Abstract: The invention features an oral pharmaceutical solution comprising a therapeutically effective amount of alendronate or a salt thereof and a pharmaceutically acceptable liquid carrier. The solution is substantially free from degradation products, with the proviso that the solution has no buffer and no complexing agent. The oral solution avoids the difficulties in swallowing tablets of the prior art. Moreover, the oral solution is surprisingly stable without the use of buffering systems and complexing agents of the prior art.

Abstract: The present invention provides compositions and methods and for increasing the bioavailability of therapeutic agents in a subject. The compositions include at least one alkyl glycoside and at least one therapeutic agent, wherein the alkylglycoside has an alkyl chain length from about 10 to about 16 carbon atoms.

Abstract: Lipid prodrugs of pharmaceutical agents and their analogs that have increased anticancer, anti-viral, anti-inflammatory, anti-proliferative activity over the parent drug, and methods for making lipid prodrugs. Compositions comprising lipid prodrugs for treating disease and methods for treating disease which involve using the compositions.

Abstract: The invention provides reagents and methods for conjugating a polymer specifically to the ?-amine of a polypeptide. The invention provides monofunctional, bifunctional, and multifunctional PEGs and related polymers having a terminal thioester moiety capable of specifically conjugating to the ?-amine of a polypeptide having a cytokine or histidine residue at the N-terminus. The invention provides reactive thioester-terminated PEG polymers that have suitable reactivity with an N-terminal cysteine or histidine residue of a polypeptide to produce an amide bond between the PEG molecule and the polypeptide.

Abstract: The present invention relates to stable aqueous oral formulation of bisphosphonic acid or its pharmaceutically acceptable salts. More particularly, the present invention relates to stable aqueous oral formulation of alendronate sodium. The present invention also relates to a process for the preparation of stable aqueous oral formulation of alendronate sodium.

Abstract: Inhibitors of bone calcium resorption are administered, and calcium intake in the subject's diet is restricted, to allow high doses of vitamin D compounds or mimetics to be given with the intent of treating diseases such as metabolic bone diseases, hyperparathyroidism, cancer, psoriasis, and autoimmune diseases without the dangers of calcification of kidney, heart, and aorta. Inhibitors of bone calcium resorption include the bis-phosphonates, OPG (osteoprotegerin) or the soluble RANKL (receptor activator of NF-?B ligand) receptor known as sRANK (soluble RANK which is the protein expressed by the NF-?B gene), and function to block the availability of calcium from bone thereby preventing hypercalcemia and the resulting calcification of soft tissues. Thus, high doses of 1?,25-dihydroxyvitamin D3 (1,25-(OH)2D3), its analogs, prodrugs, or mimetics can be utilized to treat the target disease with minimal risk to a patient.

Abstract: The invention provides methods for the adsorption of an active pharmaceutical ingredient on titianium dioxide nanoparticles which can be orally ingested allowing the drug release into the intestine without causing side effects to the upper gastrointestinal region.

Abstract: The present invention is directed to polyphosphorylated and pyrophosphate derivatives of cyclitols. More particularly, the invention relates to polyphosphorylated and pyrophosphate derivatives of inositols. The invention also relates to compositions of the polyphosphorylated and pyrophosphate derivatives of inositol and other similar, more lipophilic derivatives, and their use as allosteric effectors, cell-signaling molecule analogs, and therapeutic agents.

Abstract: There is provided a composition for promoting the production of and/or enhancing the activity of fibulin-5, said composition comprising as an active ingredient one or a plurality of pharmaceutical agents selected from the group consisting of extracts of Caesalpinia crista, extracts of Psophocarpus tetragonolobus, phytic acid and a pharmaceutically acceptable salt thereof, and L- hydroxyproline and a pharmaceutically acceptable salt thereof.

Abstract: the present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The preformulations are suitable for generating parenteral, non-parenteral and topical depot compositions for sustained release of active agents. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.

