Abstract: A drug and method of bone grafting which improves the osteoinductive and/or osteoconductive potential of a bone graft, bone graft substitute or extenders. The drug is selected from the group consisting of bisphosphonates which may be administered to a subject either prior to, during or after a bone grafting procedure.

Abstract: A method for the treatment of prostate cancers and other cancers having associated osteoblastic (osteosclerotic) metastases in a patient in need of such treatment comprising administering an effective amount of an N-bisphosphonate, especially zoledronic acid or a salt or any hydrate thereof, to the patient.

Abstract: A method for increasing bone mineral density, that includes the substantially daily consumption of at least one cup of tea for a period of years. Preferably, such consumption continues for at least about six years. Where utilized as a treatment for osteoporosis rather than as a preventative measure, it is preferred that the tea consumption be accompanied by treatment with osteoporosis-treating pharmaceutical agents, such as anti-resorptives or bone forming agents. The method should include measurements of bone mineral density, preferably occurring on a periodic basis.

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: The present invention relates to an improved injectable ready-to-use preparation of pamidronate salts, methods for its manufacture and uses of the solution of the invention in the manufacture of pharmaceutical compositions for the treatment of diseases selected from the group of tumour-induced hypercalcaemia, Paget's disease, osteoporosis, bone metastases, or breast cancer. The ready-to-use solution comprises a physiologically acceptable alkaline salt of pamidronate which is water soluble and a physiologically acceptable aqueous solvent having a concentration of between 0.1 and 100 mg/mL, wherein the solution is provided in a sealed non-reactive plastic container.

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: Inositol derivatives, compositions comprising inositol derivatives, and methods for using compositions comprising inositol derivatives as agents for activating the secretion of chloride ions and/or treatment of inflammation are described.

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 is generally directed to pharmaceutical compositions and process for the preparation of same which are suitable for oral administration to a human patient, comprising: a pharmaceutically-acceptable salt of 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid; a non-reducing sugar diluent; a binder; a disintegrant; and a lubricant, and various other excipients.

Abstract: The present invention is a method for the treatment or prevention of preferably non-insulin dependent (NIDDM or so-called Type II) diabetes mellitus, or other conditions associated with impaired glucose tolerance such as obesity, and in particular to the use of phytanic acid derivatives for the said treatment and/or prevention. A method of making a composition for the treatment or prevention of non-insulin dependent diabetes mellitus and related diseases comprising combining phytanic acid or derivatives thereof with a pharmaceutically acceptable additive or adjuvant, and a composition for the treatment or prevention of non-insulin dependent diabetes mellitus comprising phytanic acid or derivatives thereof are also provided.

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: The present invention relates to the treatment and prevention of bone diseases in humans, including osteoporosis in postmenopausal women, Paget's Disease and hypercalcemia, by administration of a bisphosphonate in an inhalation form. The invention also relates to pharmaceutical inhalation compositions suitable for the treatment and prevention of bone diseases.

Abstract: This disclosure relates to compositions suitable for a variety of treatments, including ameliorating the undesirable side effects associated with compounds such as lipase inhibitors (e.g., anal leakage of undigested fat or oil). In particular, one embodiment of the present invention relates to compositions that are suitable for administration to an animal for the purpose of stiffening one or more lipophilic substances present in the gastrointestinal tract of the animal. The stiffening agents have a complete melting point of about 33° C. or greater. Various kits comprising the compositions are also described herein.

Abstract: The invention relates to a high dose oral formulation of bisphosphonates and to a process for the preparation of such formulations.

Abstract: The invention provides a drug combination for the treatment of diseases associated with bone metastasis. The combination provides adenosine or a derivative thereof, a bisphosphonate, and a targeting agent(s) to decrease the signs or symptoms associated with such diseases.

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: A bisphosphonate for the treatment of osteonecrosis and/or osteonecrosis dissecans. The drug may further be used to prevent the onset of osteonecrosis and/or osteonecrosis dissecans and any complications associated with both diseases.

