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US 7,402,687 B2Granted
Dihydrobenzofuran derivatives and uses thereof
AssigneeWyeth
InventorsGary Paul Stack, Jianyao Wang, William Demaio, Ronald Jordan, John Chuck Lem Erve, Rasmy Elsayed Talaat, Matthew John Hoffmann
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Abstract
Compounds of formula I are described herein which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. or pharmaceutically acceptable salts thereof, wherein each of R1, R2, R3, R4, Rx, Ry, and n are as defined herein. Such compounds, and compositions thereof, are useful for treating a variety of central nervous system disorders such as schizophrenia.
Claims8
A compound of formula VII:
- or a pharmaceutically acceptable salt thereof, wherein:
- each independently represents a single or double bond, provided that both groups do not simultaneously represent a double bond;
- R1 is hydrogen, —C(O)R, -Glu, —C(O)Glu, or —C(O)OGlu;
- R is hydrogen or lower alkyl;
- R2 is hydrogen, —OH, —OS(O)2OH, or —OGlu;
- R3 is hydrogen, halogen, methyl, methoxy, —OH, —OS(O)2OH, or —OGlu;
- R4 is hydrogen, —OH, —OS(O)2OH, or —OGlu;
- Ra and Rb are each hydrogen or are taken together to form an oxo moiety;
- Rc and Rd are each hydrogen or are taken together to form an oxo moiety;
- each Rx is independently halogen or lower alkyl;
- each R5 is independently hydrogen, —OH, —OS(O)2OH, or —OGlu;
- each Glu is a glucuronyl moiety;
- and
- n is one or two;
- provided that at least one of R1, R2, R4, and R5 contains a glucuronyl moiety.
12 more elements
Dependencies are inferred from the claim text.