New benzimidazol, benzoxazol and benzothiazol derivitives,...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 401/12 (2006.01) A61K 31/41 (2006.01) A61K 31/435 (2006.01) C07D 235/06 (2006.01) C07D 235/10 (2006.01) C07D 235/12 (2006.01) C07D 235/14 (2006.01) C07D 263/56 (2006.01) C07D 277/64 (2006.01) C07D 401/06 (2006.01) C07D 401/14 (2006.01) C07D 403/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2211444

The invention concerns new compounds based on the general formula (I): (see fig. I) in which R1 represents a halogen atom, a hydroxy group, linear or ramified alkoxy (C1-C6), trihalogenomethyl amino, sulphydryl, linear or ramified alkylthio (C1-C6), linear or ramified trialkylammonium (C1-C6), aryloxy, arylthio, arylsulfonyl, arylsulfonyl- oxy, cycloalkyl (C3-C7) oxy, cycloalkyl (C3-C7) thio, bicycloalkyl (C6-C8) oxy or bicycloalkyl (C6-C8) thio, Ra/Rb, identical or different, representing a hydrogen atom or a linear or ramified alkyl group (C1-C6); X represents an atom of hydrogen or sulphur or an NR group, R representing a hydrogen atom or a linear or ramified alkyl group (C1-C6); Y represents a group--(CH2)m-Z-(CH2)n--in which m is 0, 1 or 2, n is 0, 1 or 2 and Z is an atom of oxigen or sulphur or an amino group, a group -SO2-, -CHOH-, -CH2- or CH(CH2OH)-; and R2 represents an aryl group, and their isomers as well their salts added to a pharmaceutically acceptable base or acid. The formula (I) compounds are powerful inhibiters of interleukin 1.beta. (IL1.beta.).

L'invention concerne de nouveaux composés répondant à la formule générale (I): (see fig. I) dans laquelle R1 représente un atome d'halogène, un groupement hydroxy, alkoxy (C1-C6) linéaire ou ramifié, trihalogénométhyle amino, mercapto, alkylthio (C1-C6) linéaire ou ramifié, trialkylammonium (C1-C6) linéaire ou ramifié, aryloxy, arylthio, arylsulfonyle, arylsulfonyl- oxy, cycloalkyl (C3-C7) oxy, cycloalkyl (C3-C7) thio, bicycloalkyl (C6-C8) oxy ou bicycloalkyl (C6-C8) (C6-C8) thio, Ra/ Rb, identiques ou différents, représentent un atome d'hydrogène ou un groupement alkyle (C1-C6) linéaire ou ramifié; X représente un atome d'oxygène ou de soufre ou un groupement NR, R représentant un atome d'hydrogène ou un groupement alkyle (C1-C6) linéaire ou ramifié; Y représente un groupement -(CH2)m-Z-(CH2)n- dans lequel m représente 0, 1 ou 2, n représente 0, 1 ou 2, et Z représente un atome d'oxygène ou de soufre ou un groupement amino, un groupement -SO2-, -CHOH-, -CH2- ou - CH(CH2OH)-; et R2 représente un groupement aryle, et leurs isomères ainsi que leurs sels d'adition à un acide ou à une base pharmaceutiquement acceptable. Les composés de formule (I) sont de puissants inhibiteurs de l'interleukine 1.beta. (IL1.beta.).

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