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AR079749A2 - Derivados de azaindoles heterociclicos inhibidores de quinasas jak-3, aurora a y rock, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades del sistema nervioso central y trastornos inmunologicos y/o alergicos. - Google Patents

Derivados de azaindoles heterociclicos inhibidores de quinasas jak-3, aurora a y rock, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades del sistema nervioso central y trastornos inmunologicos y/o alergicos.

Info

Publication number
AR079749A2
AR079749A2 ARP100104957A ARP100104957A AR079749A2 AR 079749 A2 AR079749 A2 AR 079749A2 AR P100104957 A ARP100104957 A AR P100104957A AR P100104957 A ARP100104957 A AR P100104957A AR 079749 A2 AR079749 A2 AR 079749A2
Authority
AR
Argentina
Prior art keywords
phenyl
optionally substituted
jak
conr
sulfur
Prior art date
Application number
ARP100104957A
Other languages
English (en)
Inventor
Jon H Come
David J Lauffer
Dean Boyall
Randy S Bethiel
Simon Everitt
Edmund M Harrington
Alex Aronov
Michael Mortimore
Jeremy Green
John J Court
Luc Farmer
Damien Fraysee
Francesco G Salituro
Francoise Pierard
Daniel Robinson
Hayley Binch
Jean-Damien Charrier
Original Assignee
Vertex Pharma
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34971569&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR079749(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of AR079749A2 publication Critical patent/AR079749A2/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
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    • C07D471/00—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
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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Abstract

Un compuesto azaindol util como inhibidor de las proteínas quinasas JAK u otras proteínas quinasas, compuesto que tiene la formula (1) o las sales farmacéuticamente aceptables del mismo, divisional de la solicitud de Patente argentina Ns P050101254, caracterizado porque el compuesto de formula (2) es cualquiera de las formulas (3), R1 es T-R' o -Si(R')3, R2, R3 y R4 son, cada uno, independientemente halogeno, -CN, -NO2, o V-R'; x es 1, 2, 3, o 4; cada ocurrencia de R5 es independientemente halogeno, -CN, -NO2, o U-R', donde al menos un R5 es -N(R')2, - NR'CH(CH2OH)R', -NR'CH(CH2CH2OH)R', -NR'(CH2)R', -NR'(CH2)2R', -NR'(CH2)N(R')2, o -NR'(CH2)2N(R')2; T, V y U son, cada uno, independientemente un enlace o una cadena de alquilideno C1-6 opcionalmente sustituida, donde hasta dos unidades de metileno de la cadena están opcional e independientemente reemplazada por -NR'-, -S-, -O-, -CS-, -CO2-, -OCO-, -CO-, -COCO-, -CONR'-, -NR'CO-, -NR'CO2-, -SO2NR'-, -NR'SO2-, -CONR'NR'-, -NR'CONR'-, -OCONR'-, -NR'NR'-, -NR'SO2NR'-, -SO-, -SO2-, -PO-, -PO2-, o -POR'-; y cada ocurrencia de R' es independientemente hidrogeno o un grupo opcionalmente sustituido seleccionado entre un grupo alifático C1-6, un anillo monocíclico de 3-8 miembros saturado, parcialmente insaturado o completamente insaturado que tiene 0-3 heteroátomos seleccionados independientemente entre nitrogeno, oxígeno o azufre, o un sistema anular bicíclico de 8-12 miembros saturado, parcialmente insaturado o completamente insaturado que tiene 0-5 heteroátomos seleccionados independientemente entre nitrogeno, oxígeno o azufre; o dos ocurrencias de R' se toman conjuntamente con el(los) átomo(s) al (los) cuales está(n) unido(s) para formar un anillo monocíclico o bicíclico de 3-12 miembros, opcionalmente sustituido, saturado, parcialmente insaturado, o completamente insaturado que tiene 1-4 heteroátomos seleccionados independientemente entre nitrogeno, oxigeno o azufre, con la condicion de que: a) si R1, R2, R3 y R4 son simultáneamente H, x es 1, R5 es -NH2 y X1 y X2 son N, entonces X3 no es CH; b) si R2, R3 y R4 son simultáneamente H, X1, X2 y X3 son CH, y dos R5 forman un anillo bicíclico opcionalmente sustituido fusionado con el anillo al que están unidos, entonces R1 no es CH2CH2N(Me)2, c) si R2 y R3 son simultáneamente H, R4 es NH2, y X1, X2 y X3 son CH, entonces R1 no es fenilo sustituido; d) si R2, R3 y R4 son simultáneamente H, entonces R1 no es Si(R')3; y e) si R1, R2 y R4 son simultáneamente H e (i) X2 y X3 son CH o CR5 o (ii) cualquiera de X1, X2 o X3 son N, entonces R3 no es fenilo o fenilo sustituido con O-fenilo o N(Me)2.
ARP100104957A 2004-03-30 2010-12-27 Derivados de azaindoles heterociclicos inhibidores de quinasas jak-3, aurora a y rock, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades del sistema nervioso central y trastornos inmunologicos y/o alergicos. AR079749A2 (es)

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ARP050101254A AR048454A1 (es) 2004-03-30 2005-03-30 Azaindoles utiles como inhibidores de las proteinas quinasas jak u otras proteinas quinasas
ARP100104957A AR079749A2 (es) 2004-03-30 2010-12-27 Derivados de azaindoles heterociclicos inhibidores de quinasas jak-3, aurora a y rock, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades del sistema nervioso central y trastornos inmunologicos y/o alergicos.

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