AR056216A1 - Derivados de piridopirazina y su uso - Google Patents

Derivados de piridopirazina y su uso

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Publication number
AR056216A1
AR056216A1 ARP060104948A ARP060104948A AR056216A1 AR 056216 A1 AR056216 A1 AR 056216A1 AR P060104948 A ARP060104948 A AR P060104948A AR P060104948 A ARP060104948 A AR P060104948A AR 056216 A1 AR056216 A1 AR 056216A1
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Argentina
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alkyl
aryl
heteroaryl
cycloalkyl
heterocyclyl
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ARP060104948A
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English (en)
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Irene Seipelt
Eckhard Claus
Tilmann Schuster
Michael Czech
Emmanuel Polymeropoulos
Eckhard Guenther
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Zentaris Ag
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Publication of AR056216A1 publication Critical patent/AR056216A1/es

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Abstract

La presente pone a disposicion compuestos de piridopirazina, que son apropiados para el tratamiento o la prevencion de estados fisiologicos y/o patofisiologicos en mamíferos mediados y/o modulados por vías de transduccion de senales y/o enzimas, en especial en el ser humano. Reivindicacion 1: Uso de un compuesto de acuerdo con la formula general (1) en donde los sustituyentes R1, R2, R3, R4 tienen el siguiente significado: R1 y R2 pueden ser, de modo independiente entre sí: (i) hidrogeno, (ii) hidroxilo, (iii) halogeno, (iv) alquilo, en donde el radical alquilo está saturado y puede estar compuesto de 1 a 8 átomos de C, (v) arilo no sustituido o sustituido, en donde el radical arilo puede estar mono- o polisustituido con F, Cl, Br, I, CF3, CN, NH2, NH-alquilo, NH-cicloalquilo, NH-heterociclilo, NH-arilo, NH-heteroarilo, NH-alquil-cicloalquilo, NH-alquil-heterociclilo, NH-alquil-arilo, NH-alquil-heteroarilo, NH-alquil-NH2, NH-alquil-OH, N(alquilo)2, NHC(O)-alquilo, NHC(O)- cicloalquilo, NHC(O)-heterociclilo, NHC(O)-arilo, NHC(O)-heteroarilo, NHC(O)-alquil-arilo, NHC(O)-alquilheteroarilo, NHSO2-alquilo, NHSO2-cicloalquilo, NHSO2-heterociclilo, NHSO2-arilo, NHSO2-heteroarilo, NHSO2-alquil-arilo, NHSO2-alquil- heteroarilo, NO2, SH, S-alquilo, S-arilo, S-heteroarilo, OH, OCF3, O-alquilo, O-cicloalquilo, O-heterociclilo, O-arilo, O-heteroarilo, O-alquil-cicloalquilo, O-alquil-heterociclilo, O-alquilarilo, O-alquilheteroarilo, O-alquil-OH, O-(CH2)n-O, OC(O)- alquilo, OC(O)-cicloalquilo, OC(O)-heterociclilo, OC(O)-arilo, OC(O)-heteroarilo, OC(O)-alquilarilo, OC(O)-alquil-heteroarilo, OSO3H, OSO2-alquilo, OSO2-cicloalquilo, OSO2-heterociclilo, OSO2-arilo, OSO2-heteroarilo, OSO2-alquil-arilo, OSO2-alquil- heteroarilo, OP(O)(OH)2, C(O)-alquilo, C(O)-arilo, C(O)-heteroarilo, CO2H, CO2-alquilo, CO2-cicloalquilo, CO2-heterociclilo, CO2-arilo, CO2-heteroarilo, CO2-alquil-cicloalquilo, CO2-alquil-heterociclilo, CO2-alquil-arilo, CO2-alquil-heteroarilo, C(O)-NH2, C(O)NH-alquilo, C(O)NH-cicloalquilo, C(O)NH-heterociclilo, C(O)NH-arilo, C(O)NH-heteroarilo, C(O)NH-alquil-cicloalquilo, C(O)NH-alquil-heterociclilo, C(O)NH-alquil-heteroarilo, C(O)N(alquilo)2, C(O)N(cicloalquilo)2, C(O)N(heteroarilo)2, C(O)N(arilo)2, SO-alquilo, SO-arilo, SO2-alquilo, SO2-arilo, SO2NH2, SO2NH-alquilo, SO2NH-arilo, SO2NH-heteroarilo, SO2NH-alquil-arilo, SO3H, SO2O-alquilo, SO2O-arilo, SO2O-alquil-arilo, alquilo, cicloalquilo, heterociclilo, arilo o heteroarilo, igual o diferente, n puede adoptar el valor 1, 2 o 3, y los sustituyentes de alquilo, cicloalquilo, heterociclilo, arilo, heteroarilo, alquil-cicloalquilo, alquil-heterociclilo, alquil-arilo y alquil-heteroarilo pueden estar, a su vez, sustituidos, (vi) heteroarilo no sustituido o sustituido, en donde el radical heteroarilo puede estar mono- o polisustituido con F, Cl, Br, I, CF3, CN, NH2, NH-alquilo, NH-cicloalquilo, NH-heterociclilo, NH-arilo, NH-heteroarilo, NH-alquil-cicloalquilo, NH- alquil-heterociclilo, NH-alquil-arilo, NH-alquil-heteroarilo, NH-alquil-NH2, NH-alquil-OH, N(alquilo)2, NHC(O)-alquilo, NHC(O)-cicloalquilo, NHC(O)-heterociclilo, NHC(O)-arilo, NHC(O)-heteroarilo, NHC(O)-alquil-arilo, NHC(O)-alquil-heteroarilo, NHSO2-alquilo, NHSO2-cicloalquilo, NHSO2-heterociclilo, NHSO2-arilo, NHSO2-heteroarilo, NHSO2-alquil-arilo, NHSO2-alquil-heteroarilo, NO2, SH, S-alquilo, S-arilo, S-heteroarilo, OH, OCF3, O-alquilo, O-cicloalquilo, O-arilo, O-heteroarilo, O-alquil- cicloalquilo, O-alquil-heterociclilo, O-alquil-arilo, O-alquil-heteroarilo, OC(O)-alquilo, OC(O)-cicloalquilo, OC(O)-heterociclilo, OC(O)-arilo, OC(O)-heteroarilo, OC(O)-alquil-heteroarilo, OSO3H, OSO2-alquilo, OSO2-cicloalquilo, OSO2-heterociclilo, OSO2-arilo, OSO2-heteroarilo, OSO2-alquil-arilo, OSO2-alquil-heteroarilo, OP(O)(OH)2, C(O)-alquilo, C(O)-arilo, C(O)-heteroarilo, CO2H, CO2-alquilo, CO2-cicloalquilo, CO2-heterociclilo, CO2-arilo, CO2-heteroarilo, CO2-alquil-cicloalquilo, CO2-alquil- heterociclilo, CO2-alquil-arilo, CO2-alquil-heteroarilo, C(O)-NH2, C(O)NH-alquilo, C(O)NH-cicloalquilo, C(O)NH-heterociclilo, C(O)NH-arilo, C(O)NH-heteroarilo, C(O)NH-alquil-cicloalquilo, C(O)NH-alquil-heterociclilo, C(O)NH-alquil-arilo, C(O)NH- alquil-heteroarilo, C(O)N(alquilo)2, C(O)N(cicloalquilo)2, C(O)N(arilo)2, C(O)N(heteroarilo)2, SO2NH2, SO2NH-alquilo, SO2NH-arilo, SO2NH-heteroarilo, SO2NH-alquil-arilo, SO3H, SO2O-alquilo, SO2O-arilo, SO2O-alquil-arilo, alquilo, cicloalquilo, heterociclilo, arilo o