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1. 发明申请

US20100048606A1 10-Substituted Cytisine Derivatives and Methods of Use Thereof 审中-公开
标题翻译： 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。

2. 发明申请

US20080132486A1 Ligands for Nicotinic Acetylcholine Receptors, and Methods of Making and Using Them 有权
标题翻译：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。

3. 发明授权

US08030300B2 Ligands for nicotinic acetylcholine receptors, and methods of making and using them 有权
标题翻译：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。

4. 发明申请

US20110269733A1 Silent Desensitizers of Neuronal nAChR and Methods of Use Thereof 有权
标题翻译：神经元nAChR的沉默脱敏剂及其使用方法
公开(公告)号：US20110269733A1
公开(公告)日：2011-11-03
申请号：US12994376
申请日：2009-05-26
申请人： Milton I. Brown , Mikell A. Paige , Yingxian Xiao , Kenneth J. Kellar
发明人： Milton I. Brown , Mikell A. Paige , Yingxian Xiao , Kenneth J. Kellar
IPC分类号： A61K31/4439 , C07D401/12 , A61K31/4427 , C07D405/14 , A61K31/443 , A61K31/444 , C07D409/14 , A61K31/4436 , A61P29/00 , A61P3/04 , A61P25/18 , A61P25/00 , A61P17/00 , A61P25/16 , A61P25/14 , A61P25/28 , A61P9/12 , A61P11/14 , A61P25/30 , C07D401/14
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14
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.
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。

5. 发明授权

US08642612B2 Nicotinic desensitizers and methods of selecting, testing, and using them 有权
标题翻译：烟碱脱敏剂及其选择，测试和使用方法
公开(公告)号：US08642612B2
公开(公告)日：2014-02-04
申请号：US12374172
申请日：2007-07-18
申请人： Yingxian Xiao , Kenneth J. Kellar
发明人： Yingxian Xiao , Kenneth J. Kellar
IPC分类号： A01N43/40 , A61K31/435
CPC分类号： C07D401/12 , A61K31/4745 , C07D471/18 , G01N33/9406 , G01N33/944 , G01N2500/02
摘要： The present invention discloses nicotinic desensitizers and methods of selecting, testing, and using them. The present invention provides methods for selecting nicotinic desensitizers from one or more compounds by using receptor, cell, and tissue models; and methods for testing one or more nicotinic desensitizers for their therapeutic utility by using animal models. The present invention also provides compounds of formula (I) and (II) as nicotinic desensitizers. Nicotinic desensitizers of the present invention are useful for the treatment of a wide range of conditions, diseases, and disorders.
摘要翻译：本发明公开了烟碱脱敏剂及其选择，测试和使用方法。本发明提供了通过使用受体，细胞和组织模型从一种或多种化合物中选择烟碱脱敏剂的方法; 以及通过使用动物模型测试一种或多种烟碱脱敏剂用于其治疗用途的方法。本发明还提供式（I）和（II）的化合物作为烟碱型脱敏剂。本发明的烟碱脱敏剂可用于治疗广泛的病症，疾病和病症。

6. 发明申请

US20100129291A1 NICOTINIC DESENSITIZERS AND METHODS OF SELECTING, TESTING, AND USING THEM 有权
标题翻译： NICOTINIC DESENSITIZERS及其选择，测试和使用方法
公开(公告)号：US20100129291A1
公开(公告)日：2010-05-27
申请号：US12374172
申请日：2007-07-18
申请人： Yingxian Xiao , Kenneth J. Kellar
发明人： Yingxian Xiao , Kenneth J. Kellar
IPC分类号： A61K31/439 , A61K31/4427 , A61K31/4439 , A61K49/00 , G01N33/53
CPC分类号： C07D401/12 , A61K31/4745 , C07D471/18 , G01N33/9406 , G01N33/944 , G01N2500/02
摘要： The present invention discloses nicotinic desensitizers and methods of selecting, testing, and using them. The present invention provides methods for selecting nicotinic desensitizers from one or more compounds by using receptor, cell, and tissue models; and methods for testing one or more nicotinic desensitizers for their therapeutic utility by using animal models. The present invention also provides compounds of formula (I) and (II) as nicotinic desensitizers. Nicotinic desensitizers of the present invention are useful for the treatment of a wide range of conditions, diseases, and disorders.
摘要翻译：本发明公开了烟碱脱敏剂及其选择，测试和使用方法。本发明提供了通过使用受体，细胞和组织模型从一种或多种化合物中选择烟碱脱敏剂的方法; 以及通过使用动物模型测试一种或多种烟碱脱敏剂用于其治疗用途的方法。本发明还提供式（I）和（II）的化合物作为烟碱型脱敏剂。本发明的烟碱脱敏剂可用于治疗广泛的病症，疾病和病症。

7. 发明授权

US08729103B2 Silent desensitizers of neuronal nAChR and methods of use thereof 有权
标题翻译：神经元nAChR的沉默脱敏剂及其使用方法
公开(公告)号：US08729103B2
公开(公告)日：2014-05-20
申请号：US12994376
申请日：2009-05-26
申请人： Milton L. Brown , Mikell A. Paige , Yingxian Xiao , Kenneth J. Kellar
发明人： Milton L. Brown , Mikell A. Paige , Yingxian Xiao , Kenneth J. Kellar
IPC分类号： A61K31/4439 , C07D401/14
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14
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.
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。

8. 发明申请

US20110281836A1 Silent desensitizers of neuronal NACHR and methods of use thereof 审中-公开
标题翻译：神经元NACHR的沉默脱敏剂及其使用方法
公开(公告)号：US20110281836A1
公开(公告)日：2011-11-17
申请号：US12927688
申请日：2010-11-19
申请人： Joel R. Walker , Milton Brown , Mikell A. Paige , Yingxian Xiao , Kenneth J. Kellar
发明人： Joel R. Walker , Milton Brown , Mikell A. Paige , Yingxian Xiao , Kenneth J. Kellar
IPC分类号： A61K31/4025 , C07D401/14 , A61P25/30 , A61P25/00 , A61P3/04 , A61P25/18 , A61P25/08 , A61P25/22 , A61P25/28 , A61P25/16 , A61P25/14 , A61P29/00 , A61P17/00 , A61P1/00 , A61P1/04 , A61P1/12 , A61P5/00 , A61P5/14 , A61P9/12 , A61P25/32 , C07D409/14 , C07D405/04 , C07D401/12
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14
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.
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。

9. 发明授权

US07964714B2 Gene expression suppression agents 失效
标题翻译：基因表达抑制剂
公开(公告)号：US07964714B2
公开(公告)日：2011-06-21
申请号：US10552909
申请日：2003-05-12
申请人： Yingxian Xiao , Xin-Hua Feng
发明人： Yingxian Xiao , Xin-Hua Feng
IPC分类号： C12Q1/68 , C12P19/34 , C12N15/00 , C07H21/02 , C07H21/04
CPC分类号： C12N15/111 , C12N2310/111 , C12N2310/14 , C12N2310/53 , C12N2330/30
摘要： A method is provided for making gene suppression agents to be used in eukaryotic cells by using a recombinant DNA construct containing at least one transcriptional unit compromising a transcriptional promoter, a template sequence for making a RNA molecule, and a transcriptional terminator. Mechanisms of the RNA mediated gene suppression include, but are not limited to, RNA interferences (RNAi). The use of the agents as tools for biomedical research as well as medicinal products is also disclosed.
摘要翻译：提供了通过使用含有至少一个转录启动子的转录单位的重组DNA构建体，用于制备RNA分子的模板序列和转录终止子来制备用于真核细胞的基因抑制剂的方法。 RNA介导的基因抑制的机制包括但不限于RNA干扰（RNAi）。还公开了作为生物医学研究工具以及药用产品的用途。

10. 发明申请

US20070129434A1 Analgesics and methods of use 审中-公开
标题翻译：止痛药和使用方法
公开(公告)号：US20070129434A1
公开(公告)日：2007-06-07
申请号：US10501692
申请日：2004-07-15
申请人： Richard Smith-Carliss , Frank Caruso , Peter Crooks , Kenneth Kellar , Yingxian Xiao
发明人： Richard Smith-Carliss , Frank Caruso , Peter Crooks , Kenneth Kellar , Yingxian Xiao
IPC分类号： A61K31/24
CPC分类号： C07D207/267 , A61K31/40 , A61K31/44 , C07D207/06 , C07D207/20 , C07D207/22 , C07D209/96 , C07D401/04
摘要： A method for inducing analgesia and/or inhibiting abuse of abusive substances includes administration of d-methadone metabolites or their structural analogs. The d-methadone metabolites, EMDP and EDDP, and their structural analogs may be incorporated into a suitable pharmaceutical composition for administration to patients. The invention includes the method itself, certain structural analogs, and pharmaceutical compositions for use in accordance with the method.
摘要翻译：用于诱导镇痛和/或抑制滥用滥用物质的方法包括给予美沙酮代谢物或其结构类似物。 d美沙酮代谢物，EMDP和EDDP及其结构类似物可以并入用于给予患者的合适的药物组合物中。本发明包括方法本身，某些结构类似物和根据该方法使用的药物组合物。

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