G.d. Searle & Company

Monsanto Company

Larry P Feigen

Steven P Adams

Daniel L Flynn

Ananthachari Srinivasan

Foe S Tjoeng

Masateru Miyano

Martin John Griffin

Debra M Meyer

Christopher P Carron

Michelle A Schmidt

Jeffery Alan Zablocki

Jodi A Pegg

Philip Needleman

Neal F Haas

Jimmy D Page

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

Transdermal N-&lsqb;N-&lsqb;5-&lsqb;4-(aminoiminomethly)phenyl&rsqb;-1-oxopentyl&rsqb;-L-&agr;-aspartyl&rsqb;-L-phenylalainine or its esters and their pharmaceutically acceptable salts

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.

Method and reagent for monitoring blood levels of antiplantelet compounds

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.

Radiopharmaceutical compositions capable of localizing at sites of

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

Novel platelet-aggregation inhibitor

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.

Novel platelet-aggregation inhibitor peptide derivatives

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Wauconda, IL, United States of America

Larry P Feigen