摘要:
Substituted mono- and bipyridylmethylpyridones are prepared either by reaction of pyridones with mono- or bipyridylmethylhalogen compounds or by reaction of pyridone-substituted halogenopyridines with tetrazolylphenylboronic acids. The substituted mono- and bipyridylmethylpyridones can be employed as active compounds in medicaments, in particular for the treatment of arterial hypertension and atherosclerosis.
摘要:
Sulphonylbenzyl-substituted imidazoles can be prepared by first reacting imidazolylaldehydes with sulphonylbenzyl compounds and then oxidising or reducing the aldehyde function in the customary manner.The sulphonylbenzyl-substituted imidazoles can be used as active compounds in medicaments.
摘要:
The present invention relates to new substituted benzoxazepines and benzothiazepines of the general formula I ##STR1## in which X, R.sup.1, R.sup.2 and R.sup.3 have the meaning given in the description, processes for their preparation and their use in medicaments having vaso- and muscle-relaxing properties, in particular as circulatory agents.
摘要:
Renin-inhibiting peptides of the formula ##STR1## in which X represents a group of the formula ##STR2## represents hydroxyl, alkoxy having up to 8 carbon atoms, benzyloxy or a group of the formula --NR.sup.4 R.sup.5,A, B, D and E are identical or different and in each caserepresent a direct bond,represent a radical of the formula ##STR3## in which Q1 denotes oxygen, sulphur or the methylene grouprepresent a grouping of the formula ##STR4## m represents a number 0, 1 or 2, and L represents a group of the formula --CH.sub.2 NR.sup.2 R.sup.3and physiologically acceptable salts thereof.
摘要:
Renin-inhibiting aminomethyl peptides of the formula ##STR1## in which A is H, an alkyl radical, a sulphonyl radical or an amino-protecting group,B, D, E and F each independently is a direct bond or an amino-organo-carbonyl group,R.sup.1 is an optionally substituted alkyl or aryl radical,R.sup.2 is H, alkyl or acyl,R.sup.3 is H, alkyl, aryl or acyl, andR.sup.4 is alkyl, alkoxy, aryl or amino,and physiologically acceptable salts thereof.
摘要:
Circulation active tetrahydropyridines of the formula ##STR1## in which R.sup.1 represents a straight-chain, branched or cyclic, saturated or unsaturated hydrocarbon radical which has up to 20 carbon atoms and can be interrupted in the chain by an oxygen atom or a sulphur atom and/or can be substituted by halogen, cyano, hydroxyl, acyloxy, nitro or nitrooxy, or by a phenyl, phenoxy, phenylthio or phenylsulphonyl group which is optionally substituted by halogen, cyano, dialkylamino with in each case 1 or 2 carbon atoms per alkyl group, alkoxy with 1 to 4 carbon atoms, alkyl with 1 to 4 carbon atoms, trifluoromethyl or nitro, or by an .alpha.-, .beta.- or .gamma.-pyridyl group, or by an amino group, this amino group carrying 2 identical or different substituents from the group comprising alkyl with up to 4 carbon atoms, alkoxyalkyl with up to 4 carbon atoms, phenyl and aralkyl, and these substitutents optionally forming, with the nitrogen atom, a 5- to 7-membered ring which can contain, as a further hetero atom, an oxygen or sulphur atom or an N-phenyl or N-alkyl grouping, this alkyl group containing 1 to 3 carbon atoms,R.sup.2 represents phenyl, naphthyl, thienyl, furyl, pyrryl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl, pyridazinyl, pyrimidyl, pyrazinyl, indolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzoxadiazolyl, benzothiadiazolyl, quinolyl, isoquinolyl, quinazolyl or quinoxalyl;whereinm denotes a number from 0 to 2 and alkyl contains 1 to 4 carbon atoms with optionally 1 to 3 fluorine atoms,R.sup.3 represents a group of the formula --CN or --COOR.sup.5, whereinR.sup.5 has the same meaning as R.sup.1 and can be identical to or different from this radical, andR.sup.4 represents hydrogen, or represents phenyl or naphthyl, and their pharmaceutically acceptable acid addition salts.
摘要:
Compositions for treating hypertension comprising an effective amount of a dihydropyridine of the formula ##STR1## in which X is 1 or 2 identical or different substituents from the group consisting of nitro, chlorine and trifluoromethyl, or together with the phenyl ring, the group ##STR2## R.sup.1 is alkyl of 1 to 4 C atoms, which is optionally substituted by alkoxy of 1 to 4 C atoms,R.sup.2 is alkyl of 1 to 12 C atoms, which is optionally substituted by alkoxy of 1 to 3 C atoms, fluorine or N-methyl-N-benzylamino andR.sup.3 is alkyl of 1 to 4 C atoms, cyano or hydroxymethyl, and a pyridazodiazepine of the formula ##STR3## in which R.sup.4 is aralkyl,R.sup.5 is hydrogen or alkyl of 1 to 8 C atoms,R.sup.6 is hydrogen or alkyl of 1 to 8 C atoms andR.sup.7 and R.sup.8 are hydrogen, or together, an oxo group, are described.
摘要翻译:用于治疗高血压的组合物,其包含有效量的式“IMAGE”的二氢吡啶,其中X是与硝基,氯和三氟甲基相同或不同的取代基,或与苯环一起,组IMA IMA > R 1为1〜4个C原子的烷基,其任选被1〜4个C原子的烷氧基取代,R 2为1〜12个C原子的烷基,其任选被1〜3个C原子的烷氧基取代,氟或N - 甲基-N-苄基氨基,R3为1-4个C原子的烷基,氰基或羟甲基,以及其中R 4为芳烷基,R 5为氢或1至8个C原子的烷基的式“IMAGE”的吡咯并二氮杂为R6 氢或1〜8个碳原子的烷基,R7和R8为氢,或一起为氧代基。
摘要:
4-(Nitrophenyl)-1,2,3,4-tetrahydropyridines of the formula ##STR1## in which R.sub.1 and R.sub.2 are identical or different and each represent hydrogen, phenyl or a straight-chain or branched alkyl radical which is optionally substituted by halogen or alkoxy,R.sub.3 represents a straight-chain or branched alkyl radical which is optionally substituted by alkoxy, halogen, alkylamino or aryl,X represents a single bond, an oxygen atom, a sulphur atom or the NH group andY denotes either the nitrile group or the radical ##STR2## wherein X' corresponds to the definition of X and can either be identical to X or different from X, andR.sub.4 corresponds to the definition of R.sub.3 and can be either identical to R.sub.3 or different from R.sub.3,or physiologically acceptable salts thereof, which are active on the circulation system, for example as vasodilators.
摘要:
Dihydropyridines of the formula ##STR1## in which R is aryl or heterocyclic,R.sup.1, R.sup.2 and R.sup.3 each is hydrogen or various organic radicals,Y is oxygen, or optionally substituted --NH--,Z is --O--NO.sub.2 or --O--NO,X is --COR.sup.4, --COOR.sup.5 or --CO--Y--A--Z,R.sup.4 is alkyl, phenyl, benzyl or an amino radical, andR.sup.5 is an organic radical,or pharmaceutically acceptable acid addition salts thereof, exhibit circulation active properties, e.g. they can be used as antihypertensives, as peripheral and cerebral vasodilators and as coronary therapeutics.
摘要:
The invention relates to substituted 4-aminomethylene-chromans and chromens of Formula (I) infra, as well as methods for making of said chromans and chromens, compositions containing said chromans and chromens and methods for the use of said chromans, chromens and compositions containing said chromans and chromens. The compounds and compositions of the invention are useful for their circulation influencing activity.