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Abstract

A thrombin inhibitor selected from boronic acids of formula (I), and salts, prodrugs and prodrug salts thereof: wherein X is H (to form NH.sub.2) or an amino-protecting group; aa.sup.1 is an amino acid residue having a side chain selected from formula (A) and (B)--(CO).sub.a--(CH.sub.2).sub.b-D.sub.c-(CH.sub.2).sub.d-E (A), --(CO).sub.a--(CH.sub.2).sub.b-D.sub.c-C.sub.e(E.sup.1)(E.sup.2)(E.sup.3) wherein E.sup.1, E.sup.2 and E.sup.3 are 5-6 membered saturated or unsaturated hydrocarbyl rings, or one of E.sup.1, E.sup.2 and E.sup.3 is hydrogen and the other two are a said hydrocarbyl ring, E, E.sup.1, E.sup.2 and E.sup.3 optionally being halogenated when saturated and mandatorily being halogenated when unsaturated, a particular halogen being fluorine; aa.sup.2 is a residue of an amino acid which binds to the thrombin S2 subsite; and R.sup.9 is a straight chain alkyl group interrupted by one or more ether linkages or R.sup.9 is --(CH2)mW and W is --OH or halogen.

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First Claim