Abstract: Administering thereto-upfront loading of a bisphosphonate agent can be used to treat primary and secondary osteoporosis, other metabolic bone diseases, alleviation of bone pain, transplant and drug-induced bone loss, Paget's disease of bone, loosening of prosthesis, or metastatic bone diseases in mammals, preferably a human female or a male. A bisphosphonate drug can be administered as a loading dose upfront. Bisphosphonates can be administered by themselves or combined with, one or more other medications acting on bone, such as HRT, selective estrogen receptor modulating drug, calcitonin, parathyroid hormone, fluoride, androgen, sex-steroid hormone analogues, nitroglycerin growth factors and their analogs, peptides and proteins and their analogues, or any other novel therapeutic agents.

Abstract: This invention relates to in-situ preparation of the derivatives of various hydroxy acids (HA), such as &agr;-(Alpha) Hydroxy Acids (AHA), &bgr;-(Beta) Hydroxy Acids (BHA), and Poly-Hydroxy Acids (PHA) with certain skin beneficial organic hetero-atom bases and their application in skin resurfacing (exfoliation), and in the synergistic treatment and regulation of topical disorders of skin such as skin aging, wrinkles, acne, rosacea, age-spots, canker sores, striae distensae (stretch marks), pimples, skin redness, and dry skin conditions of cracking, flaking, and scaling. Most HA derivatives produced by the in-situ method do not cause skin irritation and skin redness effects that are commonly experienced with AHA and BHA, yet there is no loss of their skin beneficial effects.

Abstract: The present invention relates to a composition for prevention and/or treatment of metabolic diseases of bones comprising at least one bisphosphonate; viscosity agents comprising carboxymethylcellulose and xanthan gum; at least one flavouring agent; and purified water; a process for preparing a composition according to the present invention; and use of such a composition for prevention, treatment and/or diagnosis of metabolic diseases of bones, especially for children.

Abstract: The invention relates to a method of producing the 1-hydroxy-1,1-diphosphonic acid compounds of general formula (I), and/or the pharmacologically acceptable salts thereof, in which formula R1 represents hydrogen, OH, NO2, Cl, F, Br, C1-C6 alkyl that may be substituted with halogen, amine and/or aminoalkyl, C1-6 alkoxy, aryl, heteroaryl, a group NR3R4, wherein R3 and R4 may be the same or different and represent hydrogen, C1-C6 alkyl, halogen-substituted alkyl, hydroxy-C1-alkyl; R2 represents hydrogen, halogen, amine that may be substituted, C1-C6 alkyl that may be substituted with halogen, amine and/or aminoalkyl, C1-C6 alkoxy, aryl, heteroaryl; Y represents O, S or NH; Z represents C1-C5 alkylene that may be substituted with amine groups, and m and n are 0 or 1, with the proviso that if n=1, m=1.

Abstract: The invention is directed to a method of treating chronic spinal mechanical pain by intravenous administration to a subject in need of chronic spinal mechanical pain relief of an effective amount of bisphosphonate.

Abstract: A pharmaceutical product containing pamidronate and other diphosphonate solutions in an appropriate container, a pH of between 5 and 8 and without organic acid buffer or polyethylen glycol. The container may be treated glass or made of other appropriate material. Coated elastomeric stoppers are also included. A method of producing a pharmaceutical product comprising steps of making a suspension of pamadronic acid, adding sodium hydroxide, to form a solution adjusting the pH to between 5 and 8 and transferring the solution to a container.

Abstract: Bisphosphonate (BP), pyrophosphate (PP) a complex of BP or PP, a polymer of BP or PP or pharmaceutically acceptable salt or ester thereof, are used for the prevention or treatment of vascular restenosis.

Abstract: A method for the treatment of pain, in particular antinociceptive or anti-allodynic treatment of pain, in a patient in need of such treatment, e.g. a patient with osteoporosis or osteopenia, a tumour patient or a patient suffering from an inflammatory disease, which comprises administering an effective amount of a bisphosphonate, e.g. zoledronic acid or salts or hydrates thereof, to the patient.

