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公开(公告)号：US5612311A
公开(公告)日：1997-03-18
申请号：US363963
申请日：1994-12-22
IPC分类号： A61K38/00 , C07K7/54 , C07K7/64 , C07K14/705 , C07K14/745 , C07K14/75 , C07K14/78 , A61K38/12
CPC分类号： C07K7/64 , C07K14/70557 , C07K14/745 , C07K14/75 , C07K14/78 , C07K7/54 , A61K38/00
摘要： The invention provides cyclic peptides which inhibit platelet aggregation without causing prolonged bleeding time. The invention provides RGD or KGD containing peptides which are cyclized and contain hydrophobic moieties adjacent to the carboxy terminus of the RGD sequence. Peptides of this nature are also provided which contain in addition to the hydrophobic moiety an adjacent positively charged moiety. Such peptides have a high affinity for the receptor IIb/IIIa and a low affinity for the fibronectin and vitronectin receptors. Such peptides can be administered in a suitable physiologically acceptable carrier to therapeutically treat thrombosis.
摘要翻译： 本发明提供抑制血小板聚集而不引起延长出血时间的环肽。 本发明提供含RGD或KGD的肽，其环化并含有与RGD序列的羧基末端相邻的疏水部分。 还提供了这种性质的肽，除了疏水部分外还含有相邻带正电的部分。 这样的肽对受体IIb / IIIa具有高亲和力，对纤连蛋白和玻连蛋白受体的亲和力低。 这样的肽可以在合适的生理学上可接受的载体中施用以治疗性治疗血栓形成。
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公开(公告)号：US6017877A
公开(公告)日：2000-01-25
申请号：US246852
申请日：1994-05-19
IPC分类号： A61K38/00 , C07K7/54 , C07K7/64 , C07K14/705 , C07K14/745 , C07K14/75 , C07K14/78
CPC分类号： C07K7/54 , C07K14/70557 , C07K14/745 , C07K14/75 , C07K14/78 , C07K7/64 , A61K38/00
摘要： The invention provides cyclic peptides which inhibit platelet aggregation without causing prolonged bleeding time. The invention provides RGD or KGD containing peptides which are cyclized and contain hydrophobic amino acids adjacent to the carboxy terminus of the RGD sequence. Peptides of this nature are also provided which contain in addition to the hydrophobic amino acid an adjacent positively charged amino acid. Such peptides have a high affinity for the receptor IIb/IIIa and a low affinity for the fibronectin and vitronectin receptors. Such peptides can be administered in a suitable physiologically acceptable carrier to therapeutically treat thrombosis.
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公开(公告)号：US5672585A
公开(公告)日：1997-09-30
申请号：US445745
申请日：1995-05-22
IPC分类号： A61K38/00 , C07K7/54 , C07K7/64 , C07K14/705 , C07K14/745 , C07K14/75 , C07K14/78 , A61K38/02 , C07K5/00 , C07K7/00
CPC分类号： C07K7/54 , C07K14/70557 , C07K14/745 , C07K14/75 , C07K14/78 , C07K7/64 , A61K38/00
摘要： The invention provides cyclic peptides which inhibit platelet aggregation without causing prolonged bleeding time. The invention provides RGD or KGD containing peptides which are cyclized and contain hydrophobic amino acids adjacent to the carboxy terminus of the RGD sequence. Peptides of this nature are also provided which contain in addition to the hydrophobic amino acid an adjacent positively charged amino acid. Such peptides have a high affinity for the receptor IIb/IIIa and a low affinity for the fibronectin and vitronectin receptors. Such peptides can be administered in a suitable physiologically acceptable carrier to therapeutically treat thrombosis.
