AR066125A1 - Derivados de sulfonil amida para el tratamiento del crecimiento celular anormal - Google Patents
Derivados de sulfonil amida para el tratamiento del crecimiento celular anormalInfo
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- AR066125A1 AR066125A1 ARP080101626A ARP080101626A AR066125A1 AR 066125 A1 AR066125 A1 AR 066125A1 AR P080101626 A ARP080101626 A AR P080101626A AR P080101626 A ARP080101626 A AR P080101626A AR 066125 A1 AR066125 A1 AR 066125A1
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- Prior art keywords
- cycloalkenyl
- cycloalkyl
- alkyl
- heterocycloalkenyl
- heteroaryl
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
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Abstract
Reivindicacion 1: Un compuesto caracterizado porque es de formula 1, o una sal farmacéuticamente aceptable del mismo; en la que A es un resto anillo seleccionado entre el grupo constituido por: (a) carbociclilo de 4 a 7 miembros, (b) heterociclilode 4 a 7 miembros, (c) fenilo, y (d) anillo de heteroarilo de 5 a 6 miembros, en el que cada uno de dicho carbociclilo de 4 a 7 miembros y heterociclilo de 4 a 7 miembros de dicho grupo A puede contener opcionalmente uno o dos enlaces olefínicos; yen el que uno o dos átomos de carbono en el anillo en cada uno de dicho carbociclilo de 4 a 7 miembros y heterociclilo de 4 a 7 miembros de dicho grupo A puede reemplazarse independientemente opcionalmente por uno o dos restos seleccionadosindependientemente entre el grupo constituido por -C(O)-, -C(S)- y -C(=NR4)-; B es fenilo o un heteroarilo de 5 a 6 miembros; K es CH, C(NH2) o N; cada R1 se selecciona independientemente entre el grupo constituido por -H, halo, -CF3, -CN, -NO2, -NR7R8, NR7C(NR7R8)(=CR9), -CR7(NR7R8)(=NR7), -NR7C(NR7R8)(=NR7), -NR7C(O)R9, -C(O)NR7R8, -C(O)R9, -C(O)C(O)R9, -C(O)OR10, -OC(O)R9, -OR10, -OC(O)OR10, -S(O)jR11, -S(O)(=NR7)R8, -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-10, -cicloalquenilo C5-10, -bicicloalquilo C6-10, -bicicloalquenilo C6-10, -heterocicloalquilo C1-9, -heterocicloalquenilo C4-9, -heterobicicloalquilo C6-9, -heterobicicloalquenilo C6-9, -arilo C6-10, y -heteroarilo C1-9; y en el que cada uno de losrestos anteriores -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-10, -cicloalquenilo C5-10, -heterocicloalquilo C1-9, -heterocicloalquenilo C4-9, -arilo C6-10, y -heteroarilo C1-9; de dicho R1 está sustituido opcionalmenteindependientemente con de uno a tres grupos R12; cada uno de R2 y R3 se selecciona independientemente entre el grupo constituido por -H, -halo, -OR10, -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-10, -cicloalquenilo C5-10, -heterocicloalquilo C2-9, -heterocicloalquenilo C4-9, -arilo C6-10 y -heteroarilo C1-9; y en el que cada uno de los restos anteriores -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-10, -cicloalquenilo C5-10, -heterocicloalquilo C2-9, -heterocicloalquenilo C4-9, -arilo C6-10 y -heteroarilo C1-9 de dichos R2 y R3 está opcionalmente sustituido con de uno a tres grupos R12; cada uno de R4 y R5 se selecciona independientemente entre el grupo constituido por -H, -NR7R8, -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-10, -cicloalquenilo C5-10, -heterocicloalquilo C2-9, - heterocicloalquenilo C4-9, -arilo C6-10 y -heteroarilo C1-9; y en el que cada uno de los restos anteriores -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-10, -cicloalquenilo C5-10, -heterocicloalquilo C2-9, - heterocicloalquenilo C4-9, -arilo C6-10 y -heteroarilo C1-9 