AR094982A1 - Derivados de triazolo[4,5-d]pirimidina - Google Patents

Derivados de triazolo[4,5-d]pirimidina

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Publication number
AR094982A1
AR094982A1 ARP140100697A ARP140100697A AR094982A1 AR 094982 A1 AR094982 A1 AR 094982A1 AR P140100697 A ARP140100697 A AR P140100697A AR P140100697 A ARP140100697 A AR P140100697A AR 094982 A1 AR094982 A1 AR 094982A1
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AR
Argentina
Prior art keywords
phet1
mono
denotes
oconh
nhcoo
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ARP140100697A
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English (en)
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Dr Dorsch Dieter
Dr Hoelzemann Guenter
Dr Calderini Michel
Dr Wegener Ansgar
Dr Poeschke Oliver
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Merck Patent Ges Mit Beschränkter Haftung
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Publication of AR094982A1 publication Critical patent/AR094982A1/es

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Abstract

Reivindicación 1: Compuestos de la fórmula (1), en donde R¹ denota Ar o Het; R² denota alquilo no ramificado o ramificado C₁₋₇, en donde dos átomos de carbono adyacentes pueden formar un enlace doble o triple y que puede estar mono-, di-, tri-, tetra- o pentasustituido con Hal y/o que puede estar mono- o disustituido con OR³, N(R³)₂, Het¹, CN, COOR³, OCOOR³, CONH₂, CONHA, CONA₂, NR³COA, NR³SO₂A, SO₂N(R³)₂, S(O)ₙA, COHet¹, O[C(R³)₂]ₘN(R³)₂, O[C(R³)₂]ₚHet¹, NHCOOA, NHCON(R³)₂, NHCOO[C(R³)₂]ₘN(R³)₂, NHCOO[C(R³)₂]ₚHet¹, NHCONH[C(R³)₂]ₘN(R³)₂, NHCONH[C(R³)₂]ₚHet¹, OCONH[C(R³)₂]ₘN(R³)₂, OCONH[C(R³)₂]ₚHet¹, y/o COA, o denota cicloalquilo C₃₋₇ o ciclopentenilo, cada uno de los cuales puede estar mono-, di-, tri-, tetra- o pentasustituido con A y/o Hal y/o que puede estar mono- o disustituido con [C(R³)₂]ₚOR³, O[C(R³)₂]ₚOR³, [C(R³)₂]ₚN(R³)₂, O[C(R³)₂]ₚN(R³)₂, [C(R³)₂]ₚAr, [C(R³)₂]ₚHet¹, O[C(R³)₂]ₚHet¹, CN, [C(R³)₂]ₚCOOR³, O[C(R³)₂]ₚCOOR³, CONH₂, CONHA, CONA₂, [C(R³)₂]ₚNR³COA, CONR³SO₂A, NR³SO₂A, SO₂N(R³)₂, S(O)ₙA, COHet¹, O[C(R³)₂]ₘN(R³)₂, [C(R³)₂]ₚNR³COOA, [C(R³)₂]ₚNR³COOCH₂Ph, NR³CON(R³)₂, NHCOO[C(R³)₂]ₘN(R³)₂, NHCOO[C(R³)₂]ₚHet¹, NHCONH[C(R³)₂]ₘ N(R³)₂, NHCONH[C(R³)₂]ₚHet¹, OCONH[C(R³)₂]ₘN(R³)₂, OCONH[C(R³)₂]ₚHet¹, CONH(CH₂)ₚHet², CONR³NR³COA, CONR³N(R³)₂, CONHCyc, COA, S, =NR³ y/u =O, o denota