A compound b11 as an inhibitor of histone methyltransferase nsd3 activity and its application

A methyltransferase and activity inhibitor technology, applied in the field of medicine, can solve the problems of less research and achieve good NSD3 enzyme inhibitory effect
CN109053544BActive Publication Date: 2020-07-28普美瑞(常州)生物科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
普美瑞(常州)生物科技有限公司
Publication Date
2020-07-28

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Abstract

The invention discloses a compound B11 used as a histone methyltransferase NSD3 activity inhibitor and pharmaceutical application thereof. The compound has a chemical structure shown as a formula I: the formula I is shown in the following description; a chemical name is N-(1,3-dioxoisoindolin-4-yl)-4-phenoxybenzamide; the pharmaceutical application is that at least one of the compound B11 or hydrate thereof, pharmaceutically acceptable salts, a tautomer, a stereoisomer and a precursor compound is used as an active component to be used for preparing an anti-tumor medicine. The compound B11 provided by the invention can be used for effectively inhibiting the NSD3 enzymatic activity and an enzymology level IC50 value is 26.17+ / -4.75mu mol / L; the compound B11 has a good NSD3 enzymatic inhibition effect. The compound provided by the invention is used as an effective inhibitor of a tumor important target spot NSD3, is hopefully used as the active component to prepare the anti-tumor medicineand has a medicinal prospect.
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Description

technical field

[0001] The invention belongs to the technical field of medicine, and in particular relates to a histone methyltransferase NSD3 activity inhibitor and application thereof. Background technique

[0002] Histone methylation is one of the most important modification mechanisms of epigenetic modification. The abnormal expression of histone methylation and its regulator histone methyltransferase is closely related to the occurrence of genetic diseases, autoimmune diseases, aging and cancer, especially in the occurrence and development of tumors. Therefore, histone methyltransferases are regarded as potential new targets for anti-tumor therapy.

[0003] In recent years, breakthroughs have been made in the development of inhibitors targeting histone methyltransferases. Currently, the histone methyltransferase EZH2 inhibitor EPZ-6438 (Epizyme Company) entered phase I / II clinical trials in 2014 for the treatment of patients with non-Hodgkin's lymphoma, advanced solid...

Claims

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