Back to results
US 5,508,284 AGranted
Tetrahydro-beta-carbolines
AssigneeEli Lilly and Company
InventorsJames E. Audia, James J. Droste, Deborah A. Evrard, Pawel Fludzinski, Gwyn L. Murdoch, David L. Nelson
Life of this patent
Estimating the term…
Abstract
The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided 3-ethanamine and 3-ethanamine related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds.
Claims9
A compound of the formula (I) ##STR125## wherein:
- R.sub.1 is hydrogen or C.sub.1 -C.sub.3 alkyl;
- R.sub.2 is hydrogen or C.sub.1 -C.sub.6 alkyl;
- R.sub.3 is hydrogen or C.sub.1 -C.sub.3 alkyl;
- R.sub.4 is C.sub.5 -C.sub.8 cycloalkyl, substituted C.sub.5 -C.sub.8 cycloalkyl, C.sub.5 -C.sub.8 cycloalkenyl, substituted C.sub.5 -C.sub.8 cycloalkenyl;
- A is selected from the group consisting of ##STR126## wherein R.sub.6 and R.sub.7 are, independently, hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, halo, halo(C.sub.1 -C.sub.6)alkyl, halo (C.sub.2 -C.sub.6)alkenyl, COR.sub.5, C.sub.1 -C.sub.10 alkanoyl, CO.sub.2 R.sub.5, (C.sub.1 -C.sub.6 alkyl).sub.m amino, NO.sub.2, --SR.sub.5, or OR.sub.5 ;
- each R.sub.5 is independently hydrogen or C.sub.1 -C.sub.4 alkyl;
- R.sub.5' is C.sub.1 -C.sub.4 alkyl;
- R.sub.8 is selected from the group consisting of an R.sub.6 group, substituted C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl-(C.sub.1 -C.sub.3)alkyl, C.sub.5 -C.sub.8 cycloalkenyl, substituted C.sub.5 -C.sub.8 cycloalkenyl, C.sub.5 -C.sub.8 cycloalkenyl-(C.sub.1 -C.sub.3)alkyl, C.sub.7 -C.sub.16 arylalkyl;
- or
- m is 1 or 2;
- provided that when A is of formula IV;
- R.sub.6 and R.sub.7 together with the carbon atoms of group A form a 5- to 8-member carbon ring;
- or
- a pharmaceutically acceptable salt or solvate thereof.
11 more elements
Dependencies are inferred from the claim text.