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 present invention provides an adhesive preparation having a plaster layer disposed on a support, the adhesive preparation comprising at least one active ingredient selected from the group consisting of a bisphosphonic acid derivative, its salt thereof and a hydrate of either of the bisphosphonic acid derivative or the salt, a solubilizer for the active ingredient, propylene glycol, a hydrogenated terpene resin, an adhesive base, and a softening agent in the plaster layer.

Abstract: Disclosed herein are biocompatible carbon-based nitric oxide (NO) donating polymers suitable for forming and coating medical devices. These polymers have acrylate backbones and are comprised of substantially hydrophobic monomers. The NO donating polymers are carbon based wherein the diazeniumdiolate group is attached to the acetate group on an acetate based monomer. Incorporating a vinyl acetate monomer into an acrylate based polymer allows diazeniumdiolation of a polymer that would otherwise not accommodate the diazeniumdiolate group.

Abstract: This invention provides pharmaceutical compositions and methods related to the prevention and treatment of primary tumors and metastatic, malignant or spreading cancers by selectively targeting cancer associated myeloid derived cells by the targeted delivery of a bisphosphonate formulated with a non-liposomal particle carrier. In some aspects, the bisphosphonate particles have one or more properties suitable for phagocytosis by cancer associated myeloid derived cells and release of the bisphosphonate within the macrophages. Advantageously, administering the particles to a subject reduces the level and/or activity of cancer associated myeloid derived cells in the subject.

Abstract: Provided are methods of treating bone disease including, but not limited to, osteoporosis, metastatic bone disease, or Paget's disease, by administering a combination of raloxifene and alendronate in a manner that mitigates the formation of ulcerative adverse events.

Abstract: The present invention relates to compounds and methods useful in the prevention or treatment of diseases or conditions associated with Toll-like receptor 2 activation.

Abstract: A metal coordination complex of a biologically active moiety and a metal is disclosed. The complex confers to the biologically active moiety an improved performance which can include potency, stability, absorbability, targeted delivery, and combinations thereof.

Abstract: The present invention relates to antibodies against sclerostin and compositions and methods of use for said antibodies to treat disease related to bone abnormalities such as osteoporosis. An embodiment of the invention herein provides an antibody or a functional protein comprising an antigen-binding portion of said antibody for a target in sclerostin polypeptide, characterized in that the antibody or functional protein specifically binds to sclerostin polypeptide and can increase at least one of bone formation, bone mineral density, bone mineral content, bone mass, bone quality and bone strength in a mammal.

Abstract: The invention relates to a dental implant, which comprises a coating at least in those surface areas that come into contact with hard and/or soft tissue when implanted. To ensure that the active ingredient contained in the coating (bisphosphonate) is released into the surrounding tissue or can act in the latter in a controlled manner at the correct speed, the coating is characterised in that it contains bisphosphonate, the respective pharmaceutically compatible salts or esters of the latter, in addition to at least one amphiphilic component, selected from the group containing branched or linear, substituted or unsubstituted, saturated or partially unsaturated C10-C30 alkyl-, alkenyl, alkylaryl-, aryl-, cycloalkyl-, alkylcycloalkyl-, alkylcycloaryl-carboxylates, -phosphates or -sulfates or mixtures thereof and/or a water-soluble ionic polymer component.

Abstract: The present application describes deuterium-enriched alendronate sodium, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: Novel etiology and pathogenesis of premenstrual headache and premenstrual migraine are presented and novel treatment methods are provided. Present invention identifies how declining estrogen results in a transient elevation in extracellular calcium concentrations via osteoclast upregulation. The elevated extracellular calcium pathogenesis is then traced, from bone to brain, and includes depolarization of nerves, hyperactive neurotransmitter release, and hyperactive muscle contractility. Treatment methods are provided that target the earliest steps of the underlying etiology, in order to provide the most efficacious treatment possible. The treatment methods presented include use of compounds such as calcitonin and SERMs such as raloxifene.

Abstract: The present invention provides dialkyl ether compounds and pharmaceutically acceptable salts thereof, compositions containing the same and one or more active agents, and methods of administering active agents with the same.

Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

Abstract: The invention relates to a combined pharmaceutical preparation comprising parathyroid hormone and a bone resorption inhibitor, said preparation being adapted for (a) the administration of parathyroid hormone during a period of approximately 6 to 24 months; (b) after the administration of parathyroid hormone has been terminated, the administration of a bone resorption inhibitor during a period of approximately 12 to 36 months.

