C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/12 (2006.01) A61K 31/502 (2006.01) C07C 65/30 (2006.01) C07C 65/32 (2006.01) C07D 239/32 (2006.01) C07D 239/34 (2006.01)
Patent
CA 2562100
The invention relates to 1-amino-phthalazine derivatives of general formula (I), wherein A, B = possibly substituted C¿1-4?-alkylene; L = a simple bond or C¿1-2?-alkylene, possibly substituted -CH=CH-, or -C=C- or cycloprop-1,2--diyl; R¿1? = possibly substituted aryl or heteroaryl; R¿2?, R¿3? = H, C¿1-3?-alkyl, C¿1-3?-fluoralkyl or R¿2? et R¿3? forming together with a bearing them carbon atom, a cycloprop-1,1-diyl; R¿4? = H, C¿1-5?-alkyl, C¿1-3?-fluoralkyl, C¿3?-¿6?-cycloalkyl, C¿3-6?-cycloalkyl-C¿1-3?-alkylene, C¿1-3?-alkyl-O-C¿1-3?-alkylene, HO-C¿1-3?-alkylene, C¿1-3?-alkyl-X-C¿1-3?-alkylene, wherein X = S, SO or S0¿2?; or R¿4? = R¿a?R¿b?N-C¿1?-¿3?-alkylene, aryl, aryl-C¿1?-¿3?-alkylene, aryl-O-, aryl-O-C¿1-3?-alkylene, aryl-C¿1-3?-alkylene-O-C¿1-3?-alkylene, heteroaryl or heteroaryl-C¿1-3?-alkylene; R¿5? = H, halogen, C¿1?-¿5?-alkyl, C¿1?-¿3?-fluoralkyl, C¿1-5?-alkoxy, C¿1-3?-fluoroalkoxy, HO-C¿1-3?-alkylene, -CN, C¿1-3?-alkyl-X-, wherein X = S, SO or SO¿2?; or R¿5? = R¿a?R¿b?N-, R¿a?R¿b?N-C¿1-3?-alkylene, aryl, aryl-C¿1-3?-alkylene, aryl-O- or heteroaryl; R¿6? = H, halogen, C¿1-5?-alkyl, C¿1-3?-fluoralkyl, C¿1-5?-alkoxy, C¿1-3?-fluoroalkoxy, -CN, R¿a?R¿b?N-, R¿a?R¿b?N-C¿1-3?-alkylene, aryl or heteroaryl ; R¿7? = H, halogen, C¿1?-¿5?-alkyl, C¿1-3?-fluoralkyl, C¿1-5?-alkoxy, C¿1-3?-fluoroalkoxy, HO-C¿1-3??-¿-alkylene, -CN, C¿1-3?-alkyl-X-, wherein X = S, SO or SO¿2?; or R¿7?, = R¿a?R¿b?N-, R¿a?R¿b?N-C¿1-3?--alkylene, R¿e?R¿b?NC(O)-, C¿1-3?-alkyl-C(O)-, aryl, aryl-0- or heteroaryl ; R¿8? = H, halogen, C¿1-5?-alkyl, C¿1-5?-alkoxy, C¿1-3?-fluoroalkoxy ; in the form of base or acid additional salt and in the form of a hydrate or solvent. A method for preparing and using the inventive derivatives for therapeutically purpose is also disclosed.
L'invention concerne des dérivés de la 1-amino-phthalazine, de formule générale (I) dans laquelle A, B = C1-4-alkylène éventuellement substitué ; L = liaison simple ou C1-2-alkylène, -CH=CH- éventuellement substitués, ou - C.ident.C- ou cycloprop-1,2~-diyle ; R1 = aryle ou hétéroaryle éventuellement substitués ; R2, R3 = H, C1-3-alkyle, C1-3-fluoroalkyle ou R2 et R3 forment ensemble, avec l'atome de carbone qui les porte, un cycloprop-1,1-diyle ; R4 = H, C1-5-alkyle, C1-3-fluoroalkyle, C3-6-cycloalkyle, C3-6-cycloalkyle-C1-3- alkylène, C1-3-alkyle-O-C1-3-alkylène, HO-C1-3-alkylène, C1-3~alkyle-X-C1-3- alkylène où X = S, SO ou S02; ou R4 = RaRbN-C1-3-alkylène, aryle, aryle-C1-3- alkylène, aryle-O-, aryle-O-C1-3-alkylène, aryle-C1-3-alkylène-O-C1- 3~alkylène, hétéroaryle ou hétéroaryle-C1-3-alkylène ; R5 = H, halogène, C1-5- alkyle, C1~3-fluoroalkyle, C1-5-alcoxy, C1-3-fluoroalcoxy, HO-C1-3-alkylène, - CN, C1-3-alkyle-X- où X = S, SO ou SO2; ou R5 = RaRbN-, RaRbN-C1-3-alkylène, aryle, aryle-C1-3-alkylène, aryle-O- ou hétéroaryle ; R6 = H, halogène, C1-5- alkyle, C1-3-fluoroalkyle, C1-5-alcoxy, C1-3-fluoroalcoxy, -CN, RaRbN-, RaRbN- C1-3-alkylène, aryle ou hétéroaryle ; R7 = H, halogène, C1-5-alkyle, C1-3- fluoroalkyle, C1-5-alcoxy, C1-3-fluoroalcoxy, HO-C1-3-~alkylène, -CN, C1-3- alkyle-X- où X = S, SO ou SO2; ou R7, = RaRbN-, RaRbN-C1-3-~alkylène, ReRbNC(O)-, C1-3-alkyle-C(O)-, aryle, aryle-0- ou hétéroaryle ; R8 = H, halogène, C1-5-alkyle, C1-5-alcoxy, C1-3-fluoroalcoxy ; à l'état de base ou de sel d'addition à un acide, ainsi qu'à l'état d'hydrate ou de solvat. Procédé de préparation et application en thérapeutique.
Augereau Jean Michel
Courtemanche Gilles
Geslin Michel
Kirby Eades Gale Baker
Sanofi-Aventis
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