Heterobicycles containing nitrogen as factor Xa inhibitors.
2000
A compound of formula A or B: or stereoisomer or pharmaceutically acceptable salt thereof; G is a group of formula I or II: ring D is selected from - (CH2) 3-, - (CH2) 4-, - CH2N = CH-, -CH2CH2N = CH-, and an aromatic system 5-6 members containing 0-2 selected from the group of N, O and S heteroatoms; ring D, when present, is substituted with 0-2 R, provided that when D is unsubstituted, it contains at least one heteroatom; E is selected from phenyl, pyridyl, pyrimidyl, pyrazinyl, and pyridazinyl, substituted with 0-1 R; R is selected from Cl, F, Br, I, OH, C1-3alkoxy, NH2, NH (C1-3 alkyl), N (C1-3alkyl) 2, CH2NH2, CH2NH (C1-3 alkyl), CH2N ( C1-3alkyl) 2, CH2CH2NH2, CH2CH2NH (C1-3 alkyl) alkyl, and CH2CH2N (C1-3 alkyl) 2; alternatively, ring D is absent; when ring D is absent, ring E is selected from phenyl, pyridyl, pyrimidyl, pyrazinyl, and pyridazinyl, and ring E is substituted with Ra and Rb; Ra is selected from H, F, Cl, Br, I, SR3, CO2R3, NO2, (CH2) TOR3, C1-4 alkyl, OCF3, CF3, C (O) NR7R8, and (CR8R9) tNR7R8; Rb is selected from F, Cl, Br, I, OH, C1-3alkoxy, CN, C (= NR8) NR7R9, NHC (= NR8) NR7R9, NR8CH (= NR7), C (O) NR7R8, (CR8R9) tNR7R8, SH, (C 1-3 alkyl) -S, S (O) R3b, S (O) 2R3a, S (O) 2NR2R2a, OCF3, and 5-6 membered heteroaromatic system containing 1-4 heteroatoms selected the group N, O and S and substituted with Rc; alternatively, Ra and Rb combine to form methylenedioxy or ethylenedioxy; Rc is selected from OH, SH, C1-3 alkoxy, C1-3 thioalkoxy, NH2, NH (C1-3 alkyl), N (C1-3 alkyl) 2, CH2NH2, CH2NH (C1-3 alkyl), CH2N (alkyl C1-3alkyl) 2, CH2CH2NH2, CH2CH2NH (C1-3 alkyl), and CH2CH2N (C1-3 alkyl) 2; Z is N or CR1a.
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