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AR061842A1 - Pirimidil ciclopentanos hidroxilados y metoxilados como inhibidores de la proteina quinasa akt - Google Patents

Pirimidil ciclopentanos hidroxilados y metoxilados como inhibidores de la proteina quinasa akt

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Publication number
AR061842A1
AR061842A1 ARP070103033A ARP070103033A AR061842A1 AR 061842 A1 AR061842 A1 AR 061842A1 AR P070103033 A ARP070103033 A AR P070103033A AR P070103033 A ARP070103033 A AR P070103033A AR 061842 A1 AR061842 A1 AR 061842A1
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AR
Argentina
Prior art keywords
alkyl
optionally substituted
phenyl
cycloalkyl
attached form
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ARP070103033A
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Array Biopharma Inc
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Application filed by Array Biopharma Inc filed Critical Array Biopharma Inc
Publication of AR061842A1 publication Critical patent/AR061842A1/es

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Abstract

También se proporcionan métodos de uso de los compuestos de la presente como inhibidores de la proteína quinasa AKT y para el tratamiento de enfermedades proliferativas tales como el cáncer. Reivindicacion 1: Un compuesto de formula 1 y sus tautomeros, enantiomeros resueltos, diastereomeros resueltos, solvatos, metabolitos y sales, en los cuales: R1 es H, Me, Et, vinilo, CF3, CHF2 o CH2F; R2 es H o Me; R5 es H, Me, Et o CF3; A es como se muestra en formula (2); G es fenilo sustituido en forma opcional con uno a cuatro grupos R9 o un heteroarilo de 5-6 miembros sustituido en forma opcional con un halogeno; R6 y R7 son de manera independiente H, OCH3, cicloalquil C3-6-(CH2), cicloalquil C3-6-(CH2CH2), V-(CH2)0-1 donde V es un heteroarilo de 5-6 miembros, W-(CH2)1-2 donde W es fenilo sustituido en forma opcional con F, CI, Br, I, OMe, CF3 o Me, cicloalquilo C3-6 sustituido en forma opcional con alquilo C1-3 u Oalquilo C1-3, hidroxi-cicloalquilo C3-6, fluor-cicloalquilo C3- 6, CH(CH3)CH(OH)fenilo, heterociclo de 4-6 miembros sustituido en forma opcional con F, OH, alquilo C1-3, ciclopropilmetilo o C(=O)alquilo C1-3 o alquilo C1-6 sustituido en forma opcional con uno o más grupos seleccionados de manera independiente de OH, oxo, Oalquilo C1-6, CN, F, NH2, NHalquilo C1-6, N(alquil C1-6)2, ciclopropilo, fenilo, imidazolilo, piperidinilo, pirrolidinilo, morfolinilo, tetrahidrofuranilo, oxetanilo o tetrahidropiranilo, o R6 y R7 junto con el nitrogeno al cual están unidos forman un anillo heterocíclico de 4-7 miembros sustituido en forma opcional con uno o más grupos seleccionados de manera independiente de OH, halogeno, oxo, CF3, CH2CF3, CH2CH2OH, Oalquilo C1-3, C(=O)CH3, NH2, NHMe, N(Me)2, S(O)2CH3, ciclopropilmetilo y alquilo C1-3; Ra y Rb son H, o Ra es H y Rb y R6 junto con los átomos a los cuales están unidos forman un anillo heterocíclico de 5-6 miembros que tiene uno o dos átomos de nitrogeno en el anillo; Rc y Rd son H o Me, o Rc y Rd junto con el átomo al cual están unidos forman un anillo ciclopropilo; R8 es H, Me, E u OH, o R8 y R6 junto con los átomos a los cuales están unidos forman un anillo heterocíclico de 5-6 miembros que tiene uno o dos átomos de nitrogeno en el anillo; cada R9 es de manera independiente halogeno, alquilo C1-6, cicloalquilo C3-6, O-alquilo C1-6, CF3, OCF3, Salquilo C1-6, CN, OCH2-fenilo, CH2O- fenilo, NH2, NH-alquilo C1-6, N-(alquil C1-6)2, piperidina, pirrolidina, CH2F, CHF2, OCH2F, OCHF2, OH, SO2alquilo C1-6, C(O)NH2, C(O)NHalquilo C1-6 y C(O)N(alquil C1-6)2; R10 es H o Me; y m, n y p son de manera independiente 0 o 1.
ARP070103033A 2006-07-06 2007-07-06 Pirimidil ciclopentanos hidroxilados y metoxilados como inhibidores de la proteina quinasa akt AR061842A1 (es)

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US81871806P 2006-07-06 2006-07-06

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AR061842A1 true AR061842A1 (es) 2008-09-24

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ARP070103033A AR061842A1 (es) 2006-07-06 2007-07-06 Pirimidil ciclopentanos hidroxilados y metoxilados como inhibidores de la proteina quinasa akt
ARP130104510A AR093810A2 (es) 2006-07-06 2013-12-05 Pirimidil ciclopentanos hidroxilados y metoxilados como inhibidores de la proteina quinasa ak, sus usos, composiciones, kits y formas de dosificacion
ARP170102366A AR109424A2 (es) 2006-07-06 2017-08-25 Pirimidil ciclopentanos hidroxilados y metoxilados como inhibidores de la proteína quinasa akt

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ARP130104510A AR093810A2 (es) 2006-07-06 2013-12-05 Pirimidil ciclopentanos hidroxilados y metoxilados como inhibidores de la proteina quinasa ak, sus usos, composiciones, kits y formas de dosificacion
ARP170102366A AR109424A2 (es) 2006-07-06 2017-08-25 Pirimidil ciclopentanos hidroxilados y metoxilados como inhibidores de la proteína quinasa akt

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EP (4) EP2399909B1 (es)
JP (4) JP5266216B2 (es)
KR (5) KR101495408B1 (es)
CN (2) CN101578273B (es)
AR (3) AR061842A1 (es)
AT (1) ATE524447T1 (es)
AU (1) AU2007269060B2 (es)
BR (3) BRPI0713923B8 (es)
CA (2) CA2836316A1 (es)
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