AR121929A1 - AMINOTIAZOLES SUSTITUIDOS COMO INHIBIDORES DE DGKz PARA LA ACTIVACIÓN INMUNE - Google Patents

AMINOTIAZOLES SUSTITUIDOS COMO INHIBIDORES DE DGKz PARA LA ACTIVACIÓN INMUNE

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Publication number
AR121929A1
AR121929A1 ARP210101100A ARP210101100A AR121929A1 AR 121929 A1 AR121929 A1 AR 121929A1 AR P210101100 A ARP210101100 A AR P210101100A AR P210101100 A ARP210101100 A AR P210101100A AR 121929 A1 AR121929 A1 AR 121929A1
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AR
Argentina
Prior art keywords
alkyl
group
phenyl
cycloalkyl
membered
Prior art date
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ARP210101100A
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English (en)
Inventor
Norbert Schmees
Ulrike Rhn
Dennis Kirchhoff
Kirstin Petersen
Thi Thanh Uyen Nguyen
Mareike Grees
Nicolas Werbeck
Ulf Bmer
Benjamin Bader
Detlef Stckigt
Dirk Kosemund
Rienk Offringa
Corinna Link
Katrin Nowak-Reppel
Original Assignee
Bayer Ag
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Application filed by Bayer Ag filed Critical Bayer Ag
Publication of AR121929A1 publication Critical patent/AR121929A1/es

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    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/47—Quinolines; Isoquinolines
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    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
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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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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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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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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

La presente invención cubre compuestos de aminotiazol de fórmula general (1), en la cual R¹, R², R³ y R⁴ son como se define en la presente, métodos para preparar dichos compuestos, compuestos intermediarios útiles para preparar dichos compuestos, composiciones y combinaciones farmacéuticas que comprenden dichos compuestos, y el uso de dichos compuestos para elaborar composiciones farmacéuticas para el tratamiento y/o la profilaxis de enfermedades, en particular de trastornos regulados por diacilglicerol quinasa zeta (DGKz), como agentes únicos o en combinación con otros ingredientes activos. Reivindicación 1: Un compuesto de fórmula general (1) en la cual: R¹ representa un grupo fenilo o heteroarilo de 6 miembros opcionalmente sustituido, una, dos o tres veces, cada sustituyente independientemente seleccionado de un átomo de halógeno o un grupo seleccionado de hidroxi, ciano, nitro, alquilo-C₁₋₆, (fenil)-(alquilo-C₁₋₃)-, haloalquilo-C₁₋₆, alcoxi-C₁₋₆, (fenil)-(alcoxi-C₁₋₃)-, haloalcoxi-C₁₋₆, -N(R⁵)(R⁶), en donde los grupos fenilo en dichos grupos (fenil)-(alquilo-C₁₋₃)- y (fenil)-(alcoxi-C₁₋₃)- están opcionalmente sustituidos una o dos veces, cada sustituyente independientemente seleccionado de un átomo de halógeno o un grupo seleccionado de ciano, metilo, etilo, trifluorometilo, metoxi, etoxi, dimetilamino y trifluorometoxi, o dos sustituyentes unidos a átomos de carbono adyacentes de dicho grupo fenilo o heteroarilo de 6 miembros juntos forman un