Aryl- and heteroaryl-substituted polycyclic pyrazinones for selective inhibition of the coagulation cascade.

2000 
A compound having the formula or a pharmaceutically acceptable salt thereof, wherein; B is selected from the group consisting of: (i) aryl and heteroaryl wherein a carbon adjacent to the point of attachment carbon is optionally substituted by R32, the other carbon adjacent to the point of attachment carbon is optionally substituted by R36 an adjacent R32 carbon and two atoms from the carbon at the point of attachment is optionally substituted by R33, adjacent to R36 carbon and two atoms from the carbon at the point of attachment is optionally substituted by R35, and any carbon adjacent to both R35 is R33 as optionally substituted by R34; (Ii) hydrido, alkyl of 2 to 8 carbon atoms, alkenyl of 3 to 8 carbon atoms, alkynyl of 3 to 8 carbon atoms and haloalkyl of 2 to 8 carbon atoms, wherein each member of group B is optionally substituted at any carbon up to and including 6 atoms from a junction point deB to a with one or more of the group consisting of R32, R33, R34, R35 and R36; and (iii) cycloalkyl of 3 to 7 carbon atoms and saturated 4- to 6 carbon atoms, wherein each ring carbon is optionally substituted with R33, a ring carbon other than the ring carbon at the point of attachment of B to a is optionally substituted with oxo provided that no more than one ring carbon is substituted by oxo at the same time, ring carbons and an adjacent carbon atom in the junction nitrogen are optionally substituted with R9 or R13, a ring carbon or nitrogen adjacent to the R9 position and two atoms from the point of attachment is optionally substituted with R10, a ring carbon or nitrogen adjacent to the R13 position and two atoms from the point of attachment is optionally substituted with R12.
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