Abstract: The present invention relates to the alkylidene phosphonate esters of formula I wherein, R1 is selected from a group consisting of hydrogen or alkyl group; R2 is selected from a group consisting of hydrogen, hydroxy, alkyl, alkoxy, nitro, halogen, amino, N-substituted alkylamino; alkyl group is selected from a group consisting of methyl, ethyl and isopropyl; Ar is selected from a group consisting of aryl, substituted aryl, fused aryl, heteroaryl, and substituted heteroaryl. The present invention particularly relates to synthesis and p-glycoprotein induction activity of the alkylidene phosphonate esters. In addition, the invention relates to methods of using compounds for treating or preventing Alzheimer's disease.

Abstract: Disclosed are compositions and methods for the inhibition of biofilm formation or reduction of existing or developing biofilms in a patient. These methods also inhibit the aggregation of bacteria that form biofilms in the airways. The methods include administering to a subject that has or is at risk of developing biofilms a compound or formulation that inhibits the formation or polymerization of actin microfilaments or depolymerizes actin microfilaments at or proximal to the site of biofilm formation. Such a compound can be administered in combination with a compound or formulation that inhibits the accumulation or activity of cells that are likely to undergo necrosis at or proximal to the site of biofilm formation (i.e., neutrophils). The methods and compositions can further include the use of anti-DNA and/or anti-mucin compounds, as well as other therapeutic compounds and compositions.

Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.

Abstract: The present invention concerns conjugate compounds comprising a bisphosphonate covalently bonded to a prostatic acid phosphatase inhibitor and compositions comprising such conjugates. Methods for treating and inhibiting prostate cancer bone metastases, and determining whether a conjugate is useful for such treatment are also provided. In some instances, the bisphosphonate is alendronate, and it is covalently bonded to either tartaric acid or glyceric acid.

Abstract: The present invention provides novel cell-based and animal-based assays for determining antagonists of PKC? and uses of the isolated antagonist compounds for modulating insulin clearance and secretion. The invention also provides novel animals and cells such as animals and cells suitable for use in the assays.

Abstract: An object of the present invention is to elucidate an analgesic effect as one of new cPA bioactivities and thus to provide a novel analgesic agent. The present invention provides an analgesic agent which comprises a cyclic phosphatidic acid derivative that is one type of phospholipid.

Abstract: The invention relates to the use of a compound of the formula (I) for the treatment of bacterial infections caused by mycobacteria, nocardia or corynebacteria, wherein E is phosphorus; X1, X2 and X3 are oxygen; and R1 and R2 are as defined in the specification.

Abstract: The invention relates to the use of certain cyclic acetals or ketals for improving the penetration of pharmaceutical agents into cells and organs.

Abstract: There are provided various compounds and compositions comprising polyunsaturated fatty acid monoglycerides and derivatives thereof. These compounds and compositions can be useful as cancer chemopreventive agents. They can also be useful for enhancing solubility of various active agents and enhancing their bioavailability.

Abstract: Novel flavonoid compounds having anti-oxidant activity are described. The compounds and compositions have been shown to exhibit anti-oxidant properties and are particularly useful in the treatment of ischemia and reperfusion injuries. The invention also describes a method to chemically synthesize such flavonoid compounds and test their efficacy. Such compounds and corresponding pharmaceutically acceptable derivatives and/or salts have uses in the areas of pharmaceuticals, nutraceutical, and veterinary applications.

Abstract: The present invention relates to compounds of phosphonic acid-containing T3 mimetics and monoesters thereof, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndrome x and diabetes.

Abstract: The present invention describes organophosphorus compounds of general formula (I) their preparation and their uses in the activation of gamma/delta T-cells, in the screening of GcpE and LytB enzyme inhibitors and in the prophylaxis and treatment of diseases in humans and animals.

Abstract: Provided is a method of stimulating collagen synthesis and proteoglycan (lumican and keratocan) accumulation. Collagenase isolated keratocytes were cultured with or without insulin with or without ascorbate. Insulin stimulates the synthesis of collagen but does not affect the accumulation of lumican and keratocan. Insulin plus ascorbate, however, stimulates the synthesis of collagen and increased the accumulation of these proteoglycans. The accumulation of PGDS, a KSPG that does not interact with collagen, is not affected by ascorbate. Only the collagen made in the presence of ascorbate was pepsin resistant. EDB overrode the effects of ascorbate on pepsin resistance and proteoglycan accumulation.

Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.

Abstract: There is provided an emulsion composition for therapeutic administration comprising: (a) at least one mono-electron transfer agent phosphate derivative; (b) at leas tone di-electron transfer agent phosphate derivative; wherein the amount of transfer agent phosphate derivatives is no less than equimolar to the amount of di-electron transfer agent phosphate; and (c) a suitable carrier.

Abstract: The present invention relates to application of niacinamide, niacin, and niacin esters (nicotinic acid esters) derivatives of skin beneficial organic acids (henceforth called “derivatives”) for the synergistic treatment or prevention of topical disorders of skin such as acne, rosacea, skin wrinkles, age-spots, canker sores, striae distensae (stretch marks), pimples, and skin redness. These “derivatives” are made by a very simple in-situ method. These “derivatives” provide enhanced bioavailability of both ingredients that are combined to form such derivatives. The “derivatives” of present invention can be formulated in a wide variety of delivery systems including traditional water and oil emulsions, suspensions, colloids, solutions, or anhydrous systems.

Abstract: Metformin salts of lipophilic acids, their pharmaceutical formulations, and methods of administrating the metformin salts for the treatment of hyperglycemia.

Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.

Abstract: Dioxolane analogs of the following formula: 1

Abstract: Compounds of the formula: 1

Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.

Abstract: This invention relates generally to phosphate esters of bis-amino acid sulfonamides containing substituted benzyl amines of formula I: 1

Abstract: Methods and compositions for inhibiting fouling in vinyl monomers are disclosed. Alkylphosphonate esters or acids thereof are added to vinyl monomers, particularly ethylene dichloride, that are undergoing processing to inhibit fouling.

Abstract: Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by combining chemically a diphosphonate compound with a therapeutic agent effective against the foregoing diseases.

Abstract: The invention concerns compounds of the general formula I ##STR1## in which R denotes a lower alkyl which can be substituted if desired by hydroxy, alkoxy, amino, dialkylamino, alkylmercapto, alkylsulfinyl, alkanesulfonyl, cycloalkyl, aryl or a heterocyclic ring, or it denotes lower alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocyclic ring andR.sub.1 and R.sub.2 can be, independently of one another, hydrogen, lower alkyl, cycloalkyl, aryl or arylmethyl,their optically active salts as well as their pharmacologically acceptable salts, processes for their production as well as pharmaceutical agents which contain these compounds for treating diseases of calcium metabolism. Moreover the invention concerns compounds of formula II as intermediate products for the production of compounds of formula I.

Abstract: Novel compounds and use therefor in treating neoplastic and immune system disorders are disclosed. The compound of the present invention comprises a substituted lysophospholipid, which includes a C12 to C20 alkyl ether, a C12 to C20 thioether, or a substituted C3 to C6 heterocycle containing at least two ring heteroatoms, selected from the group consisting of nitrogen, oxygen, sulfur and combinations thereof; and also includes a choline group or a C4 to C7 heterocycle containing heteroatoms selected from the group consisting of nitrogen, oxygen, sulfur and combinations thereof.The method for treating neoplastic or immune system disorders includes administering an effective dose of a compound of the present invention in a therapeutic manner. Effective doses of these compounds result in cytotoxic effects upon various leukemic cell lines.The compounds of this invention have the advantage that these compounds possess antineoplastic and immunomodulatory characteristics.

Abstract: Background of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, or ##STR2## R.sup.3 and R.sup.4 are each, independently, hydrogen, Ar, or --(CR.sup.6 R.sup.7).sub.a Y(CR.sup.8 R.sup.9).sub.b Z, or R.sup.3 and R.sup.4 may be taken together to form a 5-7 membered ring;R.sup.5 is hydrogen, alkyl, alkenyl, alkynyl, alkoxyalkyl, arylalkyl, cycloalkyl, or Ar;R.sup.6, R.sup.7, R.sup.8, and R.sup.9, are each, independently, hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, cycloalkyl, --OR.sup.10, --SR.sup.10, halogen, --CN, --NO.sub.2, --CF.sub.3, --COR.sup.10, --CO.sub.2 R.sup.10, --CONHR.sup.10, --SO.sub.2 R.sup.10, --SO.sub.3 R.sup.10, --OSO.sub.3 R.sup.10, --NR.sup.10 R.sup.11, --NHCOR.sup.10, --NHCO.sub.2 R.sup.10, --NHSO.sub.2 R.sup.10, --NHSO.sub.3 R.sup.10, or Ar;X is O or NOR.sup.12 ;Y is --O--, --CH.sub.2 --, --NR.sup.13 --, --S--, --S(O)--, --S(O).sub.2 --, or --C(O)--;R.sup.10, R.sup.11, R.sup.

