MY102088A - Amines derivatives. - Google Patents

Abstract

THE INVENTION PROVIDES COMPOUNDS OF THE GENERAL FORMULA (3) AND PHYSIOLOGICAL ACCEPTABLE ACID ADDITION SALTS, METABOLICALLY LABILE ESTERS AND SOLVATES THEREOF IN WHICH R1 REPRESENTS A HALOGEN ATOM OR A METHYL, ETHYL, N-PROPYL OR N-BUTYL GROUP; R2, R3, R4 AND R5 EACH REPRESENT HYDROGEN ATOMS OR ONE OR TWO OF R2, R3, R4, AND R5 REPRESENT A METHYL OR ETHYL GROUP; X REPRESENTS A C4-7 ALKYLENE CHAIN OPTIONALLY SUBSTITUTED BY ONE OR MORE C1-4 ALKYL OR HYDROXYL GROUPS; OR OPTIONALLY CONTAINING ONE OR TWO DOUBLE OR TRIPLE BONDS; OR OPTIONALLY INTERRUPTED BY AN OXYGEN OR SULPHUR ATOM, OR BY A SULPHONE (-SO2-) OR UREA (NHCONH-) GROUP; AND Y REPRESENTS A PHENYL RING OPTIONALLY CARRYING ONE TO THREE SUBSTITUENTS SELECTED FROM HYDROXYL, C1-4 ALKYL, C1-4 ALKOXY, AMINO, CARBOXAMIDO, C1-4 ALKYLSULPHONYL-AMINO AND NITRO GROUPS AND HALOGEN ATOMS WITH THE PROVISO THAT WHEN X IS C4-7 ALKYLENE CHAIN OPTIONALLY CONTAINING ONE DOUBLE BOND THEN Y CANNOT REPRESENT PHENYL OR PHENYL CARRYING ONE SUBSTITUENT WHICH IS HALOGEN. THE COMPOUNDS ACCORDING TO THE INVENTION DECREASE TOTAL PERIPHERAL VASCULAR RESISTANCE, INCREASE CARDIAC OUTPUT AND PRODUCE A FALL IN BLOOD PRESSURE. THEY MAY BE USED IN THE TREATMENT OR PROPHYLAXIS OF RENAL INSUFFICIENCY AND CARDIOVASCULAR DISORDERS SUCH AS HYPERTENSION, ISCHAEMIC HEART DISEASE OR HEART FAILURE, FOR EXAMPLE ACUTE OR CONGESTIVE HEART FAILURE.