IP Library Granted Patent US 9,879,001
Granted Patent B2
US 9,879,001 · App. 14/775,134 · Granted Jan 30, 2018

Glycosidase inhibitors

Inventors: Henry Yu (Wellesley, MA); Lesley Liu-Bujalski (Bedford, MA); Theresa L. Johnson (Salem, MA)
Assignee: Merck Patent GmbH
C07D417/06A61K31/426A61K31/427A61K31/454A61K31/496A61K31/498C07D277/46C07D413/06C07D417/14G01N33/6893
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Quick Facts
Patent No.
US 9,879,001
App. No.
14/775,134
Granted
Jan 30, 2018
Kind
B2
Abstract

Compounds of formula (I) wherein X 1 , X 2 , W, R 1 to R 5 , L and m have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.

Claims (17)

1. A compound of formula

wherein:

R 2 denotes COY, COAlk, CONY 2 or COOY;

R 5 denotes (CY 2 ) q Ar, Cyc or A;

Y denotes H or A;

A denotes unbranched or branched alkyl having 1-10 C atoms,

in which 1-7 H atoms can be replaced independently from one another by Hal;

Alk denotes unbranched or branched alkenyl having 2-6 C atoms;

in which 1-3 H atoms can be replaced independently from one another by Hal;

Cyc denotes cycloalkyl having 3-7 C atoms; in which 1-4 H atoms can be replaced independently from one another by Hal;

Ar denotes an unsaturated or aromatic mono- or bicyclic carbocycle having 4-12 C atoms, which can be substituted by at least one substituent selected from the group of Hal, A, OY, COOY and CN;

Hal denotes F, Cl, Br or I;

q denotes 0, 1 or 2; and

and/or a physiologically acceptable salt thereof.

2. The compound according to claim 1 selected from the group of:

and/or a physiologically acceptable salt thereof.

3. A pharmaceutical composition comprising as active ingredient an effective amount of a compound according to claim 1 , wherein the active ingredient is provided together with pharmaceutically tolerable adjuvants and/or excipients in the pharmaceutical composition, optionally in combination with one or more further active ingredients.

Continuity (3)
Provisional Application 61817493 · Apr 30, 2013
Provisional Application 61782353 · Mar 14, 2013
Related Publication 20160031871A1 · Feb 4, 2016