Aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives
AssigneeHoffmann-La Roche Inc.
InventorsBernd Buettelmann, Jiaqiang Dong, Bo Han, Henner Knust, Andrew Thomas
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Abstract
The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives of formula wherein: R1, R2, and R3 are as defined herein and pharmaceutically acceptable acid addition salts thereof. These compounds have high affinity and selectivity for GABA A α5 receptor binding sites. The invention also relates to methods for enhancing cognition and treating cognitive disorders like Alzheimer's disease.
Claims14
An aryl-isoxazol-4-yl-imidazo[1,5-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 lower alkyl;
- R2 is hydrogen, lower alkyl, or —(CO)—Ra;
- R3 is hydrogen, halogen, cyano, lower alkyl, or —(CO)—Ra;
- Ra is hydroxy, lower alkoxy, NR′R″, wherein R′ and R″ are each independently hydrogen, cycloalkyl, 5 or 6-membered heterocycloalkyl or is lower alkyl which is optionally substituted by cycloalkyl, cyano, 5 or 6-membered heterocycloalkyl or by 5 or 6-membered heteroaryl;
- and pharmaceutically acceptable acid addition salts thereof.
A pharmaceutical composition comprising a therapeutically effective amount of a compound 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 lower alkyl;
- R2 is hydrogen, lower alkyl, or —(CO)—Ra;
- R3 is hydrogen, halogen, cyano, lower alkyl, or —(CO)—Ra;
- Ra is hydroxy, lower alkoxy, NR′R″, wherein R′ and R″ are each independently hydrogen, cycloalkyl, 5 or 6-membered heterocycloalkyl or is lower alkyl which is optionally substituted by cycloalkyl, cyano, 5 or 6-membered heterocycloalkyl or by 5 or 6-membered heteroaryl;
- and pharmaceutically acceptable acid addition salts thereof.
Dependencies are inferred from the claim text.