5-arylindole derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 403/14 (2006.01) A61K 31/415 (2006.01) A61K 31/445 (2006.01) A61K 31/495 (2006.01) A61K 31/55 (2006.01) C07D 401/14 (2006.01) C07D 403/04 (2006.01) C07D 471/04 (2006.01) C07D 487/04 (2006.01)

Patent

CA 2148380

Compounds of formula (I), wherein R1 is (a), (b), (c) or (d); n is 0, l or 2; A, B, C and D are each independently nitrogen or carbon; R2, R3, R4 and R5 are each in- dependently hydrogen, C1 to C6 alkyl, aryl; C1 to C3 alkyl-aryl, halogen (e.g: fluo- rine, chlorine, bromine or iodine); cyano; nitro, -(CH2) m NR14R15, -(CH2) m OR9, -SR9, -SO2NR14R15, -(CH2) m NR14SO2R15; -(CH2) m NR14CO2R9, -(CH2) m NR14COR9, -(CH2) m NR14CONHR9, -CONR14R15, or-CO2R9; R2 and R3, R3 and R4, or R4 and R5 may be taken together to form a five- to seven- membered alkyl ring; a six-membered aryl ring; a five- to seven-membered heteroalkyl ring having l heteroatom of N, O, or S, or a five- to six-membered heteroaryl ring,having 1 or 2 heteroatoms of N, O, or S and the pharmaceutically acceptable salts thereof. These compounds are useful in treating migraine and other disorders. These com- pounds are useful psychotherapeutics, and are potent serotonin (S-HT1) agonists and benzodiazepine agonists and antagonists aid may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, mi- graine, pain and chronic paroxysmal hemicrania and headache associated with vas- cular disorders; and other disorders arising from deficient serotonergic neurotrans- mission. The compounds can also be used as centrally acting antihypertensives and vosodilators.

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