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AR083817A1 - Derivados de carboxamida y urea heteroaromaticos sustituidos como ligandos del receptor vanilloide - Google Patents

Derivados de carboxamida y urea heteroaromaticos sustituidos como ligandos del receptor vanilloide

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Publication number
AR083817A1
AR083817A1 ARP110104185A ARP110104185A AR083817A1 AR 083817 A1 AR083817 A1 AR 083817A1 AR P110104185 A ARP110104185 A AR P110104185A AR P110104185 A ARP110104185 A AR P110104185A AR 083817 A1 AR083817 A1 AR 083817A1
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AR
Argentina
Prior art keywords
polysubstituted
mono
unsubstituted
saturated
unsaturated
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ARP110104185A
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English (en)
Inventor
Frank Robert Dr
Christoph Thomas Dr
Lesch Bernhard Dr
Dr Lee Jeewoo Prof
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Gruenenthal Gmbh
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Publication date
Application filed by Gruenenthal Gmbh filed Critical Gruenenthal Gmbh
Publication of AR083817A1 publication Critical patent/AR083817A1/es

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Abstract

La presente se relaciona con derivados de carboxamida y urea heteroaromáticos sustituidos, con composiciones farmacéuticas que comprenden esos compuestos y también con el uso de esos compuestos para preparar composiciones farmacéuticas.Reivindicación 1: Los compuestos sustituidos de fórmula general (1), caracterizados porque - - - en cada caso representa la presencia precisamente de un enlace doble entre B1 y B2 o entre B2 y B3; X representa CR3 o N, donde R3 representa H; alquilo C1-10, saturado o insaturado, ramificado o no ramificado, no sustituido o mono- o polisustituido; A representa N o CR5b; n representa 1, 2, 3 ó 4; Y representa O ó S; R0 representa alquilo C1-10, saturado o insaturado, ramificado o no ramificado, no sustituido o mono- o polisustituido; cicloalquilo C3-10 o heterociclilo, respectivamente saturado o insaturado, no sustituido o mono- o polisustituido; arilo o heteroarilo, respectivamente no sustituido o mono- o polisustituido; cicloalquilo C3-10 o heterociclilo unido por un puente vía alquilo C1-8, respectivamente saturado o insaturado, no sustituido o mono- o polisustituido, donde la cadena de alquilo puede estar respectivamente ramificada o no ramificada, saturada o insaturada, no sustituida, mono- o polisustituida; o arilo o heteroarilo unido por un puente vía alquilo C1-8, respectivamente no sustituido o mono- o polisustituido, donde la cadena de alquilo puede estar respectivamente ramificada o no ramificada, saturada o insaturada, no