ES2557930T3 - Compuestos de fenilaminopirimidina y usos de los mismos - Google Patents

Compuestos de fenilaminopirimidina y usos de los mismos Download PDF

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ES2557930T3
ES2557930T3 ES08714386.3T ES08714386T ES2557930T3 ES 2557930 T3 ES2557930 T3 ES 2557930T3 ES 08714386 T ES08714386 T ES 08714386T ES 2557930 T3 ES2557930 T3 ES 2557930T3
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Christopher John Burns
Andrew Craig Donohue
John Thomas Feutrill
Thao Lien Thi Nguyen
Andrew Frederick Wilks
Jun Zeng
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YM Biosciences Australia Pty Ltd
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    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

Un compuesto de fórmula Ib**Fórmula** en donde Z se selecciona independientemente entre N y CH; R1 se selecciona independientemente entre H, halógeno, OH, CONHR2, CON(R2)2, CF3, R2OR2, CN, morfolino, tiomorfolinilo, 1,1-dióxido de tiomorfolino, piperidinilo sustituido o no sustituido, piperazinilo sustituido o no sustituido, imidazolilo, pirrolidinilo sustituido o no sustituido y alquileno C1-4, en donde los átomos de carbono están opcionalmente reemplazados por NRY y/u O sustituidos con morfolino, tiomorfolinilo, 1,1-dióxido de tiomorfolino, piperidinilo sustituido o no sustituido, piperazinilo sustituido o no sustituido, imidazolilo o pirrolidinilo sustituido o no sustituido; R2 es alquilo C1-4 sustituido o no sustituido; RY es H o alquilo C1-4 sustituido o no sustituido; R8 es RXCN; RX es alquileno C1-4 sustituido o no sustituido, en donde hasta 2 átomos de carbono pueden estar opcionalmente reemplazados por CO, NSO2R1, NRy, CONRy, SO, SO2 u O; R11 es H o alquilo C1-4, en donde los sustituyentes se seleccionan entre el grupo que consiste en alquilo C1-4, cicloalquilo C3-6, alquenilo C2-6, alquinilo C2-6, alquilarilo C1-6, arilo, heterociclilo, halo, haloarilo, haloheterociclilo, hidroxi, alcoxi C1-4, ariloxi, carboxi, amino, alquilacilo C1-6, arilacilo, heterociclilacilo, acilamino, aciloxi, alquilsulfenilo C1-6, arilsulfonilo y ciano; o un enantiómero del mismo, un profármaco del mismo o una sal farmacéuticamente aceptable del mismo, en donde los profármacos se seleccionan entre * compuestos en donde un residuo de aminoácido o una cadena polipeptídica de dos o más residuos de aminoácidos están unidos covalentemente a través de un enlace peptídico a un grupo amino, hidroxi o ácido carboxílico libres de dicho compuesto de fórmula Ib; * compuestos en donde un carbonato, un carbamato, una amida o un éster de alquilo están unidos covalentemente a un grupo amino, amido, hidroxi o ácido carboxílico libres de dicho compuesto de fórmula Ib a través de una cadena lateral de carbono de carbonilo del profármaco; y * compuestos en donde un grupo hidroxilo libre de dicho compuesto de fórmula Ib está unido a través de un enlace fósforo-oxígeno a un derivado de fosfato de un compuesto (tal como un ácido, sal de ácido o éster).