Abstract: The present invention is directed to a method of altering the amount or composition of synovial fluids secreted from joints in a subject in need of such treatment. The method comprises administering to a subject a pharmaceutical composition comprising a P2Y purinergic receptor agonist in an amount effective to alter the amount or composition of synovial fluids. The P2Y purinergic receptor agonist is administered in an amount effective to stimulate secretion of synovial fluid, lubricin, hyaluronic acid, or surface-active phospholipids; to enhance joint lubrication; or to treat osteoarthritis. The pharmaceutical compositions useful in the present invention comprise a P2Y purinergic receptor agonist of Formula I and include, but are not limited to: uridine-, adenosine-, cytidine-5?-di- or triphosphates, dinucleoside polyphosphates, and analogs thereof. The invention is useful for treating conditions associated with reduced joint lubrication and joint stiffness, such as osteoarthritis.

Abstract: Methods and composisions for enhancing cellular function through protection of a tissue components such receptors, proteins, lipids, nucleic acids, carbohydrates, hormones, vitamins, and cofactors, by administering pyrophosphate analogs or related compounds.

Abstract: Segmented water soluble polymers, containing a higher molecular weight segment linked to a lower molecular weight segment, are described. In one embodiment, the polymer segments are poly(ethylene glycol) segments. The segmented polymers are functionalized and are useful for conjugation to various moieties such as pharmacologically active substances. Also described are conjugates of such polymers and methods of their preparation.

Abstract: High molecular weight derivatives of activated poly(ethylene glycol) and the like polymers are prepared in high purity by conjugating a large PEG molecule to a small PEG molecule. Most of the reaction steps can be accomplished on the more readily purified small molecule to avoid laborious purification of the high molecular weight derivatives.

Abstract: The invention relates to use of ibandronic acid (1-hydroxy-3-(N-methyl-N-pentyl)aminopropyl-1,1-diphosphonic acid) or physiologically compatible salts or esters thereof for improving the osseointegration of cement-free anchored endoprostheses. Ibandronate or salts thereof is applied for a short time immediately after insertion of an endoprosthesis, with the surprising result that secondary stability of the implant is obtained in only 5 weeks or less after the operation.

Abstract: The present invention relates to a parenteral composition comprising a bisphosphonic acid or a pharmaceutically acceptable salt thereof (bisphosphonate) as active component and a pharmaceutically acceptable chelating agent, processes of the preparation of this composition, and methods of their use in the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, hypercalcemia of malignancy, and metabolic bone disease. The compositions are especially useful for improving the local tolerance of the active component when administered parenterally.

Abstract: Throxinyldimethylphosphinate was invented as a prodrug to stabilize thyroxine, a drug widely used to treat hypothyroidism. The presence of the dimethylphosphinate group at the phenolic hydroxyl of thyroxine is key to preventing thyroxine from decomposing through the proposed pathway. The prodrug will be hydrolyzed in the stomach or the gut into thyroxine and the biologically inert dimethylphosphinic acid. Related products may be stabilized with the same or similar protecting groups.

Abstract: The present invention relates to novel uses of 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid or any of its soluble salts or any of its hydrates, in particular its use for the manufacture of a medicament for selective modulation of osteoblasts.

Abstract: Estramustine phosphate is shown to act as an inhibitor of bone resorption and can thus be used to treat, prevent or alleviate the symptoms of bone metastasis which arise due to said bone resorption.

Abstract: The invention relates to an insecticidal and miticidal composition which contains as active ingredients chlorfenapyr in combination with one or more organophosphoric acid ester-type compounds and to a method for controlling insecticidal or miticidal pests which have acquired resistance to commercial insecticidal and miticidal agents.

Abstract: Controlled release compositions of matter are disclosed comprising complexes for treating a population of one or more aquatic organisms in a column of water. The complexes comprise at least one system wherein the system comprises at least one bioactive agent as a component selected for treating a population of aquatic organisms, at least one carrier component, and at least one coating component for regulating the controlled release rate and release profile of the bioactive agent in water or at least one bioactive agent and one joint-function component that can serve as both a carrier and coating to regulate the controlled release rate and release profile of the bioactive agent in water, with or without optional binder components and/or additional formulation materials. The components are selected to sink or float so that the complexes will permeate and/or remain in any planar or volumetric segment of a water column for a period of time that is sufficient to effectively treat a population of aquatic organisms.