grupo bivalente seleccionado de -(CH₂)₃-, -(CH₂)₄-, -(CH₂)₂-O-, -(CH₂)₃-O-, -CH₂-O-CH₂-, -(CH₂)₂-O-CH₂-, -O-CH₂-O-, -O-CH₂-CH₂-O-, -O-CF₂-O-, -O-CH₂-CF₂-O- y -O-CF₂-CF₂-O-, o R¹ representa un grupo heteroarilo de 5 miembros opcionalmente sustituido una o dos veces, cada sustituyente independientemente seleccionado de un átomo de halógeno o un grupo seleccionado de ciano, alquilo-C₁₋₃ y alcoxi-C₁₋₃; R² representa un grupo de fórmula (2), en donde “*” indica el punto de unión al átomo de nitrógeno al cual R² está unido; R³ representa un grupo seleccionado de metilo y -NH₂; R⁴ representa un grupo fenilo o heteroarilo de 6 miembros opcionalmente sustituido, una, dos o tres veces, cada sustituyente independientemente seleccionado de un átomo de halógeno o un grupo seleccionado de ciano, nitro, alquilo-C₁₋₆, (fenil)-(alquilo-C₁₋₃)-, (heteroarilo de 5 ó 6 miembros)-(alquilo-C₁₋₃)-, (cicloalquilo-C₃₋₇)-(alquilo-C₁₋₃)-, ((R⁹)O)-(alquilo-C₁₋₆)-, haloalquilo-C₁₋₆, cicloalquilo-C₃₋₇, -OR⁹, -N(R¹⁰)(R¹¹), ((R¹⁰)(R¹¹)N)-(alquilo-C₁₋₃)-, -C(=O)-N(R¹²)(R¹³), -S(=O)ₙ-R¹⁴, -C(=O)R¹⁴, -C(=O)-OR¹⁷, y un grupo heteroarilo de 5 ó 6 miembros que en sí mismo está opcionalmente sustituido con uno o dos sustituyentes seleccionados de un átomo de halógeno y un grupo metilo, o dos sustituyentes unidos a átomos de carbono adyacentes de dicho grupo fenilo o heteroarilo de 6 miembros juntos forman un grupo bivalente seleccionado de -(CH₂)₃-, -(CH₂)₄-, -(CH₂)₂-O-, -(CH₂)₃-O-, -CH₂-O-CH₂-, -(CH₂)₂-O-CH₂-, -O-CH₂-O-, -O-CH₂-CH₂-O-, -O-CF₂-O-, -O-CH₂-CF₂-O- y -O-CF₂-CF₂-O-; R⁵ y R⁶ representan, independientemente en cada ocurrencia, un átomo de hidrógeno o un grupo seleccionado de alquilo-C₁₋₄, (alquil-C₁₋₄)-C(=O)-, cicloalquilo-C₃₋₄ y (fenil)-(alquilo-C₁₋₃)-, o R⁵ y R⁶, junto con el átomo de nitrógeno al cual están unidos, representan un nitrógeno monocíclico que contiene un grupo heterocicloalquilo de 4 a 7 miembros que está opcionalmente sustituido una, dos o tres veces, cada sustituyente independientemente seleccionado de un átomo de halógeno o un grupo seleccionado de oxo, hidroxi, alquilo-C₁₋₄, (alquil-C₁₋₄)-C(=O)-, cicloalquilo-C₃₋₄ y alcoxi-C₁₋₄; R⁷ representa un átomo de hidrógeno o un grupo alquilo-C₁₋₂; R⁸ representa un grupo seleccionado de -C(=O)-NH₂ y -S(=O)₂-NH₂; R⁹ representa un átomo de hidrógeno o un grupo seleccionado de alquilo-C₁₋₆, (heteroarilo de 5 ó 6 miembros)-(alquilo-C₁₋₃)-, (fenil)-(alquilo-C₁₋₃)-, haloalquilo-C₁₋₆, hidroxialquilo-C₂-C₄, (alcoxi-C₁₋₃)-alquilo-C₂₋₃-, ((alquil-C₁₋₃)-C(=O)-O)-alquilo-C₂₋₃-, -C(R¹⁸)(R¹⁹)-C(=O)-OR¹⁷, -C(R¹⁸)(R¹⁹)-C(=O)-N(R²⁰)(R²¹), -C(=O)-N(R²⁰)(R²¹), fenilo y un grupo heteroarilo de 5 ó 6 miembros, en donde el grupo fenilo dentro de dicho grupo (fenil)-(alquilo-C₁₋₃)- y dicho grupo fenilo mismo, y el grupo heteroarilo de 5 ó 6 miembros dentro de dicho grupo (heteroarilo de 5 ó 6 miembros)-(alquilo-C₁₋₃)- y dicho grupo heteroarilo de 5 ó 6 miembros mismo están opcionalmente sustituidos una o dos veces, cada sustituyente independientemente seleccionado de un átomo de halógeno o un grupo seleccionado de ciano, metilo, etilo, trifluorometilo, metoxi, etoxi, dimetilamino y trifluorometoxi; R¹⁰ y R¹¹ representan, independientemente en cada ocurrencia, un átomo de hidrógeno o un grupo seleccionado de