MY104554A - Benzofuran derivatives. - Google Patents

Abstract

THE INVENTION PROVIDES COMPOUNDS OF THE GENERAL FORMULA (I)(FORMULA 1)OR A PHYSIOLOGICALLY ACCEPTABLE SALT, SOLVATE OR NON-TOXIC METABOLICALLY LABILE ESTER THEREOF WHEREIN R1 REPRESENTS A HYDROGEN ATOM OR A HALOGEN ATOM OR A GROUP SELECTED FROM C1-6 ALKYL, C2-6 ALKENYL, FLUORO C1-6 ALKYL, C1-6 ALKOXY, -CHO, -CO2H OR -COR2, AR REPRESENTS THE GROUP(FORMULA 2)R2 REPRESENTS A GROUP SELECTED FROM C1-6 ALKYL, C2-6 ALKENYL, C1-6 ALKOXY OR THE GROUP -NR10R11, R3 REPRESENTS A GROUP SELECTED FROM -CO2H, -NHSO2CF3 OR A C-LINKED TETRAZOLYL GROUP; R4 AND R5, WHICH MAY BE THE SAME OR DIFFERENT, EACH INDEPENDENTLY REPRESENT A HYDROGEN ATOM OR A HALOGEN ATOM OR A C1-6 ALKYL GROUP. HET REPRESENTS AN N-LINKED IMIDAZOLYL GROUP OPTIONALLY SUBSTITUTED AT THE 2-POSITION BY A C1-6 ALKYL, C2-6 ALKENYL OR A C1-6 ALKYLTHIO GROUP,THE IMIDAZOLYL GROUP OPTIONALLY BEING SUBSTITUTED AT THE 4- AND 5- POSITIONS BY ONE OR TWO FURTHER SUBSTITUENTS SELECTED FROM A HALOGEN ATOM OR GROUP SELECTED FROM CYANO, NITRO, C1-6 ALKYL, C2-6 ALKENYL, FLUORO C1-6 ALKYL, -(CH2)MR6, -(CH2)N COR7 OR -(CH2)PNR8COR9, R6 REPRESENTS A HYDROXY OR C1-6 ALKOXY GROUP, R7 REPRESENTS A HYDROGEN ATOM OR GROUP SELECTED FROM HYDROXY, C1-6ALKYL, C1-6 ALKOXY, PHENYL, PHENOXY OR THE GROUP -NR10R11, R8 REPRESENTS A HYDROGEN ATOM OR A C1-6 ALKYL GROUP, R9 REPRESENTS A HYDROGEN ATOM OR GROUP SELECTED FROM C1-6 ALKYL, C1-6 ALKOXY, PHENYL, PHENOXY OR THE GROUP -NR10R11, R10 AND R11, WHICH MAY BE THE SAME OR DIFFERENT, EACH INDEPENDENTLY REPRESENT A HYDROGEN ATOM OR A C1-4 ALKYL GROUP OR -NR10R11 FORMS A SATURATED HETEROCYCLIC RING WHICH HAS 5 OR 6 RING MEMBERS AND MAY OPTIONALLY CONTAIN IN THE RING ONE OXYGEN ATOM; M REPRESENTS AN INTERGER FROM 1 TO 4; N REPRESENTS AN INTEGER FROM 0 TO 4; AND P REPRESENTS AN INTEGER FROM 1 TO 4. THE COMPOUNDS MAY BE USED IN THE TREATMENT OR PROPHYLAXIS OF HYPERTENSION AND DISEASES ASSOCIATED WITH COGNITIVE DISORDERS.