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AR101198A1 - Pirimidinas 2,5-sustituidas como inhibidores de pde4b - Google Patents

Pirimidinas 2,5-sustituidas como inhibidores de pde4b

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Publication number
AR101198A1
AR101198A1 ARP150102233A ARP150102233A AR101198A1 AR 101198 A1 AR101198 A1 AR 101198A1 AR P150102233 A ARP150102233 A AR P150102233A AR P150102233 A ARP150102233 A AR P150102233A AR 101198 A1 AR101198 A1 AR 101198A1
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AR
Argentina
Prior art keywords
alkyl
alkylene
co2h
cycloalkyl
alkoxy
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ARP150102233A
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English (en)
Inventor
Dr Hesslinger Christian
Dr Craan Tobias
Dr Konetzki Ingo
Dr Jakob Florian
Dr Nardi Antonio
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Gruenenthal Gmbh
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Publication of AR101198A1 publication Critical patent/AR101198A1/es

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Abstract

Su uso como medicamentos, en particular como medicamentos para el tratamiento de condiciones y enfermedades que se pueden tratar por inhibición de la enzima PDE4. Reivindicación 1: Pirimidinas 2,5-sustituidas caracterizadas porque tienen la fórmula general (1), en donde A, B, C en forma independiente entre sí significan N o CH; R¹ significa C₁₋₆-alquilo, C₁₋₆-hidroxialquilo, C₁₋₆-haloalquilo, C₃₋₆-cicloalquilo, SOˣ-C₁₋₆-alquilo, CONH₂, CONH-C₁₋₆-alquilo, CON(C₁₋₆-alquilo)₂; x es 0, 1 ó 2; G es un fenilo o heteroarilo de 5 ó 6 miembros opcionalmente sustituido con al menos un sustituyente Y que contiene al menos un átomo de oxígeno, azufre o nitrógeno, donde los átomos de nitrógeno presentes en el heteroarilo pueden estar sustituidos con R⁴; R⁴ es hidrógeno, C₁₋₆-alquilo, C₁₋₆-haloalquilo, CO-C₁₋₆-alquilo, SO-C₁₋₆-alquilo, SO₂-C₁₋₆-alquilo; Y es OH, CN, SH, C₁₋₆-alquilo, C₂₋₆-alquenilo, C₂₋₆-alquinilo, C₃₋₆-cicloalquilo, C₁₋₆-alcoxi, C₁₋₆-tioalquilo, C₁₋₆-haloalquilo, C₁₋₆-tiohaloalquilo, C₁₋₆-haloalcoxi, CO₂H, CO₂-C₁₋₆-alquilo, CHO, CO-C₁₋₆-alquilo, OCO-C₁₋₆-alquilo, CONH₂, CONH-C₁₋₆-alquilo, CON(C₁₋₆-alquilo)₂, OCO-NH-C₁₋₆-alquilo, OCO-N(C₁₋₆-alquilo)₂, NH₂, NH-C₁₋₆-alquilo, N(C₁₋₆-alquilo)₂, N-pirrolidinilo, N-piperidinilo, N-morfolinilo, NH-CO-C₁₋₆-alquilo, NH-CO₂-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO₂-C₁₋₆-alquilo, NH-CO-NH₂, NH-CO-NH-C₁₋₆-alquilo, NH-CO-N(C₁₋₆-alquilo)₂, N-C₁₋₆-alquil-CO-NH₂, N-C₁₋₆-alquil-CO-NH-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO-N(C₁₋₆-alquilo)₂, NH-SO₂-C₁₋₆-alquilo, N-C₁₋₆-alquil-SO₂-C₁₋₆-alquilo, S-C₁₋₆-alquilo, SO-C₁₋₆-alquilo, SO₂-C₁₋₆-alquilo, SO₂H, SO₂OH, SO₂NH₂, SO₂NH-C₁₋₆-alquilo, SO₂N(C₁₋₆-alquilo)₂, C(=N)-NH, NHC(=N)-NH₂, -N=C=O, -S-CN, donde