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公开(公告)号：US5580953A
公开(公告)日：1996-12-03
申请号：US794288
申请日：1991-11-19
IPC分类号： A61K38/00 , A61P3/08 , A61P3/10 , C07K14/575 , A61K38/22
CPC分类号： C07K14/575 , A61K38/00
摘要： Compounds which inhibit amylin activity are provided. These compounds may be used in the treatment of conditions where it is of benefit to reduce amylin activity, including the treatment of Type 2 diabetes mellitus, impaired glucose tolerance, obesity and insulin resistance.
摘要翻译： 提供抑制胰淀素活性的化合物。 这些化合物可用于治疗有利于减少胰岛淀粉样多肽活性的病症，包括治疗2型糖尿病，葡萄糖耐量降低，肥胖和胰岛素抵抗。
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公开(公告)号：US5686411A
公开(公告)日：1997-11-11
申请号：US447849
申请日：1995-05-23
CPC分类号： C07K14/575 , A61K38/00 , Y10S514/866
摘要： Agonist analogues of amylin and related pharmaceutical compositions, and methods of treatment of diabetes and other insulin-requiring states, as well as methods of treatment of hypoglycemia, are provided.
摘要翻译： 提供胰岛淀粉样多肽和相关药物组合物的激动剂类似物，以及治疗糖尿病和其它胰岛素需要状态的方法以及治疗低血糖症的方法。
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公开(公告)号：US06610824B2
公开(公告)日：2003-08-26
申请号：US09454533
申请日：1999-12-06
IPC分类号： A61K3816
CPC分类号： C07K14/575 , A61K38/00 , Y10S514/866
摘要： Agonist analogs of amylin and related pharmaceutical compositions, and methods of treatment of diabetes and other insulin-requiring states, as well as methods of treatment of hypoglycemia, are provided.
摘要翻译： 提供胰岛淀粉样多肽和相关药物组合物的激动剂类似物，以及治疗糖尿病和其它胰岛素需要状态的方法以及治疗低血糖症的方法。
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公开(公告)号：US5998367A
公开(公告)日：1999-12-07
申请号：US892549
申请日：1997-07-14
CPC分类号： C07K14/575 , A61K38/00 , Y10S514/866
摘要： Agonist analogues of amylin and related pharmaceutical compositions, and methods of treatment of diabetes and other insulin-requiring states, as well as methods of treatment of hypoglycemia, are provided.
摘要翻译： 提供胰岛淀粉样多肽和相关药物组合物的激动剂类似物，以及治疗糖尿病和其它胰岛素需要状态的方法以及治疗低血糖症的方法。
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公开(公告)号：US07271238B2
公开(公告)日：2007-09-18
申请号：US10649138
申请日：2003-08-26
IPC分类号： A61K38/16
CPC分类号： C07K14/575 , A61K38/00 , Y10S514/866
摘要： Agonist analogues of amylin and related pharmaceutical compositions, and methods of treatment of diabetes and other insulin-requiring states, as well as methods of treatment of hypoglycemia, are provided.
摘要翻译： 提供胰岛淀粉样多肽和相关药物组合物的激动剂类似物，以及治疗糖尿病和其它胰岛素需要状态的方法以及治疗低血糖症的方法。
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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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7.发明授权
公开(公告)号：US5872101A
公开(公告)日：1999-02-16
申请号：US444361
申请日：1995-05-18
IPC分类号： A61K38/00 , C07C237/22 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/078 , C07K5/083 , A61K38/05
CPC分类号： C07K5/0808 , C07C237/22 , C07K5/0202 , C07K5/0205 , C07K5/06043 , C07K5/06078 , 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), (II) and (III): ##STR1## in which R.sub.1 is preferably 2-methyl propene, 2-butene, norleucine; 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 an alcohol, particularly a secondary alcohol.
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，正亮氨酸;式（I），（II）和（III）的化合物为： 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是醇，特别是仲醇。
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公开(公告)号：US6017887A
公开(公告)日：2000-01-25
申请号：US443931
申请日：1995-05-18
IPC分类号： A61K38/00 , C07C237/22 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/078 , C07K5/083 , A61K38/05
CPC分类号： C07K5/0808 , C07C237/22 , C07K5/0202 , C07K5/0205 , C07K5/06043 , C07K5/06078 , 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), (II) and (III): ##STR1## in which R.sub.1 is preferably 2-methyl propene, 2-butene, norleucine; 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.B 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 an alcohol, particularly a secondary alcohol.
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，正亮氨酸等;式（I），（II）和（III） 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） - ; RB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是醇，特别是仲醇。
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公开(公告)号：US5424394A
公开(公告)日：1995-06-13
申请号：US90361
申请日：1993-07-08
IPC分类号： A61K38/00 , C07K14/575 , A61K38/23 , C07K14/00
CPC分类号： C07K14/575 , A61K38/00
摘要： Synthetic amylin and amylin analogs which have high biological activity and which are substantially free from deletion peptides and other contaminating peptides are provided. Also provided are methods for the solid phase peptide synthesis of amylin and amylin analogs.
摘要翻译： 提供了具有高生物活性且基本上不含缺失肽和其它污染肽的合成胰淀素和胰岛淀粉样多肽类似物。 还提供了固相肽合成胰岛淀粉样多肽和胰岛淀粉样多肽类似物的方法。
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10.发明授权
公开(公告)号：US6051684A
公开(公告)日：2000-04-18
申请号：US442786
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
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; R.sub.5 is preferably iso-butyl; R.sub.6 is preferably H or methyl; R.sub.7 --(Q).sub.n is preferably benzyloxycarbonyl or acetyl; Q is preferably --C(O)--; 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; R5优选为异丁基; R6优选为H或甲基; R7-（Q）n优选为苄氧羰基或乙酰基; Q优选为-C（O） - ; X优选为醛，α-酮酯或α-酮酰胺。
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