AR072458A2 - Derivados de azol-pirimidina condensados, composiciones farmaceuticas que los contienen y su uso para inhibir la actividad pi3k-? - Google Patents

Derivados de azol-pirimidina condensados, composiciones farmaceuticas que los contienen y su uso para inhibir la actividad pi3k-?

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AR072458A2
AR072458A2 ARP090102458A ARP090102458A AR072458A2 AR 072458 A2 AR072458 A2 AR 072458A2 AR P090102458 A ARP090102458 A AR P090102458A AR P090102458 A ARP090102458 A AR P090102458A AR 072458 A2 AR072458 A2 AR 072458A2
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amino
alkyl
optionally substituted
alkoxycarbonyl
halogen
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Bayer Ag
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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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Abstract

Un derivado de azolpirimidina condensado de la formula (1), su forma tautomérica o estereoisomérica, o una sal del mismo, donde X representa NH; Y1 representa N; Y2 e Y3 representan CR3R4; el enlace químico entre Y2- - -Y3 representa un enlace simple; Z3 y Z4 representan CH; Z1 y Z2 representan independientemente CH o CR2; R1 representa: uno de los siguientes anillos heterocíclicos seleccionados del grupo que consiste en: pirazolilo sustituido con 1 a 3 sustituyentes seleccionados del grupo que consiste en hidroxi, halogeno, nitro, ciano, carboxi, amino, N-(alquil C1-6)amino, N-(hidroxialquil C1-6)amino, N,N-di(alquil C1-6)amino, N-(acil C1-6)amino, N-(alcoxicarbonil C1-6)amino, N-(formil)-N-(alquil C1-6)amino, N,N-di(alquil C1-6)amino (alquenil C2-6)amino, N-(alcansulfonil C1-6)amino, N-[N,N-di(alquil C1-6)amino metilen]amino, alquiltio C1-6, alcanosulfonilo C1-6, sulfamoilo, alcoxi C1-6, alcoxicarbonilo C1-6, pirrolilo, imidazolilo, pirazolilo, pirrolidinilo, piridilo, fenil alcoxicarbonilo C1-6, tiazolilo opcionalmente sustituido con piridilo, piperazinilo opcionalmente sustituido con alquilo C1-6 o alcoxi C1-6; o con 1 o 2 sustituyentes alquilo C1-6 sustituidos con mono-, di- o tri-halogeno; o con 3 sustituyentes alquilo C1-6 opcionalmente sustituidos con mono-, di- o tri- halogeno; furilo sustituido con 1 a 3 sustituyentes seleccionados del grupo que consiste en hidroxi, halogeno, nitro, ciano, carboxi, amino, N-(alquil C1-6)amino, N-(hidroxialquil C1-6)amino, N,N-di(alquil C1-6)amino, N-(acil C1-6)amino. N-(alcoxicarbonil C1-6)amino, N-(formil)-N-(alquil C1-6)amino, N,N-di(alquil C1-6)amino (alquenil C2-6)amino, N-(alcan C1-6)sulfonil amino, N-[N,N-di(alquil C1-6)aminometilen]amino, alquiltio C1-6, alcansulfonilo C1-6, sulfamoilo, alcoxi C1-6, alcoxicarbonilo C1-6, pirrolilo, imidazolilo, pirazolilo, pirrolidinilo, piridilo, fenil alcoxicarbonilo C1-6, tiazolilo opcionalmente sustituido con piridilo, piperazinilo opcionalmente sustituido con alquilo C1-6 o alcoxi C1-6 y alquilo C1-6 opcionalmente sustituido con mono, di- o tri-halogeno, tienilo sustituido con 1 a 3 sustituyentes seleccionados del grupo que consiste en hidroxi, halogeno (aunque no cloro), carboxi, amino, N-(alquil C1-6)amino, N-(hidroxialquil C1-6)amino, N,N-di(alquil C1-6)amino, N-(acil C1-6)amino, N-(alcoxicarbonil C1-6)amino, N-(formil)-N-(alquil C1-6)amino, N,N-di(alquil C1-6)amino (alquenil C2-6)amino, N-(alcan C1-6)sulfonil amino, N-[N,N-di(alquil C1-6)aminometilen]amino, alquiltio C1-6, alcansulfonilo C1-6, sulfamoilo, alcoxi C1-6, alcoxicarbonilo C1-6, pirrolilo, imidazolilo, pirazolilo, pirrolidinilo, piridilo, fenil alcoxicarbonilo C1-6, tiazolilo opcionalmente sustituido con piridilo, piperazinilo opcionalmente sustituido con alquilo C1-6 o alcoxi C1-6; o con 1 sustituyente