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AR066437A1 - Benzo-oxazinas y pirimidinas condensadas con heterociclos que contienen nitrogeno y oxigeno, composiciones farmaceuticas que las contienen y usos de las mismas para el tratamiento de diabetes,obesidad y enfermedades asociadas a ellas. - Google Patents

Benzo-oxazinas y pirimidinas condensadas con heterociclos que contienen nitrogeno y oxigeno, composiciones farmaceuticas que las contienen y usos de las mismas para el tratamiento de diabetes,obesidad y enfermedades asociadas a ellas.

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Publication number
AR066437A1
AR066437A1 ARP080101887A ARP080101887A AR066437A1 AR 066437 A1 AR066437 A1 AR 066437A1 AR P080101887 A ARP080101887 A AR P080101887A AR P080101887 A ARP080101887 A AR P080101887A AR 066437 A1 AR066437 A1 AR 066437A1
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Argentina
Prior art keywords
heterocyclyl
aryl
heteroaryl
cycloalkyl
nr9r9
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ARP080101887A
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English (en)
Inventor
John M Fevig
Dean A Wacker
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Bristol Myers Squibb Co
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Publication of AR066437A1 publication Critical patent/AR066437A1/es

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Abstract

Compuestos que son agonistas del receptor acoplado a la proteína G GPR119. Los moduladores del receptor acoplado a la proteína G GPR1 19 son utiles en el tratamiento, prevencion, o disminucion del progreso de enfermedades que requieren terapiamoduladora del receptor acoplado a la proteína G GPR119. Reivindicacion 1: Un compuesto de la formula 1 y enantiomeros, diastereomeros y sales farmacéuticamente aceptables de los mismos caracterizado porque: A, B y D son cada unoindependientemente seleccionados para ser CR4b o N; E es CH2, O o NH, con la condicion que cuando E es CH2 al menos uno de A, B o D es N; G es CH o N; Y es -NR3, O o S; Z está ausente o =O; n1 es 1 o 2; n2 y n3 son cada uno independientementeseleccionados para ser 0-2; n4 es 0-3; R1 es arilo o heteroarilo, cada uno de los cuales pueden ser opcionalmente substituidos con uno o más substituyentes seleccionados de R4; R2 se selecciona del grupo que consiste de cicloalquilo, arilo,heteroarilo, heterociclilo, -C(=O)R5 y -C(=O)OR5, en donde el cicloalquilo, arilo, heteroarilo y heterociclilo puede cada uno ser opcionalmente substituido con uno o más R6; R3 se selecciona del grupo que consiste de hidrogeno, alquilo, alcoxi,cicloalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo y heterocicliloalquilo; R4, cada vez que se presenta, se selecciona independientemente del grupo que consiste de alquilo, arilo, alquenilo, alquinilo, cicloalquilo,heteroarilo, heterociclilo, halo, -CN, -C(=O)OH, -C(=O)OR10, -OCF3, -OR10, -OH, -SH, -SR10, -S(O)3H, -P(O)3H2, -C(=O)NR9R9, -NR9R9, -S(O)2NR9R9, -NR9S(O)2CF3, -C(=O)NR9S(O)2R9, -S(O)2NR9C(=O)OR9, -S(O)2NR9C(=O)NR9R9, -C(=O)NR9S(O)2CF3 -C(=O)R10,NR9C(=O)H, -NR9C(=O)R10, -OC(=O)R10, -OC(=O)NR9R9, -C(=NR14)NR9R9, - NHC(=NR14)NR14R14, -S(=O)R10, -S(O)2R10, -NR9C(=O)OR8 y -NR9S(O2)R8, en donde el alquilo, arilo, alquenilo, alquinilo, cicloalquilo, heteroarilo y heterociclilo pueden cada uno seropcionalmente substituido con uno o más R6; R4b, cada que se presenta, se selecciona independientemente del grupo que consiste de hidrogeno, alquilo, haloalquilo, arilo, alquenilo, alquinilo, cicloalquilo, heteroarilo, heterociclilo, halo, -NH2, -CN, -NO2, -C(=O)OH, -C(=O)OR10, -OCF3, -OR10, -OH, -SH, -SR10, -S(O)3H, -P(O)3H2, -C(=O)NR9R9, -NR9R9, -S(O)2NR9R9, -NR9S(O)2CF3, -C(=O)NR9S(O)2R9, -S(O)2NR9C(=O)OR9, -S(O)2NR9C(=O)NR9R9, -C(=O)NR9S(O)2CF3 -C(=O)R10, -NR9C(=O)H, -NR9C(=O)R10, -OC(=O)R10, -OC(=O)NR9R9, -C(=NR14)NR9R9, -NHC(=NR14)NR14R14, -S(=O)R10, -S(O)2R10, - NR9C(=O)OR8 y -NR9S(O2)R8, en donde el alquilo, arilo, alquenilo, alquinilo, cicloalquilo, heteroarilo y heterociclilo pueden cada uno ser opcionalmente substituidocon uno o más R6; R5 se selecciona del grupo que consiste de alquilo, arilo, cicloalquilo, heteroarilo y heterociclilo, cada uno de los cuales pueden ser opcionalmente substituidos con uno o más R6; R6, cada vez que se presenta, se seleccionaindependientemente del grupo que consiste de alquilo, haloalquilo, arilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo, heterociclilo heterocicliloalquilo, halo, -NH2, -CN, -NO2, - C(=O)OH, -C(=O)OR10, -OCF3, -OR10, -OH, -SH, -SR10, -S(O)3H, -P(O)3H2, - C(=O)NR9R9, -NR9R9, -S(O)2NR9R9, -NR9S(O)2CF3, -C(=O)NR9S(O)2R9, -S(O)2NR9C(=O)OR9, -S(O)2NR9C(=O)NR9R9, -C(=O)NR9S(O)2CF3, -C(=O)R10, -NR9C(=O)H, -NR9C(=O)R10, -OC(=O)R10, -C(=NR14)NR9R9, -NHC(=NR14)NR14R14, -S(=O)R10, -S(O)2R10, -NR9C(=O)OR8 y -NR9S(O2)R8; R8, cada vez que se presenta, se selecciona independientemente del grupo que consiste de alquilo, arilo, cicloalquilo, heteroarilo y heterociclilo; R9, cada vez que se presenta, seselecciona independientemente del grupo que consiste de hidrogeno, alquilo, alcoxi, cicloalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo y heterocicliloalquilo, en donde el arilo, arilalquilo, heteroarilo,heteroarilalquilo, heterociclilo y heterocicliloalquilo puede cada uno ser opcionalmente substituido con 0-5 R9a, y el heteroarilo, heteroarilalquilo, heterociclilo y heterocicliloalquilo cada uno contiene 1-4 heteroátomos seleccionados de N, O y S;R9a, cada vez que se presenta, se selecciona independientemente del grupo que consiste de alquilo, haloalquilo, arilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, heterocicliloalquilo, halo,-NH2, -CN, -NO2, - C(=O)OH, -C(=O)OR14, -OCF3, -OR14, -OH, -SH, -SR14, -S(O)3H, -P(O)3H2, -C(=O)NR14R14, -NR14R14, -S(O)2NR14R14, -NR14S(O)2CF3, -C(=O)NR14S(O)2R10, - S(O)2NR14C(=O)OR10, -S(O)2NR14C(=O)NR14R14, -C(=O)NR14S(O)2CF3, -C(=O)R14, -NR14C(=O)H, -NR14C(=O)R14, -OC(=O)R14, -C(=NR14)NR14R14, -NHC(=NR14)NR14R14, -S(=O)R14, -S(O)2R14, -NR14C(=O)OR8, -NR14S(O2)R8 y arilalquilo; R10, cada vez que se presenta, se selecciona independientemente del grupo que consiste de alquilo,cicloalquilo, alquenilo, alquinilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo y heterocicliloalquilo, en donde el arilo, arilalquilo, heterociclilo y heterocicliloalquilo pueden cada uno ser opcionalmente substituido con 0-5R10a, y el heterociclilo y heterocicliloalquilo cada uno contienen 1-4 heteroátomos seleccionados de N, O y S; R10a, cada vez que se presenta, se selecciona independientemente del grupo que consiste de alquilo, haloalquilo, arilo, alquenilo,alquinilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, heterocicliloalquilo, halo, -NH2, -CN, -NO2, -C(=O)OH, -C(=O)OR14, -OCF3, -OR14, -OH, -SH, -SR14, -S(O)3H, -P(O)3H2, -C(=O)NR14R14, -NR14R14, -S(O)2NR14R14, -NR14S(O)2CF3, -C(=O)NR14S(O)2R9, -S(O)2NR14C(=O)OR9, -S(O)2NR14C(=O)NR14R14, -C(=O)NR14S(O)2CF3 -C(=O)R14, -NR14C(=O)H, -NR14C(=O)R14, -OC(=O)R14, -C(=NR14)NR14R14, -NHC(=NR14)NR14R14, -S(=O)R14, -S(O)2R14, -NR14C(=O)OR8, -R14S(O2)R8 y arilalquilo;y R14, cada vez que se presenta, se selecciona independientemente del grupo que consiste de hidrogeno, alquilo, cicloalquilo y arilo.
ARP080101887A 2007-05-04 2008-05-02 Benzo-oxazinas y pirimidinas condensadas con heterociclos que contienen nitrogeno y oxigeno, composiciones farmaceuticas que las contienen y usos de las mismas para el tratamiento de diabetes,obesidad y enfermedades asociadas a ellas. AR066437A1 (es)

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