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AR033517A1 - Derivados de piperidina, proceso para su preparacion y uso de estos derivados en la fabricacion de medicamentos - Google Patents

Derivados de piperidina, proceso para su preparacion y uso de estos derivados en la fabricacion de medicamentos

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Publication number
AR033517A1
AR033517A1 ARP010101549A ARP010101549A AR033517A1 AR 033517 A1 AR033517 A1 AR 033517A1 AR P010101549 A ARP010101549 A AR P010101549A AR P010101549 A ARP010101549 A AR P010101549A AR 033517 A1 AR033517 A1 AR 033517A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
halogen
alkoxy
itself optionally
Prior art date
Application number
ARP010101549A
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English (en)
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Astrazeneca Ab
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Publication date
Priority claimed from GB0008626A external-priority patent/GB0008626D0/en
Priority claimed from GB0019111A external-priority patent/GB0019111D0/en
Priority claimed from SE0003664A external-priority patent/SE0003664D0/xx
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR033517A1 publication Critical patent/AR033517A1/es

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Abstract

Derivados de piperidina que tiene la formula 1 en donde: q, s y t son independientemente 0 o 1; n y r son independientemente, 0, 1, 2, 3, 4 o 5; m y p son independientemente , 0, 1 o 2; X es CH2, C(O), O, S, S(O), S(O)2 o NR37; siempre que cuando m y p son ambos 1 entonces X no es CH2; Y es NHR2 u OH; T es C(O), C(S), S(O)2 o CH2; R1 es hidrogeno, alquilo C1-6, arilo o heterociclilo; R2 y R47 son, independientemente, hidrogeno, alquilo C1-6, aril-alquilo (C1-4) o CO(alquilo C1-6); R3 es alquilo C1-6 (opcionalmente sustituido con halogeno, CO2R4 o ftalimida), CR3aR3bR3c, alquenilo C2-4 (opcionalmente sustituido con arilo o heterociclilo), cicloalquilo C3-7 (opcionalmente sustituido con alquilo C1-4, arilo u oxo), cicloalquenilo C3-7 (opcionalmente sustituido con oxo, alquilo C1-6 o arilo), arilo, heterociclilo, tioarilo o tioheterociclilo; R3a es hidrogeno, alquilo C1-6, alcoxi C1-6 o cicloalquilo C3-7; R3b es arilo, heterociclilo, S(O)2arilo o S(O)2heterociclilo, y R3c es alquilo C1-6, haloalquilo C1-4, hidroxi, heterociclil(alquilo C1-4) o arilo; en donde, a menos que se declare de otra forma, las porciones arilo y heteroaciclilo mencionadas anteriormente están opcionalmente sustituidas con halogeno, OH, SH, NO2, oxo, alquilo C1-6 (en sí opcionalmente sustituido con halogeno, OC(O)alquilo C1-6, S(O)2R48, fenilo (en sí opcionalmente sustituido con halogeno (tal como uno o dos átomos de cloro o fluor), alquilo C1-6 S(O)2R38 o C(O)NR39R40), naftiloxi (en sí opcionalmente sustituido con halo o alquenilo C2-6), cicloalquilo C3-10 (en sí opcionalmente sustituido con alquilo C1-4 u oxo), o NR41C(O)OCH2(fluoren-9-ilo)), NR41 C(O)OCH2(fluoren-9-ilo), alcoxi C1-6 (en sí opcionalmente sustituido con halogeno, alcoxi C1-6, NHCO2(alquiloC1-6), CO2R4, NR5R6 o fenilo (en sí opcionalmente sustituido con halogeno o NO2)), alquiltio C1-6, haloalquiltio C1-6, cicloalquilo C3-10, NR7R8, NR9C(O)R10, CO2R11, C(O)NR12R13, C(O)R14, S(O)dR15, S(O)2NR42R43, NR44S(O)2R45, fenilo (en si opcionalmente sustituido con