Indole derivatives
AssigneeHoffmann-La Roche Inc.
InventorMichael Bos
Life of this patent
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Abstract
The invention releates to indole derivatives of the formula ##STR1## wherein R.sup.1 to R.sup.4 are, independently, hydrogen, halogen, lower-alkyl, cycloalkyl or trifluoromethyl, R.sup.5 and R.sup.6 are, independently, hydrogen, halogen, lower-alkyl, cycloalkyl, trifluoromethyl, hydroxy or lower-alkoxy and R.sup.7 is hydrogen or lower-alkyl, and pharmaceutically acceptable acid addition salts thereof. The compounds of formula I bind to serotonin receptors and are therefore useful in the treatment and/or prevention of central nervous system disorders, such as depression.
Claims7
A compound of the formula ##STR13## wherein R.sup.1 to R.sup.4 are, independently, hydrogen, halogen, lower-alkyl, cycloalkyl or trifluoromethyl, R.sup.5 and R.sup.6 are, independently, hydrogen, halogen, lower-alkyl, cycloalkyl, trifluoromethyl, hydroxy or lower-alkoxy and R.sup.7 is lower-alkyl,
- or a pharmaceutically acceptable acid addition salt thereof.
A compound selected from the group consisting of
- (RS)-2-(5-Chloro-indol-1-yl)-1-methyl-ethylamine,
- (RS)-2-(5-fluoro-indol-1-yl)-1-methyl-ethylamine,
- (RS)-2-(6-chloro-5-fluoro-indol-1-yl)-1-methyl-ethylamine,
- (R)-2-(5-fluoro-indol-1-yl)-1-methyl-ethylamine,
- (S)-2-(6-chloro-5-fluoro-indol-1-yl)-1-methyl-ethylamine,
- (R)-2-(6-chloro-5-fluoro-indol-1-yl)-1-methyl-ethylamine,
- (RS)-2-(4-methyl-indol-1-yl)-1-methyl-ethylamine,
- (RS)-2-(5-bromo-indol-1-yl)-1-methyl-ethylamine,
- (RS)-2-(6-fluoro-indol-1-yl)-1-methyl-ethylamine,
- (S)-2-(5,6-difluoro-indol-1-yl)-1-methyl-ethylamine,
- (R)-2-(5,6-difluoro-indol-1-yl)-1-methyl-ethylamine,
- (S)-2-(5-fluoro-4-trifluoromethyl-indol-1-yl)-1-methyl-ethylamine,
- (S)-2-(5-fluoro-6-trifluoromethyl-indol-1-yl)-1-methyl-ethylamine,
- (S)-2-(4-chloro-5-fluoro-indol-1-yl)-1-methyl-ethylamine, and
- (R)-2-(4-chloro-5-fluoro-indol-1-yl)- i-methyl-ethylamine.
A pharmaceutical composition comprising an effective amount of a compound of the formula ##STR14## wherein R.sup.1 to R.sup.4 are, independently, hydrogen, halogen, lower-alkyl, cycloalkyl or trifluoromethyl, R.sup.5 and R.sup.6 are, independently, hydrogen, halogen, lower-alkyl, cycloalkyl, trifluoromethyl, hydroxy or lower-alkoxy and R.sup.7 is lower-alkyl,
- or a pharmaceutically acceptable acid addition salt thereof and an inert carrier.
A method for blocking serotonin receptors in a host requiring such treatment which comprises administering an effective amount of a compound selected from the group consisting of ##STR15## wherein R.sup.1 to R.sup.4 are, independently, hydrogen, halogen, lower-alkyl, cycloalkyl or trifluoromethyl, R.sup.5 and R.sup.6 are, independently, hydrogen, halogen, lower-alkyl, cycloalkyl, trifluoromethyl, hydroxy or lower-alkoxy and R.sup.7 is lower-alkyl,
- or a pharmaceutically acceptable acid addition salt thereof.
Dependencies are inferred from the claim text.