AR085893A1 - Pirrolopirazina-amidas de piperidina espirociclica como moduladores de los canales ionicos - Google Patents
Pirrolopirazina-amidas de piperidina espirociclica como moduladores de los canales ionicosInfo
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- 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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- Prior art keywords
- cycloalkyl
- alkyl
- replaced
- units
- halo
- Prior art date
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/499—Spiro-condensed pyrazines or piperazines
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
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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.
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 |
Publications (1)
Publication Number | Publication Date |
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AR085893A1 true AR085893A1 (es) | 2013-11-06 |
Family
ID=45689011
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP120100346A AR085893A1 (es) | 2011-02-02 | 2012-02-02 | Pirrolopirazina-amidas de piperidina espirociclica como moduladores de los canales ionicos |
Country Status (27)
Country | Link |
---|---|
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) |
Families Citing this family (59)
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EP2187884B1 (en) | 2007-08-24 | 2016-03-30 | Vertex Pharmaceuticals Incorporated | Isothiazolopyridinones useful for the treatment of (inter alia) cystic fibrosis |
US8598164B2 (en) | 2010-05-06 | 2013-12-03 | Vertex Pharmaceuticals Incorporated | Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels |
HUE028789T2 (en) * | 2011-02-02 | 2017-01-30 | Vertex Pharma | Pyrrolopyrazine spirocyclic piperidinamides as modulators of ion channels |
MX2013009393A (es) | 2011-02-18 | 2013-08-29 | Vertex Pharma | Piperidinamidas cromano-espirociclicas como moduladores de canales de iones. |
MX347982B (es) | 2011-03-14 | 2017-05-22 | Vertex Pharma | Morfolina-piperidina espirociclica-amidas como moduladores de canales ionicos. |
CN104093716B (zh) | 2011-10-31 | 2017-06-23 | 克赛农制药股份有限公司 | 联芳醚磺酰胺化合物及其作为治疗剂的用途 |
RU2014121984A (ru) | 2011-10-31 | 2015-12-10 | Ксенон Фармасьютикалз Инк. | Бензолсульфонамидные соединения и их применение в качестве терапевтических средств |
IN2014MN02574A (es) | 2012-05-22 | 2015-07-24 | Genentech Inc | |
US10071957B2 (en) | 2012-07-06 | 2018-09-11 | Genentech, Inc. | N-substituted benzamides and methods of use thereof |
WO2014022639A1 (en) | 2012-08-01 | 2014-02-06 | Vertex Pharmaceuticals Incorporated | Solid forms of (4-isopropoxy-3-methoxyphenyl)(2'-methyl-6'-(trifluoromethyl)-3',4'-dihydro-2'h-spiro[piperidine-4,1'-pyrrolo[1,2-a]pyrazine]-1-yl)methanone |
CN105026373B (zh) | 2013-01-31 | 2018-03-30 | 沃泰克斯药物股份有限公司 | 作为钠通道调节剂的吡啶酮酰胺 |
ES2620379T3 (es) | 2013-01-31 | 2017-06-28 | Vertex Pharmaceuticals Inc. | Quinolina y quinoxalina amidas como moduladores de canales de sodio |
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