AR043820A1 - Derivados de piperidina como moduladores de quimioquinas - Google Patents

Derivados de piperidina como moduladores de quimioquinas

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AR043820A1
AR043820A1 ARP040101100A ARP040101100A AR043820A1 AR 043820 A1 AR043820 A1 AR 043820A1 AR P040101100 A ARP040101100 A AR P040101100A AR P040101100 A ARP040101100 A AR P040101100A AR 043820 A1 AR043820 A1 AR 043820A1
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Argentina
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4alkyl
ring
alkyl groups
attached
hydroxy
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ARP040101100A
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Brian Springthorpe
Moya Caffrey
Chris Luckhurst
Tobias Mochel
Matthew Perry
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Astrazeneca Ab
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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
    • C07D211/36—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 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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    • C07D211/26—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 with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms

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Abstract

Derivados de piperidina, proceso para preparar dicho compuesto y utilización del compuesto tal en el tratamiento de un estado de enfermedad mediado por una quimioquina (tal como CCR3) o H1. Reivindicación 1: Un compuesto caracterizado porque responde a la fórmula (1) donde: Ra y Rb son, en forma independiente, H, o C1-4 alquilo o Ra forma parte de un anillo según se define más adelante; Rc es H o hidroxi; X es CH2, C(O), O, S, SO, S(O)2 o NR3; Z es CHRd(CH2)n; N es 0 o 1; Rd es H, C1-4alquilo, hidroxi, o C1-4alcoxi, R1 es H, C1-6alquilo, arilo o heterociclilo; R2 es arilo o heterociclilo; donde, salvo que se indique de otra manera, las porciones arilo y heterociclilo anteriormente mencionadas se sustituyen opcionalmente por: halógeno, ciano, nitro, hidroxi, oxo, S(O)pR4, OC(O)NR5R6, NR7R8, NR9C(O)R10, NR11C(O)NR12R11, S(O)2NR14R15, NR16S(O)2R17, C(O)NR18R19, C(O)R20, CO2R21, NR22CO2R23, C1-6alquilo, CF3, C1-6alcoxi(C1-6)alquilo, C1-6alcoxi, OCF3, C1-6alcoxi(C1-6)alcoxi, C1-6alquiltio, C2-6 alquenilo, C2-6 alquinilo, C3-10cicloalquilo ( éste mismo opcionalmente sustituido por C1-4alquilo o oxo), metilendioxi, difluorometilendioxi, fenilo, fenil(C1-4)alquilo, fenoxi, feniltio, fenil(C1-4)alcoxi, heterociclilo, heterociclil(C1-4)alquilo, heterocicliloxi o heterociclil(C1-4)alcoxi; donde cualquiera de las porciones fenilo y heterociclilo recién mencionadas se sustituyen opcionalmente con halógeno, hidroxi, nitro, S(O)q(C1-4alquilo), S(O)2NH2, S(O)2NH(C1-4alquilo), S(O)2N(C1-4alquilo)2 (y estos grupos alquilo pueden unirse para formar un anillo como se describe para R5 y R6 más adelante), ciano, C1-4 alquilo, C1-4alcoxi, C(O)NH2, C(O)NH(C1-4alquilo), C(O)N(C1-4alquilo)2 (y estos grupos alquilo pueden unirse para formar un anillo como se describe para R5 y R6 más adelante), CO2H, CO(C1-4alquilo), NHC(O)(C1-4alquilo), NHS(O)2(C1-4alquilo), C(O)(C1-4alquilo), CF3 o OCF3; o Z, R2 y Ra junto con el átomo e C al cual Z y Ra están unidos forman un anillo; p y q son, en forma independiente, 0, 1 o 2; R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R18, R19, R20, R21 y R22 son, en forma independiente, H, C1-6alquilo (opcionalmente sustituido por halógeno, hidroxi o C3-10 cicloalquilo), CH2(C2-6alquenilo), fenilo (este mismo opcionalmente sustituido por halógeno, hidroxi, nitro, NH2, NH(C1-4alquilo), N(C1-4alquilo)2 (y estos grupos alquilo pueden unirse para formar un anillo como se describe para R5 y R6 más adelante), S(O)2(C1-4alquilo), S(O)2NH2, S(O)2NH(C1-4alquilo), S(O)2N(C1-4alquilo)2 (y estos grupos alquilo pueden unirse para formar un anillo como se