C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 491/04 (2006.01) A61K 31/55 (2006.01) A61P 29/00 (2006.01) C07D 495/04 (2006.01)
Patent
CA 2485212
The present invention relates to 1-aza-dibenzoazulene derivatives of formula I, to their pharmacologically acceptable salts and solvates, to process and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumour necrosis factor-.alpha. (TNF- .alpha.) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action. Wherein X may be CH2 or a hetero atom such as 0, S, S(=0), S(=0)2, or NRa, wherein Ra is hydrogen or a protecting group; RI may be hydrogen, halogen, an optionally substituted C1-C7 alkyl or C2-C7 alkenyl, C2-C7 alkinyl, an optionally substituted aryl or heteroaryl and a heterocycle, hydroxy, hydroxy-C2-C7 alkenyl, hydroxy-C2-C7 alkinyl, C1-C7 alkoxy, thiol, thio-C2-C7 alkenyl, thio-C2-C7 alkinyl, C1-C7 alkylthio, amino, N-(C1~-C7)alkylamino, N,N-di(C1-C7-a1kyl)amino, (C1-C7-alkyl)amino, amino-C2- C7 alkenyl, amino-C2-C7 alkinyl, amino-C1,-C7 alkoxy, C1-C7 alkanoyl, aroyl, oxo~C1-C7 alkyl, C1-C7 alkanoyloxy, carboxy, an optionally substituted C1-C7 alkyloxycarbonyl or aryloxycarbonyl, carbamoyl, N-(C1-C7-alkyl)carbamoyl, N,N- di(C1-C7-alkyl)carbamoyl, cyano, cyano-C1-C7 alkyl, sulfonyl, C1-C7 alkylsulfonyl, sulfinyl, C1-C7 alkylsulfinyl, nitro, or a substituent of the formula II.
La présente invention concerne des dérivés de 1-aza-dibenzoazulène de formule (I), leurs sels et solvats pharmacologiquement acceptables, une méthode et des intermédiaires destinés à leur préparation ainsi que leurs effets inflammatoires, en particulier l'inhibition de la production du facteur de nécrose tumorale alpha (TNF-?) et l'inhibition de la production de l'interleukine 1 (IL-1) ainsi que leur action analgésique. Dans ladite formule, X peut être CH¿2? ou un hétéroatome tel que 0, S, S(=0), S(=0)¿2?, ou <I>NR</I>?a¿ (R?a¿ étant hydrogène ou un groupe protecteur); R<SP>I</SP> peut être hydrogène, halogène, un alkyle C¿1?-C¿7? ou alcényle C¿2?-C¿7? éventuellement substitué, alkinyle C¿2?-C¿7?, un aryle ou hétéroaryle éventuellement substitué et un hétérocycle, hydroxy, hydroxy-alcényle C¿2?-C¿7?, hydroxy-alkinyle C¿2?-C¿7?, alkoxy C¿1?-C¿7?, thiol, thio-alcényle C¿2?-C¿7?, thio-alkinyle C¿2?-C¿7?, alkylthio C¿1?-C¿7?, amino, <I>N</I>-alkylamino(C¿1?-C¿7?), <I>N,N</I>-di(alkyle C¿1?-C¿7?)amino, (alkyle C¿1?-C¿7?)amino, amino-alcényle C¿2?-C¿7?, amino-alkinyle C¿2?-C¿7?, amino-alkoxy C¿1?-C¿7?, alcanoyle C¿1?-C¿7?, aroyle, oxo-alkyle C¿1?-C¿7?, alcanoyloxy C¿1?-C¿7?, carboxy, alkyloxycarbonyle ou aryloxycarbonyle C¿1?-C¿7? éventuellement substitué, carbamoyle, N-(alkyle C¿1?-C¿7?)carbamoyle, N,N-di(alkyle C¿1?-C¿7?)carbamoyle, cyano, cyano-alkyle C¿1?-C¿7?, sulfonyle, alkylsulfonyle C¿1?-C¿7?, sulfinyle, alkylsulfinyle C¿1?-C¿7?, nitro, ou un substituant de formule (II).
Mercep Mladen
Mesic Milan
Pesic Dijana
Borden Ladner Gervais Llp
Pliva-Istrazivacki Institut D.o.o.
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