Glycosidase inhibitors

Patent metadata

Field	Value
Publication number	US-9879001-B2
Application number	US-201414775134-A
Country	US
Kind code	B2
Filing date	Mar 10, 2014
Priority date	Mar 14, 2013
Publication date	Jan 30, 2018
Grant date	Jan 30, 2018

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.

First claim

The invention claimed is:

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.

Assignees

• Merck Patent Gmbh

Inventors

• Yu Henry
• Liu-Bujalski Lesley
• Johnson Theresa L

Classifications

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P25/14

  for treating abnormal movements, e.g. chorea, dyskinesia · CPC title

• A61P25/16

  Anti-Parkinson drugs · CPC title

• A61P25/28

  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 title