Substituted 3-amino-5-phenylbenzamide compounds as covalent inhibitors of enhancer zeste homolog 2 (EZH2) and proteolysis-targeting chimeric derivatives thereof (PROTACs) that induce degradation of EZH2
US12042543B2 · kind B2 · utility
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13Claims
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Key dates
| Filing date | May 2, 2022 |
| Grant date | Jul 23, 2024 |
| Priority date | — |
| Expiry date | May 2, 2042 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P35/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Disclosed are covalent inhibitors of enhancer zeste homolog 2 (EZH2) which may be utilized as EZH2 targeting agents. The disclosed compounds may be characterized as substituted 3-amino-5-phenylbenzamide compounds. The disclosed compounds may be utilized as covalent inhibitors of EZH2 and further may be derivatized to form proteolysis-targeting chimeric molecules (PROTACs) that target EZH2 for degradation. The disclosed compounds and PROTACs may be used in pharmaceutical compositions and methods for treating cell proliferative disorders associated with EZH2 activity, such as cancer.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.