Substituted peptides useful in the treatment of alzheimer's disease
AssigneePharmacia & Upjohn Company
InventorJames Beck
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Abstract
Disclosed are methods for treating Alzheimer's disease, and other diseases, and/or inhibiting beta-secretase enzyme, and/or inhibiting deposition of A beta peptide in a mammal, by use of compounds of formula (I), wherein Ar, W, Z, Q, R1, U, and L, are as herein defined.
Claims30
A method according to claim 5, wherein the disease is Alzheimer's disease. * indicates a mixture of isomers at this carbon
A method of treating a subject who has, or in preventing a subject 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 subjects with mild cognitive impairment (MCI) and 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 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, frontotemporal dementias with parkinsonism (FTDP), 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 includes administration of a therapeutically effective amount of a compound of formula (I)
- wherein Ar is
- R10 is H or OH;
- X is O or an electron pair;
- W is
- Q is
- R1 is
- Z is H or Z and Q taken together are —(CH2)3— or —(CH2)4—
- U is
- R3 is C1-11-alkyl or
- wherein R20 is H or C1-10-alkyl;
- and Ac is formyl or
- wherein R21 is C1-10-alkyl;
- L is
- R2 is
- m is 0, 1 or 2;
- p is 0, 1 or 2;
- and
- q is 0, 1, or 2;
- an epimer or racemate thereof.
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A method for inhibiting beta-secretase activity, comprising contacting an effective amount for inhibition of a compound of formula (I)
- wherein Ar is
- R10 is H or OH;
- X is O or an electron pair;
- W is
- Q is
- Z is H or Z and Q taken together are —(CH2)3— or —(CH2)4—
- U is
- R3 is C1-11-alkyl or
- wherein R20 is H or C1-10-alkyl;
- and Ac is formyl or
- wherein R21 is C1-10-alkyl;
- L is
- R2 is
- m is 0, 1 or 2;
- p is 0, 1 or 2;
- and
- q is 0, 1, or 2;
- an epimer or racemate thereof.
(canceled)
A method for inhibiting production of amyloid beta peptide (A beta) in a cell, comprising administering to said cell an effective inhibitory amount of a compound of formula (I) or pharmaceutically acceptable salt thereof:
- wherein Ar is
- R10 is H or OH;
- X is O or an electron pair;
- W is
- Q is
- R1 is
- Z is H or Z and Q taken together are —(CH2)3— or —(CH2)4—
- U is
- R3 is C1-11-alkyl or
- wherein R20 is H or C1-10-alkyl;
- and Ac is formyl or
- wherein R21 is C1-10-alkyl;
- L is
- R2 is
- m is 0, 1 or 2;
- p is 0, 1 or 2;
- and
- q is 0, 1, or 2;
- an epimer or racemate thereof.
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Dependencies are inferred from the claim text.