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1. 发明申请

WO2007115092A3 10-SUBSTITUTED CYTISINE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译： 10替代的CYTISINE衍生物及其使用方法
公开(公告)号：WO2007115092A3
公开(公告)日：2008-07-31
申请号：PCT/US2007065498
申请日：2007-03-29
申请人： UNIV GEORGETOWN , KOZIKOWSKI ALAN P , TUECKMANTEL WERNER , CHELLAPPAN SHEELA , KELLAR KENNETH J , XIAO YINGXIAN
发明人： KOZIKOWSKI ALAN P , TUECKMANTEL WERNER , CHELLAPPAN SHEELA , KELLAR KENNETH J , XIAO YINGXIAN
IPC分类号： A61K31/4375 , A61K31/439
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。本发明还涉及一种药物组合物，其包含取代的赤藓苷化合物或10-取代的仙茅素化合物。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。

2. 发明申请

WO2005000806A2 LIGANDS FOR NICOTINIC ACETYLCHOLINE RECEPTORS, AND METHODS OF MAKING AND USING THEM 审中-公开
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：WO2005000806A2
公开(公告)日：2005-01-06
申请号：PCT/US2004018340
申请日：2004-06-09
申请人： UNIV GEORGETOWN , KOZIKOWSKI ALAN P , MUSACHIO JOHN L , KELLAR KENNETH J , XIAO YINGXIAN , WEI ZHI-LIANG
发明人： KOZIKOWSKI ALAN P , MUSACHIO JOHN L , KELLAR KENNETH J , XIAO YINGXIAN , WEI ZHI-LIANG
IPC分类号： A61K31/4375 , A61K31/439 , A61P25/00 , C07D20060101 , C07D471/18 , C07D487/08 , C07D
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. 发明申请

WO2009143507A3 SILENT DESENSITIZERS OF NEURONAL NACHR AND METHODS OF USE THEREOF 审中-公开
标题翻译：神经NACHR的静电渗透剂及其使用方法
公开(公告)号：WO2009143507A3
公开(公告)日：2010-03-11
申请号：PCT/US2009045136
申请日：2009-05-26
申请人： UNIV GEORGETOWN , BROWN MILTON , PAIGE MIKELL A , XIAO YINGXIAN , KELLAR KENNETH J
发明人： BROWN MILTON , PAIGE MIKELL A , XIAO YINGXIAN , KELLAR KENNETH J
IPC分类号： C07D403/14 , A61K31/395 , A61P25/28 , C07D401/04 , 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。

4. 发明申请

WO2008011484A2 NICOTINIC DESENSITIZERS AND METHODS OF SELECTING, TESTING, AND USING THEM 审中-公开
标题翻译： NICOTINIC DESENSITIZERS及其选择，测试和使用方法
公开(公告)号：WO2008011484A2
公开(公告)日：2008-01-24
申请号：PCT/US2007073814
申请日：2007-07-18
申请人： BETHESDA PHARMACOLOGY ASSOCIAT , XIAO YINGXIAN , KELLAR KENNETH J
发明人： XIAO YINGXIAN , KELLAR KENNETH J
IPC分类号： A61K31/4745
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。

5. 发明申请

WO03018004A2 ANALGESICS AND METHODS OF USE 审中-公开
标题翻译：使用的方法和方法
公开(公告)号：WO03018004A2
公开(公告)日：2003-03-06
申请号：PCT/US0227936
申请日：2002-08-29
申请人： ENDO PHARMACEUTICALS INC , SMITH-CARLISS RICHARD , CARUSO FRANK S , CROOKS PHD PETER , KELLAR KENNETH J , XIAO YINGXIAN
发明人： SMITH-CARLISS RICHARD , CARUSO FRANK S , CROOKS PHD PETER , KELLAR KENNETH J , XIAO YINGXIAN
IPC分类号： A61K31/40 , A61K31/4015 , A61K31/44 , A61K31/4439 , A61P25/04 , C07D207/06 , C07D207/20 , C07D207/22 , C07D207/26 , C07D207/267 , C07D209/96 , C07D401/04
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。

