METHODS FOR THE PREPARATION OF N-(S)-1-AZABICYCLO[2.2.2]OCT-3-YL-1H-INDAZOLE-3-CARBOXAMIDE HYDROCHLORIDE SALT
    4.
    发明申请
    METHODS FOR THE PREPARATION OF N-(S)-1-AZABICYCLO[2.2.2]OCT-3-YL-1H-INDAZOLE-3-CARBOXAMIDE HYDROCHLORIDE SALT 有权
    制备N-(S)-1-氮杂双环[2.2.2] OCT-3-YL-1H-吲唑-3-羧酰胺盐酸盐的方法

    公开(公告)号:US20120004412A1

    公开(公告)日:2012-01-05

    申请号:US13166850

    申请日:2011-06-23

    IPC分类号: C07D401/12

    摘要: The present invention provides novel methods for preparing N—(S)-1-azabicyclo[2.2.2]oct-3-yl-1H-indazole-3-carboxamide HCl salt 1, a nicotinic α-7 receptor ligand, that are useful for the scaled-up preparation of compound 1. Compound 1 is useful in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders.

    摘要翻译: 本发明提供了制备N-(S)-1-氮杂双环[2.2.2]辛-3-基-1H-吲唑-3-甲酰胺盐酸盐1(烟碱型α-7受体配体)的新方法,它们是有用的 用于化合物1的放大制备。化合物1可用于治疗与缺陷或功能异常的烟碱乙酰胆碱受体(特别是脑)相关的疾病状况,例如用于治疗阿尔茨海默病和精神分裂症以及其他精神病学 和神经障碍。

    METHODS FOR THE PREPARATION OF INDAZOLE-3-CARBOXYLIC ACID AND N-(S)-1-AZABICYCLO[2.2.2]OCT-3-YL-1H-INDAZOLE-3-CARBOXAMIDE HYDROCHLORIDE SALT
    5.
    发明申请
    METHODS FOR THE PREPARATION OF INDAZOLE-3-CARBOXYLIC ACID AND N-(S)-1-AZABICYCLO[2.2.2]OCT-3-YL-1H-INDAZOLE-3-CARBOXAMIDE HYDROCHLORIDE SALT 审中-公开
    用于制备吲哚-3-羧酸和N-(S)-1-氮杂双环[2.2.2] OCT-3-YL-1H-吲唑-3-羧酰胺盐酸盐的方法

    公开(公告)号:US20110172428A1

    公开(公告)日:2011-07-14

    申请号:US12983906

    申请日:2011-01-04

    IPC分类号: C07D453/02 C07D231/56

    摘要: The present invention provides novel methods for preparing indazole-3-carboxylic acid 2, a key starting material for the manufacture of agonists or partial agonists of the nicotinic α-7 receptor, such as N—(S)-1-azabicyclo[2.2.2]oct-3-yl-1H-indazole-3-carboxamide HCl salt 13. Nicotinic α-7 receptor agonists and partial agonists are being useful in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders. The present methods are useful for preparing indazole-3-carboxylic acid on scaled-up levels.

    摘要翻译: 本发明提供了制备吲唑-3-羧酸2的新方法,该吲唑-3-羧酸是用于制备烟碱型α-7受体的激动剂或部分激动剂的关键起始物质,例如N-(S)-1-氮杂双环[2.2。 2]辛-3-基-1H-吲唑-3-甲酰胺盐酸盐13.烟碱型α-7受体激动剂和部分激动剂可用于治疗与缺陷或功能异常的烟碱乙酰胆碱受体(特别是脑部)相关的疾病状况 ,例如用于治疗阿尔茨海默病和精神分裂症,以及其他精神和神经障碍。 本方法可用于按比例放大水平制备吲唑-3-羧酸。

    Methods for the preparation of N-(S)-1-azabicyclo[2.2.2]oct-3-yl-1H-indazole-3-carboxamide hydrochloride salt
    7.
    发明授权
    Methods for the preparation of N-(S)-1-azabicyclo[2.2.2]oct-3-yl-1H-indazole-3-carboxamide hydrochloride salt 有权
    制备N-(S)-1-氮杂双环[2.2.2]辛-3-基-1H-吲唑-3-甲酰胺盐酸盐的方法

    公开(公告)号:US08242276B2

    公开(公告)日:2012-08-14

    申请号:US13166850

    申请日:2011-06-23

    IPC分类号: C07D453/02

    摘要: The present invention provides novel methods for preparing N—(S)-1 -azabicyclo[2.2.2]oct-3-yl-1H-indazole-3-carboxamide HCl salt 1, a nicotinic α-7 receptor ligand, that are useful for the scaled-up preparation of compound 1. Compound 1 is useful in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders.

    摘要翻译: 本发明提供了制备N-(S)-1-氮杂双环[2.2.2]辛-3-基-1H-吲唑-3-甲酰胺盐酸盐1(烟碱型α-7受体配体)的新方法,它们是有用的 用于化合物1的放大制备。化合物1可用于治疗与缺陷或功能异常的烟碱乙酰胆碱受体(特别是脑)相关的疾病状况,例如用于治疗阿尔茨海默病和精神分裂症以及其他精神病学 和神经障碍。

    Process for producing a ribofuranose
    10.
    发明授权
    Process for producing a ribofuranose 失效
    生产呋喃核糖的方法

    公开(公告)号:US07034161B2

    公开(公告)日:2006-04-25

    申请号:US10638740

    申请日:2003-08-11

    IPC分类号: C07D249/08

    CPC分类号: C07H19/056

    摘要: A method of converting pure α-anomer or β/α-anomer mixtures of 1,2,3,5-tetra-O-acetyl-L-ribofuranose to methyl-1-(2,3,5-tri-O-acetyl-β-L-ribofuranosyl)-1,2,4-triazole-3-carboxylate an intermediate for levovirin, as well as, the novel pure α-anomer, alpha 1,2,3,5-tetra-O-acetyl-L-ribofuiranose, are useful in manufacturing levovirin.

    摘要翻译: 将1,2,3,5-四-O-乙酰基-L-呋喃核糖的纯α-异头物或β/α-异头物混合物转化为甲基-1-(2,3,5-三-O-乙酰基 -beta-L-呋喃核糖基)-1,2,4-三唑-3-羧酸酯是一种中间体,用于左旋葡萄球蛋白,以及新的纯α-异头物α1,2,3,5-四-O-乙酰基 - L-ribofuiranose可用于制造levovirin。