Novel propenohydroxamic acid derivatives

Details Novel propenohydroxamic acid derivatives Novel propenohydroxamic acid derivatives

C - Chemistry, Metallurgy

07

C

C07C 259/06 (2006.01) A61K 31/17 (2006.01) A61K 31/18 (2006.01) A61K 31/44 (2006.01) A61K 31/4402 (2006.01) A61K 31/4406 (2006.01) A61K 31/4409 (2006.01) A61K 31/4453 (2006.01) A61K 31/47 (2006.01) A61P 1/04 (2006.01) A61P 3/10 (2006.01) A61P 19/02 (2006.01) A61P 29/00 (2006.01) A61P 31/04 (2006.01) A61P 35/00 (2006.01) A61P 37/06 (2006.01) A61P 43/00 (2006.01) C07C 275/34 (2006.01) C07C 275/42 (2006.01) C07C 311/08 (2006.01) C07C 311/13 (2006.01) C07C 311/21 (2006.01) C07C 311/29 (2006.01) C07C 311/44 (200

Patent

CA 2423733

Propenohydroxamic acid derivatives represented by the following general formula (1) or salts thereof and drugs containing the same: (1) wherein R1 represents hydrogen, alkyl or halogeno; R2 represents cycloalkyl, aryl, heteroaryl, etc.; R3 represents hydrogen, alkenyl, etc.; R5 represents R6CO-, R6SO2-, R6NHCO- or R6NHCS- (wherein R6 represents alkyl, cycloalkyl, cyclic amino, aryl, heteroaryl, etc.); R7 represents hydrogen or a protective group; and A represents CH, nitrogen or oxidized nitrogen. Because of having an excellent TACE inhibitory activity, the above compounds are useful as drugs for preventing and/or treating diseases such as sepsis, rheumatoid arthritis, arthritis deformans, infectious diseases, autoimmune diseases, malignant neoplasm, collagen disease, ulcerative colitis, MOF, non-insulin-dependent diabetes mellitus, etc.

L'invention concerne des dérivés d'acide propénohydroxamique représentés par la formule générale (1), ou des sels de ces dérivés, ainsi que des médicaments les contenant. Dans la formule (1), R?1¿ représente hydrogène, alkyle ou halogéno ; R?2¿ représente cycloalkyle, aryle, hétéroaryle, etc. ; R?3¿ représente hydrogène, alcényle, etc. ; R?5¿ représente R?6¿CO-, R?6¿SO¿2?, R?6¿NHCO- ou R?6¿NHCS- (R?6¿ représentant alkyle, cycloalkyle, amino cyclique, aryle, hétéroaryle, etc.) ; R?7¿ représente hydrogène ou un groupe protecteur ; et A représente CH, azote ou azote oxydé. En raison de leur excellente activité inhibitrice de TACE, lesdits composés s'utilisent comme médicaments pour prévenir et/ou traiter des maladies telles que la sepsie, la polyarthrite rhumatoïde, la polyarthrite déformante, les maladies infectieuses, les maladies auto-immunes, le néoplasme malin, la maladie du collagène, la colite ulcéreuse, la défaillance polyviscérale, le diabète non insulino-dépendant, etc.

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