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1.发明授权S-heteroatom containing alkyl substituted-3-oxo-pyrido�1,2-A!benzimidozole-4-carboxamide derivatives useful in treating central nervous system disorders 失效含有可用于治疗中枢神经系统疾病的烷基取代-3-氧代 - 吡啶并[1,2-A]苯甲亚氨基-4-甲酰胺衍生物的S-杂原子
公开(公告)号：US5817668A
公开(公告)日：1998-10-06
申请号：US943578
申请日：1997-10-03
申请人： Allen B. Reitz , Alfonzo D. Jordan , Pauline J. Sanfilippo , Malcolm K. Scott , Anna Vavouyios-Smith
发明人： Allen B. Reitz , Alfonzo D. Jordan , Pauline J. Sanfilippo , Malcolm K. Scott , Anna Vavouyios-Smith
IPC分类号： A61K31/437 , A61K31/496 , A61K31/5377 , A61P25/00 , A61P25/02 , A61P25/22 , A61P25/30 , C07D471/04 , A61K31/435 , A61K31/535
CPC分类号： C07D471/04 , A61K31/437
摘要： A compound of the general formula 1; ##STR1## is disclosed as useful in treating disorders of the central nervous system. Pharmaceutical compositions and methods of treatment are also disclosed.
摘要翻译： 通式1的化合物; 公开了一种治疗中枢神经系统疾病的方法。 还公开了药物组合物和治疗方法。
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2.发明授权5-�(heteroaryl)alkyl!-3-oxo-pyrido�1,2-a!benzimidazole-4-carboxamide derivatives useful in treating central nervous system disorders 失效5 - [（杂芳基）烷基] -3-氧代 - 吡啶并[1,2-a]苯并咪唑-4-甲酰胺衍生物，用于治疗中枢神经系统疾病
公开(公告)号：US5922731A
公开(公告)日：1999-07-13
申请号：US884804
申请日：1997-06-30
IPC分类号： A61K31/435 , A61P25/00 , C07D471/04 , A61K31/44 , C07D471/00 , C07D498/00 , C07D513/00
CPC分类号： C07D471/04
摘要： A compound of the general formula 1; ##STR1## is disclosed as useful in treating disorders of the central nervous system. Pharmaceutical compositions and methods of treatment are also disclosed.
摘要翻译： 通式1的化合物; 被公开用于治疗中枢神经系统疾病。 还公开了药物组合物和治疗方法。
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3.发明授权2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) 有权可用作β-分泌酶抑制剂的2-氨基 - 喹唑啉衍生物（BACE）公开(公告)号：US08383637B2
公开(公告)日：2013-02-26
申请号：US11197669
申请日：2005-08-04
申请人： Ellen Baxter , Francois Paul Bischoff , Robert E. Boyd , Mirielle Braeken , Steve Coats , Yifang Huang , Alfonzo D. Jordan , Chi Luo , Marc Hubert Mercken , Serge Maria Aloysius Pieters , Allen B. Reitz , Charles H. Reynolds , Tina Morgan Ross , Brett A. Tounge , Mark J. Schulz , Hans Louis Jos De Winter
发明人： Ellen Baxter , Francois Paul Bischoff , Robert E. Boyd , Mirielle Braeken , Steve Coats , Yifang Huang , Alfonzo D. Jordan , Chi Luo , Marc Hubert Mercken , Serge Maria Aloysius Pieters , Allen B. Reitz , Charles H. Reynolds , Tina Morgan Ross , Brett A. Tounge , Mark J. Schulz , Hans Louis Jos De Winter
IPC分类号： A61K31/517 , C07D239/88 , C07D239/94 , C07D401/06 , A61K31/535 , C07D265/30
CPC分类号： C07D413/06 , C07D239/84 , C07D401/06 , C07D403/06 , C07D403/12 , C07D405/06
摘要： The present invention is directed to novel 2-amino-3,4-dihydro-quinazoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of β-secretase, also known as β-site cleaving enzyme and BACE.
