C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 213/90 (2006.01) A61K 31/381 (2006.01) A61K 31/44 (2006.01) C07C 233/80 (2006.01) C07D 213/82 (2006.01) C07D 333/38 (2006.01)
Patent
CA 2513408
Objects of the present invention are new mono-acylated o-phenylendiamines derivatives of formula (A) wherein Ar is thiophen-2,5-diyl, pyridine-2,5-diyl, pyridine-5,2-diyl, pyridine-2,6-diyl, pyridine-2,4-diyl or 1,4-phenylene, R1, R2 independently from each other represent hydrogen, C1-12-alkyl, C2-12- alkenyl, C2-12-alkynyl, C3-12-cycloalkyl, the alkyl, alkenyl, alkynyl and cycloalkyl groups being optionally mono or multiple substituted by hydroxy, halogen, C3-12-cycloalkyl, alkoxy, alkylsulfanyl, acyloxy, alkoxycarbonyl, acyl, C1-6-alkyl-NH-C(O)-, C1-6-alkyl-C(O)NH- or -NR3R4, or alternatively R1 is hydrogen, and R2 is hydroxyl, alkoxy, C2-C12-alkenyloxy or phenoxy, which phenoxy group is optionally substituted with methyl, methoxy, halogen, nitro, cyano, trifluoromethyl, ethenyl or -C(O)-O-CH3, provided that if R2 is hydroxy, Ar is not thiophen-2,5-diyl; and R3 and R4 independently from each other represent hydrogen or C1-6-alkyl, or wherein R3 and R4 together with the nitrogen-atom to which they are attached form a ring, which ring is monosubstituted by oxo and which ring may contain a further heteroatom, and pharmaceutically acceptable salts thereof, as well as processes for the manufacturing of these compounds, pharmaceutical compositions containing such compounds and their use in the manufacture of drugs for the treatment of diseases such as cancer.
La présente invention concerne de nouveaux dérivés d'o-phénylendiamines monoacylées de la formule (A) dans laquelle Ar est thiophène-2,5-diyle, pyridine-2,5-diyle, pyridine-5,2-diyle, pyridine-2,6-diyle, pyridine-2,4-diyle ou 1,4-phénylène, R?1¿, R?2¿ indépendamment l'un de l'autre représentent un hydrogène, un alkyle C¿1-12?, alcényle C¿2-12?, alkynyle C¿2-12?, cycloalkyle C¿3-12?, les groupes alkyle, alcényle, alkynyle et cycloalkyle présentant facultativement une ou plusieurs substitutions par un hydroxy, halogène, cycloalkyle C¿3-12?, alcoxy, alkylsulfanyle, acyloxy, alcoxycarbonyle, acyle, C¿1-6?-alkyle-NH-C(O)-, C¿1-6?-alkyle-C(O)NH- ou -NR?3¿R?4¿, ou dans un autre mode de réalisation, R?1¿ est un hydrogène, et R?2¿ est un hydroxyle, alcoxy, C¿2-?C¿12?-alcényloxy ou phénoxy, lequel groupe phénoxy est facultativement substitué par un méthyle, méthoxy, halogène, nitro, cyano, trifluorométhyle, ethényle ou -C(O)-O-CH¿3?, à condition que si R?2¿ est un hydroxy, Ar n'est pas thiophène-2,5-diyle; et R?3¿ et R?4¿ indépendamment l'un de l'autre représentent un hydrogène ou un alkyle C¿1?-¿6?, ou dans laquelle R?3¿ et R?4¿ forment ensemble un noyau avec l'atome d'azote auquel ils sont attachés, lequel noyau est monosubstitué par un oxo et peut contenir un autre hétéroatome, et les sels pharmaceutiquement acceptables de ces derniers, de même que des procédés de fabrication desdits composés, des compositions pharmaceutiques contenant lesdits composés et leur utilisation dans la fabrication de médicaments destinés au traitement de maladies telles que le cancer.
Fertig Georg
Herting Frank
Kubbies Manfred
Limberg Anja
Reiff Ulrike
F.hoffmann-La Roche Ag
Gowling Lafleur Henderson Llp
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