AR084294A1 - Compuestos de 2-amino-4-ariltiazol, metodos para su sintesis y uso como antagonista de trpa1 - Google Patents

Compuestos de 2-amino-4-ariltiazol, metodos para su sintesis y uso como antagonista de trpa1

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Publication number
AR084294A1
AR084294A1 ARP110104687A ARP110104687A AR084294A1 AR 084294 A1 AR084294 A1 AR 084294A1 AR P110104687 A ARP110104687 A AR P110104687A AR P110104687 A ARP110104687 A AR P110104687A AR 084294 A1 AR084294 A1 AR 084294A1
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Argentina
Prior art keywords
substituted
hydrogen
alkyl
independently selected
different
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ARP110104687A
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English (en)
Inventor
Sukeerthi Kumar
Abraham Thomas
Sachin Sundarlal Chaudhari
Bipin Parsottam Kansagra
Venkata Ramana Yemireddy
Neelima Khairatkar-Joshi
Indranil Mukhopadhyay
Girish Gudi
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Glenmark Pharmaceuticals Sa
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Application filed by Glenmark Pharmaceuticals Sa filed Critical Glenmark Pharmaceuticals Sa
Publication of AR084294A1 publication Critical patent/AR084294A1/es

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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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Abstract

La presente está relacionada a derivados de 2-amino-4-ariltiazol como moduladores de TRPA (Potencial Transitorio del Receptor subfamilia A). En particular, los compuestos descriptos aquí son útiles para el tratamiento de, o para evitar, enfermedades, condiciones y/o desórdenes modulados por el TRPA1 (Potencial Transitorio del Receptor subfamilia A, miembro 1). También se proveen procesos para preparar los compuestos descriptos, intermediarios utilizados en su síntesis, composiciones farmacéuticas de ellos, y métodos para el tratamiento de, o evitar, enfermedades, condiciones y/o desórdenes modulados por el TRPA1.Reivindicación 1: Un compuesto de fórmula (1) o una de sus sales farmacéuticamente aceptables, caracterizado porque Het se selecciona del grupo de formulas (2); P se selecciona del grupo de formulas (3); R1 se selecciona de hidrógeno, halógeno, ciano, hidroxilo, alquilo sustituido o no sustituido, alcoxi, haloalquilo, haloalcoxi, cicloalquilo, cicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, anillo heterocíclico y heterociclilalquilo; en cada ocurrencia; R2, que pueden ser el mismo o diferente, es independientemente elegido de halógeno, ciano, hidroxilo, nitro, -NReRf, alquilo sustituido o no sustituido, alcoxi, haloalquilo, haloalcoxi, cicloalquilo, cicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, anillo heterocíclico y heterociclilalquilo; R3 se selecciona de -NR6R7, alquilo sustituido o no sustituido, arilo, anillo heterocíclico, heterociclilalquilo y heteroarilo; R3 o el grupo -OC(=O)R3 es independientemente elegido de aminoácidos: isoleucinato, leucinato, lisinato, metioninato, fenilalaninato, treoninato, triptofanato, valinato, alaninato, asparaginato, acetato aspártico, cisteinato, acetato glutámico, glutaminato, glicinato, prolinato, selenocisteinato, serinato, tirosinato, argininato, histidinato, ornitinato y taurinato; R4 y R5, que pueden ser los mismos o diferentes, son independientemente seleccionados de hidrógeno, alquilo sustituido o no sustituido, hidroxialquilo, arilalquilo, heterociclilalquilo, heteroarilalquilo, -(CRgRh)p-C(O)-alquilo C1-4, (CRgRh)p-C(O)-NReRf, (CRgRh)p-NReRf, -(CRgRh)p-NRe-C(O)-NReRf y -(CRgRh)p-NRe-C(=NH)-NReRf; R6 y R7, que pueden los mismos o diferentes, son independientemente seleccionados de hidrógeno, alquilo sustituido o no sustituido e hidroxialquilo; o R6 y R7 junto con el átomo de nitrógeno al que están unidos, forman un anillo cíclico, que puede ser monocíclico, bicíclico o tricíclico, que está sustituido o no sustituido y en donde el anillo cíclico opcionalmente contiene uno o más heteroátomos elegidos de O, N o S; R8 se selecciona de hidrógeno, alquilo C1-4, arilalquilo y catión farmacéuticamente aceptable (M+ ó M2+); Ra, Rb y Rd, que pueden ser los mismos o diferentes, son seleccionados cada uno en forma independiente de hidrógeno, trifluorometilo, difluorometilo, 2,2,2-trifluoroetilo y alquilo C1-4; Rc se selecciona de hidrógeno, halógeno, trifluorometilo, difluorometilo, 2,2,2-trifluoroetilo y alquilo C1-4; Re y Rf, que pueden ser los mismos o diferentes, son independientemente seleccionados de hidrógeno, alquilo sustituido o no sustituido e hidroxialquilo; o Re y Rf junto con el átomo de nitrógeno al que están unidos, forman un anillo cíclico, que puede ser monocíclico, bicíclico o tricíclico, que está sustituido o no sustituido y en donde el anillo cíclico opcionalmente contiene uno o más heteroátomos elegidos de O, N o S; Rg y Rh, que pueden ser los mismos o diferentes, son cada uno independientemente hidrógeno o alquilo C1-4; ‘m’ es un entero en el rango que va de 0 a 5, incluidos ambos; ‘n’ es un entero en el rango que va de 1 a 4, incluidos ambos; y ‘p’ es un entero en el rango que va de 1 a 3, incluidos ambos.
ARP110104687A 2010-12-20 2011-12-15 Compuestos de 2-amino-4-ariltiazol, metodos para su sintesis y uso como antagonista de trpa1 AR084294A1 (es)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
IN3451MU2010 2010-12-20
US201061428327P 2010-12-30 2010-12-30
IN748MU2011 2011-03-16
US201161466535P 2011-03-23 2011-03-23
IN1569MU2011 2011-05-25
US201161495002P 2011-06-09 2011-06-09
IN2741MU2011 2011-09-28
US201161552076P 2011-10-27 2011-10-27

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AR084294A1 true AR084294A1 (es) 2013-05-08

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US (3) US8592398B2 (es)
EP (1) EP2655377B1 (es)
JP (1) JP5694560B2 (es)
KR (1) KR101591153B1 (es)
CN (1) CN103261201B (es)
AP (1) AP3391A (es)
AR (1) AR084294A1 (es)
AU (1) AU2011346763B2 (es)
BR (1) BR112013014692A2 (es)
CA (1) CA2820448A1 (es)
CL (1) CL2013001810A1 (es)
EA (1) EA023141B1 (es)
HK (1) HK1191008A1 (es)
MX (1) MX336549B (es)
MY (1) MY159059A (es)
PE (1) PE20140234A1 (es)
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