piperidinilo, tetrahidropiranilo, pirrolidinilo, azetidinilo, tiolanilo, oxetanilo, 3-aza-biciclo[3,1,0]hexilo, tetrahidrotiofenilo, tetrahidrotiopiranilo, 4,5,6,7-tetrahidro-1H-indazol-5-ilo, 4,5,6,7-tetrahidro-1H-indazol-6-ilo, tetrahidropirazolilo, tetrahidrofuranilo o hexahidropiridazinilo, cada uno de los cuales puede estar mono-, di-, tri-, tetra- o pentasustituido con A y/o Hal y/o que puede estar mono- o disustituido con [C(R³)₂]ₚOR³, O[C(R³)₂]ₚOR³, [C(R³)₂]ₚN(R³)₂, [C(R³)₂]ₚAr, [C(R³)₂]ₚHet¹, [C(R³)₂]ₚHet3, CN, [C(R³)₂]COOR³, CO[C(R³)₂]ₚN(R³)₂, CO[C(R³)₂]ₚHet¹, CO[C(R³)₂]ₚHet3, NR³COA, NR³SO₂A, SO₂N(R³)₂, S(O)ₙA, COHet¹, O[C(R³)₂]ₘN(R³)₂, O[C(R³)₂]ₚHet¹, NHCOOA, NHCON(R³)₂, NHCOO[C(R³)₂]ₘN(R³)₂, NHCOO[C(R³)₂]ₚHet¹, NHCONH[C(R³)₂]ₘN(R³)₂, NHCONH[C(R³)₂]ₚHet¹, OCONH[C(R³)₂]ₘN(R³)₂, OCONH[C(R³)₂]ₚHet¹, C(O)R³, =S, =NR³ y/u =O; R³ denota H o alquilo no ramificado o ramificado C₁₋₆; Ar denota fenilo o naftilo, cada uno de los cuales no está sustituido o está mono-, di- o trisustituido con Hal, A, [C(R³)₂]ₚOR³, O[C(R³)₂]ₚOR³, [C(R³)₂]ₚN(R³)₂, O[C(R³)₂]ₚN(R³)₂, [C(R³)₂]ₚHet¹, [C(R³)₂]ₚHet3, NO₂, CN, [C(R³)₂]ₚCOOR³, O[C(R³)₂]ₚCOOR³, CON(R³)₂, NR³COA, NR³SO₂A, SO₂N(R³)₂, S(O)ₙA, COHet¹, O[C(R³)₂]ₚHet¹, NHCOOA, NHCON(R³)₂, NHCOO[C(R³)₂]ₘN(R³)₂, NHCOO[C(R³)₂]ₚHet¹, NHCONH[C(R³)₂]ₘN(R³)₂, NHCONH[C(R³)₂]ₚHet¹, OCONH[C(R³)₂]ₘN(R³)₂, OCONH[C(R³)₂]ₚHet¹, S(O)ₙHet¹, CHO y/o COA, o denota azulenilo; Het denota furilo, tienilo, pirrolilo, imidazolilo, pirazolilo, oxazolilo, isoxazolilo, oxadiazolilo, tiazolilo, triazolilo, tetrazolilo, piridilo, pirimidilo, piridazinilo, pirazinilo, indolilo, isoindolilo, bencimidazolilo, indazolilo, indolizinilo, cinnolinilo, quinolilo, isoquinolilo, benzoxazolilo, 1,3-benzodioxolilo, benzotiofenilo, benzofuranilo, imidazopiridilo, dihidroindolilo, quinoxalinilo, imidazo[1,2-a]piridinilo, benzo[1,2,5]tiadiazolilo, naftiridinilo, 2,3-dihidro-benzo[1,4]dioxinilo, quinazolinilo, benzotiazolilo o furo[3,2-b]piridilo, cada uno de los cuales no está sustituido o está mono- o disustituido con Hal, A, [C(R³)₂]ₚOR³, O[C(R³)₂]ₚOR³, [C(R³)₂]ₚ N(R³)₂, O[C(R³)₂]ₚN(R³)₂, [C(R³)₂]ₚHet¹, NO₂, [C(R³)₂]ₚ CN, [C(R³)₂]ₚCOOR³, O[C(R³)₂]ₚCOOR³, [C(R³)₂]ₚCON(R³)₂, NR³COA, NR³SO₂A, SO₂N(R³)₂, S(O)ₙA, COHet², O[C(R³)₂]ₚHet², NHCOOA, NHCON(R³)₂, NHCOO[C(R³)₂]ₘN(R³)₂, NHCOO[C(R³)₂]ₚHet², NHCONH[C(R³)₂]ₘN(R³)₂, NHCONH[C(R³)₂]ₚHet², OCONH[C(R³)₂]ₘN(R³)₂, OCONH[C(R³)₂]ₚHet², S(O)ₙHet², CHO, COA, =S