DERIVADOS DE 8-CARBAMOIL-2-(2,3-PIRID-6-ILO DI SUSTITUIDO)-1,2,3,4-TETRAHIDROISOQUINOLINA COMO AGENTES INDUCTORES DE LA APOPTOSIS PARA EL TRATAMIENTO DEL CANCER Y ENFERMEDADES INMUNES Y AUTOINMUNES

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专利权人:

ABBVIE INC.

发明人:

WANG, LE,DOHERTY, GEORGE,WANG, XILU,TAO, ZHI-FU,BRUNKO, MILAN,KUNZER, AARON,WENDT, MICHAEL,SONG, XIAOHONG,FREY, ROBIN,HANSEN, TODD,SULLIVAN, GERARD,JUDD, ANDREW,SOUERS, ANDREW

申请号：

PE0005062014

公开号：

PE12822014A1

申请日:

2012.10.11

申请国别(地区):

PE

年份:

2014

代理人:

摘要：

Refers to compounds derived from 8 - carbamoyl - 2 - (2,3 - disubstituted pirid - 6 - yl) - 1,2,3,4 - tetrahidroisoquinolina of formula (i) where X is optionally substituted heteroaryl y1 is phenylene or heteroarileno (c5-c6) optionally one or two FUSED rings L1 is (cr6r7 (Q,) cr6r7) S - O - (R, cr6r7) Tre, where R6 and R7 are each h, NH2, NHC (NH2, OR)Among others Q is 1 to 3 S and R are each of 0 to 3 y2 is cycloalkyl (C8 (C14), heterocicloalquilo C8 C14), among others Z1 is Halogen, NO2, CN, among others r1 is alkyl, Halo, (C1 - C6), among others R2 is Halo, alquenilo (C2 - C6), among others R3 is Halo, alkyl (C1 - C6), alquinilo (C2 - C6), between Other M is 0 to 3 n is 0 to 6 p is 0 to 2.Preferred compounds are: Acid 6 - [8 - (benzothiazol-2-yl - 1.3 - 2 - ilcarbamoil) - 3,4 - dihidroisoquinolin - 2 (1H) - yl] - 3 - [1 - [tricyclo [3.3.1.13,7] dec - 1 - methyl] - 1h-pyrazol-4-yl} pyridin - 2 - carboxylic acid 6 - [8 - (benzothiazol-2-yl - 1.3 - 2 - ilcarbamoil) - 3,4 - dihidroisoquinolin - 2 (1H) - yl] - 3 - [1 - (3,5 Dimethyl tricyclo [3.3.1.13,7] d EC - 1 - methyl) - 1h-pyrazol-4-yl] pyridin - 2 - carboxylic acid among others.It also relates to a Pharmaceutical composition. These compounds are inhibitors of the activity of antiapoptotic Proteins BCL XL being useful in the treatment of bladder cancer, Lymphoblastic Leukemia, myelomaSE REFIERE A COMPUESTOS DERIVADOS DE 8-CARBAMOIL-2-(2,3-PIRID-6-ILO DISUSTITUIDO)-1,2,3,4-TETRAHIDROISOQUINOLINA DE FORMULA (I) DONDE X ES HETEROARILO OPCIONALMENTE SUSTITUIDO Y1 ES FENILENO O HETEROARILENO(C5-C6) OPCIONALMENTE FUSIONADO A UNO O DOS ANILLOS L1 ES (CR6R7)q, (CR6R7)s-O-(CR6R7)r, ENTRE OTROS, EN DONDE R6 Y R7 SON CADA UNO H, NH2, NHC(O)NH2, ENTRE OTROS q ES DE 1 A 3 s Y r SON CADA UNO DE 0 A 3 Y2 ES CICLOALQUILO(C8-C14), HETEROCICLOALQUILO(C8-C14), ENTRE OTROS Z1 ES HALOGENO, NO2, CN, ENTRE OTROS R1 ES HALO, ALQUILO(C1-C6), ENTRE OTROS R2 ES HALO, ALQUENILO(C2-C6), ENTRE OTROS R3 ES HALO, ALQUILO(C1-C6), ALQUINILO(C2-C

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