New 1,2,3,4,6,7,12,12a-octahydro-pyrazino(1',2':1,6)pyrido(3,4-b)indole compounds are 5-hydroxy tryptamine-2 receptor antagonist useful to treat e.g. depression, anxiety, Parkinson's disease, Alzheimer's disease and cancer

摘要

1,2,3,4,6,7,12,12a-Octahydro-pyrazino[1',2':1,6]pyrido[3,4-b]indole compounds (I) and their mixtures, addition salts, isomers, enantiomers or diastereoisomers are new. 1,2,3,4,6,7,12,12a-Octahydro-pyrazino[1',2':1,6]pyrido[3,4-b]indole compounds of formula (I) and their mixtures, addition salts, isomers, enantiomers or diastereoisomers are new. X : (=O) or (=CH2); R1 : 1-6C alkyl, 2-6C alkenyl, ether-oxide group of formula (-(CH2)nOR5); R5 : 1-4C alkyl, N,N-disubstituted aminoalkyl group of formula (-(CH2)nN(R5)2), ether-oxide, 1-4C aralkyl, preferably benzyl, 3-6C cycloalkyl or indolyl-3-ethyl (optionally methoxylated and preferably the indolyl group positioned at 5); R2 : H, 1-6C alkyl or aryl, preferably phenyl (optionally substituted by 1-4C alkyl, 1-4C alkoxy or halo (preferably Cl)); R3 : H or 1-4C alkyl; R4 : H, OH or 1-4C alkoxy; and n : 1-4. Independent claims are included for: (1) the preparation of (I); (2) a combination of (I) and 5-hydroxy tryptamine-2 (5HT2) receptor antagonist compounds of formulae (VIII) or (VIIIa); and (3) a pharmaceutical composition comprising (I) or the combination and an excipient. R18 : 1-12C alkyl, phenyl or phenyl(1-6C alkyl), where the phenyl is optionally substituted by 1-6C alkoxy, halo or secondary amine; and R16, R17 : absent (when dotted line is present) or H (when dotted line is absent). [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 receptor antagonist.