HETEROCICLICAL COMPOUNDS AS INHIBITORS OF THE FACTOR VIIA.

摘要

A compound of Formula (I): (See formula) or a pharmaceutically acceptable stereoisomer, tautomer, salt or solvate thereof, wherein: X is selected from: (See formula) in which X 1, X 2 , X 3, X 4, X 5, X 6, X 7, X 8, and X 9 are independently CR 6 or N, with the proviso that X does not contain more than three nitrogen atoms in the ring; R 6 is, independently each time it appears, H, - (CH2) r -OR a, F, Cl, Br, OCF3, CN, NO2, -NR b R c, - (CF2) r CF3, or alkyl C1-6 substituted with 0-2 R e; R 8 is phenyl substituted with 0-5 R 8b, or a 5- to 6-membered heteroaryl comprising: carbon atoms and 1-4 heteroatoms that are selected from N, O, and S, wherein said heteroaryl is substituted with 0-5 R 8b; R 8a is H or C1-4 alkyl; R 8b is, independently each time it appears, H, - (CH2) r -OR a, SR a, F, Cl, Br, I, CN, NO2, -OCF3, -NR b R c, -C ( O) R a, -C (O) OR a, -NR d C (O) R a, -C (O) NR c R d, -SO2NR c R d, -NR c SO2NR c R d, -NR c SO2R a1, -NR c SO2CF3, -S (O) 2CF3, -S (O) 2R a1, -S (O) R a1, - (CF2) r CF3, C1-6 alkyl substituted with 0-2 R e, C2-6 alkenyl substituted with 0-2 R e, C2-6 alkynyl substituted with 0-2 R e, - (CH2) r - (C3-7 cycloalkyl) substituted with 0-2 R e, - (CH2) r - (C3-7 cycloalkenyl) substituted with 0-2 R e, - (CH2) r -phenyl substituted with 0-4 R f, - (CH2) r-5- to 6-membered heteroaryl comprising: carbon atoms and 1- 4 heteroatoms that are selected from N, O, and S (O) p, or - (CH2) r-4 to 7-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms that are selected from N , O, and S (O) p, wherein said heteroaryl and heterocycle are substituted with 0-4 R f; (See formula) alternatively, two R 8b groups in two adjacent carbon atoms can be taken together with the carbon atoms to which they are attached, forming a 5- to 7-membered carbocycle or heterocycle comprising: carbon atoms and 0 -4 heteroatoms that are selected from N, O, and S (O) p, wherein said carbocycle and heterocycle are substituted with 0-3 R f; it is a 5- to 6-membered heteroaryl including the nitrogen atom shown in the ring, which comprises ...