摘要翻译： 本发明提供抑制血小板聚集而不引起延长出血时间的环肽。 本发明提供含RGD或KGD的肽，其环化并含有与RGD序列的羧基末端相邻的疏水性氨基酸。 还提供了这种性质的肽，除了疏水性氨基酸之外还含有相邻的带正电荷的氨基酸。 这样的肽对受体IIb / IIIa具有高亲和力，对纤连蛋白和玻连蛋白受体的亲和力低。 这样的肽可以在合适的生理学上可接受的载体中施用以治疗性治疗血栓形成。
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公开(公告)号：US06521594B1
公开(公告)日：2003-02-18
申请号：US08445638
申请日：1995-05-22
IPC分类号： A61K3812
CPC分类号： C07K14/70557 , A61K38/00 , C07K7/54 , C07K7/64 , C07K14/745 , C07K14/75 , C07K14/78
摘要： The invention provides cyclic peptides which inhibit platelet aggregation without causing prolonged bleeding time. The invention provides RGD or KGD containing peptides which are cyclized and contain hydrophobic amino acids adjacent to the carboxy terminus of the RGD sequence. Peptides of this nature are also provided which contain in addition to the hydrophobic amino acid an adjacent positively charged amino acid. Such peptides have a high affinity for the receptor IIb/IIIa and a low affinity for the fibronectin and vitronectin receptors. Such peptides can be administered in a suitable physiologically acceptable carrier to therapeutically treat thrombosis.
摘要翻译： 本发明提供抑制血小板聚集而不引起延长出血时间的环肽。 本发明提供含RGD或KGD的肽，其环化并含有与RGD序列的羧基末端相邻的疏水性氨基酸。 还提供了这种性质的肽，除了疏水性氨基酸之外还含有相邻的带正电荷的氨基酸。 这样的肽对受体IIb / IIIa具有高亲和力，对纤连蛋白和玻连蛋白受体的亲和力低。 这样的肽可以在合适的生理学上可接受的载体中施用以治疗性治疗血栓形成。
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公开(公告)号：US06395873B1
公开(公告)日：2002-05-28
申请号：US08456466
申请日：1995-06-01
IPC分类号： A61K3812
CPC分类号： C07K7/64 , A61K38/00 , C07K7/54 , C07K14/70557 , C07K14/745 , C07K14/75 , C07K14/78
摘要： The invention provides cyclic peptides which inhibit platelet aggregation without causing prolonged bleeding time. The invention provides RGD or KGD containing peptides which are cyclized and contain hydrophobic moieties adjacent to the carboxy terminus of the RGD sequence. Peptides of this nature are also provided which contain in addition to the hydrophobic. moiety an adjacent positively charged moiety. Such peptides have a high affinity for the receptor IIb/IIIa and a low affinity for the fibronectin and vitronectin receptors. Such peptides can be administered in a suitable physiologically acceptable carrier to therapeutically treat thrombosis.
摘要翻译： 本发明提供抑制血小板聚集而不引起延长出血时间的环肽。 本发明提供含RGD或KGD的肽，其环化并含有与RGD序列的羧基末端相邻的疏水部分。 还提供了除了疏水性之外还含有这种性质的肽。 部分是相邻带正电的部分。 这样的肽对受体IIb / IIIa具有高亲和力，对纤连蛋白和玻连蛋白受体的亲和力低。 这样的肽可以在合适的生理学上可接受的载体中施用以治疗性治疗血栓形成。
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公开(公告)号：US5780303A
公开(公告)日：1998-07-14
申请号：US459566
申请日：1995-06-02
IPC分类号： A61K38/00 , C07K7/54 , C07K7/64 , C07K14/705 , C07K14/745 , C07K14/75 , C07K14/78
CPC分类号： C07K14/78 , C07K14/70557 , C07K14/745 , C07K14/75 , C07K7/54 , C07K7/64 , A61K38/00 , Y10T436/101666
摘要： A method for identifying a peptide useful for inhibiting platelet aggregation activity without substantially prolonging bleeding time comprising determining the IC.sub.50 value of the peptide in both a heparin assay and a citrate assay and then comparing the value of the IC.sub.50 from each assay.
