BENCIMIDAZOLINONAS, BENZOXAZOLINONAS, BENZOPIPERAZINONAS, INDANONAS AND THEIR DERIVATIVES AS INHIBITORS OF THE XA FACTOR.

摘要

A compound of formula I: ** (formula) ** or a stereoisomer or pharmaceutically acceptable salt thereof, wherein: one of the W, W1, W2 and W3 is C-D and the remaining are C-R1; alternatively, W-W1, W1-W2 or W2-W3 combine to form C (Da) N and the remaining ones are C-R1; D is selected from CN, C (= NR7) NR8R9, NHC ((= NR7) NR8R9, NR8CH (= NR7), C (O) NR8R9 and (CH2) t NR8R9; Da is NH2, NH (C1_3 alkyl), N (C1_3 alkyl) 2 or C1_3 alkoxy; J is selected from N (ZAB) and CR (ZAB); and Ja and Jb together are selected from CONHCReRf, SO2NHCReRf, (CRaRb) qSO2NRd and (CRaRb) bCOCO (CReRf) c, in those that b + c = 0 or 1; alternatively, J and Ja together are selected from CON (ZAB) (CRcRb) q and N (ZAB) Q (RcRb) a; and Jb is selected from NRd, O and CReRf; Q is CO or CS; alternatively, J, Ja and Jb together are selected from CR (ZAB) (CRaRb) aQNRd, CR (ZAB) (CRaRb) dC (O) O, CR (ZAB) NHCOCReRf, CR (ZAB) NHSO2CReRf, N (ZAB) (CRaRb) aQNRd, N (ZAB) (CRaRb) C (O) O, N (ZAB) SO2) (CRcRb) aCReRf; N (Z-A-B) SO2 (CRcRb) aNRd, CON (Z-A-B) CReRf; CONRb (CRcRb) aN (ZAB) and ** (formula) ** R is selected from H, C1-6 alkyl, NH2, NH (C1-6 alkyl), N (C1-6 alkyl) 2, OH, C1 alkoxy -66, C1-6 alkoxyC1-4alkyl, (CH2) tNR8R9, 5 or 6 membered aromatic heterocyclyl-C1-4alkyl and C1-4alkyl, in which the aromatic heterocyclyl and aryl groups are substituted with 0-1 R4; Ra is selected from H, C16 alkyl, C (O) R2b, 5- or 6-membered aromatic heterocyclyl-C1-4 alkyl and C1-4 arylalkyl, in which the aromatic heterocyclyl and aryl groups are substituted with 0-1 R4 ; Rb is H or C1-2 alkyl; Rc is selected from H, C1-6 alkyl, C (O) R2b, S (O) pR2b, BO2H2, 5- or 6-membered aromatic heterocyclyl, C1-4 alkyl and aryl-C1-4 alkyl, in which the aromatic heterocyclyl groups and aryl are substituted with 0-1 R4; Rd is selected from H, OH, NH2, C1-2 alkyl and C1-2-alkyl, '' alternatively, Rc and Rd, when attached to adjacent atoms, together form a double bond; Re is selected from H, OH, NH2, C1-2 alkyl and C1-2-alkyl, '' alternatively, Rc and Re, when attached to adjacent atoms, together form a double bond.