20110130559A1

    公开(公告)日：2011-06-02

    申请号：US12870319

    申请日：2010-08-27

    申请人： Marcos Sznaidman ,  George R. Painter ,  Merrick R. Almond ,  Darryl G. Cleary ,  Amir Pesyan

    发明人： Marcos Sznaidman ,  George R. Painter ,  Merrick R. Almond ,  Darryl G. Cleary ,  Amir Pesyan

    IPC分类号： C07H19/16

    CPC分类号： C07D473/16 ,  C07D317/34 ,  C07D405/04

    摘要： This application provides a process for preparing enantiomerically pure β-D-dioxolane nucleosides. In particular, a new synthesis of (−)-DAPD, suitable for large scale development, is described. In one embodiment the invention provides a process for preparing a substantially pure β-D- or β-L-1,3-dioxolane nucleosides comprising a) preparing or obtaining an esterified 2,2-dialkoxy ethanol; b) cyclizing the esterified 2,2-dialkoxy ethanol with glycolic acid to obtain a 1,3-dioxolane lactone; c) resolving the 1,3-dioxolane lactone to obtain a substantially pure D- or L-lactone; d) selectively reducing and activating the D- or L-chiral lactone to obtain a substantially pure D- or L-1,3-dioxolane; e) coupling the D- or L-1,3-dioxolane to an activated and/or protected purine or pyrimidine base; and f) optionally purifying the nucleoside to obtain a substantially pure protected β-D- or β-L-1,3-dioxolane nucleoside.

    摘要翻译： 本申请提供了制备对映异构体纯的对二氧戊环核苷的方法。 特别地，描述了适用于大规模开发的（ - ） - DAPD的新合成。 在一个实施方案中，本发明提供了制备基本上纯的二 - 或 - bgr--L-1,3-二氧戊环核苷的方法，其包括a）制备或获得酯化的2,2-二烷氧基乙醇; b）用乙醇酸环化酯化的2,2-二烷氧基乙醇得到1,3-二氧戊环内酯; c）拆分1,3-二氧戊环内酯以获得基本上纯的D-或L-内酯; d）选择性还原和活化D-或L-手性内酯，得到基本上纯的D-或L-1,3-二氧戊环; e）将D-或L-1,3-二氧戊环与活化和/或受保护的嘌呤或嘧啶碱基偶联; 和f）任选地纯化所述核苷以获得基本上纯的保护的β-和/或b-l-1,3-二氧戊环核苷。

    Methods to manufacture 1,3-dioxolane nucleosides
    4.
    发明申请
    Methods to manufacture 1,3-dioxolane nucleosides 有权
    1,3-二氧戊环核苷的制备方法

    公开(公告)号：US20060036092A1

    公开(公告)日：2006-02-16

    申请号：US11051287

    申请日：2005-02-03

    申请人： Marcos Sznaidman ,  George Painter ,  Merrick Almond ,  Darryl Gleary ,  Amir Pesyan

    发明人： Marcos Sznaidman ,  George Painter ,  Merrick Almond ,  Darryl Gleary ,  Amir Pesyan

    IPC分类号： C07D473/10 ,  C07D407/04

    CPC分类号： C07D473/16 ,  C07D317/34 ,  C07D405/04

    摘要： This application provides a process for preparing enantiomerically pure β-D-dioxolane nucleosides. In particular, a new synthesis of (−)-DAPD, suitable for large scale development, is described. In one embodiment the invention provides a process for preparing a substantially pure β-D- or β-L-1,3-dioxolane nucleosides comprising a) preparing or obtaining an esterified 2,2-dialkoxy ethanol; b) cyclizing the esterified 2,2-dialkoxy ethanol with glycolic acid to obtain a 1,3-dioxolane lactone; c) resolving the 1,3-dioxolane lactone to obtain a substantially pure D- or L-lactone; d) selectively reducing and activating the D- or L-chiral lactone to obtain a substantially pure D- or L-1,3-dioxolane; e) coupling the D- or L-1,3-dioxolane to an activated and/or protected purine or pyrimidine base; and f) optionally purifying the nucleoside to obtain a substantially pure protected β-D- or P-L-1,3-dioxolane nucleoside.

    摘要翻译： 该应用提供了制备对映体纯的β-D二氧戊环核苷的方法。 特别地，描述了适用于大规模开发的（ - ） - DAPD的新合成。 在一个实施方案中，本发明提供了制备基本上纯的β-D-或β-L-1,3-二氧戊环核苷的方法，其包括a）制备或获得酯化的2,2-二烷氧基乙醇; b）用乙醇酸环化酯化的2,2-二烷氧基乙醇得到1,3-二氧戊环内酯; c）拆分1,3-二氧戊环内酯以获得基本上纯的D-或L-内酯; d）选择性还原和活化D-或L-手性内酯，得到基本上纯的D-或L-1,3-二氧戊环; e）将D-或L-1,3-二氧戊环与活化和/或受保护的嘌呤或嘧啶碱基偶联; 和f）任选地纯化核苷以获得基本上纯的保护的β-D-或P-L-1,3-二氧戊环核苷。

    Compounds advantageous in the treatment of central nervous system diseases and disorders
    5.
    发明授权
    Compounds advantageous in the treatment of central nervous system diseases and disorders 有权
    有利于治疗中枢神经系统疾病和病症的化合物

    公开(公告)号：US09212155B2

    公开(公告)日：2015-12-15

    申请号：US12881068

    申请日：2010-09-13

    申请人： Amir Pesyan ,  Manuel F. Balandrin

    发明人： Amir Pesyan ,  Manuel F. Balandrin

    IPC分类号： A61K31/165 ,  C07C233/11 ,  C07D295/155 ,  A61K31/353 ,  A61K31/36 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K31/5375 ,  A61K45/06

    CPC分类号： C07D295/155 ,  A61K31/165 ,  A61K31/353 ,  A61K31/36 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K31/5375 ,  A61K45/06

    摘要： A series of novel compounds showing anticonvulsant, chemical countermeasure(s), and analgesic activities is described. Such pharmaceutically active compounds may also show utility in the treatment of other central nervous system (“CNS”) diseases and disorders, such as anxiety, depression, insomnia, migraine headaches, schizophrenia, Parkinson's disease, spasticity, Alzheimer's disease, and bipolar disorder. Furthermore, such compounds may additionally find utility as analgesics (e.g., for the treatment of chronic or neuropathic pain) and as neuroprotective agents useful in the treatment of stroke(s), chronic neurodegenerative diseases (such as Alzheimer's disease and Huntington's disease), and/or traumatic brain and/or spinal cord injuries. Moreover, these/such compounds may also be useful in the treatment of status epilepticus and/or as chemical countermeasures.

    摘要翻译： 描述了一系列显示抗惊厥，化学对策和止痛活性的新型化合物。 此类药物活性化合物还可用于治疗其它中枢神经系统（“CNS”）疾病和病症，例如焦虑，抑郁，失眠，偏头痛，精神分裂症，帕金森病，痉挛状态，阿尔茨海默病和双相情感障碍。 此外，这些化合物还可用作止痛剂（例如，用于治疗慢性或神经性疼痛）和用作治疗中风，慢性神经变性疾病（如阿尔茨海默病和亨廷顿疾病）的神经保护剂，以及 /或创伤性脑部和/或脊髓损伤。 此外，这些/这样的化合物也可用于治疗癫痫持续状态和/或作为化学应对措施。