Abstract: The present invention concerns therapeutic agents that modulate the activity of PTH and PTHrP.

Abstract: The invention provides composition comprising, 1) polyprenol monophosphates of the formula H—[—CH2-C(CH3)═CH—CH2]n-O—P(═O)(OH)2 wherein n is an integer from 6-19 inclusive or a salt thereof, and 2) polyprenol pyrophosphates of the formula H—[—CH2-C(CH3)═CH—CH2]m—O—P(═O)(OH)—O—P(═O)(OH)2 wherein m is an integer from 6-19 inclusive or a salt thereof, which is useful as an antiviral agent, as an immunomodulatory agent, and for treating cancer. The invention also provides pharmaceutical compositions comprising the compositions of the invention as well as therapeutic methods for using the the compositions.

Abstract: The present invention relates to derivatives of 1-hydroxymethylene-1,1-bisphosphonic acid, the pharmaceutical compositions comprising them, and their application in therapeutics, particularly for the treatment of cancerous tumors. It is also directed to a methods of preparation of such derivatives.

Abstract: The invention relates to a process for treating lameness with an osseous, articular or osteoarticular component, comprising the administration, to a human or to an animal not suffering from arthritis or from fractures, of an effective amount of a bisphosphonic acid derivative of formula: 1

Abstract: Disclosed are methods for inhibiting bone resorption in mammals while minimizing the occurrence of or potential for adverse gastrointestinal effects. Also disclosed are pharmaceutical compositions and kits for carrying out the therapeutic methods disclosed herein.

Abstract: Pharmaceutical compositions of bisphosphonic acids, and salts thereof, are prepared by wet granulation tablet formulation. These pharmaceutical compositions are useful in the treatment of disturbances involving calcium or phosphate metabolism, in particular, the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, malignant hypercalcemia, and metastatic bone disease. These compositions are prepared without the addition of binder; instead, the drug itself acts as a binder.

Abstract: The present invention relates to compounds according to formula (I) as disclosed herein as well as pharmaceutical compositions which include those compounds. Also disclosed are methods of using such compounds, which have activity as agonists or as antagonists of LPA receptors; such methods including inhibiting LPA activity on an LPA receptor, modulating LPA receptor activity, treating cancer, enhancing cell proliferation, and treating a wound.

Abstract: Compounds able to chelate bi- and trivalent paramagnetic metal ions, their chelated complexes with these metal ions and physiologically compatible salts thereof and therein magnetic resonance imaging.

Abstract: A method of inhibiting the activity or production of cytokines or growth factors associated with vascular restenosis, by administering to an individual an effective amount of an active ingredient comprising a bisphosphonate particle or a bisphosphonate particulate. The bisphosphonate may be encapsulated, embedded or adsorbed within the particle, dispersed uniformly in the polymer matrix, adsorbed on the particle surface, or in combination of any of these forms. The particles include liposomes or inert polymeric particles, such as microcapsules, nanocapsules, nanoparticles, nanospheres, or microparticles. The particulates include any suspended or dispersed form of the bisphosphonate which is not encapsulated, entrapped, or adsorbed within a polymeric particle. The particulates include suspended or dispersed colloids, aggregates, flocculates, insoluble salts and insoluble complexes of the active ingredient.

Abstract: Compounds of the formula: are provided, and are useful as cysteine protease inhibitors, particularly in the treatment of diseases such as osteoporosis or autoimmune disorders in which cathepsins K or S contribute to the pathology or symptomatolgy of the disease.

Abstract: The present invention relates to a method for the sustained release in vivo of a biologically active agent comprising administering to a subject in need of treatment an effective amount of a sustained release composition comprising a biocompatible polymer having the biologically active agent incorporated therein, and a bisphosphonate wherein the bisphosphonate compound is present in an amount sufficient to modify the release profile of the biologically active agent from the sustained release composition. Pharmaceutical compositions suitable for use in the method of the invention are also disclosed.

