PE60296A1 - NEW SULPHONAMIDE - Google Patents

Abstract

IT REFERS TO THE COMPOUND OF FORMULA I WHERE: R1 IS PHENYL, SUBSTITUTED PHENYL OR HETEROCICLYL; R2 IS PHENYL OR SUBSTITUTED PHENYL; R3 IS H, LOWER ALKYL, CYAN, CARBOXY AMONG OTHERS; R4 IS H OR LOWER ALKYL; R5 IS H OR A REST R7; R6 IS - (CH2) mR7; R5 AND R6 TOGETHER WITH THE ATOMO OF NITROGEN THAT UNITE THEM, FORM A N-HETEROCICLICO REST; R7 IS PHENYL, SUBSTITUTED PHENYL, CYCLOALKYL AMONG OTHERS; Ra IS H, LOWER ALKYL OR HYDROXY; Rb IS H or LOWER ALKYL; Z IS OH, AMINO OR A REST -OR8 AMONG OTHERS; R8 IS HETEROCICLILO, FENILO, FENILO SUBSTITUTED AMONG OTHERS; A e AND INDEPENDENTLY ARE OXYGEN OR SULFUR; X IS N or CH; n ES O, 1 or 2; IT ALSO REFERS TO THE PREPARATION PROCESSES, SUCH AS THAT CHARACTERIZED BY: a) REACTION OF THE COMPOUND OF FORMULA II IN WHICH R2, R3, R4, Ra, Rb, A, Z, Y and n HAVE ALREADY BEEN DEFINED, AND IN WHICH THE AMINO OR HYDROXY GROUPS OF R3 AND Z ARE EVENTUALLY PROTECTED WITH A REACTIVE DERIVATIVE OF A SULPHONIC ACID OF FORMULA R1SO2OH; OR b) REACTION IN A BASIC MEDIUM, OF A COMPOUND OF FORMULA III WHERE R1, R2, R3, R4, A and X HAVE ALREADY BEEN DEFINED WITH A COMPOUND OF FORMULA HalCH2 (CRaRb) nCH2OH, WHERE Hal IS HALOGEN AND THE HYDROXY GROUPS MAY PROTECTED. IT IS USED IN THE TREATMENT OF DISEASES ASSOCIATED WITH THE ACTIVITY OF ENDOTHELINE SUCH AS VASCULAR DISEASES