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PIRIMIDINAS FUSIONADAS COMO INHIBIDORES DE Akt
专利权人:
BAYER PHARMA AKTIENGESELLSCHAFT
发明人:
VENNEMANN, MATTHIAS RICHARD,BAR, THOMAS,MAIER, THOMAS,HOLDER, SWEN,BENEKE, GERRIT,DEHMEL, FLORIAN,ZULCH, ARMIN,STRUB, ANDREAS,BECKERS, THOMAS,INCE, STUART,REHWINKEL, HARTMUT,LIU, NINGSHU,BOMER, ULF
申请号:
PE0014852011
公开号:
PE05342012A1
申请日:
2010.02.02
申请国别(地区):
PE
年份:
2012
代理人:
摘要:
Referring to a pyrimidine Derivative of formula (i), where the Ring B is selected from (a), (b) and (c) r1 is H, c1-c4 alkyl, halogen, amino, among others R3 is H, c1-c4 alkyl, halogen, alkoxy c1-c4 R4 it is tienilo pyridinyl, phenyl, thiazolyl, among others R5 is H, c1-c4 alkyl, halogen,Among others, R6 H or c1-c4 alkyl R7 is - W and - W is a heteroarileno monociclico bicyclic or 5 or 6 members comprising a nitrogen Atom and optionally 1, 2 or 3 additional heteroatoms such as n, s and, optionally substituted with R8 R8 is H, alkyl C1 - C4, C3 - C7 cycloalkyl, And H, among othersAryl or heteroaryl monociclico 5 or 6 members that includes one nitrogen Atom and optionally 1, 2 or 3 heteroatoms such as o, N and S, optionally substituted with R9 and r9a R9 is c1-c4 alkyl, halogen, alkoxy c1-c4, among others r9a is c1-c4 alkyl or Halogen n and M is 1 or 2.Preferred compounds are: 6 - phenyl - 7 - (4 - [3 - (5 - (pyridin-2-yl - 1,2,4 - triazole - 3 - il - 1, il azetidin) - phenyl] methyl}) imidazo [1,2-a] pyrimidine, 2 - methyl - 4 - phenyl - (4 - 5 - [3 - (5 - (pyridin-2-yl - 1,2,4 - triazole - 3 - il) azetidin IL - 1 - methyl) phenyl]} [1,2,4] triazolo [1,5-a] pyrimidine, among others. It also relates to a Pharmaceutical Composition and a preparation method.These compounds are inhibitors of Protein Kinases and Akt are useful in the treatment of cancerREFERIDA A UN DERIVADO DE PIRIMIDINA DE FORMULA (I), DONDE EL ANILLO B SE SELECCIONA DE (a), (b) Y (c) R1 ES H, ALQUILO C1-C4, HALOGENO, AMINO, ENTRE OTROS R3 ES H, ALQUILO C1-C4, HALOGENO, ALCOXI C1-C4 R4 ES FENILO, TIENILO, PIRIDINILO, TIAZOLILO, ENTRE OTROS R5 ES H, ALQUILO C1-C4, HALOGENO, ENTRE OTROS R6 ES H O ALQUILO C1-C4 R7 ES -W-Y W ES UN HETEROARILENO MONOCICLICO O BICICLICO DE 5 O 6 MIEMBROS QUE COMPRENDE UN ATOMO DE NITROGENO Y OPCIONALMENTE 1, 2 O 3 HETEROATOMOS ADICIONALES TALES COMO O, S Y N, OPCIONALMENTE SUSTITUIDOS CON R8 R8 ES H, ALQUILO C1-C4, CICLOALQUILO C3-C7, ENTRE OTROS Y ES H, ARILO O HETEROARILO M
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