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Songorine derivatives, and pharmaceutical composition and applications thereof

A derivative, the technology of Songguolin, applied in the field of Songguolin derivatives and pharmaceutical compositions thereof, can solve the problems of lack of type II diabetes drugs, no Songguolin derivatives, and no reports of B-type G protein-coupled receptor inhibitors, etc. Achieve high clinical efficiency and less toxic and side effects

Active Publication Date: 2019-05-31
SHANGHAI OCEAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Now mainstream hypoglycemic drugs include insulin secretagogues (glibenclamide, repaglinide, etc.), metformin, α-glucosidase inhibitors (acarbose, etc.), but these drugs can only treat symptoms , there is still a lack of drugs to treat type 2 diabetes
[0004] To sum up, there is a very large market demand for drugs for the treatment of type 2 diabetes, but the current clinical application of drugs for the treatment of type 2 diabetes can only treat the symptoms but not the cause. Therefore, a new generation of drugs with high clinical efficiency and less toxic side effects has been developed. Drugs for the treatment of type II diabetes will have strong market competitiveness and market prospects
In the prior art, there is no report on the pharmaceutical composition of songlarin derivatives (1-17) as an active ingredient, and there is no application of it as a B-type G protein-coupled receptor inhibitor in a pharmaceutical composition and in the preparation and treatment of type II diabetes, Reports in Drugs for Diseases such as Obesity, Cardiovascular Disease and Mental Illness

Method used

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  • Songorine derivatives, and pharmaceutical composition and applications thereof
  • Songorine derivatives, and pharmaceutical composition and applications thereof
  • Songorine derivatives, and pharmaceutical composition and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047]

[0048] Molecular formula: C 26 h 35 NO 5

[0049] Molecular weight: 441

[0050] Appearance: white amorphous powder

[0051]

[0052] Molecular formula: C 24 h 33 NO 4

[0053] Molecular weight: 399

[0054] Appearance: white amorphous powder

[0055] resolve resolution:

[0056] Compound I (50 mg, 0.14 mmol) and 4-dimethylaminopyridine (DMAP, 17.1 mg, 0.14 mmol) were dissolved in anhydrous pyridine (2 mL), and acetyl chloride (0.2 mL, 0.34 mmol) was slowly added dropwise at room temperature, The reaction solution was stirred at room temperature until the reaction of the raw materials was complete. The reaction solution was slowly poured into ice water (20mL), extracted with dichloromethane (20mL×3), the dichloromethane layer was washed with saturated sodium bicarbonate (20mL×3) and saturated brine (15mL) successively, and washed with anhydrous After drying over sodium sulfate and concentrating under reduced pressure, it was subjected to silica gel c...

Embodiment 2

[0061]

[0062] Molecular formula: C 28 h 39 NO 5

[0063] Molecular weight: 469

[0064] Appearance: white amorphous powder

[0065] resolve resolution:

[0066] Compound I (50mg, 0.14mmol) and DMAP (17.1mg, 0.14mmol) were dissolved in anhydrous pyridine (2mL), propionic anhydride (0.29mL, 0.34mmol) was slowly added dropwise at room temperature, and the reaction solution was stirred at room temperature to react until the raw materials are completely reacted. The reaction solution was slowly poured into ice water (20mL), extracted with dichloromethane (20mL×3), the dichloromethane layer was washed with saturated sodium bicarbonate (20mL×3) and saturated brine (15mL) successively, and washed with anhydrous After drying over sodium sulfate and concentrating under reduced pressure, silica gel column chromatography with eluent petroleum ether / ethyl acetate / diethylamine (15:1:1) gave 310.5 mg of a white solid compound with a yield of 16%.

[0067] Spectral data:

[0068]...

Embodiment 3

[0070]

[0071] Molecular formula: C 30 h 43 NO 5

[0072] Molecular weight: 497

[0073] Appearance: white amorphous powder

[0074]

[0075] Molecular formula: C 26 h 37 NO 4

[0076] Molecular weight: 427

[0077] Appearance: white amorphous powder

[0078] resolve resolution:

[0079]Compound I (50mg, 0.14mmol) and DMAP (17.1mg, 0.14mmol) were dissolved in anhydrous pyridine (2mL), and butyric anhydride (0.55mL, 0.34mmol) was slowly added dropwise at room temperature, and the reaction solution was stirred at room temperature to react until the raw materials are completely reacted. The reaction solution was slowly poured into ice water (20mL), extracted with dichloromethane (20mL×3), the dichloromethane layer was washed with saturated sodium bicarbonate (20mL×3) and saturated brine (15mL) successively, and washed with anhydrous After drying over sodium sulfate and concentrating under reduced pressure, it was subjected to silica gel column chromatography, e...

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Abstract

The invention discloses songorine derivatives, and a pharmaceutical composition and applications thereof. Songorine derivatives (1-17) or pharmaceutically acceptable salts or solvates thereof are represented in the description. The invention also discloses an application of the pharmaceutical composition that comprises songorine derivatives or takes songorine derivatives as the active components in the preparation of (i) drugs for treating II type diabetes, obesity, cardiovascular diseases, and mental diseases; and (ii) a B type G protein coupled receptor antagonist. By inhibiting the B type Gprotein coupled receptors, solved is the problem that in clinic, only symptoms of II type diabetes can be treated, and the root of II type diabetes cannot be treated. The songorine derivatives (1-17)or pharmaceutically acceptable salts or solvates thereof are used to prepare drugs for treating II type diabetes or a B type G protein coupled receptor antagonist, the clinical efficiency is high, and the side and toxic effects are small.

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular, relates to songlarin derivatives and pharmaceutical compositions thereof, and preparation of medicines for treating type II diabetes, obesity, cardiovascular disease and mental illness, or B-type G protein-coupled receptor antagonists Uses in medicine. Background technique [0002] G protein-coupled receptors (GPCRs) are the largest family of membrane receptors, and there are about 800 annotated GPCRs in the human genome. These include many different signaling receptors. GPCRs bind chemicals around the cell and activate a series of signaling pathways that cause changes in the cell's internal state. GPCRs are involved in the regulation of many human functions such as vision, smell, taste, behaviour, immunity and the nervous system. GPCRs are one of the main targets of drugs, and about 40%-50% of drugs exert their efficacy by combining with GPCRs. Therefore, GPCRs are considere...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D221/22A61K31/439A61P3/04A61P3/10A61P9/00A61P25/18
Inventor 郭锐华王江茗乔武吴文惠
Owner SHANGHAI OCEAN UNIV
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