摘要:
Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3, A1 and A2 have the significance given in claim 1, can be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.
摘要:
Compounds of formula I are provided as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5, n, m and A have the significance disclosed in the specification, and can be used for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.
摘要:
The compounds of formula (I) wherein R1 has the significance as given in the description, are inhibitors of endothelin receptors and can therefore be used for the treatment of disorders which are associated with abnormal vascular tone and endothelial dysfunction.
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 compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the significance given in claim 1,in the form of optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates or mixtures of diastereomeric racemates as well as pharmaceutically usable salts thereof inhibit the activity of the natural enzyme renin and can accordingly be used in the form of pharamaceutical preparations in the control or prevention of high blood pressure and cardiac insufficiency. They can be manufactured according to various methods which are known per se.
摘要:
The compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as set forth above, are described.The compounds of formula I have an inhibitory activity on the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations for the control or prevention of high blood pressure and cardiac insufficiency.
摘要:
The compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the significance given in claim 1, in the form of optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates or mixtures of diastereomeric racemates as well as pharmaceutically usable salts thereof inhibit the activity of the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations in the control or prevention of high blood pressure and cardiac insufficiency.