AR075540A1 - Nicotinamida sustituida como moduladores kcnq2/3 - Google Patents

Nicotinamida sustituida como moduladores kcnq2/3

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AR075540A1
AR075540A1 ARP100100778A ARP100100778A AR075540A1 AR 075540 A1 AR075540 A1 AR 075540A1 AR P100100778 A ARP100100778 A AR P100100778A AR P100100778 A ARP100100778 A AR P100100778A AR 075540 A1 AR075540 A1 AR 075540A1
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alkyl
heteroaryl
aryl
substituted
unsubstituted
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Gruenenthal Chemie
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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Abstract

Se relaciona con nicotinamidas sustituidas, los procesos para su elaboracion, medicamentos que contienen estos compuestos y el uso de estos compuestos para elaborar medicamentos para el dolor, epilepsia, enfermedades cognitivas, adicciones, manía. Reivindicacion 1: Nicotinamida sustituida de la formula general (1) en donde A1 representa CR10R11 o S; A2 representa CR12R13, C(=O), O, S, S(=O) o S(=O)2; R1 representa alquilo C1-10 o heteroalquilo C2-10, ya sea saturado o no saturado, ramificado o no ramificado, no sustituido o sustituido en forma simple o multiple; cicloalquilo C3-10 o heterociclilo, ya sea saturado o no saturado, no sustituido o sustituido en forma simple o multiple; arilo o heteroarilo, ya sea no sustituido o sustituido en forma simple o multiple; cicloalquilo C3-10 o heterociclilo puenteado mediante alquilo C1-8 o heteroalquilo C2-8, ya sea saturado o no saturado, no sustituido o sustituido en forma simple o multiple, en donde la cadena de alquilo o la cadena de heteroalquilo puede ser ramificada o no ramificada, saturada o no saturada, no sustituida o sustituida en forma simple o multiple; o arilo o heteroarilo puenteado mediante alquilo C1-8 o heteroalquilo C2-8, ya sea no sustituido o sustituido en forma simple o multiple, en donde la cadena de alquilo o heteroalquilo puede ser ramificada o no ramificada, saturada o no saturada, no sustituida o sustituida en forma simple o multiple; R2, R3 y R4, en forma independiente, representan H; E; CI; Br, l; NO2; CF3; CN; OH; OCF3; SH; SCF3; metilo; CH2-O-metilo; CH2-OH; alquilo C2-6, alquilo-O C1-6, alquilo-S C1-6, ya sea saturado o no saturado, ramificado o no ramificado, no sustituido o sustituido en forma simple o multiple; cicloalquilo C3-7, saturado o no saturado, ramificado o no ramificado, no sustituido o sustituido en forma simple o multiple; NRaRb, en donde Ra y Rb, en forma independiente, representan H o alquilo C1-4, saturado o no saturado, ramificado o no ramificado, no sustituido o sustituido en forma simple o multiple, o Ra y Rb junto con el átomo de nitrogeno al cual se unen, forman un heterociclilo, saturado o no saturado, ramificado o no ramificado, no sustituido o sustituido en forma simple o multiple; R5, R6, R7, R8, R10, R11, R12 y R13, en forma independiente, representan H; F; CI; Br; l; NO2; CF3 CN; OH; OCF3; SH; SCF3; alquilo C1-10, heteroalquilo C2-10, alquilo-O C1-10 o alquilo-S C1-10, ya sea saturado o no saturado, ramificado o no ramificado, no sustituido o sustituido en forma simple o multiple; cicloalquilo C3-10, saturado o no saturado, ramificado o no ramificado, no sustituido o sustituido en forma simple o multiple; con la reserva que cuando R5, R6, R7 o R8 significan H y A1 representa S, A2 no puede significar S, S(=O) ni S(=O)2; o R5 y R6, o R7 y R8 o R10 y R11, o R12 y R13, o R5 y R11, o R5 y R7, o R5 y R13, o R7 y R13, o R7 y R11, o R11 y R13 junto con el(los) átomos de carbono al(a los) cual(es) se unen, forman un cicloalquilo C3-8 o un heterociclilo con tres a ocho elementos, ya sea saturado o no saturado, no sustituido o sustituido en forma simple o multiple; en donde los correspondientes sustituyentes restantes R5, R6, R7, R8, R10, R11, R12 y R13 poseen el significado ya mencionado; R9 representa cicloalquilo C3-10 o heterociclilo, ya sea saturado o no saturado, no sustituido o sustituido en forma simple o multiple; arilo o heteroarilo, no