Patent ID: 7112590

Claim:
Compounds of general formula (I) D-CO—B-A-Het (I) wherein Het represents a group selected from the group consisting of formulae: R 1 and R 2 independently represent H or NH 2 ; A represents group —CONH— or —CH 2 NH— attached to Het by the NH fragment, group —CONHCH 2 — or —CH 2 NHCH 2 — attached to Het by the CH 2 fragment, group —CH 2 NHCONH—, —CH 2 NHCH 2 CONH— or —CH 2 NHCOCH 2 NH— attached to Het by the NH fragment, group —CH 2 NHCONHCH 2 —, —CH 2 NHCH 2 CONHCH 2 — or —CH 2 NHCOCH 2 NHCH 2 — attached to Het by the CH 2 fragment; B is selected from the group consisting of groups of formulae: Z is CH 2 , S or CH—OH R 3 is H, straight or branched C 1 –C 4 alkyl, C 3 –C 7 cycloalkyl R 4 is H, straight or branched C 1 –C 4 alkyl, C 3 –C 7 cycloalkyl; D represents a group wherein R d is H, CH 2 OH, CH 2 SH or a group wherein R a and R b are independently selected from the group consisting of: H, C 1 –C 4 straight or branched alkyl which can be substituted with C 3 –C 7 cycloalkyl or with 1 to 9 atoms of halogen selected from F, Cl, Br, I, C 3 –C 7 cycloalkyl, C 9 –C 10 bicycloalkyl, a stable saturated or unsaturated 5- to 7-membrered monocyclic heterocyclic system, or a 8- to 10-membrered bicyclic heterocyclic system which, in addition to carbon atoms, contains 1 to 3 heteroatoms selected from the group consisting of N, O and S, in which N or S can be oxidized or N quaternized, aryl which can be optionally unsubstituted or substituted at any position with one or two substituents selected from C 1-4 alkyl, C 1-4 alkoxy, halogen or hydroxy, R c is selected from the group consisting of: NH 2 NH(CH 2 ) n CH 3 , where n is 0, 1, 2 or 3, NH(CH 2 ) m OH, where m is 2, 3 or 4, NH(CH 2 ) k COOH, where k is 1, 2 or 3, NH(CH 2 ) n COOR 5 , where n is 0, 1, 2 or 3 and R 5 represents C 1-4 straight or branched alkyl, NH(CH 2 ) k CONR 6 R 7 , where k is 1, 2 or 3 and R 6 in R 7 are independently H or straight or branched C 1-4 alkyl, or R 6 and R 7 together are —(CH 2 ) 4-5 —, —(CH 2 ) 2 O(CH 2 ) 2 — or —(CH 2 ) 2 NH(CH 2 ) 2 —, NHO 2 S(CH 2 ) n —W where n is 0, 1, 2 or 3, W represents phenyl, naphthyl, a saturated or unsaturated monocyclic 5- or 6-membered or saturated or unsaturated bicyclic 8- to 10-membered heterocyclic ring which contains from 1 to 3 heteroatoms selected from the group consisting of N, O or S in which N or S can be oxidized or N quaternized; each ring may be optionally substituted by one or more substituents selected from the group consisting of C 1-4 alkyl, C 1-4 alkoxy, amino, cyano, halogen or hydroxy, —N[O 2 S(CH 2 ) n —W][(CH 2 ) k COOH]where n is 0, 1, 2 or 3 and where k is 1, 2 or 3, NH(CH 2 ) k NH 2 , where k is 1, 2 or 3, NHC(Ph) 3 , in the form of pure diastereomers or a mixture of diastereomers or pharmaceutically acceptable salts thereof with anticoagulant activity.