Abstract: A method for inhibiting cell adhesion mediated drug resistance wherein an effective amount of a bisphosphonate compound or a pharmaceutically acceptable bisphosphonate salt is administered to a patient having cancer, whereby the efficacy of chemotherapy or radiotherapy directed against the cancer is enhanced. Preferably, the bisphosphonate compound is etidronate, clodronate, pamidronate, or zoledronate. The bisphosphonate compound is preferably administered to the patient prior to the administration of chemotherapy or radiation therapy. Inhibition of cell adhesion mediated drug resistance (CAM-DR) by bisphosphonate in multiple myeloma cells is disclosed.

Abstract: An effervescent formulation of alendronate contains an acid source, a carbonate source, a binder, a lubricant and optionally, flavoring agents, colorants and sweeteners.

Abstract: Novel methods for reduction or elimination the incidence of hot flashes and menopausal symptoms, while decreasing the risk of acquiring breast or endometrial cancer and furthermore treating and/or inhibiting the development of osteoporosis, hypercholesterolemia, hyperlipidemia, atherosclerosis, hypertension, insulin resistance, diabetes, loss of muscle mass, obesity, irregular menstruation, Alzheimer's disease, or vaginal dryness in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator, particularly compounds having the general structure: 1

Abstract: A method of treating or preventing restenosis by administering to an individual an effective amount of an active ingredient comprising a bisphosphonate particle or a bisphosphonate particulate. The bisphosphonate may be encapsulated, embedded or adsorbed within the particle, dispersed uniformly in the polymer matrix, adsorbed on the particle surface, or in combination of any of these forms. The particles include liposomes or inert polymeric particles, such as microcapsules, nanocapsules, nanoparticles, nanospheres, or microparticles. The particulates include any suspended or dispersed form of the bisphosphonate which is not encapsulated, entrapped, or adsorbed within a polymeric particle. The particulates include suspended or dispersed colloids, aggregates, flocculates, insoluble salts and insoluble complexes of the active ingredient.

Abstract: A novel process for producing extended release formulation of a water-soluble drug comprising the steps of making a “modified drug” comprising a hot-melt granulation of the drug with soluble or dispersible polymeric material of a suitable molecular weight and melting point, coating portions of the modified drug to different thicknesses or weights so as to produce subbatches, and blending the subbatches to achieve a specific drug release profile.

Abstract: The present invention comprises compounds, compositions thereof, and methods capable of delivering inositol hexaphospahte (IHP) to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering IHP to the cytoplasm of the red blood cells.

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

Abstract: The present invention provides compacted pharmaceutical composition for oral administration to a patient which expands upon contact with gastric fluid to retain a dosage form in the patient's stomach for an extended period of time, the formulation comprising a non-hydrated hydrogel, a superdisintegrant and tannic acid. The present invention further provides a pharmaceutical dosage form containing an active ingredient, and the compacted pharmaceutical composition. The invention further provides a dosage form suitable for delivering a therapeutic bis-phosphonate such as alendronate to the stomach of a patient over and extended period.

Abstract: The present invention discloses highly packed polycationic ammonium, sulfonium and phosphonium lipid compounds useful for making lipid aggregates for delivery of macromolecules and other compounds into cells. They are especially useful for the DNA-dependent transformation of cells. Methods for their preparation and use as intracellular delivery agents are also disclosed.

Abstract: Oral dosage forms are provided for the administration of a bisphosphonic acid compound in the prevention and treatment of conditions involving calcium or phosphate metabolism, i.e., conditions associated with bone resorption such as osteoporosis, Paget's disease, periprosthetic bone loss, osteolysis, malignant hypercalcemia, metastatic bone disease, multiple myeloma, and periodontal disease. The dosage forms are either enterically coated capsules housing the drug in a liquid or semi-solid carrier, or enterically coated osmotically activated drug delivery devices.

Abstract: The present invention comprises compounds, compositions thereof, and methods capable of delivering a broad range of anionic molecules to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering a ligand for the allosteric site of hemoglobin to the cytoplasm of the red blood cells.

