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AR064414A1 - Derivados de 1-azoniabiciclo[2, 2, 2]octano y 1-azabiciclo[2, 2, 2]oct-3-ilo, un proceso para su preparacion, una composicion farmaceutica que los comprende, procedimiento de obtencion de la misma, su uso en la elaboracion de un medicamento para el tratamiento de epoc y un producto farmaceutico que - Google Patents

Derivados de 1-azoniabiciclo[2, 2, 2]octano y 1-azabiciclo[2, 2, 2]oct-3-ilo, un proceso para su preparacion, una composicion farmaceutica que los comprende, procedimiento de obtencion de la misma, su uso en la elaboracion de un medicamento para el tratamiento de epoc y un producto farmaceutico que

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Publication number
AR064414A1
AR064414A1 ARP070105689A ARP070105689A AR064414A1 AR 064414 A1 AR064414 A1 AR 064414A1 AR P070105689 A ARP070105689 A AR P070105689A AR P070105689 A ARP070105689 A AR P070105689A AR 064414 A1 AR064414 A1 AR 064414A1
Authority
AR
Argentina
Prior art keywords
alkyl
halogen
formula
hydroxyl
optionally
Prior art date
Application number
ARP070105689A
Other languages
English (en)
Inventor
Antonio Mete
Rhonan Ford
Ian Millichip
Barry Teobald
Original Assignee
Astrazeneca Ab
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39166793&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR064414(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR064414A1 publication Critical patent/AR064414A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
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  • Gynecology & Obstetrics (AREA)