摘要翻译： 本发明涉及新的2-氨基-3,4-二氢 - 喹唑啉衍生物，含有它们的药物组合物及其在治疗阿尔茨海默病（AD）和相关病症中的用途。 本发明的化合物是分泌酶的抑制剂，也称为“切割酶”和BACE。
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4.发明授权Neurotrophic pyrrolidines and piperidines, and related compositions and methods 有权神经营养吡咯烷和哌啶，以及相关组合物和方法公开(公告)号：US06809107B1
公开(公告)日：2004-10-26
申请号：US09593852
申请日：2000-06-14
IPC分类号： A61K3147
CPC分类号： C07D413/14 , C07D413/04 , C07D417/14
摘要： This invention provides compounds having the following general structures: This invention also provides pharmaceutical compositions comprising same and methods of using these compositions to treat and prevent disorders characterized by neuronal damage.
摘要翻译： 本发明提供具有以下一般结构的化合物：本发明还提供包含其的药物组合物和使用这些组合物治疗和预防以神经元损伤为特征的疾病的方法。
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公开(公告)号：US08426429B2
公开(公告)日：2013-04-23
申请号：US11197608
申请日：2005-08-04
申请人： Ellen Baxter , Robert Boyd , Steven J. Coats , Alfonzo D. Jordan , Allen B. Reitz , Charles H. Reynolds , Mark Schulz , Malcolm Scott
发明人： Ellen Baxter , Robert Boyd , Steven J. Coats , Alfonzo D. Jordan , Allen B. Reitz , Charles H. Reynolds , Mark Schulz , Malcolm Scott
IPC分类号： A61K31/517 , C07D239/88 , C07D239/94 , C07D401/06 , A61K31/535 , C07D265/30
CPC分类号： C07D215/227 , C07D401/06 , C07D403/06 , C07D403/12 , C07D405/06 , C07D413/06
摘要： The present invention is directed to novel 2-amino-3,4-dihydro-quinazoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of β-secretase, also known as β-site cleaving enzyme and BACE.
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![C-6 ring-substituted pyrido[1,2-a]benzimidazole derivatives useful in treating central nervous system disorders](/abs-image/US/2002/03/19/US06358946B1/abs.jpg.150x150.jpg)
6.发明授权C-6 ring-substituted pyrido[1,2-a]benzimidazole derivatives useful in treating central nervous system disorders 有权可用于治疗中枢神经系统疾病的C-6环取代的吡啶并[1,2-a]苯并咪唑衍生物公开(公告)号：US06358946B1
公开(公告)日：2002-03-19
申请号：US09619804
申请日：2000-07-20
IPC分类号： C07D47104
CPC分类号： C07D471/04
摘要： A C-6 ring-substituted pyrido[1,2-a]benzimidazole derivative of the formula: methods of preparation and pharmaceutical compositions containing a substituted pyrido[1,2-a]benzimidzole derivative as the active ingredient are disclosed. The substituted pyrido[1,2-a]benzimidazole derivatives are useful in the treatment of central nervous system disorders.
摘要翻译： 公开了下式的C-6环取代的吡啶并[1,2-a]苯并咪唑衍生物：制备方法和含有取代的吡啶并[1,2-a]苯并咪唑衍生物作为活性成分的药物组合物。 取代的吡啶并[1,2-a]苯并咪唑衍生物可用于治疗中枢神经系统疾病。
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7.发明授权
公开(公告)号：US5314885A
公开(公告)日：1994-05-24
申请号：US943846
申请日：1992-09-11
IPC分类号： C07D295/08 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/4035 , A61K31/445 , A61K31/451 , A61K31/495 , A61P25/18 , A61P25/22 , C07D207/40 , C07D207/408 , C07D209/48 , C07D211/40 , C07D211/76 , C07D211/88 , C07D221/20 , C07D295/096 , C07D401/06
CPC分类号： C07D207/40 , C07D209/48 , C07D211/76 , C07D211/88 , C07D221/20 , C07D295/096
摘要： Compounds of the general formula I ##STR1## are disclosed as novel antipsychotic agents. Pharmaceutical compositions and methods of treating convulsions employing such compounds of formula I are also disclosed.
