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US 2007/0179178 A1Published application
Aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives
AssigneeHoffmann-La Roche Inc.
InventorsBernd Buettelmann, Bo Han, Henner Knust, Andrew Thomas
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Abstract
The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives of formula I: wherein R1 to R5 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. This class of compounds has high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
Claims16
An aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivative of formula I
- wherein
- R1 is hydrogen, halogen, hydroxy, lower alkyl, benzyloxy or —O—(CH2)—(CO)-5 or 6 membered heteroaryl optionally substituted by aryl or by lower alkyl;
- R2 is hydrogen, halogen, lower alkyl, lower alkynyl, amino, —NHC(O)—Ra or —(CO)—Ra;
- R3 is hydrogen, halogen, cyano, lower alkyl, lower alkynyl, amino, —NHC(O)—Ra, —(CO)—Ra, -5 or 6-membered heterocycloalkyl in the 1-position, optionally substituted by ═O or is a -5 or 6-membered heteroaryl in the 1-position;
- R4 is hydrogen or -5 or 6-membered heteroaryl;
- R5 is lower alkyl or cycloalkyl;
- Ra is lower alkoxy or NR′R″, wherein R′ and R″ are each independently hydrogen, lower alkyl optionally substituted by hydroxy, lower alkynyl, —(CH2)n-cycloalkyl, —(CH2)n-5 or 6-membered heterocycloalkyl or —(CH2)n-5 or 6-membered heteroaryl;
- and
- n is 0 to 3;
- or a pharmaceutically acceptable acid addition salt thereof.
7 more elements
Dependencies are inferred from the claim text.