| abstract |
Morphine derivatives of formula (I), and their salts, are new: D = 1-4C alkyl (optionally halogenated); X-Y = a bond which may be single or double; P = CLR1R2, CO-CLR1R2, CO-NL1L2 or L3; L = A1-(CR3R4)k-A2-B or A1-Q-A2-B; L1 = CR1R2-B, CR1R2-CR3R4-B or R1; L2 = CR1R2-B or CR1R2-CR3R4-B; L3 = Q-A1-B; k = 0-5; R1-R4 = H, 1-4C alkyl (optionally unsaturated), (CH2)x-OR7, (CH2)x-OC(O)R7, (CH2)x-F, (CH2)x-Cl, (CHF)x-F, (CHCl)x-Cl, (CF2)x-F or (CCl2)x-Cl; x = 0-2; A1, A2 = (CH2)m; m = 0-4; Q = a carbo- or heterocyclic, saturated or wholly or partially unsaturated, mono- or bicyclic 5-10 membered ring system, optionally substituted by R3 and/or R4, provided that Q is not a 7-10 membered monocyclic group; B = X, CHXY or CXYZ; X, Y, Z = a group (CH2)n-V; V = OH, CO2R7, CN, CONR5OR6, CONR5R6, OR5, COR5, OC(O)R7, CONR5OR6, NR5-C(O)R6, SR5, S(O)R5, SO2-NR5R6, NR5R6, NHC(O)R5, NH-SO2-R5, F, Cl, Br or NO2; n = 0-4; R5-R7 = H, 1-4C alkyl, 2-4C alkenyl, aryl or benzyl. |