HENLIN, JEAN MICHEL,LE DIGUARHER, THIERRY,LE TIRAN, ARNAUD,GENESTE, OLIVIER,SZLAVIK, ZOLTAN,KOTSCHY, ANDRAS,NYERGES, MIKLOS,TATAI, JANOS,FEJES, IMRE,MEISSNER, JOHANNES W. G.,BROUGH, PAUL,DODSWORTH, MA
申请号：
PE0000232016
公开号：
PE02412016A1
申请日:
2014.07.22
申请国别(地区):
PE
年份:
2016
代理人:
摘要：
The Invention relates to compounds of formula (i) wherein: Het is heteroaryl T R3 is Hydrogen, alkyl, etc. is C1 - C6 R4 is aryl, etc. etc. etc. R6 R5 is Hydrogen, Hydrogen, etc.R7 R8 and R9 is Hydrogen, etc. are oxo group or Halogen, P and P are 0 - 4, Q and Q are 1 - 3.Preferred compounds are: N - (4-hydroxyphenyl) - N - methyl - 3 - {7 - [(3R) - 3 - methyl - 2 - 1,2,3,4 - tetrahidroisoquinolina carbonyl] - 2 - (phenylacetyl) - 1,2,3,4 - tetrahidroisoquinolin - il - 6 - 5,6,7},8 - tetrahydro - indolizina - 1 - carboxamide {1 - [6 - (4 - hydroxyphenyl) (methyl) Carbamoyl] - minutebug - tetrahidroindolizin} - 3 - il - 7 - [(3R) - 3 - methyl - 2 - 1,2,3,4 - tetrahidroisoquinolina carbonyl] - 1,2,3,Tetrahidroisoquinol ina 4 - phenyl - 2 - carboxylate, among others. It also relates to a process for the preparation of a compound of formula (i) and to a Pharmaceutical composition.These compounds are proapoptotic Property and are useful in the treatment of Cancer and autoimmune diseasesLa invencion se refiere a compuestos de formula (I) donde: Het es heteroarilo, T es hidrogeno, etc. R3 es alquilo C1-C6, etc. R4 es arilo, etc. R5 es hidrogeno, etc. R6 es hidrogeno, etc. R7 es hidrogeno, etc. R8 y R9 son grupo oxo o halogeno, p y p son 0-4, q y q son 1-3. Son compuestos preferidos: N-(4-Hidroxifenil)-N-metil-3-{7-[(3R)-3-metil-1,2,3,4-tetrahidroisoquinolina-2-carbonil]-2-(2-fenilacetil)-1,2,3,4-tetrahidroisoquinolin-6-il}-5,6,7,8-tetrahidro- indolizina-1-carboxamida 6-{1-[(4-Hidroxifenil)(metil)carbamoil]-5,6,7,8-tetrahidroindolizin-3-il}-7-[(3R)-3-metil-1,2,3,4-tetrahidroisoquinolina-2-carbonil]-1,2,3,4-tetrahidroisoquinol ina-2-carboxilato de fenilo, entre otros. Tambien se refiere a un proceso para la preparacion de un compuesto de formula (I) y a una composicion farmaceutica. Dichos compuestos tienen propiedad proapoptoticas y son utiles en el tratamiento de cancer y enfermedades autoinmunes
