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. 31, 2023

Filed:

Jun. 04, 2020
Applicant:

The Johns Hopkins University, Baltimore, MD (US);

Inventors:

Philip Cole, Baltimore, MD (US);

Shonoi Ming, Baltimore, MD (US);

Polina Prusevich, Baltimore, MD (US);

Jay Kalin, Baltimore, MD (US);

Assignee:

The Johns Hopkins University, Baltimore, MD (US);

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
C07C 243/18 (2006.01); A61K 45/06 (2006.01); A61K 31/167 (2006.01); C07C 233/29 (2006.01); C07C 259/06 (2006.01); A61K 31/137 (2006.01); A61K 31/255 (2006.01); A61K 31/325 (2006.01); A61K 31/405 (2006.01); C07C 271/02 (2006.01); C07C 309/66 (2006.01); C07D 209/18 (2006.01);
U.S. Cl.
CPC ...
C07C 243/18 (2013.01); A61K 31/137 (2013.01); A61K 31/167 (2013.01); A61K 31/255 (2013.01); A61K 31/325 (2013.01); A61K 31/405 (2013.01); A61K 45/06 (2013.01); C07C 233/29 (2013.01); C07C 259/06 (2013.01); C07C 271/02 (2013.01); C07C 309/66 (2013.01); C07D 209/18 (2013.01); C07C 2602/02 (2017.05);
Abstract

A series of phenelzine analogs comprising a phenelzine scaffold linked to an aromatic moiety and their use as inhibitors of lysine-specific demethylase 1 (LSD1) and/or one or more histone deacetylases (HDACs) is provided. The presently disclosed phenelzine analogs exhibit potency and selectivity for LSD1 versus MAO and LSD2 enzymes and exhibit bulk, as well as, gene specific histone methylation changes, anti-proliferative activity in several cancer cell lines, and neuroprotection in response to oxidative stress. Accordingly, the presently disclosed phenelzine analogs can be used to treat diseases, conditions, or disorders related to LSD1 and/or HDACs, including, but not limited to, cancers and neurodegenerative diseases.


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