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Modified amino acid for the inhibition of platelet aggregation

Modified amino acid for the inhibition of platelet aggregation description/claims

Platelet activation and aggregation are involved in unstable angina and acute myocardial infarction, in reocclusion following thrombolytic therapy and angioplasty, in transient ischemic attacks and in a variety of other cardiovascular disorders. When a blood vessel is damaged either by acute intervention, such as angioplasty, or more chronically by the pathophysiological processes of atherosclerosis, platelets are activated to adhere to the damaged surface and to each other. This platelet activation, adherence and aggregation may lead to occlusive thrombus formation in the lumen of the blood.

Various agents have been studied for many years as potential targets for inhibiting platelet aggregation and thrombus formation. For example, aspirin has come into use as a prophylactic antithrombotic agent due its ability to inhibit platelet aggregation.

U.S. Pat. Nos. 5,773,647 ('647) and 5,866,536 ('536) describe compositions for the oral delivery of pharmacologically active agents with modified amino acids, such as N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC), N-(10-[2-hydroxybenzoyl]aminodecanoic acid (SNAD), and N-(8-[2-hydroxybenzoyl]amino)caprylic acid (SNAC). In addition, WO 00/059863 ('863) discloses the disodium salts of formula I

wherein R1, R2, R3 and R4 are independently hydrogen, —OH, —NR6R7, halogen, C1-C4alkyl or C1-C4alkoxy; R5 is a substituted or unsubstituted C2-C16alkylene, substituted or unsubstituted C2-C16alkenylene, substituted or unsubstituted C1-C12alkyl(arylene), or substituted or unsubstituted aryl(C1-C12alkylene); and R6 and R7 are independently hydrogen, oxygen or C1-C4alkyl; and hydrates and solvates thereof as particularly efficacious for the oral delivery of active agents.

Surprisingly, it has now been discovered that the modified amino acids of '647, '536 and '863 are effective inhibitors of blood platelet aggregation. Thus, pharmaceutical compositions employing the modified amino acids of '647, '536 and '863 as carriers for pharmacologically active agents have the added advantage of inhibiting blood platelet aggregation.

Accordingly, the present invention provides a method of inhibiting platelet aggregation in a mammal, preferably human, comprising the administration of a platelet aggregation inhibiting amount of a modified amino acid, or a pharmaceutically acceptable salt thereof.

In another embodiment, the invention provides a method of inhibiting platelet aggregation in a mammal, preferably human, comprising the administration of a pharmaceutical composition comprising a platelet aggregation inhibiting amount of a modified amino acid or pharmaceutically acceptable salt thereof.

In an additional embodiment, the present invention provides a method of inhibiting platelet aggregation in a mammal, preferably human, receiving a pharmacologically active agent comprising the administration of a pharmaceutical composition comprising said pharmacologically active agent and a modified amino acid or a pharmaceutically acceptable salt thereof, wherein the modified amino acid or salt thereof is present in an amount effective to inhibit platelet aggregation.

The invention is furthermore concerned with a method of inhibiting platelet aggregation in a mammal (preferably human) comprising administering a platelet aggregation inhibiting amount of N-(−5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC), or a pharmaceutically acceptable salt thereof, to said patient.

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