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AR094412A1 - Carboxamidas basadas en pirazolilo i - Google Patents

Carboxamidas basadas en pirazolilo i

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Publication number
AR094412A1
AR094412A1 ARP140100092A ARP140100092A AR094412A1 AR 094412 A1 AR094412 A1 AR 094412A1 AR P140100092 A ARP140100092 A AR P140100092A AR P140100092 A ARP140100092 A AR P140100092A AR 094412 A1 AR094412 A1 AR 094412A1
Authority
AR
Argentina
Prior art keywords
residue
polysubstituted
monosubstituted
unsubstituted
independently
Prior art date
Application number
ARP140100092A
Other languages
English (en)
Inventor
Dr Nordhoff Sonja
Dr Wachten Sebastian
Dr Kless Achim
Dr Voss Felix
Dr Ritter Stefanie
Original Assignee
Gruenenthal Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Gruenenthal Gmbh filed Critical Gruenenthal Gmbh
Publication of AR094412A1 publication Critical patent/AR094412A1/es

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Abstract

Inhibidores de ICRAC, composiciones farmacéuticas que contienen a estos compuestos y su uso en el tratamiento y/o la profilaxis de enfermedades y/o trastornos, en particular enfermedades inflamatorias y/o trastornos inflamatorios. Reivindicación 1: Un compuesto caracterizado porque es de fórmula general (1), donde R¹ denota H; residuo alifático C₁₋₄, no sustituido o monosustituido o polisustituido; o residuo cicloalifático C₃₋₆ o un residuo heterocicloalifático de entre 3 y 7 miembros, en cada caso no sustituido o monosustituido o polisustituido y en cada caso opcionalmente conectado a través de un grupo alifático C₁₋₄, que a su vez puede no estar sustituido o estar monosustituido o polisustituido; con la condición de que si R¹ representa un residuo heterocicloalifático de entre 3 y 7 miembros, dicho residuo heterocicloalifático de entre 3 y 7 miembros se conecta a la parte restante de la estructura de acuerdo con la fórmula general (1) a través de un átomo de carbono del residuo heterocicloalifático de entre 3 y 7 miembros; R² denota H; F; Cl; Br; I; NO₂; CN; CF₃; CF₂H; CFH₂; R¹³; OH; O-R¹³; NH₂; N(H)R¹³; N(R¹³)₂; T representa C-R³ o N o N⁺-O⁻, U representa C-R⁴ o N o N⁺-O⁻, y representa C-R⁵ o N o N⁺-O⁻, W representa C-R⁶ o N o N⁺-O⁻, y X representa C-R⁷ o N o N⁺-O⁻, con la condición de que 0, 1, 2 ó 3 de las variables T, U, V, W y X en forma independiente entre sí representan N o N⁺-O⁻, donde 0 ó 1 de las variables T, U, V, W y X en forma independiente entre sí representan N⁺-O⁻ y con la condición de que al menos uno de U, V y W no representa N, donde al menos uno de R⁴, R⁵ y R⁶ se selecciona entre el grupo que consiste en residuo cicloalifático C₃₋₆, no sustituido o monosustituido o polisustituido; residuo heterocicloalifático de entre 