sustituida, mono- o polisustituido; R1 representa alquilo C1-10, saturado o insaturado, ramificado o no ramificado, no sustituido o mono- o polisustituido; cicloalquilo C3-10 o heterociclilo, respectivamente saturado o insaturado, no sustituido o mono- o polisustituido; arilo o heteroarilo, respectivamente no sustituido o mono- o polisustituido; cicloalquilo de o heterociclilo unido por un puente vía alquilo C1-8, respectivamente saturado o insaturado, no sustituido o mono- o polisustituido, donde la cadena de alquilo puede estar respectivamente ramificada o no ramificada, saturada o insaturada, no sustituida, mono- o polisustituida; o arilo o heteroarilo unido por un puente vía alquilo C1-8, respectivamente no sustituido o mono- o polisustituido, donde la cadena de alquilo puede estar respectivamente ramificada o no ramificada, saturada o insaturada, no sustituida, mono- o polisustituida; C(=O)R0; C(=O)-OH; C(=O)-OR0; C(=O)-NHR0; C(=O)-N(R0)2; OH; O-R0; SH; S-R0; S(=O)2-R0; S(=O)2-OR0; S(=O)2-NHR0; S(=O)2-N(R0)2; NH2; NHR0; N(R0)2; NH-S(=O)2-R0; N(R0)(S(=O)2-R0); o SCl3; R2 representa H; R0; F; Cl; Br; I; CN; NO2; OH; SH; CF3; CF2H; CFH2; CF2Cl; CFCl2; CH2CF3; OCF3; OCF2H; OCFH2; OCF2Cl; OCFCl2; SCF3; SCF2H; SCFH2; SCF2Cl; SCFCl2; S(=O)2-CF3; S(=O)2-CF2H; S(=O)2-CFH2; o SF5; R4 representa H; F; Cl; Br; I; OH; alquilo C1-10, saturado o insaturado, ramificado o no ramificado, no sustituido o mono- o polisustituido; R5a representa H; OH; alquilo C1-10, saturado o insaturado, ramificado o no ramificado, no sustituido o mono- o polisustituido; R5b representa H o R0; o R5a y R5b forman junto con el átomo de carbono que los conecta un cicloalquilo C3-10 o un heterociclilo, respectivamente saturado o insaturado, no sustituido o mono- o polisustituido; B1 representa C, CH, N, NR6, O ó S; B2 representa C, CH, N, NR7, O ó S; B3 representa C, CH, N, NR8, O ó S; donde 1 ó 2 de las variables B1, B2 y B3 representan uno de los grupos de heteroátomos o heteroátomo mencionados anteriormente; D1 representa N o CR9; D2 representa N o CR10; D3 representa N o CR11; D4 representa N o CR12; donde 0, 1 ó 2 de las variables D1, D2, D3 y D4 representan N; R6, R7 y R8 cada uno independientemente entre si representan H o alquilo C1-4, saturado, ramificado o no ramificado, no sustituido o mono- o polisustituido; R9, R10, R11 y R12 cada uno independientemente entre si representan H; F; Cl; Br; I; NO2 