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41. 发明授权

US07098331B2 Arylvinylazacycloalkane compounds and methods of preparation and use thereof 有权
标题翻译：芳基乙烯基氮杂环烷烃化合物及其制备和使用方法
公开(公告)号：US07098331B2
公开(公告)日：2006-08-29
申请号：US10379868
申请日：2003-03-05
申请人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Arielle Genevois-Borella , Marc Capet , Michel Cheve
发明人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Arielle Genevois-Borella , Marc Capet , Michel Cheve
IPC分类号： C07D405/12 , C07D239/26
CPC分类号： A61K31/506 , C07D405/14
摘要： Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.
摘要翻译：公开了式（I）的新型乙烯基氮杂环烷化合物。这些化合物是各种nAChR的配体。化合物及其药学上可接受的盐可用于制备旨在预防或治疗与nAChR功能障碍相关的疾病，特别是在中枢神经系统或胃肠系统内的药物组合物和/或药物。可以治疗的疾病类型的实例包括神经变性疾病，包括中枢神经系统疾病如阿尔茨海默病，认知障碍，运动障碍如帕金森病，药物成瘾，行为障碍和胃肠系统内的炎性疾病。化合物也可用作治疗急性，慢性或复发性疼痛的镇痛药。

42. 发明授权

US06743812B1 Pharmaceutical compositions and methods for use 失效
标题翻译：药物组合物和使用方法
公开(公告)号：US06743812B1
公开(公告)日：2004-06-01
申请号：US09616187
申请日：2000-07-14
申请人： Gary Maurice Dull
发明人： Gary Maurice Dull
IPC分类号： A61K3144
CPC分类号： A61K31/465 , A61K31/19 , A61K2300/00
摘要： Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are 2,3-diacyltartaric acid salts of E-metanicotine.
摘要翻译：通过向有需要的患者施用作为E-间断脒的2,3-二酰基酒石酸盐的组合物来治疗易患或患有病症和障碍的患者，例如中枢神经系统疾病。

43. 发明授权

US5731314A Pharamceutical compositions for prevention and treatment of tourette's syndrome 失效
标题翻译：用于预防和治疗粪便综合征的药物组合物
公开(公告)号：US5731314A
公开(公告)日：1998-03-24
申请号：US364978
申请日：1995-01-06
申请人： Merouane Bencherif , Patrick Michael Lippiello , William Scott Caldwell , Gary Maurice Dull
发明人： Merouane Bencherif , Patrick Michael Lippiello , William Scott Caldwell , Gary Maurice Dull
IPC分类号： A61K31/44 , A61K31/4406 , A61K31/505 , C07D213/65 , C07D239/26 , A61K31/435
CPC分类号： C07D239/26 , A61K31/44 , A61K31/4406 , A61K31/505 , C07D213/65
摘要： Patients susceptible to or suffering from Tourette's syndrome are treated by administering an effective amount of an aryl substituted aliphatic compound, an aryl substituted olefinic amine compound or an aryl substituted acetylenic compound. Exemplary compounds are (E)-4-(5-pyrimidinyl)-3-butene-1-amine, (E)-4-�3-(5-methoxypyridin)yl!-3-butene-1-amine, (E)-N-methyl-4-(5-pyrimidinyl)-3-butene-1-amine, (E)-N-methyl-4-�3-(5-methoxypyrindin)yl!-3-butene-1-amine, (Z)-metanicotine, (E)-metanicotine, N-methyl-(3-pyridinyl)-butane-1-amine, N-methyl-4-(3-pyridinyl)-3-butyne-1-amine and (E)-N-methyl-4-�3-(6-methylpyrindin)yl!-3-butene-1-amine.
摘要翻译：通过施用有效量的芳基取代的脂肪族化合物，芳基取代的烯属胺化合物或芳基取代的炔属化合物来治疗易受感染或患有Tourette综合征的患者。示例性化合物是（E）-4-（5-嘧啶基）-3-丁烯-1-胺，（E）-4- [3-（5-甲氧基吡啶）基] -3-丁烯-1-胺，（E ）-N-甲基-4-（5-嘧啶基）-3-丁烯-1-胺，（E）-N-甲基-4- [3-（5-甲氧基吡啶）基] -3-丁烯-1-胺，（Z） - 间苯胺，（E） - 间苯胺，N-甲基 - （3-吡啶基） - 丁烷-1-胺，N-甲基-4-（3-吡啶基）-3-丁炔-1-胺和（ E）-N-甲基-4- [3-（6-甲基嘧啶）基] -3-丁烯-1-胺。

