TREA

Dihydrospiro[dibenzo[a,d][7]annulene-5,4'-imidazol] compounds for the inhibition of beta-secretase

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Information

  • Patent Application
  • 20070203116
  • Publication Number
    20070203116
  • Date Filed
    February 23, 2007
    17 years ago
  • Date Published
    August 30, 2007
    17 years ago
Information
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
Description
Claims
  • 1. A compound of formula I
  • 2. The compound according to claim 1 wherein X is CH2.
  • 3. The compound according to claim 1 wherein R6 is H or halogen.
  • 4. The compound according to claim 1 wherein R1 and R2 are H.
  • 5. The compound according to claim 1 wherein R3 is a C1-C4 alkyl group.
  • 6. The compound according to claim 2 wherein Y is CH2.
  • 7. The compound according to claim 6 wherein R7 is an optionally substituted phenyl or heteroaryl group and is attached in the 7-position.
  • 8. The compound according to claim 7 wherein R1 and R2 are H and R3 is a C1-C4 alkyl group.
  • 9. The compound according to claim 1 selected from the group consisting essentially of:
  • 10. A method for the treatment of a disease or disorder associated with excessive BACE activity in a patient in need thereof which comprises providing to said patient a therapeutically effective amount of a compound of formula I
  • 11. The method according to claim 10 wherein said disease or disorder is selected from the group consisting essentially of: Alzheimer's disease; cognitive impairment; Down's Syndrome; HCHWA-D; cognitive decline; senile dementia; cerebral amyloid angiopathy; and a neurodegenerative disorder.
  • 12. The method according to claim 10 wherein said disease or disorder is characterized by the production of β-amyloid deposits or neurofibrillary tangles.
  • 13. The method according to claim 12 wherein said disease or disorder is Alzheimer's disease.
  • 14. A method for modulating the activity of BACE which comprises contacting a receptor thereof with an effective amount of a compound according to claim 1.
  • 15. A pharmaceutical composition which comprises a pharmaceutically acceptable carrier and an effective amount of a compound of formula 1
  • 16. The composition according to claim 15 having a formula I compound wherein X is CH2.
  • 17. The composition according to claim 16 having a formula I compound wherein Y is CH2.
  • 18. The composition according to claim 17 having a formula I compound wherein R1 and R2 are H and R3 is methyl.
  • 19. The composition according to claim 18 having a formula I compound wherein R7 is an optionally substituted phenyl or heteroaryl group and is attached in the 7-position.
  • 20. The composition according to claim 15 having a formula I compound selected from the group consisting essentially of:
Provisional Applications (1)
Number Date Country
60776361 Feb 2006 US