AR089945A1 - DERIVADOS DE FURO[3,2-B] Y TIENO[3,2-B]PIRIDINA COMO MODULADORES DE TBK1 E IKKe - Google Patents

DERIVADOS DE FURO[3,2-B] Y TIENO[3,2-B]PIRIDINA COMO MODULADORES DE TBK1 E IKKe

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Publication number
AR089945A1
AR089945A1 ARP130100402A ARP130100402A AR089945A1 AR 089945 A1 AR089945 A1 AR 089945A1 AR P130100402 A ARP130100402 A AR P130100402A AR P130100402 A ARP130100402 A AR P130100402A AR 089945 A1 AR089945 A1 AR 089945A1
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Argentina
Prior art keywords
cyy
nyy
het1
denotes
hal
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ARP130100402A
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Dr Eggenweiler Hans
Michael-Dr Hoelzemann Guenter
Dr Dipl-Chem Dorsch Dieter
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Merck Patent Ges Mit Beschränkter Haftung
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Publication of AR089945A1 publication Critical patent/AR089945A1/es

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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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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
    • A61K31/436—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 oxygen as a ring hetero atom, e.g. rapamycin
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    • A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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Abstract

Los compuestos de la fórmula (1) en donde X denota O ó S; R¹ denota O(CYY)ₙHet¹, NY(CYY)ₙHet¹, O(CYY)ₙCyc o NY(CYY)ₙCyc; R² denota H, Hal, A, OY, NYY, O(CYY)ₘNYY, O(CYY)ₙHet², NY(CYY)ₘNYY, NY(CYY)ₙHet², Ar o Het²; Het¹ denota dihidropirrolilo, pirrolidinilo, tetrahidroimida-zolilo, dihidropirazolilo, tetrahidropirazolilo, tetrahidropiranilo, dihidropiridilo, tetrahidropiridilo, piperidinilo morfolinilo, hexahidropiridazinilo, hexahidropirimidinilo [1,3]dioxolanilo 2-oxa-6-aza-espiro[3,3]heptanilo, azepanilo, diazepanilo, tetrahidrofuranilo, furilo, tienilo, pirrolilo, imidazolilo, pirazolilo, oxazolilo, isoxazolilo, tiazolilo, piridilo, pirimidinilo, cromanilo o piperazinilo, cada uno de los cuales no está sustituido o está mono- o disustituido Hal, CN, A, COOA, OY, S(O)ₙA, S(O)ₙAr y/u =O (oxígeno del carbonilo); Het² denota un heterociclo saturado, insaturado o aromático mono-, bi- o tricíclico que tiene 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di-, tri-, tetra- o penta-sustituido con Hal, A, (CYY)ₚ-OY, -(CYY)ₚ-NYY, (CYY)ₚ-Het¹, NO₂, CN, (CYY)ₚ-COOY, CO-NYY, NY-COA, NY-SO₂A, SO₂-NYY, S(O)ₙA, -CO-Het¹, O(CYY)ₚ-NYY, -O(CYY)ₚ-Het¹, NH-COOA, NH-CO-NYY, NH-COO-(CYY)ₚ-NYY, NH-COO-(CYY)ₚ-Het¹, NH-CO-NH-(CYY)ₚ-NYY, NH-CO-NH(CYY)ₚ-Het¹, OCO-NH-(CYY)ₚ-NYY, OCO-NH-(CYY)ₚ-Het¹, CHO, COA, =S, =NY y/u =O; Ar denota fenilo, naftilo o bifenilo, cada uno de los cuales no está sustituido o que está mono-, di- o trisustituido con Hal, A, (CYY)ₚ-OY, (CYY)ₚ-NYY, (CYY)ₚ-Het¹, NO₂, CN, (CYY)ₚ-COOY, CO(CYY)ₚNH₂, CO-NYA, CONY(CYY)ₘNYCOOA, NY-COA, NY-SO₂A, SO₂-NYY, S(O)ₙA, CO-Het¹, O(CYY)ₚ-NYY, O(CYY)ₚ-Het¹, NH-COOA, NH-CO-NYY, NH-COO-(CYY)ₚ-NYY, NH-COO-(CYY)ₚ-Het¹, NH-CO-NH-(CYY)ₚ-NYY, NH-CO-NH(CYY)ₚ-Het¹, OCO-NH-(CYY)ₚ-NYY, OCO-NH-(CYY)ₚ-Het¹, CHO, CONY(CYY)ₚHet¹, CONH(CYY)ₚNHCOA y/o COA; Y denota H o alquilo C₁₋₄; A denota alquilo C₁₋₁₀ no ramificado o ramificado, en donde 1 - 7 átomos de H pueden estar reemplazados por F y/o Cl y/o en donde uno o dos grupos no adyacentes CH y/o CH₂ pueden estar reemplazados por O y/o N; Cyc denota cicloalquilo C₃₋₇, que no está sustituido o que está monosustituido con Hal, CN o A; Hal denota F, CI. Br o I; n denota 0, 1, ó 2; m denota 1, 2 ó 3; p denota 0,1, 2, 3 ó 4; y sus sales, tautómeros y estereoisómeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones. Son inhibidores de TBK1 e lKKe y se pueden emplear, inter alia, para el tratamiento de cáncer y enfermedades inflamatorias.
ARP130100402A 2012-02-09 2013-02-08 DERIVADOS DE FURO[3,2-B] Y TIENO[3,2-B]PIRIDINA COMO MODULADORES DE TBK1 E IKKe AR089945A1 (es)

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