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1.发明公开
公开(公告)号：EP0910416A2
公开(公告)日：1999-04-28
申请号：EP97931012.0
申请日：1997-06-05
发明人： FEIGEN, Larry, P. , FLYNN, Daniel, Lee , NEEDLEMAN, Philip , SRINIVASAN, Ananthachari , ZABLOCKI, Jeffery, Alan , SCHMIDT, Michelle A.
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.
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2.发明公开
公开(公告)号：EP0912901A1
公开(公告)日：1999-05-06
申请号：EP97924591.0
申请日：1997-05-12
申请人： G.D. SEARLE & CO.
发明人： CARRON, Christopher, P. , FEIGEN, Larry, P. , HAAS, Neal, F. , MEYER, Debra, M. , PAGE, Jimmy, D. , PEGG, Jodi, Ann
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.
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3.发明授权
公开(公告)号：EP0912901B1
公开(公告)日：2001-11-07
申请号：EP97924591.7
申请日：1997-05-12
申请人： G.D. SEARLE & CO.
发明人： CARRON, Christopher, P. , FEIGEN, Larry, P. , HAAS, Neal, F. , MEYER, Debra, M. , PAGE, Jimmy, D. , PEGG, Jodi, Ann
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.
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4.发明授权TRANSDERMAL COMPOSITION OF N- N- 5- 4-(AMINOIMINOMETHYL)PHENYL]-1-OXOPENTYL]-L-alpha-ASPARTYL]-L-PHENYLALANINE OR ITS ESTERS AND THEIR PHARMACEUTICALLY ACCEPTABLE SALTS 失效N-（N-（5-（4-（氨基亚氨基甲基）苯基-1-氧代戊基）的透皮组合物-L-α-天冬氨酰基）-L-苯丙氨酸或其酯衍生物及其盐PHARMAZEUTISCHVERWENDBAREN
公开(公告)号：EP0729362B1
公开(公告)日：2000-01-12
申请号：EP94931926.3
申请日：1994-10-24
申请人： G.D. SEARLE & CO.
IPC分类号： A61K38/05
CPC分类号： A61K38/05
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5.发明公开TRANSDERMAL COMPOSITION OF N- N- 5- 4-(AMINOIMINOMETHYL)PHENYL]-1-OXOPENTYL]-L-$g(a)-ASPARTYL]-L-PHENYLALANINE OR ITS ESTERS AND THEIR PHARMACEUTICALLY ACCEPTABLE SALTS 失效N-（N-（5-（4-（氨基亚氨基甲基）苯基-1-氧代戊基）的透皮组合物-L-α-天冬氨酰基）-L-苯丙氨酸或酯衍生物及其盐PHARMAZEUTISCHVERWENDBAREN
公开(公告)号：EP0729362A1
公开(公告)日：1996-09-04
申请号：EP94931926.0
申请日：1994-10-24
申请人： G.D. SEARLE & CO.
CPC分类号： A61K38/05
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-α-aspartyl]-L-phenylalanine or its esters and their pharmaceutically acceptable salts which are useful as platelet aggregation inhibitors. In formula (I), R can be independently hydrogen or alkyl having 1 to 6 carbon atoms.
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