AR052330A1 - Derivados de adamantano que comprenden quinoleinas sustituidas - Google Patents

Derivados de adamantano que comprenden quinoleinas sustituidas

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Publication number
AR052330A1
AR052330A1 ARP050104990A ARP050104990A AR052330A1 AR 052330 A1 AR052330 A1 AR 052330A1 AR P050104990 A ARP050104990 A AR P050104990A AR P050104990 A ARP050104990 A AR P050104990A AR 052330 A1 AR052330 A1 AR 052330A1
Authority
AR
Argentina
Prior art keywords
halogen
optionally substituted
represent
substituent
heterocyclic ring
Prior art date
Application number
ARP050104990A
Other languages
English (en)
Inventor
Richard Evans
Rhonan Ford
Toby Thompson
Paul Willis
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
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR052330A1 publication Critical patent/AR052330A1/es

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    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/38—Nitrogen atoms
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D215/14—Radicals substituted by oxygen atoms
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    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Health & Medical Sciences (AREA)
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  • Hematology (AREA)
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Abstract

Procesos para su preparacion; composiciones farmacéuticas que los contienen; y su uso en terapia. Reivindicacion 1: Un compuesto caracterizado porque responda a la formula (1), o una sal aceptable para uso farmacéutico o un éster hidrolizable en vivo del mismo, donde: n representa 1, 2 o 3; cada R1 representa en forma independiente hidrogeno, hidroxi o un halogeno; A es C(O)NH o NHC(O); p es 0, 1 o 2; cada R2 representa en forma independiente halogeno o alquilo C1-6 opcionalmente sustituido por al menos un sustituyente seleccionado en forma independiente entre oxidrilo, halogeno y alcoxi C1-6; q es 0, 1 o 2; cada R4 representa en forma independiente halogeno o alquilo C1-6 opcionalmente sustituido por al menos un sustituyente seleccionado en forma independiente entre oxidrilo, halogeno y alcoxi C1-6; R3 representa un grupo Y1R6 o Z1R10; R6 representa un grupo R8 o un anillo carbocíclico o heterocíclico de 4 a 9 miembros, donde dicho anillo carbocíclico o heterocíclico está sustituido por al menos un sustituyente seleccionado en forma independiente entre Y2R9 y Z2R11, y donde dicho anillo carbocíclico o heterocíclico de 4 a 9 miembros puede estar además opcionalmente sustituido por al menos un sustituyente seleccionado en forma independiente entre halogeno, oxidrilo, alcoxi C1-6, alquilo C1-6, fenilo y un anillo heteroaromático de 5 o 6 miembros, donde dicho alquilo C1-6, fenilo o anillo heteroaromático de 5 o 6 miembros puede estar opcionalmente sustituido por al menos un sustituyente seleccionado entre halogeno, oxidrilo y alcoxi C1-6; R8 y R9 representa cada uno en forma independiente tetrazolilo, 1,2,3-triazolilo, 1,2,4-triazolilo o un anillo heterocíclico de 5 o 6 miembros que comprende entre 1 y 4 heteroátomos seleccionados en forma independiente entre nitrogeno, oxígeno y azufre, donde el anillo heterocíclico está sustituido por al menos un sustituyente seleccionado entre oxidrilo, =O y =S, y