alquilo-C₁₋₄, haloalquilo-C₁₋₄, hidroxialquilo-C₂-C₄-, (alcoxi-C₁₋₃)-alquilo-C₂₋₃-, ((R²²)(R²³)N)-alquilo-C₂₋₃, (cicloalquil-C₃₋₇)-(alquilo-C₁₋₃)-, (alquil-C₁₋₄)-C(=O)-, cicloalquilo-C₃₋₇, (cicloalquil-C₃₋₇)-C(=O)-, (fenil)-(alquilo-C₁₋₃)-, (fenil)-(alquilo-C₁₋₃)-C(=O)-, (fenil)-(alquilo-C₁₋₃)-O-C(=O)-, fenilo y un grupo heteroarilo de 5 ó 6 miembros, en donde el cicloalquilo-C₃₋₇ y el cicloalquilo-C₃₋₇ dentro de dichos grupos (cicloalquil-C₃₋₇)-(alquilo-C₁₋₃)- y (cicloalquil-C₃₋₇)-C(=O)- están opcionalmente sustituidos una o dos veces, cada sustituyente independientemente seleccionado de un átomo de flúor o un grupo seleccionado de ciano, alquilo-C₁₋₂ y haloalquilo-C₁₋₂, y en donde dicho fenilo y dicho grupo heteroarilo de 5 ó 6 miembros, y los grupos fenilo dentro de dichos grupos (fenil)-(alquilo-C₁₋₃)-, (fenil)-(alquilo-C₁₋₃)-C(=O)- y (fenil)-(alquilo-C₁₋₃)-O-C(=O)-, están opcionalmente sustituidos una o dos veces, cada sustituyente independientemente seleccionado de un átomo de halógeno o un grupo seleccionado de ciano, metilo, etilo, trifluorometilo, metoxi, etoxi, dimetilamino y trifluorometoxi, o R¹⁰ y R¹¹, junto con el átomo de nitrógeno al cual están unidos, representan un nitrógeno monocíclico que contiene un grupo heterocicloalquilo de 4 a 7 miembros, o un nitrógeno bicíclico que contiene un grupo heterocicloalquilo de 5 a 11 miembros, que están opcionalmente sustituidos una, dos o tres veces, cada sustituyente independientemente seleccionado de un átomo de halógeno o un grupo seleccionado de ciano, oxo, hidroxi, alquilo-C₁₋₄, haloalquilo-C₁₋₄, (alquil-C₁₋₄)-C(=O)-, cicloalquilo-C₃₋₇, alcoxi-C₁₋₄, -N(R²²)(R²³), y un grupo heterocicloalquilo monocíclico de 4 a 7 miembros; R¹² y R¹³ representan, independientemente en cada ocurrencia, un átomo de hidrógeno o un grupo seleccionado de alquilo-C₁₋₄, haloalquilo-C₁₋₄, hidroxialquilo-C₁₋₄, (alcoxi-C₁₋₄)-alquilo-C₂₋₃-, (haloalcoxi-C₁₋₄)-alquilo-C₂₋₃-, (fenoxi)-alquilo-C₂₋₃-, cicloalquilo-C₃₋₇, heterocicloalquilo monocíclico de 4 a 7 miembros y (fenil)-(alquilo-C₁₋₃)-, en donde el cicloalquilo-C₃₋₇ y heterocicloalquilo monocíclico de 4 a 7 miembros están opcionalmente sustituidos una, dos o tres veces, cada sustituyente independientemente seleccionado de un átomo de halógeno o un grupo seleccionado de ciano, oxo, hidroxi, alquilo-C₁₋₄, (alquil-C₁₋₄)-C(=O)-, cicloalquilo-C₃₋₄ y alcoxi-C₁₋₄, y en donde los grupos fenilo dentro de dicho grupo (fenoxi)alquilo-C₂₋₃- y dicho grupo (fenil)-(alquilo-C₁₋₃)- están opcionalmente sustituidos una o dos veces, cada sustituyente independientemente seleccionado de un átomo de halógeno o un grupo seleccionado de ciano, metilo, etilo, trifluorometilo, metoxi, etoxi, dimetilamino y trifluorometoxi, o R¹² y R¹³, junto con el átomo de nitrógeno al cual están unidos, representan un nitrógeno monocíclico que contiene un grupo heterocicloalquilo de 4 a 7 miembros que está opcionalmente sustituido una, dos o tres veces, cada sustituyente independientemente seleccionado de un átomo de halógeno o un grupo seleccionado de ciano, oxo, hidroxi, alquilo-C₁₋₄, (alquil-C₁₋₄)-C(=O)-, cicloalquilo-C₃₋₄ y alcoxi-C₁₋₄; R¹⁴ representa un grupo seleccionado de alquilo-C₁₋₄, haloalquilo-C₁₋₄ y fenilo, en donde el grupo fenilo está opcionalmente sustituido una o dos veces, cada sustituyente independientemente seleccionado de un átomo de halógeno o un grupo seleccionado