describe para R5 y R6 más adelante), ciano, C1-4alquilo, C1-4alcoxi, C(O)NH2, C(O)NH(C1-4alquilo), C(O)N(C1-4alquilo)2 (y estos grupos alquilo pueden unirse para formar un anillo como se describe para R5 y R6 más adelante), CO2H, CO2(C1-4alquilo), NHC(O)(C1-4alquilo), NHS(O)2(C1-4alquilo), C(O)(C1-4alquilo), CF3 o OCF3) o heterociclilo (este mismo opcionalmente sustituido por halógeno, hidroxi, nitro, NH2, NH(C1-4alquilo), N(C1-4alquilo)2 (y estos grupos alquilo pueden unirse para formar un anillo como se describe para R5 y R6 más adelante), S(O)2(C1-4alquilo), S(O)2NH2, S(O)2NH(C1-4alquilo), S(O)2N(C1-4alquilo)2 (y estos grupos alquilo pueden unirse para formar un anillo como se describe para R5 y R6 más adelante), ciano, C1-4alquilo, C1-4alcoxi, C(O)NH2, C(O)NH(C1-4alquilo), C(O)N(C1-4alquilo)2 (y estos grupos alquilo pueden unirse para formar un anillo como se describe para R5 y R6 más adelante), CO2H, CO2(C1-4alquilo), NHC(O)(C1-4alquilo), NHS(O)2(C1-4alquilo), C(O)(C1-4alquilo), CF3 o OCF3); como alternativa NR5R6, NR7R8, NR12R13, NR14R15, NR18R19, pueden, en forma independiente, formar un anillo heterocíclico de 4 a 7 miembros, azetidina, pirrolidina, piperidina, azepina, morfolina o piperazina, éste último opcionalmente sustituido por C1-4alquilo en el N distal; R4, R17 y R23 son, en forma independiente, C1-6alquilo (opcionalmente sustituido por halógeno, hidroxi o C3-10cicloalquilo), CH2(C2-6alquenilo), fenilo (este mismo opcionalmente sustituido por halógeno, hidroxi, nitro, NH2, NH(C1-4alquilo), N(C1-4alquilo)2 (y estos grupos alquilo pueden unirse para formar un anillo como se describe para R5 y R6 precedentemente), S(O)2(C1-4alquilo), S(O)2NH2, S(O)2NH(C1-4alquilo), S(O)2N(C1-4alquilo)2 (y estos grupos alquilo pueden unirse para formar un anillo como se describe para R5 y R6 precedentemente), ciano, C1-4alquilo, C1-4alcoxi, C(O)NH2, C(O)NH(C1-4alquilo), C(O)N(C1-4alquilo)2 (y estos grupos alquilo pueden unirse para formar un anillo como se describe para R5 y R6 precedentemente), CO2H, CO2(C1-4alquilo), NHC(O)(C1-4alquilo), NHS(O)2(C1-4alquilo), C(O)(C1-4alquilo), CF3 o OCF3) o heterociclilo ( éste mismo opcionalmente sustituido por halógeno, hidroxi, nitro, NH2, NH(C1-4alquilo), N(C1-4alquilo)2 (y estos grupos alquilo pueden unirse para formar un anillo como se describe para R5 y R6 precedentemente), S(O)2(C1-4alquilo), S(O)2NH2, S(O)2NH(C1-4alquilo), S(O)2N(C1-4alquilo)2 (y estos grupos alquilo pueden unirse para formar un anillo como se describe para R5 y R6 precedentemente), ciano, C1-4alquilo, C1-4alcoxi, C(O)NH2, C(O)NH(C1-4alquilo), C(O)N(C1-4alquilo)2 (y estos grupos alquilo pueden unirse para formar un anillo como se describe para R5 y R6 precedentemente), CO2H, CO2(C1-4alquilo), NHC(O)(C1-4alquilo), NHS(O)2(C1-4alquilo), C(O)(C1-4alquilo), CF3 o OCF3); R3 es H, C1-6alquilo o bencilo; o un N-óxido del mismo; o una sal aceptable para uso farmacéutico del mismo; o un solvato del mismo.
ARP040101100A 2003-04-01 2004-04-01 Derivados de piperidina como moduladores de quimioquinas AR043820A1 (es)

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MXPA05010374A (es) 2005-11-17
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US20070032523A1 (en) 2007-02-08
UY28248A1 (es) 2004-11-08
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IS8089A (is) 2005-10-25
RU2005128793A (ru) 2006-05-10
EP1620400A1 (en) 2006-02-01
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UA81014C2 (en) 2007-11-26
US7495013B2 (en) 2009-02-24
MY135396A (en) 2008-04-30
KR20050108419A (ko) 2005-11-16
AU2004226010A1 (en) 2004-10-14
CL2004000677A1 (es) 2005-04-22
CN1768037A (zh) 2006-05-03
SE0300957D0 (sv) 2003-04-01
TW200505857A (en) 2005-02-16
ES2398462T3 (es) 2013-03-19
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CO5611151A2 (es) 2006-02-28
AU2004226010B2 (en) 2007-06-07
CN100460391C (zh) 2009-02-11

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