Abstract: The present application describes deuterium-enriched ibandronate, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: This invention relates to methods of treating or preventing bone loss by administering to a human or animal subject pyrimidine and pyridine derivatives that inhibit the activity of glycogen synthase kinase 3 (GSK3), to pharmaceutical compositions containing the compounds, and to the use of the compounds and compositions alone or in combination with other pharmaceutically active agents.

Abstract: Methods of treating a subject with neoplasm (e.g., mesothelioma) or at risk of developing neoplasm by administering a mevalonate pathway inhibitor such as a nitrogen-containing bisphosphonate are disclosed. Examples of nitrogen-containing bisphosphonates include alendronate, ibandronate, minodronate, neridronate, olpadronate, pamidronate, risedronate, and zoledronate. The methods can further include the administration of a p38 inhibitor. Further disclosed are compositions and kits including a nitrogen-containing bisphosphonate and optionally a p38 inhibitor.

Abstract: Provided are crystalline forms of ibandronate sodium, as well as processes for the preparation thereof.

Abstract: The combination of an interleukin-6 (IL-6) antagonist and an antiproliferative drug is described. In its preferred embodiment, the present invention describes the combination of an IL-6 superantagonist, particularly a superantagonist totally incapable of binding gp130 and an antiproliferative drug belonging to the glucocorticoid class (SANT-7 and dexamethasone). The combination according to the present invention has shown surprising synergism in an animal model of multiple myeloma and the ability to overcome the resistance to the antiproliferative drug developed by myeloid cells. The combination according to the present invention is useful for the preparation of a medicament for the treatment of tumours, particularly IL-6-dependent tumours.

Abstract: Improved treatments of joint diseases, such as, e.g.

Abstract: Provided are crystalline forms of ibandronate sodium, as well as processes for the preparation thereof.

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: A buccal delivery system capable of being blended in a normal dry powder process and compressed using a standard tabletting machine, said buccal delivery system comprising a matrix of: (a) an effective amount of one or more active ingredients; (b) an amount of one or more polyethylene glycols or derivatives thereof having a molecular weight between 1000 to 8000 sufficient to provide the required hardness and time for dissolution of the matrix; (c) 0.05-2% by weight of the total matrix of one or more suspending agents; (d) 0.05-2% by weight of the total matrix of one or more flowing agents; and (e) 0.05-2% by weight of the total matrix of one or more sweeteners.

Abstract: A method of treating osteoporosis in a human in need thereof by administering alternating amine and non-amine bisphosphonates in a defined dosing schedule. The invention demonstrates an effective response and sustained benefit in the treatment of osteoporosis. Particularly, the method involves administration of a time-dependent dose of more than one bisphosphonate, specifically, alternating administration of a first bisphosphonate with a second bisphosphonate, wherein at least one bisphosphonate is administered in a stepped-up dosage amount.

Abstract: Anti-resorptive bone cements, comprising an anti-resorptive amount of one or more anti-resorptive agents, preferably the anti-resorptive agent is a bisphosphonate. The anti-resorptive bone cements are useful for reducing bone voids and bonding prosthetic devices to bone. The invention also relates to anti-resorptive allogeneic, autografic, and xenografic bone grafts, which bone grafts comprise an anti-resorptive amount of an anti-resorptive agent such as a bisphosphonate. The anti-resorptive bone grafts are useful for reconstructive bone surgery.

Abstract: This invention relates to methods of inhibiting a Cav3 calcium channel in a cell using a C2-C10 alkyl alcohol, or mixtures thereof. This invention further relates to methods of treating a thalamocortical dysrhythmia disorder in a mammal and for treating a neurological disorder in a mammal associated with the thalamocortical dysrhythmia using a C2-C10 alkyl alcohol, a lipophilic molecule with a partition coefficient substantially similar to that of a C2-C10 alkyl alcohol, or mixtures thereof, or a pharmaceutical composition comprising the same.

Abstract: Disclosed are methods for treating bone disorders in mammals. The methods comprise a loading period with a bisphosphonate followed by a maintenance period. The loading dose is two to twenty times per day greater than the corresponding maintenance dose. Also disclosed are compositions and kits for implementing the methods disclosed herein.

Abstract: A compound represented by the following formula (1), a pharmaceutically acceptable salt thereof or an optically active form thereof: wherein each symbol is as defined in the specification. A compound having a calcium-sensing receptor antagonistic action, a pharmaceutical composition comprising the compound, particularly a calcium receptor antagonist and a therapeutic drug for osteoporosis are provided.

