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US 9,309,262 B2Granted
Thienylindole azepines as serotonin 5-HT2C receptor ligands and uses thereof
AssigneeABT Holding Company
InventorsMichael Robarge, Michelle Zawadski, John Harrington
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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 thienylindole azepines. These compounds are serotonin receptor (5-HT2c) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT2c) is desired (e.g. addiction, anxiety, depression, obesity, and others).
Claims9
A compound of the formula
- where
- R1 is selected from the group consisting of H, alkyl, perhaloalkyl, alkanoyl, C1-8 alkylaryl, and C1-8 alkylheteroaryl;
- R2 and R3 are independently selected from the group consisting of H, halogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, perhalo alkyl, CN, OR8, NR7R8, SR7, OCOR9, CONR7R8, NR7COR9, NR7CO2R9, SO2NR7R8, SO2R9, NR7SO2R9, aryl, heteroaryl, C1-8 alkylaryl, and C1-8 alkylheteroaryl;
- R4 is selected from the group consisting of H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, perhaloalkyl, CONR7R8, CORS, SO2R9, aryl, heteroaryl, C1-8 alkylaryl, and C1-8 alkylheteroaryl;
- R5a and R5b are independently selected from the group consisting of H, C1-8alkyl, OR7, aryl, and heteroaryl;
- or R5a and R5b taken together are —CH2CH2—;
- R6a and R6b are independently selected from the group consisting of H, C1-8alkyl, OR7, aryl, and heteroaryl;
- or R6a and R6b taken together are —CH2CH2—;
- R7 is selected from the group consisting of H, C1-8alkyl, C2-8 alkenyl, C2-8 alkynyl, perhaloalkyl, C1-8 alkyl-O—C1-8 alkyl, aryl, heteroaryl, C1-8 alkyl-O-aryl, C1-8 alkyl-O-heteroaryl, C1-8 alkylaryl, and C1-8 alkylheteroaryl;
- R8 is selected from the group consisting of H, C1-8alkyl, C2-8 alkenyl, C2-8 alkynyl, perhaloalkyl, C1-8 alkyl-O—C1-8 alkyl, aryl, heteroaryl, C1-8 alkyl-O-aryl, C1-8 alkyl-O-heteroaryl, C1-8 alkylaryl, and C1-8 alkylheteroaryl;
- and
- R9 is selected from the group consisting of C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, perhaloalkyl, C1-8 alkyl-O—C1-8 alkyl, aryl, heteroaryl, C1-8 alkyl-O-aryl, C1-8 alkyl-O-heteroaryl, C1-8 alkylaryl, and C1-8 alkylheteroaryl, or a pharmaceutically acceptable salt thereof.
9 more elements
Dependencies are inferred from the claim text.