44. 发明授权

US07714001B2 Arylvinylazacycloalkane compounds and methods of preparation and use thereof 有权
标题翻译：芳基乙烯基氮杂环烷烃化合物及其制备和使用方法
公开(公告)号：US07714001B2
公开(公告)日：2010-05-11
申请号：US12187584
申请日：2008-08-07
申请人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Arielle Genevois-Borella , Marc Capet , Michel Cheve
发明人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Arielle Genevois-Borella , Marc Capet , Michel Cheve
IPC分类号： C07D401/02 , A61K31/351
CPC分类号： A61K31/506 , C07D405/14
摘要： Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.
摘要翻译：公开了式（I）的新型乙烯基氮杂环烷化合物。这些化合物是各种nAChR的配体。化合物及其药学上可接受的盐可用于制备旨在预防或治疗与nAChR功能障碍相关的疾病，特别是在中枢神经系统或胃肠系统内的药物组合物和/或药物。可以治疗的疾病类型的实例包括神经变性疾病，包括中枢神经系统疾病如阿尔茨海默病，认知障碍，运动障碍如帕金森病，药物成瘾，行为障碍和胃肠系统内的炎性疾病。化合物也可用作治疗急性，慢性或复发性疼痛的镇痛药。

45. 发明授权

US06489349B1 Pharmaceutical compositions for inhibition of cytokine production and secretion 失效
标题翻译：用于抑制细胞因子产生和分泌的药物组合物
公开(公告)号：US06489349B1
公开(公告)日：2002-12-03
申请号：US09656284
申请日：2000-09-06
申请人： Merouane Bencherif , William Scott Caldwell , Gary Maurice Dull , Grayland Page Dobson
发明人： Merouane Bencherif , William Scott Caldwell , Gary Maurice Dull , Grayland Page Dobson
IPC分类号： A61K3144
CPC分类号： C07D213/38 , A61K31/4406 , Y02A50/411
摘要： Pharmaceutical compositions incorporate compounds that affect cytokine production and/or secretion. Such compounds include aryl substituted olefinic amine compounds, pyridyloxylalkylamines and phenoxyalkylamines, and aryl substituted amine compounds, such as 3-aminophenyl amine compounds. Such pharmaceutical compositions can be used for treating a wide variety of conditions, diseases and disorders, and particularly those associated with dysfunction of cytokine production and/or secretion. Of particular interest are pharmaceutical compositions useful for preventing and treating conditions, diseases and disorders associated with undesirably high levels of cytokine production and/or secretion. Such pharmaceutical compositions are useful for treating the effects of inflammatory bowel disease, inflammation, arthritis, cachexia in neoplastics diseases or associated with AIDS, and autoimmune diseases.
摘要翻译：药物组合物包含影响细胞因子产生和/或分泌的化合物。这些化合物包括芳基取代的烯属胺化合物，吡啶氧基烷基胺和苯氧基烷基胺，以及芳基取代的胺化合物，例如3-氨基苯基胺化合物。这样的药物组合物可用于治疗各种各样的病症，疾病和病症，特别是与细胞因子产生和/或分泌功能障碍相关的那些。特别感兴趣的是可用于预防和治疗与不希望的高水平的细胞因子产生和/或分泌相关的病症，疾病和病症的药物组合物。这样的药物组合物可用于治疗炎症性肠病，炎症，关节炎，恶病质在新生儿疾病中或与AIDS相关的恶病质和自身免疫疾病的作用。

46. 发明授权

US06432975B1 Pharmaceutical compositions and methods for use 有权
标题翻译：药物组合物和使用方法
公开(公告)号：US06432975B1
公开(公告)日：2002-08-13
申请号：US09210113
申请日：1998-12-11
申请人： Jeffrey Daniel Schmitt , Peter Anthony Crooks , Gary Maurice Dull
发明人： Jeffrey Daniel Schmitt , Peter Anthony Crooks , Gary Maurice Dull
IPC分类号： A61K3144
CPC分类号： C07D453/02
摘要： Pharmaceutical compositions include aryl substituted amine compounds, and in particular, carbon-linked aromatic azabicyclo compounds, and in particular, aromatic alkylene azabicyclo compounds and aromatic alkyl azabicyclo compounds.
摘要翻译：药物组合物包括芳基取代的胺化合物，特别是碳连接的芳族氮杂双环化合物，特别是芳族亚烷基氮杂双环化合物和芳族烷基氮杂双环化合物。

47. 发明授权

US6100269A Pharmaceutical compositions for prevention and treatment of central nervous system disorders 失效
标题翻译：用于预防和治疗中枢神经系统疾病的药物组合物
公开(公告)号：US6100269A
公开(公告)日：2000-08-08
申请号：US306497
申请日：1999-05-06
申请人： Merouane Bencherif , William Scott Caldwell , Gary Maurice Dull , Patrick Michael Lippiello
发明人： Merouane Bencherif , William Scott Caldwell , Gary Maurice Dull , Patrick Michael Lippiello
IPC分类号： C07D401/04 , C07D453/06 , A61K31/505 , A61K31/44
CPC分类号： C07D401/04 , C07D453/06
摘要： Patients susceptible to or suffering from central nervous system disorders (e.g., neurodegenerative diseases including presenile dementia, senile dementia of the Alzheimer's type, and Parkinsonism including Parkinson's disease, and other CNS disorders including attention deficit disorder, schizophrenia and Tourette's syndrome) are treated by administering an effective amount of 2-azabicyclo [2.2.1] heptane and 2-azabicyclo [2.2.2] octane compounds.
摘要翻译：患有中枢神经系统疾病（例如，老年性痴呆，老年痴呆症，阿尔茨海默氏型老年痴呆，帕金森综合征，包括帕金森病，其他CNS疾病，包括注意力缺陷障碍，精神分裂症和图雷特氏综合症）的易感或患中枢神经系统疾病的患者，有效量的2-氮杂双环[2.2.1]庚烷和2-氮杂双环[2.2.2]辛烷化合物。

