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AR031528A1 - Compuestos de pirazolopirimidina y su uso para preparar una composicion farmaceutica - Google Patents

Compuestos de pirazolopirimidina y su uso para preparar una composicion farmaceutica

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Publication number
AR031528A1
AR031528A1 ARP000104888A ARP000104888A AR031528A1 AR 031528 A1 AR031528 A1 AR 031528A1 AR P000104888 A ARP000104888 A AR P000104888A AR P000104888 A ARP000104888 A AR P000104888A AR 031528 A1 AR031528 A1 AR 031528A1
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Argentina
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substituted
unsubstituted
alkyl
group
independently
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ARP000104888A
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Abbott Gmbh & Co Kg
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    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

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Abstract

Un compuesto de pirazolopirimidina que posee una formula (1): la mezclas diastereomérico racémicas, isomeros opticos, sales farmacéuticamente aceptables, prodrogas o metabolitos biologicamente activos del mismo en los cuales: G es formula (2) donde Z100 es formula (3) o un grupo opcionalmente sustituido con R1 seleccionado del grupo que consiste de cicloalquilo, naftilo, tetrahidronaftilo, benzotenilo, furanilo, tienilo, benzoxazolilo, benzotiazolilo de formulas (4) y (5), tiazolilo, benzofuranilo, 2,3-dihidrobenzofuranilo, indolilo, isoxazolilo, tetrahidropiranilo, tetrahidrofuranilo, piperidinilo, pirazolilo, pirrolilo, oxazolilo, isotiazolilo, oxadiazolilo, tiadiazolilo, indolinilo, indazolilo , benzoisotiazolilo, pirido-oxazolilo, pirido-tiazolilo, pirimido-oxazolilo, pirimidotiazolilo y bencimidazolilo; Z110 es un enlace covalente, o un (C1-6) opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo que consiste de alquilo, CN, OH, halogeno, NO2, COOH, amino sustituido o sin sustituir y fenilo sustituido o sin sustituir; Z111 es un enlace covalente,(C1-6) opcionalmente sustituido o un û(CH2)n-cicloalquil-(CH2)n- opcionalmente sustituido; donde los grupos opcionalmente sustituidos con uno o más sustituyentes seleccionados del grupo que consiste de alquilo, CN, OH, halogeno, NO2, COOH, amino sustituido o sin sustituir y fenilo sustituido o sin sustituir; Ra y R1 cada uno representa uno o más sustituyentes para cada circunstancia seleccionada independientemente del grupo que consiste de hidrogeno, halogeno, -CN, -NO2, -C(O)OH, -C(O)H, -OH, -C(O)O-alquilo, carboxamido sustituido o sin sustituir, tetrazolilo, trifluorometilcarbonilamino, trifluorometilsulfonamido, alquilo sustituido o sin sustituir, alcoxilo sustituido o sin sustituir, arilo sustituido o sin sustituir, alquenilo sustituido o sin sustituir, ariloxilo sustituido o sin sustituir, heteroariloxilo sustituido o sin sustituir, arilalquilo sustituido o sin sustituir, alquinilo sustituido o sin sustituir, amino, sustituido o sin sustituir, aminoalquilo sustituido o sin sustituir, grupo amido sustituido o sin sustituir, heteroariltio sustituido o sin sustituir, ariltio sustituido o sin