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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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Argentina
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cycloalkyl
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refers
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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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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    • A61K31/33—Heterocyclic compounds
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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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    • A61K31/00—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
    • A61K31/55—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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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • 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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AU2019392524B2 (en) 2018-12-03 2025-05-08 Boehringer Ingelheim International Gmbh Heteroaromatic compounds as vanin inhibitors
EA202191476A1 (ru) 2018-12-03 2021-10-26 Бёрингер Ингельхайм Интернациональ Гмбх Гетероароматические соединения в качестве ингибиторов ванина
KR20210099092A (ko) 2018-12-03 2021-08-11 베링거 인겔하임 인터내셔날 게엠베하 바닌 억제제로서의 헤테로방향족 화합물
EP4219479A4 (en) * 2020-09-25 2024-12-25 Shanghai Meiyue Biotech Development Co., Ltd. PYRIMIDINCARBOXAMIDE COMPOUND AND USE THEREOF
TWI811901B (zh) * 2020-12-17 2023-08-11 大陸商上海美悅生物科技發展有限公司 一種嘧啶甲醯胺類化合物及其應用
CN116768909B (zh) * 2022-03-18 2025-08-08 上海美悦生物科技发展有限公司 Vanin酶抑制剂的盐型、晶型及其制备方法和应用

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