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AR087710A1 - Inhibidores de la quinurenina-3-monooxigenasa, sus composiciones farmaceuticas y metodos para su uso - Google Patents

Inhibidores de la quinurenina-3-monooxigenasa, sus composiciones farmaceuticas y metodos para su uso

Info

Publication number
AR087710A1
AR087710A1 ARP120103185A ARP120103185A AR087710A1 AR 087710 A1 AR087710 A1 AR 087710A1 AR P120103185 A ARP120103185 A AR P120103185A AR P120103185 A ARP120103185 A AR P120103185A AR 087710 A1 AR087710 A1 AR 087710A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
hydrogen
lower alkyl
chemical entity
pyrimidin
Prior art date
Application number
ARP120103185A
Other languages
English (en)
Original Assignee
Chdi Foundation Inc
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 Chdi Foundation Inc filed Critical Chdi Foundation Inc
Publication of AR087710A1 publication Critical patent/AR087710A1/es

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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Abstract

En la presente se proporcionan ciertas entidades químicas. También se proporcionan composiciones farmacéuticas que comprenden al menos una entidad química y uno o más vehículos farmacéuticamente aceptables. Se describen métodos para tratar pacientes que padecen ciertas enfermedades y trastornos que responden a la inhibición de la actividad KMO, que comprenden administrar a dichos pacientes una cantidad de al menos una entidad química eficaz para reducir las señales o los síntomas de la enfermedad o trastorno. Estas enfermedades incluyen trastornos neurodegenerativos, tales como la enfermedad de Huntington. También se describen métodos de tratamiento que incluyen administrar al menos una entidad química como único agente activo, o administrar al menos una entidad química en combinación con uno o más agentes terapéuticos distintos. También se proporcionan métodos para seleccionar compuestos capaces de inhibir la actividad KMO. Reivindicación 1: Al menos una entidad química seleccionada de los compuestos de fórmula (1) y sus sales y profármacos farmacéuticamente aceptables, en la que: X e Y se seleccionan independientemente de -N- y -CH-, con la condición de que al menos uno de X e Y es -N-; R¹ es arilo, o heteroarilo monocíclico, cada uno de los cuales está sustituido con un primer grupo de fórmula -Z-R⁶-, en la que Z se selecciona de -O-, -S-, -S(O)-, -S(O)₂-, -CR¹¹R¹²-, -OCR¹¹R¹²-, -NR¹³-, -NR¹³CR¹¹R¹²-, -CR¹¹R¹²NR¹³-, y -C(O)-, en la que R¹¹, R¹², y R¹³ se seleccionan independientemente de hidrógeno, alquilo inferior, hidroxilo, y alcoxi inferior; R⁶ se selecciona de hidrógeno, alquilo C₁₋₆ opcionalmente sustituido, cicloalquilo opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, y heterocicloalquilo opcionalmente sustituido, con la condición de que si Z es -O-, entonces R⁶ no es bencilo opcionalmente sustituido, ni piridilmetilo opcionalmente sustituido, o R⁶ y R¹³, tomados conjuntamente con el nitrógeno al cual están unidos, forman un anillo heterocicloalquilo de 5 a 7 miembros opcionalmente sustituido, y un segundo grupo seleccionado de halógeno y alquilo inferior opcionalmente sustituido con halógeno, o R¹ se selecciona de 2,3-dihidrobenzofuran-5-ilo, croman-6-ilo, 1,3-benzodioxol-5-ilo, 2,3-dihidro-1,4-benzodioxin-6-ilo, 1,3-benzoxazol-5-ilo, benzoimidazol-5-ilo, 1,3-benzoxazol-6-ilo, 2-oxo-2,3-dihidro-1,3-benzoxazol-5-ilo, benzotiofen-5-ilo, benzotiazol-5-ilo, benzofuran-5-ilo, 1H-indol-5-ilo, 1H-indazol-5-ilo, isoindolin-5-ilo, benzo[c][1,2,5]oxadiazol-5-ilo, 1,2,3,4-tetrahidroquinolin-6-ilo, imidazo[1,2-a]piridin-6-ilo, pirazolo[1,5-a]piridin-5-ilo, quinolin-6-ilo, quinazolin-6-ilo, quinazolin-7-ilo, y quinoxalin-6-ilo, cada uno de los cuales está opcionalmente sustituido, o R¹ y R³, tomados conjuntamente con los átomos intermedios, forman un anillo bicíclico de fórmula (2) que está opcionalmente sustituido, en el que m es 0 ó 1, y n es 0 ó 1, con la condición de que al menos uno de m y n es 1, y W es -O-, o -N(R⁸)-, en la que R⁸ es hidrógeno o alquilo inferior; R² se selecciona de hidrógeno y alquilo inferior opcionalmente sustituido; R³ se selecciona de hidrógeno, halógeno, alquilo inferior opcionalmente sustituido, hidroxilo, alcoxi inferior opcionalmente sustituido, y amino opcionalmente sustituido; L se selecciona de -C(O)-, -C(O)O-, -C(O)N(R⁴)-, -C(O)N(OR⁷)-, -N(R⁴)S(O)₂-, -S(O)₂N(R⁴)-, y -C(O)N(R⁴)-S(O)₂-; R⁴ se selecciona de hidrógeno y alquilo inferior; R⁵ se selecciona de hidrógeno, alquilo inferior opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, y heterocicloalquilo opcionalmente sustituido; con la condición de que cuando L es -N(R⁴)S(O)₂-, entonces R⁵ no es hidrógeno, o R⁴ y R⁵, tomados conjuntamente con el nitrógeno al cual están unidos, forman un anillo heterocicloalquilo de 4 a 7 miembros opcionalmente sustituido, que está opcionalmente condensado con un cicloalquilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, arilo opcionalmente sustituido, o anillo heteroarilo opcionalmente sustituido; o R³ y R⁵, tomados conjuntamente con los átomos intermedios, forman un anillo de 5 a 7 miembros opcionalmente sustituido; y R⁷ se selecciona de hidrógeno y alquilo inferior; con la condición de que el compuesto de fórmula (1) no se selecciona de: éster metílico del ácido 6-(3-cloro-4-metilfenil)pirimidin-4-carboxílico; ácido 6-(3-cloro-4-metilfenil)pirimidin-4-carboxílico; éster metílico del ácido 6-(3-cloro-4-metoxifenil)pirimidin-4-carboxílico; y ácido 6-(3-cloro-4-metoxifenil)pirimidin-4-carboxílico.
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