abstract |
These compounds, which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants, are of the formula (I), where one of R1 and R2 is of the formula Ia and the other is H, OH, halo, CN, NO, C(O)OR, NRR or optionally substituted alkoxy or alkyl, R3 is OH, halo, CN, NO, C(O)OR, NRR or optionally substituted alkoxy or alkyl, Z is O or NR, Ar1 is optionally substituted aryl or heteroaryl; Y is O, S, S(O), S(O)2 or N(R), n is 0-4 and B is of the formula Ib, Ic, Id or Ie. |