Pyrazolecarboxamide derivatives and application thereof

Abstract

The invention relates to pyrazolecarboxamide derivatives or pharmaceutically acceptable salt or precursors thereof. The structure of the pyrazolecarboxamide derivatives is shown in the general formula (I) in the specification, wherein R1 is selected from -H and -C1-C4 linear or branched alkyl groups, -C3-C6 naphthenic groups, 6-10-element acryl groups, C1-C4 alkyl substituted 6-10-element acryl groups, 5-10-element heteroaryl groups, C1-C4 alkyl substituted 5-10-element heteroaryl groups, 5-10-element saturated or partially saturated heterocyclic groups or C1-C4 alkyl substituted 5-10-element saturated or unsaturated heterocyclic groups, and each of the heteroaryl groups and the heterocyclic groups contains 1-3 heteroatoms selected from N,O and S; R2 is selected from -H and -C1-C4 linear or branched alkyl groups, -C3-C6 naphthenic groups or 3-6-element saturated or unsaturated heterocycles formed with R1; R3 is selected from -H and -C1-C4 linear or branched alkyl groups or -C3-C6 naphthenic groups; R4 is selected from -H and -C1-C4 linear or branched alkyl groups, -C3-C6 naphthenic groups or -COR41. The derivatives have relatively high anti-tumor activity and CDK11 protein kinase inhibition activity and have to the potential to be developed into clinically effective medicines.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a group of pyrazole amide derivatives and their application in the preparation of antitumor drugs. Background technique [0002] Tumor is a major disease that threatens human health. It is estimated that by 2020, the incidence of cancer worldwide will increase by 50%, and 15 million new cases will be added every year. The "2012 China Cancer Registration Annual Report" released by the National Cancer Registration Center shows that in the past 20 years, there have been about 3.12 million new cancer cases in China every year, with an average of 8,550 people per day. At present, the incidence of tumors in China is increasing at a rate of 3%-5% per year. [0003] In terms of disease types, lung cancer ranks first in the incidence of malignant tumors in the country, followed by gastric cancer, colorectal cancer, liver cancer, esophageal cancer and other gastrointestinal tumors. Ga...

AI Technical Summary

Problems solved by technology

In Henan Province, the morbidity and mortality of upper gastrointestinal tumors (mainly including esophageal cancer and gastric cancer) with obvious regional characteristics still rank first among all kinds of malignant tumors, although clinically significant progress has been made through early diagnosis and surgical treatment. However, the prevention and treatment of advanced diseases and how to better prolong the survival rate of patients are still a big problem for clinicians.

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