The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
May. 24, 2022

Filed:

Apr. 03, 2018
Applicant:

Vivoryon Therapeutics N.v., Halle, DE;

Inventors:

Ulrich Heiser, Halle, DE;

Torsten Hoffmann, Halle, DE;

Ingeborg Lues, Seeheim-Jugenheim, DE;

Antje Meyer, Halle, DE;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 417/12 (2006.01); C07D 235/08 (2006.01); C07D 249/14 (2006.01); C07D 277/40 (2006.01); C07D 285/135 (2006.01); C07D 401/04 (2006.01); C07D 401/12 (2006.01); C07D 403/12 (2006.01); C07D 417/04 (2006.01); A61K 45/06 (2006.01);
U.S. Cl.
CPC ...
C07D 417/12 (2013.01); C07D 235/08 (2013.01); C07D 249/14 (2013.01); C07D 277/40 (2013.01); C07D 285/135 (2013.01); C07D 401/04 (2013.01); C07D 401/12 (2013.01); C07D 403/12 (2013.01); C07D 417/04 (2013.01); A61K 45/06 (2013.01); C07B 2200/13 (2013.01);
Abstract

The invention relates to a compound of formula (I): A-B-D-E (I) or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein: A is selected from monocyclic and bicyclic heteroaryl, which may independently substituted by alkyl or amino; B is selected from alkyl, heteroalkyl, alkyl-amino, aryl, heteroaryl, cycloalkyl, heterocyclyl and alkylene, wherein said groups may independently be substituted by alkyl; D is selected from aryl-amino, heteroaryl-amino, cycloalkyl-amino, heterocyclyl, heterocyclyl-amino, urea, thioamide, thiourea, sulfonamide, sulfoximine and sulfamoyl, wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl groups may independently be substituted; and E is selected from aryl, heteroaryl, cycloalkyl, heterocyclyl, wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl groups may independently be substituted. The compounds of formula (I) are inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.


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