benzimidazole compounds containing morpholinyl, their use as respiratory syncytial virus replication inhibitors, the composition comprising them and the process for preparing said compounds
Christophe Meyer,Frédéric Marc Maurice Doublet,Jean-François Bonfanti,Jérôme Michel Claude Fortin,Koenraad Jozef Lodewijk Andries,Philip Maria Martha Bern Timmerman,Philippe Muller,Rudy Edmond Willebr
申请号：
BRPI0417268
公开号：
BRPI0417268B1
申请日:
2004.12.20
申请国别(地区):
BR
年份:
2018
代理人:
摘要：
"Morpholinyl-containing benzimidazoles as inhibitors of respiratory syncytial virus replication." The present invention relates to morpholinyl-containing benzimidazoles having respiratory syncytial virus replication inhibiting activity and of formula (1), a prodrug, n-oxide, addition salt, quaternary amine, metal complex and stereochemically isomeric form of the even wherein g is a direct or optionally substituted C 1-10 alkanediyl bond； R4 is R4 or a monocyclic or bicyclic heterocycle which is R7, pyrrolidinyl, substituted with R7, piperidinyl, substituted with R7, or homopiperidinyl, substituted with R7； one of R 2a 4 and R 3a 4 is chosen from halo, C 1-6 alkyl, optionally mono- or polysubstituted, C 2-6 alkenyl, optionally mono- or polysubstituted, nitro, hydroxy, ar 2 ^, n (r ^ 4a ^ r ^ 4b ^), n (r ^ 4a ^ r ^ 4b ^) sulfonyl, n (r ^ 4a ^ r ^ 4b ^) arbonyl, C 1-6-alkyloxy, ar ^ C 1-6 alkyloxy, carboxy, C 1-6 alkyloxy, caronyl, or (c = z) ar 2； if r 2a is different from hydrogen, then r 2b is hydrogen, C 1-6 alkyl or halogen and r 3b is hydrogen； In the case of R3a4 other than hydrogen, then R3b is hydrogen, C1-6 alkyl or halogen, and R2b is hydrogen. The invention further relates to the preparation thereof and compositions comprising such compounds as well as to their use as a medicament."benzimidazóis que contêm morfolinila, como inibidores da replicação de vírus sinciciais respiratórios". a presente invenção refere-se a benzimidazóis contendo morfolinila, com atividade inibidora sobre a replicação do vírus sincicial respiratório e com a fórmula (1), uma prodroga, n-óxido, sal de adição, amina quatemária, complexo metálico e forma estereoquimicamente isomérica do mesmo, no qual g é uma ligação direta ou c~ 1-10~alcanodiila, opcionalmente substituída； r^ 1^ é ar^ 1^ ou um heterociclo monocíclico ou bicíclico q é r^ 7^, pirrolidinila, substituída com r^ 7^, piperidinila, substituída com r^ 7^ ou homopiperidinila, substituída com r^ 7^； um de r^ 2a^ e r^ 3a^ é escol
