| 摘要 |
The compounds of formula I may be used to treat infection or disease caused by a retrovirus. The compounds may be used in combination with a HIV reverse transcriptase inhibitor, AZT or ddC. In formula I: R1 is H, 2- or 3- or 4- (CH2)n' OR' or (CH2)n' N(R')2 where n' is 0 or 1 and wherein 2- or 3- or 4- refer to the point of substitution on the phenyl ring; R2 and R3 are independently H, OR, N(R)2, a straight or branched alkyl of 1-4 carbons, a cycloalkyl of 3-6 carbons, F, Cl, Br, NRCOR, COR, CON(R)2, OCOR, CO2R, NRSO2R, SO2N(R)2, NRSO3R, NRSO2N(R)2, NRCON(R)2, or R2 and R3 may be taken together to form a ring of 5-6 atoms optionally containing 1 or 2 heteroatoms; R4 is a straight or branched alkyl of 1-7 carbons, a cycloalkyl of 3-7 carbons, a heterocycle of 4-7 atoms containing 1-2 heteroatoms, or (CH2)n Ph, all of which may be optionally substituted by F, Cl, Br, R, OR, SR, N(R)2, CON(R)2, NRCOR, SO2R and COR; R5 is H, (CH2)nOR, (CH2)nN(R)2, (CH2)nNRCOR, (CH2)nOSO2N(R)2, (CH2)nOSO2R, (CH2)nNRSO2 N(R)2, OCH2CH2OR, NRCH2CH2OR, (CH2)nCN, (CH2)nCON(R)2, (CH2)nNRCON(R)2, C(CH3)2OR, (CH2)nCOR, (CH2)nNRSO2R, (CH2)nCO2R, O(CH2)nCO2R, OCON(R)2, NR(CH2)nCO2R, -(CH2)n-NR-CS-N(R)2, (CH2)n-NRSO2OR, wherein n is an integer of from 0 to 3; R6 is methyl, ethyl or isopropyl; R is independently H, a straight or branched alkyl of 1-5 carbons, a -(CH2)n-cycloalkyl wherein the cycloalkyl is of 3-6 carbons and wherein n is an integer of from 0 to 3, -(CH2)m-Ph, a (CH2)m-heterocycle wherein the heterocycle is of 5-6 atoms with 1-3 heteroatoms and wherein m is an integer of from 0 to 3, and wherein the (R)2 in N(R)2 may be a heterocycle containing the nitrogen, all optionally substituted by F, Cl, Br, =O, -CN, -CF3, OR', COR', N(R')2, CON(R')2, or NR'COR'; and R' is H, a straight or branched alkyl of 1-3 carbons, or Ph; and n" is an integer of from 1-2.
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