公开(公告)号：US6132697A

公开(公告)日：2000-10-17

申请号：US870042

申请日：1997-06-05

申请人： Ananthachari Srinivasan ,  Larry P. Feigen ,  Daniel Lee Flynn ,  Jeffery Alan Zablocki ,  Philip Needleman ,  Michelle A. Schmidt

发明人： Ananthachari Srinivasan ,  Larry P. Feigen ,  Daniel Lee Flynn ,  Jeffery Alan Zablocki ,  Philip Needleman ,  Michelle A. Schmidt

IPC分类号： A61K38/00 ,  A61K51/00 ,  A61K51/08 ,  C07K5/072 ,  C07F5/00

CPC分类号： C07K5/06113 ,  A61K51/088 ,  A61K2121/00 ,  A61K2123/00

摘要： A radiopharmaceutical capable of localizing at a site of thrombus containing activated platelets within a mammalian body is provided wherein the radiopharmaceutical comprises a linear peptidomimetic containing ligand capable of specifically binding to the GPIIb/IIIa integrin receptor of platelets in the thrombus and a radionuclide covalently bound to the peptidomimetic containing ligand. The ligand compositions of the invention are provided complexed with a selected metal radionuclide to form a diagnostic or therapeutic radiopharmaceutical to image a site of thrombus or provide radiotherapy to the site of thrombus, respectively. Methods of imaging a site of thrombus in a mammalian body by administering a diagnostically effective amount of the radiopharmaceutical composition of this invention complexed with a selected diagnostic metal radionuclide and methods of providing therapy to a site of thrombus in a mammalian body by administering a therapeutically effective amount of the radiopharmaceutical composition of this invention complexed with a selected therapeutic metal radionuclide are also provided as well as kits for preparing such radiopharmaceutical compositions.

摘要翻译： 提供了能够在哺乳动物体内含有活化血小板的血栓位点定位的放射性药物，其中放射性药物包含能够特异性结合血栓中血小板的GPIIb / IIIa整联蛋白受体的线性拟肽含量配体和共价结合的放射性核素 含有拟肽的配体。 提供本发明的配体组合物与所选择的金属放射性核素复合以形成诊断或治疗性放射性药物，以分别对血栓位点成像或向血栓部位提供放射治疗。 通过施用诊断上有效量的本发明的放射性药物组合物与选定的诊断性金属放射性核素复合而在哺乳动物体内成像血栓位点的方法和通过施用治疗有效的方法向哺乳动物体内的血栓位点提供治疗 还提供了与选定的治疗性金属放射性核素复合的本发明的放射性药物组合物的量以及用于制备这种放射性药物组合物的试剂盒。

公开(公告)号：US4857508A

公开(公告)日：1989-08-15

申请号：US128379

申请日：1987-12-03

申请人： Steven P. Adams ,  Larry P. Feigen ,  Masateru Miyano

发明人： Steven P. Adams ,  Larry P. Feigen ,  Masateru Miyano

IPC分类号： A61K38/00 ,  A61P7/02 ,  C07K5/06 ,  C07K5/08 ,  C07K5/083 ,  C07K5/09 ,  C07K5/10

CPC分类号： C07K5/1019 ,  C07K5/0806 ,  C07K5/0817 ,  A61K38/00

摘要： Novel tetrapeptide derivatives are provided which have useful activity as inhibitors of platelet aggregation. These compounds have the sequence X-Gly-Asp-Y wherein X is illustrated by arginine and Y is illustrated by O-methyltyrosine amide.

公开(公告)号：US06387880B1

公开(公告)日：2002-05-14

申请号：US08633734

申请日：1996-04-22

申请人： Larry P. Feigen ,  Martin John Griffin

发明人： Larry P. Feigen ,  Martin John Griffin

IPC分类号： A61K3144

CPC分类号： A61K31/198

摘要： The present invention is for pharmaceutical compositions and a method of use for the transdermal delivery of N-[N-[5-[4-(aminoiminomethyl)phenyl]-1-oxopentyl]-L-&agr;-aspartyl]-L-phenylalanine or its esters and their pharmaceutically acceptable salts which are useful as platelet aggregation inhibitors.

摘要翻译： 本发明是用于药物组合物和用于透皮递送N- [N- [5- [4-（氨基亚氨基甲基）苯基] -1-氧代戊基] -L-α-天冬氨酰基] -L-苯丙氨酸或 其酯及其药学上可接受的盐，其可用作血小板聚集抑制剂。

公开(公告)号：US06150114A

公开(公告)日：2000-11-21

申请号：US856761

申请日：1997-05-15

申请人： Larry P. Feigen ,  Christopher P. Carron ,  Neal F. Haas ,  Debra M. Meyer ,  Jimmy D. Page ,  Jodi A. Pegg

发明人： Larry P. Feigen ,  Christopher P. Carron ,  Neal F. Haas ,  Debra M. Meyer ,  Jimmy D. Page ,  Jodi A. Pegg

IPC分类号： C12P21/08 ,  C07K16/44 ,  C12N5/10 ,  C12N5/18 ,  G01N33/53 ,  G01N33/577 ,  G01N33/86 ,  G01N33/94 ,  G01N33/96 ,  C12P21/06 ,  C12Q1/56 ,  G01N33/567

CPC分类号： C07K16/44 ,  G01N33/86 ,  G01N33/94 ,  Y10S435/808 ,  Y10S435/975

摘要： A method for determining the amount of an antiplatelet compound in a subject being treated with the compound which comprises calculating the ACT number of the subject's blood containing a reagent which immunoreacts with the antiplatelet compound and comparing the figure to a standardized concentration figure. In subjects concurrently being treated with heparin and antiplatelet compounds, the method can be practiced without additional heparin added to the blood sample. The invention also provides reagents which immunoreact with antiplatelet compounds and kits comprising immunoreactive reagents.

摘要翻译： 一种用于测定用化合物治疗的受试者中抗血小板化合物的量的方法，包括计算含有与抗血小板药化合物免疫反应的试剂的受试者血液的ACT数，并将该比值与标准化浓度值进行比较。 在同时使用肝素和抗血小板药物治疗的受试者中，可以在不加入血液样品的另外肝素的情况下实施该方法。 本发明还提供了与抗血小板药物免疫反应的试剂和包含免疫反应性试剂的试剂盒。

公开(公告)号：US5053393A

公开(公告)日：1991-10-01

申请号：US540953

申请日：1990-06-20

申请人： Foe S. Tjoeng ,  Larry P. Feigen ,  Steven P. Adams

发明人： Foe S. Tjoeng ,  Larry P. Feigen ,  Steven P. Adams

IPC分类号： A61K38/00 ,  A61K38/46 ,  A61P7/02 ,  C07C279/14 ,  C07K5/02 ,  C07K5/06 ,  C07K5/072 ,  A61K31/21

CPC分类号： C07C279/14 ,  C07K5/021 ,  C07K5/06113 ,  A61K38/00

摘要： N-[8-[(Aminoiminomethyl)amino]-1-oxooctyl]-N-L-.alpha.-aspartyl-L-phenylanine is disclosed as a highly potent inhibitor of platelet aggregation.

摘要翻译： 公开了N- [8 - [（氨基亚氨基甲基）氨基] -1-氧代辛基] -N-L-天冬酰基-L-苯丙氨酸作为血小板聚集的高效抑制剂。