AR064491A1 - Derivados de imidazo[1, 2-a]pirimidina, un proceso para su preparacion, una composicion farmaceutica que los comprende y su uso en el tratamiento de enfermedades mediadas por las quinasas fgfr. - Google Patents

Derivados de imidazo[1, 2-a]pirimidina, un proceso para su preparacion, una composicion farmaceutica que los comprende y su uso en el tratamiento de enfermedades mediadas por las quinasas fgfr.

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Publication number
AR064491A1
AR064491A1 ARP070105856A ARP070105856A AR064491A1 AR 064491 A1 AR064491 A1 AR 064491A1 AR P070105856 A ARP070105856 A AR P070105856A AR P070105856 A ARP070105856 A AR P070105856A AR 064491 A1 AR064491 A1 AR 064491A1
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Argentina
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alkyl
formula
compound
imidazo
pyrazolyl
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ARP070105856A
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English (en)
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Astex Therapeutics Ltd
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Priority claimed from GB0625826A external-priority patent/GB0625826D0/en
Priority claimed from GB0720000A external-priority patent/GB0720000D0/en
Application filed by Astex Therapeutics Ltd filed Critical Astex Therapeutics Ltd
Publication of AR064491A1 publication Critical patent/AR064491A1/es

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    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
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Abstract