Description

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El término "administración" debe entenderse que significa proporcionar un compuesto de la invención a un sujeto que necesita tratamiento.
La expresión "enfermedades asociadas a cinasas" se refiere a un trastorno o trastornos que son resultado directo o 5 indirecto o se agravan por la actividad cinasa anormal, en particular la actividad JAK, y/o que se alivian mediante la inhibición de una o más de estas enzimas cinasas.
En una realización preferida, la patología asociada a cinasas implica una o más de las cinasas JAK, JAK1, JAK2, JAK3 o TYK2. En una realización particularmente preferida, la enfermedad implica la cinasa JAK2. Dichas 10 enfermedades incluyen, pero no se limitan a, las enumeradas en la Tabla a continuación.
Activación de la vía JAK/STAT en diversas patologías
Tipo de enfermedad
Tipos celulares implicados Citocinas implicadas Cinasa JAK implicada Características
Atopia
Asma alérgica, dermatitis atópica (eccema), rinitis alérgica,
Mastocitos, eosinófilos, células T, células B, IL-4, IL-5, IL-6, IL-7, IL-13 JAK1, JAK2, JAK3, Tyk2 Activación de las células B por las células T seguida de la activación de mastocitos residentes y eosinófilos mediada por IgE
IMC
Dermatitis alérgica de contacto, neumonitis por hipersensibilidad
Células T, células B, macrófagos, neutrófilos IL-2, IL-4, IL-5, IL-6, IL-10, IFNγ, TNF, IL7, IL-13, JAK1, JAK2, JAK3, Tyk2 Activación de células B y/o TDH. Activación de macrófagos/granulocitos
Enfermedades autoinmunes
Esclerosis múltiple, glomerulonefritis, lupus eritematoso sistémico (LES), artritis reumatoide, artritis juvenil, síndrome de Sjögren, esclerodermia, polimiositis, espondilitis anquilosante, artritis psoriásica
células B, células T, monocitos, macrófagos, neutrófilos, mastocitos, eosinófilos, IL-2, IL-4, IL-5, IL-6, IL-7, IL-10, IL-13, IFNγ, TNF, GM-CSF; G-CSF, JAK1, JAK2, JAK3, Tyk2 Producción de citocinas (por ejemplo TNFα/β, IL-1, CSF-1, GM-CSF), activación de células T, activación de células B, activación de JAK/STAT
Trasplante
Rechazo de aloinjerto EICH
Células T, células B, macrófagos IL-2, IL-4, IL-5, IL-7, IL-13, TNF JAK1, JAK2, JAK3 Necrosis mediada por macrófagos/células T, apoptosis mediada por células Tc, opsonización/necrosis del injerto ajeno mediada por célula B/Ig
Enfermedades Virales
Virus de Epstein Barr (VEB)
Linfocitos Citocinas virales, IL-2, JAK1, JAK2, JAK3 Mediación de JAK/STAT
Hepatitis B
Hepatocitos
Hepatitis C
Hepatocitos
VIH
Linfocitos
VLTH 1
Linfocitos
Virus de la varicela-zoster (VVZ)
Fibroblastos
Virus del Papiloma Humano (VPH)
Células epiteliales
Enfermedades hiperproliferativas – cáncer
Leucemia
Leucocitos Varias citocinas autocrinas, Activación intrínseca JAK1, JAK2, JAK3 Producción de citocinas, activación de JAK/STAT
Linfoma
Linfocitos
Mieloma Múltiple
Varios
Cáncer de próstata
Varios
Cáncer de mama
Varios
Linfoma de Hodgkins
Varios
Leucemia linfocítica crónica de células B
Varios
Cáncer de pulmón
Varios
38
Hepatoma
Varios
Glioma melanoma metastásico
Varios
Enfermedades mieloproliferativas
Policitemia vera (PV), mielofibrosis primaria, trombocitemia, trombocitemia esencial (TE), mielofibrosis idiopática, leucemia mielógena crónica, mastocitosis sistémica (MS), leucemia neutrofílica crónica (LNC), síndrome mielodisplásico (SMD), la enfermedad mastocitaria sistémica (EMS)
Hematopoyéticas Interleucina-3, eritropoyetina, trombopoyetina Mutación de la JAK2 Activación de JAK/STAT
Enfermedad vascular
Hipertensión, hipertrofia, insuficiencia cardíaca, isquemia, hipertensión arterial pulmonar
Células endoteliales, células del músculo liso incluyendo células del músculo liso de la arteria pulmonar, miocitos cardiacos, fibroblastos, células endoteliales IL-6, angiotensina II, LIP, TNFα, serotonina, caveolina 1 JAK1, JAK2, TYK2 Activación de JAK/STAT
