Abstract: The present invention provides diphosphonic acid derivatives of the general formula: ##STR1## according to claim 1. These compounds are useful for the treatment or prophylaxis of calcium metabolism disturbance or disease.

Abstract: The present invention provides 1-Hydroxy-3-(N-methyl-N-propylamino)propane-1,1-diphosphonic acid of formula ##STR1## wherein R is hydrogen or C.sub.1 -C.sub.4 alkyl and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of a diphosphonic acid of formula I and pharmaceutical compositions containing it for the treatment of diseases of the calcium metabolism.

Abstract: The present invention provides disphosphonates of the general formula: ##STR1## wherein R.sub.1 is a straight-chain or branched, saturated or unsaturated aliphatic hydrocarbon radical of 1-9 carbon atoms which is optionally substituted by phenyl or cyclohexyl, R.sub.2 is cyclohexyl or cyclohexylmethyl, benzyl or a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon of 4 to 18 carbon atoms which is optionally substituted by phenyl or oxygen wherein the oxygen can be esterified or etherified, R.sub.3 is hydrogen or a straight-chain or branched alkyl of 1-4 carbon atoms, X is a straight-chain or branched alkylene chain of 1-6 carbon atoms and Y is hydrogen, hydroxyl or an amino group optionally substituted by alkyl radicals of 1-6 carbon atoms; as well as the pharmacologically acceptable salts thereof.

Abstract: The present invention provides diphosphonates of the general formula: ##STR1## wherein Het is 1,2,3-triazole, or 1,2,4-triazole radical, which is optionally substituted by alkyl, alkoxy, halogen, hydroxyl, carboxyl, an amino group optionally substituted by alkyl or acyl radicals or is a benzyl radical optionally substituted by alkyl, nitro, amino or aminoalkyl, A is a straight-chained or branched, saturated or unsaturated hydrocarbon chain containing 2 to 8 carbon atoms, X is a hydrogen atom, optionally substituted by acyl, or an amino group optionally substituted by alkyl or acyl radicals and R is a hydrogen atom or an alkyl radical; and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these diphosphonates and pharmaceutical compositions containing them.

Abstract: The present invention produces alkyldiphosphonic acid derivative of the general formula: ##STR1## wherein Het is a heteroaromatic five-membered ring containing to 3 heteroatoms which can be partly hydrogenated and optionally substituted one or more times by alkyl, alkoxy, phenyl, cyclohexyl, cyclohexylmethyl, halogen or amino, and two adjacent alkyl substituents can together also form a ring, Y is a hydrogen atom or a lower alkyl radical, X is a hydrogen atom, a hydroxyl group or an amino group optionally substituted by lower alkyl and R is a hydrogen atom or a lower alkyl radical, with the proviso that Het is not a pyrazole ring; as well as the pharmacologically acceptable salts thereof.

Abstract: Diphosphonate compounds, processes for their preparation and pharmaceutical compositions containing them and being useful for treating calcium metabolism disorders. The diphosphonates are of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen, acyl or alkyl which can be substituted by aryl, R.sub.3 and R.sub.4 are hydrogen or alkyl or R.sub.3 and R.sub.4 together represent lower alkylene, R.sub.5 is a hydrogen atom or alkyl, X is a valency bond or alkylene, Y is a valency bond, alkylene or substituted alkylene, Z is hydrogen, hydroxyl or amino group optionally substituted by alkyl and n is 1, 2 or 3; and including the pharmacologically acceptable salts thereof.

Abstract: The present invention provides diphosphonates of the general formula: ##STR1## wherein Het is an imidazole, oxazole, isoxazole, thiazole, pyridine, 1,2,3-triazole, 1,2,4-triazole or benzimidazole radical, which is optionally substituted by alkyl, alkoxy, halogen, hydroxyl, carboxyl, an amino group optionally substituted by alkyl or alkanoyl radicals or a benzyl radical optionally substituted by alkyl, nitro, amino or aminoalkyl, A is a straight-chained or branched, saturated or unsaturated hydrocarbon chain containing 2 to 8 carbon atoms, X is a hydrogen atom, optionally substituted by alkanoyl, or an amino group optionally substituted by alkyl or alkanoyl radicals and R is a hydrogen atom or an alkyl radical; and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these diphosphonates and pharmaceutical compositions containing them.

