Abstract:
PROBLEM TO BE SOLVED: To provide a novel triazolopyridine compound having a PIM kinase inhibition effect and useful for treatment of cancer, autoimmune disease, inflammatory disease and the like.SOLUTION: There is provided a compound represented by the formula I or pharmaceutically acceptable salt thereof. I, where A represents a C1 to 3 alkyloxy substituted by 4 to 7-membered heterocycle and the like, a C1 to 6 alkyloxy substituted by amino and the like, an amino substituted by 4 to 7-membered heterocycle and the like, and the like, B, Rto Rand Rare each independently H, F, Me and the like. cis-3-fluoropiperidine-4-yloxy, piperidine-3-ylmethoxy, 3-amino-2,2-dimethylpropane-1-yloxy, (piperidine-4-yl)amino and the like are preferable as the A.
Abstract:
Compounds of Formula I and II: I II having the chemical names cis-6-fluoro-8-(3-fluoropiperidin-4-yloxy)-2-(7-(2-methoxyethoxy)imidazo[1,2-a]pyridin-3-yl)quinoline and 6-fluoro-8-(trans-3-fluoropiperidin-4-yloxy)-2-(7-(2-methoxyethoxy)imidazo[1,2-a]pyridin-3-yl)quinoline, respectively, and enantiomers and pharmaceutically acceptable salts thereof, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class 3 and class 5 receptor tyrosine kinases. The compounds of this invention have also been found to be inhibitors of Pim-1.
Abstract:
This invention provides compounds of Formula (I), wherein B, G, A, E, R 1 , R 2 , R 3 , m and n are as defined herein, which are useful as type I receptor tyrosine kinase inhibitors, and methods of use thereof in the treatment of hyperproliferative disorders in mammals.
Abstract:
This invention provides compounds of Formula (I), wherein B, G, A, E, R 1 , R 2 , R 3 , m and n are as defined herein, which are useful as type I receptor tyrosine kinase inhibitors, and methods of use thereof in the treatment of hyperproliferative disorders in mammals.
Abstract:
ΗεφεύρεσηαυτήπαρέχειενώσειςτουΤύπου (I), όπουΒ, G, Ε, το R1, το R2, το R3, m και n είναιόπωςορίζονταιεδώ, οιοποίεςείναιχρήσιμεςωςαναστολείςυποδοχέακινάσηςτυροσίνηςτύπου I καιμεθόδουςχρήσηςαυτώνστηθεραπείαυπερπολλαπλασιαστικώνδιαταραχώνσεθηλαστικά.
Abstract:
Compounds of Formula (I), in which A, B, R1, R1a, R2, R3, R4, R5, R6, and R7 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of immune cell-associated diseases and disorders, such as inflammatory and autoimmune diseases.
Abstract:
Compuesto que tiene la fórmula general I o una sal farmacéuticamente aceptable del mismo, en el que: R1 es hetAr1CH2-, hetAr2CH2-, (cicloalquilo C3-6)-CH2-, tetrahidropiranilCH2-, bencilo que está opcionalmente sustituido con alcoxi(C1-4), o (N-alquilo C1-3)piridinonil-CH2- que está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de alquilo(C1-6); hetAr1 es piridilo opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de entre alquilo(1-6C), alcoxi(C1-4), halógeno, hetCyc1, hetCyc1-CH2-, aminoalcoxi(C2-4), [di(alquil C1- 3)amino]alcoxi(C2-4), dihidroxialcoxi(C3-4), hetCyc2O-, hetCyc2a15 alcoxi(C1-2) y OH; hetCyc1 es un heterociclo de 6 miembros que tiene 1-2 átomos de N anulares, y opcionalmente sustituido con NH2; hetCyc2 y hetCyc2a 20 son independientemente un heterociclo de 5-6 miembros que tiene 1-2 átomos de N anulares y opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de alquilo(C1-6), OH, y halógeno; hetAr2 es un anillo heteroarílico de 5 miembros que tiene 2-3 heteroátomos anulares seleccionados independientemente de entre N, S y O en el que al menos uno de dichos heteroátomos es N, en el que dicho anillo está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de entre alquilo(C1-6), hidroxialquilo(C2-4), dihidroxialquilo(C3-4), (cicloalquilo C3-6)CH2-, hetCyc3, hetCyc3aalquilo(C1-2), y bencilo opcionalmente sustituido con alcoxi(C1-4); hetCyc3 y hetCyc3a son independientemente un anillo heterocíclico de 6 miembros que tiene 1-2 átomos de N anulares y opcionalmente sustituido con un halógeno; R2 es alquilo(C2-4), ciclopropilo, OMe, I o Br; R3 es H o Cl; R4 es H o CN; R5 es H, halógeno, OH, hetAr3, hetAr4, N-(alquilo C1-3)piridinona, hetAr5, hetCyc4, hetCyc5C(>=O)-, hetCyc6(alquilo C1-4)-, hetCyc7alcoxi(C1-4), (hetCyc8)-O-, hetCyc940 alcoxi(C1-4), (alcoxi C1-3)alcoxi(C1-4), hidroxialcoxi(C1-4), dihidroxialcoxi(C2-4), difluoroaminoalcoxi(C1-4), [di(alquil C1-3)amino]alcoxi(C1-4), [(alcoxi C1-4)carbonilamida]difluoroalcoxi(C1-4), (alquilo C1-4)C(>=O)NHalquiltio(C2-4)-, (alquilo C1-4)OC(>=O)-, (alquilo C1-4)C(>=O)-, hidroxialquilo(C1-4), [hidroxialquil(C2-4))amino]-alquilo(C1-4), [(alcoxi C1-4)(alquilo C1- 4)amino]alquilo(C1-4), [di(alquilo C1-4)amino]alquilo(C1-4), R'R"NC(>=O)-, alquiltio C1-6, benciloxi, [hidroxialcoxi(C1-4)]alcoxi(C1-4), o [(alqueniloxi C2-4)alcoxi(C1-4)]alcoxi(C1-4).