SUBSTITUTED PYRIDONES, USE THEREOF, COMPOSITION AND METHOD FOR INHIBITING THROMBOTIC CONDITIONS AND METHODS OF PROPHYLAXIS AND TREATMENT

摘要

The invention relates to substituted polycyclic aryl and heteroaryl pyridone compounds having Formula (I) or a pharmaceutically acceptable salt thereof, wherein B is selected from phenyl, C1-C6 alkyl and C3-C6 cycloalkyl; A is selected from a single covalent bond, -(CH2)n-, wherein n is an integer from 1 to 5, -SO2- and -C(O)-; R<1> and X<0> are hydrogen; R<2> is an optionally substituted phenyl, or R<2> is together with R<1> form quinoline; K is -(CH2)m-, wherein m is an integer from 1 to 3; E<0> is -C(O)NH-, -NH- or -SO2NH-; and Y<0> is benzyl optionally substituted by amidino- or guanidino group, or an optionally substituted C1-C6 alkyl. The compounds of the present invention are useful as inhibitors of serine proteases of the coagulation cascade and can be used for manufacturing corresponding pharmaceutical compositions. The invention also relates to compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.