Abstract: A method for the treatment of angiogenesis in a patient in need of such treatment, e.g. a tumor patient or a patient suffering from an inflammatory disease, which comprises administering, preferably via an intra-arterial route, an effective amount of a bisphosphonate, e.g. pamidronic acid or zoledronic acid or salts or hydrates thereof, to the patient.

Abstract: The invention provides a liquid pharmaceutical composition and methods for use in the treating of bone diseases, the composition being an aqueous solution comprising 0.05% to 35% by weight of ibandronaic acid or salts thereof; 0.1% to 5% by weight of a pH regulating agent; 1% to 15% by weight of a co-solvent; 0.005% to 0.5% by weight of a conserving agent; 1% to 90% by weight of a deionized water; and excipients and pharmaceutically acceptable stabilizers, wherein the composition has a pH of about 2 to 7. The composition is formulated for sublingual administration and enteric administration.

Abstract: The present invention is directed to particular bisphosphonate compounds, and in particular, to bisphosphonate conjugates that are useful in the treatment of soft tissues surrounding bone and bone-related diseases, such as bone cancer and osteoporosis.

Abstract: Pharmaceutical compositions of bisphosphonic acids, and salts thereof, are prepared by wet granulation tablet formulation. These pharmaceutical compositions are useful in the treatment of disturbances involving calcium or phosphate metabolism, in particular, the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, malignant hypercalcemia, and metastatic bone disease. These compositions are prepared without the addition of binder; instead, the drug itself acts as a binder.

Abstract: Stable tablets comprising fosinopril sodium are prepared by employing either stearic acid or zinc stearate as the lubricant.

Abstract: Methods of treating a fungal or yeast infection and of killing or inhibiting fungi or yeast are disclosed. The methods use derivatives of triterpenes that are abundant in birch bark and other plants. The triterpenes include betulin, allobetulin, and lupeol.

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: Bisphosphonates inhibit bone resorption associated with periodonatal or orthopedic surgery when applied topically to the bone. A novel formulation for topical application contains a gelatin matrix which is soaked in a solution containing a bone absorption inhibiting effective amount of a bisphosphonate or a pharmaceutically acceptable salt.

Abstract: The present invention is a method and composition to increase bone strength in a manner that decreases fracture incidence, which may or may not include increasing bone mineral density (“BMD”). The invention includes administering an effective amount of a bisphosphonate to a host in need thereof to increase bone strength, which inhibits the apoptosis of osteoblasts and osteocytes, without a significant effect on osteoclasts. In one embodiment, the bisphosphonate is not 1-amino-3-(N,N-dimethylamino)-propyliden-1,1-bisphosphonic acid or its pharmaceutically acceptable salt. An increase in osteoblast life span can lead to an increase in bone mass, i.e., an anabolic effect. Preservation of osteocyte life span can increase bone strength, which may be disproportional to the increase in bone mass.

Abstract: The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds, which comprise a phosphocholine moiety covalently conjugated with one or more therapeutic agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt or a prodrug thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus.

Abstract: The present invention relates to oral compositions and methods for inhibiting bone resoprtion in a mammal while counteracting the occurrence of potentially adverse gastrointestinal effects. The compositions useful herein comprise the combination of a pharmaceutically effective amount of a nitrogen-containing bisphosphonate or a pharmaceutically-acceptable salt thereof and a pharmaceutically effective amount of an isoprenoid compound.

Abstract: Disclosed are methods for inhibiting bone resorption in mammals while minimizing the occurrence of or potential for adverse gastrointestinal effects. Also disclosed are pharmaceutical compositions and kits for carrying out the therapeutic methods disclosed herein.

Abstract: A pharmaceutical composition is provided for treatment of malignancies which comprises in combination a bisphosphonate and a matrix metalloproteinase inhibitor for simultaneous, sequential or separate use, provided that the bisphosphonate is not ibandronate when the MMP inhibitor is TIMP-2, e.g. for inhibiting the development of soft tissue metastases during the treatment of a malignant disease with a bisphosphonate wherein treatment with the bisphosphonate gives rise to increased MMP secretion.

