ANTAGONISTS OF ALPHAVBETA3 AND ALPHAVBETA6 INTEGRINS AND ANTIFIBROTIC AGENTS Russian patent published in 2010 - IPC A61K31/44 A61P1/16 

Abstract RU 2388472 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention proposes application of αγβ integrn antagonist for obtainig a remedy for treatment of hepatic billary fibrosis, the antagonist being 3-{3-benziloxy-2-[5-(pyridine-2-ylamino) pentanoylamino]propanoylamino}-3-(3.5-dichlorphenyl)-propionic acid It is demonstrated that the compound inhibits αv integins, particularly αvβ3 and αvβ6 integrins, effect decreasing regulation of fibrogenesis through inhibiting cellular migration and migration of profibrogen molecules (e.g. collagenase, TMP-1), and cytokines (e.g., CTGF) with the help of activated stellar hepatic cells /miofibroblasts, activated epithelium and endothelium.

EFFECT: antagonist can effectively prevent, reduce or even cause regression of secondary hepatic billary fibrosis by reducing total amount of collagen in the liver by 50-70% after 5-6 week-long occlusion of the bile duct.

7 dwg, 1 tbl

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RU 2 388 472 C2

Authors

Gudman Zimon

Shuppan Detlef

Patzenker Ehleonora

Popov Jurij

Bauer Mikhaehl'

Vizner Mattias

Jonchik Al'Fred

Dates

2010-05-10Published

2004-09-16Filed