las cadenas alquilo mencionadas, precedentemente pueden estar sustituidas con al menos uno de los siguientes sustituyentes: OH, CN, C₃₋₆-cicloalquilo, C₁₋₆-alcoxi, CO₂H, CO₂-C₁₋₆-alquilo o -NH₂; R² y R³ en forma independiente entre sí significan hidrógeno o C₁₋₆-alquilo, C₁₋₆-haloalquilo, C₁₋₆-hidroxialquilo, C₁₋₆-alcoxi-C₁₋₆-alquileno, C₁₋₆-alquilen-CO₂H, C₁₋₆-alquilen-CO₂-C₁₋₆-alquilo, C₁₋₆-alquilen-CONH₂, C₁₋₆-alquilen-CONH-C₁₋₆-alquilo, C₁₋₆-alquilen-CON(C₁₋₆-alquilo)₂, C₁₋₆-alquilen-C₃₋₆-cicloalquilo, C₁₋₆-hidroxialquil-C₃₋₆-cicloalquileno opcionalmente sustituido, un grupo L¹V, un grupo L²W, o R² y R³ junto con el átomo de nitrógeno al cual están unidos forman un residuo heteroalifático monocíclico o bicíclico de entre 3 y 12 miembros opcionalmente sustituido con al menos un sustituyente XQ Q que puede contener adicionalmente al menos un átomo de oxígeno, azufre o nitrógeno adicional, donde estos átomos de nitrógeno adicionales están sustituidos con R⁵; XQ en forma independiente entre sí significan =O (carbonilo), halógeno, OH, CN, SH, C₁₋₆-alquilo, C₁₋₆-hidroxialquilo, C₁₋₆-cianoalquilo, C₂₋₆-alquenilo, C₂₋₆-alquinilo, C₃₋₆-cicloalquilo, C₁₋₆-alcoxi, C₁₋₆-alcoxi-C₁₋₆-alquileno, C₁₋₆-tioalquilo, C₁₋₆-haloalquilo, C₁₋₆-tiohaloalquilo, C₁₋₆-haloalcoxi, -NH₂, NH-C₁₋₆-alquilo, N(C₁₋₆-alquilo)₂, C₁₋₆-alquilen-NH-C₁₋₆-alquilo, C₁₋₆-alquilen-N(C₁₋₆-alquilo)₂, NH-CHO, NH-CO-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO-C₁₋₆-alquilo, NH-CO-O-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO-O-C₁₋₆-alquilo, NH-CO-NH₂, NH-CO-NH-C₁₋₆-alquilo, NH-CO-N(C₁₋₆-alquilo)₂, N-C₁₋₆-alquil-CO-NH₂, N-C₁₋₆-alquil-CO-NH-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO-N(C₁₋₆-alquilo)₂, NH-SO₂-C₁₋₆-alquilo, N-C₁₋₆-alquil-SO₂-C₁₋₆-alquilo, CO₂H, CO₂-C₁₋₆-alquilo, CHO, CO-C₁₋₆-alquilo, O-CO-C₁₋₆-alquilo, CO-NH₂, CO-NH-C₁₋₆-alquilo, CO-N(C₁₋₆-alquilo)₂, O-CO-NH-C₁₋₆-alquilo, O-CO-N(C₁₋₆-alquilo)₂, S-C₁₋₆-alquilo, SO-C₁₋₆-alquilo, SO₂-C₁₋₆-alquilo, SOOH, SO₂OH, SO₂NH₂, SO₂NH-C₁₋₆-alquilo, SO₂N(C₁₋₆-alquilo)₂, C(=N)-NH, NHC(=N)-NH₂, -N=C=O, -S-CN, donde las cadenas alquilo mencionadas precedentemente pueden estar sustituidas con al menos uno de los siguientes sustituyentes: