| 主权项 |
1. A compound of the formula I: wherein R1 is selected from the group consisting of:
(i) H;(ii) C1-C8 alkyl substituted by one or more radicals selected from the group consisting of hydroxy, C1-C8 alkoxy, cyano, carboxy, aminocarbonyl, C1-C8 (alkyl)aminocarbonyl, di(C1-C8)alkylaminocarbonyl, C1-C8 (alkoxy)carbonyl, and C1-C8 (alkyl)carbonyloxy;(iii) —CORS, wherein R8 is C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C3-C8 cycloalkyl, aryl, or heteroaryl, wherein said alkyl, alkenyl, alkynyl, aryl, or heteroaryl group is optionally substituted by one or more of the following groups: halogen atoms, C1-C8 alkyl, hydroxy, amino, C1-C8 alkylamino, di(C1-C8)alkylamino, mercapto, C1-C8 alkylthio, cyano, C1-C8 alkoxy, carboxy, C1-C8 (alkoxy)carbonyl, C1-C8 (alkyl)carbonyloxy, C1-C8 (alkyl)sulfonyl, C1-C8 (alkyl)carbonylamino, aminocarbonyl, C1-C8 (alkyl)aminocarbonyl, or di(C1-C8)alkylaminocarbonyl, or a C1-C5 alkyl group is substituted by an amino group at the α-position to the CO group and may be further substituted by a group selected from the group consisting of hydroxy, methylthio, mercapto, phenyl, hydroxyphenyl, indolyl, aminocarbonyl, carboxy, amino, guanidino, and imidazolyl;(iv) —COOR9, wherein R9 is C1-C8 alkyl optionally substituted by halogen, C1-C8 alkoxy, phenyl optionally substituted by nitro, hydroxy, carboxy, or C3-C6 cycloalkyl; C2-C4 alkenyl; C2-C4 alkynyl; C5-C7 cycloalkyl; or phenyl optionally substituted by halogen, amino, nitro, C1-C8 alkyl, C1-C8 (alkoxy)carbonyl, or C1-C8 alkoxy;(v) —CH2—O—CO—R10, or —CH(CH3)—O—CO—R10, wherein R10 is C1-C8 alkyl optionally substituted by halogen or C1-C8 alkoxy; C2-C4 alkenyl optionally substituted by phenyl; C3-C6 cycloalkyl; phenyl optionally substituted by C1-C8 alkoxy; or heteroaryl selected from the group consisting of furyl, thienyl, isoxazolyl, or pyridyl optionally substituted by halogen or C1-C8 alkyl; and(vi) —PO(OR11)2, —CH2—O—PO(OR11)2 or —CH(CH3)—O—PO(OR11)2, wherein R11 is independently selected from the group consisting of H, C1-C8 alkyl, or C1-C8 alkyl optionally substituted by hydroxy, C1-C8 alkoxy, or C1-C8 (alkyl)carbonyloxy;R2 and R3 each independently is H, C1-C8 alkyl, Cl or F, or halo(C1-C8)alkyl;R4 is H or C1-C8 alkyl, and R5 is propargyl, allyl, cyclobutyl, or cyclopropyl;R6 is H, C1-C8 alkyl, C1-C8 alkoxy, mercapto, C1-C8 alkylthio, hydroxy, mercapto, amino, C1-C8 alkylamino, di(C1-C8)alkylamino or oxo, thioxo, imino, or C1-C8 alkylimino at the 2- or 4-position of the ring;R7 is H, halogen, C1-C8 alkyl, perhalo C1-C8 alkyl, C3-C8 cycloalkyl, C1-C8 alkoxy, C1-C8 alkylthio, hydroxy, mercapto, amino, C1-C8 alkylamino, di(C1-C8)alkylamino, cyano, C1-C8 alkylsulfonyl, C1-C8 alkylcarbonylamino, C1-C8 alkylcarbonyl(C1-C8)amino, or C1-C8 alkylsulfonyl(C1-C8)amino;n is 0-8,and pharmaceutically acceptable salts thereof,but excluding the compounds wherein R1, R2, R3, R6, R7 are H; n is 0; R4 is H or CH3, and R5 is propargyl, or R1, R2, R3, R4, R6, R7 are H; n is 1, and R5 is propargyl. |
