BRADBURY, ROBERT HUGH,CARR, GREGORY RICHARD,RABOW, ALFRED ARTHUR,RAO KORUPOJU, SRINIVASA,TUMMA, HARIKRISHNA
申请号:
PE2011001469
公开号:
PE20120603A1
申请日:
2010.02.08
申请国别(地区):
PE
年份:
2012
代理人:
摘要:
1. It refers to the compound of triazole [4,3-b] pyridine (I), wherein R1 is halotars (C1-C4);K is 1 or 2, N, C, ch or COH from 0 to 2, N and P respectively; dotted line is a simple or double link; L1 is a direct link, - (cr3r4) T -,- yes.-S (O) -Among them, R3 and R4 are h or methyl; t is 1-3; J is arilo, cyclo (C3-C6),A four to seven member non bicycle ring, etc., L2 is a direct link, s (o)-S (O) 2-R2 is, among other things, halogen, tar (C1-C6),CARBOXI, CN, AMINO, AMONG OTHERS; r IS 0 TO 3. THEY ARE PREFERRED COMPOUNDS: 6- [4- (4-FLUOROBENCIL) PIPERAZIN-1-IL] -3- (TRIFLUOROMETIL) -7,8-DIHYDRO [1,2,4] TRIAZOLO [4, 3-b] PIRIDAZINE; 6- [4- (1H-INDOL-3-IL) -3,6-DIHIDROPIRIDIN-1 (2H) -IL] -3- (TRIFLUOROMETIL) -7,8-DIHIDRO [1,2,4] TRIAZOLO [4 , 3-b] PIRIDAZINE; 6- (4- {4- [2- (4-ACETILPIPERAZIN-1-IL) ETOXI] FENYL} PIPERIDIN-1-IL) -3- (TRIFLUOROMETIL) -7,8-DIHIDRO [1,2,4] TRIAZOLO [4,3-b] PIRIDAZINE; AMONG OTHERS. IT ALSO REFERS TO A PREPARATION PROCEDURE AND A PHARMACEUTICAL COMPOSITION. SUCH COMPOUNDS ARE LINKED TO THE ANDROGEN RECEPTOR (AR) BEING USEFUL IN THE TREATMENT OF CANCER OF PROSTATESE 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]PIRIDAZINA; 6-(4-{4-[2-(4-ACETILPIPERAZIN-1-IL)ETOXI]FENIL}PIPERIDIN-1-IL)-3-(TRIFLUOROMETIL)-7,8-DI