4-O and 5-aminomethylation of synthetic capsaicin derivatives, a new discovery of capsaicin antagonist
US5840720A · kind A · utility
Assignee
Inventor
Key dates
| Filing date | Oct 23, 1995 |
| Grant date | Nov 24, 1998 |
| Priority date | — |
| Expiry date | Oct 23, 2015 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D273/00
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
A series of 4-O & 5-aminomethylation of synthetic capsaicin derivatives selectively reveal antagonist activity on capsaicin-sensitive sensory neurons, and inhibit its innervating atrium, airway, and ileum smooth muscles in vitro. The compound of this invention has the following formula ##STR1## wherein R is a member selected from the group consisting of ##STR2## wherein R.sub.1 is a member selected from the group consisting of C.sub.1-12 alkyl, C.sub.1-12 alkenyl, C.sub.1-12 alkylene, and C.sub.1-12 alkenylene, and wherein R.sub.2 is a member selected from the group consisting of H, C.sub.1-3 alkylene-NR.sub.1 R.sub.1, and C.sub.1-6 alkenylene-NR.sub.1 R.sub.1.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.