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US 7,022,724 B2Granted
Cognition enhancing derivatives of isoxazole triazoloindane GABA-A α5 receptor subunit ligands
AssigneeMerck Sharp & Dohme Corp.
InventorsAmanda Louise Boase, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant
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Abstract
The present invention relates to compounds of formula I: in which R1 is a linear group or a five membered heterocycle optionally fused to a phenyl ring, R2 is a 5-membered heterocycle, R3 is chosen from a range of substituents, m is 0–3 and n is 0 or 1; the compounds are generally inverse agonists at GABA-A receptors containing the alpha 5 subunit and so are useful in methods of enhancing cognition in subjects with diminished cognition in diseases such as Alzheimer's Disease.
Claims7
A compound of formula 1:
- in which:
- R1 is hydrogen, halogen, cyano, amino, nitro, hydroxy, aminocarbonyl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6alkoxy, C2-6alkenyloxy, C2alkynyloxy, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aminoC1-6alkyl or C1-6alkylcarbonyl each of which is unsubstituted or substituted by one, two or three halogen atoms;
- R2 is phenyl, which is unsubstituted or substituted with at least one group selected from halogen, cyano, amino, nitro, hydroxy, aminocarbonyl, C1-6alkyl, C26alkenyl, C2-6alkynyl, C1-6alkoxy, C2-6alkenyloxy, C2alkynyloxy, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aminoC1-6alkyl or C1-6alkylcarbonyl each of which is itself unsubstituted or substituted by one, two or three halogen atoms;
- R3 is hydrogen, halogen, cyano, amino, nitro, hydroxy, aminocarbonyl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6alkoxy, C2-6alkenyloxy, C2alkynyloxy, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aminoC1-6alkyl, C1-6alkylcarbonyl or NRcRd, each of which is unsubstituted or substituted by one, two or three halogen atoms;
- Ra and Rb are each independently hydrogen, C1-6alkyl, C1-6alkoxy, C2-6alkenyl, C2-6alkynyl, aminoC1-6alkyl or phenyl;
- Rc and Rd are each independently hydrogen, C1-6alkyl, C1-6alkoxy, C2-6alkenyl or C2-6alkynyl;
- m is 0, 1, 2 or 3;
- and
- n is 0 or 1;
- or a pharmaceutically acceptable salt thereof.
7 more elements
Dependencies are inferred from the claim text.