Abstract: A zero-order release pharmaceutical dosage form for oral administration to a patient comprising a core tablet sheathed in an annular body of compressed powder or granular material is provided. A preferred embodiment of the zero-order release pharmaceutical dosage form is a solid pharmaceutical dosage form which reduces contact of the active ingredient in solid form with the mucosa lining the gastrointestinal tract, which is particularly advantageous for delivering an ulcerative drug. A process for making the zero-order release pharmaceutical dosage form are also provided.

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: A composition and method for treating soft nails, particularly soft fingernails, the composition including bisphosphonate, preferably alendronate sodium, in a vehicle effective for topical administration.

Abstract: The present invention is directed to a pharmaceutical composition for administering active ingredients that cause upper gastrointestinal tract irritation. Said dosage form comprises the irritating active ingredient and an ion exchange resin. Said dosage form protects the tissues of the buccal cavity, pharynx, esophagus, and the stomach from erosion and ulceration due to exposure of the irritating active ingredient to said tissues.

Abstract: Provided is a novel method of making bisphosphonic acids, e.g. risedronic acid, including the step of combining a carboxylic acid, phoshorous acid, and a halophosphorous compound in the presence of a diluent that is an aromatic hydrocarbon or a silicone fluid. When the diluent is an aromatic hydrocarbon, a inert support or ortho-phosphoric acid codiluent is advantageously included.

Abstract: A method for providing bone therapy in a patient in need of bone therapy comprises administering to the patient a pharmaceutically effective amount of a compound comprising a biologically inert carrier, a bone vector; and a therapeutic agent. The bone vector preferably comprises a bisphosphonate, the carrier preferably comprises a fullerene, and more preferably C60, the therapeutic agent preferably comprises fluoride.

Abstract: The present invention relates to compositions and methods of preventing or reducing the risk or incidence of skeletal injuries in horses. The present invention further relates to compositions and methods for alleviating pain associated with skeletal injuries in horses and to treating skeletal injuries in horses.

Abstract: The present invention is directed to a novel enteric-coated oral dosage form of a risedronate active ingredient comprised of a safe and effective amount of a pharmaceutical compostion which is comprised of a risedronate active ingredient and pharmaceutically-acceptable excipients. Said dosage forms prohibit the exposure of the risedronate active ingredient to the epithelial and mucosal tissues of the buccal cavity, pharynx, esophagus, and stomach and thereby protects said tissues from erosion, ulceration or other like irritation. Accordingly, the said dosage forms effect the delivery to the lower intestinal tract of said human or other mammal of a safe and effective amount of the risedronate active ingredient, and substantially alleviate the esophagitis or esophageal irritation which sometimes accompanies the oral administration of risedronate active ingredients.

Abstract: A new and more efficient synthesis of combretastatin A-3 (2a) was completed (8.4% overall yield) starting front methyl gallate and isovanillin with aldehyde 5 and phosphonium salt 8 as key intermediates. Conversion of combretastatin A-3 (2a) to a series of diphosphate prodrugs (IOa-IOl) containing selected anions was achieved.

Abstract: The present invention relates to a method for maintaining a healthy bone structure by administering to a patient a bone health promoting effective amount of a medicament containing 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid, any of its soluble salts or any of its hydrates.

Abstract: Disclosed is a phosphate transport inhibiting compound represented by Structural Formula (I): 1

Abstract: The present invention relates to a novel dibenzoxazepine derivative, its synthesis, and its use as an &agr;v integrin receptor antagonist. More particularly, the compound of the present invention is an antagonist of the integrin receptors &agr;v&bgr;3 and &agr;v&bgr;5 and therefor useful for inhibiting bone resorption, treating and/or preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, artheroscietosis, inflammatory arthritis, cancer and metastatic tumor growth.

Abstract: The invention relates to an alveolar bone resorption inhibitor for use in topical injection by an alveolar mucosa injection method, which comprises a bisphosphonic acid derivative or a salt thereof as an active ingredient and to an alveolar bone resorption inhibitor for human periodontal tissue topical injection, which comprises a bisphosphonic acid derivative or a salt thereof in a concentration small enough so that local irritation to human periodontal tissues as the administrating site is acceptable but sufficient enough for expressing alveolar bone resorption inhibitory action by topical injection.