de ciano, metilo, etilo, trifluorometilo, metoxi, etoxi, dimetilamino y trifluorometoxi; R¹⁷ representa un grupo alquilo-C₁₋₄; R¹⁸ y R¹⁹ representan, independientemente en cada ocurrencia, un átomo de hidrógeno o un grupo alquilo-C₁₋₄; R²⁰ representa un átomo de hidrógeno o un grupo seleccionado de alquilo-C₁₋₆, alquenilo-C₃₋₄, alquinilo-C₃₋₄, alcoxi-C₁₋₃, cicloalquilo-C₃₋₇, cicloalquilo-C₅₋₁₁ bicíclico, adamantilo, heterocicloalquilo monocíclico de 4 a 7 miembros, heterocicloalquilo bicíclico de 5 a 11 miembros, fenilo, naftilo y heteroarilo de 5 a 10 miembros, en donde dicho grupo alquilo-C₁₋₆ está opcionalmente sustituido una, dos o tres veces, cada sustituyente independientemente seleccionado de un átomo de halógeno o un grupo seleccionado de hidroxi, ciano, alcoxi-C₁₋₃, -N(R²²)(R²³), cicloalquilo-C₃₋₇, cicloalquilo-C₅₋₁₁ bicíclico, adamantilo, heterocicloalquilo monocíclico de 4 a 7 miembros, heterocicloalquilo bicíclico de 5 a 11 miembros, fenilo y heteroarilo de 5 a 10 miembros, dichos sustituyentes fenilo y heteroarilo de 5 a 10 miembros mismos estando opcionalmente sustituidos una o dos veces, cada sustituyente independientemente seleccionado de un átomo de halógeno o un grupo seleccionado de ciano, metilo, etilo, trifluorometilo, metoxi, etoxi, dimetilamino y trifluorometoxi, y en donde el cicloalquilo-C₃₋₇, cicloalquilo-C₅₋₁₁ bicíclico, adamantilo, heterocicloalquilo monocíclico de 4 a 7 miembros y heterocicloalquilo bicíclico de 5 a 11 miembros están opcionalmente sustituidos una, dos o tres veces, cada sustituyente independientemente seleccionado de un átomo de halógeno o un grupo seleccionado de ciano, oxo, hidroxi, alquilo-C₁₋₄, (alquil-C₁₋₄)-C(=O)-, cicloalquilo-C₃₋₄ y alcoxi-C₁₋₄, y en donde dichos grupos fenilo, naftilo y heteroarilo de 5 a 10 miembros están opcionalmente sustituidos una, dos o tres veces, cada sustituyente independientemente seleccionado de un átomo de halógeno o un grupo seleccionado de ciano, alquilo-C₁₋₄, haloalquilo-C₁₋₄, alcoxi-C₁₋₄, haloalcoxi-C₁₋₄, -N(R²²)(R²³) y -C(=O)-N(R²⁴)(R²⁵), R²¹ representa un átomo de hidrógeno o un grupo alquilo-C₁₋₄, o R²⁰ y R²¹, junto con el átomo de nitrógeno al cual están unidos, representan un nitrógeno monocíclico que contiene un grupo heterocicloalquilo de 4 a 7 miembros que está opcionalmente benzocondensado, y que está opcionalmente sustituido una, dos o tres veces, cada sustituyente independientemente seleccionado de un átomo de halógeno o un grupo seleccionado de ciano, oxo, hidroxi, alquilo-C₁₋₄, haloalquilo-C₁₋₄, (fenil)-(alquilo-C₁₋₃)-, (alquil-C₁₋₄)-C(=O)-, cicloalquilo-C₃₋₄, alcoxi-C₁₋₄, haloalcoxi-C₁₋₃, -N(R²²)(R²³) y -C(=O)-N(R²⁴)(R²⁵); R²² y R²³ representan, independientemente en cada ocurrencia, un átomo de hidrógeno o un grupo seleccionado de alquilo-C₁₋₂ y (alquil-C₁₋₂)-C(=O)-; R²⁴ y R²⁵ representan, independientemente en cada ocurrencia, un átomo de hidrógeno o un grupo alquilo-C₁₋₄, y n representa un número entero 0, 1 ó 2, o un estereoisómero, un tautómero, un N-óxido, un hidrato, un solvato o una sal del mismo, o una mezcla de ellos.
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US20230167103A1 (en) 2020-04-24 2023-06-01 Bayer Aktiengesellschaft Substituted aminothiazoles as dgkzeta inhibitors for immune activation

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