BRADBURY, ROBERT HUGH,CARR, GREGORY RICHARD,RABOW, ALFRED ARTHUR,RAO KORUPOJU, SRINIVASA,TUMMA, HARIKRISHNA
申请号：
PE0014692011
公开号：
PE06032012A1
申请日:
2010.02.08
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Refers to compounds derived from [4,3-b] triazolo pyridazine hydrochloride of formula (i) wherein R1 is haloalquilo (c1-c4) K is from 0 to 2 n and P are each 1 or 2 and is n, C, CH or COH Dashed Lines are single or Double Link L1 is a direct link (cr3r4), - T, - S, - S (o) -, among others, where R3 and R4 are each H or Methyl t is 1 to 3 J is aryl, cycloalkyl (C3, C6)A Heterocyclic Ring of 4 to 7 members, among others L2 is a direct link - (OR) - S, - S (o) 2 -, among others R2 is alkyl, Halo, (C1 - C6), CN, amino, carboxy, among others R is 0 to 3.Preferred compounds are: 6 - [4 - (4-fluorobenzyl) piperazin-1-yl] - 3 - (trifluoromethyl) - 7.8 -] [1,2,4] triazolo [4,3-b] pyridazine hydrochloride 6 - [4 - (1h indole - 3 - yl) - 3.6 - dihidropiridin (2H) - 1 - il] - 3 - (trifluoromethyl) - 7.8 -] [1,2,4] triazolo [4,3-b] pyridazine hydrochloride 2 - (4 - (4 - [2 - (4 - acetilpiperazin - 1 - il) ethoxy] piperidin yl} 1 - il) - 3 - (trifluoromethyl) - 7.8 -] [1,2,4] triazolo [4,3-b] pyridazine hydrochloride among others.It also relates to a preparation method and a Pharmaceutical composition. These compounds are ligands of the androgen receptor (AR) to be useful in the treatment of Prostate CancerSE REFIERE A COMPUESTOS DERIVADOS DE TRIAZOLO[4,3-b]PIRIDAZINA DE FORMULA (I) DONDE R1 ES HALOALQUILO(C1-C4) k ES DE 0 A 2 n Y p SON CADA UNO 1 O 2 Y ES N, C, CH O COH LAS LINEAS PUNTEADAS SON UN ENLACE SIMPLE O DOBLE L1 ES UN ENLACE DIRECTO, -(CR3R4)t-, -S-, -S(O)-, ENTRE OTROS, EN DONDE R3 Y R4 SON CADA UNO H O METILO t ES DE 1 A 3 J ES ARILO, CICLOALQUILO(C3-C6), UN ANILLO HETEROCICLICO DE 4 A 7 MIEMBROS, ENTRE OTROS L2 ES UN ENLACE DIRECTO, -S(O)-, -S(O)2-, ENTRE OTROS R2 ES HALO, ALQUILO(C1-C6), CARBOXI, CN, AMINO, ENTRE OTROS r ES DE 0 A 3. SON COMPUESTOS PREFERIDOS: 6-[4-(4-FLUOROBENCIL)PIPERAZIN-1-IL]-3-(TRIFLUOROMETIL)-7,8-DIHIDRO[1,2,4]TRIAZOLO[4,3-b]PIRIDAZINA 6-[4-(1H-INDOL-3-IL)-3,6-DIHIDROPIRIDIN-1(2H)-IL]-3-(TRIFLUOROMETIL)-7,8-DIHIDRO[1,2,4]TRIAZOLO[4,3-b]PIRIDA