alquilo C1-6 sustituido con mono-, di- o tri-halogeno; o con 2 o 3 sustituyentes alquilo C1-6 opcionalmente sustituidos con mono-, di- o tri-halogeno; tiazolilo sustituido con 1 a 3 sustituyentes seleccionados del grupo que consiste en hidroxi, halogeno, nitro, ciano, carboxi, amino, N-(alquil C1-6)amino, N-(hidroxialquil C1-6)amino, N,N-di(alquil C1-6)amino, N-(acil C1-6)amino, N-(formil)-N-(alquil C1-6)amino, N,N-di(alquil C1-6)amino (alquenil C2-6)amino, N-(alcan C1-6)sulfonil amino, N-[N,N-di(alquil C1-6)aminometilen]amino, alquiltio C1-6, alcansulfonilo C1-6, sulfamoilo, alcoxi C1-6, alcoxicarbonilo C1-6, pirrolilo, imidazolilo, pirazolilo, pirrolidinilo, piridilo, fenil alcoxicarbonilo C1-6, tiazolilo opcionalmente sustituido con piridilo, piperazinilo opcionalmente sustituido con alquilo C1-6, o alcoxi C1-6 y alquilo C1-6 opcionalmente sustituido con mono-, di- o tri-halogeno; o con 1 o 2 sustituyentes alquilo C1-6 sustituido con mono-, di- o tri-halogeno; o con 3 sustituyentes alquilo C1-6 opcionalmente sustituidos con mono-, di- o tri-halogeno; o con 3 sustituyentes piridilo; o con 3 sustituyentes N-(alcoxicarbonil C1-6)amino; isotiazolilo opcionalmente sustituido con 1 a 3 sustituyentes seleccionados del grupo que consiste en hidroxi, halogeno, nitro, ciano, carboxi, amino, N-(alquil C1-6)amino, N-(hidroxialquil C1-6)amino, N,N-di(alquil C1-6)amino, N-(acil C1-6)amino, N-(alcoxicarbonil C1-6)amino, N-(formil)-N-(alquil C1-6)amino, N,N-di(alquil C1-6)amino (alquenil C2-6)amino, N-(alcan C1-6)sulfonil amino, N-[N,N-di(alquil C1-6)aminometilen]amino, alquiltio C1-6, alcansulfonilo C1-6, sulfamoilo, alcoxi C1-6, alcoxicarbonilo C1-6, pirrolilo, imidazolilo, pirazolilo, pirrolidinilo, piridilo, fenil alcoxicarbonilo C1-6, tiazolilo opcionalmente sustituido con piridilo, piperazinilo opcionalmente sustituido con alquilo C1-6 o alcoxi C1-6 y alquilo C1-6 opcionalmente sustituido con mono-, di- o tri-halogeno; oxazolilo opcionalmente sustituido con 1 a 3 sustituyentes seleccionados del grupo que consiste en hidroxi, halogeno, nitro, ciano, carboxi, amino, N-(alquil C1-6)amino, N-(hidroxialquil C1-6)amino, N,N-di(alquil C1-6)amino, N-(acil C1-6)amino, N-(alcoxicarbonil C1-6)amino, N-(formil)-N-(alquil C1-6)amino, N,N-di(alquil C1-6)amino (alquenil C2-6)amino, N-(alcan C1-6)sulfonil amino, N-[N,N-di(alquil C1-6)aminometilen]amino, alquiltio C1-6, alcansulfonilo C1-6, sulfamoilo, alcoxi C1-6, alcoxicarbonilo C1-6, pirrolilo, imidazolilo, pirazolilo, pirrolidinilo, piridilo, fenil alcoxicarbonilo C1-6, tiazolilo opcionalmente sustituido con piridilo, piperazinilo opcionalmente sustituido con alquilo C1-6 o alcoxi C1-6 y alquilo C1-6 opcionalmente sustituido con mono-, di- o tri-halogeno; isoxazoliIo sustituido con 1 a 3 sustituyentes seleccionados del grupo que consiste en hidroxi, halogeno, nitro, ciano, carboxi, amino, N-(alquil C1-6)amino, N-(hidroxialquil C1-6)amino, N,N-di(alquil C1-6)amino, N-(acil C1-6)amino, N-(alcoxicarbonil C1-6)amino, N-(formil)-N-(alquil C1-6)amino, N,N-di(alquil C1-6)amino (alquenil C2-6)amino, N-(alcan C1-6)sulfonil amino, N-[N,N-di(alquil C1-6)aminometilen]amino, alquiltio C1-6, alcansulfonilo C1-6, sulfamoilo, alcoxi C1-6, alcoxicarbonilo C1-6, pirrolilo, imidazolilo, pirazolilo, pirrolidinilo, piridilo, fenil alcoxicarbonilo C1-6, tiazolilo opcionalmente sustituido con piridilo, piperazinilo opcionalmente sustituido con alquilo C1-6 o alcoxi C1-6; o con 1 o 2 sustituyentes alquilo C1-6 sustituidos con mono-, di- o tri-halogeno; o con 3 sustituyentes alquilo C1-6 opcionalmente sustituidos con mono-, di- o tri-halogeno; imidazolilo sustituido con 1 a 3 sustituyentes seleccionados del grupo que consiste en