OH, CN, C₃₋₆-cicloalquilo, C₁₋₆-alcoxi, CO₂H, CO₂-C₁₋₆-alquil-CO-C₁₋₆-alquilo, NH-CO-O-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO-O-C₁₋₆-alquilo, NH-CO-NH₂, NH-CO-NH-C₁₋₆-alquilo, NH-CO-N-C₁₋₆-alquilo)₂, N-C₁₋₆-alquil-CO-NH₂, N-C₁₋₆-alquil-CO-NH-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO-N(C₁₋₆-alquilo)₂, NH-SO₂-C₁₋₆-alquilo, N-C₁₋₆-alquil-SO₂-C₁₋₆-alquilo, CO₂H, CO₂-C₁₋₆-alquilo, CHO, CO-C₁₋₆-alquilo, O-CO-C₁₋₆-alquilo, CO-NH₂, CO-NH-C₁₋₆-alquilo, CO-N(C₁₋₆-alquilo)₂, O-CO-NH-C₁₋₆-alquilo, O-CO-N(C₁₋₆-alquilo)₂, S-C₁₋₆-alquilo, SO-C₁₋₆-alquilo, SO₂-C₁₋₆-alquilo, SOOH, SO₂OH, SO₂NH₂, SO₂NH-C₁₋₆-alquilo, SO₂N(C₁₋₆-alquilo)₂, C(=N)-NH, NHC(=N)-NH₂, -N=C=O, -S-CN, donde las cadenas alquilo mencionadas precedentemente pueden estar sustituidas con al menos uno de los siguientes sustituyentes: OH, CN, C₃₋₆-cicloalquilo, C₁₋₆-alcoxi, CO₂H, CO₂-C₁₋₆-alquilo o -NH₂; R⁶ es hidrógeno, C₁₋₆-alquilo, C₁₋₆-haloalquilo, CO-C₁₋₆-alquilo, SO-C₁₋₆-alquilo, SO₂-C₁₋₆-alquilo; L² es una unión o un grupo C₁₋₆-alquileno de cadena ramificada o lineal opcionalmente sustituido conectado al nitrógeno de amida; W es un fenilo o heteroarilo de 5 ó 6 miembros opcionalmente sustituido con al menos un sustituyente Z que contiene al menos un átomo de oxígeno, azufre o nitrógeno; y Z en forma independiente entre sí significan halógeno, OH, CN, SH, C₁₋₆-alquilo, C₂₋₆-alquenilo, C₂₋₆-alquinilo, C₃₋₆-cicloalquilo, C₁₋₆-alcoxi, C₁₋₆-tioalquilo, C₁₋₆-haloalquilo C₁₋₆-tiohaloalquilo, C₁₋₆-haloalcoxi, -NH₂, NH-C₁₋₆-alquilo, N(C₁₋₆-alquilo)₂, N-pirrolidinilo, N-piperidinilo, N-morfolinilo, NH-CHO, NH-CO-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO-C₁₋₆-alquilo, NH-CO₂-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO₂-C₁₋₆-alquilo, NH-CO-NH₂, NH-CO-NH-C₁₋₆-alquilo, NH-CO-N(C₁₋₆-alquilo)₂, N-C₁₋₆-alquil-CO-NH₂, N-C₁₋₆-alquil-CO-NH-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO-N(C₁₋₆-alquilo)₂, NH-SO₂-C₁₋₆-alquilo, N-C₁₋₆-alquil-SO₂-C₁₋₆-alquilo, CO₂H, CO₂-C₁₋₆-alquilo, CHO, CO-C₁₋₆-alquilo, O-CO-C₁₋₆-alquilo, CO-NH₂, CO-NH-C₁₋₆-alquilo, CO-N(C₁₋₆-alquilo)₂, O-CO-NH-C₁₋₆-alquilo, O-CO-N(C₁₋₆-alquilo)₂-, S-C₁₋₆-alquilo, SO-C₁₋₆-alquilo, SO₂-C₁₋₆-alquilo, SO₂H, SO₂OH, SO₂NH₂, SO₂NH-C₁₋₆-alquilo, SO₂N(C₁₋₆-alquilo)₂, C(=N)-NH, NHC(=N)-NH₂, -N=C=O, -S-CN, donde las cadenas alquilo mencionadas precedentemente pueden estar sustituidas con al menos uno de los siguientes sustituyentes: OH, CN, C₃₋₆-cicloalquilo, C₁₋₆-alcoxi, CO₂H, CO₂-C₁₋₆-alquilo o -NH₂.
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