AR094975A1 - Dihidropirimidinonas bicíclicas sustituidas y su uso como inhibidores de la actividad de elastasa neutrofílica - Google Patents
Dihidropirimidinonas bicíclicas sustituidas y su uso como inhibidores de la actividad de elastasa neutrofílicaInfo
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- AR094975A1 AR094975A1 ARP140100690A ARP140100690A AR094975A1 AR 094975 A1 AR094975 A1 AR 094975A1 AR P140100690 A ARP140100690 A AR P140100690A AR P140100690 A ARP140100690 A AR P140100690A AR 094975 A1 AR094975 A1 AR 094975A1
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Abstract
Dihidropirimidinonas bicíclicas sustituidas, su uso como inhibidores de la actividad de elastasa neutrofílica, a composiciones farmacéuticas que la contienen y sus métodos de uso como agentes para el tratamiento y/o prevención de enfermedades pulmonares, gastrointestinales y genitourinarias, enfermedades inflamatorias de la piel y el ojo y otros trastornos autoinmunes y alérgicos, rechazo a aloinjerto y enfermedades oncológicas. Reivindicación 1: Un compuesto de caracterizado por la fórmula (1), en donde R¹ es fenilo o un heteroarilo de cinco o seis miembros, en donde uno, dos o tres elementos están reemplazados por un elemento seleccionado, de modo independiente, del grupo que consiste en N, O ó S; cada anillo opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados, de modo independiente, del grupo que consiste en halógeno, O₂N-, NC-, H₂N-, HO-, R¹,¹, R¹,¹O-, R¹,², R¹,³S-, R¹,³(O)S- y R¹,³(O)₂S-; R¹,¹ está seleccionado, de modo independiente, del grupo que consiste en alquilo C₁₋₆, cicloalquilo C₃₋₆, haloalquilo C₁₋₆ y halocicloalquilo C₃₋₆; R¹,² es HO-alquilo C₁₋₆ o R¹,¹-O-alquilo C₁₋₆; R¹,³ está seleccionado, de modo independiente, del grupo que consiste en H, HO-, R¹,¹ y R¹,²; R² es fenilo o un heteroarilo de cinco o seis miembros, en donde uno o dos elementos están reemplazados por un elemento seleccionado, de modo independiente, del grupo que consiste en N, O ó S; cada anillo opcionalmente sustituido con uno o dos sustituyentes seleccionados, de modo independiente, del grupo que consiste en halógeno, alquilo C₁₋₄, haloalquilo C₁₋₄ y alquil C₁₋₄-O-; R³ es un residuo seleccionado, de modo independiente, del grupo que consiste en: R³,¹-; R³,²(O)C-; R³,²O(O)C-; R³,²O(O)C-A-; R³,²S-; R³,²(O)S-; R³,²(O)₂S-; (R³,²)₂N(O)C-; y (R³,²)₂N(O)C-A-; R³,¹ está seleccionado, de modo independiente, del grupo que consiste en H, R³,³, R³,⁴, alquil C₁₋₆-cicloalquilo C₃₋₆ y cicloalquil C₃₋₆-alquilo C₁₋₆, cada uno opcionalmente sustituido con uno o dos sustituyentes seleccionados, de modo independiente, de entre R³,¹,¹-; R³,¹,¹ está seleccionado del grupo que consiste en