| 摘要 |
<p>PCT No. PCT/SE97/00315 Sec. 371 Date Oct. 6, 1997 Sec. 102(e) Date Oct. 6, 1997 PCT Filed Feb. 25, 1997 PCT Pub. No. WO97/31940 PCT Pub. Date Sep. 4, 1997The present invention is directed to compounds that act as analgesics and that have the structure of formula (I): wherein; Z is wherein, n is 1 or 2, and R0 is C6-12 aryl or C7-8 aralkyl; or R1 is selected from the group consisting of hydrogen; -NH-C1-6 alkyl; C1-6 alkyl; C6-12 aryl; C7-18 aralkyl; arginyl; and R30NHC(=NH)-, wherein R30 is hydrogen, C6-12 aryl, C7-18 aralkyl, or C1-6 alkyl; R2 is hydrogen; C1-6 alkyl; or OH; R3 is C6-12 aryl; C7-18 aralkyl; -CH2-C6H2R8R9;or -CH2-OHC6HR8R9, wherein each of R8 and R9 is independently, or hydrogen; R4 C6-12 aryl; C7-18 aralkyl; C1-12 alkyl; or a substituted or unsubstituted cyclohexyl; R5 is C1-6 alkyl; hydrogen; OH; halogen; SH; NO2; NH2; -NH-C1-6 alkyl; NH2C (=NH-; NH2C (=NH)-NH-; COOR31, wherein, R31 is hydrogen, or C1-6 alkyl; X is CH2NHC(O)-; CH2NHC(O)O; -C(O)NH-; or CH2NH-; and L is a C1-12 alkylene chain which can be substituted with at least one substituent selected from the group consisting of; a C3-C12 cycloalkyl containing at least one heteroatom; C1-6 alkyl; OR31; -NHC(O)R33; -OC(O)R34 -NHR35 wherein; and NR6R7; with the proviso that when R5 is hydrogen, Z is and X is -C(O)NH-, or -CH2NH-, then L is a C1-12 alkyl chain substituted with at least one substituent selected from the group consisting of; a C3-C12 cycloalkyl containing at least one heteroatom; C1-6 alkyl; OR31; SR32; -NHC(O)R33; -OC(O)R34, -NHR35; and NR6R7.</p> |