Compuestos derivados heterocíclicos bicíclicos, a composiciones farmacéuticas que comprenden dichos compuestos y al uso de dichos compuestos en el tratamiento de enfermedades, por ej., el cáncer. También se provee un método para su preparacion. Reivindicacion 1: Un compuesto de formula (1), en el cual X1, X2 y X3 se seleccionan, cada uno de manera independiente, de carbono o nitrogeno, de manera tal que por lo menos uno de X1-X3 representa nitrogeno; X4 representa CR3 o nitrogeno; X5 representa CR6, nitrogeno o C=O; siempre que no más de tres de X1-X5 representen nitrogeno; ------ representa un enlace simple o doble, de manera tal que por lo menos un enlace dentro del sistema anular de 5 miembros sea un doble enlace; R3 representa hidrogeno, halogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, cicloalquilo C3-6, cicloalquenilo C3-6, ciano, haloalquilo C1-6, haloalcoxi C1-6 o =O; A representa un grupo carbocíclico o heterocíclico aromático o no aromático que puede estar sustituido en forma opcional con uno o más (por ej. 1, 2 o 3) grupos Ra; R1 representa -NHCONR4R5, -NHCOOR4, -NH-CO-(CH2)n-NR4R5, -NH(CH2)n-CONR4R5, -NH-CO-(CH2)n-COOR4, -NH-CO-(CH2)n-CSOR4, -NHSO2R4, -NHSO2NR4R5, - NHCSNR4R5, -NHCOR4, -NHCSR4, -NHCSSR4, -NHC(=NR4)NR5, NHC(=NR4)R5, -NH-C(=NH2)-NH-CO-R4, -NHCSOR4 o -NHCOSR4; R4 y R5 representan en forma independiente hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquenilo C3-8, alcanol C1-6, haloalquilo C1-6, -(CH2)n-NRxRy, -(CH2)sCOORz, -(CH2)n-O-(CH2)m-OH, -(CH2)n-arilo, -(CH2)n-O-arilo, -(CH2)n-heterociclilo o -(CH2)n-O-heterociclilo, donde dichos grupos alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquenilo C3-8, arilo y heterociclilo pueden estar sustituidos en forma opcional con uno o más (por ej. 1, 2 o 3) grupos Ra; Rx, Ry y Rz representan en forma independiente hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcanol C1-6, - COOalquilo C1-6, hidroxi, alcoxi C1-6, haloalquilo C1-6, -CO-(CH2)n-alcoxi C1-6, alquilamino C1-6, cicloalquilo C3-8 o cicloalquenilo C3-8; R2 y R6 representan en forma independiente halogeno, hidrogeno, alquilo C1-6, alcoxi C1-6, alquenilo C2-6, alquinilo C2-6, -C:::N, cicloalquilo C3-8, cicloalquenilo C3-8, NHSO2Rw, -CH=N-ORw, un grupo arilo o heterociclilo donde dichos grupos alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo y heterociclilo pueden estar sustituidos en forma opcional con uno o más grupos Rb siempre que R2 y R6 no representen ambos hidrogeno; Rw representa hidrogeno o alquilo C1-6; Ra representa los grupos halogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquenilo C3-8, -ORx, -(CH2)n-O- alquilo C1-6, -O-(CH2)n-ORw, haloalquilo C1-6, haloalcoxi C1-6, alcanol C1-6, =O, =S, nitro, Si(Rx)4, -(CH2)s-CN, -S-Rx, -SO-Rx, -SO2-Rx, -CORx, -(CRxRy)s-COORz, -(CH2)s-CONRxRy, -(CH2)s-NRXRy, -(CH2)s-NRxCORy, -(CH2)s-NRxSO2-Ry, -(CH2)s-NH-SO2- NRxRy, -OCONRxRy, -(CH2)s-NRxCO2Ry, -O-(CH2)s-CRxRy-(CH2)t-ORz o -(CH2)s-SO2NRxRy; Rb representa un grupo Ra o un grupo -Y-carbociclilo o -Z-heterociclilo, donde dichos grupos carbociclilo y heterociclilo pueden estar sustituidos en forma opcional con uno o más (por ej. 1, 2 o 3) grupos Ra; Y y Z representan en forma independiente un enlace, -CO-(CH2)s-, -COO-, -(CH2)n-, -NRx(CH2)n-, -(CH2)n-NRx, -CONRx-, -NRxCO-, -SO2NRx, -NRxSO2-, -NRxCONRy-, -NRxCSNRy-, -O-(CH2)s--, -(CH2)s-O-, S-, -SO- o - (CH2)s-SO2-; m y n representan en forma independiente un numero entero desde 1-4; s y t representan en forma independiente un numero entero desde 0-4; o una de sus sales, solvatos o derivados aceptables desde el punto de vista farmacéutico, con la salvedad de que el compuesto de formula (1) no sea: 3-(3-acetamidofenil)-6-(4-metilfenil) pirazolo(1,5a)pirimidina; 3-(3-acetamidofenil)-6-(4-metoxifenil)pirazolo(1,5a)pirimidina; N-(4-{6-[3-(4-fluorofenil)-1H-4-pirazolil]imidazo[1,2-a]-piridin-3- il}fenil)-metansulfonamida; N-(4-{6-[3-(4-fluorofenil)-1-tritil-1H-4-pirazolil]-imidazo[1,2-a]piridin-3-il}- fenil)metansulfonamida; N-ciclohexil-N'-{2-fluoro-4-[6-(1-tritil-1H-4-pirazolil)imidazo[1,2-a]piridin-3-il]-fenil} urea; N-{2-fluoro-4-[6-(1- tritil-1H-4-pirazolil)imidazo[1,2-a]piridin-3-il]fenil}-N'-isopropil urea; N-ciclohexil-N'-{2-fluoro-4-[6-(1H-4-pirazolil)imidazo[1,2-a]piridin-3-il]fenil} urea; N-1 2-fluoro-4-[6-(1H-4-pirazolil)imidazo[1,2-a]piridin-3-iI]fenil}-N'-isopropil urea; o N1-{2-fluoro-4-[6-(1H-4-pirazolil)imidazo[1,2-a]piridin-3-il]fenil}-4- fluorobenzamida. Reivindicacion 34: Un proceso para la preparacion de un compuesto de formula (1) como se define en cualquiera de las reivindicaciones precedentes, proceso que comprende: (i) la reaccion de un compuesto de formula (20) o (21), o una de sus formas protegidas, con un isocianato sustituido en forma apropiada o una amina sustituida en forma apropiada en presencia de carbonil diimidazol (CDI); o (ii) la reaccion de un compuesto de formula (20) o (21), o una de sus formas protegidas, con un aldehído o cetona sustituidos en forma apropiada; o (iii) la reaccion de un compuesto de formula (20) o (21), en el cual X1-5, A y R2 son como se los define aquí; o una de sus formas protegidas, con un ácido carboxílico o un derivado reactivo sustituidos en forma apropiada; o (iv) hacer reaccionar un compuesto de formula (5) y (6), y luego eliminar cualquier grupo protector presente; y en forma opcional posteriormente convertir un compuesto de formula (1) en otro compuesto de formula (1).
ARP070105856A 2006-12-22 2007-12-21 Derivados de imidazo[1, 2-a]pirimidina, un proceso para su preparacion, una composicion farmaceutica que los comprende y su uso en el tratamiento de enfermedades mediadas por las quinasas fgfr. AR064491A1 (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US87154306P 2006-12-22 2006-12-22
GB0625826A GB0625826D0 (en) 2006-12-22 2006-12-22 New compounds
US97958707P 2007-10-12 2007-10-12
GB0720000A GB0720000D0 (en) 2007-10-12 2007-10-12 New compounds
US98103907P 2007-10-18 2007-10-18

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AR064491A1 true AR064491A1 (es) 2009-04-08

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US (1) US8895745B2 (es)
EP (1) EP2114941B1 (es)
JP (1) JP5442448B2 (es)
CN (1) CN101679408B (es)
AR (1) AR064491A1 (es)
AU (1) AU2007337886C1 (es)
CA (1) CA2672172C (es)
HR (1) HRP20150642T1 (es)
MX (1) MX2009006706A (es)
NO (1) NO343370B1 (es)
WO (1) WO2008078091A1 (es)

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MX2009006706A (es) 2009-07-02
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