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    Process for enantiomerically pure .beta.-L-1,3-oxathiolane nucleosides
    3.
    发明授权
    Process for enantiomerically pure .beta.-L-1,3-oxathiolane nucleosides 失效
    对映体纯β-1,3-氧硫杂环戊烷核苷的方法

    公开(公告)号：US5248776A

    公开(公告)日：1993-09-28

    申请号：US803086

    申请日：1991-12-05

    申请人： Chung K. Chu ,  Lak-Shin Jeong ,  J. Warren Beach

    发明人： Chung K. Chu ,  Lak-Shin Jeong ,  J. Warren Beach

    IPC分类号： A61K31/675 ,  C07D327/04 ,  C07D411/04 ,  C07D473/00 ,  C07D497/08

    CPC分类号： A61K31/7076 ,  A61K31/675 ,  C07D327/04 ,  C07D411/04 ,  C07D473/00 ,  C07D497/08

    摘要： An asymmetric process for the preparation of enantiomerically pure .beta.-L-(-)-1,3-oxathiolane-nucleosides that includes the initial preparation of the key chiral intermediates (2R,5R) and (2R,5S)-5-(O-protected)-2-(protected-oxymethyl)-1,3-oxathiolane from 1,6-thioanhydro-L-gulose. The 2R,5(R,S)-5-(O-protected)-2-(protected-oxymethyl)-1,3-oxathiolane is condensed with a desired heterocyclic base, typically a purine or pyrimidine base, to provide the product nucleoside. The synthesis can be used to prepare the pharmaceutically important compound, .beta.-L-(-)-1-[(2.beta.,4.beta.)-2-(hydroxymethyl)-4-(1,3-thioxolane)]cytosine (.beta.-L-(-)BCH-189).

    摘要翻译： 用于制备对映体纯的β-L-（ - ） - 1,3-氧硫杂环戊烷 - 核苷的不对称方法，其包括关键手性中间体（2R，5R）和（2R，5S）-5-（O 保护的）-2-（保护的 - 氧甲基）-1,3-氧硫杂环戊烷，由1,6-硫代氢化-L-古洛糖。 将2R，5（R，S）-5-（O-保护的）-2-（保护的 - 氧甲基）-1,3-氧硫杂环戊烷与所需的杂环碱（通常为嘌呤或嘧啶碱基）缩合，得到产物 核苷。 该合成可用于制备药学上重要的化合物，β-L-（ - ） - 1 - [（2β，4β）-2-（羟甲基）-4-（1,3-硫代羟烷基）]胞嘧啶 -L - （ - ）BCH-189）。

    NOVEL ANALOGS OF CHOLINE FOR NEUROPROTECTION AND COGNITIVE ENHANCEMENT IN NEURODEGENERATIVE DISORDERS
    4.
    发明申请
    NOVEL ANALOGS OF CHOLINE FOR NEUROPROTECTION AND COGNITIVE ENHANCEMENT IN NEURODEGENERATIVE DISORDERS 审中-公开
    神经保护和神经增生性疾病的认知增强的新型胆固醇

    公开(公告)号：US20100324064A1

    公开(公告)日：2010-12-23

    申请号：US12841684

    申请日：2010-07-22

    申请人： Jerry J. BUCCAFUSCO ,  Alvin V. Terry ,  J. Warren Beach ,  Rammamohanna R. Jonnala

    发明人： Jerry J. BUCCAFUSCO ,  Alvin V. Terry ,  J. Warren Beach ,  Rammamohanna R. Jonnala

    IPC分类号： A61K31/496 ,  C07D207/277 ,  A61K31/4015 ,  C07D401/04 ,  A61K31/4439 ,  C07D401/06 ,  C07C211/03 ,  A61K31/137 ,  C07D213/38 ,  A61K31/4406 ,  C07C69/14 ,  A61K31/222 ,  A61P25/00 ,  A61P25/28

    CPC分类号： C07D213/38 ,  C07C215/08 ,  C07C219/06 ,  C07D213/74 ,  C07D295/088 ,  C07D401/06

    摘要： The present invention relates to novel analogs of choline and methods of use or treatment of neurodegenerative disorders and/or conditions such as Parkinson's disease, Huntington disease, Alzheimer's disease and related disorders such as amyotrophic lateral sclerosis, spinal muscular atrophy, Friedrich's ataxia, Pick's disease, Bassen-Kornzweig syndrome, Refsom's disease, retinal degeneration, Cruetzfelt-Jacob syndrome or prion disease (mad cow disease), dementia with Lewy bodies, schizophrenia, paraneoplastic cerebellar degeneration and neurodegenerative conditions caused by stroke. The present compounds are effective to treat any neurological condition where acetylcholine transmission neurons and their target cells are affected. Compounds according to the present invention are effective to alleviate and/or reverse the effects of a neurodegenerative condition, prevent further deterioration and/or enhance cognition and memory in patients suffering from neurodegenerative disorders, especially Alzheimer's disease.

