专利名称：Aryl- and hetaryl-sulfonamide derivatives, their preparation and their u as endothelin
营养排骨汤antagonists
发明人：Volker Breu,Kaspar Burri,Jean-Marie
Cassal,Martine Clozel,Georges Hirth,Bernd-
Michael Loffler,Marcel Muller,Werner
Neidhart,Henri Ramuz
申请号：US09/263034
申请日：19990305
公开号：US06133442A
公开日：星期六
20001017
专利内容由知识产权出版社提供
摘要：Compounds of formula I ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl;
R.sup.2 signifies phenyl or substituted phenyl;
R.sup.3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, substituted phenyl, heterocyclyl or a residue --CONR.sup.5 R.sup. 6 or --NR.sup.5 COR. sup.7 ;
R.sup.4 signifies hydrogen or lower-alkyl;< P>
R.sup.5 signifies hydrogen or a residue R.sup.7, and< P>
R.sup.6 signifies --(CH.sub.2).sub.m R.sup. 7 ; or
R.sup.5 and R.sup.6 together with the N atom associated with them signify a抗震救灾
heterocyclic residue;进字成语
R. sup.7 signifies phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower-alkyl, cyano- lower- alkyl, hydroxy-lower-alkyl, di-lower- alkylamino-lower-alkyl, carboxy-lower-alkyl, lower-alkoxycarbonyl-lower- alkyl, lower- alkoxycarbonylamino- lower-alkyl or phenyl-lower- alkoxycarbonyl;
R.sup.a signifies hydrogen, lower-alkyl or hydroxy;个体发育
< P>R.sup.b signifies hydrogen or lower-alkyl;
洛阳年票
Z signifies hydroxy, amino or a residue --OR.sup.8, -- OC(O)NHR.sup.8, --董明珠谈营销
OC(O)OR.sup.8, --NHC(O)NHR.sup.8 or --NHC(O)OR.sup.8 ;
R.sup.8 signifies heterocyclyl, phenyl, substituted phenyl or lower-alkyl;
A and Y each independently signify oxygen or sulphur,
X signifies nitrogen or CH;
m signifies 0, 1 or 2; and
n signifies 0, 1 or 2;
and pharmaceutically usable salts thereof are inhibitors of endothelin receptors.
They can therefore be ud for the treatment of disorders which are associated with endothelin activities, especially circulatory disorders such as hypertension, ischaemia, vasospasms and angina pectoris.
申请人：HOFFMANN-LA ROCHE INC.
代理人：George W. Johnston,William H. Epstein,John P. Pari
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