Abstract: The present invention provides diphosphonic acid derivatives of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, independently of one another or also together, signify hydrogen atoms or lower alkyl radicals, whereby R.sub.1 and X or R.sub.3 and Y or R.sub.4 and Z, together with the nitrogen atom to which they are attached, can form a five- or six-membered ring, X and Y, which can be the same or different, represent a straight-chained or branched alkylene chain with up to 6 carbon atoms which can optionally be substituted by aromatic or heteroaromatic radicals, Z is a straight-chained or branched alkylene chain with up to 6 carbon atoms, which can be interrupted by heteroatoms and can optionally also be substituted by aromatic or heteroaromatic radicals, n is 0, 1 or 2 and A is a hydrogen atom or a hydroxyl group, and the pharmacologically acceptable salts thereof.

Abstract: The present invention provides phospholipids of the general formula: ##STR1## wherein X is a valency bond, an oxygen or sulphur atom or a sulfonyl, sulfinyl, phenylene, cycloaklylene, carbonylamino, aminocarbonyl, ureido or carbonyl group, R.sub.1 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon radical containing up to 18 carbon atoms, which is optionally substituted one or more times by halogen, alkoxy, alkylthio, alkanesulfinyl, alkanesulfonyl, carbalkoxy or phenyl, R.sub.2 is a straight-chained or branched, saturated or unsaturated divalent aliphatic hydrocarbon radical containing up to 18 carbon atoms, which is optionally substituted one or more times by halogen, alkoxy, alkylthio, alkanesulphinyl, alkanesulphonyl, carbalkoxy or phenyl, Y is an oxygen atom or a --O--CO--O--, --O--CO--NH-- or --O--CS--NH-- group, R.sub.

Abstract: Sulfur-containing phospholipid compounds of the formula ##STR1## pharmaceutical compositions having anti-tumor activity which include said phospholipid compounds, and the method of use for combating tumors, of said phospholipid compounds.

Abstract: 2-Substituted-1-aziridine-carboxylic acid esters exhibiting immuno-stimulant activity and of the formula ##STR1## wherein X is a carbamoyl or alkoxycarbonyl radical, andR.sup.1 is an aliphatic hydrocarbon radical optionally substituted by halogen, alkoxy, amino, carbamoyloxy, cycloalkyl, hydroxyl, an imido or heterocyclic radical, cycloalkyl; or aryl, aralkyl, aryloxyalkyl or arylthioalkyl wherein the aryl moiety is optionally substituted by halogen, alkyl, alkoxy, hydroxyl, amino, nitro, cyano, acyl, carbalkoxy, thioalkyl, alkylsulphonyl, phenyl or trifluoromethyl. Counterparts where X is --CN and R.sup.1 is as above, except for ethyl, are also new.

Abstract: 1-(N-Acyl-carbamoyl)-2-cyanoaziridines of the formula ##STR1## wherein X is oxygen or sulphur,Z is hydrogen or an organic radical, andY is a carbonyl, sulphonyl, sulphinyl, sulphenyl, phosphoryl or phosphonyl radical,and salts thereof, exhibit immune-stimulating and cancerostatic activities.

Abstract: 1-Acyl-2-cyanoaziridines of the formula ##STR1## wherein R is an acyl radical of a carboxylic, sulphonic, sulphinic, sulphenic, phosphonic or phosphoric acid,exhibit immune-stimulating and cancerostatic activities.

Abstract: New 3-nitropyrazole compounds of the formula: ##STR1## wherein R.sub.1 is lower alkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is cyano, carboxyl or lower alkoxycarbonyl or the radical --CO-NR.sub.4 R.sub.5, in whichR.sub.4 is hydrogen or hydroxyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, thiocarbamoyl, ureido, thioureido, hydroxyphenyl, picolyl or is a lower alkyl, alkenyl or cycloalkyl radical substituted, if desired, by a cyano, hydroxyl, pyrrolidino, piperidino, amino, lower alkylamino, lower dialkylamino or lower acylamino substituent andR.sub.5 is a hydrogen atom or a lower alkyl radical orR.sub.4 and R.sub.5 together represent a lower alkylene bridge;And the pharmacologically compatible salts thereof are outstandingly effective as anti-microbial agents, particularly systemically and in the urinary tract.

