| abstract |
Disclosed are compounds of the formula: X Y Z A P Q T which are highly potent, selective factor IIa inhibitors. X, when present, may be connected to T, may be H, CH3, an acyl group, or a general protective group. Y is D-DPA, D-Phe, D-Val, D-Ile, D-Nle, a phenylsulfonyl, Dansyl, or 8-(1,2,3,4-tetrahydroquinolinosulfonyl) compound. Z, when present, is Gly, L/D-Pro, L/D-Ala, L/D-Leu, aminoisobutyric acid, a substituted or unsubstituted L/D-Pro ring homologue, or L/D-Val. A may be <CHEM> wherein M is -CO-CF2-(CO)s-, -(CO)d-NH-, -(CO)d-(CH2)p-, or -CH(OH)-(CH2)p-, d is 0=2, p and q are 0-5, and s is 0 or 1, or A is a proline-like group. P and Q (if Q is present) are substituted or unsubstituted amino acids selected from the group consisting of L/D-Phe, L/D-Cha, L/D-Nal(1), L/D-Nal(2), L/D-phenylglycinyl, L/D-Leu, L/D-Ile, L/D-Nle, L/D-Arg, L/D-Lys, or L/D-His. T may be connected to X, or may be -OH, -OR<4>, -NH2, -NHR<4>, or -NR<4>R<5>, wherein R<4> and R<5> are independently selected from alkyl, aryl, (ar)alkyl, and wherein R<4> and R<5> can be cyclically bonded one to another. |