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Hydrolase inhibitor of adenosine homeotypic cysteamine acid and usage

A technology of medicament and emulsion, which is applied in the direction of emulsion delivery, skin diseases, anti-tumor drugs, etc., and can solve problems such as no effect

Inactive Publication Date: 2005-06-15
BEIJING STRONG BIOTECH INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

TRIAZURE.TM (triacetoxy 6-azuridine) has been tested topically on the skin of patients with lupus erythematosus, but had no effect (William Drell, personalcommunication, May, 1993)
There are no reports on the use of adenosylhomocysteine ​​hydrolase inhibitors DHCaA or DHCeA, and their 3-nitrogen analogues, in the treatment of lupus erythematosus or other skin diseases caused by excessive epithelial cell proliferation

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0112] Application of adenosine homocysteine ​​hydrolase inhibitor with anti-proliferative effect on EFAD mouse model

[0113] Adenosylhomocysteine ​​hydrolase inhibitors of antiproliferative nucleoside analogues are prepared by the methods described above. 9-[(1'R, 2'S, 3'R)-2', 3'-dihydroxycyclopentyl]adenine (DHCaA), 9-(trans-2', trans-3'-dihydroxy Cyclopent-4'-enyl ester) adenine (DHCeA) and their 3-nitrogen analogs were individually made into topical polyethylene ointments, as described above, including from 0.001 gm% to 10 gm% propylene glycol Active ingredients in solids, macrogol 400 and macrogol 3350, for the manufacture of ointment mixtures. Similar formulations containing ingredients that enhance skin penetration (eg, dimethyl sulfoxide or AZONE.TM.) can also be made.

[0114] 9-[(1'R, 2'S, 3'R)-2', 3'-dihydroxycyclopentyl]adenine (DHCaA), 9-(trans-2', trans-3'-dihydroxy The ointment of cyclopent-4'-enyl ester) adenine (DHCeA) and their 3-position nitrogen analog...

Embodiment 2

[0120] Application of DHCaA and DHCeA with anti-proliferative effect on mice transplanted with lupus human skin

[0121] Skin biopsies were used to examine the antiproliferative effects of 5-fluorodeoxyuridine triphosphate and 5-fluorouridine triphosphate when applied topically to athymic mice grafted with human lupus erythematosus skin. Human lupus erythematosus skin approximately 1-10 mm in diameter was grafted onto the back of athymic mice using techniques well known in the literature. After sufficient transplantation, lupus erythematosus human skin is treated with an anti-lupus erythematosus drug comprising DHCaA or DHCeA as an active ingredient. These compounds were synthesized using the method described in Example 1. Drug manufacture with externally applied polyethylene ointment comprising the active ingredient, by the method described previously, with a concentration of 0.1 gm% to 10 gm% of the active ingredient. The ointment containing the active ingredient is extern...

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Abstract

An adenosine homotype of cysteine hydrolase depressant, 9-[(1'R, 2', S, 3'R)-2',3'-dihydroxycyclopentyl] adenine (DHCaA), 9-(trans-2', trans-3'-dihydroxycyclopentyl-4'-enylester) adenine (DHCeA) and its 3-site nitrogen analog is disclosed. It can be used to treat lupus erythematosus and allergic dermatitis.

Description

technical field [0001] The present invention relates to an adenosylhomocysteine ​​hydrolase inhibitor, suitable for external application of pharmaceutical formulations and uses thereof, the pharmaceutical formulation has a therapeutic effect on lupus erythematosus and other diseases caused by excessive proliferation of epithelial cells, external application contains adenosine Glycoside homocysteine ​​hydrolase inhibitors DHCaA or DHCeA, and 3-nitrogen analogs thereof. Background technique [0002] Lupus erythematosus is a benign human skin disorder generally characterized by thickened plaques overlaid with thin scales of skin. The disease is caused by increased epidermal cell proliferation for unknown reasons. For normal skin, it takes about 5 weeks for cells to move from the base layer to the upper granular layer. For the skin of lupus erythematosus, it only needs 6 to 9 days, the reason is due to the increase in the number of proliferating cells and the increase in the p...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/52A61P17/00A61P17/12A61P35/00
Inventor 余凯茜刘希
Owner BEIJING STRONG BIOTECH INC
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