de dichos R4 y R5 está opcionalmente sustituido con de uno a tres grupos R12; R6 se selecciona entreel grupo constituido por -halo, -NR7R8, -OR10, -C(O)R9, -CO2R10, -CONR7R8, -S(O)jR11, -NR7CONR7R8, y -NR8SO2R11, -NO2, -CN, -CF3, -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -alquilo C2-6 perfluorado, -alquenilo C2-6 perfluorado, -alquinilo C3-6 perfluorado, -cicloalquilo C3-7, -cicloalquenilo C5-10, -bicicloalquilo C6-10, -bicicloalquenilo C6-10, -heterociclilo C1-9, -heterocicloalquenilo C1-10, -heterobicicloalquilo C6-9, -heterobicicloalquenilo C6-9, -arilo C6-10, -heteroarilo C1-9, -arilo C6-10 perfluorado, y -heteroarilo C1-9 perfluorado; y en el que cada uno de dichos restos -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-7, -cicloalquenilo C5-10, -bicicloalquilo C6-10, -bicicloalquenilo C6-10, -heterociclilo C1-9, -heterocicloalquenilo C1-10, -heterobicicloalquilo C6-9, -heterobicicloalquenilo C6-9, -arilo C6-10, y -heteroarilo C1-9, de dicho R6 está opcionalmente sustituido con de uno a tres grupos R12; cada uno de R7 y R8 se seleccionaindependientemente entre el grupo constituido por -H, -OR10, -S(O)jR11, -NO2, -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-10, -cicloalquenilo C5-10, -bicicloalquilo C6-10, -bicicloalquenilo C6-10, -heterocicloalquilo C2-9, -heterocicloalquenilo C4-9, -heterobicicloalquilo C6-9, heterobicicloalquenilo C6-9, -arilo C6-10, y -heteroarilo C1-9; y en el que cada uno de los restos anteriores -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-10, -cicloalquenilo C5-10, -heterocicloalquilo C2-9, -heterocicloalquenilo C4-9, -arilo C6-10 y -heteroarilo C1-9 de dichos R7 y R8 está opcionalmente sustituido con de uno a tres grupos R12; cada R9 se selecciona independientemente entre el grupoconstituido por -H, -halo, -NR13R14, -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-10, -cicloalquenilo C5-10, -bicicloalquilo C6-10, bicicloalquenilo C6-10, -heterocicloalquilo C2-9, -heterocicloalquenilo C4-9, -heterobicicloalquilo C6-9, -heterobicicloalquenilo C6-9, -arilo C6-10 y -heteroarilo C1-9; y en el que cada uno de los restos anteriores -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-10, -cicloalquenilo C5-10, -heterocicloalquiloC2-9, -heterocicloalquenilo C4-9, -arilo C6-10 y -heteroarilo C1-9 de dicho R9 está opcionalmente sustituido con de uno a tres grupos R12; cada R10 se selecciona independientemente entre el grupo constituido por -H, -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-10, -cicloalquenilo C5-10, -bicicloalquilo C6-10, -bicicloalquenilo C6-10, - heterocicloalquilo C2-9, -heterocicloalquenilo C4-9, -heterobicicloalquilo C6-9, -heterobicicloalquenilo C6-9, -arilo C6-10, y -heteroariloC1-9; y en el que cada uno de los restos anteriores -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-10, -cicloalquenilo C5-10, - heterocicloalquilo C2-9, -heterocicloalquenilo C4-9, -arilo C6-10 y -heteroarilo C1-9 de dicho R10está opcionalmente sustituido con de uno a tres grupos R12; cada R11 se selecciona independientemente entre el grupo constituido por -H, -NR13R14, -C(O)R13, -CF3, -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-10, -cicloalqueniloC5-10, -bicicloalquilo C6-10, -bicicloalquenilo C6-10, - heterocicloalquilo C2-9, -heterocicloalquenilo C4-9, -heterobicicloalquilo C6-9, -heterobicicloalquenilo C6-9, -arilo C6-10, y -heteroarilo C1-9; y en el que cada uno de los restos anteriores -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-10, -cicloalquenilo