ES2354824T3 - Pirazolo[1,5-a]pirimidinas útiles como inhibidores de proteínas cinasas. - Google Patents

Pirazolo[1,5-a]pirimidinas útiles como inhibidores de proteínas cinasas. Download PDF

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ES2354824T3
ES2354824T3 ES05816516T ES05816516T ES2354824T3 ES 2354824 T3 ES2354824 T3 ES 2354824T3 ES 05816516 T ES05816516 T ES 05816516T ES 05816516 T ES05816516 T ES 05816516T ES 2354824 T3 ES2354824 T3 ES 2354824T3
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inhibitors
useful
pirazolo
pyrimidins
kinase proteins
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Dean Stamos
Juan-Miguel Jimenez
Alex Aronov
Ronald Knegtel
Jon R. Come
Jean-Damien Charrier
Pan Li
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Abstract

Un compuesto de fórmula I': Fórmula a I' o una sal farmacéuticamente aceptable del mismo, en la que R es -(C=Q)R2a, CN, o Y; en la que Y es un anillo de heterociclilo, arilo o heteroarilo, monocíclico o bicíclico, de 5-10 miembros; cada Y está independiente y opcionalmente sustituido con 0-5 JY; Q es O, NH, NR', o S; R' es alquilo C1-6 opcionalmente sustituido con 0-4 apariciones de halo, alifático C1-6, NO2, NH2, -N(alquil C1-6), -N (alquil C1-6)2, SH, -S(alquil C1-6), OH, -O(alquil C1-6), -C(O)(alquil C1- 6), -C(O)NH2, -C(O)N(alquil C1-6), o -C(O)N (alquil C1-6)2; R2a es alifático C1-6, arilo C6-10, heteroarilo de 5-10 miembros, heterociclilo de 5-10 miembros, OR5, o N(R5)2; cada R2a está independiente y opcionalmente sustituido con 0-5 J2a; R1 es H, -C(O)(alquil C1-6), -C(O)O(alquil C1-6), -C(O)NH2, -C(O)N(alquil C1-6), - C(O)N(alquil C1-6)2; o alifático C1-6; cada R1 está opcionalmente sustituido con 0-4 apariciones de halo, haloalquilo C1-6, alifático C1-6, NO2, NH2, -N (alquil C1-6), -N(alquil C1-6)2, SH, -S(alquil C1-6), OH, o -O(alquil C1-6); Z es un enlace o alifático C1-6 en la que hasta dos unidades metileno de la cadena alifática están opcional e independientemente reemplazadas por un heteroátomo seleccionado entre O, N o S, en una disposición químicamente estable; cada R3 y R4 es, independientemente, H, halógeno, alcoxi C1-6, N(R5)2, CN, NO2, o Um-V en la que m es 0 ó 1; V es H, arilo C6-10, heteroarilo de 5-10 miembros, cicloalifático C3-10, heterociclilo de 5-10 miembros, o alifático C1-12 en la que hasta dos unidades metileno de la cadena de alquilideno están opcional e independientemente reemplazadas por un heteroátomo seleccionado entre O, N o S, en una disposición químicamente estable; V está opcionalmente sustituido con 0-4 R8; U es alquilideno de cadena de C1-12 en la que hasta dos unidades metileno de la cadena están opcional e independientemente reemplazadas por -NH-, -NR530 -, -O-, -S-, -CO2-, -OC(O)-, - C(O)CO-, -C(O)-, -C(O)NH-, -C(O)NR5-, -C(=N-CN), -NH-CO-, -NR5CO-, -NHC(O)O-, - NR5C(O)O-, -SO2NH-, -SO2NR5-, -NHSO2-, -NR5SO2-, -NHC(O)NH-, -NR5C(O) NH-, - NHC(O)NR5-, -NR5C(O)NR5, -OC(O)NH-, -OC(O)NR5-, -NHNH-, -NHNR5-, -NR5NR5-, -NR5NH-, -NHSO2NH-, -NR5SO2NH-, -NHSO2NR5-, -NR5SO2NR5-, -SO-, -SO2-, -PO-, -PO2-, o -POR5-; U está opcionalmente sustituido con 0-6 JU; R5 es haloalquilo C1-4, -C(O)COR6, -C(O)R6, -C(O)OR6, -C(O)N(R6)2, -SO2R6, alquil C0-6- heterociclilo, alquil C0-6-heteroarilo, alquil C0-6-arilo, alquil C0-6- cicloalifático o alifático C1-6 en 5 la que hasta tres unidades metileno de la cadena alifática están opcional e independientemente reemplazadas por -NR"-, -O-, -S-, -CO2-, - OC(O)-, -C(O)CO-, -C (O)-, -C(O)NR"-, -NR"CO-, - NR"C(O)O-, -SO2NR"-, -NR"SO2-, -C(O)NR"NR"-, -NR"C(O)NR"-, -OC(O)NR"-, -NR"NR"-, - NR"SO2NR"-, -SO-, -SO2-, -PO-, -PO2-, o -POR"- en una disposición químicamente estable; cada R5 está independiente y opcionalmente sustituido con 0-5 JR5; o dos grupos R5 10 tomados junto con el átomo al que están enlazados, se unen opcionalmente para formar un anillo carbocíclico o heterocíclico de 5-10 miembros; en el que dicho anillo está opcionalmente sustituido con 0-4 J'; R6 es H, alcoxi C1-6, haloalquilo