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: This procedure consists in the first stage, of the administration of enough quantity of bisphosphonate preparation during the necessary period of time to acquire a degree of volumetric mineral density of the cortical tissue of application, within the normal range (average.±.1 DS). Then the administration of the bisphosphonate preparation is interrupted in order to enable the development of the sectional momentum of inertia. The length of the second stage can be determined by means of a tomography. That is to say, that the periods of administration or non-administration of the mineralizing agent are defined or controlled by precise osteologic variables and therefore are not fixed. If during the second stage the cortical mineral density drops by 6-10% of the maximum value previously obtained, administration of bishphosphonate preparation should be resumed until the corresponding maximum adjusted value is reached again.

Abstract: The solid precursor is used for the preparation of a pasty bone replacement material by admixture of a liquid. The precursor comprises calcium-containing ceramic particles and a hydrogel or a substance which can be swelled into a hydrogel; whereby said precursor has been obtained by wet autoclaving and subsequent drying.

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.

Abstract: An antimicrobial composition, including a synergistic combination of three or more agents as an active ingredient. Each of the three or more potentiating agents can be selected from the following types of compounds: sequestering agents, carbohydrates and carbohydrate derivatives, terpenes/terpenoids, amines and amine derivatives, plant-derived oils, sulfonates, phenols, fatty acids, dibenzofuran derivatives, organo isothiocyanates, quaternary ammonium compounds, peroxides and peroxide donors, and macrolide polyenes. At least two of the three or more potentiating agents are not of the same type of compound. The antimicrobial composition can have strong antimicrobial efficacy in control of microorganisms having resistance to currently used antimicrobials.

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: The present invention relates to liquid pharmaceutical compositions comprising a bisphosphonate compound.

Abstract: The present invention provides for methods of administering a bisphosphonate active agent to a subject in need thereof. Aspects of the invention include administering the bisphosphonate active agent to the subject by a pulmonary route, where the bisphosphonate active agent is bonded, either directly or through an intervening linking group, to a non-peptide polymer, such that the bisphosphonate active agent is a polymer-linked-bisphosphonate active agent. Also provided are compositions for use in practicing methods according to embodiments of the invention. Methods and compositions according to embodiments of the invention find use in a variety of different applications, including but not limited to, the treatment of bone adsorption disease conditions.

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: The present invention relates to pharmaceutical compositions comprising a bisphosphonate compound.

Abstract: Pharmaceutical compositions for long-term sustained release of bisphosphonate drugs are provided. In one embodiment, the composition includes an aqueous suspension of a solid which includes a salt of a bisphosphonate drug and a salt of pentavalent phosphorus oxoacid. The compositions can be used to treat a variety of bone diseases, including osteoporosis.

Abstract: Provided is a pharmaceutical composition having improved oral absorption of a bisphosphonate drug, comprising at least one active substance selected from bisphosphonate drugs having non-permeability to a lipid biomembrane due to ionization and high water-solubility in vivo and having bioavailability of less than 10%, and at least one selected from biocompatible water-soluble chitosan, as essential ingredients.

Abstract: A composition for transdermal delivery of a non-traditional active agent is described. The compositions comprise: (a) a non-traditional transdermal active agent; (b) a solvent; (c) a non-miscible liquid; (d) a stabilizer; and (e) water, wherein the composition is formulated into an emulsion.

Abstract: Solid pharmaceutical compositions comprising a diphosphonic acid or a pharmaceutically acceptable salt, solvate, hydrate, prodrug, enantiomer or racemic mixture thereof. The invention includes compositions with inner and outer phases, wherein the inner phase comprises no more than about 80% w/w and the outer phase comprises at least about 20% w/w.

Abstract: The present invention provides for methods of administering by a pulmonary route an effective amount of a bisphosphonate active agent to a subject. Aspects of the invention including administering the active agent to the subject in conjunction with one or more mucosal membrane protecting agents, where the protecting agent may include one or more of a protecting enzyme and/or a protecting amino acid and/or a protecting peptide. Also provided are inhalant compositions for use in practicing methods according to embodiments of the invention. Methods and compositions according to embodiments of the invention find use in a variety of different applications, including but not limited to, the treatment of bone adsorption disease conditions.

Abstract: Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner.

Abstract: Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

Abstract: Compounds and compositions for the delivery of bisphosphonates are provided. Methods of preparation, administration and treatment are provided as well.

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: 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: This invention relates to a method of treating a patient suffering from ionizing radiation exposure, or of treating a patient about to undergo ionizing radiation therapy. The method includes administering to a patient in need of treatment an effective amount of a thiol or reducible disulfide compound according to the formula set forth in the specification.

Abstract: Compounds of the formula wherein the substitutents are defined as in the specification useful for modulating immune responses in warm-blooded animals.