Abstract: Described herein is the synthesis and pharmacology of a series of ?-substituted methylene phosphonate analogs, in which the ?-CH2 moiety is replaced with CHCl or CHBr.

Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

Abstract: A composition for preventing, mitigating, and alleviating irritation and skin trauma is described. The composition contains calcium glycerophosphate and at least one skin compatible, film-forming component. The composition may be applied to the skin prior to application of an adhesive tape to reduce damage to the skin which is inflicted upon removal of the tape by forming a film on the skin. Upon removal of the adhesive tape from the skin, the film, rather than skin cells, is removed with the tape. The calcium glycerophosphate component of the composition also penetrates the skin and serves to alleviate any damage which may be inflicted on the skin. The composition may also be applied to the skin to prevent subsequent irritation, such as irritation inflicted by contact with poison ivy, clothing, jewelry, insect bites, a prosthetic, etc. A medical dressing which contains the composition is also included.

Abstract: A biodelivery system has been found which increases the efficiency and effectiveness of introducing antimicrobial compounds into complex biofilm matrices through the use of liposome carriers, thereby removing the biofouling in industrial water bearing systems, including piping, heat exchanges, condensers, filtration systems and fluid storage tanks. According to one embodiment of the invention, antimicrobial containing liposomes are added to water systems prone to biofouling and biofilm formation. The liposomes, being similar in composition to microbial membranes or cells, are readily incorporated into the existing biofilm. Once the antimicrobial compound containing liposomes become entrained within the biofilm matrix, the decomposition or disintegration of the liposome proceeds. Thereafter the biocidal core is released to react directly with the biofilm encased microorganisms.

Abstract: The present invention relates to a solid pharmaceutical composition comprising memantine, which dissolves or disintegrates in the oral cavity preferably within about 60 seconds. The present invention further discloses orally disintegrating tablets of taste-masked memantine of optimal mechanical strength comprising memantine along with a taste-masking agent and pharmaceutically acceptable excipients.

Abstract: Glycerophosphate salts have been found to drastically improve the treatment of urogenital disorders such as urethral strictures and vaginal atrophy. Methods, devices and kits are described for treating urogenital disorders using a composition comprising an effective amount of a glycerophosphate salt.

Abstract: A composition and method of treating Alzheimer's disease or a dementia of vascular origin are disclosed. The composition and method utilize an endothelin antagonist as the active agent to treat Alzheimer's disease or a dementia of vascular origin in mammals, including humans.

Abstract: The present invention relates to new substituted hydroxyphenylamine based modulators of hormone and/or pigment levels, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: A composition and method of treating Alzheimer's disease or a dementia of vascular origin are disclosed. The composition and method utilize an endothelin antagonist as the active agent to treat Alzheimer's disease or a dementia of vascular origin in mammals, including humans.

Abstract: Calcium glycerophosphate is found to be effective in treating and preventing a disease, disorder and/or condition of the respiratory system. The disease, disorder and/or condition is related to an obstructive or a restrictive condition of the respiratory airway.

Abstract: The invention relates to 5-HT6 receptor modulators. Compositions comprising arylamine compounds and acetylcholinesterase inhibitors and use of these compositions are disclosed. Such uses include e.g., the treatment, modulation and/or prevention of Alzheimer's disease and memory disorders, and psychological disorders such as schizophrenia, are disclosed.

Abstract: Compounds and related methods for synthesis, and the use of compounds and combination therapies for the treatment of cancer and modulation of apoptosis in cells are disclosed. Particularly disclosed are phosphonate esters. Compounds, methods of making the compounds, medicaments and method of manufacture of medicaments and therapeutic methods with applications against cancer including breast cancer, melanoma, colon cancer, leukemia and lymphoma, and other cancer cells are described.

Abstract: Pathogenic effector proteins which include one or more RxLR, dEER, Pexel or analogous motifs are blocked from entry into plant or animal cells by binding one or more of the motifs with a blocking compound which prevents binding of phosphoinositides or other polar lipids to the motifs which is a prerequisite for translocation of the pathogenic effector proteins into the plant or animal cell. The blocking compounds can take a variety of forms including synthetic peptides or the hydrophilic head-groups of phosphoinositides, phosphatidic acids, phospholipids, or sphingolipids. Suitable blocking compounds can be identified by assays demonstrating binding to RxLR, dEER, Pexel or analogous motifs. In addition, pathogenic effector proteins can be identified by analyzing whether they contain structural RxLR motifs using hidden markov modeling.