摘要翻译： 通式I的化合物作为新型抗精神病药被公开。 还公开了使用式I化合物治疗惊厥的药物组合物和方法。
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8.发明授权
公开(公告)号：US5449677A
公开(公告)日：1995-09-12
申请号：US120015
申请日：1993-09-10
IPC分类号： C07D295/08 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/4035 , A61K31/445 , A61K31/451 , A61K31/495 , A61P25/18 , A61P25/22 , C07D207/40 , C07D207/408 , C07D209/48 , C07D211/40 , C07D211/76 , C07D211/88 , C07D221/20 , C07D295/096 , C07D211/08 , C07D403/00
CPC分类号： C07D207/40 , C07D209/48 , C07D211/76 , C07D211/88 , C07D221/20 , C07D295/096
摘要： Compounds of the general formula I ##STR1## are disclosed as novel antipsychotic agents. Pharmaceutical compositions and methods of treating convulsions employing such compounds of formula I are also disclosed.
摘要翻译： 通式I的化合物作为新型抗精神病药被公开。 还公开了使用式I化合物治疗惊厥的药物组合物和方法。
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9.发明授权Method of treating neurodegenerative disorders via inhibition of amyloid beta peptide binding 有权通过抑制淀粉样蛋白β肽结合治疗神经变性疾病的方法公开(公告)号：US06441049B2
公开(公告)日：2002-08-27
申请号：US09320885
申请日：1999-05-27
申请人： Allen B. Reitz , David A. Demeter , Daniel H. S. Lee , Hoau-Yan Wang , Robert H. Chen , Tina Morgan Ross , Malcolm K. Scott , Carlos R. Plata-Salaman
发明人： Allen B. Reitz , David A. Demeter , Daniel H. S. Lee , Hoau-Yan Wang , Robert H. Chen , Tina Morgan Ross , Malcolm K. Scott , Carlos R. Plata-Salaman
IPC分类号： A61K31135
CPC分类号： C07D295/096 , A61K31/00 , A61K31/135 , A61K31/5375 , C07C215/64 , C07C217/74 , C07C229/14 , C07C323/25 , C07C2602/10 , C07D295/088 , C07D333/20 , C07F9/3282
摘要： The invention is directed to a method of treating a neurodegenerative disorder in a subject in need thereof which comprises administering to the subject an amount of a compound effective to inhibit the interaction of amyloid-beta with alpha-7 nicotinic acetylcholine receptors.
摘要翻译： 本发明涉及一种在有需要的受试者中治疗神经变性疾病的方法，该方法包括向受试者施用一定量的有效抑制淀粉样蛋白-β与α-7烟碱乙酰胆碱受体相互作用的化合物。
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10.发明授权1,4-dithiin and 1,4-dithiepin-1,1,4,4, tetroxide derivatives useful as antagonists of the human galanin receptor 有权可用作人甘丙肽受体拮抗剂的1,4-二硫辛酸和1,4-二硫辛啶-1,1,4,4四氧化物衍生物公开(公告)号：US06407136B1
公开(公告)日：2002-06-18
申请号：US09563147
申请日：2000-05-02
IPC分类号： A61K31385
CPC分类号： C07D409/04 , C07D339/00 , C07D339/08
摘要： The invention is directed to 1,4-dithiin- and 1,4-dithiepin-1,1,4,4-tetroxide derivatives useful as galanin receptor antagonists for treating disorders of the central nervous system. Pharmaceutical compositions comprising the compounds of the present invention and methods of treating conditions such as an eating disorder, obesity, bulimia nervosa, anorexia nervosa, binge eating, diabetes, dyslipidemia, hypertension, memory loss, sleep disturbances, pain, depression, anxiety, Alzheimer's disease, senile dementia, cerebral hemorrhage, or diarrhea are also described.
摘要翻译： 本发明涉及用作治疗中枢神经系统疾病的甘丙肽受体拮抗剂的1,4-二硫辛酸和1,4-二硫辛啶-1,1,4,4-四氧化物衍生物。 包含本发明化合物的药物组合物和治疗诸如进食障碍，肥胖症，神经性贪食症，神经性厌食症，暴饮暴食症，糖尿病，血脂异常，高血压，记忆丧失，睡眠障碍，疼痛，抑郁，焦虑，阿尔茨海默病 还描述了疾病，老年性痴呆，脑出血或腹泻。
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