AR083816A1 - Derivados biciclicos sustituidos de carboxamida y urea, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del dolor, alzheimer y otras afecciones del sistema nervioso central, asi como tambien enfermedades dermatologicas y respiratorias - Google Patents

Derivados biciclicos sustituidos de carboxamida y urea, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del dolor, alzheimer y otras afecciones del sistema nervioso central, asi como tambien enfermedades dermatologicas y respiratorias

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Publication number
AR083816A1
AR083816A1 ARP110104184A ARP110104184A AR083816A1 AR 083816 A1 AR083816 A1 AR 083816A1 AR P110104184 A ARP110104184 A AR P110104184A AR P110104184 A ARP110104184 A AR P110104184A AR 083816 A1 AR083816 A1 AR 083816A1
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Argentina
Prior art keywords
monosubstituted
unsubstituted
polysubstituted
alkyl
saturated
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ARP110104184A
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English (en)
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Frank Robert Dr
Christoph Thomas Dr
Frormann Sven Dr
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Gruenenthal Gmbh
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Publication of AR083816A1 publication Critical patent/AR083816A1/es

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Abstract

Reivindicación 1: Compuestos sustituidos de la fórmula general (1), en la cual X representa CR3 o N, en donde R3 representa H; alquilo C1-10, saturado o insaturado, ramificado o no ramificado, no sustituido o monosustituido o polisustituido; A representa N o CR5b; B1 y B2, cada uno independientemente entre sí representan C o CH; n representa 1, 2, 3 ó 4; p representa 0, 1, 2 ó 3; Y representa O ó S; R0 representa alquilo C1-10, saturado o insaturado, ramificado o no ramificado, no sustituido o monosustituido o polisustituido; cicloalquilo C3-10 o heterociclilo, respectivamente saturado o insaturado, no sustituido o monosustituido o polisustituido; arilo o heteroarilo, respectivamente no sustituido o monosustituido o polisustituido; cicloalquilo C3-10 o heterociclilo, que forma un puente vía alquilo C1-8, respectivamente saturado o insaturado, no sustituido o monosustituido o polisustituido, en donde la cadena alquilo puede estar, respectivamente ramificada o no ramificada, saturada o insaturada, no sustituida o monosustituida o polisustituida; o arilo o heteroarilo formando un puente alquilo C1-8, respectivamente no sustituido o monosustituido o polisustituido, en donde la cadena alquilo puede estar respectivamente ramificada o no ramificada, saturada o insaturada, no sustituida, monosustituida o polisustituida; R1 representa alquilo C1-10, saturado o insaturado, ramificado o no ramificado, no sustituido o monosustituido o polisustituido; cicloalquilo C3-10 o heterociclilo, respectivamente saturado o insaturado, no sustituido o monosustituido o polisustituido; arilo o heteroarilo, respectivamente no sustituido o monosustituido o polisustituido; cicloalquilo C3-10 o heterociclilo, que forma un puente vía alquilo C1-8, respectivamente saturado o insaturado, no sustituido o monosustituido o polisustituido, en donde la cadena alquilo puede estar, respectivamente ramificada o no ramificada, saturada o insaturada, no sustituida, monosustituida o polisustituida; o arilo o heteroarilo forman un puente vía alquilo C1-8, respectivamente no sustituido o monosustituido o polisustituido, en donde la cadena alquilo puede estar respectivamente ramificada o no ramificada, saturada o insaturada, no sustituida, monosustituida 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)2NHR0; 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 monosustituido o polisustituido; R5a representa H; OH; alquilo C1-10, saturado o insaturado, ramificado o no ramificado, no sustituido o monosustituido 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 monosustituido o polisustituido; R6 representa 0 - 4 sustituyentes que se seleccionan independientemente del grupo que consiste de F, Cl, Br, I, OH, CF3, OCF3, alquilo C1-4 y O-alquilo C1-4, en donde el alquilo está saturado, ramificado o no ramificado, no sustituido o monosustituido o polisustituido; R7 y R8 junto con el grupo -B1-B2- que los conecta forma un anillo, anillo el cual está por lo menos monoinsaturado o es aromático, anillo el cual es de 5, 6 ó 7 miembros, anillo el cual opcionalmente está sustituido con 1, 2, 3 ó 4 sustituyentes R9 y anillo el cual puede contener por lo menos un heteroátomo o grupo de heteroátomos, que se seleccionan del grupo que consiste de N, NR10, O y S; R9 representa F; Cl; Br; I; 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; NR0S(=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; S(=O)2N(R0)2; R10 representa H o R0; en el cual “alquilo sustituido”, “heterociclilo sustituido” y “cicloalquilo sustituido” se relaciona, con respecto a los residuos correspondientes, a la sustitución de uno o más átomos de hidrógeno, cada uno independientemente entre sí 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)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)N(R0)2; en el cual “arilo sustituido” y “heteroarilo sustituido” se relaciona, 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; 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)-NR2; 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(=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 forma de los compuestos libres, los tautómeros, los N-óxidos; el racemato; los enantiómeros, diastereoisómeros, mezclas de los enantiómeros o diastereoisómeros o de un enantiómero o diastereoisómero individual; o en forma de las sales de ácidos o bases fisiológicamente compatibles.
ARP110104184A 2010-11-10 2011-11-09 Derivados biciclicos sustituidos de carboxamida y urea, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del dolor, alzheimer y otras afecciones del sistema nervioso central, asi como tambien enfermedades dermatologicas y respiratorias AR083816A1 (es)

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