Piperazine, piperidine and tetrahydropyridine derivatives
US5977116A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | May 12, 1998 |
| Grant date | Nov 2, 1999 |
| Priority date | — |
| Expiry date | May 12, 2018 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D249/08
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
A class of N-substituted piperazine, piperidine and tetrahydropyridine derivatives, linked by a fluoro-substituted alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at the 4-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D recptor agonists.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.