donde el anillo heterocíclico puede estar además opcionalmente sustituido por al menos un sustituyente seleccionado entre halogeno, nitro, amino, ciano, alquilsulfonilo C1-6, alcoxicarbonilo C1-6 y un grupo alquilo C1-6 en donde dicho grupo alquilo C1-6 puede estar opcionalmente sustituido por al menos un sustituyente seleccionado entre halogeno, oxidrilo y amino; R10 y R11 representa cada uno en forma independiente carboxilo, alquilsulfonilaminocarbonilo C1-6, C(O)NHOH o NHR12; R12 representa CN, alquilsulfonilo C1-6, alquilcarbonilo C1-6, alcoxicarbonilo C1-6, alquilaminosulfonilo C1-6 o di-alquilaminosulfoniloC1-6; Y1 e Y2 representa cada uno en forma independiente un enlace, O, S(O)0-2, NR7C(O), C(O)NR7, SO2NR7, NR7SO2, >NR7, O(CH2)1-6, S(O)0-2(CH2)1-6, NR7(CH2)1-6, (CH2) 1-3O(CH2)1-3, (CH2)1 3S(O)0-2(CH2)1-3, (CH2)1-3NR7(CH2)1-3, (CH2)1-3NR7C(O)(CH2)0-3, (CH2)1-3C(O)NR7(CH2)0-3, S(O)0-2(CH2) 1-6NR7 o a alquileno C1-6 en donde dicho alquileno C1-6 puede estar opcionalmente sustituido por al menos un sustituyente seleccionado en forma independiente entre oxidrilo, halogeno y alcoxi C1-6; Z1 y Z2 representa cada uno en forma independiente un enlace, O(CH2)1-6, S(O)0-2(CH2)1-6, NR7(CH2)1-6, (CH2)1-3O(CH2)1-3, (CH2)1-3S(O)0-2(CH2)1-3, (CH2)1- 3NR7(CH2)1-3, (CH2) 1-3NR7C(O)(CH2)1-3 , (CH2)1-3C(O)NR7(CH2)1-3 o a alquileno C1-6 en donde dicho alquileno C1-6 puede estar opcionalmente sustituido por al menos un sustituyente seleccionado en forma independiente entre oxidrilo, halogeno y alcoxi C1-6; y cada R7 representa en forma independiente hidrogeno o un grupo alquilo C1-6 que puede estar opcionalmente sustituido por al menos un sustituyente seleccionado en forma independiente entre oxidrilo, halogeno y alcoxi C1-6; con las siguientes salvedades: a) cuando R3 representa Y1R6 e Y1 representa NR7(CH2)1-6, S(CH2)1-6, O(CH2)1-6 o un alquileno C1-6 opcionalmente sustituido, entonces R6 no representa oxopirrolidinilo; b) cuando R3 representa Z1R10 y Z1 representa (CH2)1-3NR7(CH2)1-3, entonces R10 no representa carboxilo; c) cuando R3 representa Y1R6 e Y1 representa (CH2)1-3NR7(CH2)1-3 y R6 representa un grupo R8 entonces R8 no representa un anillo heterocíclico de 5 o 6 miembros sustituido con oxidrilo o =O; d) cuando R3 representa Y1R6 e Y1 representa (CH2)1-3NR7(CH2)1-3 y R6 representa un anillo carbocíclico o heterocíclico de 4 a 9 miembros sustituido con Z2R11 y Z2 representa un enlace, entonces R11 no representa carboxilo; e) cuando R3 representa Y1R6 e Y1 representa NR7(CH2)1-6, S(CH2)1-6, O(CH2)1-6 o un alquileno C1-6 opcionalmente sustituido y R6 representa fenilo sustituido con Z2R11 y Z2 representa un enlace, entonces R11 no representa alquilsulfonilamino C1-6; f) cuando R3 representa Z1R10 y Z1 representa O(CH2)1-6, S(CH2)1-6, NR7(CH2)1-6 o un alquileno C1-6 opcionalmente sustituido y R10 representa NHR12, entonces R12 no representa alquilcarbonilo C1-6; y g) el compuesto no se selecciona entre tert-butilo 1-{5-[(1-adamantilacetil)]-6- metilquinolin-2-il}piperidin-4-ilcarbamato y tert-butilo (3S)-1-{5-[(1-adamantilacetil) amino]-6-metilquinolin-2-il}pirrolidin-3-ilcarbamato.
ARP050104990A 2004-11-30 2005-11-29 Derivados de adamantano que comprenden quinoleinas sustituidas AR052330A1 (es)

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