AR085893A1 - Pirrolopirazina-amidas de piperidina espirociclica como moduladores de los canales ionicos - Google Patents

Pirrolopirazina-amidas de piperidina espirociclica como moduladores de los canales ionicos

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Publication number
AR085893A1
AR085893A1 ARP120100346A ARP120100346A AR085893A1 AR 085893 A1 AR085893 A1 AR 085893A1 AR P120100346 A ARP120100346 A AR P120100346A AR P120100346 A ARP120100346 A AR P120100346A AR 085893 A1 AR085893 A1 AR 085893A1
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Argentina
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cycloalkyl
alkyl
replaced
units
halo
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ARP120100346A
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Corey Anderson
Peter Diederik Jan Grootenhuis
Ruah Sara S Hadida
Edward Adam Kallel
Mark Thomas Miller
Vijayalaksmi Arumugam
Jason Mcartney
Licong Jiang
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Vertex Pharma
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Publication of AR085893A1 publication Critical patent/AR085893A1/es

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    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract

La presente se refiere a compuestos de pirrolopirazina-amida de piperidina espirocíclica útiles como inhibidores de los canales iónicos. La presente también provee composiciones farmacéuticamente aceptables que comprenden los compuestos de la presente y métodos para utilizar las composiciones para el tratamiento de varios trastornos.Reivindicación 1: Un compuesto caracterizado porque tiene la fórmula (1) o una sal farmacéuticamente aceptable del mismo, donde, independientemente de cada aparición: R1 es H, alquilo C1-8, cicloalquilo C3-8, halo, CN, NR8SO2R8, SO2R8, SR8, SOR8, NR8COR8, NR8CO2R8, CON(R8)2, SO2N(R8)2, CF3, heterocicloalquilo, o un C1-8-R9 de cadena recta, ramificada o cíclico donde hasta dos unidades CH2 pueden ser reemplazadas por O, CO, S, SO, SO2 o NR8, o dos R1 tomados juntos forman un grupo oxo, o un anillo cicloalquilo fusionado de 3 a 7 miembros, o un anillo espirocíclico de 3 a 7 miembros; R2 es H, alquilo C1-8, halo, haloalquilo C1-8, CN, OH, SO2R8, SR8, SOR8, COR8, CO2R8, CON(R8)2, SO2N(R8)2, CF3, CHF2, o un C1-8-R9 de cadena recta, ramificado o cíclico donde hasta dos unidades CH2 pueden ser reemplazadas por O, CO, S, SO, SO2, CF2, o NR8; R3 es H, alquilo C1-8, cicloalquilo C3-8, CO2R8, COR8, COH, CON(R8)2, CF3, CH2CF3, CH2CHF2, o un C1-8-R9 de cadena recta, ramificada o cíclico donde hasta dos unidades CH2 pueden ser reemplazadas por O, CO, S, SO, SO2 o NR8; R4 es H, alquilo C1-8, halo, cicloalquilo C3-8, donde hasta dos unidades CH2 pueden ser reemplazadas por O, CO, S, SO, SO2, o NR8, o 2 R4 tomados juntos pueden formar un anillo cicloalquilo de 3 a 7 miembros; R8 es H, alquilo C1-8, CF3, cicloalquilo C3-8, fluoroalquilo, arilo, heteroarilo, o un C1-8-R9 de cadena recta, ramificada o cíclico donde hasta dos unidades CH2 pueden ser reemplazadas por O, CO, S, SO, SO2 o NR, o 2 R8 tomados junto con los átomos a los que están ligados, forman un anillo; R9 es H, CF3, CO2R, OH, arilo, heteroarilo, cicloalquilo C3-8, heterocicloalquilo, N(R)2, NRCOR, CON(R)2, CN, halo, o SO2R; R es H, alquilo C1-8, arilo, heteroarilo, cicloalquilo C3-8, o heterocicloalquilo; A es un arilo, heteroarilo o heterocíclico opcionalmente sustituido; m es un entero entre 0 y 4 inclusive; n es un entero entre 0 y 3 inclusive; y o es un entero entre 0 y 4 inclusive.
ARP120100346A 2011-02-02 2012-02-02 Pirrolopirazina-amidas de piperidina espirociclica como moduladores de los canales ionicos AR085893A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161438685P 2011-02-02 2011-02-02
US201161440987P 2011-02-09 2011-02-09
US201161495538P 2011-06-10 2011-06-10

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AR085893A1 true AR085893A1 (es) 2013-11-06

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US (3) US8916565B2 (es)
EP (2) EP3056495A1 (es)
JP (2) JP6021824B2 (es)
KR (1) KR101923367B1 (es)
CN (2) CN106008504A (es)
AR (1) AR085893A1 (es)
AU (1) AU2012212196B2 (es)
BR (1) BR112013019211A2 (es)
CA (1) CA2825204C (es)
CY (1) CY1117471T1 (es)
DK (1) DK2670752T3 (es)
ES (1) ES2573497T3 (es)
HR (1) HRP20160382T8 (es)
HU (1) HUE028789T2 (es)
IL (1) IL227815B (es)
MX (1) MX355907B (es)
NZ (1) NZ613028A (es)
PL (1) PL2670752T3 (es)
PT (1) PT2670752E (es)
RS (1) RS54785B1 (es)
RU (1) RU2634900C2 (es)
SG (1) SG192248A1 (es)
SI (1) SI2670752T1 (es)
SM (1) SMT201600162B (es)
TW (2) TWI520964B (es)
WO (1) WO2012106499A1 (es)
ZA (1) ZA201305152B (es)

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