CN; CF3; CF2H; CFH2; CF2Cl; CFCl2; R0; C(=O)H; C(=O)R0; CO2H; C(=O)OR0; CONH2; C(=O)NHR0; C(=O)N(R0)2; OH; OCF3; OCF2H; OCFH2; OCF2Cl; OCFCl2; OR0; O-C(=O)-R0; O-C(=O)-O-R0; O-(C=O)-NH-R0; O-C(=O)-N(R0)2; O-S(=O)2-R0; O-S(=O)2OH; O-S(=O)2OR0; O-S(=O)2NH2; O-S(=O)2NHR0; O-S(=O)2N(R0)2; NH2; NH-R0; N(R0)2; NH-C(=O)-R0; NH-C(=O)-O-R0; NH-C(=O)-NH2; NH-C(=O)-NH-R0; NH-C(=O)-N(R0)2; NR0-C(=O)-R0; NR0-C(=O)-O-R0; NR0-C(=O)-NH2; NR0-C(=O)-NH-R0; NR0-C(=O)-N(R0)2; NH-S(=O)2OH; NH-S(=O)2R0; NH-S(=O)2OR0; NH-S(=O)2NH2; NH-S(=O)2NHR0; NH-S(=O)2N(R0)2; NR0-S(=O)2OH; NR0-S(=O)2R0; NR0-S(=O)2OR0; NR0-S(=O)2NH2; NR0-S(=O)2NHR0; NR0-S(=O)2N(R0)2; SH; SCF3; SCF2H; SCFH2; SCF2Cl; SCFCl2; SR0; S(=O)R0; S(=O)2R0; S(=O)2OH; S(=O)2OR0; S(=O)2NH2; S(=O)2NHR0; o S(=O)2N(R0)2; en la cual “alquilo sustituido”, “heterociclilo sustituido”, y “cicloalquilo sustituido”, se relacionan, con respecto a los residuos correspondientes, con la sustitución de uno o más átomos de hidrógeno cada uno independientemente entre si por F; Cl; Br; I; NO2 CN; =O; =NH; =N(OH); =C(NH2)2; CF3; CF2H; CFH2; CF2Cl; CFCl2; R0; C(=O)H; C(=O)R0; CO2H; C(=O)OR0; CONH2; C(=O)NHR0; C(=O)N(R0); OH; OCF3; OCF2H; OCFH2; OCF2Cl; OCFCl2; OR0; O-C(=O)-R0; O-C(=O)-O-R0; O-(C=O)-NH-R0; O-C(=O)-N(R0)2; O-S(=O)2-R0; O-S(=O)2OH; O-S(=O)2OR0; O-S(=O)2NH2; O-S(=O)2NHR0; O-S(=O)2N(R0)2; NH2; NH-R0; N(R0)2; NH-C(=O)-R0; NH-C(=O)-O-R0; NH-C(=O)-NH2; NH-C(=O)-NH-R0; NH-C(=O)-N(R0)2; NR0-C(=O)-R0; NR0-C(=O)-O-R0; NR0-C(=O)-NH2; NR0-C(=O)-NH-R0; NR0-C(=O)-N(R0)2; NH-S(=O)2OH; NH-S(=O)2R0; NH-S(=O)2OR0; NH-S(=O)2NH2; NH-S(=O)2NHR0; NH-S(=O)2N(R0)2; NR0-S(=O)2OH; NR0-S(=O)2R0; NR0-S(=0)2OR0; NR0-S(=0)2NH2; NR0-S(=O)2NHR0; NR0-S (=O)2N(R0)2; SH; SCF3 SCF2H; SCFH2; SCF2Cl; SCFCl2; SR0; S(=O)R0; S(=O)2R0; S(=O)2OH; S(=O)2OR0; S(=O)2NH2; S(=O)2NHR0; o S(=O)2N(R0)2; en la cual “arilo sustituido” y “heteroarilo sustituido”, se relacionan, con respecto a los residuos correspondientes de la sustitución de uno o más átomos de hidrógeno, cada uno independientemente entre sí por F; Cl; Br; I; NO2; CN; CF3; CF2H; CFH2; CF2Cl; CFCl2; R0; C(=O)H; C(=O)R0; CO2H; C(=O)OR0; CONH2; C(=O)NHR0; C(=O)N(R0)2; OH; OCF3; OCF2H; OCFH2; OCF2Cl; OCFCl2; OR0; O-C(=O)-R0; O-C(=O)O-R0; O-(C=O)-NH-R0; O-C(=O)-N(R0)2; O-S(=O)2-R0; O-S(=O)2OH; O-S(=O)2OR0; O-S(=O)2NH2; O-S(=O)2NHR0; O-S(=O)2N(R0)2; NH2; NH-R0; N(R0)2; NH-C(=O)-R0; NH-C(=O)-O-R0; NH-C(=O)-NH2; NH-C(=O)-NH-R0; NH-C(=O)-N(R0)2; NR0-C(=O)-R0; NR0-C(=O)-O-R0; NR0-C(=O)-NH2; NR0-C(=O)-NH-R0; NR0-C(=O)-N(R0)2; NH-S(=O)2OH; NH-S(=O)2R0; NH-S(=O)2OR0; NH-S(=O)2NH2; NH-S(=O)2NHR0; NH-S(=O)2N(R0)2; NR0-S(=O)2OH; NR0-S(=O)2R0; NR0-S(=O)2OR0; NR0-S(=O)2NH2; NR0-S(=O)2NHR0; NR0-S(=O)2N(R0)2; SH; SCF3; SCF2H; SCFH2; SCF2Cl; SCFCl2; SR0; S(=O)R0; S(=O)2R0; S(=O)2OH; S(=O)2OR0; S(=O)2NH2; S(=O)2NHR0; o S(=O)2N(R0)2; en forma de los compuestos libres, los tautómeros, los N-óxidos; el racemato; los enantiómeros, diastereómeros; mezclas de los enantiómeros o diastereómeros; o de un enantiómeros o diastereómeros; o en forma de las sales de ácidos o bases fisiológicamente compatibles.
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