AR041010A1 - Compuestos de acido piperidinoil carboxilico utiles como antagonistas selectivos del receptor de integrina - Google Patents

Compuestos de acido piperidinoil carboxilico utiles como antagonistas selectivos del receptor de integrina

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AR041010A1
AR041010A1 ARP030102976A ARP030102976A AR041010A1 AR 041010 A1 AR041010 A1 AR 041010A1 AR P030102976 A ARP030102976 A AR P030102976A AR P030102976 A ARP030102976 A AR P030102976A AR 041010 A1 AR041010 A1 AR 041010A1
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alkyl
aryl
group
cycloalkyl
heterocyclyl
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Janssen Pharmaceutica Nv
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Abstract

Reivindicación 1: Un compuesto de fórmula (1), en el cual: W se selecciona del grupo formado por -(alquil C0-3)(R1), -(alquil C1-3)(R1a); -(alquil C0-3)-aril(R1, R8), -(alquil C0-3)-heterociclil(R1, R8), -(alcoxi C0-3)(R1), -(alcoxi C0-3)-aril(R1, R8), y -(alcoxi C0-3)-heterociclil(R1, R8); R1 se selecciona del grupo formado por hidrógeno, -N(R4)2, -N(R4)(R5), -N(R4)(R6), -heterociclil(R8) y -heteroaril(R8); R1a se selecciona del grupo formado por -C(R4)(=N-R4), -C(=N-R4)-(N(R4)2, -C(=N-R4)-N(R4)-C(=O)-R4, -C(=N-R4)-N(R4)-C(=O)-R4, -C(=N-R4)-N(R4)-C(=O)-N(R4)2, -C(=N-R4)-N(R4)-CO2-R4, -C(=N-R4)-N(R4)-SO2-(alquil C1-8) y -C(=N-R4)-N(R4)-SO2-N(R4)2; R4 se selecciona del grupo formado por hidrógeno y -(alquil C1-8)(R7); R5 se selecciona del grupo formado por -(C=O)-R4, -(C=O)-N(R4)2, -(C=O)-cicloalquil(R8), -(C=O)-heterociclil(R8), -(C=O)-aril(R8), -(C=O)-heteroaril(R8), -(C=O)-N(R4)-cicloalquil(R8), -(C=O)-N(R4)-aril(R8), -CO2(R4), -CO2-cicloalquil(R8), -CO2-aril(R8), -C(R4)(=N-R4), -C(=N-R4)-N(R4)2, -C(=N-R4)-N(R4)(R6), -C(=N-R4)-N(R4)-C(=O)-R4, -C(=N-R4)-N(R4)-C(=O)-N(R4)2, -C(=N-R4)-N(R4)-CO2-R4, -C(=N-R4)-N(R4)-SO2-(alquil C1-8)(R7), -C(=N-R4)-N(R4)-SO2-N(R4)2, -N(R4)-C(R4)(=N-R4), N(R4)-C(=N-R4)-N(R4)2, -N(R4)-C(=N-R4)-N(R4)(R6), -N(R4)-C(=N-R4)-N(R4)-C(=O)-R4, -N(R4)-C(=N-R4)-N(R4)-C(=O)-N(R4)2, -N(R4)-C(=N-R4)-N(R4)-CO2R4, -N(R4)-C(=N-R4)-N(R4)-SO2-(alquil C1-8)(R7), -N(R4)-C(=N-R4)-N(R4)-SO2-N(R4)2, -SO2-(alquil C1-8)(R7), -SO2-N(R4)2, -SO2-cicloalquil(R8) y -SO2-aril(R8); R6 se selecciona del grupo formado por -cicloalquil(R8), -heterociclil(R8), -aril(R8) y -heteroaril(R8); R7 es uno a dos sustituyentes seleccionados en forma independiente del grupo formado por hidrógeno, (alcoxi C1-8)(R9), -NH2, -NH-(alquil C1-8)(R9), -N(alquil C1-8)(R9))2, -C(=O)H, -C(=O)-(alquil C1-8)(R9), -C(=O)-NH2, -C(=O)-NH-(alquil C1-8)(R9), -C(=O)-N(alquil C1-8)(R9))2, -C(=O)-NH-aril(R10), -C(=O)-cicloalquil(R10), -C(=O)-heterociclil(R10), -C(=O)-aril(R10), -C(=O)-heteroaril(R10), -CO2H, -CO2-(alquil C1-8)(R9), -CO2-aril(R10), -C(=NH)-NH2, -SH, -S-(alquil C1-8)(R9), -S-(alquil C1-8)-S-(alquil C1-8)(R9), -S-(alquil C1-8)-(alcoxi C1-8)(R9), -S-(alquil C1-8)-NH-(alquil C1-8)(R9), -SO2-(alquil C1-8)(R9), -SO2-NH2, -SO2-NH-(alquil C1-8)(R9), -SO2-N(alquil C1-8)(R9))2, -SO2-aril(R10), ciano, (halo)1-3, hidroxi, nitro, oxo, -cicloalquil(R10), -heterociclil(R10), -aril(R10) y -heteroaril(R10); R8 es uno a cuatro sustituyentes seleccionados en forma independiente del grupo formado por hidrógeno, -(alquil C1-8)(R9), -C(=O)H, -C(=O)-(alquil C1-8)(R9), -C(=O)-NH2, -C(=O)-NH-(alquil C1-8)(R9), -C(=O)-N(alquil C1-8)(R9))2, -C(=O)-NH-aril(R10), -C(=O)-cicloalquil(R10), -C(=O)-heterociclil(R10), -C(=O)-aril(R10), -C(=O)-heteroaril(R10), -CO2H, -CO2-(alquil C1-8)(R9), -CO2-aril(R10), -C(=NH)-NH2, -SO-(alquil C1-8)(R9), -SO2-NH2, -SO2-NH-(alquil C1-8)(R9), -SO2-N(alquil C1-8)(R9))2, -SO2aril(R10), -cicloalquil(R10) y -aril(R10) cuando se unen a un átomo