Abstract: The invention provides compositions for topical use, comprising at least one glycoglyceride and at least one sequestering agent. The glycoglyceride has very good stability in the composition of the invention. The glycoglyceride is preferably a galactolipid such as digalactosyl diglyceride or monogalactosyl diglyceride. The sequestering agent may be chosen in particular from phosphonic derivatives and salts thereof. This composition may in particular constitute a cosmetic and/or dermatological composition.

Abstract: A stable injectable solution containing pamidronate and a method for preparing a therapeutic aqueous disodium pamidronate solution. The method comprises preparing a slurry of pamidronic acid in water, combining aqueous sodium hydroxide with the slurry in an amount about 2:1 molar ratio of sodium hydroxide to pamidronic acid to yield a solution of disodium pamidronate having visual clarity and a pH of about 6.5, and packaging the solution in sealed containers. A unit dosage form including the solution and a vial or ampule comprising the unit dosage form are also described.

Abstract: Pharmaceutical compositions of bisphosphonic acids, and salts thereof, are prepared by direct compression/dry mix tablet formulation. These pharmaceutical compositions are useful in the treatment of disturbances involving calcium or phosphate metabolism, in particular, the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, malignant hypercalcemia, and metastatic bone disease.

Abstract: The present invention relates to novel cysteine protease inhibitors of Formula I: 1

Abstract: The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme.

Abstract: The present invention relates to methods for prevention and treatment of bone-related or nutrition-related disorders using a GLP molecule or GLP activator either alone or in combination with another therapeutic. The present invention also encompasses methods of diagnosing or monitoring the progression of a disorder. The invention also encompasses methods of monitoring the effectiveness of treatment of the invention.

Abstract: Antiviral compounds and the water-soluble salts thereof have formula (I), wherein n is from 1 to 8; R1 is selected from the group consisting of (a), wherein m is zero, 1, 2 or 3; and (b), wherein q is from 1 to 20; R2 is independently selected from the group consisting of oxygen and sulfur; R3 is independently selected from the group consisting of hydrogen and hydroxyl; and R4 is selected from the group consisting of hydrogen, hydroxyl and (b); R5 is selected from the group consisting of hydroxyl and (b); R6 is selected from the group consisting of (c), (d) et (e), wherein x is from 1 to 20; provided that one of R1, R4 and R5 is (b) wherein R6 is defined as above; or water soluble salt thereof.

Abstract: The present invention relates to the use of D-chiro-inositol (DCI) as a regulator of hypothalamic gene expression and, more particularly, to the use of DCI and derivatives and metabolites thereof to treat neuroendocrine impairments such as obesity, polycystic ovarian syndrome (PCOS), impaired regulation of hormones during aging and to correct such neuroendocrine impairments and associated functions.

Abstract: Methods and compositions 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: This invention comprises methods of treating bone disorders and lowering blood LDL levels comprising administration of a bisphosphonate, an estrogen and compound of the formulae I or II: 1

Abstract: Compositions and methods for treating osteoporosis using the compositions are disclosed where the compositions have reduced GI toxicity and improved bio-availability and include a bisphosphonate and zwitterionic phospholipid.

Abstract: This invention comprises methods of treating bone disorders comprising administration of a bisphosphonate and compound of the formulae I or II: 1

Abstract: The present invention provides compacted pharmaceutical composition for oral administration to a patient which expands upon contact with gastric fluid to retain a dosage form in the patient's stomach for an extended period of time, the formulation comprising a non-hydrated hydrogel, a superdisintegrant and tannic acid. The present invention further provides a pharmaceutical dosage form containing an active ingredient, and the compacted pharmaceutical composition.

Abstract: The invention relates to a solid pharmaceutical form of administration containing a diphosphonic acid or a physiologically compatible salt thereof as the active substance, wherein the active substance is present in granulate form, optionally together with pharmaceutical adjuvants in the inner phase, and the outer phase contains a lubricant in the form of less than 5% by weight of stearic acid relative to the total weight of the form of administration.

Abstract: The present invention relates to methods for stimulating bone formation in a mammal comprising administering to a mammal in need thereof a therapeutically effective amount of an EP4 receptor subtype agonist.