ALTMAN, Michael D.,ANDRESEN, Brian,CHANG, Wonsuk,CHILDERS, Matthew Lloyd,CUMMING, Jared N.,HAIDLE, Andrew Marc,HENDERSON, Timothy J.,JEWELL, James P.,LIANG, Rui,LIM, Jongwon,LIU, Hong,LU, Min,NORTHRUP
申请号:
PE0002352018
公开号:
PE6882018A1
申请日:
2016.08.11
申请国别(地区):
PE
年份:
2018
代理人:
摘要:
Cyclic dinucleotides relates to compounds of formula (i), (i) or (I ), where Base1 and base2,,,, XA1, XA, XB, XC, xD xC1 XB1,,, XD1, A1A, R1, R2, R3, R4, 2a, R4A, R5, R6 r6a R7a, R7,,,R8 and r8a are as defined in the description.Preferred compounds are: 2 - amino - 2 - [(5R, 7R, 8R, 12ar, 14R, 15s, 15ar, 16R) - 4 - (7 - amino - 3h [1,2,3] triazolo [4,5-d] - pyrimidine - 3 - il) 15,16 - difluoro - 2 - hydroxy - 3 - dioxide sulfaniloctahidro - - - 10 - 12 58 - metanofuro [3.2] [- l] 1,3,9,11,6,2,10 tetraoxatiadifosfaciclotetradecin - 7 - yl] - 1.9 - dihydro - 6h purin-6 - One among others. It also relates to a Pharmaceutical composition.These compounds induce the production of Type I interferon activated via Sting being useful in the treatment of disorders such as Cancer Cell ProliferationSE REFIERE A COMPUESTOS DINUCLEOTIDOS CICLICOS DE FORMULAS (I), (I) O (I"), DONDE BASE1, BASE2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8 y R8a SON COMO SE DEFINEN EN LA DESCRIPCION. SON COMPUESTOS PREFERIDOS: 2-AMINO-9-[(5R,7R,8R,12aR,14R,15S,15aR,16R)-14-(7-AMINO-3H-[1,2,3]TRIAZOLO[4,5-d]PIRIMIDIN-3-IL)-15,16-DIFLUORO-2-HIDROXI-2,10-DIOXIDO-10-SULFANILOCTAHIDRO-12H-5,8-METANOFURO[3,2-l][1,3,9,11,6,2,10]TETRAOXATIADIFOSFACICLOTETRADECIN-7-IL]-1,9-DIHIDRO-6H-PURIN-6-ONA ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INDUCTORES DE LA PRODUCCION DE INTERFERON DE TIPO I QUE ACTIVAN LA VIA DE STING SIENDO UTILES EN EL TRATAMIENTO DE TRANSTORNOS DE PROLIFERACION CELULAR COMO CANCER