Abstract: The object of the invention are novel halogen substituted methylenebisphosphonic acid anhydrides, ester anhydrides, amide anhydrides, and ester amide anhydrides, processes for the preparation of these novel compounds, as well as pharmaceutical preparations comprising these novel compounds.

Abstract: Alendronate, an aminobisphosphonate, can prevent osteoporosis in early post menopausal women.

Abstract: The invention relates to an insecticidal and miticidal composition which contains as active ingredients chlorfenapyr in combination with one or more organophosphoric acid ester-type compounds and to a method for controlling insecticidal or miticidal pests which have acquired resistance to commercial insecticidal and miticidal agents.

Abstract: Methods are disclosed for correcting biological information transfer in a patient in need of such therapy which comprise administration to a patient of a composition comprising a therapeutically effective amount of a biocomplex comprising at least one bioactive agent from each of the three informational blocks of biological information transfer, each agent being present in an amount sufficient to correct the biological information transfer of the patient under treatment and resulting in the resumption of normal cell metabolism, said amount being less than the buffering amount of said agent; together with a carrier therefor.

Abstract: It has been discovered that certain phosphoinositides demonstrate antibacterial activity. Particularly, these phosphoinositides have been discovered to prevent the adhesion of H. influenzae onto the nasopharyngeal cells of mammals, and, in particular, humans.

Abstract: Inositol derivatives, compositions comprising inositol derivatives, and methods for using compositions comprising inositol derivatives as agents for inhibiting superoxide anion production are described. The inositol derivatives are obtainable via conventional organic synthesis. The inositol derivatives inhibit superoxide anion produced by neutrophils and macrophages which cause tissue damage.

Abstract: A low volatile organic compound co-solvent system is disclosed for preparing emulsion concentrates of low melting organophosphorous insecticides wherein the bioefficacy of the insecticide active is significantly enhanced. The co-solvent system comprises a water-soluble ethoxylated fatty acid/rosin acid-nonionic surfactant composition.

Abstract: Tissue-destructive conditions related to excess protemase activity in a biological system are treated or prevented by administering to the system a composition which combines a tetracycline and a bisphosphonate in synergistic proteinase inhibiting amounts.

Abstract: A composition for modulating immune response in mammals, comprises a therapeutic agent such as a stereoisomer of inositol, derivatives, salts, and mixtures thereof, and optionally a carrier. The composition is provided in solid and liquid formulations, including solutions, suspensions, spreadable and solid forms, as an implant, inhalant, and in vaporizable, injectable, oral and transdermal forms, and the like. The composition of the invention is useful for modulating (enhancing/inhibiting) the immune response. The therapeutic agent of this invention enhances/suppresses B and/or T lymphocyte activity(ies) in normal, aging and immunodeficient mammals, as well as those afflicted with auto-immune disease (s), or subjected to transplants.

Abstract: Membrane-permeant phosphoinositides, including phosphatidylinositol phosphate esters, are described. A membrane-permeant phosphoinositide includes groups that neutralize the charges of the phosphate moieties of the phosphoinositide. A cell can be treated with the membrane-permeant phosphoinositide, which is then absorbed into the cell. The neutralizing groups can be removed intracellularly to afford the charged phosphoinositide.

Abstract: Methods are disclosed for correcting biological information transfer in a patient in need of such therapy which comprise administration to a patient of a composition comprising a therapeutically effective amount of a biocomplex comprising at least one bioactive agent from each of the three informational blocks of biological information transfer, each agent being present in an amount sufficient to correct the biological information transfer of the patient under treatment and resulting in the resumption of normal cell metabolism, said amount being less than the buffering amount of said agent; together with a carrier therefor.