HO-, halógeno, NC-, R³,³O-, R³,⁵, R³,⁶ y R³,⁷; R³,¹,¹ denota un anillo seleccionado, de modo independiente, de fenilo y un anillo heterocíclico de cuatro miembros que contiene un elemento seleccionado, de modo independiente, de entre N, O, S, S(O) y S(O)₂; R³,¹,¹ denota un anillo heterocíclico o heteroarilo de cinco o seis miembros que contiene uno, dos o tres elementos seleccionados, de modo independiente, de entre N, O, S, S(O) y S(O)₂; cada uno de los anillos opcionalmente sustituido con uno o dos sustituyentes seleccionados, de modo independiente, de entre HO-, O=, halógeno, NC-, R³,³, R³,³O-, R³,³-(O)C-, R³,⁴, R³,⁵, R³,⁶ y R³,⁷ o dos sustituyentes son juntos R³,⁸; R³,² está seleccionado, de modo independiente, de entre R³,¹, fenilo, anillo heterocíclico de cuatro miembros que contiene un elemento seleccionado, de modo independiente, del grupo que consiste en N, O, S, S(O) y S(O)₂; o un anillo heterocíclico o heteroarilo de cinco o seis miembros que contiene uno, dos o tres elementos seleccionados, de modo independiente, del grupo que consiste en N, O, S, S(O) y S(O)₂; cada anillo opcionalmente sustituido con uno o dos sustituyentes seleccionados, de modo independiente, del grupo que consiste en HO-, O=, NC-, halógeno, R³,³, R³,³O-, R³,³-(O)C-, R³,⁴, R³,⁵, R³,⁶, R³,⁷ o dos sustituyentes son juntos R³,⁸; o dos R³,² son juntos un anillo heterocíclico o heteroarilo monocíclico de tres, cuatro, cinco o seis miembros o bicíclico de seis, siete, ocho, nueve o diez miembros que opcionalmente contiene adicional al nitrógeno uno o dos elementos seleccionados, de modo independiente, del grupo que consiste en N, O, S, S(O) y S(O)₂; opcionalmente sustituido con uno o dos sustituyentes, seleccionados, de modo independiente, del grupo que consiste en HO-, F, O=, NC-, R³,³, R³,³O-, R³,³-(O)C-, R³,⁴, R³,⁵, R³,⁶, R³,⁷, fenilo, un anillo heterocíclico o heteroarilo de cinco o seis miembros que contiene uno, dos o tres elementos seleccionados, de modo independiente, del grupo que consiste en N, O, S, S(O) y S(O)₂; o dos sustituyentes son juntos R³,⁸; R³,³ está seleccionado, de modo independiente, del grupo que consiste en alquilo C₁₋₆, cicloalquilo C₃₋₆, haloalquilo C₁₋₆, halocicloalquilo C₃₋₆; R³,⁴ es HO-alquilo C₁₋₆ o R³,³-O-alquilo C₁₋₆; R³,⁵ está seleccionado, de modo independiente, del grupo que consiste en H₂N-, R³,³-HN-, (R³,³)₂N-, R³,³-(O)C-HN-, R³,³-(O)C-(R³,³)N-; R³,⁶ está seleccionado, de modo independiente, del grupo que consiste en R³,³-(O)S-, R³,³-(O)₂S-, R³,³(HN)S-, R³,³(HN)(O)S-, R³,³(R³,³N)S-, R³,³(R³,³N)(O)S-, R³,³(R³,⁴N)S-, R³,³(R³,⁴N)(O)S-; R³,³(NC-N)S-, R³,³(NC-N)(O)S-; R³,⁷ está seleccionado, de modo independiente, del grupo que consiste en