AR046119A1 - Pirimidinas sustituidas con sulfoximina como inhibidores de cdk y / o vegf su preparacion y sus usos como medicamento - Google Patents

Pirimidinas sustituidas con sulfoximina como inhibidores de cdk y / o vegf su preparacion y sus usos como medicamento

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AR046119A1
AR046119A1 ARP040103755A ARP040103755A AR046119A1 AR 046119 A1 AR046119 A1 AR 046119A1 AR P040103755 A ARP040103755 A AR P040103755A AR P040103755 A ARP040103755 A AR P040103755A AR 046119 A1 AR046119 A1 AR 046119A1
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Argentina
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alkyl
alkoxy
hydroxy
cycloalkyl
group
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ARP040103755A
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Ulrich Lucking
Gerhard Siemeister
Martin Kruger
Rolf Jautelat
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Schering Ag
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Abstract

Derivados de pirimidina de la fórmula general (1), en donde: Q es el grupo de fórmulas (2); D, E, G, L, M y T son en cada caso de forma independiente entre sí, son carbono, oxígeno, nitrógeno o azufre; R1 es hidrógeno, halógeno, alquilo C1-6, CF3, CN, nitro, o el grupo -COR8 u -O-alquilo-(C1-6); R2 es hidrógeno o alquilo-(C1-10), alquenilo-(C2-10), alquinilo-(C2-10), ciclo-alquilo-(C3-10), arilo o heteroarilo opcionalmente mono-sustituido o polisustituido, igual o diferente, con hidroxi, halógeno, alcoxi-(C1-6), amino, ciano, alquilo-(C1-6), -NH-(CH2)n-cicloalquilo-(C3-10), -cicloalquilo-(C3-10), hidroxialquilo-(C1-6), alquenilo-(C2-6), alquinilo-(C2-6), alcoxi-(C1-6)-alquilo-(C1-6), -alcoxi-(C1-6)-alcoxi-(C1-6)-alquilo-(C1-6), NH- alquilo-(C1-6), -N(alquilo-C1-6)2, alcanoilo-(C1-6), -CONR9R10, -COR8, alquilo-(C1-6)-Ac, carboxi, arilo, heteroarilo, -(CH2)n-arilo, -(CH2)n-heteroarilo, fenil-(CH2)n-R8, -(CH2)n-PO3(R8)2 o con el grupo -R6 o -NR9R10 y el fenilo, -cicloalquilo-C3- 10, AM, heteroarilo, -(CH2)n-arilo y -(CH2)n-heteroarilo en sí puede estar opcionalmente monosustituido o polisustituido, igual o diferente, con halógeno, hidroxi, alquilo-(C1-6), alcoxi-(C1-6), o con el grupo -CF3 u -OCF3, y el anillo del cicloalquilo-(C3-10) y el alquilo-(C1-10) puede estar opcionalmente interrumpido por uno o varios átomos de nitrógeno, oxígeno y/o azufre y/o por uno o varios grupos -C(O)- en el anillo y/o en el anillo puede haber opcionalmente uno o varios enlaces dobles posibles; X es oxígeno, azufre o el grupo -NH- o -N(alquilo-C1-3)-; o X y R2 juntos forman un anillo cicloalquilo-(C3-10), que opcionalmente puede contener uno o varios heteroátomos, y opcionalmente puede estar monosustituido o polisustituido, igual o diferente, con hidroxi, alquilo-(C1-6), alcoxi-(C1-6), halógeno o el grupo -NR9R10; R3 es hidrógeno, hidroxi, halógeno, CF3, OCF3 o el grupo -NR9R10 o alquilo-(C1-6), cicloalquilo-(C3-6) o alcoxi-(C1-6) opcionalmente monosustituido o polisustituido, igual o diferente, con halógeno, hidroxi, alcoxi-(C1-6) o el grupo -NR9R10; m es 0-4; R4 es hidrógeno o el grupo -COR8, NO2, trimetilsilanilo (TMS), ter-butil-dimetilsilanilo (TBDMS), tert-butil-difenilsilanilo (TBDPS), trietilsilanilo (TES) o -SO2R7 o alquilo-(C1-10) o cicloalquilo-(C3-10), opcionalmente monosustituido o polisustituido, igual o diferente, con hidroxi, halógeno, alcoxi-(C1-6), alquiltio-(C1-6), ciano, cicloalquilo-(C3-10), hidroxialquilo- (C1-6), alquenilo-(C2-6), alquinilo-(C2-6), alcoxi-(C1-6)-alquilo-(C1-6), alcoxi-(C1-6)-alcoxi-(C1-6)-alquilo-(C1-6) o con el grupo -CONR9R10, -COR8, -CF3, -OCF3 o -NR9R10; R5 es alquilo-(C1-10), alquenilo-(C2-6), alquinilo-(C2-6) o cicloalquilo-(C3- 10) opcionalmente monosustituido o polisustituido, igual o diferente, con hidroxi, alcoxi-(C1-6), cicloalquilo-(C3-10), halógeno o el grupo -NR9R10; o R4 y R5 pueden formar juntos un anillo cicloalquilo-(C5-10) del grupo de fórmula (3), en donde: V, W e Y son en cada caso de forma independiente entre sí, -CH2- opcionalmente monosustituido o polisustituido, igual o diferente, con hidroxi, alquilo-(C1-10), alcoxi-(C1-10) o -NR9R10, en donde alquilo-(C1-10) o alcoxi-(C1-10) también puede estar monosustituido o polisustituido, igual o diferente, con hidroxi, -NR9R10 o alcoxi-(C1-10) y/o puede estar interrumpido por uno o varios grupos -C(O)- en el anillo y/o en el anillo puede haber opcionalmente uno o varios enlaces dobles; R6 es un anillo heteroarilo o cicloalquilo-(C3-10), que opcionalmente puede contener uno o varios heteroátomos y opcionalmente puede estar monosustituido o polisustituido, igual o diferente, con hidroxi, alquilo-(C1-6), alcoxi-(C1-6) o halógeno; R7 es alquilo-(C1-10) o arilo opcionalmente monosustituido o polisustituido, igual o diferente, con halógeno, hidroxi, alquilo-(C1-6), alcoxi-(C1-6) o con el grupo trimetilsilanilo (TMS) o -NR9R10; R8 es hidrógeno, alquilo-(C1-6), hidroxi, alcoxi-(C1-6), alquiltio-(C1-6), benzoxi o -NR9R10; R9 y R10 son en cada caso de forma independiente entre sí, hidrógeno, alquilo-(C1-6), alcoxi-(C1-6), hidroxi, hidroxi-alquilo-(C1-6), di-hidroxi-alquilo-(C1-6), fenilo, heteroarilo o el grupo -(CH2)n-NR9R10, - CNHNH2 o -NR9R10; o R9 y R10 juntos forman un anillo cicloalquilo -(C3-10), que opcionalmente puede estar interrumpido por uno o varios átomos de nitrógeno, oxígeno y/o azufre y/o puede estar interrumpido por uno o varios grupos -C(O)- en el anillo y/o en el anillo puede haber opcionalmente uno o varios enlaces dobles posibles; y n es 1-6, así como sus isómeros, diastereoisómeros, enantiómeros y/o sales, como inhibidores de las quinasas dependientes de ciclinas y tirosina quinasas de los receptores de VEGF, su preparación, y sus usos como medicamento para el tratamiento de diversas enfermedades.
ARP040103755A 2003-10-16 2004-10-15 Pirimidinas sustituidas con sulfoximina como inhibidores de cdk y / o vegf su preparacion y sus usos como medicamento AR046119A1 (es)

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DE10349423A DE10349423A1 (de) 2003-10-16 2003-10-16 Sulfoximinsubstituierte Parimidine als CDK- und/oder VEGF-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel

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