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US 7,608,626 B2Granted
Substituted indolizines and derivatives as CNS agents
AssigneeWyeth
InventorsAnnmarie Louise Sabb, Robert Lewis Vogel
Life of this patent
Estimating the term…
Abstract
Compounds of formula 1 or pharmaceutically acceptable salts thereof are provided: which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
Claims21
A compound of formula (1):
- or a pharmaceutically acceptable salt thereof;
- wherein
- R is H, C1-C6 alkyl, C6-C10 aryl, 5 to 10 membered heteroaryl having 1 to 3 heteroatoms each independently selected from nitrogen, oxygen and sulfur, or —C(O)R′, wherein R′ is C1-C6 alkyl, C6-C10 aryl, or 5 to 10 membered heteroaryl having 1 to 3 heteroatoms each independently selected from nitrogen, oxygen and sulfur;
- R1 is H, C1-C6 alkyl, C3-C8 cycloalkyl, or C1-C6 fluoroalkyl;
- R2 is C1-C6 alkyl, C3-C8 cycloalkyl, C1-C6 fluoroalkyl, C6-C10 aryl, or 5 to 10 membered heteroaryl having 1 to 3 heteroatoms each independently selected from nitrogen, oxygen and sulfur;
- R3 is C3-C6 alkyl, C1-C6 alkyl-C3-C8 cycloalkyl, or C1-C6 fluoroalkyl;
- or alternatively R2 and R3 can be taken together with the carbon atoms to which they are attached to form a ring of 5-8 carbon atoms;
- R4, R5, R6, and R7 are each independently H, halogen, cyano, hydroxyl, carboxyl, C1-C6 alkyl, C1-C6 fluoroalkyl, C1-C6 alkoxy, C1-C6 fluoroalkoxy, C6-C10 aryl, C6-C10 aryloxy, 5 to 10 membered heteroaryl having 1 to 3 heteroatoms each independently selected from nitrogen, oxygen and sulfur, C2-C8 alkenyl, C2-C6 alkanoyl, C2-C6 alkanoyloxy, C2-C6 alkoxycarbonyl, carboxamido, C2-C6 alkanamido, C1-C6 alkanesulfonamido, amino, C1-C6 monoalkylamino, dialkylamino of 1 to 6 carbon atoms per alkyl moiety, C3-C8 cycloalkyl, or a 3 to 8 membered heterocycloalkyl having 1 to 3 heteroatoms each independently selected from nitrogen, oxygen and sulfur;
- R8 is H, C1-C6 alkyl, C3-C8 cycloalkyl, or C6-C10 aryl;
- wherein any cycloalkyl or heterocycloalkyl group is saturated or partially saturated, and any aryl, heteroaryl, cycloalkyl, or heterocycloalkyl group may optionally be substituted with 1 to 5 substituents independently selected from halogen, hydroxyl, C1-C6 alkyl, C1-C6 fluoroalkyl, C1-C6 alkoxy, and C1-C6 fluoroalkoxy.
7 more elements
A compound which is 2-(2-phenylindolizin-1-yl)ethylamine or 2-(2-ethylindolizin-1yl)ethylamine.
Dependencies are inferred from the claim text.