Abstract: New 3-nitropyrazole compounds of the formula: ##STR1## wherein R.sub.1 is lower alkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is cyano, carboxyl or lower alkoxycarbonyl or the radical --CO--NR.sub.4 R.sub.5, in whichR.sub.4 is hydrogen or hydroxyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, thiocarbamoyl, ureido, thioureido, hydroxyphenyl, picolyl or is a lower alkyl, alkenyl or cycloalkyl radical substituted, if desired, by a cyano, hydroxyl, pyrrolidino, piperidino, amino, lower alkylamino, lower dialkylamino or lower acylamino substituent andR.sub.5 is a hydrogen atom or a lower alkyl radical orR.sub.4 and R.sub.5 together represent a lower alkylene bridge;And the pharmacologically compatible salts thereof, are outstandingly effective as anti-microbial agents, particularly systemically and in the urinary tract.

Abstract: New nitropyrazole compounds of the formula ##STR1## wherein R.sub.1 is alkyl or hydroxyalkylR.sub.2 and R.sub.3, which may be the same or different, are alkyl orR.sub.2 and R.sub.3 together represent a 4- or 5-membered alkylene bridge which is optionally interrupted by an oxygen atom or by the grouping >N-R, in which R is an alkyl or hydroxyalkyl radical;And the pharmacologically compatible salts thereof, possess excellent anti-microbial action not only in vitro but also in vivo, especially systemically.

Abstract: Nitroimidazolyl-s-triazolo[4,3-b]pyridazines of the formula: ##STR1## wherein R is hydrogen or lower alkyl optionally substituted in the 2-position by hydroxyl or by lower acyloxy or lower alkoxy;A is hydrogen, halogen, azido, cyano; lower alkyl alkoxy, alkylthio, alkylsulfonyl, carboxyl; lower alkoxycarbonyl, lower alkoxycarbonimidoyl; or hydrazino, carbamoyl, amidino or a carboximidohydrazide group optionally substituted by one or two lower acyl, alkyl or cycloalkyl radicals; orA is a radical of the formula: ##STR2## wherein R.sub.1 and R.sub.2 are, individually, hydrogen or a number of organic radicals or, taken together, can be an alkylene bridge; andR.sub.3 is hydrogen or lower alkyl; or, together with R.sub.2, R.sub.3 can form an alkylene bridge;n is 0 or 1;And the pharmaceutically compatible thereof, possess high in vivo effectiveness as antimicrobials.

Abstract: Nitroimidazolyl-s-triazolo[4,3-b]pyridazines of the formula: ##SPC1##Wherein R is hydrogen or lower alkyl optionally substituted in the 2-position by hydroxyl or by lower acyloxy or lower alkoxy;A is hydrogen, halogen, azido, cyano; lower alkyl, alkoxy, alkylthio, alkylsulfonyl, carboxyl; lower alkoxycarbonyl, lower alkoxycarbonimidoyl; or hydrazino, carbamoyl, amidino or a carboximidohydrazide group optionally substituted by one or two lower acyl, alkyl or cycloalkyl radicals; orA is a radical of the formula: ##EQU1## wherein R.sub.1 and R.sub.2 are, individually, hydrogen or a number of organic radicals or, taken together, can be an alkylene bridge; andR.sub.3 is hydrogen or lower alkyl; or, together with R.sub.2, R.sub.3 can form an alkylene bridge;n is 0 or 1;And the pharmaceutically compatible thereof, possess high in vivo effectiveness as antimicrobials.

Abstract: Nitrofuryl-triazolo[4,3-b]pyridazine compounds of the formula ##SPC1##WhereinR.sub.1 is lower alkoxy radical or a saturated 5- or 6-membered heterocyclic ring attached via a cyclic nitrogen atom, which heterocyclic ring can also contain, in addition to said cyclic nitrogen atom, a cyclic oxygen atom or an optionally lower alkylated cyclic nitrogen atom and R.sub.2 is a hydrogen atom or R.sub.1 and R.sub.2 together represent an additional valency bond,Are outstandingly effective as bacteriostats and are particularly useful in the treatment of bacterial infections in the urinary tract.

Abstract: Certain novel nitrofuran compounds of the formula: ##SPC1##WhereinHet is an aromatic heterocylic linkage;B is a bond or vinylene;Y is O or S;m is 0 or 1;X is hydrogen, lower alkyl or alkanoyl; andThe R's are variously defined;Are outstandingly effective bacteriostats and bactericides.