Benzothiophene compound and application thereof in preventive and/or treatment medicine for breast cancer and osteoporosis
A compound and application technology, applied in drug combination, bone disease, organic chemistry, etc., can solve the problems of low water solubility, achieve the effects of small side effects, low dosage, and high effective bioavailability
Inactive Publication Date: 2012-05-30
苏州波锐生物医药科技有限公司
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Problems solved by technology
In addition, the water solubility of raloxifene is very low, only 2ug / ml
Method used
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Embodiment 1
[0056] This embodiment provides a compound represented by formula (II):
[0057]
Embodiment 2
[0059] This embodiment provides a compound represented by formula (III):
[0060]
Embodiment 3
[0062] This embodiment provides a compound represented by formula (IV):
[0063]
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Abstract
The invention relates to a novel benzothiophene derivative and application thereof in preventive and / or treatment medicine for breast cancer and osteoporosis. The benzothiophene derivative is an ideal selective estrogen receptor modulator, can be used for treating or preventing various indications related to estrogen functions, and is particularly applicable to treating post-menopause breast cancer and osteoporosis. The compound has the advantages that oxidative metabolism is lowered, effective bioavailability is higher, and accordingly, dosage of the compound is little, tolerance of the compound is fine, and side effects are low.
Description
Technical field [0001] The invention relates to benzothiophene compounds and their use in preparing medicines for preventing and / or treating breast cancer osteoporosis. Background technique [0002] Selective estrogen receptor modulators (SERMs) refer to a series of compounds with different structures that can interact with estrogen receptors and produce specific effects according to different target tissues and hormone internal environments. They In some tissues, it exhibits estrogen-like effects and in other tissues it exhibits anti-estrogen-like effects. A selective estrogen receptor modulator that has an estrogen-like effect on the bone and cardiovascular system, but has an anti-estrogen-like effect on the breast and uterus, and at the same time has no side effects such as endometrial cancer and vascular complications, is desired. [0003] At present, the selective estrogen receptor modulators in clinical trials or clinical use mainly include triphenylethylene derivatives (Tri...
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IPC IPC(8): C07D409/12A61K31/4535A61P5/30A61P19/10A61P15/12A61P9/00A61P35/00A61P3/04A61P13/00
Inventor 殷建明朱惠霖
Owner 苏州波锐生物医药科技有限公司
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