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AR114975A1 - Moduladores de molécula pequeña de sting humana, conjugados y aplicaciones terapéuticas - Google Patents

Moduladores de molécula pequeña de sting humana, conjugados y aplicaciones terapéuticas

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Publication number
AR114975A1
AR114975A1 ARP190101730A ARP190101730A AR114975A1 AR 114975 A1 AR114975 A1 AR 114975A1 AR P190101730 A ARP190101730 A AR P190101730A AR P190101730 A ARP190101730 A AR P190101730A AR 114975 A1 AR114975 A1 AR 114975A1
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Argentina
Prior art keywords
optionally substituted
bicyclic
mono
cycloalkyl
alkyl
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ARP190101730A
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English (en)
Inventor
Monali Banerjee
Arjun Surya
Ritesh Shrivastava
Dharmendra Yadav
David PRYDE
Rajib Ghosh
Sourav Basu
Sandip Middya
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Curadev Pharma Ltd
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Priority claimed from GB1709959.9A external-priority patent/GB2563642A/en
Application filed by Curadev Pharma Ltd filed Critical Curadev Pharma Ltd
Publication of AR114975A1 publication Critical patent/AR114975A1/es

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Abstract

La presente se refiere a conjugados de moduladores de molécula pequeña de la proteína estimuladora de genes de interferón (STING, por sus siglas en inglés). Reivindicación 1: Un compuesto de la fórmula (1), o una sal o profármaco farmacéuticamente aceptable de este, caracterizado porque: L¹ y L² son enlazadores; T es un resto de direccionamiento; a es un entero entre 1 y 5; b es un entero entre 1 y 10; z es un entero entre 1 y 5; y C un compuesto de fórmula (2); donde X¹ es CR¹ o N; X² es CR² o N; X³ es CR³ o N; Q es C=O, S=O, SO₂, C=S o CR⁴R⁵; L es alquilo C₁₋₆ sustituido opcionalmente, polifluoroalquilo C₁₋₃, cicloalquilo C₃₋₆ sustituido opcionalmente, alquenilo C₂₋₆ sustituido opcionalmente, alquinilo C₂₋₆ sustituido opcionalmente, C=O, S=O, SO₂, -CH₂C(O)-, -CH₂CONH- o -CONH-; Y es alquilo C₁₋₆ sustituido opcionalmente, polifluoroalquilo C₁₋₃ sustituido opcionalmente, alquenilo C₂₋₆ sustituido opcionalmente, alquinilo C₂₋₆ sustituido opcionalmente, cicloalquilo C₃₋₆ sustituido opcionalmente o un heterociclo mono o bicíclico de 3 a 8 miembros sustituido opcionalmente; cada uno de R¹, R² y R³ se selecciona independientemente del grupo que consiste en H, halógeno, CN, hidroxilo, COOH, CONR¹R², NR¹R², NHCOR¹ alquilo C₁₋₆ sustituido opcionalmente, polifluoroalquilo C₁₋₃ sustituido opcionalmente, alquilsulfonilo C₁₋₆ sustituido opcionalmente, cicloalquilo C₃₋₆ mono o bicíclico sustituido opcionalmente, alquenilo C₂₋₆ sustituido opcionalmente, alquinilo C₂₋₆ sustituido opcionalmente, alcoxi C₁₋₆ sustituido opcionalmente, grupo alcoxicarbonilo C₁₋₆ sustituido opcionalmente, arilo C₅₋₁₀ mono o bicíclico sustituido opcionalmente, heteroarilo de 5 a 10 miembros mono o bicíclico sustituido opcionalmente, heterociclo de 3 a 8 miembros mono o bicíclico sustituido opcionalmente, ariloxi sustituido opcionalmente, heteroariloxi sustituido opcionalmente y heterocicliloxi sustituido opcionalmente; cada uno de R⁴ y R⁵ se selecciona independiente del grupo que consiste en H, halógeno, alquilo C₁₋₆ sustituido opcionalmente y cicloalquilo C₃₋₆ sustituido opcionalmente; o R⁴ y R⁵ juntos con el átomo al cual se unen forman un anillo espirocíclico; R⁶ es un anillo sustituido opcionalmente con uno o más