摘要翻译： 用于鉴定用于抑制血小板聚集活性而不显着延长出血时间的肽的方法，包括在肝素测定和柠檬酸盐测定中测定肽的IC 50值，然后比较来自每个测定的IC 50值。
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公开(公告)号：US6013625A
公开(公告)日：2000-01-11
申请号：US322409
申请日：1994-10-12
IPC分类号： A61K38/00 , A61P7/02 , C07K7/00 , C07K7/06 , C07K7/54 , C07K7/64 , C07K14/00 , C07K14/705 , C07K14/745 , C07K14/75 , C07K14/78
CPC分类号： C07K7/06 , C07K14/70557 , C07K14/745 , C07K14/75 , C07K14/78 , C07K7/54 , C07K7/64 , A61K38/00
摘要： The invention provides RGD containing peptides which are cyclized and contain hydrophobic moieties adjacent the carboxy terminus of the RGD sequence. Such peptides have an high affinity for the receptor IIb/IIIa and low affinity for the fibronectin and vitronectin receptors. Such peptides can be administered in a suitable physiologically acceptable carrier to therapeutically treat thrombosis.
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公开(公告)号：US5648330A
公开(公告)日：1997-07-15
申请号：US459565
申请日：1995-06-02
IPC分类号： A61K38/00 , C07K7/06 , C07K7/54 , C07K7/64 , C07K14/705 , C07K14/745 , C07K14/75 , C07K14/78 , A61K38/02 , C07K5/00 , C07K7/00
CPC分类号： C07K7/06 , C07K14/70557 , C07K14/745 , C07K14/75 , C07K14/78 , C07K7/54 , C07K7/64 , A61K38/00
摘要： The invention provides RGD containing peptides which are cyclized and contain hydrophobic moieties adjacent the carboxy terminus of the RGD sequence. Such peptides have an high affinity for the receptor IIb/IIIa and low affinity for the fibronectin and vitronectin receptors. Such peptides can be administered in a suitable physiologically acceptable carrier to therapeutically treat thrombosis.
摘要翻译： 本发明提供含RGD的肽，其环化并且在RGD序列的羧基末端附近含有疏水部分。 这些肽对受体IIb / IIIa具有高亲和力，对纤连蛋白和玻连蛋白受体的亲和力低。 这样的肽可以在合适的生理学上可接受的载体中施用以治疗性治疗血栓形成。
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公开(公告)号：US6100236A
公开(公告)日：2000-08-08
申请号：US465498
申请日：1995-06-05
IPC分类号： A61K38/00 , A61P7/02 , C07K7/00 , C07K7/06 , C07K7/54 , C07K7/64 , C07K14/00 , C07K14/705 , C07K14/745 , C07K14/75 , C07K14/78 , A61K38/08 , A61K38/12
CPC分类号： C07K7/06 , C07K14/70557 , C07K14/745 , C07K14/75 , C07K14/78 , C07K7/54 , C07K7/64 , A61K38/00
摘要： The invention provides RGD containing peptides which are cyclized and contain hydrophobic moieties adjacent the carboxy terminus of the RGD sequence. Such peptides have an high affinity for the receptor IIb/IIIa and low affinity for the fibronectin and vitronectin receptors. Such peptides can be administered in a suitable physiologically acceptable carrier to therapeutically treat thrombosis.
摘要翻译： 本发明提供含RGD的肽，其环化并且在RGD序列的羧基末端附近含有疏水部分。 这些肽对受体IIb / IIIa具有高亲和力，对纤连蛋白和玻连蛋白受体的亲和力低。 这样的肽可以在合适的生理学上可接受的载体中施用以治疗性治疗血栓形成。
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公开(公告)号：US5985827A
公开(公告)日：1999-11-16
申请号：US458638
申请日：1995-06-02
摘要： Novel synthetic Arg-Gly-Asp containing peptides which have high affinity and specificity for their receptors by virtue of restrictions on their stereochemical conformation. Such restrictions can be provided by cyclization, by inclusion into a constraining conformational structure such as a helix, by providing an additional chemical structure such as an amide or an enantiomer of a naturally occurring amino acid, or by other methods. In particular, there are provided cyclic peptides having increased affinity and selectivity for the certain receptors over that of linear, Arg-Gly-Asp-containing synthetic peptides.
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