AR037351A1 - Derivados de piperidina, proceso para preparar estos compuestos, composicion farmaceutica, uso de estos compuestos para la manufactura de un medicamento util para el tratamiento de una enfermedad mediada por ccr5 (tal como artritis reumatoidea) y compuestos intermediarios - Google Patents

Derivados de piperidina, proceso para preparar estos compuestos, composicion farmaceutica, uso de estos compuestos para la manufactura de un medicamento util para el tratamiento de una enfermedad mediada por ccr5 (tal como artritis reumatoidea) y compuestos intermediarios

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AR037351A1
AR037351A1 ARP020104333A ARP020104333A AR037351A1 AR 037351 A1 AR037351 A1 AR 037351A1 AR P020104333 A ARP020104333 A AR P020104333A AR P020104333 A ARP020104333 A AR P020104333A AR 037351 A1 AR037351 A1 AR 037351A1
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Argentina
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alkyl
optionally substituted
halo
alkoxy
cyano
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ARP020104333A
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Astrazeneca Ab
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    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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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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Abstract

Un derivado heterocíclico que tiene la fórmula (1), en la cual: L es CH ó N; M es CH ó N; siempre que L y M no sean CH en ambos casos; R1 es hidrógeno, alquilo C1-6 [optativamente sustituido con fenilo {que a su vez está optativamente sustituido con halo, alquilo C1-4, alcoxi C1-4, ciano, nitro, CF3, OCF3, (alquilo C1-4)C(O)NH, S(O)2NH2, alquiltio C1-4, S(O)(alquilo C1-4) ó S(O)2(alquilo C1-4)} ó heteroarilo {que a su vez está optativamente sustituido con halo, alquilo C1-4, alcoxi C1-4, ciano, nitro, CF3, (alquilo C1-4)C(O)NH, S(O)2NH2, alquiltio C1-4, S(O)(alquilo C1-4) ó S(O)2(alquilo C1-4)}], fenilo {optativamente sustituido con halo, alquilo C1-4, alcoxi C1-4, ciano, nitro, CF3, OCF3, (alquilo C1-4)C(O)NH, S(O)2NH2, alquiltio C1-4, S(O)(alquilo C1-4) ó S(O)2(alquilo C1-4)}, heteroarilo {optativamente sustituido con halo alquilo C1-4, alcoxi C1-4, ciano, nitro, CF3, (alquilo C1-4)C(O)NH, S(O)2NH2, alquiltio C1-4, S(O)(alquilo C1-4) ó S(O)2(alquilo C1-4)}, S(O)2R6, S(O)2NR10R11, C(O)R7, C(O)2(alquilo C1-6), C(O)2(fenil(alquilo C1-2)) ó C(O)NHR7 y cuando M es CH, R1 también puede ser NHS(O)2R6, NHS(O)2NHR7, NHC(O)R7 ó NHC(O)NHR7; R2 es fenilo o heteroarilo, cualquiera de los cuales está optativamente sustituido con halo, alquilo C1-4, alcoxi C1-4, S(O)n(alquilo C1-4), nitro, ciano ó CF3; R3 es hidrógeno o alquilo C1-4; R4 es hidrógeno, metilo, etilo, alilo ó ciclopropilo; R5 es fenilo, heteroarilo, fenil-NH, heteroaril-NH, fenilalquilo C1-2, heteroarilalquilo C1-2, fenil (alquil C1-2)-NH ó heteroaril (alquil C1-2)NH, donde los anillos de fenilo y heteroarilo de R5 están optativamente sustituidos con halo, ciano, nitro, hidroxi, alquilo C1-4, alcoxi C1-4, S(O)k(alquilo C1-4), S(O)2NR8R9, NHS(O)2(alquilo C1-4), NH2, NH(alquilo C1-4), N(alquilo C1-4)2, NHC(O)NH2, C(O)NH2, C(O)NH(alquilo C1-4), NHC(O)(alquilo C1-4), CO2H, CO2(alquilo C1-4), C(O)(alquilo C1-4), CF3, CHF2, CH2F, CH2CF3 ó OCF3; k, m y n representan independientemente 0, 1 ó 2; R6 es alquilo C1-6 [optativamente sustituido con halo, alcoxi C1-4, fenilo {que a su vez está optativamente sustituido con halo, alquilo C1-4, alcoxi C1-4, ciano, nitro, CF3, OCF3, (alquilo C1-4)C(O)NH, S(O)2NH2, alquiltio C1-4, S(O)(alquilo C1-4) ó S(O)2(alquilo C1-4)} ó heteroarilo {que a su vez está optativamente sustituido con halo, alquilo C1-4, alcoxi C1-4, ciano, nitro, CF3, (alquilo C1-4)C(O)NH, S(O)2NH2, alquiltio C1-4, S(O)(alquilo C1-4) ó S(O)2(alquilo