HO(O)C-, H₂N(O)C-, R³,³-O-(O)C-, R³,³-NH-(O)C-, (R³,³)₂N-(O)C-; R³,⁸ está seleccionado, de modo independiente, del grupo que consiste en alquileno C₁₋₆ o haloalquileno C₁₋₆, en donde opcionalmente uno o dos grupos CH₂ están reemplazados, de modo independiente entre sí, por -HN-, -(R³,³)N-, -(R³,⁴)N-, -(R³,³(O)C-)N-, -(R³,⁴(O)C-)N-, -O-, -S-, -S(O)- o -S(O)₂-; A es -CH₂-, -CH₂-CH₂- o -CH₂-CH₂-CH₂-; opcionalmente sustituido con uno o dos sustituyentes seleccionados, de modo independiente, del grupo que consiste en halógeno, R³,³, R³,³O- y R³,⁴ o dos sustituyentes son juntos R³,⁸; R⁴ está seleccionado, de modo independiente, del grupo que consiste en halógeno, alquilo C₁₋₆, cicloalquilo C₃₋₆, haloalquilo C₁₋₆, halocicloalquilo C₃₋₆, HO-alquilo C₁₋₆, alquil C₁₋₆-O-alquilo C₁₋₆; dos R⁴ son juntos alquileno C₁₋₆ o haloalquileno C₁₋₆, en donde opcionalmente un grupo CH₂ se puede reemplazar por -O-, -S-, -S(O)- o -S(O)₂-; x es 0, 1 ó 2; R⁵ está seleccionado, de modo independiente, del grupo que consiste en halógeno, NC-, R⁵,¹; HO(O)C-, H₂N(O)C-, R⁵,¹-O-(O)C-, R⁵,¹-NH-(O)C-, (R⁵,¹)₂N-(O)C-; fenilo o un anillo heterocíclico o heteroarilo de cinco o seis miembros que contiene uno, dos o tres elementos seleccionados, de modo independiente, del grupo que consiste en N, O, S, S(O) y S(O)₂; cada anillo opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados, de modo independiente, del grupo que consiste en halógeno, HO-, O=, NC-, O₂N-, H₂N-, R⁵,¹, R⁵,¹O-, R⁵,¹-HN-, (R⁵,¹)₂N-, R⁵,¹-(O)C-HN-, R⁵,¹(O)C-(R⁵,¹)N-, R⁵,¹-(O)S-, R⁵,¹-(O)₂S-, R⁵,¹-(HN)S-, R⁵,¹-(HN)(O)S-, R⁵,¹-(R⁵,¹N)S-, R⁵,¹-(R⁵,¹N)(O)S-, R⁵,¹-(NC-N)S-, R⁵,¹-(NC-N)(O)S-, HO(O)C-, H₂N(O)C-, R⁵,¹-O-(O)C-, R⁵,¹-NH-(O)C-, (R⁵,¹)₂N-(O)C-; R⁵,¹ está seleccionado, de modo independiente, del grupo que consiste en alquilo C₁₋₆, cicloalquilo C₃₋₆, alquil C₁₋₆cicloalquilo C₃₋₆, cicloalquil C₃₋₆-alquilo C₁₋₆, haloalquilo C₁₋₆, halocicloalquilo C₃₋₆, HO-alquilo C₁₋₆, alquil C₁₋₆-O-alquilo C₁₋₆, cicloalquil C₃₋₆-O-alquilo C₁₋₆, haloalquil C₁₋₆-O-alquilo C₁₋₆, halocicloalquil C₃₋₆-O-alquilo C₁₋₆, o dos R⁵,¹ son juntos alquileno C₁₋₆ o haloalquileno C₁₋₆, en donde opcionalmente uno o dos grupos CH₂ están reemplazados por -HN-, -(alquilo C₁₋₆)N-, -(cicloalquilo C₃₋₆)N-, -(haloalquilo C₁₋₆)N-, -(halocicloalquilo C₃₋₆)N-, -(HO-alquilo C₁₋₆)N-, -(alquil C₁₋₆-O-alquilo C₁₋₆)N-, -(cicloalquil C₃₋₆-O-alquilo C₁₋₆)N-, -(alquilo C₁₋₆-(O)C-)N-, -(cicloalquilo C₃₋₆-(O)C-)N-, -(haloalquilo C₁₋₆-(O)C-)N-, -(HO-alquilo C₁₋₆-(O)C-)N-, -(alquil C₁₋₆-O-alquilo C₁₋₆-(O)C-)N-, -(cicloalquil C₃₋₆-O-alquilo C₁₋₆-(O)C-)N-, -O-, -S-, -S(O)- o -S(O)₂-; y es 0, 1 ó 2; o una de sus sales.
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