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US 2005/0090449 A1Published application
Novel statine derivatives for the treatment of Alzheimer's disease
AssigneeBoehringer Ingelheim International GmbH
InventorsKlaus Fuchs, Stefan Peters, Comelia Dorner-Ciossek, Marcus Kostka, Sandra Handschuh, Christian Haass
Life of this patent
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Abstract
The invention relates to a compound of the formula wherein R1, R2, X, Y, n, t and m are defined as in the specification and claims and to its use for treating or preventing Alzheimer's disease and other similar diseases.
Claims18
A compound of the formula
- wherein
- R1 represents a hydrogen atom or a group selected from the formulae (A) and (B)
- (A) R3—CO—(CH2)s—CO—,
- in which
- R3 represents R4-Z1 with Z1 being O or NR5, R4, R5 being each independently hydrogen or C1-6 alkyl, and
- s is an integer from 1 to 4;
- (B) R6—CO—
- in which
- R6 represents a C1-6alkyl group, a C1-6 haloalkyl group or a phenyl group being optionally substituted by one or more substituents selected from the group consisting of halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, amino, C1-6 alkylamino, di-(C1-6 alkyl)-amino, C1-6 alkoxycarbonyl, formyl, carboxy, hydroxy, cyano, SO3H and nitro;
- Xaa1 each independently represent an amino acid or the N-alkylated derivative thereof, at least one of which being N-terminally linked to R1;
- n is 0 or an integer from 1 to 3;
- Y represents a single bond, or if t is 0, a spacer group selected from —O— and —NH—;
- R2 represents a hydroxy group or a group of formula (C)
- (C) -Z2-R7
- in which
- Z represents O or NR8,
- R7 represents
- (a) a C1-6 alkyl group being optionally substituted by one or more substituents selected from the group consisting of halogen, C3-8-cycloalkyl, phenyl, C1-6 alkoxy, C1-6 haloalkoxy, amino, C1-6 alkylamino, di-(C1-6 alkyl)-amino, C1-6 alkoxycarbonyl, formyl, carboxy, hydroxy, cyano and nitro, or
- (b) a phenyl group being optionally substituted by one or more substituents selected from the group consisting of halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, amino, C1-6 alkylamino, di-(C1-6 alkyl)-amino, C1-6 alkanoylamino, C1-6 alkoxycarbonyl, formyl, carboxy, hydroxy, cyano and nitro,
- R2 represents a hydrogen atom or C1-6 alkyl group;
- Xaa2 each independently represent an amino acid or the N-alkylated derivative thereof, in which the amino group of the N-terminally amino acid may have been replaced by Y, and one of which being C-terminally linked to R2;
- t is 0 or an integer from 1 to 3;
- X is selected from ethyl, thiomethyl and C3-C8-cycloalkyl;
- and
- m is 1 or 2,
- or a pharmaceutically acceptable salt or solvate thereof.
23 more elements
Dependencies are inferred from the claim text.