DE HARO GARCIA, Teresa,DELIGNY, Michael,HEER, Jag Paul,QUINCEY, Joanna Rachel,XUAN, Mengyang,ZHU, Zhaoning,BROOKINGS, Daniel Christopher,CALMIANO, Mark Daniel,EVRARD, Yves,HUTCHINGS, Martin Clive,JOHN
申请号：
PE0005442017
公开号：
PE06932017A1
申请日:
2015.10.02
申请国别(地区):
PE
年份:
2017
代理人:
摘要：
Refers to pentacyclic FUSED imidazole derivative compounds of formula (i) where X represents - - - - - - or, or - C (o) -, - C (o) - O -, among others Z is methylene e is 1h benzimidazole, imidazo [1,2-a] pyridine or imidazo [1,2-a] pyrazine optionally substituted R5 and R8 are each h, halogen, hydrous I, CN, among others R6 and R7 are each h, halogeno, trifluoromethyl,Among others, R12 is H or c1-c6 alkyl. Preferred compounds are (7R, 14R) - 1 - (Difluoromethoxy) - 10 11 - fluoro - [2 - (2 - hidroxipropan - il) pyrimidin-5-yl] - 6.7 - dihydro - 7:14 - metanobencimidazo [1,2-b] [2.5] benzodiazocin - 5 (14h) - One (7R, 14R) - 1 - (Difluoromethoxy) - 5 - [2 - (2 - hidroxipropan - il) pyrimidin-5-yl] - 6.7 - dihydro - 7:14 - metanobencimidazo [1,2-b] [2.5] Benzodiazocin - 5 (14h) - One among others.These compounds are modulators of TNF alpha activity of human being useful in the treatment of inflammatory disorders, neurological and neurodegenerative DisordersSE REFIERE A COMPUESTOS DERIVADOS DE IMIDAZOL PENTACICLICOS FUSIONADOS DE FORMULA (I) DONDE -X-Q- REPRESENTA -O-, -O-C(O)-, -C(O)-O-, ENTRE OTROS Z ES METILENO E ES 1H-BENZIMIDAZOL, IMIDAZO[1,2-a]PIRIDINA O IMIDAZO[1,2-a]PIRAZINA OPCIONALMENTE SUSTITUIDOS R5 Y R8 SON CADA UNO H, HALOGENO, HIDROXI, CN, ENTRE OTROS R6 Y R7 SON CADA UNO H, HALOGENO, TRIFLUOROMETILO, ENTRE OTROS R12 ES H O C1-C6 ALQUILO. SON COMPUESTOS PREFERIDOS: (7R,14R)-1-(DIFLUOROMETOXI)-10-FLUORO-11-[2-(2-HIDROXIPROPAN-2-IL)PIRIMIDIN-5-IL]-6,7-DIHIDRO-7,14-METANOBENCIMIDAZO[1,2-b][2,5]BENZODIAZOCIN-5(14H)-ONA (7R,14R)-1-(DIFLUOROMETOXI)-11-[2-(2-HIDROXIPROPAN-2-IL)PIRIMIDIN-5-IL]-6,7-DIHIDRO-7,14-METANOBENCIMIDAZO[1,2-b][2,5]BENZODIAZOCIN-5(14H)-ONA ENTRE OTROS. DICHOS COMPUESTOS SON MODULADORES DE LA ACTIVIDAD DE TNF ALFA HUMANO SIENDO UTILES EN EL TRATAMIENTO DE TRASTORNOS INFLAMATORIOS, TRASTORNOS NEUROLOGICOS Y NEURODEGENERATIVOS
