Patent ID: 6974800

Claim:
A formulation comprising: (i) an inhibitor of carboxypeptidase U or a pharmaceutically acceptable salt thereof; and (ii) a thrombin inhibitor or an ester or prodrug thereof, or a salt and/or solvate of any of these, in admixture with a pharmaceutically acceptable adjuvant, diluent, or carrier, wherein the inhibitor of carboxypeptidase U is a compound of formula I or a pharmaceutically acceptable salt or solvate thereof, or a solvate of such a salt, wherein: R 1 s selected from the group consisting of: cycloalkyl, substituted with one or more basic groups; heterocyclyl, comprising at least one nitrogen atom, and substituted with one or more basic groups; heterocyclyl, comprising at least one hetero atom selected from S or O, and substituted with one or more basic groups; and aryl, substituted with one or more basic groups; R 2 is selected from the group consisting of H, acyl, acylamino, alkyl, alkylcarbamoyl, alkylthio, alkoxy, aroyl, aroylamino, aryloxy, arylthio, amidino, amino, aryl, carbamoyl, carboxy, cyano, cycloalkyl, formyl, guanidino, halogen, heterocyclyl, hydroxy, nitro, thiol, a Z 2 N—CO—o—group, a ZO—CO—NZ— group, and a Z 2 N—CO—NZ— group; R 3 is selected from the group consisting of COOR 5 , SO(OR 5 ), SO 3 R 5 , P═O(OR 5 ) 2 , B(OR 5 ) 2 , P═OR 5 (OR 5 ), tetrazole, and a carboxylic acid isostere; R 4 is SH, S—CO—C 1 , —C alkyl, or S—CO-aryl; R 5 is H, C 1 –C 6 alkyl, or aryl; R 6 is H or C 1 –C 6 alkyl; X is selected from the group consisting of O, S, SO, SO 2 , C(Z) 2 , N(Z), NR 6 SO 2 , and SO 2 NR 6 ; Y is C(Z) 2 ; and Z is independently selected from the group consisting of H, C 1 –c 6 alkyl, aryl, cycloalkyl and heterocyclyl.