Alkylene phenylsulfonamide type selective ZAK inhibitor and application thereof

A technology of alkynephenylbenzenesulfonamide and benzenesulfonamide, applied in the field of alkynephenylbenzenesulfonamide selective ZAK inhibitors, can solve the problems of limited research and lack of ZAK selectivity
CN108117553AActive Publication Date: 2018-06-05JINAN UNIVERSITY
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
JINAN UNIVERSITY
Publication Date
2018-06-05

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Abstract

The invention relates to application of an alkylene phenylsulfonamide compound with a structure of formula (I) (shown in the description) or pharmaceutically acceptable salt thereof or stereisomer thereof or a prodrug molecule thereof in preparation of a ZAK inhibitor. The alkylene phenylsulfonamide compound is capable of effectively and selectively inhibiting ZAK protein kinase and further regulating the activation of multiple routes such as downstream JNK / SAPK, p38 and ERK, can be used for preparing drugs for preventing and treating several ZAK kinase relevant diseases such as myocardial hypertrophy, myocardial fibrosis, stenocardia, coronary heart disease, cardiac failure and myocardial infarction and has the characteristics of relatively good pharmacokinetics, low toxicity and relatively high druggability.
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Description

technical field

[0001] The invention relates to the field of chemistry and medicine, in particular to an alkynephenylbenzenesulfonamide selective ZAK inhibitor and its application. Background technique

[0002] ZAK kinase (Leucine-zipper and sterile-αmotif kinase) belongs to the mixed lineage kinase (Mixed lineage kinase, MLK) family, is a new type of mitogen-activated protein kinase kinase kinase (Mitogen-activited protein kinase kinase kinase, MAP3K), Widely distributed in various tissues and organs of the human body, such as heart, skeletal muscle, placenta, pancreas, lung, liver, etc. ZAK kinase consists of 800 amino acids, and its structure includes kinase domain (KD), leucine zipper (Leucine-zipper, LZ) and sterile α motif (sterile-α motif, SAM). Overexpression of ZAK kinases in vivo is closely related to cardiac hypertrophy, myocardial fibrosis, inflammation and tumor formation. Biological studies have shown that ZAK is overexpressed in infarcted cardiomyocytes. Hi...

Claims

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