sustituir, -Z105-C(O)NR2, -Z105-N(R)-CO2-Z100, -Z105-N(R)-SO2-Z200, -Z105-N(R)-C(O)-N(R)-Z200, Rc y CH2ORc; donde Rc para cada circunstancia es independientemente hidrogeno, alquilo sustituido o sin sustituir, arilo sustituido o sin sustituir, -CH2-NRdRe, -W-(CH2)t-NRdRe, -W- -(CH2)t-O alquilo, -W-(CH2)t-S-alquilo, o ûW-(CH2)t-OH; Z105 para cada circunstancia es independientemente un enlace covalente o (C1-6); Z200 para cada circunstancia es independientemente (C1-6) sustituido o sin sustituir, fenilo sustituido o sin sustituir o û(C1-6)-fenilo sustituido o sin sustituir; Rd y Re para cada circunstancia es independientemente H, alquilo, alcanoilo o SO2-alquilo; o Rd, Re y el átomo de nitrogeno al cual estos están unidos forman un anillo heterocíclico de cinco o seis miembros; t para cada circunstancia es independientemente un entero de valor 2 a 6 ; W para cada circunstancia es independientemente un enlace directo u O, S, S(O), SO2, o NRf en donde Rf para cada circunstancia es independientemente H o alquilo; o Rf es un anillo carbocíclico o heterocíclico sustituido sin sustituir fusionado con el anillo 2; R3 es hidrogeno, hidroxilo, alquilo sustituido o sin sustituir o alcoxilo sustituido o sin sustituir; A es ûO-; -S-; SOp-; -N(R)-; -N(C(O)OR)-; -N(C(O)R)-; -N(SO2R)-; -CH2O-; -CH2S-; -CH2N(R)-; -CH(NR)-; CH2N(C(O)R)-; -CH2N(C(O)OR)-; -CH2N(SO2R)-; -CH(NHR)-; -CH(NHC(O)R)-; -CH(NHSO2R)-; -CH(NHC(O)OR)-; -CH(OC(O)R)-; -CH(OC(O)NHR)-; -CH=CH-; -C(=NOR)-; -C(O)-;-CH(OR)-; -C(O)N(R)-; -N(R)C(O)-; -N(R)S(O)p-; -OC(O)N(R)-; -N(R)-C(O)-(CH2)n-N(R)-, -N(R)C(O)O-; -N(R)(CH2)n+1 -C(O)-, -S(O)pN(R)-; -O-(CR2)n+1-C(O). ûO-(CR2)n+1-O-, ûN(C(O)R)S(O)p-; -N(R)S(O)pN(R)-; N(R)-C(O)-(CH2)n-O-, -C(O)N(R)C(O)-; -S(O)pN(R)C(O)-;-OS(O)pN(R)C(O)-; -OS(O)pN(R)-; -N(R)S(O)pO-; -N(R)S(O)pC(O)-; -SOpN(C(O)R)-; -N(R)SOpN(R)-; -C(O)O-; -N(R)P(ORb)O-; -N(R)P(ORb)-; N(R)P(O)(ORb)O-; -N(R)P(O)(ORb)-; -N(C(O)R)P(ORb)O-; -N(C(O)R)P(ORb)-; -N(C(O)R)P(O)(ORb)O-; o ûN(C(O)R)P(ORb)-; donde R para cada circunstancia es independientemente H, alquilo sustituido o sin sustituir, arilalquilo sustituido o sin sustituir o arilo sustituido o sin sustituir; Rb para cada circunstancia es independientemente H, alquilo sustituido o sin sustituir, arilalquilo sustituido o sin sustituir, cicloalquilo sustituido o sin sustituir o arilo sustituido o sin sustituir; p es 1 o 2; o en el grupo conteniendo fosforo, el átomo de nitrogeno, el átomo de fosforo, R y Rb juntos forman un anillo heterocíclico de cinco o seis miembros; o A es NRSO2 y R y Ra y el átomo de nitrogeno forman juntos un anillo heterocíclico de cinco o seis miembros sustituidos o sin sustituir fusionado al anillo1; A es NRSO2 y R, Ra y el átomo de nitrogeno forman juntos un anillo 1; R2 es ûZ101, Z102 es un enlace covalente, -(alquiloC1-6)-, -(alquiloC1-6)-O-, -(C1-6)-C(O)-, -(alquiloC1-6)-C(O)-NH-, -(C1-6)-C(O)-N((alquiloC1-6))- o un grupo de fenilo sustituido o sin sustituir; Z102 es hidrogeno, un grupo alquilo sustituido o sin sustituir, un grupo cicloalquilo sustituido o sin sustituir, un grupo heterocíclico saturado o no saturado, sustituido o sin sustituir , los grupos heterobicíclico saturados o no saturados, sustituido o sin sustituir; dicho grupo