AR096149A1 - Macrociclos como inhibidores de quinasa - Google Patents

Macrociclos como inhibidores de quinasa

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Publication number
AR096149A1
AR096149A1 ARP140101780A ARP140101780A AR096149A1 AR 096149 A1 AR096149 A1 AR 096149A1 AR P140101780 A ARP140101780 A AR P140101780A AR P140101780 A ARP140101780 A AR P140101780A AR 096149 A1 AR096149 A1 AR 096149A1
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Argentina
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phet1
oconh
nhcoo
nhconh
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ARP140101780A
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Dr Hoelzemann Guenter
Dr Dorsch Dieter
Dr Wegener Ansgar
Dr Poeschke Oliver
Dr Busch Michael
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Merck Patent Ges Mit Beschränkter Haftung
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Publication of AR096149A1 publication Critical patent/AR096149A1/es

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Abstract

Reivindicación 1: Compuestos de la fórmula (1) en donde X denota N o CH; Y denota Het-diilo o Ar; Q¹ denota (CH₂)ₙ, O(CH₂)ₙ o (CH₂)ₙHet¹-diílo; M denota (CH₂)ₚNR³CO, CONR³, NR³ o CO; Q² denota (CH₂)ₙO o (CH₂)ₙ; B denota Ar o Het-diilo; Het denota furano, tiofeno, pirrol, imidazol, pirazol, oxazol, isoxazol, oxadiazol, tiazol, triazol, tetrazol, piridina, pirimidina, piridazina, pirazina, indol, isoindolindolina, bencimidazol, indazol, quinolina, isoquinolina, benzoxazol, 1,3-benzo dioxol, benzotiofeno, benzofurano, imidazopiridina, dihidroindol, quinoxalina, benzo[1,2,5]tiadiazol o furo[3,2-b]piridina, cada uno de los cuales no está sustituido o está mono- o disustituido con Hal, A, [C(R³)₂]ₚOR³, [C(R³)₂]ₚN(R³)₂, [C(R³)₂]ₚHet¹, NO₂, CN, [C(R³)₂]ₚCOOR³, CON(R³)₂, 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), 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, CHO, COA, =S, =NR³ y/u =O; Ar denota fenileno, que no está sustituido o que 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, NO₂, CN, [C(R³)₂]ₚCOOR³, O[C(R³)₂]ₚCOOR³, CON(R³)₂, NR³COA, NR³SO₂A, SO₂N(R³)₂, S(O)₂A, 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)₂Het¹, CHO y/o COA; Het¹ denota dihidropirrol, pirrolidina, azetidina, oxetano, tetrahidroimidazol, dihidropirazol, tetrahidropirazol, tetrahidrofurano, dihidro piridina, tetrahidropiridina, piperidina, morfolina, hexahidropiridazina, hexahidropirimidina, [1,3]dioxolano, tetrahidropirano o piperazina, que no está sustituido o que está mono- o disustituido con Hal, CN, OH, OA, COOA, CONH₂, S(O)₂A, S(O)₂Ar, COA, A y/u =O; A denota alquilo no ramificado o ramificado con 1 - 10 átomos de C, en donde uno o dos grupos no adyacentes CH y/o CH₂ pueden estar reemplazados por átomos de N, O y/o S y en donde 1 - 7 átomos de H pueden estar reemplazados por F o Cl; R³ denota H o alquilo con 1, 2, 3 ó 4 átomos de C; Hal denota F, Cl, Br o I; n denota 1, 2, 3, 4 ó 5; m denota 1, 2 ó 3; p denota 0, 1, 2, 3 ó 4; y sus solvatos, sales, tautómeros y estereoisómeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones.
ARP140101780A 2013-05-06 2014-04-30 Macrociclos como inhibidores de quinasa AR096149A1 (es)

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EP (1) EP2994471B1 (es)
JP (1) JP6401247B2 (es)
CN (1) CN105164136B (es)
AR (1) AR096149A1 (es)
AU (1) AU2014264973B2 (es)
CA (1) CA2911259A1 (es)
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CN105164136B (zh) 2017-12-22
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ES2637721T3 (es) 2017-10-16
US9861635B2 (en) 2018-01-09
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CA2911259A1 (en) 2014-11-13
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