SUBSTITUTED POLYCYCLIC ARYL AND HETEROARYLPYRAZINONES USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE

摘要: 1. The compound having the Formula: or a pharmaceutically acceptable salt thereof, wherein; B is selected from group consisting of aryl and heteroaryl wherein carbon adjacent to at point attachment optionally substituted by R , other two atoms any both ; are independently hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, lower alkylamino, C1-10 alkylthio, amidosulfonyl, monoC1-10 alkyl diC1-10 alkyl, halo, haloC1-10 haloalkoxy, hydroxyC1-10 carboalkoxy, carboxy, carboxamido, cyano, Q; A single covalent bond (CH(R ))pa-(W )rr rr an integer 0 through 1, pa 3, W (R )NC(O) N(R ); hydroxy alkyl; halo; Z -Q; CH2; Q alkylsulfonamido, alkylsulfinyl, alkylsulfonyl, cyano; aminoC1-10 carboxyC1-10 amidocarbonyl, Y formula (IV): D J C, N, O, S with provisos that no more than one bond, K S, must be when O four N; alkanoyl, haloalkanoyl, proviso NR C(NR )NR same time; hydroxy; CH2, CH2CH2. 2. as recited in Claim 1 wherein: phenyl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, 1,3,5-triazin-2-yl, methoxy, ethoxy, isopropoxy, propoxy, methoxyamino, ethoxyamino, trifluoroacetamido, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, NH, N(CH3), N(OH), CH3CH, CF3CH, NHC(O), N(CH3)C(O), C(O)NH, C(O)N(CH3), CH2CH2, CH2CH2CH2, CH3CHCH2 CF3CHCH2; methyl, ethyl, propyl, bromo; isopropyl, N,N-dimethylamino, methanesulfonamido, carboxymethyl, aminomethyl, 1-aminoethyl, 2-aminoethyl, of: 1-Q-4-Q -2-R -3-R -5-R -6-R benzene, 2-Q-5-Q -4-R pyridine, 3-Q-6-Q 2-Q-4-Q pyrazine, pyridazine, pyrimidine, 5-Q-2-Q 3-Q-5-Q thiophene, furan, pyrrole, 4-Q-2-Q imidazole, isoxazole, 5-Q-3-Q pyrazole, thiazole thiazole; met