Abstract: The present invention relates to synthetic lung surfactant compositions that contain one or more of phospholipase-resistant phospho-glycerol derivatives, phospholipase-resistant phospho-choline derivatives, and surface active proteins or peptides, more preferably a combination of at least two or all three of these materials. Novel phospholipase-resistant phospho-glycerol derivatives, phospholipase-resistant phospho-choline derivatives, and surface active peptides are also disclosed herein. Uses of the surfactant compositions of the present invention to treat endogenous surfactant dysfunctional or deficient lung tissue, to prepare synthetic peptides for use in the surfactant compositions, and to deliver therapeutic agents are also disclosed.

Abstract: The invention relates to a stent having a coating or cavity filling comprising or containing an organic Au complex.

Abstract: Glycerophosphate salts have been found to mitigate the syndromes or conditions of discomfort associated with inflammation. Therefore, methods are provided for treating or preventing an inflammatory condition using a glycerophosphate salt. In particular, methods are provided for treating or preventing an inflammatory condition using calcium glycerophosphate (CGP).

Abstract: The invention provides compounds comprising at least one phosphohalohydrin group of the formula: where X is a halogen selected from among I, Br, Cl, R1 is selected from among —CH3 and —CH2—CH3, Cat+ is an organic or inorganic cation, and n is an integer between 2 and 20, processes for the production thereof and uses thereof, in particular therapeutic uses and for activating primate T?9?2 lymphocytes.

Abstract: One aspect of the present invention relates to methods of treating corneal edema comprising contacting a cornea with an ophthalmic irrigating composition comprising histidine. In certain embodiments, the ophthalmic irrigating compositions contact the corneal endothelium. Another aspect of the present invention relates to ophthalmic irrigating compositions for treating corneal edema comprising histidine and optionally, calcium glycerophosphate and/or glutathione disulfide.

Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) in order to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, as well as in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. The antiviral activity of enzyme inhibitors is demonstrated.

Abstract: Methods of using compatible solutes cyclic 2,3-diphosphoglycerate (cDPG), 1,-di-glyccrol phosphate (DGP), firoin and firoin-A, and/or derivatives of these compounds or combinations thereof, for treating skin conditions such as dermatoses and age spots. The methods include the application to the skin of a cosmetic and/or dermatological preparation containing the compatible solutes.

Abstract: The compounds of formula (I): where Ar is an aromatic ring and Ra, Rb, are as defined in the description, are useful in therapy as drugs for the treatment of diseases mediated by infiltrations of neutrophils induced by IL-8, such as psoriasis, rheumatoid arthritis, ulcerative cholitis and for the treatment of damages caused by ischemia and reperfusion.

Abstract: A skin treatment composition is provided which contains calcium glycerophosphate and a fatty acid source derived from an animal or a vegetable. The composition enhances skin cell proliferation and growth and repair of damage to skin cells. Methods for enhancing skin cell repair, proliferation, and growth and for enhancing ceramide synthesis involve topically applying to the skin a composition containing calcium glycerophosphate and a fatty acid source derived from an animal or a vegetable.

Abstract: There is provided a dietary or health supplement comprising an effective amount of a micronutrient selected from the group consisting of phosphate derivatives of tocopherol, ubiquinol, ascorbic acid, tocotrienol, retinol and mixtures thereof delivered with an acceptable carrier.

Abstract: A synergistic composition comprising a THP salt and a biopenetrant, in which the biopenetrant comprises a polymer of an unsaturated carboxylic acid or a copolymer of an unsaturated carboxylic acid with a sulphonic acid, said polymer or copolymer being terminated by a mono- or diphosphonated unsaturated carboxylic acid group or having such monomers incorporated into the polymer backbone. This composition acts synergistically to enhance the biocidal efficacy of the THP salt against both planktonic (free-swimming) and sessile (attached) bacteria, and also acts synergistically to enhance the efficacy of the THP salt in the dissolution of iron sulphide scale.