halogeno, alquilo C1-6, haloalquilo C1-6, CN, NO2, alcoxi C1-6 (en sí opcionalmente sustituido con halogeno, OH o piridinilo), fenilo (en sí opcionalmente sustituido con halogeno, alquilo C1-6 haloalquilo C1-6, CN, NO2, alcoxi C1-6 o haloalcoxi C1-6) o heterociclilo (en sí opcionalmente sustituido con halogeno, alquilo C1-6, haloalquilo C1-6, CN, NO2, alcoxi C1-6 o haloalcoxi C1-6), heterociclilo (en sí opcionalmente sustituido con halogeno, alquilo C1-6, haloalquilo C1-6, CN, NO2, alcoxi C1-6, haloalcoxi C1-6, fenilo (en sí opcionalmente sustituido con halogeno, alquilo C1-6, haloalquilo C1-6, NO2, alcoxi C1-6 o haloalcoxi C1-6) o heterociclilo (en sí opcionalmente sustituido con halogeno, alquilo C1-6, haloalquilo C1-6, CN, NO2, alcoxi C1-6 o haloalcoxi C1-6), fenoxi (en sí opcionalmente sustituido con halogeno, alquilo C1-6, haloalquilo C1-6, CN, NO2, alcoxi C1-6, haloalcoxi C1-6, fenilo (en sí opcionalmente sustituido con halogeno, alquilo C1-6, haloalquilo C1-6, CN, NO2, alcoxi C1-6 o haloalcoxi C1-6) o heterociclilo (en sí opcionalmente sustituido con halogeno, alquilo C1-6, haloalquilo C1-6, CN, NO2, alcoxi C1-6 o haloalcoxi C1-6), SCN, CN, SO3H(o una sal metálica alcalina del mismo), metilendioxi o difluormetilendioxi; cuando arilo es fenilo pueden unirse sustituyentes adyacentes para formar, junto con el anillo fenilo al cual están unidos, una porcion dihidrofenantreno; d es 0, 1 o 2; R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R37, R39, R40, R41, R42, R43 y R44 son, independientemente, hidrogeno, alquilo C1-6, arilo (en sí opcionalmente sustituido con halogeno, alquilo C1-6, haloalquilo C1-6, CN, NO2, alcoxi C1-6 o haloalcoxi C1-6) o heterociclilo (en sí opcionalmente sustituido con halogeno, alquilo C1-6, haloalquilo C1-6, CN, NO2, alcoxi C1-6 o haloalcoxi C1-6); R15, R38 y R48 son, independientemente, alquilo C1-6 (opcionalmente sustituido con halogeno, hidroxi o cicloalquilo C3-10), alquenilo C3-6, arilo (en sí opcionalmente sustituido con halogeno, alquilo C1-6, haloalquilo C1-6, CN, NO2, alcoxi C1-6 o haloalcoxi C1-6) o heterociclilo (en sí opcionalmente sustituido con halogeno, alquilo C1-6, haloalquilo C1-6, CN, NO2, alcoxi C1-6 o haloalcoxi C1-6); o un N-oxido del mismo; o una sal farmacéuticamente aceptable del mismo; o un solvato del mismo siempre que: cuando m y p son ambos 1, n, q y r son todos O; T y X son ambos S(O)2 y R1 es metoxifenilo, entonces R3 no es propilo; cuando m, p, q y r son todos 1, n es 0, Y es NH2, T es CO y R1X es (CH3)2N, entonces R3 no es 3,5-dibromo-4-aminofenilo, 1-metilindol-3-ilo o 1-(ter-butoxicarbonil)indol-3-ilo; y cuando m y p son ambos 1, n q y r son todos 0, T es CO, X es NH y R1 es 3-(4-fluorbencil)bencimidazol-2-ilo, entonces R3 no es 4-fluorfenilo; proceso para la preparacion de dicho compuesto, y usos de dichos compuestos para la fabricacion de medicamentos, en especial de medicamentos para el uso en la modulacion de la actividad del receptor de quimioquina o en la actividad antagonizante de H1, o de un estado de enfermedad mediado por CCR3.
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EP1493743B1 (en) 2008-09-03
DE60111734T2 (de) 2006-05-04
US20040014783A1 (en) 2004-01-22
CA2403012A1 (en) 2001-10-18
EP1493743A1 (en) 2005-01-05
ATE298748T1 (de) 2005-07-15
NO20024774D0 (no) 2002-10-03

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