Unlock instant, AI-driven research and patent intelligence for your innovation.

A class of isopimarane-type diterpene derivatives, its pharmaceutical composition and its use

A technology of isopimarane and derivatives, applied in pharmaceutical compositions for treating estrogen-related diseases, applications in medicines, and the field of estrogen biosynthesis regulators, can solve the problem of no pharmaceutical composition, no isopimarane diterpene derivatives things, etc.

Inactive Publication Date: 2021-02-02
YUNNAN UNIV +1
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are few reports on its chemical composition and biological activity.
[0005] So far, there is no report of this type of isopimarane type diterpene derivatives (1-7 shown in formula I) in the prior art, and there is no report of its pharmaceutical composition as an active ingredient, nor is there any report of this type of isopimarane diterpene derivatives. Report on the application of terpene derivatives (1-9 shown in formula I) and pharmaceutical compositions thereof in the preparation of estrogen biosynthesis regulators and in the preparation of drugs for treating estrogen-mediated diseases

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A class of isopimarane-type diterpene derivatives, its pharmaceutical composition and its use
  • A class of isopimarane-type diterpene derivatives, its pharmaceutical composition and its use
  • A class of isopimarane-type diterpene derivatives, its pharmaceutical composition and its use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Preparation of isopimarane-type diterpene derivatives (1-7) (I):

[0048] Extraction and separation of isopimarane-type diterpene derivatives (1–7)(I):

[0049] The semi-preparative HPLC used in the experiment is Agilent 1260 and Zorbax SB-C18 (9.4mm × 25cm) chromatographic column; thin-layer chromatography silica gel, column chromatography silica gel (100-200 mesh and 200-300 mesh) were purchased from Qingdao Mei High Group Ltd.; reverse C18 silica gel was Lichroprep RP-18gel (40-63 μm, Merck, Darmstadt, Germany), and Sephadex LH-20 (Pharmacia) was used for Sephadex.

[0050] Collect the leaf branches of Premnafulva, dry, crush, extract three times with 80% ethanol at room temperature, combine the ethanol extracts, filter, and concentrate under reduced pressure; suspend the extract in aqueous solution, and wash with ethyl acetate After extraction, the ethyl acetate extraction part was concentrated under reduced pressure, dissolved and adsorbed on silica gel with chlor...

Embodiment 2

[0132] According to the method of Example 1, the isopimarane-type diterpene derivatives (1-7) were firstly prepared, dissolved with a small amount of DMSO respectively, added water for injection as usual, finely filtered, potted and sterilized to make an injection.

Embodiment 3

[0134] According to the method of Example 1, the isopimarane type diterpene derivative (1-7) was first prepared, and after dissolving with a small amount of DMSO, it was dissolved in sterile water for injection, stirred to dissolve, and filtered through a sterile suction funnel Filtration, and then aseptic fine filtration, sub-package in ampoules, freeze-drying at low temperature and then aseptically melt-seal to obtain powder injection.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The isopimarane type diterpene derivative (1-7) shown in the structural formula (I), containing it is a pharmaceutical composition composed of an active ingredient and a pharmaceutical carrier. ) and the preparation method of its pharmaceutical composition, its application in the preparation of medicines for treating human diseases, especially its application in the preparation of medicines for the treatment of various diseases mediated by estrogen, and its use as estrogen biosynthesis regulator agent.

Description

Technical field: [0001] The invention belongs to the technical field of medicines, and in particular relates to a class of isopimarane-type diterpene derivatives, a pharmaceutical composition containing it as an active ingredient for treating estrogen-related diseases, especially for preparing and treating estrogen-mediated diseases. Use in medicine for various diseases, process for its preparation, and use as regulator of estrogen biosynthesis. Background technique: [0002] Estrogen is an important endogenous substance in the human body and mediates many important physiological functions. There are three main types of estrogen, the most active is estradiol (17β-estradiol, E2), followed by estrone (estrone, E1), and the least active is estriol (E3), its biological effects are mainly through Combines with estrogen receptor α / β, activates its transcriptional or non-transcriptional activity, and plays an important role in reproduction, immunity, bone, cardiovascular and centr...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C07C49/513C07C45/80C07C45/79C07J73/00C07C33/14C07C29/86C07C29/76C07C29/78A61K31/122A61K31/047A61K31/58A61P5/30
CPCA61P5/30C07C29/76C07C29/78C07C29/86C07C33/14C07C45/79C07C45/80C07C49/513C07J73/003C07C2603/26C07C2603/40
Inventor 肖伟烈王飞普德兵杜宝文张芮菡史楠高俊博张兴杰
Owner YUNNAN UNIV