Novel sulfonic acid derivative and medicinal use thereof

Details Novel sulfonic acid derivative and medicinal use thereof Novel sulfonic acid derivative and medicinal use thereof

C - Chemistry, Metallurgy

07

D

C07D 307/93 (2006.01) A61K 31/34 (2006.01) A61K 31/395 (2006.01) C07D 405/04 (2006.01)

Patent

CA 2123890

The present invention discloses sulfonamide derivative represented by the following general formula: (see fig. I) [wherein, R1 is (i) -COOR2 (where, R2 is (1) hydrogen, (2) a pharmacologically acceptable cation, or (3) an alkyl having 1 to 14 carbon atoms) or, (ii) -C(=O)-R3 (wherein, R3 represents an alkyl having 1 to 4 carbon atoms); A is (i) -(CH2)n- (wherein, n represents an integer of 0 to 3), (ii) -CH=CH-, or the group: (iii) -O-C(R4)(R5)- (wherein, R4 and R5 represent (1) hydrogen or (2) an alkyl having 1 to 4 carbon atoms, and R4 and R5 may be identical or different); and, W is NH or -O-], as well as a thromboxane A2 receptor antagonistic drug having said derivative for its active ingredient. Since the compound of the present invention has excellent thromboxane A2 receptor antagonistic action, it can be used as a thromboxane A2 receptor antagonist of high activity and long duration.

La présente invention porte sur un dérivé du sulfonamide de formule générale : (voir fig. I) [où, R1 est (i) -COOR2 (où, R2 est (1) un atome d'hydrogène, (2) un cation pharmacologiquement acceptable ou (3) un alkyle comptant de 1 à 14 atomes de carbone) ou (ii) -C(=O)-R3 (où, R3 représente un alkyle de 1 à 4 atomes de carbone); A est (i) -(CH2)n- (où, n représente un nombre entier variant de 0 à 3), (ii) -CH=CH- ou le groupe : (iii) -O-C(R4)(R5)- (où, R4 et R5 représentent (1) un atome d'hydrogène ou (2) un alkyle de 1 à 4 atomes de carbone, et R4 et R5 peuvent être identiques ou différents); et W est NH ou -O-]; la présente invention porte également sur un médicament qui est un antagoniste du récepteur de la thromboxane A2 possédant ledit dérivé comme ingrédient actif. Comme le composé de la présente invention possède une excellente activité antagoniste du récepteur de la thromboxane A2, il peut être utilisé comme antagoniste de haute activité et de longue durée de ce récepteur.

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