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AR116022A1 - Compuestos heteroaromáticos como inhibidores de vanina - Google Patents

Compuestos heteroaromáticos como inhibidores de vanina

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Publication number
AR116022A1
AR116022A1 ARP190102432A ARP190102432A AR116022A1 AR 116022 A1 AR116022 A1 AR 116022A1 AR P190102432 A ARP190102432 A AR P190102432A AR P190102432 A ARP190102432 A AR P190102432A AR 116022 A1 AR116022 A1 AR 116022A1
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cycloalkyl
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membered
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ARP190102432A
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Hannes Fiepko Koolman
Martin Thomas Fleck
Cdrickx Godbout
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Boehringer Ingelheim Int
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Publication of AR116022A1 publication Critical patent/AR116022A1/es

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    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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  • Pyridine Compounds (AREA)

Abstract

Compuestos derivados de pirrolo[2,3-b]piridina como inhibidores de vanina, composiciones farmacéuticas que los comprenden y su uso en el tratamiento de enfermedades mediadas por la inhibición de la enzima vanina 1. Reivindicación 1: Un compuesto caracterizado por la fórmula (1), o una sal de este aceptable desde el punto de vista farmacéutico, o solvatos de este, en donde n se refiere a 1, 2 ó 3; m se refiere a 1, 2 ó 3; R¹ y R² se seleccionan, independientemente entre sí, del grupo que consiste en H, C₁₋₄-alquilo opcionalmente sustituido con 1 - 3 átomos F o C₁₋₂-alcoxi, arilo de 6 - 10 miembros sustituido por R².¹ y heteroarilo de 5 - 6 miembros sustituido por R².¹, en donde R².¹ se selecciona del grupo que consiste en H, F, Cl, Br, -CN, NR².¹.¹R².¹.², SO₂R².¹.³ y OR².¹.⁴, en donde R².¹.¹, R².¹.², independientemente entre sí, se refiere a H, C₁₋₄-alquilo o C₃₋₄-cicloalquilo; o R².¹.¹ y R².¹.², junto con el átomo de N al que están unidos, forman un heterociclilo de 4 - 5 miembros o un heterociclilo de 6 miembros que opcionalmente contiene un heteroátomo adicional seleccionado del grupo que consiste en N y O; R².¹.³ se refiere a C₁₋₄-alquilo o NR².¹.¹R².¹.²; R².¹.⁴ se selecciona del grupo que consiste en H, C₁₋₄-alquilo, C₃₋₅-cicloalquilo, heterociclilo de 4 - 5 miembros que contiene 1 heteroátomo seleccionado del grupo que consiste en N y O, en donde en la definición de R².¹.¹, R².¹.², R².¹.³ y R².¹.⁴ dicho alquilo, cicloalquilo y heterociclilo son opcionalmente sustituidos por 1 - 3 átomos de F o un C₁₋₂-alcoxi; o R¹ y R² juntos pueden formar un carbociclo de 3 - 5 miembros o un heterociclilo de 4 - 6 miembros que contiene un heteroátomo seleccionado del grupo que consiste en N y O; R³ se refiere a NR³.¹R³.²; o R³ se refiere a un grupo de la fórmula (2) ó (3), en donde X se refiere a CH₂, NRX u O; en donde RX se refiere a H o C₁₋₃-alquilo; R³.¹ se selecciona del grupo que consiste en C₁₋₄-alquil-CO- opcionalmente sustituido por 1 - 3 átomos de F, C₃₋₄-cicloalquilo o C₁₋₂-alcoxi, R³.¹.³R³.¹.⁴N-CO-, R³.¹.⁵-N-CO-, pirimidina, piridina, C₃₋₅-cicloalquil-CO- sustituido con R³.¹.¹ y R³.¹.², fenil-CO- sustituido con R³.¹.¹ y R³.¹.²; en donde R³.¹.¹, R³.¹.² se seleccionan, independientemente entre sí, del grupo que consiste en H, -CH₃, -OR³.¹.¹.¹, F y -CN; R³.¹.³, R³.¹.⁴, independientemente entre sí, se refieren a H, C₁₋₄-alquilo o C₃₋₄-cicloalquilo; o R³.¹.³ y R³.¹.⁴, junto con el átomo de N al que están unidos, forman un heterociclilo de 4 - 5 miembros o un heterociclilo de 6 miembros que opcionalmente contiene un heteroátomo adicional seleccionado del grupo que consiste en N y O; R³.¹.⁵ se selecciona del grupo que consiste en C₁₋₄-alquilo, C₃₋₅-cicloalquilo, heterociclilo de 4 - 5 miembros y C₃₋₄-cicloalquil-CH₂-; R³.¹.¹.¹ se refiere a C₁₋₄-alquilo, C₃₋₅-cicloalquilo o heterociclilo de 4 - 5 miembros; en donde en la definición de R³.¹.¹, R³.¹.², R³.¹.³, R³.¹.⁴, R³.¹.⁵ y R³.¹.¹.¹ dicho alquilo, cicloalquilo y heterociclilo son opcionalmente sustituidos por 1 - 3 átomos de F o un C₁₋₂-alcoxi; R³.² se selecciona del grupo que consiste en H, C₁₋₄-alquilo, C₃₋₄-cicloalquilo, C₃₋₄-cicloalquil-C₁₋₂-alquil y fenil-C₁₋₂-alquil-; en donde en la definición de R³.² dicho alquilo, cicloalquilo y fenilo son opcionalmente sustituidos por 1 - 3 átomos de F o un C₁₋₂-alcoxi; R⁴ se refiere a hidrógeno o C₁₋₄-alquilo opcionalmente sustituido con 1 a 3 átomos de F; o R³ y R⁴ juntos forman un heterociclo de 4 - 6 miembros que contiene un átomo de oxígeno.
ARP190102432A 2018-08-28 2019-08-27 Compuestos heteroaromáticos como inhibidores de vanina AR116022A1 (es)

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IL283397B2 (en) 2018-12-03 2025-03-01 Boehringer Ingelheim Int Heteroaromatic compounds as vanin inhibitors
EA202191477A1 (ru) 2018-12-03 2021-10-13 Бёрингер Ингельхайм Интернациональ Гмбх Гетероароматические соединения в качестве ингибиторов ванина
IL301556A (en) * 2020-09-25 2023-05-01 Shanghai Meiyue Biotech Dev Co Ltd Pyrimidine carboxamide compound and its use
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US20250197414A1 (en) * 2022-03-18 2025-06-19 Shanghai Meiyue Biotech Development Co., Ltd. Salt form and crystal form of vanin enzyme inhibitor, method for preparing same, and use thereof

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