Abstract: The present invention comprises compounds, compositions thereof, and methods capable of delivering modified inositol hexaphospahte (IHP) comprising an internal pyrophosphate ring 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: The present invention is directed to a method for the preparation of a pharmaceutical composition having osteoclast formation inhibiting or suppressing activity, characterized in that, as the active agent, a compound of the formula (I) is used, in which formula Q1 is hydrogen, hydroxyl, halogen, amino —NH2, or —OR′, wherein R′ is C1-C4-alkyl or acyl, Q2 is straight or branched alkyl, hydroxyalkyl or aminoalkyl, or a corresponding unsaturated group optionally substituted at the hydroxy or amino group, or a unsubstituted or substituted, saturated or unsaturated cycloalkyl, which can be bound to the methylene carbon over a straight or branched alkylene group, or is the group (a) wherein Y is a saturated or unsaturated heterocyclic group, or a carbocyclic aromatic group, X is a bond, O, S or NR3, wherein R3 is hydrogen or a protecting group, especially lower alkyl, acyl, aryl or arylalkyl, and n is an integer 0 to 6, R1 and R2 are independently hydrogen or C1-C4-alkyl, or it is halogen, an

Abstract: The invention relates to compositions and methods for use in treating skeletal system disorders in a vertebrate at risk for bone loss, and in treating conditions that are characterized by the need for bone growth, in treating fractures, and in treating cartilage disorders. More specifically, the invention concerns the use of NO-bisphosphonate assembly for enhancing bone growth.

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 trans carotenoid salt compounds, methods for making them, methods for solubilizing them and uses thereof. These compounds are useful in improving diffusivity of oxygen between red blood cells and body tissues in mammals including humans.

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: A method of prophylaxis of a subject having or having had a soft tissue cancer, whereby to combat metastatic bone cancer therein, the method comprising administering to said subject a physiologically tolerable polyphosphonate and, parenterally, a prophylactically effective amount of a soluble radium-223 or -224 salt or complex. A kit comprising a first container containing a soluble radium-223 or -224 salt or complex and a second container containing at least one dose of a physiologically tolerable polyphosphonate is also provided.

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: Devices, methods, and improved formulation for transmucosal vaginal delivery of bisphosphonates. A targeted site delivery of bisphosphonates to the systemic circulation using a vaginal device comprising an improved bisphosphonate formulation for transmucosal delivery. A method for treatment of osteoporosis and related bone and skeleton diseases, for prevention of bone breakdown and loss of bone mass and strength by intravaginal administration of bisphosphonates to the vagina and transmucosal delivery of bisphosphonates to the general circulation.

Abstract: The present invention refers to a pharmaceutical composition of a bisphosphonic acid or salt thereof, and an excipient thereof, and a method of treating disorder characterized by pathologically increased bone resorption comprising orally administering at least 150% of the expected efficious daily dose of a bisphosphonic acid or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable excipients thereof and administering the dose at a period of one two or three consecutive days per month.

Abstract: Compositions and methods for vaginal, buccal or nasal transmucosal delivery of drugs and for cryoprotecting of cells and embryos. For cryoprotection, the composition consisting essentially consist of a non-ionizable glycol derivative. For transmucosal delivery, the compositions essentially consist of a non-ionizable glycol derivative in a combination with a pharmaceutically active agent. For transmucosal delivery, the non-ionizable glycol derivative may be further combined with a mucoadhesive agent and/or a penetration enhancer and/or lipophilic or hydrophilic carrier for adhesion to and transport through a mucosa. The compositions are particularly suitable for administration of drugs through a nasal, buccal and vaginal mucosa or for long-term preservation of cell or embryos.

Abstract: Novel quinazoline derivatives possessing activity as estrogen receptor beta (ER&bgr;) modulators are provided which have the general formula I 1