hidroxi, halogeno, nitro, ciano, carboxi, amino, N-(alquil C1-6)amino, N-(hidroxialquil C1-6)amino, N,N-di(alquil C1-6)amino, N-(acil C1-6)amino, N-(alcoxicarbonil C1-6)amino, N-(formil)-N-(alquil C1-6)amino, N,N-di(alquil C1-6)amino (alquenil C2-6)amino, N-(alcan C1-6)sulfonil amino, N-[N,N-di(alquil C1-6)aminometilen]amino, alquiltio C1-6, alcansulfonilo C1-6, sulfamoilo, alcoxi C1-6, alcoxicarbonilo C1-6 , pirrolilo, imidazolilo, pirazolilo, pirrolidinilo, piridilo, fenil alcoxicarbonilo C1-6, tiazolilo opcionalmente sustituido con piridilo, piperazinilo opcionalmente sustituido con alquilo C1-6 o alcoxi C1-6 y alquilo C1-6 opcionalmente sustituidos con mono-, di- o tri-halogeno; isoimidazolilo opcionalmente sustituido con 1 a 3 sustituyentes seleccionados del grupo que consiste en hidroxi, halogeno, nitro, ciano, carboxi, amino, N-(alquil C1-6)amino, N-(hidroxialquil C1-6)amino, N,N-di(alquil C1-6)amino, N-(acil C1-6)amino, N-(alcoxicarbonil C1-6)amino, N-(formil)-N-(alquil C1-6)amino, N,N-di(alquil C1-6)amino (alquenil C2-6)amino, N-(alcan C1-6)sulfonil amino, N-[N,N-di(alquil C1-6)aminometilen]amino, alquiltio C1-6, alcansulfonilo C1-6, sulfamoilo, alcoxi C1-6, alcoxicarbonilo C1-6, pirrolilo, imidazolilo, pirazolilo, pirrolidinilo, piridilo, fenil alcoxicarbonilo C1-6, tiazolilo opcionalmente sustituido con piridilo, piperazinilo opcionalmente sustituido con alquilo C1-6 o alcoxi C1-6 y alquilo C1-6 opcionalmente sustituido con mono-, di- o tri-halogeno; 1,2,3-tiadiazolilo sustituido con 1 a 3 sustituyentes seleccionados del grupo que consiste en hidroxi, halogeno, nitro, ciano, carboxi, amino, N-(alquil C1-6)amino, N-(hidroxialquil C1-6)amino, N,N-di(alquil C1-6)amino, N-(acil C1-6)amino, N-(alcoxicarbonil C1-6)amino, N-(formil)-N-(alquil C1-6)amino, N,N-di(alquil C1-6)amino (alquenil C2-6)amino, N-(alcan C1-6)sulfonil amino, N-[N,N-di(alquil C1-6)aminometilen]amino, alquiltio C1-6, alcansulfonilo C1-6, sulfamoilo, alcoxi C1-6, alcoxicarbonilo C1-6, pirrolilo, imidazolilo, pirazolilo, pirrolidinilo, piridilo, fenil alcoxicarbonilo C1-6, tiazolilo opcionalmente sustituido con piridilo, piperazinilo opcionalmente sustituido con alquilo C1-6 o alcoxi C1-6 y alquilo C1-6 opcionalmente sustituido con mono-, di- o tri-halogeno; 1,2,4-tiadiazolilo, 1,2,5-tiadiazolilo o 1,3,4-tiadiazolilo opcionalmente sustituidos con 1 a 3 sustituyentes seleccionados del grupo que consiste en hidroxi, halogeno, nitro, ciano, carboxi, amino, N-(alquil C1-6)amino, N-(hidroxialquil C1-6)amino, N,N-di(alquil C1-6)amino, N-(acil C1-6)amino, N-(alcoxicarbonil C1-6)amino, N-(formil)-N-(alquil C1-6)amino, N,N-di(alquil C1-6)amino (alquenil C2-6)amino, N-(alcan C1-6)sulfonil amino, N-[N,N-di(alquil C1-6)aminometilen]amino, alquiltio C1-6, alcansulfonilo C1-6, sulfamoilo, alcoxi C1-6, alcoxicarbonilo C1-6, pirrolilo, imidazolilo, pirazolilo, pirrolidinilo, piridilo, fenil alcoxicarbonilo C1-6, tiazolilo opcionalmente sustituido con piridilo, piperazinilo opcionalmente sustituido con alquilo C1-6 o alcoxi C1-6 y alquilo C1-6 opcionalmente sustituido con mono-, di- o tri-halogeno; 1,2,3-oxadiazolilo, 1,2,4-oxadiazolilo, 1,2,5-oxadiazolilo o 1,3,4-oxadiazolilo, opcionalmente sustituidos con 1 a 3 sustituyentes seleccionados del grupo que consiste en hidroxi, halogeno, nitro, ciano, carboxi, amino, N-(alquil C1-6)amino, N-(hidroxialquil C1-6)amino, N,N-di(alquil C1-6)amino, N-(acil C1-6)amino, N-(alcoxicarbonil C1-6)amino, N-(formil)-N-(alquil C1-6)amino,
ARP090102458A 2002-09-30 2009-07-01 Derivados de azol-pirimidina condensados, composiciones farmaceuticas que los contienen y su uso para inhibir la actividad pi3k-? AR072458A2 (es)

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