AR111594A1 - Agentes inhibidores de la tirosina quinasa de bruton - Google Patents

Agentes inhibidores de la tirosina quinasa de bruton

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Publication number
AR111594A1
AR111594A1 ARP180100935A ARP180100935A AR111594A1 AR 111594 A1 AR111594 A1 AR 111594A1 AR P180100935 A ARP180100935 A AR P180100935A AR P180100935 A ARP180100935 A AR P180100935A AR 111594 A1 AR111594 A1 AR 111594A1
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Argentina
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alkyl
membered monocyclic
alkynyl
alkenyl
carbocyclyl
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ARP180100935A
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English (en)
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Daniel B Patience
Matthew Peterson
Fengmei Zheng
Joseph P Lyssikatos
Isaac Marx
Robin Prince
Bin Ma
Brian T Hopkins
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Biogen Ma Inc
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic 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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    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D471/02Heterocyclic 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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  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Abstract

Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable, en donde: el anillo A es un heteroarilo monocíclico de 5 miembros que contiene 3 heteroátomos seleccionados independientemente entre N, O y S, en donde dicho heteroarilo monocíclico de 5 miembros está opcionalmente sustituido con uno o más R¹; Q¹, Q² y Q³ son cada uno, independientemente, seleccionados de O, N(R²) y CH-R³, en donde al menos dos de Q¹, Q² y Q³ son C-R³; W se selecciona de CH y N; Y se selecciona de CH y N; R¹ en cada caso se selecciona independientemente de alquilo C₁₋₆ y carbociclilo de 3 a 5 miembros, en donde dicho alquilo C₁₋₆ y carbociclilo de 3 a 5 miembros están opcionalmente sustituidos con uno o más R¹⁰; R¹⁰ en cada caso se selecciona independientemente de halo, -CN, alquilo C₁₋₆ y carbociclilo de 3 a 5 miembros; R² se selecciona de H, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros, heterociclilo monocíclico de 4 a 6 miembros, -CN, -C(O)R²ᵃ, -C(O)₂R²ᵃ, -C(O)N(R²ᵃ)₂, -S(O)₂R²ᵃ, y -S(O)₂N(R²ᵃ)₂, en donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros, y heterociclilo monocíclico de 4 a 6 miembros están opcionalmente sustituidos con uno o más R²⁰; R²ᵃ en cada aparición se selecciona independientemente de H, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros, y heterociclilo monocíclico de 4 a 6 miembros, en donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros, y heterociclilo monocíclico de 4 a 6 miembros en cada aparición están opcionalmente e independientemente sustituidos con uno o más R²⁰; R²⁰ en cada aparición se selecciona independientemente de alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros, heterociclilo monocíclico de 4 a 6 miembros, halo, -CN, -C(O)R²⁰ᵃ, -C(O)₂R²⁰ᵃ, -C(O)N(R²⁰ᵃ)₂, -N(R²⁰ᵃ)₂, -N(R²⁰ᵃ)C(O)R²⁰ᵃ, -N(R²⁰ᵃ)C(O)₂R²⁰ᵃ, -N(R²⁰ᵃ)C(O)N(R²⁰ᵃ)₂, -N(R²⁰ᵃ)S(O)₂R²⁰ᵃ, -OR²⁰ᵃ, -OC(O)R²⁰ᵃ, -OC(O)N(R²⁰ᵃ)₂, -SR²⁰ᵃ, -S(O)R²⁰ᵃ, -S(O)₂R²⁰ᵃ, -S(O)N(R²⁰ᵃ)₂, y -S(O)₂N(R²⁰ᵃ)₂; R²⁰ᵃ en cada aparición se selecciona independientemente de H, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros y heterociclilo monocíclico de 4 a 6 miembros; R³ se selecciona de H, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros, heterociclilo monocíclico de 4 a 6 miembros, halo, -CN, -C(O)R³ᵃ, -C(O)₂R³ᵃ, -C(O)N(R³ᵃ)₂, -N(R³ᵃ)₂, -N(R³ᵃ)C(O)R³ᵃ, -N(R³ᵃ)C(O)₂R³ᵃ, -N(R³ᵃ)C(O)N(R³ᵃ)₂, -N(R³ᵃ)S(O)₂R³ᵃ, -OR³ᵃ, -OC(O)R³ᵃ, -OC(O)N(R³ᵃ)₂, -SR³ᵃ, -S(O)R³ᵃ, -S(O)₂R³ᵃ, -S(O)N(R³ᵃ)₂, y -S(O)₂N(R³ᵃ)₂, en donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros, y heterociclilo monocíclico de 4 a 6 miembros están opcionalmente sustituidos con uno o más R³⁰; R³ᵃ en cada aparición se selecciona independientemente de H, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros, y heterociclilo monocíclico de 4 a 6 miembros, en donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros y heterociclilo monocíclico de 4 a 6 miembros en cada aparición están opcional e independientemente sustituidos con uno o más R³⁰; R³⁰ en cada aparición se selecciona independientemente de alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros heterociclilo monocíclico de 4 a 6 miembros, halo, -CN, -C(O)R³⁰ᵃ, -C(O)₂R³⁰ᵃ, -C(O)N(R³⁰ᵃ)₂, -N(R³⁰ᵃ)₂, -N(R³⁰ᵃ)C(O)R³⁰ᵃ, -N(R³⁰ᵃ)C(O)₂R³⁰ᵃ, -N(R³⁰ᵃ)C(O)N(R³⁰ᵃ)₂, -N(R³⁰ᵃ)S(O)₂R³⁰ᵃ, -OR³⁰ᵃ, -OC(O)R³⁰ᵃ, -OC(O)N(R³⁰ᵃ)₂, -SR³⁰ᵃ, -S(O)R³⁰ᵃ, -S(O)₂R³⁰ᵃ, -S(O)N(R³⁰ᵃ)₂, y -S(O)₂N(R³⁰ᵃ)₂; R³⁰ᵃ en cada aparición se selecciona independientemente de; H, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico do 4 a 6 miembros y heterociclilo monocíclico de 4 a 6 miembros; R⁴ se selecciona de H y alquilo C₁₋₆, en donde dicho alquilo C₁₋₆ está opcionalmente sustituido con uno o más halo; R⁵ se selecciona de H y alquilo C₁₋₆ en donde dicho alquilo C₁₋₆ está opcionalmente sustituido con uno o más halo; R⁶ se selecciona de H y alquilo C₁₋₆, en donde dicho alquilo C₁₋₆ está opcionalmente sustituido con uno o más halo; o R⁵ y R⁶, junto con los átomos a los que están unidos, forman un anillo que contiene uno o dos heteroátomos seleccionados de O, N y S, en donde el anillo está opcionalmente sustituido con uno o mas R⁵⁰; y R⁵⁰ es alquilo C₁₋₆. Reivindicación 38: La forma A cristalina de (R)-1-(terc-butil)-N-(8-(2-((1-metil-1H-pirazol-4-il)amino)pirimidin-4-il)-2-(oxetan-3-il)-2,3,4,5-tetrahidro-1H-benzo[c]azepin-5-il)-1H-1,2,3-triazol-4-carboxamida. Reivindicación 48: La forma G cristalina de (R)-1-(terc-butil)-N-(8-(2-((1-metil-1H-pirazol-4-il)amino)pirimidin-4-il)-2-(oxetan-3-il)-2,3,4,5-tetrahidro-1H-benzo[c]azepin-5-il)-1H-1,2,3-triazol-4-carboxamida.
ARP180100935A 2017-04-14 2018-04-13 Agentes inhibidores de la tirosina quinasa de bruton AR111594A1 (es)

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