Abstract: A method of treating otosclerosis in a human in need thereof by administering a bisphosphonate in a defined dosing schedule. The invention demonstrates an effective response and sustained benefit in the treatment of otosclerosis. Particularly, the method involves administration of a bisphosphonate in a stepped-up dosage amount, e.g., in a dose that is at least one and a half times the recommended dose for osteoporosis. It also includes administration of a time-dependent dose of more than one bisphosphonate, specifically, alternating administration of a first bisphosphonate with a second bisphosphonate. The inventive method further includes intravenous administration of a bisphosphonate, and optionally oral administration of a bisphosphonate.

Abstract: The present invention relates to a method of preventing or alleviating the problems associated with corrosion and to novel formulations for use in such a method.

Abstract: A liposome formulation for stably incorporating high content of hydrophobic substance is disclosed. The liposome includes two phospholipids with different phase transition temperatures such as saturated and unsaturated phosphatidyl cholines, hydrophobic substances, cholesterol, cholesterol derivatives, antioxidant and hydrophilic polymer-modified lipids such as MPEG-DSPE.

Abstract: The invention relates to the use of a Dipeptidyl peptidase IV inhibitor (DPP-IV inhibitor) or a pharmaceutically acceptable salt thereof for the prevention, delay of progression or the treatment of neurodegenerative disorders, cognitive disorders and for improving memory (both short term and long term) and learning ability.

Abstract: The invention provides a protein in a form that is functional for the enzymatic conversion of 2C-methyl-D-erythritol 2,4-cyclodiphosphate to 1-hydroxy-2-methyl-2-butenyl 4-diphosphate notably in its (E)-form of the non-mevalonate biosynthetic pathway to isoprenoids. The invention also provides a protein in a form that is functional for the enzymatic conversion of 1-hydroxy-2-methyl-2-butenyl 4-diphosphate, notably in its (E)-form, to isopentenyl diphosphate and/or dimethylallyl diphosphate. Further, screening methods for inhibitors of these proteins are provided. Further, 1-hydroxy-2-methyl-2-butenyl 4-diphosphate is provided and chemical and enzymatic methods of its preparation.

Abstract: The invention provides a pharmaceutical composition comprising a synthetic or naturally occurring charged phospholipid, which is formulated into a dosage form for administration to a subject or which is administered as a food additive. Negatively charged phospholipid composition increase the net negative charge on intravascular lipoproteins, enhance the clearance of cholesterol and regulate the function of lipolytic enzymes, retard prothrombin formation and aid in the clearance of virus and bacterial particles. Negatively charged lipid compositions can therefore be administered to humans and animals for the treatment of hyperlipidemia and blood coagulation disorders and to reduce the levels of virus, bacteria, and endotoxins in the blood stream. Positively charged lipid compositions can be administered to delay lipoprotein clearance from the plasma compartment and give longer duration of activity for drugs which are associated with lipoproteins.

Abstract: The invention provides compounds comprising at least one phosphoepoxide group of the formula: where R1 is selected from among —CH3 and —CH2—CH3. Cat+ is an organic or inorganic cation, n is an integer between 2 and 20, processes for the production thereof and uses thereof, in particular therapeutic uses and for activating primate T?9?2 lymphocytes.

Abstract: The present invention relates to prevention of congenital deformations The invention further relates to cancer inhibition and prevention. The invention further relates to methods and compositions to modulate, antagonize, or agonize disparate signaling pathways that may converge to regulate patterning events gene expression during prenatal development, post-natal development and during development in the adult organism.

Abstract: Disclosed are inhibitors of the serine/threonine kinase Akt, pharmaceutical compositions comprising such inhibitors, and a method of preventing or treating a disease or condition in an animal by the use of such inhibitors.

Abstract: The present invention relates to a phosphorylated glyceryl ether aluminum salt represented by the general formula (1): (wherein R1 represents an alkyl or an alkenyl group with 8 to 32 carbon atoms; R2 represents a hydrogen atom, a phosphoric acid residue or —CH2CH(OR2)CH2OR1 (wherein R1 and R2 are the same as described above, provided that a repeated binding number is 4 at the most when R2 is —CH2CH(OR2)CH2OR1); X1 represents a hydrogen atom or a phosphoric acid residue, and at least one of X1 and R2 is a phosphoric acid residue; Y represents an alkali metal atom or an alkaline earth metal atom; m represents a number from 0.3 to 1, and n represents a number from 0 to 1), and an external dermatological agent containing the same. The compound has benefits such as an excellent pore contracting activity and also a good solubility in oil.