sustituido o sustituido en forma simple o multiple; o representa CRcRd, en donde Rc y Rd, en forma independiente, significan alquilo C1-4, ya sea saturado o no saturado, ramificado o no ramificado, no sustituido o sustituido en forma simple o multiple; con la reserva que cuando A2 es O o S y R9 es heterociclilo, saturado o no saturado, no sustituido o sustituido en forma simple o multiple; o heteroarilo, no sustituido o sustituido en forma simple o multiple, se produce el enlace del heteroarilo o heterociclilo mediante un átomo de carbono del heteroarilo o heterociclilo; en donde ôalquilo sustituidoö, ôheteroalquilo sustituidoö, ôheterociclilo sustituidoö y ôcicloalquilo sustituidoö se refiere a la sustitucion de uno o varios átomos de hidrogeno en forma independiente, por F; CI; Br; l; NO2; CF3; CN; =O; alquilo C1-8; heteroalquilo C2-8; arilo; heteroarilo; cicloalquilo C3-10; heterociclilo; arilo, heteroarilo, cicloalquilo C3-10 o heterociclilo puenteado mediante alquilo C1-8 o heteroalquilo C2-8; CHO; alquilo C(=O) C1-8; C(=O)arilo; C(=O)-heteroarilo; CO2H; alquilo C(=O)O C1-8; C(=O)O-arilo; C(=O)O-heteroarilo; CONH2; alquilo C(=O)NH C1-8; C(=O)N(alquilo C1-8)2; C(=O)NH-arilo; C(=O)N(arilo)2; C(=O)NH-heteroarilo; C(=O)N(heteroarilo)2; C(=O)N(alquilo C1-8)(arilo); C(=O)N(alquilo C1-8)(heteroarilo); C(=O)N(heteroarilo)(arilo); OH; alquilo-O C1-8; OCF3; O-(alquilo C1-8)-OH; alquilo C1-8-O-(alquilo C1-8)-O-; O-bencilo; O-arilo; O-heteroarilo; alquilo-O-C(=O) C1-8; O-C(=O)arilo; OC(=O)heteroarilo; NH2; alquilo-NH C1-8; N(alquilo C1-8)2; alquilo-NH-C(=O) C1-8; alquilo-N(alquilo C1-8)-C(=O) C1-8; N(C(=O)alquilo C1-8)2; NH-C(=O)-arilo; NH-C(=O)-heteroarilo; SH; alquilo-S C1-8; SCF3; S-bencilo; S-arilo; S-heteroarilo; alquilo-S(=O)2 C1-8; S(=O)2arilo; S(=O)2heteroarilo; S(=O)2OH; alquilo-S(=O)2O C1-8; S(=O)2O-arilo; S(=O)2O-heteroarilo; alquilo-S(=O)2-NH-C1-8; S(=O)2-NH-arilo; y S(=O)2-NH-heteroarilo; en donde ôarilo sustituidoö y ôheteroarilo sustituidoö se refiere a la sustitucion de uno o varios átomos de hidrogeno, en forma independiente, por F; CI; Br; l; NO2; CF3; CN; alquilo C1-8; heteroalquilo C2-8; arilo; heteroarilo; cicloalquilo; heterociclilo; arilo; heteroarilo; cicloalquilo C3-10 o heterociclilo puenteado mediante alquilo C1-8 o heteroalquilo C2-8; CHO; alquilo-C(=O) C1-8; C(=O)arilo; C(=O)heteroarilo; CO2H; alquilo-C(=O)O C1-8; C(=O)O-arilo; C(=O)O-heteroarilo; CONH2; alquilo-C(=O)NH- C1-8; C(=O)N(alquilo C1-8)2; C(=O)NH-arilo; C(=O)N(arilo)2; C(=O)NH-heteroarilo; C(=O)N(heteroarilo)2; C(=O)N(alquilo C1-8)(arilo); C(=O)N(alquilo C1-8)(heteroarilo); C(=O)N(heteroarilo)(arilo); OH; alquilo-O- C1-8; OCF3; O-(alquilo C1-8)-OH; alquilo-O C1-8-(alquilo C1-8)-O-; O-bencilo; O-arilo; O-heteroarilo; alquilo-O-C(=O) C1-8; O-C(=O)arilo; O-C(=O)heteroarilo; NH2; alquilo NH- C1-8; N(alquilo C1-8)2; alquilo NH-C(=O) C1-8; alquilo C1-8N(alquilo C1-8)-C(=O); N(C(=O)alquilo C1-8)2; NH-C(=O)-arilo; NH-C(=O)-heteroarilo; SH; alquilo-S C1-8; SCF3; S-bencilo; S-arilo; S-heteroarilo; alquilo-S(=O)2 C1-8; S(=O)2arilo; S(=O)2heteroarilo; S(=O)2OH; alquilo-S(=O)2O C1-8; S(=O)2O-arilo; S(=O)2O-heteroarilo; alquilo-S(=O)2-NH C1-8; S(=O)2-NH-arilo; S(=O)2-NH-heteroarilo; en la forma de compuestos libres o ácidos o bases fisiologicamente compatibles con sales.
ARP100100778A 2009-03-12 2010-03-12 Nicotinamida sustituida como moduladores kcnq2/3 AR075540A1 (es)

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AU2010223555A1 (en) * 2009-03-10 2011-11-03 Grünenthal GmbH Substituted 3-aminoisoxazolopyridines as KCNQ2/3 modulators
TWI504395B (zh) * 2009-03-10 2015-10-21 Substituted 3-amino-2-mercaptoquinoline as a KCNQ2 / 3 modifier
TWI461197B (zh) * 2009-03-12 2014-11-21 2-mercaptoquinoline-3-carboxamide as a KCNQ2 / 3 modifier
TW201038565A (en) 2009-03-12 2010-11-01 Gruenenthal Gmbh Substituted 2-mercapto-3-aminopyridines as KCNQ2/3 modulators
PE20140214A1 (es) 2010-08-27 2014-02-19 Gruenenthal Chemie 2-oxo- y 2-tioxo-dihidroquinolina-3-carboxamidas sustituidos como moduladores kcnq2/3
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