grupos R¹², donde el anillo se selecciona del grupo que consiste en arilo C₅₋₁₀ mono o bicíclico; un heteroarilo mono o bicíclico de 5 a 10 miembros; cicloalquilo C₃₋₆; y un heterociclo mono o bicíclico de 3 a 8 miembros; R⁷ es H, alquilo C₁₋₆ sustituido opcionalmente, sulfonilo sustituido opcionalmente, alquilsulfonilo C₁₋₆ sustituido opcionalmente, cicloalquilo C₃₋₆ sustituido opcionalmente, alquenilo C₂₋₆ sustituido opcionalmente o alquinilo C₂₋₆ sustituido opcionalmente; R⁸ es un arilo C₅₋₁₀ mono o bicíclico sustituido opcionalmente, un heteroarilo de 5 a 10 miembros mono o bicíclico sustituido opcionalmente, cicloalquilo C₃₋₆ mono o bicíclico sustituido opcionalmente o un heterociclo de 3 a 8 miembros mono o bicíclico sustituido opcionalmente; cada uno de R⁹ y R¹⁰ se selecciona independientemente del grupo que consiste en alquilo C₁₋₆ sustituido opcionalmente, H, halógeno, CN, CO₂H, CONR¹R², azido, sulfonilo, polifluoroalquilo C₁₋₃, tioalquilo C₁₋₆ sustituido opcionalmente, alquilosulfonilo C₁₋₆ sustituido opcionalmente, cicloalquilo C₃₋₆ sustituido opcionalmente, alquenilo C₂₋₆ sustituido opcionalmente, alquinilo C₂₋₆ sustituido opcionalmente, alcoxi C₁₋₆ sustituido opcionalmente, alcoxicarbonilo C₁₋₆ sustituido opcionalmente, arilo C₅₋₁₀ mono o bicíclico sustituido opcionalmente, heteroarilo de 5 a 10 miembros mono o bicíclico sustituido opcionalmente, heterociclo sustituido opcionalmente, ariloxi sustituido opcionalmente, y heteroariloxi sustituido opcionalmente; o R⁹ y R¹⁰ juntos con el átomo de C al cual están unidos pueden combinarse para formar un anillo espirocíclico sustituido opcionalmente; R¹¹ se selecciona del grupo que consiste en alquilo C₁₋₆ sustituido opcionalmente, H, hidroxilo, polifluoroalquilo C₁₋₃, tioalquilo C₁₋₆ sustituido opcionalmente, alquilosulfonilo C₁₋₆ sustituido opcionalmente, cicloalquilo C₃₋₆ sustituido opcionalmente, alquenilo C₂₋₆ sustituido opcionalmente, alquinilo C₂₋₆ sustituido opcionalmente, alcoxi C₁₋₆ sustituido opcionalmente, alcoxicarbonilo C₁₋₆ sustituido opcionalmente, arilo C₅₋₁₀ mono o bicíclico sustituido opcionalmente, heteroarilo de 5 a 10 miembros mono o bicíclico sustituido opcionalmente, heterociclo sustituido opcionalmente, ariloxi sustituido opcionalmente, y heteroariloxi sustituido opcionalmente; el o cada grupo R¹² se selecciona independientemente del grupo que consiste en halo, OH, SH, OP(O)(OH)₂, NR¹³R¹⁴, CONR¹³R¹⁴, CN, COOR¹³, NO₂, azido, SO₂R¹³, OSO₂R¹³, NR¹³SO₂R¹⁴, NR¹³C(O)R¹⁴, O(CH₂)ₙOC(O)R¹³, NR¹³(CH₂)ₙOC(O)R¹⁴, OC(O)R¹³, OC(O)OR¹⁴, OC(O)NR¹³R¹⁴, OC(O)O(CH₂)ₙCOOR¹⁴, OC(O)NR¹³(CH₂)ₙCOOR¹⁴, alquilo C₁₋₆ sustituido opcionalmente, alcoxi C₁₋₆ sustituido opcionalmente, ariloxi sustituido opcionalmente, heteroariloxi sustituido opcionalmente, arilo C₅₋₁₀ mono o bicíclico sustituido opcionalmente, un heteroarilo de 5 a 10 miembros mono o bicíclico sustituido opcionalmente, cicloalquilo C₃₋₆ sustituido opcionalmente y un heterociclo de 3 a 8 miembros mono o bicíclico sustituido opcionalmente; cada uno de R¹³ y R¹⁴ se selecciona independientemente del grupo que consiste en H, alquilo C₁₋₆ sustituido opcionalmente, cicloalquilo C₃₋₆ mono o bicíclico sustituido opcionalmente, arilo C₅₋₁₀ mono o bicíclico sustituido opcionalmente, heteroarilo de 5 a 10 miembros mono o bicíclico sustituido opcionalmente y heterociclo de 3 a 8 miembros mono o bicíclico sustituido opcionalmente; y n es un entero entre 0 y 6; o un complejo, sal, solvato, forma tautomérica o forma polimórfica farmacéuticamente aceptable de estos.
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