摘要:
A compound of the formula ##STR1## wherein R.sup.1 to R, R.sup.a, R.sup.b X, Y, Z, m and n have the significance given in the description, can be used as medicaments, especially for the treatment and prophylaxix of conditions which are associated with endothelin activities.
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;R.sup.5 signifies hydrogen or a residue R.sup.7, andR.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; orR.sup.5 and R.sup.6 together with the N atom associated with them signify a heterocyclic residue;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;R.sup.b signifies hydrogen or lower-alkyl;Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.8, --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; andn signifies 0, 1 or 2;and pharmaceutically usable salts thereof are inhibitors of endothelin receptors.They can therefore be used for the treatment of disorders which are associated with endothelin activities, especially circulatory disorders such as hypertension, ischaemia, vasospasms and angina pectoris.
摘要:
Compounds of the formula: ##STR1## where A, B, R.sup.1 -R.sup.8 are as described herein are endothelin inhibitors that can be used in treating diseases associated with endothelin, such as high blood pressure. Chemical synthesis of these compounds and pharmaceutical compositions containing these compounds are also useful.
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; R.sup.5 signifies hydrogen or a residue R.sup.7, and 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 heterocyclic residue; 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; R.sup.b signifies hydrogen or lower-alkyl; Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.8, --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 used for the treatment of disorders which are associated with endothelin activities, especially circulatory disorders such as hypertension, ischaemia, vasospasms and angina pectoris.
摘要:
Compounds of the formula ##STR1## wherein the variables are hereinbelow defined. The compounds of formula I are inhibitors for endothelin receptors. They can be used for the treatment of disorders which are associated with endothelin activities, especially circulatory disorders such as hypertension, ischaemia, vasospasms and angina pectoris.
摘要:
The invention is concerned with novel sulphonamides and their use as medicaments. In particular, the invention is concerned with compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, lower-alkyl, lower-alkoxy, lower-alkylthio, halogen or trifluoromethyl;R.sup.2 is hydrogen, lower-alkyl, halogen, lower-alkoxy, trifluoromethyl or --OCH.sub.2 COOR.sup.9 ;R.sup.3 is hydrogen, lower-alkyl, halogen, lower-alkylthio, trifluoromethyl, lower-alkoxy or trifluoromethoxy;R.sup.2 and R.sup.3 together are butadienyl, methylenedioxy, ethylenedioxy or isopropylidenedioxy;R.sup.4 is hydrogen, lower-alkyl, trifluoromethyl, lower-alkoxy, lower-alkylthio, hydroxy-lower-alkyl, hydroxy-lower-alkoxy, hydroxy-lower-alkoxy-lower-alkyl, hydroxy-lower-alkoxy-lower-alkoxy, alkoxy-lower-alkyl, alkoxy-lower-alkyloxy, lower-alkylsulfinyl, lower-alkylsulfonyl, 2-methoxy-3-hydroxypropoxy, 2-hydroxy-3-phenylpropyl, amino-lower-alkyl, lower-alkylamino-lower-alkyl, di-lower-alkylamino-lower-alkyl, amino, lower-alkylamino, di-lower-alkylamino, arylamino, aryl, arylthio, aryloxy, aryl-lower-alkyl, heterocyclyl, heterocyclo-lower-alkyl, heterocyclylamino, heterocyclylthio, heterocyclyloxy, --CHO, --CH.sub.2 OH or --CH.sub.2 Cl;R.sup.5 to R.sup.8 are independently hydrogen, halogen, trifluoromethyl, lower-alkoxy, lower-alkylthio or cyano;R.sup.6 and R.sup.5 or R.sup.7 together are butadienyl, methylene-dioxy, ethylenedioxy or isopropylidenedioxy;X is --O-- or --S--;Y is --CHO, C.sub.1-4 -alkyl, --(CH.sub.2).sub.1-4 --Z--R.sup.9, --(CH.sub.2).sub.1-4 --OC(O)(CH.sub.2).sub.1-4 CH.sub.3, --(CH.sub.2).sub.1-4 OC(O)Het, --(CH.sub.2).sub.1-4 NHC(O)R.sup.10, --(CH.sub.2).sub.1-4 OCH.sub.2 CH(OH)CH.sub.2 OH and cyclic ketals thereof, --(CH.sub.2).sub.1-4 NR.sup.9 CH.sub.2 CH(OH)CH.sub.2 OH, --(CH.sub.2).sub.1-4 OCH.sub.2 CH.sub.2 SCH.sub.3, --(CH.sub.2).sub.1-4 OCH.sub.2 CH.sub.2 S(O)CH.sub.3, --(CH.sub.2).sub.1-4 O(CH.sub.2).sub.1-4 --Z H, --(CH.sub.2).sub.1-4 O(CH.sub.2).sub.1-4 OC(O)R.sup.10, --(CH.sub.2).sub.1-4 NR.sup.9 (CH.sub.2).sub.1-4 Z H, --(CH.sub.2).sub.1-4 O(CH.sub.2).sub.1-4 OC(O)Het, --(CH.sub.2).sub.0-3 CH(OH)R.sup.10, --(CH.sub.2).sub.0-3 CH(OH)(CH.sub.2).sub.1-4 Z H, --(CH.sub.2).sub.0-3 CH(OH)CH.sub.2 SCH.sub.3, --(CH.sub.2).sub.0-3 CH(OH)CH.sub. 2 S(O)CH.sub.3, --(CH.sub.2).sub.0-3 CH(OH)OCH.sub.2 CH.sub.2 OH, --(CH.sub.2).sub.0-3 C(O)(CH.sub.2).sub.1-4 CH.sub.3, --(CH.sub.2).sub.0-3 C(O)(CH.sub.2).sub.1-4 Z R.sup.11, --(CH.sub.2).sub.0-3 C(O)CH.sub.2 Hal, --(CH.sub.2).sub.1-4 Hal, --(CH.sub.2).sub.1-4 CN, --(CH.sub.2).sub.0-3 C(O)OR.sup.9, --OR.sup.12 or --SR.sup.12 ;R.sup.9 is hydrogen or C.sub.1-4 -alkyl;R.sup.10 is C.sub.1-4 -alkyl;R.sup.11 is hydrogen, C.sub.1-4 -alkanoyl or heterocyclylcarbonyl;R.sup.12 is C.sub.1-4 -alkyl or --(CH.sub.2).sub.0-4 -aryl;Z is --O--, --S-- or --NR.sup.9 --;Het is a heterocyclic residue;Hal is halogen; andn is 0 or 1; and salts thereof.
摘要:
The novel sulfonamides of formula I, ##STR1## in which the symbols R.sup.1 -R.sup.9, R.sup.a, R.sup.b, X, Y and n have the significance given in the description and salts thereof can be used for the treatment of circulatory disorders, especially hypertension, ischemia, vasopasms and angina pectoris.
摘要:
Sulfonamides of formula I, in which the symbols R.sup.1 -R.sup.6, X, Y and n have the significance given in the description and which are in part novel compounds, and salts thereof, which can be used as active ingredients for the manufacture of medicaments for the treatment of circulatory disorders, especially hypertension, ischemia, vasospasms and angina pectoris, are described.
摘要:
The invention relates to a product containing the compound of formula (I) below or a pharmaceutically acceptable salt of this compound, in combination with at least one compound having prostacyclin receptor (IP) agonist properties, or a pharmaceutically acceptable salt thereof.