| abstract |
Compounds of formula (I), wherein n is 0, 1 or 2; R1 is hydrogen; R2 is selected from hydrogen, halogen, cyano, OR4, -(CH2)m-(C=O)NR5R6, -(CH2)m-SO2NR5R6, -(CH2)m-NR7(C=O)R8, -(CH2)m-NR7SO2R8, -(CH2)m-S(O)xR8, -(CH2)m-NR7(C=O)NR5R6, -(CH2)m-NR7(C=O)OR9, and -CH=CH(CH2)yR10; R3 is selected from hydrogen and C1 to C6 linear or branched alkyl; R4 is selected from hydrogen, C1 to C6 alkyl, and aryl; R5 and R6 are independently selected from hydrogen, C1 to C6 alkyl, aryl, and C1 to C3 alkyl-aryl or R5 and R6 taken together to form a 4, 5, or 6 membered ring; R7 and R8 are independently selected from hydrogen, C1 to C6 alkyl, aryl, and C1 to C3 alkyl-aryl; R9 is selected from hydrogen, C1 to C6 alkyl, aryl, and C1 to C3 alkyl-aryl R10 is selected from -(C=O)NR5R6 and -SO2NR5R6, wherein R5 and R6 are defined as above, and -NR7(C=O)R8, -NR7SO2R8, -NR7(C=O)NR5R6, -S(O)xR8 and -NR7(C=O)OR9, wherein R7, R8, and R9 are as defined above; y is 0, 1, or 2; x is 1 or 2; m is 0, 1, 2, or 3; and the above aryl groups and the aryl moieties of the above alkylaryl groups are independently selected from phenyl and substituted phenyl, wherein said substituted phenyl may be substituted with one to three groups selected from C1 to C4 alkyl, halogen, hydroxy, cyano, carboxamido, nitro, and C1 to C4 alkoxy and the pharmaceutically acceptable salts thereof are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators. |