'NOVEL DIOXCYCLOBUTENE DERIVATIVES, PROCESSES FOR THEIR PREPARATIONS, AND THEIR USE AS ANGIOTENSIN II ANTAGONISTS'

摘要

THE INVENTION PROVIDES COMPOUNDS OF FORMULA I ( FORMULA 1 ) AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF;WHEREIN R50 IS HYDROGEN OR C1-4 ALKYL, A51 IS OXYGEN, SULPHUR OR A GROUP OF THE FORMULA -NR52- WHEREIN R52 IS HYDROGEN OR C1-4 ALKYL; A50 COMPRISES I) A MONO OR BICYCLIC AROMATIC RING OPTIONALLY CONTAINING ONE OR MORE NITROGEN, OXYGEN OR SULPHUR ATOMS, II) A CYCLOALKENDYL GROUP, OR III)AN ACYCLIC BRIDGING GROUP HAVING A CHAIN OF ONE, TWO OR THREE ATOMS BETWEEN THE CYCLOBUTENEDIONE GROUP AND X50, SAID CHAIN BEING A CHAIN OF ONE OR TWO CARBON ATOMS OR A CHAIN OF ONE CARBON ATOM ONE OR MORE NITROGEN, OXYGEN OR SULPHUR ATOMS OR IV) A BOND; X50 IS EITHER A BOND OR A SPACER GROUP PROVIDING A CHAIN BETWEEN A50 AND B50 OF ONE OR TWO ATOMS LENGTH; B50 IS A MONO OR BICYCLIC AROMATIC RING OPTIONALLY CONTAINING ONE OR MORE NITROGEN, OXYGEN OR SULPHUR ATOMS; R IS AN INTEGER FROM 1 TO 6; AND HET IS A RING SYSTEM OPTIONALLY CONTAINING ONE OR MORE IS A PHOSPHONATE, PHOSPHINATE OR AMINE DERIVATIVES (WHEREIN EACH OF A50, X50, B50 AND HET ARE OPTIONALLY SUBSTITUTED).THE COMPOUNDS HAVE ANGIOTENSIN II ANTAGONIST ACTIVITY AND ARE USEFUL IN THE TREATMENT OF CARDIOVASCULAR DISORDERS SUCH AS HYPERTENSION.