Amidine inhibitors of serine proteases

A compound of formula (I)

• 52
• wherein
• X is O, CR6R6′, NR6 or S, wherein R6 and R6, are independently H or alkyl;
• R1 is H, —OR7, an amino acid or —NR7R7′ wherein R7 and R7′ are independently H or a hydrocarbon chain, a carbocycle, a heterocycle, a carbocycle-substituted hydrocarbon chain or a heterocycle-substituted hydrocarbon chain optionally substituted with hydroxyl, halogen, cyano, amino, nitro, amidine, guanidine alkyl, halo-substituted alkyl, alkoxy, aryl or carboxyl;
• or R7 and R7′ together form a heterocyle optionally fused to another heterocycle or carbocycle wherein said heterocycle and carbocycle are optionally substituted with hydroxyl, halogen, amino, nitro, amidine, guanidine, alkyl, halo-substituted alkyl, alkoxy or carboxyl;
• R2 is H or a hydrocarbon chain, a carbocycle or a carbocycle-substituted hydrocarbon chain optionally substituted with hydroxyl, oxo, halogen, cyano, amino, nitro, amidine, guanidine, alkyl, halo-substituted alkyl, alkoxy or carboxyl;
• and wherein said hydrocarbon chain is optionally interrupted with N, O, S, SO or SO2;
• R3 is H or a protecting group;
• R4 is selected from the group consisting of H, hydroxyl, halogen, amino, nitro, amidine, guanidine and acylamino;
• R5 is H or R4 and R5 together form a 5 or 6 member carbocycle or heterocycle ring optionally substituted with hydroxyl, halogen, amino, nitro, amidine, guanidine or acylamino;
• n is 0 or 1;
• and
• salts, solvates and hydrates thereof.