| abstract |
This invention relates to novel substituted tryptamines and related derivatives, as well as pharmaceutical compositions formulated therefrom, the substituted tryptamines having the formula (see above formula) and their acid addition salts where the compounds are basic, wherein: R1 is hydrogen, halogen, C1-4alkyl, C1-4 alkoxy, NR'R", N(R')C(:O)R o, nitro, aryl, aryl-C1-4 alkyl, or aryl-C1-4 alkoxy, and each of R2 and R3 is independently selected from among hydrogen, halogen, C1-4alkyl, C1-4alkoxy, NR'R", N(R')C(:O)R o, nitro, aryl, aryl-C1-4 alkyl, or aryl-C1-4 alkoxy, R o is C1-4alkyl or aryl, and each of R' and R" is independently H or C1-4 alkyl, or R' = R" = CICH2CH2, or NR'R" constitutes a saturated heterocyclic ring containing 3-8 ring members; m is 0-4; t is 0-3; and X is NH, N-C1-4alkyl, O or S; provided that X is not NH when simultaneously (R1)m is 5-methoxy, R2 is H or I and t = 0, and that X is not S when simultaneously R2 is H and m=t=0. These compounds, compositions and their salts can be used in the manufacture of medicaments for interacting with the melatoninergic system. These compounds and conditions can be used for heating several types of medical conditions, such as central nervous system and psychiatric disorders (sleep disorders, epilepsy and other convulsive disorders, anxiety, neurodegenerative diseases), chronobiological-based disorders (jet lag, delayed sleep syndrome, shift-work, seasonal affective disorder), neoplastic conditions, and conditions associated with senescence. |