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Polyhydroxystilbenes and stibene oxides as antisoriatic agents and protein kinase inhibitors

A hydroxyl and acyl technology, applied in the field of using hydroxystilbene, novel stilbene derivatives and their analogs for anti-inflammatory, treating psoriasis and inhibiting protein-activating enzymes, which can solve the problems of increased erythrocyte giant cells and lack of mutual relationship, etc.

Inactive Publication Date: 2003-04-02
BEIJING WEN FENG TIANJI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Mice lacking Pim-1 appeared normal, healthy and fertile; however, careful analysis confirmed the correlation between Pim-1 deficiency and microcytosis, whereas Pim-1 overexpression in transgenic mice macrocytosis

Method used

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  • Polyhydroxystilbenes and stibene oxides as antisoriatic agents and protein kinase inhibitors
  • Polyhydroxystilbenes and stibene oxides as antisoriatic agents and protein kinase inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Embodiment 1-synthesis of compounds of the present invention

[0050] Compounds useful in the compositions of the present invention can be prepared from 3,5-dihydroxybenzoic acid and 4-bromo-3,5-dihydroxybenzoic acid of the formula with

[0051] Synthetic methods include hydroxymethylation, reduction of esters, oxidation of alcohols, witting reactions (or Horner reactions or Horner-Emmons-Wadsworth reactions) and demethylation reactions. This synthetic route is well established and available in the art.

[0052] Other stilbene derivatives can be obtained by reaction of hydroxylated stilbene derivatives with an acid or derivatives thereof, such as the corresponding salts, chlorides and anhydrides, by standard esterification reactions. Such reactions are well known in the art. For example, an alcohol is added to a mixture of anhydride and pyridine at low temperature and the mixture is left at room temperature for a time sufficient to complete the reaction. After t...

Embodiment 2

[0107] Example 2 - Formulation of Compounds of the Invention

[0108] Element

quantity

Active ingredient (compound of the present invention)

0.05-20.0mg

ethanol

100μl

Mineral oil, USP

50.0mg

White petrolatum, USP

made into 1.0g

[0109] step

[0110] Heat the weighed white petrolatum and mineral oil to 65°C and mix well. The mixture was cooled to 50-55°C with stirring. Certain active ingredients, dissolved in ethanol and ground, are added to the above mixture with stirring. The ointment was cooled to room temperature.

[0111] Element

quantity

Active ingredient (compound of the present invention)

0.05-20.0mg

ethanol

100μl

Micronized aluminum monostearate

50.0mg

Isopropyl myristate

made into 1.0g

[0112] step

[0113] About 90% of the desired isopropyl myristate was heated to 60°C. Add the aluminum monostearate with stirring and ...

Embodiment 3

[0120] Example 3 - Application as an antipsoriatic agent

[0121] Since there is no suitable animal model for this disease, the antipsoriatic activity of the compounds of the present invention can be determined by testing the effect of the compounds in vivo. The compound was tested by volunteers. In these tests, a representative compound of the invention, 3,5-dihydroxy-4-isopropylstilbene, showed activity in reducing or eliminating psoriasis symptoms.

[0122] The composition of the present invention comprises an antipsoriatic amount of a compound of formula I or formula II, and a suitable pharmaceutical carrier. An antipsoriatic amount is defined as the amount of compound necessary to eliminate psoriatic symptoms, ie psoriatic lesions. In the usual course of treatment, the active compound is incorporated into an acceptable carrier to form a composition for topical administration to the affected area, or into a composition suitable for oral administration. in the form of ca...

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PUM

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Abstract

Disclosed herein are compositions containing hydroxylstilbenes or their derivatives or analogues. The compositions are useful to inhibit protein kinease, and for the treatment of inflammatory diseases, including psoriasis, multiple sclerosis, rhumatoid arthritis, restinosis, inflammatory bowel disease, and inflammatory lung disease. They are also useful to treat surgical adhesions and graft rejection. Novel derivatives and analogues are also disclosed.

Description

Background of the invention [0001] Stilbenes isolated from phobic rod-type bacteria have antimicrobial activity. See V.J.Paul, S.Frautschv, W.Fenical, K.H.Nealson,. Journal of Chemical Ecology, 7:589-597 (1981); K.Hu, J.Li, W.Wang, H.Wu, H.LinJ.M . Webster, Canadian Journal of Microbiology, 44: 1072-1077 (1998). However, these compounds have not been shown to have other biological activities. One analogue, resveratrol, however, has been disclosed as having anticancer activity (Jang et al., 1997) and inhibiting activity of protein-activating enzymes (Garcia-Garcia et al., 1999). [0002] There are many common conditions that cannot be successfully treated with antibiotics. Some of the diseases that cannot be treated are inflammation. However, the compounds of the present invention have specific anti-inflammatory properties. [0003] Inflammatory diseases, whether chronic or acute, represent a fundamental class of problems in healthcare. Chronic inflammation is considered ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K9/08A61K31/05A61K31/336A61K31/36A61K47/06A61K47/10A61K47/12A61K47/14A61P3/10A61P9/00A61P9/10A61P17/06A61P29/00A61P35/00A61P35/04A61P43/00C07D303/14C07D303/16C07D303/20C07D303/22C07D405/04C07D407/04
CPCC07D303/14A61K47/14A61K31/336A61K31/05A61K47/06C07D303/16A61K47/12C07D405/04A61K47/10A61K9/0014C07D303/22A61P17/06A61P29/00A61P3/10A61P35/00A61P35/04A61P43/00A61P9/00A61P9/10Y02A50/30A61K9/0019A61K31/047
Inventor 陈庚辉约翰·麦尔康姆·韦伯斯特李建雄胡凯基朱江
Owner BEIJING WEN FENG TIANJI PHARMA CO LTD
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