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    10-Substituted Cytisine Derivatives and Methods of Use Thereof
    1.
    发明申请
    10-Substituted Cytisine Derivatives and Methods of Use Thereof 审中-公开
    10取代的Cytisine衍生物及其使用方法

    公开(公告)号：US20100048606A1

    公开(公告)日：2010-02-25

    申请号：US12295157

    申请日：2007-03-29

    申请人： Alan P. Kozikowski ,  Werner Tueckmantel ,  Sheela Chellappan ,  Kenneth J. Kellar ,  Yingxian Xiao

    发明人： Alan P. Kozikowski ,  Werner Tueckmantel ,  Sheela Chellappan ,  Kenneth J. Kellar ,  Yingxian Xiao

    IPC分类号： A61K31/439 ,  C07D471/18

    CPC分类号： C07D471/18

    摘要： The present invention relates to substituted cytisine compounds that are useful in treating diseases impacted by a nicotinic ACh receptor. One aspect of the invention relates to 10-substituted cytisine compounds. In certain instances, the cytisine is substituted in the 10-position by an alkyl, aryl or aralkyl group. The present invention also relates to a pharmaceutical composition comprises the substituted cytisine compound or the 10-substituted cytisine compound. The invention also relates to a method of modulation a nicotinic ACh receptor in a mammal, comprising the step of administering to a mammal in need thereof a therapeutically effective amount of a substituted cytisine. In certain instances, the substituted cytisine is a 10-substituted cytisine. Another aspect of the present invention relates a method of treating a disease impacted by a nicotinic ACh receptor, comprising the step of administering to a mammal in need thereof a therapeutically effective amount of a substituted cytisine. In certain instances, the substituted cytisine is a 10-substituted cytisine.

    摘要翻译： 本发明涉及可用于治疗受烟碱性ACh受体影响的疾病的取代的仙培酮化合物。 本发明的一个方面涉及10-取代的仙客来化合物。 在某些情况下，通过烷基，芳基或芳烷基在十位置替代赤藓酸。 本发明还涉及药物组合物，其包含取代的仙客来化合物或10-取代的仙客来化合物。 本发明还涉及一种调节哺乳动物中烟碱性ACh受体的方法，其包括向有需要的哺乳动物施用治疗有效量的取代的氰尿酸的步骤。 在某些情况下，取代的洋甘菊是一种10-取代的胞苷。 本发明的另一方面涉及一种治疗由烟碱性ACh受体影响的疾病的方法，其包括向有需要的哺乳动物施用治疗有效量的取代的洋甘菊的步骤。 在某些情况下，取代的洋甘菊是一种10-取代的胞苷。

    Ligands for nicotinic acetylcholine receptors, and methods of making and using them
    2.
    发明授权
    Ligands for nicotinic acetylcholine receptors, and methods of making and using them 有权
    烟碱乙酰胆碱受体的配体，以及制造和使用它们的方法

    公开(公告)号：US08030300B2

    公开(公告)日：2011-10-04

    申请号：US10558607

    申请日：2004-06-09

    申请人： Alan P. Kozikowski ,  John L. Musachio ,  Kenneth J. Kellar ,  Yingxian Xiao ,  Zhi-Liang Wei ,  Hong Fan

    发明人： Alan P. Kozikowski ,  John L. Musachio ,  Kenneth J. Kellar ,  Yingxian Xiao ,  Zhi-Liang Wei ,  Hong Fan

    IPC分类号： A61K31/4427 ,  C07D401/12

    CPC分类号： C07D471/18 ,  C07D487/08

    摘要： One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor. The present invention also relates to the use of a compound of the invention for treating a mammal suffering from Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism or trichtillomania.

    摘要翻译： 本发明的一个方面涉及作为烟碱乙酰胆碱受体配体的杂环化合物。 本发明的第二方面涉及本发明化合物用于调节哺乳动物烟碱乙酰胆碱受体的用途。 本发明还涉及本发明化合物用于治疗患有阿尔茨海默病，帕金森病，运动障碍，图雷特综合征，精神分裂症，注意力缺陷障碍，焦虑，疼痛，抑郁，强迫症，化学物质滥用的哺乳动物的用途 酒精中毒，记忆缺陷，假性痴呆，甘ser综合征，偏头痛，贪食症，肥胖症，经前期综合征或晚期黄体期综合征，烟草滥用，创伤后综合征，社交恐惧症，慢性疲劳综合征，早泄，勃起障碍，神经性厌食症， 睡眠障碍，自闭症，多发性或三叉神经痛。

    Ligands for Nicotinic Acetylcholine Receptors, and Methods of Making and Using Them
    3.
    发明申请
    Ligands for Nicotinic Acetylcholine Receptors, and Methods of Making and Using Them 有权
    尼古丁乙酰胆碱受体配体及其制备和使用方法

    公开(公告)号：US20080132486A1

    公开(公告)日：2008-06-05

    申请号：US10558607

    申请日：2004-06-09

    申请人： Alan P. Kozikowski ,  John L. Musachio ,  Kenneth J. Kellar ,  Yingxian Xiao ,  Zhi-Liang Wei

    发明人： Alan P. Kozikowski ,  John L. Musachio ,  Kenneth J. Kellar ,  Yingxian Xiao ,  Zhi-Liang Wei

    IPC分类号： A61K31/55 ,  A61K31/4745 ,  C07D471/14

    CPC分类号： C07D471/18 ,  C07D487/08

    摘要： One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor. The present invention also relates to the use of a compound of the invention for treating a mammal suffering from Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism or trichtillomania.