Abstract: The present invention relates to the use of an ester of inositoltrispbosphate for the preparing of a medicament effective against retroviral diseases.

Abstract: Selectin binding and inflammation is modulated by a method which utilizes inositol polyaninon.

Abstract: The invention provides a method for inhibiting protein isoprenylation by administration of a polyisoprenyl pyrophosphate analogue. The polyisoprenyl pyrophosphate analogue may have formula 1, ##STR1## wherein: Pren represents a C.sub.10 -C.sub.30 terpenoid group or a derivative thereof;A.sup.1, A.sup.2, A.sup.3 and A.sup.4 independently represent a direct bond or a C.sub.1 -C.sub.4 alkylene or alkenylene group, optionally having substituents selected from methyl, hydroxy, methoxy, mercapto, methylthio, amino, methylamino, dimethylamino, halogen and a group having formula --X.sup.5 --A.sup.5 --P(.dbd.Z.sup.2)Y.sup.2 Y.sup.3 ; A.sup.5 represents a direct bond or a C.sub.1 -C.sub.4 alkylene or alkenylene group;X.sup.1, X.sup.2, X.sup.3, X.sup.4 and X.sup.5 independently represent a direct bond, oxygen, sulphur, imino or methylimino;Y.sup.1, Y.sup.2 and Y.sup.

Abstract: The invention relates to an inositol phosphate containing pharmaceutical composition which comprises an aliphatic ester or ether for improvement of the bioavailability of the inositol phosphate in mammals including man at non-parenteral administration. The invention also covers the use of at least one aliphatic ester or ether compound for the preparing of an inositol phosphate containing medicament with improved bioavailability of inositol phosphate in mammals including man at non-parenteral administration.

Abstract: The present invention relates to a pharmaceutical composition for the intravenous administration of the sparingly soluble staurosporin derivative N-benzoyl-staurosporin. The composition comprises the following preferred components:a) the therpeutic agent N-benzoyl-staurosporin;b) a polyoxyethylene/polyoxypropylene block copolymer;c) ethanol and water as carrier liquids; andd) purified lecithin from soybeans ande) as water-soluble excipients glycerol and sorbitol.

Abstract: A dermatologic composition is disclosed which comprises a hydrogenated phospholipid having an iodine value of 10 or less and a phosphatidylcholine content of 90% or more, a cholesterol and an oily ingredient.

Abstract: The present invention relates to methods of inhibiting alveolar bone resorption or the undesirable movement of teeth of a human or other animal comprising:a) administering a reservoir to the gingival tissue of the oral cavity such that the reservoir is in contact with the exposed tissue nearest to the alveolar bone to be treated wherein the reservoir is a composition having a pH which maintains an active compound in a negatively charged state and comprises a safe and effective amount of the active compound having the structure: ##STR1## wherein: n is an integer from 0 to 7 (preferably from 0 to 3, more preferably 1); R.sup.1 is hydrogen, chloro, amino, or hydroxy (preferably hydrogen or hydroxy); X is --NH--, quaternary amine, oxygen, sulfur, or a single bond (preferably --NH-- or single bond); R.sup.

Abstract: Compounds are described of general formula (I) ##STR1## and salts and solvates thereof, including physiologically acceptable salts and solvates thereof, in which:Z represents either Het, ##STR2## Het represents an optionally substituted bicyclic or tricyclic ring selected from acricine isoquinolin-1-yl, isoquinolin-3-yl,The novel compounds of formula (I) can sensitize multi-drug resistant cancer cells to chemotherapeutic agents and may be formulated for use in therapy, particularly to improve or increase the efficacy of an anti-tumour drug.

Abstract: Disclosed are oral compositions such as toothpastes, mouthrinses, liquid dentifrices, lozenges and gums containing at least one phosphate derivative and a copper source.