de nitrógeno; y, en donde R8 es uno a cuatro sustituyentes seleccionados en forma independiente del grupo formado por hidrógeno, -(alquil C1-8)(R9), -(alcoxi C1-8)(R9), -O-cicloalquil(R10), -O-aril(R10), -C(=O)H, -C(=O)-(alquil C1-8)(R9), -C(=O)-NH2, -C(=O)-NH-(alquil C1-8)(R9), -C(=O)-N(alquil C18)(R9))2, -C(=O)-NH-aril(R10), -C(=O)-cicloalquil(R10), -C(=O)-heterociclil(R10), -C(=O)-aril(R10), -C(=O)-heteroaril(R10), -CO2H, -CO2-(alquil C1-8)(R9), -CO2-aril(R10), -C(=NH)-NH2, SO2-(alquil C1-8)(R9), SO2-NH2, -SO2-NH-(alquil C1-8)(R9), -SO2-N(alquil C1-8)(R9))2, -SO2-aril(R10), -SH, -S-(alquil C1-8)(R9), -S-(alquil C1-8)-S-(alcoxi C1-8)(R9), -S-(alquil C1-8)-(alcoxi C1-8)(R9), -S-(alquil C1-8)-NH-(alquil C1-8)(R9), -NH2, -NH-(alquil C1-8)(R9), -N(alquil C1-8)(R9))2, ciano, halo, hidroxi, nitro, oxo, -cicloalquil(R10), -heterociclil(R10), -aril(R10) y -heteroaril(R10) cuando se unen a un átomo de carbono; R9 se selecciona del grupo formado por hidrógeno, -(alcoxi C1-8), -NH2, -NH-(alquilo C1-8), -N(alquilo C1-8)2, -C(=O)H, -C(=O)-NH2, -C(=O)-NH-(alquilo C1-8), -C(=O)-N(alquilo C1-8)2, -CO2H, -CO2-(alquilo C1-8), -SO2-(alquilo C1-8), -SO2-NH2, -SO2-NH-(alquilo C1-8), -SO2-N(alquilo C1-8)2, ciano, (halo)1-3, hidroxi, nitro y oxo; R10 es uno a cuatro sustituyentes seleccionados del grupo formado por hidrógeno, alquilo C1-8, -C(=O)H, -C(=O)-(alquilo C1-8), C(=O)-NH2, -C(=O)-NH-(alquilo C1-8), -C(=O)-N(alquilo C1-8)2, -CO2H, -CO2-(alquilo C1-4), -SO2-(alquilo C1-8), -SO2-NH2, -SO2-NH2, -SO2-NH(alquil C1-8) y -SO2N(alquilo C1-8)2 cuando se unen a un átomo de nitrógeno; y, en donde R10 es uno a cuatro sustituyentes seleccionados en forma independiente del grupo formado por hidrógeno, -(alquilo C1-8), -(alcoxi C1-8), -C(=O)H, -C(=O)-(alquilo C1-8), -C(=O)-NH2, -C(=O)-NH-(alquilo C1-8), -C(=O)-N(alquilo C1-8)2, -CO2H, -CO2-(alquilo C1-4), -SO2-(alquilo C1-8), -SO2-NH2, -SO2-NH-(alquilo C1-8)-SO2-N(alquilo C1-8)2, -NH2, -NH-(alquilo C1-8), -N(alquilo C1-8)2, ciano, halo, hidroxi, nitro y oxo cuando se une a un átomo de carbono; R2 se selecciona del grupo formado por hidrógeno, -(alquil C1-8)(R7), -(alquenil C2-8)(R7), -(alquinil C2-8)(R7), -cicloalquil(R8), -heterociclil(R8), -aril(R8) y -heteroaril(R8); y q se selecciona del grupo formado por 0, 1, 2 ó 3; Z se selecciona del grupo formado por hidroxi, -NH2, -NH-(alquilo C1-8), -N(alquilo C1-8)2, O-(alquil C1-8)-OH, -O-(alquil C1-8)(alcoxi C1-8), -O-(alquil C1-8)carbonil(alquilo C1-8), -O-(alquil C1-8)-CO2H, -O-(alquil C1-8)-CO2H, -O-(alquil C1-8)-C(O)O-(alquilo C1-8), -O-(alquil C1-8)-O-C(O)(alquilo C1-8), -O-(alquil C1-8)-NH2, -O-(alquil C1-8)-NH-(alquilo C1-8), -O-(alquil C1-8)-N(alquilo C1-8)2, -O-(alquil C1-8)amida, -O-(alquil C1-8)-C(O)-NH-(alquilo C1-8), -O-(alquil C1-8)-C(O)-N(alquilo C1-8)2, y NHC(O)(alquilo C1-8), y sus sales, mezclas racémicas y enantiómeros aceptables para uso farmacéutico.
ARP030102976A 2002-08-16 2003-08-15 Compuestos de acido piperidinoil carboxilico utiles como antagonistas selectivos del receptor de integrina AR041010A1 (es)

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EP1539739B1 (en) 2010-11-24
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DK1539739T3 (da) 2011-03-07
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NO332036B1 (no) 2012-06-04
SI1539739T1 (sl) 2011-04-29
AU2010236002B2 (en) 2012-05-03
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US20040077684A1 (en) 2004-04-22
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EP1539739A1 (en) 2005-06-15
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BR0313534A (pt) 2005-07-12
CA2496127C (en) 2012-05-29
UA83467C2 (uk) 2008-07-25
CA2496127A1 (en) 2005-02-16
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