y/u =O; Het¹ denota pirazolilo, piridazinilo, piridinilo, oxazolilo, isoxazolilo, oxadiazolilo, pirazinilo, indolilo, dihidropirrolilo, pirrolidinilo, azetidinilo, oxetanilo, tetrahidroimidazolilo, dihidropirazolilo, tetrahidropirazolilo, tetrahidrofuranilo, dihidropiridilo, tetrahidropiridilo, piperidinilo, morfolinilo, hexahidropiridazinilo, hexahidropirimidinilo, [1,3]dioxolanilo, tetrahidropiranilo o piperazinilo, cada uno de los cuales no está sustituido o está mono- o disustituido con Hal, A, [C(R³)₂]ₚOR³, O[C(R³)₂]ₚOR³, [C(R³)₂]ₚN(R³)₂, [C(R³)₂]ₚHet², NO₂, [C(R³)₂]ₚCN, [C(R³)₂]ₚCOOR³, O[C(R³)₂]ₚCOOR³, [C(R³)₂]ₚCON(R³)₂, NR³COA, NR³SO₂A, SO₂N(R³)₂, S(O)ₙA, COHet², O[C(R³)₂]ₘN(R³)₂, O[C(R³)₂]ₚHet², NHCOOA, NHCON(R³)₂, NHCOO[C(R³)₂]ₘN(R³)₂, NHCOO[C(R³)₂]ₚ Het², NHCONH[C(R³)₂]ₘN(R³)₂, NHCONH[C(R³)₂]ₚHet², OCONH[C(R³)₂]ₘN(R³)₂, OCONH[C(R³)₂]ₚHet², S(O)ₙHet², CHO, COA, =S y/u =O; Het² denota pirazolilo, oxadiazolilo, piridinilo, triazolilo, tetrazolilo, piridazinilo, pirrolidinilo, azetidinilo, azoxetanilo, tetrahidroimidazolilo, tetrahidropirazolilo, tetrahidrofuranilo, piperidinilo, morfolinilo, tetrahidropiranilo o piperazinilo, cada uno de los cuales no está sustituido o está mono- o disustituido con Hal, A, OA, CN, COOA, CONH₂, S(O)ₙA, S(O)ₙAr, COA y/u =O; Het³ denota pirazolilo, piridinilo, pirimidinilo o pirazinilo, cada uno de los cuales no está sustituido o está mono- o disustituido con Hal, A, [C(R³)₂]ₚOR³, O[C(R³)₂]ₚOR³, [C(R³)₂]ₚN(R³)₂, [C(R³)₂]ₚHet², NO₂, CN, [C(R³)₂]ₚCOOR³, O[C(R³)₂]ₚCOOR³, CON(R³)₂, NR³COA, NR³SO₂A, SO₂N(R³)₂, S(O)ₙA, COHet², O[C(R³)₂]ₘN(R³)₂, O[C(R³)₂]ₚHet², NHCOOA, NHCON(R³)₂, NHCOO[C(R³)₂]ₘN(R³)₂, NHCOO[C(R³)₂]ₚHet², NHCONH[C(R³)₂]ₘN(R³)₂, NHCONH[C(R³)₂]ₚHet², OCONH[C(R³)₂]ₘN(R³)₂, OCONH[C(R³)₂]ₚHet², S(O)ₙHet², CHO, COA, =S y/u =O; Cyc es cicloalquilo C₃₋₇, que puede estar mono- o disustituido con OH; Ph denota fenilo; A denota alquilo no ramificado o ramificado C₁₋₁₀, en donde uno, dos o tres grupos CH y/o CH₂ no adyacentes pueden estar reemplazados por átomos de N, O y/o S y en donde 1 - 7 átomos de H pueden estar reemplazados por OH, F y/o Cl; Hal denota F, Cl, 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 solvatos, sales, tautómeros y estereoisómeros farmacéuticamente aceptables, incluyendo su mezclas en todas las proporciones.
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