PRMT type-I inhibitor, and preparation method and application thereof

A compound and isomer technology, which is applied in the preparation of sulfides, amino compounds, chemical instruments and methods, etc., can solve the problems of off-target, poor cell membrane penetration, and no significant improvement in activity, etc.
CN108947879AActive Publication Date: 2018-12-07SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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Patent Information

Authority / Receiving Office
CN Β· China
Current Assignee / Owner
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Publication Date
2018-12-07

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Abstract

The invention discloses a PRMT type-I inhibitor, and a preparation method and an application thereof. The PRMT type-I inhibitor has a structure as shown in a formula I which is described in the specification. In the formula I, substituents are as defined in the specification and the claims. The compound provided by the invention can prepare a drug used for treating or preventing human and mammalian diseases associated with modulation of PRMT type-I abnormalities.
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Description

technical field

[0001] The invention relates to the field of biomedicine, in particular to a multi-substituted protein arginine methyltransferase PRMTI-type activity-inhibiting compound, a preparation method, a pharmaceutical composition and an application thereof. Background technique

[0002] Protein arginine methyltransferase PRMT can catalyze the methylation modification of many proteins including histone H4 in vivo. Arginine methylation is a ubiquitous post-translational modification in eukaryotes, involved in the regulation of numerous protein functions including histone methylation. The level of methylation is closely related to the physiological state of cells, which in turn affects the occurrence and development of diseases. Therefore, it is particularly important to regulate the methylation level in vivo. In mammals, the methylation modification of arginine is mainly completed by arginine methyltransferase PRMT.

[0003] At present, there are 9 kinds of arginine...

Claims

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