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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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AR
Argentina
Prior art keywords
monosubstituted
unsubstituted
polysubstituted
alkyl
saturated
Prior art date
Application number
ARP110104184A
Other languages
English (en)
Inventor
Frank Robert Dr
Christoph Thomas Dr
Frormann Sven Dr
Original Assignee
Gruenenthal Gmbh
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Filing date
Publication date
Application filed by Gruenenthal Gmbh filed Critical Gruenenthal Gmbh
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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