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AR059778A1 - Compuestos de pirrolotriazina inhibidores de quinasas p38,composiciones farmaceuticas que los contienen y usos en gran variedad de procesos inflamatorios. - Google Patents

Compuestos de pirrolotriazina inhibidores de quinasas p38,composiciones farmaceuticas que los contienen y usos en gran variedad de procesos inflamatorios.

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Publication number
AR059778A1
AR059778A1 ARP070100944A ARP070100944A AR059778A1 AR 059778 A1 AR059778 A1 AR 059778A1 AR P070100944 A ARP070100944 A AR P070100944A AR P070100944 A ARP070100944 A AR P070100944A AR 059778 A1 AR059778 A1 AR 059778A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
independently selected
alkyl
cycloalkyl
hydrogen
Prior art date
Application number
ARP070100944A
Other languages
English (en)
Inventor
Vivekananda Y Vrudhula
James Lin
Chunjian Liu
Katerina Leftheris
Original Assignee
Bristol Myers Squibb Co
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
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AR059778A1 publication Critical patent/AR059778A1/es

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    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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Abstract

Reivindicacion 1: Compuesto de la formula (1) o sales del mismo farmacéuticamente aceptables, caracterizado porque al menos un de X1, X2 o X3 escomo se muestra en formula (2) y cualquier X1, X2 o X3 restante es hidrogeno; A1 y A2 son cada uno independientemente seleccionados de alquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, arilo opcionalmente sustituido, aralquilo opcionalmente sustituido, heterociclo opcionalmente sustituido y heteroarilo opcionalmente sustituido; R1, R3 y R5 son cada uno independientemente seleccionados de hidrogeno, alquilo opcionalmente sustituido, -OR14. -C(=O)NR14R14a, -NR14R14a, SO2NR14R14a, -NR14SO2NR14aR14b, -NR14aSO2R14, -NR14C(=O)R14a, -NR14CO2R14a, -NR14C(O)NR14aR14b, halogeno, ciano, cicloalquilo opcionalmente sustituido, arilo opcionalmente sustituido, heterociclo opcionalmente sustituido y heteroarilo opcionalmente sustituido; R2 es independientemente seleccionado de hidrogeno y alquilo opcionalmente sustituido; R4 es independientemente seleccionado del grupo de formulas (3), R6 se une a cualquier átomo de carbono disponible del anillo fenilo y en cada caso es independientemente seleccionado de alquilo opcionalmente sustituido, halogeno, trifluorometoxi, trifluorometilo, hidroxi, alcoxi, alcanoilo, alcanoiloxi, tiol, alquiltio, ureido, nitro, ciano, carboxi, carboxialquilo, carbamilo, alcoxicarbonilo, alquiltiono, ariltiono, arilsulfonilamina, alquilsulfonilamina, ácido sulfonico, alquilsulfonilo, sulfonamido, fenilo, bencilo, ariloxi y benciloxi, en donde cada grupo R6 a su vez puede ser adicionalmente sustituido por uno o dos R18; R14, R14a y R14b se seleccionan independientemente de hidrogeno, alquilo opcionalmente sustituido, arilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, heterociclo opcionalmente sustituido, y heteroarilo opcionalmente sustituido, excepto cuando R14 se une a un grupo sulfonilo, como en -S(=O)R14, -SO2R14, y - NR14aSO2R14, entonces R14 no es hidrogeno; R18 se selecciona independientemente de alquilo de C1-6, alquenilo C2-6, halogeno, haloalquilo, haloalcoxi, ciano, nitro, amino, alquilamino C1-4, aminoalquilo C1-4, hidroxi, hidroxialquilo C1-4, alcoxi, alquiltio C1-4, arilo, heterociclo, (aril)alquilo, ariloxi, y (aril)alcoxi; R27 y R28 se seleccionan independientemente de hidrogeno, alquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, arilo opcionalmente sustituido, aralquilo opcionalmente sustituido, heterociclo opcionalmente sustituido y heteroarilo opcionalmente sustituido; uno de D, E, G, J o L es =N- y cada D, E, G, J o L, restante es =C-; m es 0, 1, 2 o 3; n es 0 o 1;y k es 0, 1 o 2.
ARP070100944A 2006-03-07 2007-03-07 Compuestos de pirrolotriazina inhibidores de quinasas p38,composiciones farmaceuticas que los contienen y usos en gran variedad de procesos inflamatorios. AR059778A1 (es)

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EP (1) EP2001886A2 (es)
JP (1) JP2009535295A (es)
KR (1) KR20080107408A (es)
CN (1) CN101395158A (es)
AR (1) AR059778A1 (es)
AU (1) AU2007223342A1 (es)
BR (1) BRPI0708644A2 (es)
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CA2645031A1 (en) * 2006-03-07 2007-09-13 Bristol-Myers Squibb Company Pyrrolotriazine aniline prodrug compounds useful as kinase inhibitors
WO2009158446A2 (en) * 2008-06-25 2009-12-30 Bristol-Myers Squibb Company Crystalline forms of ((((4-((5-(cyclopropylcarbamoyl)-2-methylphenyl)amino)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)carbonyl)(propyl)carbamoyl)oxy)methyl (4-(phosphonooxy)phenyl)acetate, method of preparation and use thereof
WO2009158450A1 (en) * 2008-06-25 2009-12-30 Bristol-Myers Squibb Company Crystalline forms of ((((4-((5-(cyclopropylcarbamoyl)-2-methylphenyl)amino)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)carbonyl)(propyl)carbamoyl)oxy)methyl (4-(phosphonooxy)phenyl)acetate, preparation and use thereof
NZ602496A (en) 2008-08-19 2013-09-27 Xenoport Inc Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions thereof, and methods of use
TW201035100A (en) 2008-12-19 2010-10-01 Cephalon Inc Pyrrolotriazines as ALK and JAK2 inhibitors
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US20090156555A1 (en) 2009-06-18
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