3 y 7 miembros, no sustituido o monosustituido o polisustituido; arilo, no sustituido o monosustituido o polisustituido; y heteroarilo, no sustituido o monosustituido o polisustituido, y los sustituyentes restantes de R³, R⁴, R⁵, R⁶ y R⁷ se seleccionan en forma independiente entre sí entre el grupo que consiste en H; F; Cl, Br; I; NO₂; CN; CF₃; CF₂H; CFH₂; CF₂Cl; CFCl₂; R¹³; R¹⁴; C(=O)OH; C(=O)-R¹³; C(=O)R¹⁴; C(=O)-OR¹³; C(=O)-OR¹⁴; C(=O)-N(H)(OH); C(=NOH)-H; C(=N-OH)-R¹³; C(=N-OH)-R¹⁴; C(=N-O-R¹³)-H; C(=N-OR¹³)-R¹³; C(=N-O-R¹³)-R¹⁴; C(O)NH₂; C(=O)-N(H)R¹³; C(=O)-N(R¹³)₂; C(=O)-N(H)R¹⁴; C(=O)-N(R¹⁴)₂; C(=O)-N(R¹³)(R¹⁴); C(=O)-N(Rᵃ) (Rᵇ); OH; OR¹³; OCF₃; OCF₂H; OCFH₂; OCF₂Cl; OCFCl₂; OR¹⁴; O-C(=O)-R¹³; O-C(=O)-R¹⁴; O-C(=O)-N(H)R¹³; O-C(=O)-N(H)R¹⁴; OC(O)-N(R¹³)₂; O-C(=O)-N(R¹⁴)₂; O-C(=O)-N(R¹³)(R¹⁴); O-C(=O)-N(Rᵃ)(Rᵇ); NH₂; N(H)R¹³; N(R¹³)₂; N(H)R¹⁴; N(R¹⁴)₂; N(R¹³)(R¹⁴); N(Rᵃ)(Rᵇ); NH-C(=O)R¹⁴; NH-C(=O)-R¹³; N(R¹³)C(=O)-R¹³; N(R¹³)C(=O)-R¹⁴; NH-S(=O)₂-R¹³; N(R¹³)S(=O)₂-R¹³; NHS(=O)₂-R¹⁴; N(R¹³)-S(=O)₂-R¹⁴; N(H)C(=O)-OR¹³; N(H)-C(=O)-OR¹⁴; N(R¹³)-C(=O)-OR¹³; N(R¹³)C(=O)OR¹⁴; N(H)C(=O)-NH₂; N(H)C(=O)-N(H)R¹³; N(H)-C(=O)-N(H)R¹⁴; N(H)C(=O)-N(R¹³)₂; N(H)-C(=O)-N(R¹⁴)₂; N(H)-C(=O)-N(R¹³)(R¹⁴); N(H)-C(=O)N(Rᵃ)(Rᵇ); N(R¹³)-C(=O)-NH₂; N(R¹³)-C(=O)-N(H)R¹³; N(R¹³)-C(=O)-N(H)R¹⁴; N(R¹³)-C(=O)-N(R¹³)₂; N(R¹³)-C(=O)-N(R¹⁴)₂; N(R¹³)-C(=O)-N(R¹³)(R¹⁴); N(R¹³)-C(=O)-N(Rᵃ)(Rᵇ); SH; S-R¹³; SCF₃; S-R¹⁴; S(=O)₂OH; S(=O)₂-R¹³; S(=O)₂-R¹⁴; S(=O)-R¹³; S(=O)-R¹⁴; S(=O)₂-OR¹³; S(=O)₂-OR¹⁴; S(=O)₂-N(H)(R¹³); S(=O)₂-N(R¹³)₂; S(=O)₂-N(H)(R¹⁴); S(=O)₂-N(R¹³)(R¹⁴); S(=O)₂-N(Rᵃ)(Rᵇ); n representa 0 ó 1, donde, si n representa 1, luego J representa C-R⁸ o N o N⁺-O⁻, K representa C-R⁹ o N o N⁺-O⁻, M representa C-R¹⁰ o N o N⁺-O⁻, Q representa C-R¹¹ o N o N⁺-O⁻, y R representa C-R¹² o N o N⁺-O⁻, con la condición de que 0, 1, 2 ó 3 de las variables J, K, M, Q y R en forma independiente entre sí representan N o N⁺-O⁻, donde 0 ó 1 de las variables J, K, M, Q y R en forma independiente representa N⁺-O⁻, donde, si n representa 0, entonces J representa C-R⁸ o N o N⁺-O⁻ ó O ó S o NH o N(residuo alifático C₁₋₄), K representa C-R⁹ o N o N⁺-O⁻ ó O ó S o NH o N(residuo alifático C₁₋₄), M representa C-R¹⁰ o N o N⁺-O⁻ ó O ó S o NH o N(residuo alifático C₁₋₄) y Q representa C-R¹¹ o N o N⁺-O⁻ ó O ó S o NH o N(residuo alifático C₁₋₄), con la condición de que uno de J, K, M y Q representa O ó S o NH o N(residuo alifático C₁₋₄) y los restantes de J, K, M y Q en forma independiente representan C-R⁸, respectivamente C-R⁹, respectivamente C- R¹⁰, respectivamente C-R o N o N⁺-O⁻ y con la condición de que 0, 1, 2 ó 3 de J, K, M y Q en forma independiente entre sí representan N o N⁺-O⁻, donde 0 ó 1 de las variables J, K, M y Q representa N⁺-O⁻, donde R⁸, R⁹, R¹⁰, R¹¹ y R¹² se seleccionan