.beta.-Carboline-derived compounds, lamchart benzodiazepine-receptor ligands, having an inverse agonist and antagonist effect on benzodiazepines, and drugs containing them
US5258385A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Feb 12, 1992 |
| Grant date | Nov 2, 1993 |
| Priority date | — |
| Expiry date | Feb 12, 2012 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D491/14
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The invention relates to novel .beta.-carboline-derived compounds which are benzodiazepine-receptor ligands having an inverse agonist and antagonist effect on benzodiazepines. These compounds are of the formulae: ##STR1## in which: X is O, S, ##STR2## or alternatively, ##STR3## represents the radical --N(R.sub.6)--C(=O)--CH.sub.2 --X, R.sub.1 is a hydroxyl, alkoxy or alkyl radical substituted by a hydroxyl or alkoxy radical, PA0 R.sub.2 is a hydrogen atom or an alkyl, hydroxyl, alkoxy, acyloxy or benzyloxy radical, it being possible for said radicals to be optionally substituted, PA0 R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are chosen from a hydrogen atom or an alkyl radical optionally substituted by a hydroxyl, alkoxy or alkoxycarbonylmethyl radical, as well as the corresponding tetrahydro derivatives of .beta.-carboline and the quaternary ammonium salts or derivatives of these pharmaceutically acceptable compounds.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.