1,4-dihydrobithiophene [3', 2': 5, 6] bithiapyran [4, 3-c] pyrazol-3-carboxylic acid derivative and application thereof

Abstract

The invention belongs to the technical field of medicine and relates to a 1,4-dihydrobithiophene [3', 2': 5, 6] bithiapyran [4, 3-c] pyrazol-3-carboxylic acid derivative and application thereof used as an estrogen receptor, in particular to a 1,4-dihydrobithiophene [3', 2': 5, 6] bithiapyran [4, 3-c] pyrazol-3-carboxylic acid derivative and a pharmaceutically acceptable salt, or a stereoisomer thereof and a prodrug as well as a pharmaceutically acceptable vector in compatibility or a diluent used as an estrogen receptor. The structural general formula of the derivative is disclosed in the specification, and in the structural formula, n R1 can be independently selected from a substituted or unsubstituted amido group, and R2 can be independently selected from H or an acetyl group. The derivative can be used for treating and preventing various diseases related to estrogen functions, such as diseases related to estrogen deficiency, estrogen sensitive cancer and hyperplasia, endometriosis, uterus myoma and osteoarthritis. Compounds or compositions of the derivative can also be independently used or combined with progestogen or a hormoneantagonist as a contraceptive.

Description

technical field The present invention relates to 1,4-dihydrothieno[3',2':5,6]thiapyro[4,3-c]pyrazole-3-carboxylic acid derivatives or pharmaceutically acceptable salts thereof. The present invention also relates to preparation methods of said compounds and pharmaceutically acceptable compositions containing them and their application in treating diseases. Background technique Estrogens are known as female sex hormones. However, there have been many recent reports on the tissue specificity of estrogens in organs, properties not traditionally considered estrogen-sensitive or estrogen-responsive. The secretion of estrogen significantly decreases during menopause. Decreased estrogen induces short- and long-term symptoms of disorders of the vasomotor, genitourinary, cardiovascular, skeletal, and central nervous systems: e.g., hot flashes, genitourinary atrophy, increased risk of cardiovascular disease, osteoporosis Alzheimer's disease, cognitive decline and psychological defic...

AI Technical Summary

Problems solved by technology

Furthermore, neither raloxifene nor any other currently available selective estrogen receptor modulator provides all the benefits of currently available ERT, such as controlling postmenopausal syndrome and preventing Alzheimer's disease, without causing uterine Adverse side effects such as increased risk of endometrial and breast cancer and bleeding

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