Five-membered ring compounds

Details Five-membered ring compounds Five-membered ring compounds

C - Chemistry, Metallurgy

07

D

C07D 277/42 (2006.01) A61K 31/421 (2006.01) A61K 31/426 (2006.01) A61K 31/427 (2006.01) A61K 31/4439 (2006.01) A61K 31/4709 (2006.01) A61K 31/4725 (2006.01) A61K 31/498 (2006.01) A61K 31/506 (2006.01) A61K 31/5377 (2006.01) A61P 29/00 (2006.01) A61P 37/06 (2006.01) A61P 37/08 (2006.01) C07D 263/48 (2006.01) C07D 277/56 (2006.01) C07D 417/04 (2006.01) C07D 417/12 (2006.01) C07D 417/14 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2413000

The present invention is directed to a 5-membered cyclic compound of the formula: (see above formula) wherein X is oxygen or sulfur, R1 is hydrogen, substituted or unsubstituted alkyl, etc., R2 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, etc., Y1 is a direct bond, substituted or unsubstituted alkylene, -CO(CH2)n-, etc., the wavy line means (E)-configuration or (Z)-configuration, R3 is substituted or unsubstituted aryl, etc., Y2 is substituted or unsubstituted alkylene, etc., R4 is hydrogen, substituted or unsubstituted alkanoyl, substituted or unsubstituted alkyl, etc., R5 is hydrogen, etc., or a salt thereof. These compounds being able to inhibit infiltration of leukocytes such as eosinophils and lymphocytes, and are, therefore, useful for the treatment of various kinds of inflammation.

L'invention concerne un composé annulaire à cinq chaînons représenté par la formule (I) ou un sel de celui-ci: dans laquelle X désigne un oxygène ou un soufre; R1 désigne un hydrogène, un alkyle (non)substitué, etc.; R2 désigne un hydrogène, un alkyle (non)substitué, un aryle (non)substitué, etc.; Y1 désigne une liaison simple, un alkylène (non)substitué, -CO(CH2)n-, etc.; le trait ondulé désigne la configuration (E) ou (Z), R3 désigne un aryle (non)substitué, etc.; Y2 désigne un alkylène (non)substitué; R4 désigne un hydrogène, un alkanoyle (non)substitué, un alkyle (non)substitué, etc. et R5 désigne un hydrogène, etc. Ces produits inhibent une infiltration des leucocytes, tels que des éosinocytes et des lymphocytes, et sont, par conséquent, utiles pour le traitement de plusieurs types d'inflammation.

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