| 主权项 |
1. A compound represented by one of the general formulae: wherein X is O or S; Y is selected from the group consisting of O, S, NR3 and CR3R4;and wherein the ring system represented by A in formula V, below, is a 5 or 6 membered aryl group,wherein said aryl group is selected from the group consisting of:and wherein the ring system represented by B in formula VI, above, is a five membered unsaturated heterocyclic ring wherein said unsaturated heterocyclic ring is selected from the group consisting of:wherein Z is selected from the group consisting of [C(R2)2]c, O, NR3 and S;and wherein the ring system represented by C in formula VII, above, is a 5 or 6 membered aryl group e.g. a carbocyclic aryl or heterocyclic aryl, wherein said aryl group is selected from the group consisting of:wherein R1 is selected from the group consisting of halogen, aryl, C1 to C8 alkyl, C2 to C8 alkenyl; CF3, OCF3, OCF2H, S(O)fR2, (CR3R4)dC(O)OR2, O(CR3R4)eC(O)OR2, NR2(CR3R4)dC(O)R2, NR2(CR3R4)dC(O)OR2, OP(O)(OR2)2, OC(O)OR2, OCH2O, NR2(CH2)eN(R2)2, O(CH2)eN(R2)2, (CR3R4)dCN, O(CR3R4)eCN, (CR3R4)gAr, NR2(CR3R4)eAr, O(CR3R4)eAr, S(O)f(CR3R4)eAr, (CR3R4)eSO2R2, (CR3R4)eC(O)N(R2)2, NR2(CR3R4)eC(O)N(R2)2, O(CR3R4)dC(O)N(R2)2, C(O)(CR2CR3)eAr, S(O)f(CR3R4)eC(O)N(R2)2, (CR3R4)dOR2, NR2(CR3R4)eOR2, O(CR3R4)eOR2, S(O)f(CR3R4)dOR2, C(O)(CR3R4)dR3, NR2C(O)(CR3R4)eR3, OC(O)(CR3R4)dN(R2)2, C(O)(CR3R4)eN(R2)2, NR2C(O)(CR3R4)dN(R2)2, OC(O)(CR3R4)dN(R2)2, (CR3R4)dR3, NR2(CR3R4)dR3, O(CR3R4)dR3, S(O)f(CR3R4)dR3, (CR3R4)eN(R2)2, NR2(CR3R4)eN(R2)2, O(CR3R4)eN(R2)2, S(O)f (CR3R4)dN(R2)2;R2 is selected from the group consisting of hydrogen, C1 to C8 alkyl, C2 to C8 alkenyl, C2 to C8 alkynyl, C1 to C4 alkylol, lower alkylphenyl, phenyl, (CR3R4)dAr, (CR3R4)dC(O)OR6, (CR3R4)dSO2R6, (CR3R4)dOR6, (CR3R4)dOSO2R6, (CR3R4)dP(O)(OR6)2, (CR3R4)dR6, (CR3R4)eN(R6)2 and (CR3R4)eNR6C(O)N(R6)2;wherein N(R6)2 may form a 3-7 membered heterocyclic ring, for example, pyrrolidine, 3-fluoropyrrolidine, piperidine, 4-fluoropiperidine, N-methylpiperazine, morpholine, 2,6-dimethylmorpholine, thiomorpholine, and wherein said heterocyclic ring may be substituted with one or more of R3; and[C(R2)2]c may form a 3-7 membered carbocyclic or heterocyclic ring;R is selected from the group consisting of halogen, C1 to C8 alkyl, C2 to C8 conjugated alkenyl, (CR2═CR2)dCON(R2)2, CF3, OCF3, OCF2H, (CR3R4)dCN, NR2(CR3R4)eCN, O(CR3R4)eCN, S(O)fR2, (CR3R4)dC(O)OR2, NR2(CR3R4)dC(O)OR2, O(CR3R4)dC(O)OR2, S(O)f(CR3R4)dC(O)OR2, (CR3R4)dAr, NR2(CR3R4)dAr, O(CR3R4)dAr, S(O)f(CR3R4)dAr, (CR3R4)dSO2R2, NR2(CR3R4)dS(O)fR2, O(CR3R4)d S(O)fR2, S(O)f(CR3R4)eS(O)fR2, (CR3R4)dC(O)N(R2)2, NR2(CR3R4)dC(O)N(R2)2, O(CR3R4)dC(O)N(R2)2, S(O)f(CR3R4)eC(O)N(R2)2, (CR3R4)dOR2, NR2 (CR3R4)eOR2, O(CR3R4)eOR2, S(O)f(CR3R4)dOR2, (CR3R4)dOSO2R2, NR2 (CR3R4)eOSO2R2, O(CR3R4)eOSO2R2, S(O)f(CR3R4)eOSO2R2(CR3R4)dP(O)(OR2)2, NR2 (CR3R4)dP(O)(OR2)2, O(CR3R4)dP(O)(OR2)2, S(O)f(CR3R4)eP(O)(OR2)2, C(O)(CR3R4)dR3, NR2C(O)(CR3R4)dR3, OC(O)(CR3R4)dN(R2)2, C(O)(CR3R4)dN(R2)2, NR2C(O)(CR3R4)dN(R2)2, OC(O)(CR3R4)dN(R2)2, (CR3R4)dR3, NR2(CR3R4)dR3, O(CR3R4)dR3, S(O)f(CR3R4)dR3, HNC(O)R2, HN—C(O)OR2, (CR3R4)dN(R2)2, NR2(CR3R4)eN(R2)2, O(CR3R4)eN(R2)2, S(O)f (CR3R4)dN(R2)2, OP(O)(OR2)2, OC(O)OR2, OCH2O, HN—CH═CH, —N(COR2)CH2CH2, HC═N—NH, N═CH—S, (CR3R4)dC═C(CR3R4)dR2, (CR3R4)dC═C(CR3R4)dOR2, (CR3R4)dC═C(CR3R4)dN(R2)2, (CR3R4)dCC(CR3R4)dR2, (CR3R4)dCC(CR3R4)eOR2, (CR3R4)dCC(CR3R4)eN(R2)2, (CR3R4)dC(O)(CR3R4)dR2, (CR3R4)dC(O)(CR3R4)dOR2 and (CR3R4)dC(O)(CR3R4)dN(R2)2;R3 and R4 may be selected from the group consisting of H, F, hydroxy, and C1-C4 alkyl or CR3R4 may represent a carbocyclic or heterocyclic ring of from 3 to 6 carbons or alternatively, (CR3R4)d and (CR3R4)e may form a 3-7 membered carbocyclic or heterocyclic ring, preferablyR3 and R4 are H, F, CH3 or hydroxy;R5 is Ar—R1b wherein Ar is 5-7 membered carbocyclic aryl or 5-7 membered heterocyclic aryl;R6 is selected from the group consisting of hydrogen, C1-C8 alkyl, hydroxylmethyl and phenyl;R7 is selected from the group consisting of hydrogen, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, (R2CCR2)aCN and aryl;a is 0 or an integer of from 1 to 3;b is 0 or an integer of from 1 to 2;c is an integer of from 1 to 2;d is 0 or an integer of from 1 to 5;e is an integer of from 1 to 4;f is 0 or an integer of from 1 to 2;g is an integer of from 2 to 5, and further provided said alkyl or aryl radicals may be substituted with one or two halo, hydroxy, lower alkyloxy, lower alkyl amino or cycloalkylamino radicals wherein the cycloalkyl ring can include an enchained oxygen, sulfur or additional nitrogen atom and may be substituted with one or two halo or lower alkyl radicals; and pharmaceutically acceptable salts thereof. |