C5-10, - heterocicloalquilo C2-9, -heterocicloalquenilo C4-9, -arilo C6-10 y -heteroarilo C1-9 de dicho R10 está opcionalmente sustituido con de uno a tres gruposR12; cada R12 se selecciona independientemente entre el grupo constituido por -H, -OR13, -C(O)R13, -C(O)OR13, -OC(O)R13, -OC(O)OR13, -C(O)NR13R14, -NR13C(O)NR13R14, -NR13R14, -NR13C(NR13R14)(=NR13), -NR13C(NR13R14)(=N-C(O)R13), -NR13C(O)R14, -NR13S(O)jR13, -S(O)jR13, -CF3, -CN, -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-10, -cicloalquenilo C5-10, -bicicloalquilo C6-10, bicicloalquenilo C6-10, -heterocicloalquilo C2-9, -heterocicloalquenilo C4-9, -heterobicicloalquilo C6-9, -heterobicicloalquenilo C6-9, -arilo C6-10 y -heteroarilo C1-9; en el que cada uno de los anteriores -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-10, -cicloalquenilo C5-10, -bicicloalquilo C6-10,bicicloalquenilo C6-10, -heterocicloalquilo C2-9, -heterocicloalquenilo C4-9, -heterobicicloalquilo C6-9, -heterobicicloalquenilo C6-9, -arilo C6-10 y -heteroarilo C1-9 de dicho R12 están sustituido opcionalmente independientemente con de uno a tresgrupos seleccionados entre el grupo constituido por -halo, -CF3, -CN, -NO2, -OH, -O(alquilo C1-6), -C(O)R15, C(O)NR15R16, -S(O)jR15, y -S(O)jNR15R16, -cicloalquilo C3-10, -heterocicloalquilo C2-9, -SH, -S(alquilo C1-6), -NH2,-NH(alquilo C1-6) y -N(alquilo C1-6)2; cada uno de R13 y R14 se selecciona independientemente entre el grupo constituido por -H, -NR15C(O)R16, -CF3, -CN, -S(O)jR15, -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-10, -cicloalquenilo C5-10, -bicicloalquilo C6-10, -bicicloalquenilo C6-10, -heterocicloalquilo C2-9, -heterocicloalquenilo C4-9, -heterobicicloalquilo C6-9, -heterobicicloalquenilo C6-9, -arilo C6-10, y -heteroarilo C1-9; y en el que cada uno de los anteriores -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-10, -cicloalquenilo C5-10, -bicicloalquilo C6-10, -bicicloalquenilo C6-10, -heterocicloalquilo C2-9, -heterocicloalquenilo C4-9, -heterobicicloalquilo C6-9, -heterobicicloalquenilo C6-9, -arilo C6-10, y -heteroarilo C1-9 de dichos R13 y R14 están sustituidos opcionalmente independientemente con de uno a tres grupos seleccionados entre el grupo constituido por -halo, -CF3, -CN, -NO2, -OH, -O(alquilo C1-6), -C(O)(alquilo C1-6), -cicloalquilo C3-10, heterocicloalquilo C2-9, -SH, -S(alquilo C1-6), -NH2, -NH(alquilo C1-6) y-N(alquilo C1-6)2; cada uno de R15 y R16 se selecciona independientemente entre el grupo constituido por -H, -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquiloC3-10, -cicloalquenilo C5-10, -bicicloalquilo C6-10, -bicicloalquenilo C6-10, -heterocicloalquilo C2-9, -heterocicloalquenilo C4-9, -heterobicicloalquilo C6-9, -heterobicicloalquenilo C6-9, -arilo C6-10, y -heteroarilo C1-9; y en el que cada uno delos anteriores -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-10, -cicloalquenilo C5-10, -bicicloalquilo C6-10, -bicicloalquenilo C6-10, -heterocicloalquilo C2-9, -heterocicloalquenilo C4-9, -heterobicicloalquilo C6-9, -heterobicicloalquenilo C6-9, -arilo C6-10, y -heteroarilo C1-9 de dichos R15 y R16 están sustituidos opcionalmente independientemente con de uno a tres grupos seleccionados entre el grupo constituido por -halo, -CF3, -CN, -NO2, -OH, -O(alquilo C1-6), -C(O)(alquilo C1-6), -cicloalquilo C3-10, heterocicloalquilo C2-9, -SH, -S(alquilo C1-6), -NH2, -NH(alquilo C1-6) y-N(alquilo C1-6)2; en el que uno o dos átomos de carbono en el anillo en
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