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AR087301A1 - Derivados de carboxamida y urea que contienen pirazol heteroaromatico sustituido como ligandos del receptor de vanilloide - Google Patents

Derivados de carboxamida y urea que contienen pirazol heteroaromatico sustituido como ligandos del receptor de vanilloide

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Publication number
AR087301A1
AR087301A1 ARP120102684A ARP120102684A AR087301A1 AR 087301 A1 AR087301 A1 AR 087301A1 AR P120102684 A ARP120102684 A AR P120102684A AR P120102684 A ARP120102684 A AR P120102684A AR 087301 A1 AR087301 A1 AR 087301A1
Authority
AR
Argentina
Prior art keywords
nhr0
polysubstituted
mono
unsubstituted
residue
Prior art date
Application number
ARP120102684A
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English (en)
Inventor
Christoph Thomas Dr
Bahrenberg Gregor Dr
Frank Robert Dr
Dr Lee Jeewoo Prof
Lesch Bernhard Dr
Original Assignee
Gruenenthal Gmbh
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46640622&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR087301(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Gruenenthal Gmbh filed Critical Gruenenthal Gmbh
Publication of AR087301A1 publication Critical patent/AR087301A1/es

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Abstract

La presente se relaciona con composiciones farmacéuticas que contienen esos compuestos y también con esos compuestos para usarse en el tratamiento y/o profilaxis del dolor y enfermedades y/o trastornos adicionales.Reivindicación 1: Un compuesto sustituido de fórmula general (1), caracterizado porque R0 representa un residuo alifático de C1-10, no sustituido o mono- o polisustituido; un residuo cicloalifático de C3-10 o un residuo heterocicloalifático de 3 a 10 miembros, en cada caso no sustituido o mono- o polisustituido y en cada caso opcionalmente unido por un puente vía un grupo alifático de C1-8, el cual a su vez puede estar no sustituido o mono- o polisustituido; arilo o heteroarilo, en cada caso no sustituido o mono- o polisustituido y en cada caso opcionalmente unido por un puente vía un grupo alifático de C1-8, el cual a su vez puede estar no sustituido o mono- o polisustituido; R1 representa H; R0; 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; R3 representa H o un residuo alifático de C1-10, no sustituido o mono- o polisustituido; n representa 1, 2, 3 ó 4; R3a representa H o un residuo alifático de C1-4, no sustituido o mono- o polisustituido; R4a representa H o un residuo alifático de C1-4, no sustituido o mono- o polisustituido, un residuo cicloalifático de C3-6, no sustituido o mono- o polisustituido, o un arilo, no sustituido o mono- o polisustituido; Y representa O, S, o N-CN; Z representa N o C-R4b; R4b representa H o un residuo alifático de C1-4, no sustituido o mono- o polisustituido; o R4a y R4b junto con el átomo de carbono que los conecta forman un residuo cicloalifático de C3-6, no sustituido o mono- o polisustituido; T1 representa N o C-R5; U1 representa N o C-R6; V representa N o C-R7; U2 representa N o C-R8; T2 representa N o C-R9; con la condición de que 1, 2 ó 3 de las variables T1, U1, V, U2 y T2 representa un átomo de nitrógeno; R5, R6, R7, R8 y R9 cada uno independientemente del otro representa 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 el cual un “grupo alifático” y un “residuo alifático” pueden en cada caso, independientemente entre si, estar ramificados o no ramificados, saturados o insaturados; en el cual un “residuo cicloalifático” y un “residuo heterocicloalifático” pueden en cada caso, independientemente entre si, estar saturados o insaturados; en el cual “mono- o polisustituido” con respecto a un “grupo alifático”, un “residuo alifático”, un “residuo cicloalifático” y un “residuo heterocicloalifático” se relaciona en cada caso independientemente entre sí, con respecto a los residuos o grupos correspondientes, con la sustitución de uno o más átomos de hidrógeno cada uno independientemente entre sí por al menos un sustituyente seleccionado del grupo que consiste de 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; C(=O)-OH; C(=O)-OR0; CO-NH2; 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)2-OH; O-S(=O)2-OR0; O-S(=O)2-NH2; O-S(=O)2-NHR0; O-S(=O)2-N(R0)2; NH2; NH-R0; N(R0)2; NH-C(=O)-R0; NH-C(=O)-O-R0; NH-C(=O)NH2; NH-C(=O)-NHR0; NH-C(=O)-N(R0)2; NR0-C(=O)-R0; NR0-C(=O)-O-R0; NR0-C(=O)-NH2; NR0-C(=O)-NHR0; NR0-C(=O)-N(R0)2; NH-S(=O)2-OH; NH-S(=O)2-R0; NH-S(=O)2-OR0; NH-S(=O)2NH2; NH-S(=O)2-NHR0; NH-S(=O)2-N(R0)2; NR0-S(=O)2-OH; NR0-S(=O)2-R0; NR0-S(=O)2-OR0; NR0-S(O)2-NH2; NR0-S(=O)2-NHR0; NR0-S(=O)2-N(R0)2; SH; SCF3; SCF2H; SCFH2; SCF2Cl; SCFCl2; SR0; S(=O)-R0; S(=O)2-R0; S(=O)2-OH; S(=O)2-OR0; S(=O)2-NH2; S(O)2-NHR0; y S(=O)2-N(R0)2; en el cual “mono- o polisustituido” con respecto a un “arilo” y un “heteroarilo” se relaciona, con respecto a los residuos correspondientes, en cada caso independientemente entre sí, con la sustitución de uno o más átomos de hidrógeno, cada uno independientemente entre sí por al menos un sustituyente seleccionado del grupo que consiste de F; Cl; Br; I; NO2; CN; CF3; CF2H; CFH2; CF2Cl; CFCl2; R0; C(=O)-H; C(=O)-R0; C(=O)-OH; C(=O)-OR0; CO-NH2; C(=O)-NHR0; C(=O)N(R0)2; OH; un resto del grupo de fórmulas (2); 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)2-OH; O-S(=O)2-OR0; O-S(=O)2-NH2; O-S(=O)2-NHR0; O-S(=O)2-N(R0)2; NH2; NHR0; 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)2-OH; NH-S(=O)2-R0; NH-S(=O)2-OR0; NH-S(O)2-NH2; NH-S(=O)2-NHR0; NH-S(=O)2-N(R0)2; NR0-S(=O)2-OH; NR0-S(=O)2R0; NR0-S(=O)2-OR0; NR0-S(=O)2-NH2; NR0-S(=O)2-NHR0; NR0-S(=O)2N(R0)2; SH; SCF3; SCF2H; SCFH2; SCF2Cl; SCFCl2; SR0; S(=O)-R0; S(=O)2-R0; S(=O)2-OH; S(=O)2-OR0; S(=O)2-NH2; S(=O)2-NHR0; y S(=O)2-N(R0)2; opcionalmente en forma de un solo estereoisómero o una mezcla de estereoisómeros, en forma del compuesto libre y/o una sal o un solvato farmacéuticamente aceptable, en particular un hidrato de los mismos.
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