AR055271A1 - Compuesto del acido bifenil carboxilico, composicion farmaceutica que lo comprende, su uso para preparar esta ultima y proceso para prepararlo - Google Patents

Compuesto del acido bifenil carboxilico, composicion farmaceutica que lo comprende, su uso para preparar esta ultima y proceso para prepararlo

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Publication number
AR055271A1
AR055271A1 ARP050104182A ARP050104182A AR055271A1 AR 055271 A1 AR055271 A1 AR 055271A1 AR P050104182 A ARP050104182 A AR P050104182A AR P050104182 A ARP050104182 A AR P050104182A AR 055271 A1 AR055271 A1 AR 055271A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
hydrogen
independently
groups
Prior art date
Application number
ARP050104182A
Other languages
English (en)
Original Assignee
Smithkline Beecham Corp
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 Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of AR055271A1 publication Critical patent/AR055271A1/es

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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/65—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
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    • C07C233/67—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/68—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/69—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of an acyclic saturated carbon skeleton
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    • C07C233/77—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • C07C233/78—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
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    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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  • Endocrinology (AREA)

Abstract

Compuestos del ácido bifenil carboxílico de la formula (1), en la que R1 se selecciona entre hidrogeno; alquilo C1-6 opcionalmente sustituido con hasta tres grupos seleccionados independientemente entre alcoxi C1-6, halogeno e hidroxi; cicloalquilo C3-7 opcionalmente sustituido independientemente con uno o más grupos de alquilo C1-6; un anillo arilo, heteroarilo, o heterociclilo cada uno opcionalmente sustituido, independientemente, con uno a tres grupos seleccionados entre R5 y R6; R2 es hidrogeno, alquilo C1-6 o un -(CH2)p-cicloalquiloC3-7 opcionalmente sustituido independientemente con uno o más grupos alquilo C1-6, o (CH2)mR1 y R2, junto con el átomo de nitrogeno al que están unidos, forman un anillo heterocíclico de cuatro a seis miembros opcionalmente sustituido, que contiene opcionalmente otro heteroátomo seleccionado entre O/N/S; R3 es halogeno o metilo; R4 es hidrogeno, alquilo C1-6, alquilo C1-6, halo-alquiloC1-4 sustituido o cicloalquilo C3-7; R5 es independientemente alquilo C1-6, OR4, -(CH2)p-cicloalquiloC3-7 opcionalmente sustituido independientemente con uno o más grupos alquilo C1-6, -CONR9R10, -NHCOR10, -SO2NHR9, -(CH2)qNHSO2R10, halogeno, CN, -(CH2)qNR11R12, y trifluorometilo; R6 es independientemente hidrogeno, alquilo C1-6, OR4, halogeno, trifluorometilo y -(CH2)qNR11R12; R8 se selecciona entre hidrogeno, alquilo C1-6, cicloalquilo C3-7 opcionalmente sustituido con uno o más grupos alquilo C1-6, OH, alquilo C1-6 opcionalmente sustituido con uno o más grupos hidroxilo, CONHR9, fenilo opcionalmente sustituido con R13 y/o R14, o un heteroarilo opcionalmente sustituido con R13 y/o R14; cada uno de R9 y R10 se selecciona independientemente entre hidrogeno y alquilo C1-6, o R9 y R10, junto con el átomo de nitrogeno al que están unidos, forman un anillo heterocíclico de cinco a seis miembros que opcionalmente contiene un heteroátomo adicional seleccionado entre oxígeno, azufre y N-R15, donde el anillo está opcionalmente sustituido con hasta dos grupos alquilo C1-6; R11 se selecciona entre hidrogeno, alquilo C1-6 y -(CH2)p-cicloalquiloC3-7 opcionalmente sustituido con uno o más grupos alquilo C1-6; R12 se selecciona entre hidrogeno y alquilo C1-6, o R11 y R12, junto con el átomo de nitrogeno al que están unidos, forman un anillo heterocíclico de cinco o seis miembros que opcionalmente contiene un heteroátomo adicional seleccionado entre oxígeno, azufre y N-R15; R13 se selecciona entre alquilo C1-6, alcoxi C1-6, -(CH2)p-cicloalquiloC3-7 opcionalmente sustituido con uno o más grupos alquilo C1-6, -CONR9R10, -NHCOR10, halogeno, CN, -(CH2)qNR11R12, trifluorometilo, fenilo opcionalmente sustituido independientemente con uno o más grupos R14, heterociclilo opcionalmente sustituido independientemente con uno o más grupos R14, y un heteroarilo opcionalmente sustituido independientemente con uno o más grupos R14; R14 se selecciona entre alquilo C1-6, alcoxi C1-6, halogeno, halo-alquiloC1-4 sustituido y NR11R12; R15 se selecciona entre hidrogeno y metilo; cada uno de X e Y se selecciona independientemente entre hidrogeno, metilo y halogeno; Z se selecciona entre -(CH2)sCOOR16, o -(CH2)sCONR16R17; R16 y R17 se seleccionan independientemente entre hidrogeno, alquilo C1-6 opcionalmente sustituido, -(CR20R21)vOR18, -(CR20R2I)vNR18R19, -(CR20R21)vNHSO2R18, -(CR20R21)vCONR18R19, -(CR20R21)vCOOR18, -(CR20R21)theteroarilo opcionalmente sustituido, -(CR20R21)tarilo opcionalmente sustituido, - (CR20R21)theterociclilo opcionalmente sustituido, -(CR20R21)tcicloalquiloC3-7 opcionalmente sustituido o -(CR20R21)tcicloalqueniloC3-7 opcionalmente sustituido; o R16 y R17, junto con el átomo de nitrogeno al que están unidos, forman un anillo de cinco a seis miembros opcionalmente sustituido que opcionalmente contiene al menos un heteroátomo adicional seleccionado entre oxígeno, azufre y N-R15; cada uno de R18 y R19 se selecciona independientemente entre hidrogeno y alquilo C1-6 opcionalmente sustituido con hasta dos grupos hidroxi; o R18 y R19, junto con el átomo de nitrogeno al que están unidos, forman un anillo de cinco a seis miembros, que opcionalmente contiene un heteroátomo adicional seleccionado entre oxígeno, azufre y N-R15, y donde el anillo está opcionalmente sustituido con hasta dos grupos seleccionados independientemente entre oxo, halogeno y alquilo C1-6; R20 y R21 se seleccionan independientemente entre hidrogeno o alquilo C1-4; m es 0 o un numero entero seleccionado entre 1, 2, 3 y 4; p es 0 o un numero entero seleccionado entre 1 y 2; q es 0 o un numero entero seleccionado entre 1, 2 y 3; r es 0 o el numero entero 1; s es 0 o un numero entero seleccionado entre 1, 2, 3 y 4; y t es 0 o un numero entero seleccionado entre 1, 2, 3, 4, 5 y 6; v es un numero entero seleccionado entre 1, 2, 3, 4, 5 y 6; o una sal farmacéuticamente aceptable o un derivado del mismo. Composicion farmacéutica que los comprende y su uso para la preparacion de dicha composicion farmacéutica util para el tratamiento de una afeccion o estado de enfermedad mediado por la actividad quinasa de p38 o mediado por citoquinas producidas por la actividad quinasa de p38. proceso para preparar dichos compuestos. Se aplican en el tratamiento de la inflamacion y enfermedades cronicas relacionadas.
ARP050104182A 2004-10-05 2005-10-03 Compuesto del acido bifenil carboxilico, composicion farmaceutica que lo comprende, su uso para preparar esta ultima y proceso para prepararlo AR055271A1 (es)

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