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US 2012/0252859 A1Published application
Tricyclic Indeno-Pyrrole Derivatives as Serotonin Receptor Modulators
AssigneeAthersys, Inc.
InventorsYoussef L. Bennani, Bayard Huck, Michael J. Robarge
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Abstract
The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are tricyclic indeno-pyrrole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).
Claims3
A compound of the formula
- where
- R1 is selected from the group consisting of H, halogen, C1-10alkyl, C2-10 alkenyl, C2-10 alkynyl, perhaloalkyl, CN, N(R6)2, SR6, CON(R6)2, NR6COR7, NR6CO2R7, SO2N(R6)2, NR6SO2R7, aryl, heteroaryl, C1-10alkylaryl, and C1-10alkylheteroaryl;
- R2 is selected from the group consisting of halogen, C1-10alkyl, C2-10 alkenyl, C2-10 alkynyl, perhaloalkyl, CN, OR6, N(R6)2, SR6, OCOR7, CON(R6)2, NR6COR7, NR6CO2R7, SO2N(R6)2, NR6SO2R7, aryl, heteroaryl, C1-10, alkylaryl, and C1-10alkylheteroaryl;
- and R2 may also be H when R5 is C1-10 alkyl or R4 is H;
- R3 is selected from the group consisting of halogen, C1-10alkyl, C2-10 alkenyl, C2-10 alkynyl, perhaloalkyl, CN, OR6, N(R6)2, SR6, OCOR7, CON(R6)2, NR6COR7, NR6CO2R7, SO2N(R6)2, NR6SO2R7, aryl, heteroaryl, C1-10 alkylaryl, and C1-10alkylheteroaryl;
- R4 is selected from the group consisting of H, halogen, C1-10alkyl, C2-10 alkenyl, C2-10 alkynyl, perhaloalkyl, CN, N(R6)2, SR6, CON(R6)2, NR6COR7, NR6CO2R7, SO2N(R6)2, NR6SO2R7, aryl, heteroaryl, C1-10, alkylaryl, and C1-10alkylheteroaryl;
- R5 is selected from the group consisting of H, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, perhaloalkyl, CN, OR6, N(R6)2, SR6, OCOR7, CON(R6)2, NR6COR7, NR6CO2R7, NR6SO2R7, aryl, heteroaryl, C1-10alkylaryl, and C1-10 alkylheteroaryl;
- R5a is H;
- R6 is selected from the group consisting of H, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, perhaloalkyl, C1-10 alkyl-O—C1-10 alkyl, aryl, heteroaryl, C1-10alkyl-0-aryl, C1-10 alkyl-O-heteroaryl, C1-10 alkylaryl, and C1-10 alkylheteroaryl;
- and
- R7 is selected from the group consisting of C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, perhaloalkyl, C1-10alkyl-O—C1-10 alkyl, aryl, heteroaryl, C1-10alkyl-O-aryl, C1-10alkyl-O-heteroaryl, C1-10 alkylaryl, and C1-10 alkylheteroaryl;
- provided that if R1, R2, R5 and R5a are H, then R3 and/or R4 must be H,
- or a pharmaceutically acceptable salt thereof.
10 more elements
Dependencies are inferred from the claim text.