Abstract: The compound of the formula I ##STR1## in which R is an aldehyde group or a group which can be converted into an aldehyde, R.sup.1 and R.sup.2 are alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, hydrogen, sodium, potassium, calcium, magnesium, aluminum, lithium, ammonium or triethylamnonium, orR.sup.1 and R.sup.2 together form a cyclic diester,R.sup.3 and R.sup.4 are alkyl, alkenyl, alkynyl, cycloalkyl, hydrogen, alkoxy or halogen, R.sup.5 and R.sup.8 are alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, alkoxy, phenyl, cyanide, hydroxyl or hydrogen, and X, Y or Z are oxygen or sulfur, or prodrug forms of the compound of the formula I can be used for the treatment of diseases caused by viruses.The preparation of these compounds and pharmaceutical preparations containing them and their use is described.

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: The present application discloses novel potassium salts of particular tellurium and selenium compounds which are useful for the stimulation of the production of cytokines.

Abstract: The present invention describes novel 2,4-disubstituted 1,3-dioxolanes having the formula I ##STR1## wherein R.sup.1 represents a long chain alkyl group; X is a covalent single bond, a carbonyl group, a carboxyl group, a carbamoyl group or a --O--P(.dbd.O)(O.sup.z)-- group; z is a negative charge (-) when q is zero, or z is an hydrogen atom when q is one; n is an integer from 2 to 10; R.sup.2, R.sup.3 and R.sup.4 are lower alkyl groups, or R.sup.2 R.sup.3 R.sup.4 N.sup.+ represents an aromatic cyclic ammonium group or R.sup.2 R.sup.3 R.sup.4 N.sup.+ represents a non-aromatic cyclic ammonium group in which two of the groups (R.sup.2, R.sup.3 or R.sup.4) form a non-aromatic ring together with the quaternary nitrogen atom; and A.sup.- is a pharmaceutically acceptable anion. These compounds are in vitro inhibitors of the platelet aggregation induced by the platelet activating factor (PAF) and, thus, useful for the treatment of the diseases in which this substance is involved.

Abstract: A therapeutically effective class of low toxicity aldoxime-substituted functionalized imidazolium compounds and compositions is disclosed which is effective in the treatment of living species poisoned by organophosphorus chemicals which inactivate the enzyme acetylcholinesterase. In vivo administration of therapeutically effective amounts of these aldoxime-substituted imidazolium derivatives has been found to save mammals having inhibited acetylcholinesterase due to injection with lethal dosages of Soman.

Abstract: Compounds of formula (I): ##STR1## (wherein: l is 2-4; A and B are oxygen or sulfur; one of R.sup.1 and R.sup.2 represents a long chain alkyl, alkylcarbamoyl or aliphatic acyl group and the other of R.sup.1 and R.sup.2 represents a group of formula (III) or (II.sub.f): ##STR2## in which E represents a single bond, a bivalent heterocyclic group or a group of formula --CO--, --COO-- or --CONR.sup.6 --, where R.sup.6 is hydrogen or an imino-protecting group; m is 0-3; n is 0-10; q is 0 or 1; R.sup.4 is optionally protected hydroxy, mercapto group or carboxy; Q is an amino or nitrogen-containing heterocyclic group;R.sub.f.sup.4 R.sub.f.sup.5 and R.sub.f.sup.6 are independently selected from the group consisting of hydrogen atoms and C.sub.1 -C.sub.6 alkyl groups, or R.sub.f.sup.4 and R.sub.f.sup.5 or R.sub.f.sup.4, R.sub.f.sup.5 and R.sub.f.sup.

Abstract: The present invention relates to novel compounds of the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and stand for alkyl having 1 to 4 carbon atoms optionally substituted by one or more halogen atoms, alkenyl having 2 to 6 carbon atoms, cycloalkyl having 3 to 6 carbon atoms, phenyl or lower alkoxy-alkyl group,R.sub.3 stands for alkyl having 1 to 6 carbon atoms or alkenyl having 2 to 6 carbon atoms,R.sub.4 and R.sub.5 are the same or different and represent hydrogen, alkyl having 1 to 6 carbon atoms, alkenyl having 2 to 6 carbon atoms, cycloalkyl having 3 to 6 carbon atoms, phenyl, benzyl, phenyl substituted by one or more alkyl having 1 to 3 carbon atoms and/or by one or more halogen atoms, lower alkoxy-alkyl, a group of the formula --(CH.sub.2).sub.n --R.sub.6, wherein n is an integer between 0 to 3 and R.sub.

Abstract: Compounds having the formula ##STR1## R.sub.1 is hydrogen, benzyl or alkanoyl, X is C.sub.2-4 alkylene; andZ-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain and their use as CNS agents, antidiarrheals and antiemetics. Processes for their preparation and intermediates therefor are described.

Abstract: A compound with alpha 1-blocking activity having the formula: ##STR1## wherein R.sub.1 is --H, --CH.sub.3 or --COCH.sub.3 ; R.sub.2 is --H or CH.sub.3 ; and R.sub.3 is ##STR2## wherein .SIGMA. is --H or one or more substituents selected from the group consisting of halogen, --OH and --OCH.sub.3 ; or a pharmaceutically acceptable salt thereof.

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: Certain tellurium compounds have been found to have the ability to stimulate the in vivo and in vitro production of cytokines and their receptors. These compounds may be utilized in the treatment of certain tumors, autoimmune diseases, immune diseases and infectious diseases.

Abstract: New 1-hydroxyethyl-azole derivatives of the general formula ##STR1## in which R represents an alkyl radical, an optionally substituted cycloalkyl radical or an optionally substituted phenyl radical,X represents a nitrogen atom or a CH group,Y represents a grouping --OCH.sub.2 --, -- CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--,Z represents a halogen atom, an alkyl, cycloalkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy or halogenoalkylthio radical, an optionally substituted phenyl radical, an optionally substituted phenoxy radical, an optionally substituted phenylalkyl radical or an optionally substituted phenylalkoxy radical andm is 0, 1, 2 or 3,a process for their preparation and their use as plant growth regulators and fungicides.

Abstract: Oxime N-alkyl-N-.alpha.-(alkylthio-phosphorothio)acyl carbamates represented the structure: ##STR1## wherein the R represents various imino radicals, Q is oxygen or sulfur and the numbered R groups represent various alkyl substituents, which exhibit superior insecticidal and miticidal activity.

Abstract: This invention relates to phosphoroamidothioate and phosphoroamidodithioate compounds, to compositions thereof which are useful as pesticides, for example, as athropodicides (that is, insecticides and acaricides), nematocides, and fungicides, and to a method of controlling pests, such as insects, acarids, nematodes, and fungi. The compounds of the invention are effective against soil insects, especially the corn rootworm, when applied by soil application techniques and are also effective when applied to agricultural plants and other plants by foliar application techniques.

Abstract: A cyanohydrin phosphate of the formula ##STR1## wherein R represents a hydrogen atom or an optionally substituted radical selected from alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aralkyl, aralkenyl and aryl, or an optionally substituted heterocyclic radical,R.sup.1 and R.sup.2 are identical or different and individually represent optionally substituted radicals selected from alkyl, alkenyl, alkynyl, aryl, aralkyl, alkoxy, aryloxy, aralkoxy, alkylthio, alkenylthio, alkinylthio, arylthio, aralkylthio, alkylamino (monoalkylamino or dialkylamino), arylamino and aralkylamino, or together represent alkanediyl, alkanedioxy, aminoalkyloxy or alkanediamino, andX represents oxygen or sulphur,are obtained by the reaction of a phosphoric acid chloride of the general formula ##STR2## wherein X, R.sup.1 and R.sup.2 have the meaning given above, with an aldehyde of the general formulaR--CHO (III)wherein R has the meaning given above, in the presence of an approximately equimolar quantity of water-soluble cyanides.

Abstract: Novel, aryl N-(alkylthio-phosphorothio)acyl carbamates represented by structure: ##STR1## wherein the R groups represent various alkyl substituents, and Ar represents an aryl radical with various organic substituents, which exhibit superior insecticidal and miticidal activity.