COMPUESTOS HETEROCICLICOS INHIBIDORES DE LAS PROTEINAS ANTI-APOPTOTICAS Bcl2

• Main Authors: BUI, CHINH THIEN, TAO, ZHI-FU, FLYGARE, JOHN A, DUDLEY, DANETTE A, NIKOLAKOPOULOS, GEORGE, WATSON, KEITH GEOFFREY, SLEEBS, BRAND EDMUND, COLMAN, PETER, LESSENE, GUILLAUME LAURENT, SMITH, BRIAN JOHN, NDUBAKU, CHUDI, WANG LE, HASVOLD, LISA A, WANG, XILU, ELMORE, STEVEN W, PETROS, ANDREW M, BAELL, JONATHAN BAYLDON, CZABOTAR, PETER, DESHAYES, KURT, FAIRBROTHER, WAYNE J, SOUERS, ANDREW J
• Format: Patent
• Language: Spanish
• Published: 16.04.2012
• Subjects: AGRICULTURE; ANIMAL HUSBANDRY; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES, AS HERBICIDES; FISHING; FORESTRY; HUMAN NECESSITIES; HUNTING; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS; PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTSTHEREOF; TRAPPING

REFERIDA A UN COMPUESTO DE FORMULA I, DONDE Q ES -CO, -CH2-, -CH(Ra)-, -C(Ra)2-; Ra ES ALQUILO C1-C4, HALOALQUILO C1-C4; R1 ES, SI ESTA PRESENTE, HALOGENO, =O, ALQUILO C1-C6, HALOALQUILO C1-C6, ENTRE OTROS; X1a, X1b Y X1c SON CADA UNO CH, N, C(OH), C(NH2), ENTRE OTROS; X1d ESTA AUSENTE O ES O, -NH, -N(ALQUILO C1-C4)-, -N(C(O)ALQUILO C1-C4); m ES 1-2; n ES 2-3; A ES DE PREFERENCIA BENZO[d]TIAZOL; B ES DE PREFERENCIA ACIDO 2(1H)-TIAZOL-4-CARBOXILICO; L ESTA AUSENTE O ES LIGADOR (ARILEN C6-C10)-(HETEROALQUILENO C1-C6), HETEROALQUILENO C1-C6, HALOALQUILENO C1-C6, -NH-, S, ENTRE OTROS; E ES DE PREFERENCIA H, HALOGENO. SON COMPUESTOS PREFERIDOS: ACIDO 2-(8-(BENZO[d]TIAZOL-2-ILCARBAMOIL)-3,4-DIHIDROIDOQUINOLIN-2(1H)-IL)-5-(3-(3-(TERBUTOXICARBONILAMINO)FENOXI)PROPIL)TIAZOL-4-CARBOXILICO; ACIDO 2-(8-(BENZO[d]TIAZOL-2ILCARBAMOIL)-3,4-DIHIDROISOQUINOLIN-2(1H)-IL)-5-(3-(4-(1-FENILCICLOPENTIL)FENOXI)PROPIL)TIAZOL-4-CARBOXILICO; ENTRE OTROS. DICHOS COMPUESTOS SON INHIBIDORES DE UN TIPO O SUBCONJUNTO DE PROTEINAS Bcl-2 ANTIAPOPTOTICAS UTILES EN EL TRTAMIENTO DE DEFERENTES TIPOS DE CANCER In one aspect, the present invention provides for a compound of Formula I in which the variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.