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Abietane type diterpene derivative as well as medicine composition and purpose thereof

A technology of abietane and its derivatives, applied in medicine, spleen tyrosine kinase inhibitor, and the field of pharmaceutical compositions for the treatment of rheumatoid arthritis, can solve the problem that there are no application reports of abietane diterpene derivatives, no drugs Insufficient research on composition, anti-inflammatory medicinal ingredients and anti-inflammatory targets

Inactive Publication Date: 2018-06-08
YUNNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the research on its anti-inflammatory active ingredients and anti-inflammatory targets is not enough
[0005] So far, there is no report of this type of abietane diterpene derivative (1-9 shown in formula I) in the prior art, nor does it have the report of its pharmaceutical composition as an active ingredient, nor does this type of abietane diterpene derivative (1-9 shown in formula I) and the application report of pharmaceutical composition thereof in the medicine of preparing SYK inhibitor and treating the disease of SYK mediation

Method used

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  • Abietane type diterpene derivative as well as medicine composition and purpose thereof
  • Abietane type diterpene derivative as well as medicine composition and purpose thereof
  • Abietane type diterpene derivative as well as medicine composition and purpose thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Preparation of abietane-type diterpene derivatives (1-9) (I):

[0045] Extraction and separation of abietane-type diterpene derivatives (1–9)(I):

[0046] 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.

[0047] Collect purple bead (Callicarpa bodinieri) leaf branches, dry, pulverize, extract 3 times with 85% ethanol at room temperature, combine the ethanol extracts, filter, and concentrate under reduced pressure; suspend the extracts in aqueous solution, and successively wash with petroleum ether, Ethyl acetate and n-butanol extraction, the ethyl acetate extraction part was concentrated under reduced pressure...

Embodiment 2

[0148] According to the method of Example 1, abietane-type diterpene derivatives (1-9) were first 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

[0150] The abietane type diterpene derivative (1-9) is first prepared by the method of Example 1, and after dissolving with a small amount of DMSO respectively, it is dissolved in sterile water for injection, stirred to dissolve, and filtered with a sterile suction filter funnel , and then aseptically finely filtered, divided into ampoules, freeze-dried at low temperature, and aseptically melt-sealed to obtain a powder injection.

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PUM

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Abstract

The invention relates to an abietane type diterpene derivative (1-9) shown as a structural formula (I), a medicine composition prepared from the compound 1-9 at the effective treatment quantity and amedicinal carrier, preparation method of the abietane type diterpene derivative (1-9) and the medicine combination, and application thereof to preparation of medicine for treating human diseases, particularly, application as a selective SYK (spleen tyrosine kinase) inhibitor and application to preparation of medicine for treating various diseases mediated by SYK.

Description

Technical field: [0001] The invention belongs to the technical field of medicines, and specifically relates to a class of abietane-type diterpene derivatives, a pharmaceutical composition for treating rheumatoid arthritis containing it as an active ingredient, a preparation method thereof, and a selective spleen tyrosine Acid kinase (Spleen tyrosine kinase, SYK) inhibitor, application in the preparation of medicines for treating various diseases mediated by SYK. Background technique: [0002] Spleen tyrosine kinase (SYK) is a non-receptor tyrosine kinase that is ubiquitously expressed in various tissues of the human body. SYK is critical to the function of the immune system, especially in the development of the lymphatic system and B cell receptor signal transduction process. SYK dysfunction is closely related to the occurrence and development of various diseases such as autoimmune diseases and B cell lymphoma. Rheumatoid Arthritis (Rheumatoid Arthrtis, RA) is a chronic au...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C62/38C07C62/32C07C69/16C07C69/157A61K31/192A61K31/222A61P19/02A61P29/00A61P37/02A61P35/02A61P35/00
CPCC07C62/32C07C62/38C07C69/157C07C69/16
Inventor 肖伟烈张芮菡高俊博杨双静张兴杰普德兵李晓莉
Owner YUNNAN UNIV
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