Inhibitors of histone lysine specific demethylase (LSD1) and histone deacetylases (HDACS)
US11565994B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jun 4, 2020 |
| Grant date | Jan 31, 2023 |
| Priority date | — |
| Expiry date | Jun 4, 2040 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07C2602/02
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.