摘要 |
THE PRESENT INVENTION CONCERNS MORPHOLINYL CONTAINING BENZIMIDAZOLES HAVING INHIBITORY ACTIVITY ON THE REPLICATION OF THE RESPIRATORY SYNCYTIAL VIRUS AND HAVING THE FORMULA A PRODRUG, N-OXIDE, ADDITION SALT, QUATERNARY AMINE, METAL COMPLEX OR STEREOCHEMICALLY ISOMERIC FORM THEREOF WHEREIN G IS A DIRECT BOND OR OPTIONALLY SUBSTITUTED C1-10ALKANEDIYL; R1 IS AR1 OR A MONOCYCLIC OR BICYCLIC HETEROCYCLE Q IS R7, PYRROLIDINYL SUBSTITUTED WITH R7, PIPERIDINYL SUBSTITUTED WITH R7 OR HOMOPIPERIDINYL SUBSTITUTED WITH R7; ONE OF R2A AND R3A IS SELECTED FROM HALO, OPTIONALLY MONO- OR POLYSUBSTITUTED C1-6ALKYL, OPTIONALLY MONO- OR POLYSUBSTITUTED C2-6ALKENYL, NITRO, HYDROXYL, AR2, N(R4AR4B), N(R4AR4B)SULFONYL, N(R4AR4B)CARBONYL, C1-6ALKYLOXY, AR2 OXY, AR2C1-6ALKYLOXY, CARBOXYL, C1-6ALKYLOXYCARBONYL, OR–C(=Z)AR2; AND THE OTHER ONE OF R2A AND R3A IS HYDROGEN; IN CASE R2A IS DIFFERENT FROM HYDROGEN THEN R2B IS HYDROGEN, C1-6ALKYL OR HALOGEN AND R3B IS HYDROGEN; IN CASE R3A IS DIFFERENT FROM HYDROGEN THEN R3B IS HYDROGEN, C1-6ALKYL OR HALOGEN AND R2B IS HYDROGEN. IT FURTHER CONCERNS THE PREPARATION THEREOF AND COMPOSITIOS COMPRISING THESE COMPOUNDS, AS WELL AS THE USE THEREOF AS A MEDICINE. |
申请人 |
TIBOTEC PHARMACEUTICALS LTD |
发明人 |
BONFANTI, JEAN-FRANCOIS;ANDRIES, KOENRAAD JOZEF LODEWIJK;FORTIN, JEROME MICHEL CLAUDE;MULLER, PHILIPPE;DOUBLET, FREDERIC MARC MAURICE;MEYER, CHRISTOPHE;WILLEBRORDS, RUDY EDMOND;GEVERS, TOM VALERIUS JOSEPHA;TIMMERMAN, PHILIP MARIA MARTHA BERN |