C1-4, alquil C0-6-heterociclilo, alquil C0-6-heteroarilo, alquil C0-6-arilo, alquil C0-6-cicloalifático, o alifático C1-6 en la que hasta dos unidades metileno de la cadena alifática están opcional e independientemente reemplazadas por un heteroátomo seleccionado entre O, N o S, en una disposición químicamente estable; cada R6 está independiente y opcionalmente sustituido con 0-5 JR6; o dos grupos R6 tomados junto con el átomo al que están enlazados, se unen opcionalmente para formar un anillo carbocíclico o heterocíclico de 5-10 miembros; en el que dicho anillo está opcionalmente sustituido con 0-4 J"; R8 es halógeno, haloalquilo C1-4, fenilo, heterociclilo de 5-8 miembros, heteroarilo de 5-6 miembros, -OR6, -N(R6)2, -SR6, NO2, CN, -COOR6, -C(O)N(R6)2, -SO2R6, - SO2N(R6)2, - NR6C(O)R6, -C(O)R6, -OC(O)R6, -NR6C(O)O-R6, -NR6SO2-R6, -C(O)NR6N(R6)2, - NR6C(O)N(R6)2, -OC(O)N(R6)2, -NR6N(R6)2, -NR6SO2N(R6)2 o alifático C1-12, en la que hasta tres unidades metileno de la cadena alifática pueden estar opcionalmente interrumpidas con - C(O)R6, -C(O)O-, -OC(O)-, -C(O)-, -C(O)N(R6)-, -NR6CO(R6)-, -O-, -NR6-, o -S-; cada R8 está independiente y opcionalmente sustituido con 0-5 JR8; cada JY, J2a, Ju, JR5, JR6, JR8, J', y J" se selecciona independientemente entre N(R9)2, SR9, OR9, halo, CN, NO2, COOR9, C(O)R9, SO2R9, SOR9, -X-CF3, -X-SH, -X-OH, haloalquilo C1- 4, arilo C6-10, -X-(arilo C6-10), heteroarilo de 5-10 miembros, -X-(heteroarilo de 5-10 miembros), cicloalifático C3-10, -X-(cicloalifático C3-10), heterociclilo de 5-10 miembros, -X-(heterociclilo de 5- 10 miembros), o X; X es alifático C1-12 en la que hasta dos unidades metileno de la cadena de alquilideno están opcional e independientemente reemplazadas por -NH-, -NR"-, -O-, -S-, -CO2-, -OC(O)-, - C(O)CO-, -C(O)-, -C(O)NH-, -C(O)NR"-, -C(=N-CN), -NHCO-, -NR"CO-, -NHC(O)O-, - NR"C(O)O-, -SO2NH-, -SO2NR"-, -NHSO2-, -NR"SO2- -NHC(O)NH-, -NR"C(O)NH-, - NHC(O)NR"-, -NR"C(O)NR", -OC(O)NH-, -OC(O)NR"-, -NHNH-, -NHNR"-, -NR"NR"-, -NR"NH-, -NHSO2NH-, -NR"SO2NH-, -NHSO2NR"-, -NR"SO2NR"-, -SO-, -SO2-, -PO-, -PO2-, o -POR"-; en una disposición químicamente estable; en las que R" es H o alifático C1-6; cada JY, J2a, Ju, JR5, JR6, J', y J" está opcional e independientemente sustituido con 0-5 4 apariciones de N(R9)2, SR9, OR9, halo, CN, NO2, COOR9, C(O)R9, SO2R9, SOR9, -X-CF3, -X-SH, -X-OH, haloalquilo C1-4, arilo C6-10, -X-(arilo C6-10), heteroarilo de 5-10 miembros, -X-(heteroarilo de 5-10 miembros), cicloalifático C3-10, -X-(cicloalifático C3-10), heterociclilo de 5-10 miembros, - X-(heterociclilo de 5-10 miembros), o X; R9 es H, alifático C1-6, haloalquilo C1-4, arilo C6-10, -X-(arilo C6-10), heteroarilo de 5-10 miembros, -X-(heteroarilo de 5-10 miembros), cicloalifático C3-10, -X-(cicloalifático C3-10), heterociclilo de 5-10 miembros, -X-(heterociclilo de 5-10 miembros) o X, o en las que dos R9, tomados junto con el átomo al que están unidos, forman un heterociclilo de 5-10 miembros, en la que dicho heterociclilo está opcionalmente sustituido con 0-4 apariciones de halo, CN, NO2, - COOH, -COO(alquil C1-6), -C(O)H, SO2H, SO2(alquil C1-6), haloalifático C1-6, NH2, -NH(alquil C1- 6), -N (alquil C1-6)2 , SH, -S(alquil C1-6) , OH, - O(alquil C1-6), -C(O)(alquil C1-6), -C(O)NH2, - C(O)NH(alquil C1-6), -C(O)N(alquil C1-6)2, -C(O)NH2, -C(O)NH(alquil C1-6), o -C(O)N(alquil C1-6)2, haloalquilo C1-4, arilo C6-10, -X-(arilo C6-10), heteroarilo de 5-10 miembros, -X-(heteroarilo de 5-10 miembros), cicloalifático C3-10, -X-(cicloalifático C3-10), heterociclilo de 5-10 miembros, -X- (heterociclilo de 5-10 miembros), o X, con lo que se excluyen los siguientes compuestos: - 3-(2-amino-5-metil-pirazolo[1,5-a]pirimidin-3-il)azo-4,6- dimetiltieno[2,3-b]piridina, - 5-fenil-3-fenilazo-pirazolo[1,5-a]pirimidin-2-ilamina.
ES05816516T 2004-11-04 2005-11-04 Pirazolo[1,5-a]pirimidinas útiles como inhibidores de proteínas cinasas. Active ES2354824T3 (es)

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