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US 8,410,104 B2Granted
Pyridazines
AssigneesHoffmann-La Roche Inc., Roche Palo Alto LLC
InventorsMatthew C. Lucas, Andrew Thomas
Life of this patent
Estimating the term…
Abstract
The present invention is concerned with isoxazole-pyridazines of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
Claims13
A compound of formula I,
- wherein
- R1 is lower alkyl or lower alkyl substituted by 1-5 substituents individually selected from amino, halogen, (lower alkyl, lower alkyl)N— and (lower alkyl, H)N—;
- R2 is H, lower alkyl or lower alkyl substituted by 1-5 substituents individually selected from amino, halogen, halogen-lower alkoxy, hydroxy, lower alkoxy, (lower alkyl, lower alkyl)N—, (lower alkyl, H)N—, nitro and lower alkyl-S(O)2—;
- R3 is H, lower alkyl or lower alkyl substituted by 1-5 substituents individually selected from amino, halogen, halogen-lower alkoxy, hydroxy, lower alkoxy, (lower alkyl, lower alkyl)N—, (lower alkyl, H)N—, nitro and lower alkyl-S(O)2—;
- R4 is selected from the group consisting of
- i) H,
- ii) lower alkyl,
- iii) lower alkyl substituted by 1-5 substituents individually selected from amino, halogen, halogen-lower alkoxy, hydroxy, lower alkoxy, (lower alkyl, lower alkyl)N—, (lower alkyl, H)N—, nitro and lower alkyl-S(O)2—;
- iv) heterocyclyl, and
- v) heterocyclyl substituted by 1-4 substituents individually selected from amino, halogen, halogen-lower alkoxy, halogen-lower alkyl, hydroxy, hydroxy-lower alkyl, lower alkoxy, lower alkoxy-lower alkyl, lower alkyl, (lower alkyl, lower alkyl)N—, (lower alkyl, H)N—, nitro and lower alkyl-S(O)2—;
- or a pharmaceutically acceptable salt or ester thereof.
8 more elements
A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula I
- wherein
- R1 is lower alkyl or lower alkyl substituted by 1-5 substituents individually selected from amino, halogen, (lower alkyl, lower alkyl)N— and (lower alkyl, H)N—;
- R2 is H, lower alkyl or lower alkyl substituted by 1-5 substituents individually selected from amino, halogen, halogen-lower alkoxy, hydroxy, lower alkoxy, (lower alkyl, lower alkyl)N—, (lower alkyl, H)N—, nitro and lower alkyl-S(O)2—;
- R3 is H, lower alkyl or lower alkyl substituted by 1-5 substituents individually selected from amino, halogen, halogen-lower alkoxy, hydroxy, lower alkoxy, (lower alkyl, lower alkyl)N—, (lower alkyl, H)N—, nitro and lower alkyl-S(O)2—;
- R4 is selected from the group consisting of
- i) H,
- ii) lower alkyl,
- iii) lower alkyl substituted by 1-5 substituents individually selected from amino, halogen, halogen-lower alkoxy, hydroxy, lower alkoxy, (lower alkyl, lower alkyl)N—, (lower alkyl, H)N—, nitro and lower alkyl-S(O)2—;
- iv) heterocyclyl, and
- v) heterocyclyl substituted by 1-4 substituents individually selected from amino, halogen, halogen-lower alkoxy, halogen-lower alkyl, hydroxy, hydroxy-lower alkyl, lower alkoxy, lower alkoxy-lower alkyl, lower alkyl, (lower alkyl, lower alkyl)N—, (lower alkyl, H)N—, nitro and lower alkyl-S(O)2—;
- or a pharmaceutically acceptable salt or ester thereof and a pharmaceutically acceptable carrier.
8 more elements
Dependencies are inferred from the claim text.