| 主权项 |
1. A compound of formula I or pharmaceutical acceptable salts or prodrugs thereof wherein: Het moiety is a 4- to 14-membered cyclic or bicyclic ring system having from one to five hetero atoms selected from N, O, and S, optionally substituted with one to three R6; R1 and R2 are each independently
a. H,b. —C1-8alkyl, optionally substituted with one or more OH, —SH, —CN, —NO2, halo, —NHR5, —NC1-4alkylR5, —OC1-4alkyl, —SC1-4alkyl, —S(C═O)C1-4alkyl, —C(═O)NR5R5, —SO2R5, —SO2NR5R5, or —C3-6cycloalkyl,c. —C3-8cycloalkyl, optionally substituted with one to three R6,d. —SO2R5, —C(═O)NR5R5, —SO2NR5R5, —C(═O)OR5, or —C(═O)R5,e. 4- to 6-membered heterocyclic ring moiety optionally having from one to four hetero atoms selected from the group consisting from N, S and O, wherein the ring or atom is optionally substituted with one to three R6, orf. R1 and R2 taken together with the nitrogen to which they are attached form a 4- to 11-membered cyclic or bicyclic ring moiety optionally having an additional one to two hetero atoms selected from the group consisting of N, S and O, wherein the ring or atom is optionally substituted with one to three R6; R3 and R4 are each independently
a. —H,b. —C1-8alkyl optionally substituted with OH, —SH, halo, —CF3, —CN, —NO2, NH2, —NHR5, —NHR5—OC1-4alkyl, —CH2—O—CH3, —SC1-4alkyl, —S(C═O)C1-4alkyl, —C(═O)NR5R5, —C(═O)OH, —SO2NR5, or —SO2R5,c. —C3-8cycloalkyl, optionally substituted with one to three R6,d. —C(═O)C1-8alkyl wherein alkyl is optionally substituted with —S(═O2)R5, —SO2NR5, or —C(═O)R5,e. 4- to 6-membered heterocyclic ring moiety optionally having from one to three hetero atoms selected from the group consisting from N, S and O, wherein the heterocyclic ring is optionally substituted with one to three R6,f. R3 and R4 taken together form a C3-8cycloalkyl, optionally substituted with one to three R6; org. R3 and R4 taken together with one or two hetero atoms selected from the group consisting of N, S and O to form an oxo group (═O) or to form a 4- to 6-membered heterocyclic ring moiety, wherein the heterocyclic ring is optionally substituted with one to three R6; or R1 and R3, R2 and R4, Wand R4 or R2 and R3 taken together with the nitrogen atom to which they are attached form a 4- to 6-membered heterocyclic ring moiety optionally having from one to two hetero atoms selected from the group consisting from N, S and O, wherein the heterocyclic ring is optionally substituted with one to three R6; at each occurrence, R5 is independently hydrogen, C1-6alkyl, —C3-6cycloalkyl, NH2 or tetrahydro-2H-pyranyl, wherein said alkyl is optionally substituted with one, two or three R6; at each occurrence, R6 is H, C1-6alkyl, halo, —CN, —NO2, —CF3, —C3-6cycloalkyl, oxo (═O), —NH2, —NHC1-4alkyl, —N(C1-4alkyl)2, —OC1-4alkyl, oxo, —SH, —SC1-4alkyl, —S(C═O)C1-4alkyl, —SO2R5, —SONC1-4alkyl, —C(═O)C1-4 alkyl, —C(═O)NH2, —C(═O)NHC1-4alkyl, —C(═O)N(C1-4alkyl)2, —NC(═O)NH2, —NC(═O)NHC1-4alkyl, NC(═O)N(C1-4alkyl)2, CF3 or a 4- to 6-membered heterocyclic ring moiety optionally having from one to four hetero atoms selected from the group consisting of N, S and O; W is —H, —PO(OH)2, —PO(OH)halo, —CH2OPO(OH)2, —C(═O)C1-4alkyl, or —CH2OC(═O)C1-4alkyl, wherein C1-4alkyl is optionally substituted with —OCO2H, —OCO2C1-4alkyl, or —OC(═O)NHC1-4alkyl; and X, Y and Z are each independently H, halo, C1-4alkyl, C3-6cycloalkyl, —OH, CF3, —NH2, —CN, N3 or —S—CF3; provided that when R3 and R4 are taken together to form an oxo group (═O), then R1 and R2 are not both hydrogen. |