C1-4)}], cicloalquilo C3-7, piranilo, fenilo {optativamente sustituido con halo, alquilo C1-4, alcoxi C1-4, ciano, nitro, CF3, OCF3, (alquilo C1-4)C(O)NH, S(O)2NH2, alquiltio C1-4, S(O)(alquilo C1-4) ó S(O)2(alquilo C1-4)} ó heteroarilo { optativamente sustituido con halo, alquilo C1-4, alcoxi C1-4, ciano, nitro, CF3, (alquilo C1-4)C(O)NH, S(O)2NH2, alquiltio C1-4, S(O)(alquilo C1-4) ó S(O)2(alquilo C1-4)}, R7 es hidrógeno, alquilo C1-6 [optativamente sustituido con halo, alcoxi C1-4, fenilo {que a su vez está optativamente sustituido con halo, alquilo C1-4, alcoxi C1-4, ciano, nitro, CF3, OCF3, (alquilo C1-4)C(O)NH, S(O)2NH2, alquiltio C1-4, S(O)(alquilo C1-4) ó S(O)2(alquilo C1-4)} ó heteroarilo{que a su vez está optativamente sustituido con halo, alquilo C1-4, alcoxi C1-4, ciano, nitro, CF3, (alquilo C1-4)C(O)NH, S(O)2NH2, alquiltio C1-4, S(O)(alquilo C1-4) ó S(O)2(alquilo C1-4)}], cicloalquilo C3-7, piranilo, fenilo {optativamente sustituido con halo, alquilo C1-4, alcoxi C1-4, ciano, nitro, CF3, OCF3, (alquilo C1-4)C(O)NH, S(O)2NH2, alquiltio C1-4, S(O)(alquilo C1-4) ó S(O)2(alquilo C1-4)} ó heteroarilo {optativamente sustituido con halo, alquilo C1-4, alcoxi C1-4, ciano, nitro, CF3, (alquilo C1-4)C(O)NH, S(O)2NH2, alquiltio C1-4, S(O)(alquilo C1-4) ó S(O)2(alquilo C1-4}; R8 y R9 son, independientemente, hidrógeno ó alquilo C1-4 ó, junto con un átomo de nitrógeno u oxígeno, pueden unirse para formar un anillo de 5 ó 6 miembros que está optativamente sustituido con alquilo C1-4, C(O)H ó C(O)(alquilo C1-4); R10 y R11 son, independientemente, hidrógeno ó alquilo C1-4, ó se pueden unir para formar un anillo de 5 ó 6 miembros que está optativamente sustituido con alquilo C1-4 o fenilo (donde el anillo de fenilo está optativamente sustituido con halo, ciano, nitro, hidroxi, alquilo C1-4, alcoxi C1-4, S(O)m alquilo C1-4, S(O)2NH2, S(O)2NH(alquilo C1-4), S(O)2N(alquilo C1-4)2, NHS(O)2 (alquilo C1-4), NH2, NH(alquilo C1-4), N(alquilo C1-4)2, NHC(O)NH2, C(O)NH2, C(O)NH(alquilo C1-4), NHC(O)(alquilo C1-4), CO2H, CO2(alquilo C1-4, C(O)(alquilo C1-4), CF3, CHF2, CH2F, CH2CF3 ó OCF3); ó una sal farmacéuticamente aceptable del mismo o un solvato del mismo; siempre que cuando R1 es hidrógeno o alquilo no sustituido, R4 es hidrógeno, metilo o etilo; L es CH y M es N, luego la porción fenilo o heteroarilo de R5 está sustituida con uno de los siguientes: S(O)k(alquilo C1-4), NHC(O)NH2, C(O)(alquilo C1-4), CHF2, CH2F, CH2CF3 ó OCF3; y optativamente también está sustituido con uno o más de halo, ciano, nitro, hidroxi, alquilo C1-4, alcoxi C1-4, S(O)k alquilo C1-4, S(O)2NR8R9, NHS(O)2(alquilo C1-4), NH2, NH(alquilo C1-4), N(alquilo C1-4)2, NHC(O)NH2, C(O)NH2, C(O)NH(alquilo C1-4), NHC(O)(alquilo C1-4), CO2H, CO2(alquilo C1-4), C(O)(alquilo C1-4), CF3, CHF2, CH2F, CH2CF3 ó OCF3. Proceso para preparar estos compuestos, composición farmacéutica, uso de estos compuestos para la manufactura de un medicamento útil para el tratamiento de una enfermedad mediada por CCR5 (tal como artritis reumatoidea), y compuestos intermediarios útiles en la preparación de los compuestos de fórmula (1).
ARP020104333A 2001-11-15 2002-11-12 Derivados de piperidina, proceso para preparar estos compuestos, composicion farmaceutica, uso de estos compuestos para la manufactura de un medicamento util para el tratamiento de una enfermedad mediada por ccr5 (tal como artritis reumatoidea) y compuestos intermediarios AR037351A1 (es)

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AR037351A1 true AR037351A1 (es) 2004-11-03

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US (2) US7192973B2 (es)
EP (1) EP1448548A1 (es)
JP (1) JP4459622B2 (es)
KR (1) KR20050044470A (es)
CN (1) CN100398535C (es)
AR (1) AR037351A1 (es)
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IS7256A (is) 2004-05-10
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