Abstract: A skin treatment composition is provided which contains calcium glycerophosphate and a fatty acid source derived from an animal or a vegetable. The composition enhances skin cell proliferation and growth and repair of damage to skin cells. Methods for enhancing skin cell repair, proliferation, and growth and for enhancing ceramide synthesis involve topically applying to the skin a composition containing calcium glycerophosphate and a fatty acid source derived from an animal or a vegetable.

Abstract: Base compositions (premix) comprising the following components: A) a perfluoropolyether phosphate; B) a solvent; C) water.

Abstract: The present invention relates to the preparation and biological activity of 3-deoxy-Dmyo-inositol ether lipid analogs as inhibitors of phosphatidylinositol-3-kinase signaling and cancer cell growth. The compounds of the present invention are useful as anti-tumor 5 agents which effectively inhibit the growth of mammalian cells.

Abstract: The invention provides compounds comprising at least one phosphohalohydrin group of the formula: where X is a halogen selected from among I, Br, Cl, R1 is selected from among —CH3 and —CH2—CH3, Cat+ is an organic or inorganic cation, and n is an integer between 2 and 20, processes for the production thereof and uses thereof, in particular therapeutic uses and for activating primate T?9?2 lymphocytes.

Abstract: Acidic oral compositions having reduced tooth erosion characteristics, especially acid beverages such as fruit juice drink concentrates, or oral healthcare products such as mouthwashes, are prepared by adding a calcium compound to the acid composition so that the mol ratio of calcium to acid ranges from 0.3 to 0.8, and the pH of the composition, if necessary after adjustment with an alkali, is from 3.5 to 4.5.

Abstract: The present invention relates to novel estrogenic compounds. The present invention also relates to methods of treating estrogen deprivation in a subject comprising administering novel estrogenic compounds. Additionally, the present invention relates to methods of synthesizing novel estrogenic compounds.

Abstract: The invention relates to novel active compound combinations of certain cyclic ketoenols and certain active compounds that together have unexpectedly good insecticidal and acaricidal properties.

Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

Abstract: A method for treating symptoms, diseases and conditions in extra-reproductive tract tissues that are responsive to treatment with estrogen, using triarylethanes of formula (I) wherein R1 is —O(CH2)mR3 or —(CH2)nR3; wherein R3 is an anionic substituent; m is an integer from 1 to 4; and n is an integer from 0 to 4; and wherein R2 is either H or —OH. Each of R1 and R2 can be either meta or para to its respective phenyl ethyl linkage. Compounds having the formula (I) wherein R1 is —O(CH2)mR3 or —(CH2)nR3; R3 is an anionic substituent; m is 1, 2, 3 or 4; n is 0, 1, 2, 3 or 4; R2 is H or —OH; and wherein each of R1 and R2 is independently meta or para to its respective phenyl ethyl linkage are also provided, with the proviso that R2 is not para —OH when m is 1 and R3 is —COOH.

Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound which is a EP4 agonist.

Abstract: The invention provides compounds of formula I: wherein X, R1, R2, and n have any of the values defined in the specification, and their pharmaceutically acceptable salts. The compounds are useful, for example, for blocking prenylation transferase enzymes, for probing or diagnosing protein prenylation processes, and for treating cancer in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and intermediates useful for the synthesis of compounds of formula I.

Abstract: A diverse set of tubulin binding agents have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, phosphoramidates, and other prodrugs capable of demonstrating selective targeting and destruction of tumor cell vasculature.

Abstract: Base compositions (premix) comprising the following components: A) a perfluoropolyether phosphate; B) a solvent; C) water.

Abstract: Cosmetic or pharmaceutical compositions comprising compounds of formula (I) and the corresponding salts thereof: 1

Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.

Abstract: Geriatric depression is treated with L-carnitine or an alkanoyl L-carnitine, desirably acetyl L-carnitine thereby avoiding unwanted side-effects exhibited by conventional antidepressant agents.