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US 2015/0175628 A1Published application
Imidazo-oxadiazole and imidazo-thiadiazole derivatives
AssigneeMerck Patent GmbH
InventorsAnna Quattropani, Dominique Swinnen
Life of this patent
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Abstract
The present invention provides compounds of Formula (I) used as Amyloid beta lowering agent for the treatment of neurodegenerative diseases.
Claims12
A compound of Formula (I)
- wherein
- X denotes O or S,
- U is selected from
- (i) a phenyl ring which may be substituted by 1 or 2 groups independently selected from C1-C6-alkoxy, C1-C6-alkyl, halogen, and CN;
- (ii) a 5- or 6-membered unsaturated or aromatic heterocyclic system comprising 1 nitrogen atom and optionally up to 2 additional heteroatoms independently selected from N, O or S, which may be substituted by 1 or 2 groups independently selected from C1-C6-alkoxy, C1-C6-alkyl, halogen, and CN, and
- (iii) a single bond;
- T denotes —NR5CO—, —CONR5, —NR5—CO—NR5, or —CO—;
- W is selected from
- (i) a linear or branched C1-C6-alkylen wherein 1 to 2 H atoms may be replaced by a phenyl ring, halogen, CN, or CF3,
- (ii) a linear or branched C1-C6-alkylen wherein 1 CH2 group is replaced by a 3- to 7-membered saturated carbocyclic ring,
- (iii) a linear or branched C1-C6-alkylen wherein 1 CH2 group is replaced by
- a phenyl ring optionally fused with the phenyl ring A,
- a 5- or 6-membered saturated heterocyclic system containing 1 or 2 nitrogen atoms, or
- a 5-membered aromatic heterocyclic system containing 1 to 3 heteroatoms independently selected from N, O and S, and optionally fused with a saturated 6-membered carbocyclic ring, or optionally fused with the phenyl ring A,
- and wherein another CH2 group which is not linked to T is optionally replaced by —O— or NR5;
- and
- (iv) a single bond,
- each R5 is independently H or a linear or branched C1-C6-alkyl,
- R1 denotes a linear or branched alkyl having 1 to 6 carbon atoms;
- Ra denotes H, CN, halogen, a linear or branched alkyl having 1 to 6 carbon atoms, wherein 1 to 3 H atoms may be replaced by halogens, or linear or branched alkoxy having 1 to 6 carbon atoms, wherein 1 to 3 H atoms may be replaced by halogens,
- R2, R3, R4 are each independently selected from CN, halogen, a linear or branched alkyl having 1 to 6 carbon atoms, wherein 1 to 3 H atoms may be replaced by halogens, and linear or branched alkoxy having 1 to 6 carbon atoms, wherein 1 to 3 H atoms may be replaced by halogens,
- and pharmaceutically acceptable derivatives, solvates, tautomers, salts, hydrates and stereoisomers thereof, including mixtures thereof in all ratios.
19 more elements
(canceled)
Dependencies are inferred from the claim text.