heteroarilo, igual o diferente, y los sustituyentes de alquilo, cicloalquilo, heterociclilo, arilo y heteroarilo pueden estar, a su vez, sustituidos, (vii) OR5, en donde R5 puede ser alquilo, cicloalquilo, heterociclilo, arilo, heteroarilo, alquilcicloalquilo, alquil-heterociclilo, alquil-arilo o alquil-heteroarilo, y los sustituyentes de alquilo, cicloalquilo, heterociclilo, arilo, heteroarilo, alquil-cicloalquilo, alquil-heterociclilo, alquilarilo o alquil- heteroarilo pueden estar, a su vez, sustituidos, (viii) SR6, en donde R6 puede ser alquilo, cicloalquilo, heterociclilo, arilo, heteroarilo, alquil-cicloalquilo, alquil-heterociclilo, alquil-arilo o alquil-heteroarilo, y los sustituyentes de alquilo, cicloalquilo, heterociclilo, arilo y heteroarilo, alquil-cicloalquilo, alquil-heterociclilo, alquil-arilo, alquil-heteroarilo pueden estar, a su vez, sustituidos, (ix) NR7R8, en donde R7 y R8 pueden ser, de modo independiente entre sí, hidrogeno, alquilo, cicloalquilo, heterociclilo, arilo, heteroarilo, alquil-cicloalquilo, alquil-heterociclilo, alquil-arilo o alquil-heteroarilo, y los sustituyentes de alquilo, cicloalquilo, heterociclilo, arilo y heteroarilo, alquil-cicloalquilo, alquil heterociclilo alquil-arilo o alquil-heteroarilo pueden estar, a su vez, sustituidos, o R7 y R8 son juntos cicloalquilo o heterociclilo, en donde cicloalquilo y heterociclilo pueden estar, a su vez, sustituidos; R3 y R4 pueden ser, de modo independiente entre sí, hidrogeno o NR9R10, con la condicion de que, cuando R3 = NR9R10, R4 = H, y cuando R4 = NR9R10, R3 = H, en donde R9 puede ser hidrogeno, alquilo, cicloalquilo, heterociclilo, arilo, heteroarilo, alquil-cicloalquilo, alquil- heterociclilo, alquil-arilo o alquil-heteroarilo, y los sustituyentes de alquilo, cicloalquilo, heterociclilo, arilo y heteroarilo, alquil-cicloalquilo, alquil heterociclilo alquil-arilo o alquil-heteroarilo pueden estar, a su vez, sustituidos, y R10 puede ser a) -C(Y)NR11R12, en donde Y = O, S y R11 y R12 son, de modo independiente entre sí, (i) hidrogeno, (ii) alquilo no sustituido o sustituido, en donde el radical alquilo puede estar mono- o polisustituido con F, Cl, Br, I, CF3, CN, NH2, NH-alquilo, NH-cicloalquilo, NH-heterociclilo, NH-arilo, NH-heteroarilo, NH-alquil-cicloalquilo, NH-alquil-heterociclilo, NH-alquil-arilo, NH-alquil-heteroarilo, N(alquilo)2, NHC(O)-alquilo, NHC(O)-cicloalquilo, NHC(O)-heterociclilo, NHC(O)-arilo, NHC(O)-heteroarilo, NHC(O)-alquil-arilo, NHC(O)-alquil-heteroarilo, NHSO2-alquilo, NHSO2-cicloalquilo, NHSO2-heterociclilo, NHSO2-arilo, NHSO2-heteroarilo, NHSO2-alquil-arilo, NHSO2-alquil-heteroarilo, NO2, SH, S-alquilo, S-cicloalquilo, S- heterociclilo, S-arilo, S-heteroarilo, OH, OCF3, O-alquilo, O-cicloalquilo, O-heterociclilo, O-arilo, O-heteroarilo, O-alquil-cicloalquilo, O-alquil-heterociclilo, O-alquilarilo, O-alquilheteroarilo, OC(O)-alquilo, OC(O)-cicloalquilo, OC(O)- heterociclilo, OC(O)-arilo, OC(O)-heteroarilo, OC(O)-alquil-arilo, OC(O)-alquil-heteroarilo, OSO3H, OSO2-alquilo, OSO2-cicloalquilo, OSO2-heterociclilo, OSO2-arilo, OSO2-heteroarilo, OSO2-alquil-arilo, OSO2-alquil-heteroarilo, OP(O)(OH)2, C(O)- alquilo, C(O)-arilo, C(O)-heteroarilo, CO2H, CO2-alquilo, CO2-cicloalquilo, CO2-heterociclilo, CO2-arilo, CO2-heteroarilo, CO2-alquil-cicloalquilo, CO2-alquil-heterociclilo, CO2-alquil-arilo, CO2-alquil-heteroarilo, C(O)-NH2, C(O)NH-alquilo, C(O)NH- cicloalquilo, C(O)NH-heterociclilo, C(O)NH-arilo, C(O)NH-heteroarilo, C(O)NH-alquil-cicloalquilo, C(O)NH-alquil-heterociclilo, C(O)NH-alquil-arilo, C(O)NH-alquil-heteroarilo, C(O)N(alquilo)2, C(O)N(cicloalquilo)2, C(O)N(heteroarilo)2, C(O)N(arilo)2, SO-alquilo, SO-arilo, SO2-alquilo, SO2-arilo, SO2NH2, SO2NH-alquilo, SO2NH-arilo, SO2NH-heteroarilo, SO2NH-alquil-arilo, SO3H, SO2O-alquilo, SO2O-arilo, SO2O-alquil-arilo, cicloalquilo, heterociclilo, arilo o heteroarilo, igual o diferente, (iii) cicloalquilo no sustituido o sustituido, en donde el radical cicloalquilo puede estar mono- o polisustituido con F, Cl, Br, I, NH2, NH-alquilo, NH-cicloalquilo, NH-heterociclilo, NH-arilo, NH-heteroarilo, NH-alquil-arilo, NH-alquil-heteroarilo, N(alquilo)2, NHC(O)-alquilo, NHC(O)-cicloalquilo, NHC(O)-heterociclilo, NHC(O)-arilo, NHC(O)-heteroarilo, NHC(O)-alquil-arilo, NHC(O)-alquil-heteroarilo, NHSO2-alquilo, NHSO2-cicloalquilo, NHSO2-heterociclilo, NHSO2-arilo, NHSO2-heteroarilo, NHSO2- alquil-arilo, NHSO2-alquil-heteroarilo, OH, O-alquilo, O-cicloalquilo, O-heterociclilo, O-arilo, O-heteroarilo, O-alquilarilo, O-alquilheteroarilo, OC(O)-alquilo, OC(O)-cicloalquilo, OC(O)-heterociclilo, OC(O)-arilo, OC(O)-heteroarilo, OC(O)-alquil- arilo, OC(O)-alquil-heteroarilo, OSO3H, OSO2-alquilo, OSO2-cicloalquilo, OSO2-heterociclilo, OSO2-arilo, OSO2-heteroarilo, OSO2-alquil-arilo, OSO2-alquil-heteroarilo, OP(O)(OH)2, CO2H, CO2-alquilo, CO2-cicloalquilo, CO2-heterociclilo, CO2-arilo, CO2- heteroarilo, CO2-alquil-cicloalquilo, CO2-alquil-heterociclilo, CO2-alquil-arilo, CO2-alquil-heteroarilo, C(O)-NH2, C(O)NH-alquilo, C(O)NH-cicloalquilo, C(O)NH-heterociclilo, C(O)NH-arilo, C(O)NH-heteroarilo, C(O)NH-alquil-cicloalquilo, C(O)NH- alquil-heterociclilo, C(O)NH-alquil-arilo, C(O)NH-alquil-heteroarilo, C(O)N(alquilo)2, C(O)N(cicloalquilo)2, C(O)N(heteroarilo)2, C(O)N(arilo)2, alquilo o arilo, igual o diferente, (iv) heterociclilo no sustituido o sustituido, en donde el radical heterociclilo puede estar mono- o polisustituido con OH, O-alquilo, O-arilo, NH2, NH-alquilo, NH-arilo, alquilo, alquil-arilo, o aril
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