Preparation method and medical application of benzisothiazole and benzothiophene

A technology of benzisothiazole and benzothiophene is applied in the field of preparation of benzisothiazole and benzothiophene or their pharmaceutically acceptable salts, benzisothiazole and benzothiophene, and can solve the problem of increasing renal anemia Patients, high risk of cardiovascular disease and mortality, high price of rhEPO, to achieve good industrialization prospects, enhanced activity, good agonistic effect
CN113264900AActive Publication Date: 2021-08-17NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE +1
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
Publication Date
2021-08-17

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Abstract

The invention discloses a preparation method and medical application of benzisothiazole and benzothiophene, and telates to the field of pharmaceutical chemistry. According to the invention, benzisothiazole and benzothiophene are the first type of HIF-2 agonists; compared with a compound M1001 found by the applicant in the earlier stage, the invention has better HIF-2 agonist activity, and has remarkable enhancement activity on expression of mRNA and protein of EPO, VGEF, Glut1, NDRG1 and the like at the downstream of HIF-2, so that the invention can be used for preparing drugs for treating and / or preventing chronic kidney diseases / chronic renal anemia, dyslipidemia and high cholesterol caused by abnormal expression of HIF-2; and the method has a good industrialization prospect.
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Description

technical field

[0001] The present invention relates to the field of medicinal chemistry, and relates to a preparation method of benzisothiazole and benzothiophene and their medical use; more specifically, to a kind of benzisothiazole and benzothiophene or pharmaceutically acceptable salts thereof, Isomers, prodrugs, polymorphs or solvates, methods for their preparation and medical uses. Background technique

[0002] The kidney is an important organ of the human body. In addition to the basic functions of the urinary system, it can also secrete erythropoietin (EPO) to promote red blood cell production. It is the main place for EPO production; The incidence of renal anemia exceeds 10%, which has become a global public health problem; renal anemia is one of the main complications of CKD, mainly due to insufficient EPO output after renal injury; currently, the main treatment for renal anemia is Inject recombinant human EPO (recombinant human EPO, rhEPO) and its related product...

Claims

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