Abstract: A methane diphosphonic acid derivative represented by the general formula (I): ##STR1## wherein, X and Y are defined in the specification; m represents an integer of 0 to 3; n represents an integer of 0 to 4; and each X of the (X).sub.m and each Y of the (Y).sub.n may be either identical or different; . . . represents a double bond or single bond; A is --(CH.sub.2)a--(D)b--(CH.sub.2)c-- (wherein D is sulfur, oxygen, NH, alkyl-substituted N, or CH.sub.2, a and c are integers of 0 to 10 and b is 0 or 1), or --(CH.dbd.CH)d.dbd.CH= (wherein d is an integer of 0 to 2, and B does not exist when A represents --CH.dbd.CH)d--CH.dbd.), B refers to a hydrogen atom, alkyl group, amino group, monoalkylamino group, dialkylamino group, acylamino group, hydroxyl group, alkoxy group, trialkylsiloxy group or acyloxy group, and each of R.sup.1, R.sup.2, R.sup.3 and R.sup.

Abstract: Bisphosphonate, particularly alendronate, can prevent or treat bone loss associated with immunosuppressive therapy, whether or not the immunosuppressive therapy is associated with an organ transplant.

Abstract: The invention is directed to controlling and alleviating itchiness of human skin. Itchiness is treated with a composition that includes inositol phosphate, particularly phytic acid and its salts, in a cosmetically acceptable carrier.

Abstract: The invention relates to an inositol phosphate containing pharmaceutical composition which comprises a nitrogen-containing compound for improvement of the bioavailability of the inositol phosphate in mammals including man at non-parenteral administration. The invention also covers the use of at least one nitrogen-containing compound for the preparing of an inositol phosphate containing medicament with improved bioavailibility of inositol phosphate in mammals including man at non-parenteral administration.

Abstract: A method of preventing or alleviating retroviral disease by administering to a human or a mammal in need thereof a pharmaceutical composition comprising an amount of at least one specific isomer of inositol triphosphate sufficient to obtain said prevention or alleviation.

Abstract: A bisphosphonic acid derivative of the general formula (I): ##STR1## wherein A is an optionally substituted cyclic group; R.sup.1 is hydrogen atom or a lower alkanoyl group; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and are hydrogen atom or a lower alkyl group; m is 0, 1 or 2; and n is an integer from 2 to 10, or a salt thereof is disclosed. A process for its production and a bone resorption inhibitor containing the compound of the general formula (I) or a salt thereof are also disclosed.

Abstract: A non-radioactive, spectrophotometric, microtiter plate assay for human cystolic phospholipase A.sub.2 (cPLA.sub.2) is described. The assay utilizes a novel synthetic thiol-phospholipid analog as a substrate. In one embodiment, the substrate is a phosphatidylcholine derivative with an arachidonoylthioester in the sn-2 position and an alkenyl-ether or alkenyl-ether in the sn-1 position. The alkyl-ether and the alkenyl-ether in the sn-1 position of the substrate ensures that the assay will only measure cPLA.sub.2 activity and will not be complicated by metabolism of the lysophospholipid product by the enzyme's and lysophospholypase activity.

Abstract: Modified ceramides are defined, together with their synthesis and compositions comprising them for topical application to human skin, hair and nails. The modified pseudoceramides have a structure: ##STR1## and an approximate summary is that R and R.sup.1 are aliphatic hydrocarbon, A is CH.sub.2, CHOR.sup.2, CH.dbd.CH or CHOY, and at least one of R.sup.2, R.sup.3 and R.sup.4 is sulphate, phosphate or similar. The presence of phosphate or sulphate facilitates skin absorption, after which the phosphate or sulphate is removed by enzymes present in vivo.

Abstract: Substituted derivatives of deoxymyoinositol of general formula (I): ##STR1## in which R.sup.1, R.sup.2 and R.sup.5 are identical or different and represent a linear or branched alkyl group of 3 to 14 carbon atoms.R.sup.3 and R.sup.4 are identical or different and represent a hydrogen atom, a protecting group of the hydroxyl groups or the residue of formula --CO--(CH.sub.2).sub.n --CH.sub.3in whichn represents the number 12, 13, 14, 15, 16 or 17, and their salts, process for preparing them and their use in medicaments.