Abstract

Un proceso para su preparacion, composiciones farmacéuticas que contienen a los mismos, un proceso para preparar composiciones farmacéuticas, su uso en terapias e intermediarios de utilidad en su preparacion. Reivindicacion 1: Un compuesto, caracterizado porque es de la formula (1), en donde R1 representa alquilo C1-6; R2 representa fenilo o un anillo heteroarilo de 5 a 6 miembros, cada uno de los cuales se puede sustituir opcionalmente con uno o más sustituyentes seleccionados en forma independiente entre halogeno, ciano, nitro, SH, S(O)0-2R10, NR11R12, S(O)2NR13R14, C(O)NR15R16, C(O)2R17, NR18S(O)2R19, NR20C(O)R21, NR22C(O)2R23, NR24C(O)NR25R26, OR27 y alquilo C1-6 donde alquilo C1-6 se puede sustituir opcionalmente con uno o más sustituyentes seleccionados en forma independiente entre halogeno, hidroxilo, alcoxi C1-6, NH2, NH(alquilo C1-6) y N(alquil C1-6)2; R3 y R4 junto con el átomo de nitrogeno al cual ambos se encuentran unidos forman un anillo heterocíclico alifático de 4 a 8 miembros el cual puede contener opcionalmente un heteroátomo adicional seleccionado entre oxigeno, azufre y nitrogeno, y donde el anillo heterocíclico se puede sustituir opcionalmente con uno o más sustituyentes seleccionados en forma independiente entre halogeno, hidroxilo y alquilo C1-6, donde alquilo C1-6 se puede sustituir opcionalmente con uno o más sustituyentes seleccionados en forma independiente entre halogeno e hidroxilo; R5 representa un grupo de la formula (2) o (3) en donde Y es -CH2-, -CH2CH2- o -CH2CH2CH2- y la sustitucion sobre el anillo en grupo (2) puede ser en las posiciones 3 o 4; a es 1 o 2; b es 1 o 2; Z es -CH2-; R6 representa un grupo de la formula (4), en donde w es 0 o 1; R7 representa alquileno C1-4 opcionalmente sustituido con uno o más sustituyentes seleccionados en forma independiente entre halogeno, hidroxilo, alcoxi C1-6, NH2, NH(alquilo C1-6) y N(alquilo C1-6)2; cuando w es 0, y es 0; cuando w es 1, y es 0 o 1; Q representa O, C(O), S(O)0-2, NR9, -CONR9-, -SO2NR9-, -NR9CO-, -NR9SO2, -OC(O)-, -C(O)O-, -HC=CH- o etinileno; R8 representa un grupo cíclico Cic1 o un grupo alquilo C1-4 donde alquilo C1-4 se puede sustituir opcionalmente con uno o más sustituyentes seleccionados en forma independiente entre halogeno, hidroxilo, alcoxi C1-4, NH2, NH(alquilo C1-4), N(alquilo C1-4)2, un grupo cíclico Cic2 y OCic2; y R8 pueden representar adicionalmente hidrogeno cuando Q representa O, NR9, CONR9-, -SO2NR9-, - C(O)O-, -HC=CH- o etinileno; Cic1 y Cic2 cada uno en forma independiente representan arilo, heteroarilo, un anillo carbocíclico alifático de 3 a 8 miembros o un anillo heterocíclico alifático de 4 a 8 miembros, cada uno de los cuales se puede sustituir opcionalmente con uno o más sustituyentes seleccionados en forma independiente entre halogeno, ciano, nitro, SH, S(O)0-2R10, NR11R12, S(O)2NR13R14, C(O)NR15R16, C(O)2R11, NR18S(O)2R19, NR20C(O)R21, NR22C(O)2R23, NR24C(O)NR25R26, OR27, fenilo, heteroarilo y alquilo C1-6 donde fenilo, heteroarilo o alquilo C1-6 se puede sustituir opcionalmente con uno o más sustituyentes seleccionados en forma independiente entre halogeno, hidroxilo, ciano, alcoxi C1-6, NH2, NH(alquilo C1-6) y N(alquilo C1-6)2; R9 representa hidrogeno o alquilo C1-6; R10 y R19 cada uno en forma independiente representan alquilo C1-6, donde alquilo C1-6 se puede sustituir opcionalmente con uno o más sustituyentes seleccionados en forma independiente entre halogeno, hidroxilo, alcoxi C1-6, NH2, NH(alquilo C1-6) y N(alquil C1-6)2; y R11, R12, R13, R14, R15, R16, R17, R18, R20, R21, R22, R23, R24, R25, R26 y R27 cada uno en forma independiente representa hidrogeno o alquilo C1-6, donde alquilo C1-6 se puede sustituir opcionalmente con uno o más sustituyentes seleccionados en forma independiente entre halogeno, hidroxilo, alcoxi C1-6, NH2, NH(alquilo C1-6) y N(alquilo C1-6)2; o cualquiera de R11 y R12, R13 y R14, R15 y R16 o R25 y R26, junto con el átomo de nitrogeno al cual ambos se encuentran unidos, pueden formar un anillo heterocíclico alifático de 4 a 8 miembros, donde el anillo heterocíclico se puede sustituir opcionalmente con uno o más sustituyentes seleccionados en forma independiente entre halogeno, hidroxilo y alquilo C1-6, donde alquilo C1-6 se puede sustituir opcionalmente con uno o más sustituyentes seleccionados en forma independiente entre halogeno e hidroxilo; y X representa un anion aceptable para uso farmacéutico de un ácido mono o polivalente. Reivindicacion 10: Un proceso para preparar un compuesto de la formula (1) segun se definio en la cláusula 1, caracterizado porque comprende hacer reaccionar un compuesto de la formula (10) en donde R1, R2 y R3 tienen los valores que se definen en la formula (1), o un alquiléster C1-6, anhídrido ácido o haluro ácido del mismo, con un compuesto de la formula (11) o de la formula (12), en donde Y, Z, a y b son como se definieron en la formula (1) y el grupo hidroxilo en (11) se encuentra en la posicion 3 o 4 para obtener un compuesto de la formula (5S) o (5b) en donde R1, R2 y R3 son como se definieron en la cláusula 1 y posteriormente hacer reaccionar (5a) o (5b) con un compuesto R6-LG (13), en donde LG es un grupo saliente y R6 es como se definio en la formula (1): y opcionalmente convertir el compuesto en otro compuesto de la formula (1); formar una sal aceptable para uso farmacéutico con un anion de un ácido mono o polivalente.
ARP070105689A 2006-12-19 2007-12-18 Derivados de 1-azoniabiciclo[2, 2, 2]octano y 1-azabiciclo[2, 2, 2]oct-3-ilo, un proceso para su preparacion, una composicion farmaceutica que los comprende, procedimiento de obtencion de la misma, su uso en la elaboracion de un medicamento para el tratamiento de epoc y un producto farmaceutico que AR064414A1 (es)

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