Indole derivatives

Details Indole derivatives Indole derivatives

C - Chemistry, Metallurgy

07

D

C07D 403/06 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) C07D 401/06 (2006.01)

Patent

CA 2178161

Compounds of the formula Image I wherein n is 0, 1, or 2; X is chlorine, bromine, or iodine; 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-NR,(C=O)NR5R6, -(CH2)m-NR,(C=O)OR9, and -CH=CH(CH2)yR10; R3 is C1 to C6 linear or branched alkyl, 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. A process for forming indoles by transition metal catalyzed cyclization of a dihalogenated intermediate.

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