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:
Jan. 14, 2025

Filed:

Dec. 11, 2019
Applicant:

Hoffmann-la Roche Inc., Little Falls, NJ (US);

Inventors:

Beat Frei, Basel, CH;

Hasane Ratni, Basel, CH;

Assignee:

Hoffmann-La Roche Inc., Little Falls, NJ (US);

Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07D 487/04 (2006.01); C07D 471/04 (2006.01); A61K 31/46 (2006.01); A61P 25/28 (2006.01); A61P 27/16 (2006.01);
U.S. Cl.
CPC ...
C07D 487/04 (2013.01); C07D 471/04 (2013.01);
Abstract

The invention provides 7-phenoxy-N-(3-azabicyclo[3.2.1]octan-8-yl)-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazol-2-amine derivatives and related compounds of the general formula (I) wherein R, Ar, n and m are as described herein, compositions including the compounds, processes of manufacturing the compounds and the compounds for use in methods of medical treatment. The present compounds are as gamma-secretase modulators for the treatment of diseases associated with the deposition of β-amyloid in the brain, such as Alzheimer's disease, cerebral amyloid angiopathy, cochlear synaptopathy, hearing loss, hereditary cerebral hemorrhage with amyloidosis-Dutch type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome. The present description discloses the preparation of exemplary compounds as well as pharmacological data thereof (e.g. pages 54 to 74; examples 1 to 64; table). An exemplary compound is e.g. (R)-7-(3,5-difluorophenoxy)-N-((1R,5S,8s)-3-(6-methoxypyridazin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazol-2-amine (example 1).


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