heterocíclico sustituido o heterobicíclico sustituido que posee uno o mas sustituyentes cada uno seleccionado independientemente del grupo que consiste de hidroxilo, ciano, alcoxilo sustituido o sin sustituir, sulfonamido sustituido o sin sustituir, ureido sustituido o sin sustituir, carboxamido sustituido o sin sustituir; amino sustituido o sin sustituir, oxo, un grupo heterocíclico saturado, no saturado o aromático sustituido o sin sustituir que comprende uno o más átomos de nitrogeno, uno más átomos de oxígeno o una combinacion de los mismos; en donde dichos átomos de nitrogeno se sustituyen independientemente opcionalmente por un alquilo sustituido o sin sustituir, arilo sustituido o sin sustituir o grupo arilalquilo sustituido o sin sustituir, o R2 es de la formula B-E, en donde B es un cicloalquilo sustituido o sin sustituir, azacicloalquilo sustituido o sin sustituir, amino sustituido o sin sustituir, aminoalquilsulfonilo sustituido o sin sustituir, alcoxialquilo sustituido o sin sustituir, alcoxilo sustituido o sin sustituir, aminoalquilcarbonilo sustituido o sin sustituir, hidroxilo, alquileno sustituido o sin sustituir, aminoalquilo, sustituido o sin sustituir, alquilencarbonilo sustituido o sin sustituir o grupo aminoalquilcarbonilo sustituido o sin sustituir, y E es azacicloalquilo sustituido o sin sustituir azacicloalquilcarbonilo sustituido o sin sustituir, azacicloalquilsulfonilo sustituido o sin sustituir azacicloalquilalquilo sustituido o sin sustituir, heteroarilo sustituido o sin sustituir, heteroarilcarbonilo sustituido o sin sustituir, heteroarilsulfonilo sustituido o sin sustituir, heteroaril alquilo sustituido o sin sustituir, azacicloalquilcarbonilamino sustituido o sin sustituir, heteroaril carbonilamino sustituido o sin sustituir o arilo sustituido o sin sustituir; a es 1 y D1, G1, J1, L1 y M1 son independientemente cada uno seleccionado del grupo que consiste de CRa y N, con la condicion que por lo menos dos de D1, G1, J1, L1, y M1, sea CRa; o a es 0, y cada uno de D1, G1, L1, y M1 es NRa, uno de D1, G1, L1, y M1 es CRa y el resto es independientemente seleccionado del grupo que consiste de CRa y N, en donde Ra es igual al definido precedentemente; b es uno y D2, G2, J2, L2 y M2 son independientemente cada uno seleccionado del grupo que consiste de CRa y N, con la condicion que por lo menos dos de D2, G2, J2, L2, y M2 son CRa; o b es 0, y uno de D2, G2, L2, y M2 es MRa, uno de D2, G2, L2, y M2 es CRa; y el resto se selecciona independientemente del grupo que consiste de CRa y N, en donde Ra es igual al definido precedentemente; y n para cada circunstancia es independientemente un entero de valor de 0 a 6. Uso del compuesto de pirazolopirimidina de la formula (1) para preparar una composicion farmacéutica para inhibir la actividad de la quinasaproteínica. La composicion farmacéutica es util para afectar desordenes hiperproliferativos, angiogénesis, una o más ulceras, para tratar una condicion patologica o para disminuir la fertilidad de un paciente.
ARP000104888A 1999-09-17 2000-09-18 Compuestos de pirazolopirimidina y su uso para preparar una composicion farmaceutica AR031528A1 (es)

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