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US 7,582,667 B2Granted
Dihydrospiro[dibenzo[a,d][7]annulene-5,4′-imidazol] compounds for the inhibition of beta-secretase
AssigneeWyeth
InventorsDominick Anthony Quagliato, Patrick Michael Andrae, Yi Fan
Life of this patent
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Abstract
The present invention provides a 10,11-dihydrospiro[dibenzo[a,d][7]annulene -5,4′-imidazol]-5′(1′H)-one compound of formula I Also provided are methods and compositions for the inhibition of β-secretase (BACE) and the treatment of β-amyloid deposits and neurofibrillary tangles.
Claims11
A compound of formula I
- wherein
- X is CH2;
- Y is CH2;
- R1 and R2 are each independently H, or an optionally substituted alkyl group;
- R3 is H or an alky group optionally substituted;
- R4 and R5 are each independently H, halogen, OR11, or an alkyl, alkenyl, or alkynyl, group optionally substituted;
- R6 and R7 are each independently H, halogen, CN, OR25, NR26R27 or an alkyl, alkenyl, alkynyl cycloalkyl, cycloheteroalkyl, aryl or heteroaryl group each optionally substituted;
- each R11 is independently H or an alkyl, haloalkyl, alkenyl, or alkynyl group each optionally substituted;
- R12, R13, and R25 are each independently H or an alkyl, haloalkyl, alkenyl, alkynyl cycloalkyl or aryl group each optionally substituted;
- R26 and R27 are each independently H, OR11, COR12, CO2R13 or an alkyl, alkenyl, alkynyl cycloalkyl, cycloheteroalkyl, aryl or heteroaryl group each optionally substituted or R26 and R27 may be taken together with the atom to which they are attached to form an optionally substituted 5- to 7-membered ring optionally interrupted by an additional heteroatom selected from O, N or S;
- or
- a tautomer thereof, a stereoisomer thereof or a pharmaceutically acceptable salt thereof.
9 more elements
A pharmaceutical composition which comprises a pharmaceutically acceptable carrier and an effective amount of a compound of formula 1
- wherein
- X is CH2;
- Y is CH2;
- R1 and R2 are each independently H, or an optionally substituted alkyl group;
- R3 is H or an alkyl group optionally substituted;
- R4 and R5 are each independently H, halogen, OR11 or an alkyl, alkenyl, or alkynyl, group optionally substituted;
- R6 and R7 are each independently H, halogen, CN, OR25, NR26R27 or an alkyl, alkenyl, alkynyl cycloalkyl, cycloheteroalkyl, aryl or heteroaryl group each optionally substituted;
- each R11 is independently H or an alkyl, haloalkyl, alkenyl or alkynyl group each optionally substituted;
- R12, R13, and R25 are each independently H or an alkyl, haloalkyl, alkenyl, alkynyl cycloalkyl or aryl group each optionally substituted;
- R26 and R27 are each independently H, OR11, COR12, CO2R13 or an alkyl, alkenyl, alkynyl cycloalkyl, cycloheteroalkyl, aryl or heteroaryl group each optionally substituted or R26 and R27 may be taken together with the atom to which they are attached to form an optionally substituted 5- to 7-membered ring optionally interrupted by an additional heteroatom selected from O, N or S;
- or
- a tautomer thereof, a stereoisomer thereof or a pharmaceutically acceptable salt thereof.
9 more elements
Dependencies are inferred from the claim text.