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公开(公告)号：US5962419A
公开(公告)日：1999-10-05
申请号：US442514
申请日：1995-05-17
申请人： Ian Alexander McDonald , Elisabeth Albrecht , Benito Munoz , Blake Alan Rowe , Robert Steven Siegel , Steven Lee Wagner
发明人： Ian Alexander McDonald , Elisabeth Albrecht , Benito Munoz , Blake Alan Rowe , Robert Steven Siegel , Steven Lee Wagner
IPC分类号： A61K38/00 , A61K31/00 , A61P25/00 , A61P25/16 , A61P25/28 , C07C237/22 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/078 , C07K5/08 , C07K5/083 , A61K38/05
CPC分类号： C07K5/0808 , C07C237/22 , C07K5/0202 , C07K5/0205 , C07K5/06043 , C07K5/06078 , C07K5/06139 , C07K5/06165 , C07K5/06191 , A61K38/00
摘要： Methods of use of compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds provided for use in the methods are those of the formula: ##STR1## in which R.sub.1 is preferably 2-methylpropenyl, 2-butenyl, cyclohexyl or cyclohexylmethyl; R.sub.2, R.sub.4, and R.sub.8 are each preferably independently methyl or ethyl; R.sub.3 is preferably iso-butyl or phenyl; Q is preferably --C(O)--; R.sub.B is preferably iso-butyl; R.sub.A is --(T).sub.m --(D).sub.m --R.sub.1, in which T is preferably oxygen or NH, m is 0 or 1, and D is preferably C.sub.1-4 alkyl or C.sub.2-4 alkenyl; and X is preferably an aldehyde, .alpha.-ketoester or .alpha.-ketoamide.
摘要翻译： 提供了化合物用于治疗以沉淀淀粉样蛋白为特征的疾病的方法。 在该方法中提供的化合物中的那些是下式的化合物：其中R 1优选为2-甲基丙烯基，2-丁烯基，环己基或环己基甲基; R2，R4和R8各自优选独立地为甲基或乙基; R3优选为异丁基或苯基; Q优选为-C（O） - ; RB优选为异丁基; RA是 - （T）m-（D）m -R1，其中T优选为氧或NH，m为0或1，D优选为C 1-4烷基或C 2-4烯基; X优选为醛，α-酮酯或α-酮酰胺。
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2.发明授权
公开(公告)号：US6153171A
公开(公告)日：2000-11-28
申请号：US443048
申请日：1995-05-17
IPC分类号： A61K38/00 , A61K31/00 , A61P25/00 , A61P25/16 , A61P25/28 , C07C237/22 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/078 , C07K5/08 , C07K5/083 , G01N33/53
CPC分类号： C07K5/0808 , C07C237/22 , C07K5/0202 , C07K5/0205 , C07K5/06043 , C07K5/06078 , C07K5/06139 , C07K5/06165 , C07K5/06191 , A61K38/00
摘要： Methods for identifying compounds that can be used for treatment of neurodegenerative diseases, for monitoring the progression of these diseases, and for monitoring therapeutic intervention of these diseases are provided. These methods are effected by determining the relative amount of .alpha.-sAPP and the ratio of .alpha.-sAPP to total sAPP in body fluids, tissues or in cell culture.
摘要翻译： 提供了用于鉴定可用于治疗神经变性疾病的化合物，用于监测这些疾病的进展以及用于监测这些疾病的治疗性干预的方法。 这些方法通过测定体液，组织或细胞培养物中α-APP的相对量和α-APP与总sAPP的比例来实现。
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公开(公告)号：US5714471A
公开(公告)日：1998-02-03
申请号：US443901
申请日：1995-05-17
IPC分类号： A61K38/00 , A61K31/00 , A61P25/00 , A61P25/16 , A61P25/28 , C07C237/22 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/078 , C07K5/08 , C07K5/083 , G01N33/53 , G01N33/543 , G01N33/561 , C07K13/00
CPC分类号： C07K5/0808 , C07C237/22 , C07K5/0202 , C07K5/0205 , C07K5/06043 , C07K5/06078 , C07K5/06139 , C07K5/06165 , C07K5/06191 , A61K38/00
摘要： Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds are those of formulae I and II: ##STR1## in which R.sub.1 is preferably 2-methyl propene, 2-butene, cyclohexyl or cyclohexylmethyl; R.sub.2, R.sub.4, and R.sub.8 are each independently methyl or ethyl; R.sub.3 is preferably iso-butyl or phenyl; R.sub.5 is preferably iso-butyl; R.sub.6 is H or methyl; R.sub.7 --(Q).sub.n is preferably benzyloxycarbonyl or acetyl; Q is preferably --C(O)--; R.sub.8 is preferbly iso-butyl; R.sub.A =--(T).sub.m --(D).sub.m --R.sub.1, is which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C.sub.3-4 alkenyl being more preferred; and X is preferably an .alpha.-ketoester or .alpha.-ketoamide.
摘要翻译： 提供了化合物和化合物用于治疗以沉淀淀粉样蛋白为特征的疾病的方法。 其中R 1优选为2-甲基丙烯，2-丁烯，环己基或环己基甲基;其中R 1优选为2-甲基丙烯，2-丁烯，环己基或环己基甲基; R2，R4和R8各自独立地是甲基或乙基; R3优选为异丁基或苯基; R5优选为异丁基; R6是H或甲基; R7-（Q）n优选为苄氧羰基或乙酰基; Q优选为-C（O） - ; R8优选为异丁基; RA = - （T）m-（D）m -R 1，其中T优选为氧或碳，D优选为单不饱和C 3-4烯基; X优选为α-酮酯或α-酮酰胺。
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