5-HT 3 receptor agonists, novel thiazole derivatives and intermediates thereof (5-HT 3 receptor agonist, novel thiazole derivative, and intermediate therefor)

摘要

The present invention relates to 5-HT (5-HT) derivatives containing a thiazole derivative of formula (1)₃Receptor agonists, 5-HT₃Certain compounds useful as receptor agonists and certain thioamide derivatives useful as intermediates thereto include:;(1) a benzene ring or (2) a group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, which may be substituted by at least one substituent selected from the group consisting of a halogen atom, a lower alkyl group and a lower alkoxyl group Or a 5-membered or 6-membered unsaturated heterocyclic ring containing 1 or 2 hetero atoms selected from L_OneAnd L₂Is either a single bond and the other is absent, an alkylene group having 1 to 4 carbon atoms or an alkenylene group having 2 to 5 carbon atoms, and R is And And L³Is a lower alkylene group, L⁴Is a single bond or lower alkylene group, R^OneAnd R²Are the same or different and each is a hydrogen atom, a lower alkyl group or an amino-protecting group, R³Is a hydrogen atom, a lower alkyl group, an oxo group or a protected or unprotected amino group, R⁴(1) the number of ring-forming atoms is in the range of from 4 to 20, preferably from 1 to 4, and R 2 is hydrogen or a lower alkyl group, (2) one unsaturated bond-containing ring-forming atom 4 to 16 is a nitrogen-containing heterocyclic ring, and the ring D is a saturated carbon ring having 4 to 8 ring-forming atoms , With the proviso that the nitrogen atom in the group R may be a quaternary ammonium salt carrying a substituent.