Substituted alcohols useful in treatment of Alzheimer's disease

• US 20060178345A1
• Filed: 01/03/2006
• Published: 08/10/2006
• Est. Priority Date: 06/27/2001
• Status: Abandoned Application

• Current Assignee: John Tucker, Roy Hom, Varghese John
• Original Assignee: John Tucker, Roy Hom, Varghese John
• Inventors: Tucker, John, John, Varghese, Hom, Roy
• Application Number:
  US11/324,678
• Publication Number:
  US 20060178345A1
• Time in Patent Office: Days
• US Class Current: 514/81
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: C07D 233/84 Sulfur atoms
• CPC Class Codes: C07D 233/90 Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• CPC Class Codes: C07D 235/28 Sulfur atoms
• CPC Class Codes: C07D 249/12 Oxygen or sulfur atoms
• CPC Class Codes: C07D 409/04 directly linked by a ring-member-to-ring-member bond
• CPC Class Codes: C07D 473/38 attached in position 6

Abstract

The invention relates to substituted alcohol compounds of the formula (I):
wherein X, R₁, R₂, R₃, R_N, R₂₀ and R_C are defined herein. The compounds are useful in the treatment or prevention of Alzheimer'"'"'s disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer'"'"'s sufferers.

Claims

1. A compound of the formula I:

2. A pharmaceutically acceptable salt or ester of a compound according to claim 1.

3. A compound according to claim 1, wherein X is CR₂R₃.

4. A compound according to claim 1, wherein X is O.

5. A compound according to claim 1, wherein X is S.

6. A compound according to claim 1, wherein X is SO.

7. A compound according to claim 1, wherein X is SO₂.

8. A method for making a compound of formula (I)

9. A method of treating a patient who has, or in preventing a patient from getting, a disease or condition selected from the group consisting of Alzheimer'"'"'s disease, for helping prevent or delay the onset of Alzheimer'"'"'s disease, for treating patients with mild cognitive impairment (MCI) and/or preventing or delaying the onset of Alzheimer'"'"'s disease in those who would progress from MCI to AD, for treating Down'"'"'s syndrome, for treating humans who have Hereditary Cerebral Hemorrhage with Amyloidosis of the Dutch-Type, for treating cerebral amyloid angiopathy and/or preventing its potential consequences, i.e. single and recurrent lobar hemorrhages, for treating other degenerative dementias, including dementias of mixed vascular and degenerative origin, dementia associated with Parkinson'"'"'s disease, dementia associated with progressive supranuclear palsy, dementia associated with cortical basal degeneration, or diffuse Lewy body type of Alzheimer'"'"'s disease and who is in need of such treatment which comprises administration of a therapeutically effective amount of a compound selected from the group consisting of a substituted alcohol of formula (I)

10. A compound selected from the group consisting of: