| 摘要 |
<p>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</SUB>) or an amino-protecting group; aa<SUP>1 </SUP>is an amino acid residue having a side chain selected from formula (A) and (B)-(CO)<SUB>a</SUB>-(CH<SUB>2</SUB>)<SUB>b</SUB>-D<SUB>c</SUB>-(CH<SUB>2</SUB>)<SUB>d</SUB>-E (A), -(CO)<SUB>a</SUB>-(CH<SUB>2</SUB>)<SUB>b</SUB>-D<SUB>c</SUB>-C<SUB>e</SUB>(E<SUP>1</SUP>)(E<SUP>2</SUP>)(E<SUP>3</SUP>) wherein E<SUP>1</SUP>, E<SUP>2 </SUP>and E<SUP>3 </SUP>are 5-6 membered saturated or unsaturated hydrocarbyl rings, or one of E<SUP>1</SUP>, E<SUP>2 </SUP>and E<SUP>3 </SUP>is hydrogen and the other two are a said hydrocarbyl ring, E, E<SUP>1</SUP>, E<SUP>2 </SUP>and E<SUP>3 </SUP>optionally being halogenated when saturated and mandatorily being halogenated when unsaturated, a particular halogen being fluorine; aa<SUP>2 </SUP>is a residue of an amino acid which binds to the thrombin S2 subsite; and R<SUP>9 </SUP>is a straight chain alkyl group interrupted by one or more ether linkages or R<SUP>9 </SUP>is -(CH2)mW and W is -OH or halogen.</p> |
