abstract |
PCT No. PCT/EP93/00799 Sec. 371 Date Sep. 21, 1994 Sec. 102(e) Date Sep. 21, 1994 PCT Filed Mar. 26, 1993 PCT Pub. No. WO93/20071 PCT Pub. Date Oct. 14, 1993Substituted phenylcarbamates and ureas of formula (I) <IMAGE> (I) wherein R1 represents a hydrogen or a halogen atom, or a C1-6alkyl, C1-6alkoxy or hydroxy group; R2 represents an oxadiazole or thiadiazole ring substituted by a group selected from C1-6alkyl, C3-7cycloalkyl, -CH2C2-5alkenyl, -CH2C2-5alkynyl, phenyl or benzyl; X represents NH or an oxygen atom; m represents zero, 1 or 2; R3 represents C1-6alkyl, benzyl, -(CH2)nR4 or <IMAGE> R4 represents a group selected from cyano, hydroxyl, C1-6alkoxy, phenoxy, C(O)C1-6alkyl, C(O)C6H5, -CONR6R7, -NR6COR7, -SO2NR6R7 or -NR6SO2R7 (wherein each of R6 and R7 independently represent a hydrogen atom, a C1-6alkyl or phenyl group); n represents 2 or 3; R5 represents COR8 or SO2R8 (wherein R8 represents a hydrogen atom, a C1-6alkyl or phenyl group); and quaternary ammonium derivatives, piperidine N-oxides and pharmaceutically acceptable salts and solvates thereof; which compounds are potent and specific antagonists of 5-hydroxytryptamine (5HT; serotonin). |