en forma independiente entre sí entre el grupo que consiste en H; F; Cl; Br; I; NO₂; CN; CF₃ CF₂H; CFH₂ CF₂Cl; CFCl₂; R¹³; R¹⁴; C(=O)OH; C(=O)-R¹³; C(=O)R¹⁴; C(=O)-OR¹³; C(=O)-OR¹⁴; C(=O)-N(H)(OH); C(=N-OH)-H; C(=N-OH)-R¹³; C(=NOH)-R¹⁴; C(=N-O-R¹³)-H; C(=N-O-R¹³)-R¹³; C(=N-O-R¹³)-R¹⁴; C(=O)NH₂; C(=O)-N(H)R¹³; C(=O)-N(R¹³)₂; C(=O)-N(H)R¹⁴; C(=O)-N(R¹⁴)₂; C(=O)-N(R¹³)(R¹⁴); C(=O)-N(Rᵃ)(Rᵇ); OH; OR¹³; OCF₃; OCF₂H; OCFH₂ OCF₂Cl; OCFCl₂; OR¹⁴; OC(=O)R¹³; O-C(=O)R¹⁴; O-C(=O)-N(H)R¹³; O-C(=O)-N(H)R¹⁴; OC(=O)-N(R¹³)₂; OC(=O)-N(R¹⁴)₂; O-C(=O)-N(R¹³)(R¹⁴); O-C(=O)-N(Rᵃ)(Rᵇ); NH₂; N(H)R¹³; N(R¹³)₂; N(H)R¹⁴; N(R¹⁴)₂; N(R¹³)(R¹⁴); N(Rᵃ)(Rᵇ); NH-C(=O)-R¹⁴; NH-C(=O)-R¹³; N(R¹³)-C(=O)-R¹³; N(R¹³)-C(=O)-R¹⁴; NH-S(=O)₂-R¹³; N(R¹³)-S(=O)₂-R¹³; NH-S(=O)₂-R¹⁴; N(R¹³)-S(=O)₂-R¹⁴; N(H)-C(=O)OR¹³; N(H)-C(=O)-OR¹⁴; N(R¹³)-C(=O)-OR¹³; N(R¹³)-C(=O)-OR¹⁴; N(H)-C(=O)-NH₂; N(H)C(=O)-N(H)R¹³; N(H)-C(=O)N(H)R¹⁴; N(H)-C(=O)-N(R¹³)₂; N(H)-C(=O)-N(R¹⁴)₂; N(H)-C(=O)-N(R¹³)(R¹⁴); N(H)-C(=O)-N(Rᵃ)(Rᵇ); N(R¹³)-C(=O)-NH₂; N(R¹³)-C(=O)-N(H)R¹³, N(R¹³)-C(=O)-N(H)R¹⁴; N(R¹³)-C(=O)-N(R¹³)₂; N(R¹³)-C(=O)-N(R¹⁴)₂; N(R¹³)-C(=O)-N(R¹³)(R¹⁴); N(R¹³)-C(=O)-N(Rᵃ)(Rᵇ); SH; S-R¹³; SCF₃; SR¹⁴; S(=O)OH; S(=O)₂-R¹³; S(=O)₂-R¹⁴; S(=O)-R¹³; S(=O)R¹⁴; S(=O)₂-OR¹³; S(=O)₂-OR¹⁴; S(=O)₂-N(H)(R¹³); S(=O)₂-N(R¹³)₂; S(=O)₂-N(H)(R¹⁴); S(=O)₂-N(R¹³)(R¹⁴); S(=O)₂-N(Rᵃ)(Rᵇ); con la condición de que al menos uno de R⁸, R⁹, R¹⁰, R¹¹ y R¹² no denota H; cada R¹³ en forma independiente en cada caso denota residuo alifático C₁₋₈, no sustituido o monosustituido o polisustituido; o residuo cicloalifático C₃₋₆ o residuo heterocicloalifático de entre 3 y 7 miembros, en cada caso no sustituido o monosustituido o polisustituido; o residuo cicloalifático C₃₋₆ o residuo heterocicloalifático de entre 3 y 7 miembros, en cada caso no sustituido o monosustituido o polisustituido, y en cada caso conectado a través de un residuo alifático C₁₋₄, no sustituido o monosustituido o polisustituido; cada R¹⁴ en forma independiente en cada caso denota residuo arilo y heteroarilo, en cada caso en forma independiente entre sí no sustituido o monosustituido o polisustituido, o residuo arilo y heteroarilo, en cada caso en forma independiente entre sí no sustituido o monosustituido o polisustituido y en cada caso conectado a través de un grupo alifático C₁₋₄, no sustituido o monosustituido o polisustituido; Rᵃ y Rᵇ junto con el átomo de N que los conecta forman un residuo heterocíclico de entre 3 y 7 miembros, no sustituido o monosustituido o polisustituido; opcionalmente en forma de un único estereoisómero o una mezcla de estereoisómeros, en forma del compuesto libre y/o una sal fisiológicamente aceptable del mismo y/o un solvato fisiológicamente aceptable del mismo.
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