New substituted amides, their production and their use

Details New substituted amides, their production and their use New substituted amides, their production and their use

C - Chemistry, Metallurgy

07

C

C07C 311/21 (2006.01) A61K 31/19 (2006.01) A61K 31/195 (2006.01) A61K 31/44 (2006.01) A61K 31/505 (2006.01) C07C 233/76 (2006.01) C07C 235/82 (2006.01) C07C 237/52 (2006.01) C07D 213/56 (2006.01) C07D 215/36 (2006.01) C07D 239/70 (2006.01) C07D 239/96 (2006.01)

Patent

CA 2328435

The invention relates to amides of general formula (I) and their tautomeric and isomeric forms, their possible enantiomeric and diastereomeric forms and possible physiologically compatible salts, where the variables have the following meanings: R1 is C1-C6 alkyl, phenyl, naphthyl, quinolyl, pyridyl, pyrimidyl, pyridazyl, quinazolyl and quinoxalyl, whereby the rings can still be substituted with up to 2 R4 rests; R2 is -(CH2)m-R8, where R8 is phenyl, cyclohexyl or indolyl and m is 1 to 6; X is a bond, -CH2-, -CH2CH2-, -CH=CH-, - CC-, -CONH-, -, -SO2NH-, and R1-X together can also be formula (a), R3 is hydrogen and CO-NR6R7; R4 is hydrogen, branched or unbranched C1-C4 alkyl and O-C1-C4-alkyl; R5 is hydrogen, branched or unbranched C1-C4 alkyl and O-C1-C4- alkyl; R6 is hydrogen, branched or unbranched C1-C6 alkyl; R7 is hydrogen, branched or unbranched C1-C6 alkyl; and n is 0, 1 or 2. The amides of formula (I) are inhibitors of enzymes, especially cysteine proteases such as calpains (calcium dependent cysteine proteases) and their isoenzymes and cathepsins, such as B and L.

L'invention concerne des amides de la formule (I) et leurs formes tautomères et isomères, leurs éventuelles formes énantiomères et diastéréomères ainsi que leurs sels physiologiquement compatibles, où les variables ont la signification suivante : R1 représente alkyle C¿1?-C¿6?, phényle, naphtyle, quinolyle, pyridyle, pyrimidyle, pyridazyle, quinazolyle et quinoxalyle, les cycles pouvant encore être substitués par maximum 2 restes R4, R2 représente (CH¿2?)¿m?-R8, R8 représentant du phényle, cyclohexylindolyle ou indolyle et m vaut 1 à 6, et X représente une liaison, -CH¿2?-, -CH¿2?CH¿2?-, -CH=CH-, -C?C-, -CONH-, -, SO¿2?NH, R1 et X ensemble représentent formule (a) et R3 représente de l'hydrogène et CO-NR6R7, R4 représente de l'hydrogène, alkyle C1-C4, ramifié ou non ramifié et O-C1-C4 alkyle; R5 représente de l'hydrogène, alkyle C1-C4, ramifié ou non ramifié et O-C1-C4 alkyle; R6 représente de l'hydrogène, alkyle C¿1?-C¿6?, ramifié ou non ramifié et R7 représente de l'hydrogène, alkyle C¿1?-C¿6?, ramifié ou non ramifié et n vaut 0, 1 ou 2. Les amides de la formule (I) sont des inhibiteurs d'enzymes, notamment de protéases de cystéine, telles que la calpaïne (= protéases de cystéine dépendant du calcium) et ses iso-enzymes et cathépsines, par exemple, B et L.

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