48. 发明授权

US5885998A Methods for prevention and treatment of attention deficit disorder 失效
标题翻译：预防和治疗注意力缺陷障碍的方法
公开(公告)号：US5885998A
公开(公告)日：1999-03-23
申请号：US23040
申请日：1998-02-12
申请人： Merouane Bencherif , Patrick Michael Lippiello , William Scott Caldwell , Gary Maurice Dull
发明人： Merouane Bencherif , Patrick Michael Lippiello , William Scott Caldwell , Gary Maurice Dull
IPC分类号： A61K31/44 , A61K31/4406 , A61K31/505 , C07D213/65 , C07D239/26 , A61K31/435
CPC分类号： C07D239/26 , A61K31/44 , A61K31/4406 , A61K31/505 , C07D213/65
摘要： Patients susceptible to or suffering from attention deficit disorder are treated by administering an effective amount of an aryl subsistituted aliphatic compound, an aryl substituted olefinic amine compound or an aryl substituted acetylenic compound. Exemplary compounds are (E)-4-(5-pyrimidinyl)-3-butene-1-amine, (E)-4-�3-(5-methoxypyridin)yl!-3-butene-1-amine, (E)-N-methyl-4-(5-pyrimidinyl)-3-butene-1-amine, (E)-N-methyl-4-�3-(5-methoxypyrindin)yl!-3-butene-1-amine, (Z)-metanicotine, (E)-metanicotine, N-methyl-(3-pyridinyl)-butane-1-amine, N-methyl-4-(3-pyridinyl)-3-butyne-1-amine and (E)-N-methyl-4-�3-(6-methylpyrindin)yl!-3-butene-1-amine.
摘要翻译：通过施用有效量的芳基取代的脂族化合物，芳基取代的烯属胺化合物或芳基取代的炔属化合物来治疗患有注意力缺陷障碍或患有注意力缺陷障碍的患者。示例性化合物是（E）-4-（5-嘧啶基）-3-丁烯-1-胺，（E）-4- [3-（5-甲氧基吡啶）基] -3-丁烯-1-胺，（E ）-N-甲基-4-（5-嘧啶基）-3-丁烯-1-胺，（E）-N-甲基-4- [3-（5-甲氧基吡啶）基] -3-丁烯-1-胺，（Z） - 间苯胺，（E） - 间苯胺，N-甲基 - （3-吡啶基） - 丁烷-1-胺，N-甲基-4-（3-吡啶基）-3-丁炔-1-胺和（ E）-N-甲基-4- [3-（6-甲基嘧啶）基] -3-丁烯-1-胺。

49. 发明申请

US20100028447A1 Intranasal, Buccal, And Sublingual Administration Of Metanicotine Analogs 审中-公开
标题翻译：鼻内，颊和舌下给予异烟碱类似物
公开(公告)号：US20100028447A1
公开(公告)日：2010-02-04
申请号：US12523406
申请日：2008-01-22
申请人： Sharon Rae Letchworth , Merouane Bencherif , Gary Maurice Dull , David Moore , John W. James
发明人： Sharon Rae Letchworth , Merouane Bencherif , Gary Maurice Dull , David Moore , John W. James
IPC分类号： A61K31/4412 , A61K31/60 , A61K9/14 , A61K9/68 , A61P25/00 , A61P25/28 , A61P25/08 , A61P25/04 , A61P25/18 , A61P25/24
CPC分类号： A61K9/006 , A61K9/0056 , A61K31/44
摘要： The present invention generally relates to pharmaceutical compositions for the intranasal, buccal, or sublingual administration of metanicotine analogs.
摘要翻译：本发明一般涉及间苯二胺类似物的鼻内，口腔或舌下施用的药物组合物。

50. 发明授权

US06603011B1 3-pyridinyl compounds 失效
标题翻译： 3-吡啶基化合物
公开(公告)号：US06603011B1
公开(公告)日：2003-08-05
申请号：US09642351
申请日：2000-08-21
申请人： William Scott Caldwell , Gary Maurice Dull , Grayland Page Dobson
发明人： William Scott Caldwell , Gary Maurice Dull , Grayland Page Dobson
IPC分类号： C07D21338
CPC分类号： C07D213/38
摘要： Patients susceptible to or suffering from central nervous system disorders are treated by administering effective amounts of aryl substituted aliphatic amine compounds, aryl substituted olefinic amine compounds or aryl substituted acetylenic amine compounds. A representative compound is (E)-N-methyl-5-(3-pyridinyl)-4-penten-2-amine.
摘要翻译：通过施用有效量的芳基取代的脂族胺化合物，芳基取代的烯属胺化合物或芳基取代的炔属胺化合物来治疗易患或患有中枢神经系统疾病的患者。代表性的化合物是（E）-N-甲基-5-（3-吡啶基）-4-戊烯-2-胺。

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