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AR067568A1 - Agonistas de receptor acoplado a proteina g gpr119 de piridona y una composicion farmaceutica que los contiene - Google Patents

Agonistas de receptor acoplado a proteina g gpr119 de piridona y una composicion farmaceutica que los contiene

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Publication number
AR067568A1
AR067568A1 ARP080103060A ARP080103060A AR067568A1 AR 067568 A1 AR067568 A1 AR 067568A1 AR P080103060 A ARP080103060 A AR P080103060A AR P080103060 A ARP080103060 A AR P080103060A AR 067568 A1 AR067568 A1 AR 067568A1
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AR
Argentina
Prior art keywords
heterocyclyl
cycloalkyl
aryl
nr14r14
alkyl
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ARP080103060A
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English (en)
Inventor
Dean A Wacker
Karen A Rossi
Ying Wang
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Bristol Myers Squibb Co
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Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AR067568A1 publication Critical patent/AR067568A1/es

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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

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Abstract

Los moduladores del receptor acoplado a proteína G GPR119 son utiles en el tratamiento, prevencion o ralentizacion de la progresion de enfermedades que requieren tratamiento modulador del receptor acoplado a proteína G GPR119, tales como la diabetes Reivindicacion 1: Un compuesto caracterizado. porque es seleccionado de compuestos, de Formula 1 y Formula 1A: y sus enantiomeros, diastereoisomeros, solvatos y sales farmacéuticamente aceptables que tienen el anillo A y anillo B, en las que: el anillo A está opcionalmente sustituido con uno o. más R mostrados como R20 y R21; G es CH o N; Q es C o N; X es CH o N, con la condicion de que Q y X no son ambos N; Y es CH2, N(R3), C(=O), O, OCR9R9, S, S(=O) o S(O)2; n1 es 0-2; n2 es 0-2; n3 es 1-2; R1 es un arilo monocíclico de 6 miembros, un heteroarilo monocíclico de 5 miembros o un heteroarilo monocíclico de 6 miembros, cada uno de los cuales puede estar opcionalmente sustituido con uno o más miembros seleccionados de R1a, R1b, R1c, R1d y R1e; R1a, R1b, R1c, R1d y R1e se selecciona cada uno independientemente del grupo constituido por hidrogeno, alquilo, alquenilo, alquinilo, cicloalquilo, arilo heterociclilo, halo, -NH2, -CN, -NO2, -C(=O)OH, -C(=O)OR10, -OCF3, -OR11, -OH, -SH, -SR11, -S(O)3H, -P(O)3H2, -C(=O)NR9R9, -NR12R12, -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)R11, -NR9C(=O)H, -NR9C(=O)R10, -OC(=O)R10, -OC(=O)NR9R9, -C(=NR14)NR9R9, -NHC(=NR14)NR14R14, -S(=O)R11, -S(O)2R11, -NR9C(=O)OR8 y -NR9S(O2)R8, donde: (a) el alquenilo, alquinilo, cicloalquilo, arilo y heterociclilo puede estar cada uno opcionalmente sustituido con uno o más R6; y (b) el alquilo puede estar opcionalmente sustituido con uno o más de R7; R2 es cicloalquilo, arilo, heteroarilo, heterociclilo, -S(O)2R5, -C(=O)NR3R5, -C(=O)R5 o -C(=O)OR5, pudiendo estar cada uno de cicloalquilo, arilo, heteroarilo y heterociclilo opcionalmente sustituido con uno o más R6; R3 es hidrogeno, alquilo, alcoxi, cicloalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo o heterociclilalquilo; R5 es alquilo, alquenilo, arilo, cicloalquilo, heteroarilo o heterociclilo, cada uno de los cuales puede estar opcionalmente sustituido con uno o más R6; R6, cada vez que aparece, se selecciona independientemente de alquilo, haloalquilo, arilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, heterociclilalquilo, 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, =O, -NR9C(=O)OR8 y -NR9S(O2)R8, pudiendo estar cada uno de alquilo, alquenilo, alquinilo, arilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo, heterociclilo y heterociclilalquilo opcionalmente sustituido con 0-5 R9a; R7, cada vez que aparece, se selecciona independientemente del grupo constituido por alquilo, haloalquilo, arilo, alquenilo, alquinilo, cicloalquilo cicloalquilalquilo, 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, -C(=NR14)NR9R9, -NHC(=NR14)NR14R14, -S(=O)R10, -S(O)2R10, =O, -NR9C(=O)OR8 y -NR9S(O2)R8, pudiendo estar cada uno de alquilo, alquenilo, alquinilo, arilo, cicloalquilo, cicloalquilalquilo y heterociclilo opcionalmente sustituido con 0-5 R9a; R8, cada vez que aparece, se selecciona independientemente del grupo constituido por alquilo, arilo, cicloalquilo, heteroarilo y heterociclilo, cada uno de los cuales puede estar opcionalmente