LE DIGUARHER, THIERRY,CASARA, PATRICK,STARCK, JEROME BENOIT,HENLIN, JEAN-MICHEL,DAVIDSON, JAMES EDWARD PAUL,MURRAY, JAMES BROOKE,GRAHAM, CHRISTOPHER JOHN,CHEN, I-JEN,GENESTE, OLIVIER,HICKMAN, JOHN,DEP
申请号：
PE0010762014
公开号：
PE14052014A1
申请日:
2013.01.23
申请国别(地区):
PE
年份:
2014
代理人:
摘要：
Indolizina refers to compounds of formula (i) where X and y are each C o n Het is a Aromatic Cycle or 5 to 7 members each R1 and R2 is H, alkyl (C1 - C6), among others R3 is alkyl (C1 - C6), alquenilo (C2 - C6), cycloalkyl, among others R4 is aryl, heteroaryl, cicloalq Uilo, among others R5 is H or Halogen ra, RB, RC and Rd are each Halogen, alkyl (C1 - C6)Alkoxy (C1 - C6), Hydroxy, among others.Preferred compounds are: N - (4-hydroxyphenyl) - 3 - [6 - [(3S) - 3 - (4 - morfolinilmetil) - 3,4-dihydro - 2 (1H) - isoquinolinil) carbonyl] - 1,3-benzodioxol-5-yl} - N - phenyl - 5,6,7,8-tetrahydro - 1 - indolizina carboxamide 3 - {5-chloro-2 - [(3S) - 3 - (4 - morfolinilmetil) - 3,4-dihydro - 2 (1H) - isoquinolinil) carbonyl] phenyl) - N - (4 - hydrous Ifenil) - N - (1 - methyl) - 1H indole - 5 - yl) - 5,6,7,8-tetrahydro - 1 - indolizina carboxamide among others.It also relates to a preparation method and a Pharmaceutical composition. These compounds are inhibitors of anti apoptotic activity of bcl-2 Proteins being useful in the treatment of Leukemia, melanoma, non small cell lung cancerSE REFIERE A COMPUESTOS DERIVADOS DE INDOLIZINA DE FORMULA (I) DONDE X E Y SON CADA UNO C O N HET ES UN CICLO AROMATICO O NO DE 5 A 7 MIEMBROS R1 Y R2 SON CADA UNO H, ALQUILO(C1-C6), ENTRE OTROS R3 ES ALQUILO(C1-C6), ALQUENILO(C2-C6), CICLOALQUILO, ENTRE OTROS R4 ES ARILO, HETEROARILO, CICLOALQUILO, ENTRE OTROS R5 ES H O HALOGENO Ra, Rb, Rc Y Rd SON CADA UNO HALOGENO, ALQUILO(C1-C6), ALCOXI(C1-C6), HIDROXI, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-(4-HIDROXIFENIL)-3-{6-[((3S)-3-(4-MORFOLINILMETIL)-3,4-DIHIDRO-2(1H)-ISOQUINOLINIL)CARBONIL]-1,3-BENZODIOXOL-5-IL}-N-FENIL-5,6,7,8-TETRAHIDRO-1-INDOLIZINA CARBOXAMIDA 3-{5-CLORO-2-[((3S)-3-(4-MORFOLINILMETIL)-3,4-DIHIDRO-2(1H)-ISOQUINOLINIL)-CARBONIL]FENIL}-N-(4-HIDROXIFENIL)-N-(1-METIL-1H-INDOL-5-IL)-5,6,7,8-TETRAHIDRO-1-INDOLIZINA CARBOXAMIDA ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DI
