Application of 3-(benzoyl phenyl) propionic acid derivative in treatment of connexin CX31 mediated skin diseases

A cyclopentyloxybenzoyl, skin disease technology, applied in the field of pharmacy, can solve problems such as poor curative effect

Inactive Publication Date: 2015-04-29
TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE +1
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  • Abstract
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  • Claims
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Problems solved by technology

[0010] Therefore, aiming at the problem of poor curative effect of drugs used to treat connexin CX31-mediated skin diseases in the prior art, the present invention provides 3-{[2-[3-oxo-(1,2-benzoisoxan Azol-6-yl)methoxy]-5-[(2-hydroxy-4-cyclop...

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  • Application of 3-(benzoyl phenyl) propionic acid derivative in treatment of connexin CX31 mediated skin diseases
  • Application of 3-(benzoyl phenyl) propionic acid derivative in treatment of connexin CX31 mediated skin diseases
  • Application of 3-(benzoyl phenyl) propionic acid derivative in treatment of connexin CX31 mediated skin diseases

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Embodiment Construction

[0021] The following will clearly and completely describe the technical solutions in the embodiments of the present invention with reference to the accompanying drawings in the embodiments of the present invention. Obviously, the described embodiments are only some, not all, embodiments of the present invention. All other embodiments obtained by persons of ordinary skill in the art based on the embodiments of the present invention belong to the protection scope of the present invention.

[0022] 1. Chemical synthesis part

[0023] 1.1 Synthesis of 6-[(2,4-methoxyphenyl)carbonyl]-coumarin

[0024] Add 25g of 6-methylcoumarin and chlorobenzene (25mL) into 62.5% sulfuric acid (150mL), stir and heat up. At 70-90°C, add 30g of active manganese dioxide in 8 times, and add 62.5% sulfuric acid (19mL) dropwise at 70-90°C. Control the temperature at 80-90°C and stir for 1h. Cool to room temperature. Add about 150mL of water, dropwise add 43mL of 20% ammonia water, 100mL of ethyl a...

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Abstract

The invention provides an application of a 3-[[2-[3-oxo-(1, 2-benzisoxazole-6-yl) methoxyl]-5-[(2-hydroxyl-4-cyclopentoxyl benzoyl)] phenyl] propionic acid (compound I) in preparation for treatment of connexin CX31 mediated skin disease. The connexin CX31 mediated skin disease comprises erythrokeratodermia variabilis or psoriasis. The pharmacological experiment proves that a low-dose group and a high-dose group of the compound I can remarkably reduce skin damage degree of a psoriasis animal sample; the content of TNF-alpha in murine serum can be restrained by the low-dose group of the compound I, then inflammatory cell infiltration is restrained, the inflammatory response is relieved, and the compound I has good psoriasis treatment effect and can be used for treating the connexin CX31 mediated skin disease.

Description

technical field [0001] The present invention relates to the field of pharmacy, in particular to 3-{[2-[3-oxo-(1,2-benzisoxazol-6-yl)methoxy]-5-[(2-hydroxyl- Application of 4-cyclopentyloxybenzoyl)]phenyl}propionic acid compound in the preparation and treatment of skin diseases mediated by connexin CX31. Background technique [0002] Psoriasis, commonly known as "psoriasis", is a common chronic inflammatory skin disease characterized by scaly erythema. The age of onset is mostly young adults, and men are slightly more than women. It has characteristic red papules, plaques, and silvery white scales, which tend to occur on the scalp and extremities. The onset has obvious seasonality, and it is easy to recur or aggravate in spring and winter, and it is usually relieved in summer and autumn. Clinically divided into two types of psoriasis vulgaris and unusual psoriasis. Unusual psoriasis includes pustular, articular, and erythrodermic types, which are relatively rare, accounting...

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Application Information

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IPC IPC(8): A61K31/423A61P17/00A61P17/06
Inventor 饶子和张灼华杨诚陈卫强王丹玲张炜程夏昆付文华赵佩佩
Owner TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE
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