TRYPTAMINE ANALOGUES AS 5-HT1-LIKE AGONISTS

摘要

A compound of structure (I), in which R1 is an optionally substituted 6- to 10-membered aryl or heteroaryl ring; suitably R1 is an optionally substituted 6- or 10-membered aryl ring such as phenyl or naphthyl; suitably R1 is an optionally substituted 6- to 10-membered heteroaryl ring containing from 1 to 4 nitrogen atoms. R2 is hydrogen, halogen, C¿1-4? alkyl, CN, NO2 or CF3; R?3¿ is hydrogen, halogen, C¿1-4? alkyl, CN, NO2 or CF3; R?3 is C(R4)(R5)CH¿2NR6R7, -CH = NNHC(NH)NH¿2? or a; R?4 and R5¿ are independently hydrogen or C¿1-4? alkyl; R?6 and R7¿ are the same or different and are each hydrogen or C¿1-4? alkyl or together with the nitrogen atom to which they are attached form a ring; R?8¿ is hydrogen, C¿1-4? alkyl, or C3-6 alkenyl; R?a¿ is hydrogen and Rb is hydrogen or hydroxy, or R?a and Rb¿ together represent a bond; and q and m are independently 1 or 2; and pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds are 5-HT¿1?-like agonists (or partial agonists) and as such are expected to have utility in medicine in the treatment and/or prophylaxis of migraine, and other conditions associated with cephalic pain, such as cluster headache, headache associated with vascular disorders and other neuralgia. They are also expected to have utility in the treatment or prophylaxis of portal hypertension.