Abstract: The invention relates to new gem-diphosphonates derivatives substituted by phenol groups of formula (I): ##STR1## as well as the process for their preparation and the pharmaceutical compositions containing them.

Abstract: Araliphatylaminoalkanediphosphonic acids of formula ##STR1## wherein R.sub.1 is an aromatically substituted aliphatic radical, R.sub.2 is hydrogen or a monovalent aliphatic radical and alk is a divalent aliphatic radical, and their salts, exhibit a pronounced regulatory action on the calcium metabolism and can be used as medicaments for the treatment of diseases that are attributable to calcium metabolism disorders. They are prepared, for example, by reacting a compound of formula ##STR2## wherein X.sub.3 is a carboxy and R.sub.0 is a radical R.sub.2, with phosphorous acid and phosphorous trichloride and hydrolysing the primary product.

Abstract: The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, guadinine, isourea, isothiourea an biguanide functions may be converted to such pro-drugs. The pro-drugs are hydrolyzed in the body, regenerating the original drugs with the release of a salt of phsophoric acid.

Abstract: The invention relates to new gem-diphosphonates derivatives substituted by phenol groups of formula (I): ##STR1## as well as the process for their preparation and the pharmaceutical compositions containing them.

Abstract: Pharmaceutical compositions and a method for inhibiting the growth of tumor cells by administering a tumor cell growth-inhibiting amount of a bis[bis (diphenylphosphino)hydrocarbon]-, bis[bis(diethylphsophino) hydrocarbon]-, bis[bis(diphenylphosphine-deithylphosphino) hydrocarbon]gold(I), silver(I) or copper(I) complex or a tris[bis(diphenylphosphino)ethane] dicopper(I) complex to an animal afflicted with said tumor cells.

Abstract: Compounds of the formula I ##STR1## in which R.sub.1 is an aromatic radical, n is 0, 1, 2 or 3, X is an oxy group, a thio group which can be oxidized or an imino group which is unsubstituted or has aliphatic substituents, alk.sub.1 and alk.sub.2 are identical or different divalent aliphatic radicals, and R.sub.2 is hydrogen or a monovalent aliphatic radical and salts thereof have properties which regulate calcium metabolism and can be employed for the treatment of diseases connected with disturbances in this metabolism. They are prepared, for example, by reacting a compound of the formula ##STR2## in which X.sub.3 is carboxyl with a phosphorylating agent and hydrolysing the primary product.

Abstract: The present invention provides compounds of the formula: ##STR1## The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them useful in treatment and prophylaxis of disorders of calcium metabolism.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 -A- is a group of the formula: ##STR2## in which R.sup.1 is aryl or a heterocyclic group, each of which may be substituted with substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, halo(lower)alkyl, acyl, acylamino and halogen, or lower alkyl which may be substituted with a heterocyclic group optionally substituted with acyl, andX is O or S, andR.sup.2 is hydrogen or lower alkyl, provided that when R.sup.1 is lower alkyl, thenR.sup.1 -A- is a group of the formula: ##STR3## in which R.sup.1 and X are each as defined above, processes for the preparation thereof and pharmaceutical composition comprising the same.

Abstract: Compounds of the formula: ##STR1## and stereoisomers thereof wherein X and Y, which are the same or different, are hydrogen, halogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted heteroaryloxy, optionally substituted arylalkoxy, optionally substituted heteroarylalkoxy, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, cyano, --CO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, or --COR.sup.6, except that X and Y are not both hydrogen; R.sup.1 and R.sup.2, which are the same or different, are alkyl or fluoroalkyl; and R.sup.3, R.sup.4, R.sup.5 and R.sup.6, which are the same or different, are hydrogen, alkyl, alkenyl, alkynyl, optionally substituted aryl, optionally substituted aralkyl, or cycloalkylalkyl.

Abstract: A method for treating or preventing osteoporosis utilizing a cyclic regimen comprising alternating for two or more cycles the administration of a bone resorption inhibiting polyphosphonate and a no treatment (rest) period. Further disclosed is a kit for use in implementing this method of treatment.

Abstract: 2-Substituted-1,3-propylidenediphosphonates of formula (I), where A, R.sup.1 and R.sup.2 are defined in claim 1, are therapeutically active compounds, namely for the treatment of cardiovascular diseases.They can be prepared by reacting phosphonating agents with 1,3- dibromopropanes or ditosylates of 1,3-propanediols substituted in position 2. ##STR1## .

Abstract: A composition and method for the treatment of melanomas in human beings wherein the composition comprises at least one O-phosphorylated derivative of 3-(3,4-dihydroxy)phenylalanine.

Abstract: A granulor formulation of a mosquito larvicide is prepared by impregnating corncob granules with an oil suspension or solution of a suitable toxicant in order to deposit the material on the surface of the granules. The impregnated granules float and are suitable for dispersion over a wide variety of larval mosquito sources.

Abstract: The invention relates to novel urease inhibited fertilizer compositions containing urea and a urease inhibiting amount of one or more diaminophosphinyl compounds having oxidized sulfur functions, and methods and composition for inhibiting the activity of urease through use of such compounds.

Abstract: The invention relates to novel urease inhibited fertilizer compositions containing urea and a urease inhibiting amount of one or more o-diaminophosphinyl derivatives of oximes, and methods and composition for inhibiting the activity of urease through use of such compounds.

Abstract: A composition and method for the treatment of melanomas in human beings wherein the composition comprises at least one O-phosphorylated derivative of 3-(3,4-dihydroxy)phenylalanine.

Abstract: 1-hydroxy-1,1-diphosphonic acid compounds corresponding to the following general formula ##STR1## in which R and R.sub.1 represent hydrogen or methyl,X represents hydrogen, halogen, amino, which may be acyl substituted, lower alkyl, which may be substituted by amino or acyl substituted amino, or lower alkoxy,Y represents O, S or NHZ represents lower alkylene, which may be substituted by amino or acyl substituted amino, andm and n have the value 0 or 1 with the proviso that, where n is 1, m is also 1;and to pharmacologically compatible salts thereof.The invention also relates to a process for producing these compounds and to their use in pharmacological preparations having cytostatic activity.

Abstract: A composition and method useful for increasing the accumulation of melanin in the skin of humans and other mammals wherein the composition comprises at least one O-phosphorylated derivative of 3-(3,4-dihydroxy)phenylalanine.

Abstract: Diphosphonic acid derivatives of Formula I ##STR1## wherein R is hydrogen, an alkali metal atom, an alkaline earth metal atom, or an alkyl group of 1-4 carbon atoms andA is derived from a carboxylic acid having anti-inflammatory and antiphlogistic activity and containing an aromatic or heteroaromatic group, of Formula IIACOOH (II),are pharmacologically efficacious compounds.