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:
Dec. 01, 2020

Filed:

Jun. 07, 2017
Applicant:

Glaxosmithkline Intellectual Property Development Limited, Brentford, GB;

Inventors:

Jeffrey Michael Axten, Collegeville, PA (US);

Mui Cheung, Collegeville, PA (US);

Anthony William Dean, Stevenage, GB;

Michael P. DeMartino, Collegeville, PA (US);

Hilary Schenck Eidam, Collegeville, PA (US);

Biswajit Kalita, Bangalore, IN;

Raghava Reddy Kethiri, Bangalore, IN;

Rajendra Kristam, Bangalore, IN;

Attorneys:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
A61K 31/403 (2006.01); A61K 31/4025 (2006.01); A61K 31/4015 (2006.01); A61K 31/44 (2006.01); A61K 31/4439 (2006.01); C07D 209/52 (2006.01); C07D 207/26 (2006.01); C07D 207/09 (2006.01); C07D 401/06 (2006.01); C07D 401/12 (2006.01); C07D 401/14 (2006.01); A61P 25/28 (2006.01); A61P 25/00 (2006.01); A61P 35/00 (2006.01); C07D 487/10 (2006.01); C07D 405/06 (2006.01); C07D 405/12 (2006.01); C07D 487/04 (2006.01);
U.S. Cl.
CPC ...
C07D 207/26 (2013.01); A61P 25/00 (2018.01); A61P 35/00 (2018.01); C07D 207/09 (2013.01); C07D 209/52 (2013.01); C07D 401/06 (2013.01); C07D 405/06 (2013.01); C07D 405/12 (2013.01); C07D 487/04 (2013.01); C07D 487/10 (2013.01);
Abstract

The invention is directed to substituted pyrrolidine derivatives. Specifically, the invention is directed to compounds according to Formula III: wherein A, B, L, L, L, R, R, R, R, R, R, R, R, R, Y, Y, z, z, z, and zare as defined herein, and salts thereof.The compounds of the invention are inhibitors of the ATF4 pathway and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, spinal cord injury, traumatic brain injury, ischemic stroke, stroke, diabetes, Parkinson disease, Huntington's disease, Creutzfeldt-Jakob Disease, and related prion diseases, progressive supranuclear palsy, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, inflammation, fibrosis, chronic and acute diseases of the liver, chronic and acute diseases of the lung, chronic and acute diseases of the kidney, chronic traumatic encephalopathy (CTE), neurodegeneration, dementia, cognitive impairment, atherosclerosis, ocular diseases, arrhythmias, in organ transplantation and in the transportation of organs for transplantation. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting the ATF4 pathway and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.


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