    摘要翻译： 本发明涉及胆碱的新类似物以及使用或治疗神经退行性疾病和/或病症如帕金森病，亨廷顿病，阿尔茨海默病和相关疾病如肌萎缩性侧索硬化，脊髓性肌萎缩，弗里德里希共济失调，皮克病 ，Bassen-Kornzweig综合征，Refsom病，视网膜变性，Cruetzfelt-Jacob综合征或朊病毒疾病（疯牛病），路易体痴呆，精神分裂症，副肿瘤性小脑变性和由中风引起的神经变性疾病。 本发明化合物可有效治疗乙酰胆碱传递神经元及其靶细胞受影响的任何神经病症。 根据本发明的化合物有效地减轻和/或逆转神经变性病症的作用，防止进一步恶化和/或增强患有神经退行性疾病，特别是阿尔茨海默病的患者的认知和记忆。

    Analogs of choline for neuroprotection and cognitive enhancement in neurodegenerative disorders
    7.
    发明授权
    Analogs of choline for neuroprotection and cognitive enhancement in neurodegenerative disorders 有权
    类似物胆碱在神经退行性疾病中的神经保护和认知增强

    公开(公告)号：US07786147B2

    公开(公告)日：2010-08-31

    申请号：US11075473

    申请日：2005-03-09

    申请人： Jerry J. Buccafusco ,  Alvin V. Terry ,  J. Warren Beach ,  Rammamohanna R. Jonnala

    发明人： Jerry J. Buccafusco ,  Alvin V. Terry ,  J. Warren Beach ,  Rammamohanna R. Jonnala

    IPC分类号： C07D401/02 ,  C07D401/06 ,  A61K31/4439

    CPC分类号： C07D213/38 ,  C07C215/08 ,  C07C219/06 ,  C07D213/74 ,  C07D295/088 ,  C07D401/06

    摘要： The present invention relates to novel analogs of choline and methods of use or treatment of neurodegenerative disorders and/or conditions such as Parkinson's disease, Huntington disease, Alzheimer's disease and related disorders such as amyotrophic lateral sclerosis, spinal muscular atrophy, Friedrich's ataxia, Pick's disease, Bassen-Kornzweig syndrome, Refsom's disease, retinal degeneration, Cruetzfelt-Jacob syndrome or prion disease (mad cow disease), dementia with Lewy bodies, schizophrenia, paraneoplastic cerebellar degeneration and neurodegenerative conditions caused by stroke. The present compounds are effective to treat any neurological condition where acetylcholine transmission neurons and their target cells are affected. Compounds according to the present invention are effective to alleviate and/or reverse the effects of a neurodegenerative condition, prevent further deterioration and/or enhance cognition and memory in patients suffering from neurodegenerative disorders, especially Alzheimer's disease.

    摘要翻译： 本发明涉及胆碱的新类似物以及使用或治疗神经退行性疾病和/或病症如帕金森病，亨廷顿病，阿尔茨海默病和相关疾病如肌萎缩性侧索硬化，脊髓性肌萎缩，弗里德里希共济失调，皮克病 ，Bassen-Kornzweig综合征，Refsom病，视网膜变性，Cruetzfelt-Jacob综合征或朊病毒疾病（疯牛病），路易体痴呆，精神分裂症，副肿瘤性小脑变性和由中风引起的神经变性疾病。 本发明化合物可有效治疗乙酰胆碱传递神经元及其靶细胞受影响的任何神经病症。 根据本发明的化合物有效地减轻和/或逆转神经变性病症的作用，防止进一步恶化和/或增强患有神经退行性疾病，特别是阿尔茨海默病的患者的认知和记忆。

    Analogs of choline for neuroprotection and cognitive enhancement in neurodegenerative disorders
    8.
    发明授权
    Analogs of choline for neuroprotection and cognitive enhancement in neurodegenerative disorders 有权
    类似物胆碱在神经退行性疾病中的神经保护和认知增强

    公开(公告)号：US06881738B2

    公开(公告)日：2005-04-19

    申请号：US10199205

    申请日：2002-07-18

    申请人： Jerry J. Buccafusco ,  Alvin V. Terry ,  J. Warren Beach ,  Rammamohanna R. Jonnala

    发明人： Jerry J. Buccafusco ,  Alvin V. Terry ,  J. Warren Beach ,  Rammamohanna R. Jonnala

    IPC分类号： A61P25/28 ,  C07C215/08 ,  C07C219/06 ,  C07D213/38 ,  C07D213/74 ,  C07D295/088 ,  C07D401/06 ,  A61K31/496 ,  C07D401/14 ,  C07D403/06

    CPC分类号： C07D213/38 ,  C07C215/08 ,  C07C219/06 ,  C07D213/74 ,  C07D295/088 ,  C07D401/06

    摘要： The present invention relates to novel analogs of choline and methods of use or treatment of neurodegenerative disorders and/or conditions such as Parkinson's disease, Huntington disease, Alzheimer's disease and related disorders such as amyotrophic lateral sclerosis, spinal muscular atrophy, Friedrich's ataxia, Pick's disease, Bassen-Kornzweig syndrome, Refsom's disease, retinal degeneration, Cruetzfelt-Jacob syndrome or prion disease (mad cow disease), dementia with Lewy bodies, schizophrenia, paraneoplastic cerebellar degeneration and neurodegenerative conditions caused by stroke. The present compounds are effective to treat any neurological condition where acetylcholine transmission neurons and their target cells are affected. Compounds according to the present invention are effective to alleviate and/or reverse the effects of a neurodegenerative condition, prevent further deterioration and/or enhance cognition and memory in patients suffering from neurodegenerative disorders, especially Alzheimer's disease.

    摘要翻译： 本发明涉及胆碱的新类似物以及使用或治疗神经退行性疾病和/或病症如帕金森病，亨廷顿病，阿尔茨海默病和相关疾病如肌萎缩性侧索硬化，脊髓性肌萎缩，弗里德里希共济失调，皮克病 ，Bassen-Kornzweig综合征，Refsom病，视网膜变性，Cruetzfelt-Jacob综合征或朊病毒疾病（疯牛病），路易体痴呆，精神分裂症，副肿瘤性小脑变性和由中风引起的神经变性疾病。 本发明化合物可有效治疗乙酰胆碱传递神经元及其靶细胞受影响的任何神经病症。 根据本发明的化合物有效地减轻和/或逆转神经变性病症的作用，防止进一步恶化和/或增强患有神经退行性疾病，特别是阿尔茨海默病的患者的认知和记忆。