sustituido con uno o más R8a; R8a, cada vez que aparece, se selecciona independientemente de alquilo, haloalquilo, arilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, heterociclilalquilo, 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)2R14, -S(O)2NR14C(=O)OR14, -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, =O, -NR14C(=O)OR14 y -NR14S(O2)R14; R9, cada vez que aparece, se selecciona independientemente de hidrogeno, alquilo, alcoxi, cicloalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo y heterociclilalquilo, pudiendo estar cada uno de alquilo, cicloalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo y heterociclilalquilo opcionalmente sustituido con 0-5 R9a; R9a, cada vez que aparece, se selecciona independientemente de alquilo, haloalquilo, arilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, heterociclilalquilo, 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, =O y arilalquilo; R10, cada vez que aparece, se selecciona independientemente de alquilo, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo y heterociclilalquilo, pudiendo estar cada uno de cicloalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo y heterociclilalquilo opcionalmente sustituido con 0-3 R10a; R10a, cada vez que aparece, se selecciona independientemente de alquilo, haloalquilo, arilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, heterociclilalquilo, 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, -NR14S(O2)R8 y arilalquilo; R11, cada vez que aparece, se selecciona independientemente de alquilo, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heterociclilo y heterociclilalquilo, pudiendo estar cada uno de cicloalquilo, arilo, arilalquilo, heterociclilo y heterociclilalquilo opcionalmente sustituido con 0-3 R11a; R11a, cada vez que aparece, se selecciona independientemente de alquilo, haloalquilo, arilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, heterociclilalquilo, halo, -NR2, -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, -NR14S(O2)R8 y arilalquilo; R12, cada vez que aparece, se selecciona independientemente de hidrogeno, alquilo, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heterociclilo y heterociclilalquilo, pudiendo estar cada uno de cicloalquilo, arilo, arilalquilo, heterociclilo y heterociclilalquilo opcionalmente sustituido con 0-3 R10a; R14, cada vez que aparece, se selecciona independientemente de hidrogeno, alquilo, cicloalquilo y arilo: y R20 y R21 se selecciona cada uno independientemente del grupo constituido por hidrogeno, alquilo, haloalquilo, cicloalquilo, halo, -CN, -C(=O)OH, -C(=O)OR10, -OCF3, -OR10, -OH, -C(=O)NR9R9, -C(=O)R10 y -OC(=O)R10.
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PL2170864T3 (pl) 2012-02-29
CN101801957A (zh) 2010-08-11
CN103550218A (zh) 2014-02-05
HRP20110806T1 (hr) 2011-11-30
BRPI0815097A2 (pt) 2018-07-24
CL2008002111A1 (es) 2008-10-24
CA2693439A1 (en) 2009-01-22
TW200904440A (en) 2009-02-01
EP2173737A1 (en) 2010-04-14
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JP5301539B2 (ja) 2013-09-25
US20090023702A1 (en) 2009-01-22
CY1112751T1 (el) 2016-02-10
BRPI0814428A2 (pt) 2015-01-06
US8178561B2 (en) 2012-05-15
AU2008276057B2 (en) 2013-01-31
PT2170864E (pt) 2011-11-25
US20120258959A1 (en) 2012-10-11
PE20090888A1 (es) 2009-07-15
CA2693444A1 (en) 2009-01-22
ATE524460T1 (de) 2011-09-15
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ES2371515T3 (es) 2012-01-04
EP2170864B1 (en) 2011-09-14
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US8232404B2 (en) 2012-07-31
AU2008276055B2 (en) 2013-01-31
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CO6160315A2 (es) 2010-05-20
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NZ582661A (en) 2012-03-30
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US7928230B2 (en) 2011-04-19
SI2170864T1 (sl) 2012-04-30
HRP20120221T1 (hr) 2012-04-30
US20120232048A1 (en) 2012-09-13
PT2173737E (pt) 2012-03-19
EP2170864A1 (en) 2010-04-07
WO2009012275A1 (en) 2009-01-22
ZA201000151B (en) 2011-03-30
US20110245227A1 (en) 2011-10-06
ZA201000326B (en) 2011-03-30
KR20100051814A (ko) 2010-05-18
EA201000210A1 (ru) 2010-06-30
CN101801956B (zh) 2013-11-20
AU2008276055A1 (en) 2009-01-22
US20110190327A1 (en) 2011-08-04
US20090042919A1 (en) 2009-02-12
ATE540945T1 (de) 2012-01-15
AR067569A1 (es) 2009-10-14
DK2170864T3 (da) 2012-01-16
US8003796B2 (en) 2011-08-23
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PL2173737T3 (pl) 2012-06-29
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KR20100045471A (ko) 2010-05-03

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