Enfermedad metabólica Obesidad, síndrome metabólico
Adipocitos, células pituitarias, neuronas, monocitos Leptina JAK2 Activación de JAK/STAT
La expresión "enfermedad inmunitaria e inflamatoria" se refiere a una enfermedad inmunitaria, inflamatoria o autoinmune, incluyendo, pero no limitada a, artritis reumatoide, poliartritis, espondilitis reumatoide, osteoartritis, gota, asma, bronquitis, rinitis alérgica, enfermedad pulmonar obstructiva crónica, fibrosis quística, enfermedad inflamatoria 5 intestinal, síndrome del intestino irritable, colitis mucosa, colitis ulcerosa, colitis diabética, enfermedad de Crohn, trastornos autoinmunes de la tiroides, gastritis, esofagitis, hepatitis, pancreatitis, nefritis, psoriasis, eczema, acné vulgaris, dermatitis, urticaria, esclerosis múltiple, enfermedad de Alzheimer, enfermedad neurodegenerativa (enfermedad de Lou Gehrig), enfermedad de Paget, sepsis, conjuntivitis, catarro renal, artrorreumatismo crónico, síndrome de respuesta inflamatoria sistémica (SRIS), polimiositis, dermatomiositis (DM), poliarteritis nodosa (PN),
10 trastorno mixto del tejido conectivo (EMTC), síndrome de Sjoegren, síndrome de Crouzon, acondroplasia, lupus eritematoso sistémico, esclerodermia, vasculitis, displasia tanatofórica, resistencia a la insulina, diabetes de tipo I y complicaciones de la diabetes y síndrome metabólico.
La expresión "enfermedades hiperproliferativas" incluye el cáncer y las patologías mieloproliferativas tales como las
15 patologías proliferativas celulares, incluyendo pero no limitadas a: Cardíacas: sarcoma (angiosarcoma, fibrosarcoma, rabdomiosarcoma, liposarcoma), mixoma, rabdomioma, fibroma, lipoma y teratoma; Pulmonares: carcinoma broncogénico (células escamosas, células pequeñas indiferenciadas, células grandes indiferenciadas, adenocarcinoma), carcinoma alveolar (bronquiolar), adenoma bronquial, sarcoma, linfoma, hamartoma condromatoso, mesotelioma; Gastrointestinales: esófago (carcinoma de células escamosas, adenocarcinoma,
20 leiomiosarcoma, linfoma), estómago (carcinoma, linfoma, leiomiosarcoma), páncreas (adenocarcinoma ductal, insulinorna, glucagonoma, gastrinoma, tumores carcinoides, vipoma), intestino delgado (adenocarcinoma, linfoma, tumores carcinoides, sarcoma de Kaposi, leiomioma, hemangioma, lipoma, neurofibroma, fibroma), intestino grueso (adenocarcinoma, adenoma tubular, adenoma velloso, hamartoma, leiomioma); Tracto genitourinario: riñón (adenocarcinoma, tumor de Wilms [nefroblastoma], linfoma, leucemia), vejiga y uretra (carcinoma de células
25 escamosas, carcinoma de células transicionales, adenocarcinoma ), próstata (adenocarcinoma, sarcoma), testículos (seminoma, teratoma, carcinoma embrionario, teratocarcinoma, coriocarcinoma, sarcoma, carcinoma de células intersticiales, fibroma, fibroadenoma, tumores adenomatoides, lipoma); Hepáticas: hepatoma (carcinoma hepatocelular), colangiocarcinoma, hepatoblastoma, angiosarcoma, adenoma hepatocelular, hemangioma; Óseas: sarcoma osteogénico (osteosarcoma), fibrosarcoma, histiocitoma fibroso maligno, condrosarcoma, sarcoma de
30 Ewing, linfoma maligno (sarcoma de células reticulares), mieloma múltiple, tumor maligno de las células gigantes, cordoma, osteocondroma (exostosis osteocartilaginosas), condroma benigno, condroblastoma, condromixofibroma, osteoma osteoide y tumores de las células gigantes, Sistema nervioso: cráneo (osteoma, hemangioma, granuloma, xantoma, osteítis deformante), meninges (meningioma, meningiosarcoma, gliomatosis), cerebro (astrocitoma,
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Claims (1)

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