    摘要翻译： 本发明的一个方面涉及作为烟碱乙酰胆碱受体配体的杂环化合物。 本发明的第二方面涉及本发明化合物用于调节哺乳动物烟碱乙酰胆碱受体的用途。 本发明还涉及本发明化合物用于治疗患有阿尔茨海默病，帕金森病，运动障碍，图雷特综合征，精神分裂症，注意力缺陷障碍，焦虑，疼痛，抑郁，强迫症，化学物质滥用的哺乳动物的用途 酒精中毒，记忆缺陷，假性痴呆，甘ser综合征，偏头痛，贪食症，肥胖症，经前期综合征或晚期黄体期综合征，烟草滥用，创伤后综合征，社交恐惧症，慢性疲劳综合征，早泄，勃起障碍，神经性厌食症， 睡眠障碍，自闭症，多发性或三叉神经痛。

    Process for preparing procyanidin(4-6 or 4-8) oligomers and their derivatives
    4.
    发明授权
    Process for preparing procyanidin(4-6 or 4-8) oligomers and their derivatives 失效
    原花青素（4-6或4-8）寡聚体及其衍生物的制备方法

    公开(公告)号：US06207842B1

    公开(公告)日：2001-03-27

    申请号：US08948226

    申请日：1997-10-09

    申请人： Leo J. Romanczyk, Jr. ,  Alan P. Kozikowski ,  Werner Tueckmantel

    发明人： Leo J. Romanczyk, Jr. ,  Alan P. Kozikowski ,  Werner Tueckmantel

    IPC分类号： C07D31126

    CPC分类号： C07H17/06 ,  A61K31/35 ,  C07D311/32 ,  C07D311/60 ,  C07D311/62

    摘要： A process is disclosed for the production of polyphenol oligomers having n polyphenol monomers, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomers. Advantageously, polyphenol monomers forming the polyphenol oligomers may be the same or different.

    摘要翻译： 公开了一种制备具有n多酚单体的多酚低聚物的方法，n是2-18的整数。 该方法包括将被保护的酚羟基的被保护的多酚与C-4官能化的多酚单体的偶联。 受保护的多酚可以是受保护的多酚单体或具有2-17个单体的被保护的多酚低聚物。 有利地，形成多酚低聚物的多酚单体可以相同或不同。

    Synthetic methods for preparation of protected proanthocyanidin(s)
    6.
    发明授权
    Synthetic methods for preparation of protected proanthocyanidin(s) 失效
    用于制备被保护的原花色素的合成方法

    公开(公告)号：US06420572B1

    公开(公告)日：2002-07-16

    申请号：US09169554

    申请日：1998-10-09

    申请人： Leo J. Romanczyk, Jr. ,  Alan P. Kozikowski ,  Werner Tueckmantel ,  Marc E. Lippman

    发明人： Leo J. Romanczyk, Jr. ,  Alan P. Kozikowski ,  Werner Tueckmantel ,  Marc E. Lippman

    IPC分类号： C07D31160

    CPC分类号： C07H17/06 ,  A61K31/35 ,  C07D311/32 ,  C07D311/60 ,  C07D311/62

    摘要： A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.

    摘要翻译： 公开了用于生产具有多酚单体单元的多酚低聚物的方法，n为2-18的整数。 该方法包括将被保护的酚羟基的被保护的多酚与C-4官能化的多酚单体的偶联。 受保护的多酚可以是受保护的多酚单体或具有2-17单体单元的被保护的多酚低聚物。 有利地，形成多酚低聚物的多酚单体单元可以是相同或不同的类黄酮化合物。

    Combination of huperzine and nicotinic compounds as a neuroprotective agent
    10.
    发明授权
    Combination of huperzine and nicotinic compounds as a neuroprotective agent 有权
    组合石杉碱和烟碱化合物作为神经保护剂

    公开(公告)号：US06369052B1

    公开(公告)日：2002-04-09

    申请号：US09910819

    申请日：2001-07-23

    申请人： Kenneth J. Kellar ,  Alan P. Kozikowski

    发明人： Kenneth J. Kellar ,  Alan P. Kozikowski

    IPC分类号： A61K3155

    CPC分类号： A61K31/465 ,  A61K31/44 ,  A61K2300/00

    摘要： The present invention provides compositions and methods for treating, preventing, or reversing neuronal dysfunction including cognitive decline, such as cognitive decline associated with aging and minimal cognitive impairment; severe neurodegenerative disorders, such as Alzheimer's disease; and neuronal dysfunction associated with loss of motor skills, such as Parkinson's disease and amyotrophic lateral sclerosis. The compositions and methods of the invention can also treat or prevent neuronal dysfunction resulting from CNS injury, such as stroke, spinal-cord injury, and peripheral-nerve injury. The compositions of the invention comprises a huperzine compound and a nicotinic compound.

    摘要翻译： 本发明提供用于治疗，预防或逆转神经元功能障碍的组合物和方法，包括认知衰退，例如与衰老相关的认知衰退和最小的认知障碍; 严重的神经变性疾病，如阿尔茨海默病; 以及与运动技能丧失相关的神经元功能障碍，例如帕金森病和肌萎缩性侧索硬化。 本发明的组合物和方法还可以治疗或预防由CNS损伤引起的神经元功能障碍，例如中风，脊髓损伤和外周神经损伤。 本发明的组合物包含石杉碱化合物和烟碱化合物。