Tripeptide antithrombotic agents

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 5/078 (2006.01) A61K 38/05 (2006.01) A61K 38/06 (2006.01) C07K 5/065 (2006.01) C07K 5/08 (2006.01) C07K 5/087 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2052013

Thrombin inhibitors represented by the formula (see formula I) as provided wherein A(C=O)- is, inter alia, phenylglycyl, cyclohexylglycyl, cyclohexenylglycyl, thienylglycyl or naphthylglycyl, wherein the .alpha.-amino group is preferably substituted by alkyl e.g. methyl or an alkoxycarbonyl, cycloalkoxycarbonyl or arylkoxycarbonyl group e.g. t-butyloxycarbonyl. A(C=O)- also represents an .alpha.-substituted acetyl group such as .alpha.-methoxyphenylacetyl; or a bicyclic group such as a tetrahydroisoquinolin-1-oyl group; or a 1-amino or (substituted amino) cycloalkylcarbonyl group such as 1-aminocyclohexylcarbonyl. Also provided are a method for inhibiting the formation of blood clots in man and animals by administering a thrombin inhibitor of the above formula and pharmaceutical formulations useful in the method.

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