6. 发明公开

EP2776423A4 PHENYL-SUBSTITUTED NICOTINIC LIGANDS, AND METHODS OF USE THEREOF 审中-公开
标题翻译：尼日利亚联合王国维多利亚州立大学
公开(公告)号：EP2776423A4
公开(公告)日：2015-01-07
申请号：EP12847869
申请日：2012-11-09
申请人： UNIV GEORGETOWN , UNIV DUKE
发明人： BROWN MILTON L , PAIGE MIKELL A , XIAO YINGXIAN , KELLAR KENNETH J , YENUGONDA VENKATA MAHIDHAR , LEVIN EDWARD D , REZVANI AMIR H
IPC分类号： C07D403/06
CPC分类号： C07D401/12 , C07D213/65
摘要： Disclosed are compounds and methods of using them to treat a disorder selected from the group consisting of addiction, pain, obesity, schizophrenia, epilepsy, mania and manic depression, anxiety, Alzheimer's disease, learning deficit, cognition deficit, attention deficit, memory loss, Lewy Body Dementia, Attention Deficit Hyperactivity Disorder (ADHD), Parkinson's disease, Huntington's disease, Tourette's syndrome, amyotrophic lateral sclerosis, inflammation, stroke, spinal cord injury, dyskinesias, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, autism, mutism, trichotillomania, hypothermia, and disorders of sleep.
摘要翻译：公开了使用它们治疗选自瘾，疼痛，肥胖，精神分裂症，癫痫，躁狂和躁狂抑郁，焦虑，阿尔茨海默病，学习缺陷，认知缺陷，注意力缺陷，记忆丧失，路易体痴呆，注意缺陷多动障碍（ADHD），帕金森病，亨廷顿病，图雷特综合征，肌萎缩性侧索硬化，炎症，中风，脊髓损伤，运动障碍，强迫症，化学物质滥用，酒精中毒，记忆缺陷，假性痴呆，甘ser综合征，偏头痛，贪食症，经前期综合征或晚黄体期综合症，烟草滥用，创伤后综合征，社交恐惧症，慢性疲劳综合征，早泄，勃起困难，神经性厌食症，孤独症，多发症，头痛，低体温和失调的睡眠

7. 发明公开

EP2983666A4 2-HALO-5-ALKYNYL-PYRIDYL NICOTINIC LIGANDS 审中-公开
标题翻译： 2-卤代-5-炔基 - 吡啶基 - NIKOTINLIGANDEN
公开(公告)号：EP2983666A4
公开(公告)日：2016-11-16
申请号：EP14775233
申请日：2014-03-26
申请人： UNIV GEORGETOWN
发明人： XIAO YINGXIAN , KELLAR KENNETH J , BROWN MILTON L , PAIGE MIKELL A , LIU YONG
IPC分类号： A61K31/44 , A61K31/397 , C07D205/02
CPC分类号： C07D401/12
摘要： Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including 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, trichotillomania, and hypothermia.

8. 发明公开

EP2324014A4 SILENT DESENSITIZERS OF NEURONAL NACHR AND METHODS OF USE THEREOF 审中-公开
标题翻译：神经元MESS SILENT脱敏物质和申请流程。
公开(公告)号：EP2324014A4
公开(公告)日：2011-10-19
申请号：EP09751735
申请日：2009-05-26
申请人： UNIV GEORGETOWN
发明人： BROWN MILTON , PAIGE MIKELL A , XIAO YINGXIAN , KELLAR KENNETH J
IPC分类号： C07D401/12 , A61K31/395 , A61P25/28 , C07D401/14 , C07D405/14 , C07D409/14
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14

9. 发明公开

EP2776030A4 2,5-DISUBSTITUTED-PYRIDYL NICOTINIC LIGANDS, AND METHODS OF USE THEREOF 审中-公开
标题翻译： 2,5-取代的吡啶基烟碱配体及其用途
公开(公告)号：EP2776030A4
公开(公告)日：2015-05-06
申请号：EP12848512
申请日：2012-11-09
申请人： UNIV GEORGETOWN , UNIV DUKE
发明人： XIAO YINGXIAN , KELLAR KENNETH J , BROWN MILTON L , PAIGE MIKELL A , LIU YONG , LEVIN EDWARD D , REZVANI AMIR H
IPC分类号： A61K31/44 , C07D401/12
CPC分类号： A61K31/4427 , A61K9/0019 , A61K9/0043 , A61K9/0053 , A61K9/006 , A61K31/4439 , C07D401/12
摘要： Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including 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, trichotillomania, and hypothermia.
摘要翻译：公开了作为烟碱乙酰胆碱受体配体的杂环化合物。这些化合物可用于治疗患有一系列治疗适应症，包括阿尔茨海默病，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，焦虑症，疼痛，抑郁症，强迫症，化学物质滥用酒精中毒，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，孤独症，多发性，头发性短暂症和低体温。

10. 发明申请

WO0211712A3 COMBINATION OF HUPERZINE AND NICOTINIC COMPOUNDS AS A NEUROPROTECTIVE AGENT 审中-公开
公开(公告)号：WO0211712A3
公开(公告)日：2002-12-27
申请号：PCT/US0124302
申请日：2001-08-03
申请人： UNIV GEORGETOWN
发明人： KELLAR KENNETH J , KOZIKOWSKI ALAN P
IPC分类号： A61K31/465 , A61P25/00
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.

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