SULFONEAMIDE DERIVATIVES AND PHARMACEUTICAL PREPARATION Russian patent published in 2001 - IPC

Abstract RU 2173317 C2

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to novel sulfoneamide derivatives or their pharmaceutically acceptable salts that show properties of endothelin receptor antagonist and can be used in treatment of patients with circulating system disorders, for example, such as hypertensia, ischemia, stenocardia, blood vessels spasms and to pharmaceutical preparation based on thereof. Sulfoneamide derivatives correspond to the general formula (I) where R1 means phenyl substituted with lower alkyl or lower alkoxy-group, substituted heterocyclyl representing pyridyl substituted with lower alkyl; R2 means phenyl substituted with lower alkoxy- -group and/or halogen atom; R3 means hydroxy-group, lower alkoxy-group or residue -NR4R5; R4 means hydrogen or residue -R6; R5 means hydrogen atom or R4 and R5 in common with bound N-atom mean N-heterocyclic residue representing morpholine-4-yl; R6 means phenyl, phenyl substituted with hydroxy-group or hydroxy(lower)alkyl, heterocyclyl taken among tetrazolyl or pyridyl and hydroxy(lower)alkyl; Ra means hydrogen atom or hydroxy-group; Rb means hydrogen atom; X means oxygen atom; Y means oxygen atom; Z means hydrogen atom, lower alkyl, heterocyclyl representing pyrimidine-2-yl and n = 0 or 1, and their pharmaceutically acceptable salts. Invention relates to also pharmaceutical preparation showing effect of endothelin inhibitor and containing one compound of the formula (I), standard filling agents and accessory substances. EFFECT: new sulfoneamide derivatives indicated above, valuable pharmacological properties. 9 cl, 27 ex

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Authors

Fol'Ker Broj

Zhan-Mari Kassal'

Zhorzh Khirt

Marsel' Mjuller

Khenri Ramuts

Kaspar Burri

Martin Klozel'

Bernd-Mikhaehl' Leffler

Verner Najdkhart

Dates

2001-09-10Published

1996-10-11Filed