BAELL, JONATHON BAYLDON,BUI, CHIHN THIEN,COLMAN, PETER,DUDLEY, DANNETE A.,FAIRBROTHER, WAYNE J.,FLYGARE, JOHN A.,LASSENE, GUILLAUME LAURENT,NIKOLAKOPOULOS, GEORGE,RYE, CARL STEVEN,SLEEBS, BRAD EDMUND
申请号：
PE0012492011
公开号：
PE03052012A1
申请日:
2009.12.17
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Referring to a Heterocyclic Compound of formula (i), wherein R1 is alkyl of C1 - C6, alquenilo C2 - C6, halogen n is an integer from 0 to 2 x1 is CH2, o, S, SW, among others x2a, x2b and x2c are CR2 or R2 CH, N is CN, halogen, NO2, among others is a Group (1), (2), (3), among others R3 is C No, NO2, halogen, among others b is a Group (a) or (b) X3 is N (NH, C1 - C3 alkyl)S R4A is c1-c4 alkyl, halogen, alquinilo c2-c4, among others r4b is Halogen, NO2, CN, among others l is alquileno C1 - C6, alquenileno C2 - C6, NH, S, among others and it is H, halogen, phenyl, among others.Preferred compounds are: acid, 6 - (4 - (benzo [d] thiazole - 2 - ilcarbamoil) - 1 - methyl - 1,2,3,4 - tetrahidroquinoxalin - 6 - il) Picolinic Acid, 6 - (1 - (benzo [d] thiazole - 2 - ilcarbamoil) - 1,2,3,4 - tetrahidroquinolin - 7 - il) - 3 - (2 - phenoxyethoxy) Picolinic Acid, 6 - (1 - (benzo [d] thiazole - 2 - ilcarbamoil) - 1,2,3,4 - tetrahidroquinolin - 7 - (L) - 3 - (2 - (3 - (dimethylamino) ethoxy phenoxy) Picolinic), among others.It also relates to a Pharmaceutical composition. These compounds inhibit the activity of Proteins bcl-2 and BCL XL and are useful in the treatment of cancer, thrombocythemia, among othersREFERIDA A UN COMPUESTO HETEROCICLICO DE FORMULA (I), DONDE R1 ES ALQUILO C1-C6, ALQUENILO C2-C6, HALOGENO, ENTRE OTROS n ES UN ENTERO DE 0 A 2 X1 ES CH2, O, S, SO, ENTRE OTROS X2a, X2b Y X2c SON CH, CR2 O N R2 ES CN, HALOGENO, NO2, ENTRE OTROS A ES UN GRUPO (1), (2), (3), ENTRE OTROS R3 ES CN, NO2, HALOGENO, ENTRE OTROS B ES UN GRUPO (a) O (b) X3 ES NH, N(ALQUILO C1-C3), S R4a ES ALQUILO C1-C4, ALQUINILO C2-C4, HALOGENO, ENTRE OTROS R4b ES HALOGENO, NO2, CN, ENTRE OTROS L ES ALQUILENO C1-C6, ALQUENILENO C2-C6, NH, S, ENTRE OTROS E ES H, HALOGENO, FENILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ACIDO 6-(4-(BENZO[d]TIAZOL-2-ILCARBAMOIL)-1-METIL-1,2,3,4-TETRAHIDROQUINOXALIN-6-IL)PICOLINICO, ACIDO 6-(1-(BENZO[d]TIAZOL-2-ILCARBAMOIL)-1,2,3,4-TETRAHIDROQUINOLIN-7-IL)-3-(2-FENOXIETOX
