CANALES EDA,CHONG LEE,CLARKE MICHAEL ONEIL HANRAHAN,DOERFFLER EDWARD,LAZERWITH SCOTT E.,LEW WILLARD,MERTZMAN MICHAEL,MORGANELLI PHILIP A.,WATKINS WILLIAM J.,YE HONG,LIU QI
申请号:
PE0000692012
公开号:
PE06662012A1
申请日:
2010.07.19
申请国别(地区):
PE
年份:
2012
代理人:
摘要:
Refers to compounds of thiophene - 2 - carboxylic acid Derivatives of formula (i) wherein R1 is alkyl (C12 alquenilo (C1, C2) - C12 cycloalkyl (C3), C12), among others R2 is alquinilo (C2 C12 cycloalkyl (C3), C12, C14 aryl (C6)), among others R3 is alquileno (C1, C12 (C2) alquenileno arylene (C6 C12, C14), entr And others L - O -, - S -,- s or - S (o) - 2 - (OR) Het is heterociclilo 3 to 12 members or heteroaryl 3 to 14 members optionally substituted with Q4 to Q4, which is Halogen, Oxo, NO2, N (= o), among others.Preferred compounds are: acid, 5 - (3,3 - dimethyl - but - 1 - inil) - 3 - (Trans - 4 - methyl - ciclohexanocarbonil) - trans - [4 - (2 - pirazin - iloxi) cyclohexyl] amino} - 2 - thiophene carboxylic acid, 5 - (3,3 - dimethyl - but - 1 - inil) - 3 - (Trans - 4 - methyl - ciclohexanocarbonil) - trans - [4 - (2 - methyl - 3 - iloxi pyridazin-3) cyclohexyl] amino} - Uncle Feno - carboxylic acid - 2 - (3, 53 - dimethyl - but - 1 - inil) - 3 - (Trans - 4 - methyl - ciclohexanocarbonil) - trans - [4 - (3 - pyridin - iloxi) cyclohexyl] amino} - 2 - thiophene carboxylic acid among others. It also relates to a Pharmaceutical composition. These compounds are inhibitors of Flaviviridae Viruses being useful in the treatment of infection by the hepatitis C virus (HCV)SE REFIERE A COMPUESTOS DERIVADOS DE TIOFENO-2-CARBOXILICO DE FORMULA (I) DONDE R1 ES ALQUILO(C1-C12), ALQUENILO(C2-C12), CICLOALQUILO(C3-C12), ENTRE OTROS R2 ES ALQUINILO(C2-C12), CICLOALQUILO(C3-C12), ARILO(C6-C14), ENTRE OTROS R3 ES ALQUILENO(C1-C12), ALQUENILENO(C2-C12), ARILENO(C6-C14), ENTRE OTROS L ES -O-, -S-, -S(O)- O -S(O)2- HET ES HETEROCICLILO DE 3 A 12 MIEMBROS O HETEROARILO DE 3 A 14 MIEMBROS OPCIONALMENTE SUSTITUIDOS CON Q4, EN DONDE Q4 ES HALOGENO, OXO, NO2, N(=O), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ACIDO 5-(3,3-DIMETIL-BUT-1-INIL)-3-{(TRANS-4-METIL-CICLOHEXANOCARBONIL)-[TRANS-4-(PIRAZIN-2-ILOXI)-CICLOHEXIL]-AMINO}-TIOFENO-2-CARBOXILICO ACIDO 5-(3,3-DIMETIL-BUT-1-INIL)-3-{(TRANS-4-MET