AR088641A1 - Compuestos de heteroaril piridona y aza-piridona - Google Patents

Compuestos de heteroaril piridona y aza-piridona

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Publication number
AR088641A1
AR088641A1 ARP120104128A ARP120104128A AR088641A1 AR 088641 A1 AR088641 A1 AR 088641A1 AR P120104128 A ARP120104128 A AR P120104128A AR P120104128 A ARP120104128 A AR P120104128A AR 088641 A1 AR088641 A1 AR 088641A1
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AR
Argentina
Prior art keywords
heterocyclyl
heteroaryl
alkyl
nhch3
carbocyclyl
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ARP120104128A
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English (en)
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Genentech Inc
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Publication of AR088641A1 publication Critical patent/AR088641A1/es

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    • A61K31/495Heterocyclic 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
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    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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Abstract

Se proporcionan compuestos de heteroaril piridona y aza-piridona, que resultan de utilidad para inhibir la Btk quinasa, y para tratar trastornos inmunes, tales como la inflamación mediada por la Btk quinasa. Se revelan métodos para usar los compuestos de la fórmula (1) para el diagnostico y el tratamiento in vitro, in situ e in vivo de tales trastornos en células de mamífero, o afecciones patológicas asociadas. Reivindicación 1: Un compuesto que se selecciona de la fórmula (1) o sus estereoisómeros, tautómeros o sales farmacéuticamente aceptables, donde: X¹ es CR¹ o N; X² es CR² o N; X³ es CR³ o N; donde uno o dos de X¹, X² y X³ son N; R¹, R² y R³ se seleccionan, de manera independiente, de H, F, Cl, -NH₂, -NHCH₃, -N(CH₃)₂, -OH, -OCH₃, -OCH₂CH₃, -OCH₂CH₂OH, y alquilo C₁₋₃; R⁴ se selecciona de H, F, Cl, CN, -CH₂OH, -CH(CH₃)OH, -C(CH₃)₂OH, -CH(CF₃)OH, -CH₂F, -CHF₂, -CH₂CHF₂, -CF₃, -C(O)NH₂, -C(O)NHCH₃, -C(O)N(CH₃)₂, -NH₂, -NHCH₃, -N(CH₃)₂, -NHC(O)CH₃, -OH, -OCH₃, -OCH₂CH₃, -OCH₂CH₂OH, ciclopropilo, ciclopropilmetilo, 1-hidroxiciclopropilo, imidazolilo, pirazolilo, 3-hidroxi-oxetan-3-ilo, oxetan-3-ilo y azetidin-1-ilo; R⁵ es arilo C₆₋₂₀ opcionalmente sustituido, carbociclilo C₃₋₁₂, heterociclilo C₂₋₂₀, heteroarilo C₁₋₂₀, -(arilo C₆₋₂₀)-(heterociclilo C₂₋₂₀), -(heteroarilo C₁₋₂₀)-(heterociclilo C₂₋₂₀), -(heteroarilo C₁₋₂₀)-(heterociclilo C₂₋₂₀)-(heterociclilo C₂₋₂₀), -(heteroarilo C₁₋₂₀)-(heterociclilo C₂₋₂₀)-(alquilo C₁₋₆), -(heteroarilo C₁₋₂₀)-(alquilo C₁₋₆), -(heterociclilo C₂₋₂₀)-(alquilo C₁₋₆), -(heterociclilo C₂₋₂₀)-(carbociclilo C₃₋₁₂), -(heteroarilo C₁₋₂₀)-(carbociclilo C₃₋₁₂) o -(heteroarilo C₁₋₂₀)-C(=O)-(heterociclilo C₂₋₂₀); R⁶ es H, -CH₃, -CH₂CH₃, -CH₂CH₂OH, -CHF₂, -NH₂ u -OH; R⁷ se selecciona de las estructuras del grupo de formulas (2), donde la línea ondulada indica el sitio de unión; e Y¹ e Y² se seleccionan, de manera independiente, de CH y N, donde cada uno de Y¹ e Y² no es N; donde el alquilo, carbociclilo, heterociclilo, arilo y heteroarilo están opcionalmente sustituidos con uno o más sustituyentes que se seleccionan, de manera independiente, de F, Cl, Br, I, -CN, -CH₃, -CH₂CH₃, -CH(CH₃)₂, -CH₂CH(CH₃)₂, -CH₂OH, -CH₂OCH₃, -CH₂CH₂OH, -C(CH₃)₂OH, -CH(OH)CH(CH₃)₂, -C(CH₃)₂CH₂OH, -CH₂CH₂SO₂CH₃, -CH₂OP(O)(OH)₂, -CH₂F, -CHF₂, -CF₃, -CH₂CF₃, -CH₂CHF₂, -CH(CH₃)CN, -C(CH₃)₂CN, -CH₂CN, -CO₂H, -COCH₃, -CO₂CH₃, -CO₂C(CH₃)₃, -COCH(OH)CH₃, -CONH₂, -CONHCH₃, -CON(CH₃)₂, -C(CH₃)₂CONH₂, -NH₂, -NHCH₃, -N(CH₃)₂, -NHCOCH₃, -N(CH₃)COCH₃, -NHS(O)₂CH₃, -N(CH₃)C(CH₃)₂CONH₂, -N(CH₃)CH₂CH₂S(O)₂CH₃, -NO₂, =O, -OH, -OCH₃, -OCH₂CH₃, -OCH₂CH₂OCH₃, -OCH₂CH₂OH, -OCH₂CH₂N(CH₃)₂, -OP(O)(OH)₂, -S(O)₂N(CH₃)₂, -SCH₃, -S(O)₂CH₃, -S(O)₃H, ciclopropilo, oxetanilo, azetidinilo, 1-metilazetidin-3-il)oxi, N-metil-N-oxetan-3-ilamino, azetidin-1-ilmetilo y morfolino.
ARP120104128A 2011-11-03 2012-11-02 Compuestos de heteroaril piridona y aza-piridona AR088641A1 (es)

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