New 1-hydroxy-3-oxo-propen-1-yl-hexahydro-pyrrolo-indole compounds are 5-hydroxy tryptamine-2 receptor antagonists useful to treat e.g. depression, anxiety, Parkinson's disease, Alzheimer's diseases, cancer, skin diseases and anxiety

摘要

1-(1-Hydroxy-3-oxo-propen-1-yl)-1,2,3,3a,8,8a-hexahydro-pyrrolo[2,3-b]indole compounds (I) and their mixtures, addition salts, isomers, enantiomers or diastereoisomers are new. 1-(1-Hydroxy-3-oxo-propen-1-yl)-1,2,3,3a,8,8a-hexahydro-pyrrolo[2,3-b]indole compounds of formula (I) and their mixtures, addition salts, isomers, enantiomers or diastereoisomers are new. R1 : H, 1-6C alkyl or 1-6C alkoxy; R2 : H, 1-6C alkyl or aryl; and R3 : H, 1-6C alkyl, 3-12C cycloalkyl or (hetero)aryl optionally substituted with halo, 1-6C alkyl or 1-6C alkoxy. R18 : 1-12C alkyl, phenyl or phenyl (1-6C alkyl), where the phenyl group is optionally replaced by 1-6C alkoxy, halo or secondary amine; and R16, R17 : absent (when dotted line is present) or H (when dotted line is absent). Independent claims are included for: (1) the preparations of (I); and (2) combining (I) and a 5HT2 receptor antagonist compounds of formula (X) or (Xb). [Image] [Image] ACTIVITY : Hypnotic; Neuroprotective; Antidepressant; Tranquilizer; Antiparkinsonian; Nootropic; Muscle relaxant; Sedative; Analgesic; Neuroleptic; Anticonvulsant; Cytostatic; Dermatological; Antipsoriatic; Antiseborrheic; Ophthalmological; Gynecological. MECHANISM OF ACTION : 5-Hydroxy tryptamine-2 (5HT3) receptor antagonist.