Abstract: Novel C-2-substituted bicyclic compounds of Formula I have been prepared and found to be useful as inhibitors of by inhibiting geranylgeranylation of proteins. The application is directed to these compounds, to compositions comprising these compounds and to their use, in particular as medicaments to cancer and other conditions treatable by inhibiting human geranylgeranylation pyrophosphate hGGPPS activity.

Abstract: The present invention relates to a composition for use in the treatment of osteoarthritis (OA), wherein said composition comprises from 5 to 40 mg of sodium chlodronate, or an equivalent amount of chlodronic acid, or other pharmaceutically acceptable salts thereof, and wherein said composition is administered intra-articularly in a unitary dosage form once monthly, once biweekly or once weekly. Single-dose medicaments and kits comprising them are also described.

Abstract: Disclosed herein are compositions and methods for treating tauopathies such as Alzheimer's disease (AD). Also provided herein are methods of reducing or disrupting tau aggregation in a subject, and methods of reducing tau protein in a subject. The methods may include administering to the subject a therapeutic amount of hexachlorophene, or a pharmaceutically acceptable salt thereof. Further provided herein are pharmaceutical compositions comprising hexachlorophene, or a pharmaceutically acceptable salt thereof, for the treatment of a tauopathy in a subject.

Abstract: Disclosed herein are compositions and methods for treating tauopathies such as Alzheimer's disease (AD). Also provided herein are methods of reducing or disrupting tau aggregation in a subject, and methods of reducing tau protein in a subject. The methods may include administering to the subject a therapeutic amount of hexachlorophene, or a pharmaceutically acceptable salt thereof. Further provided herein are pharmaceutical compositions comprising hexachlorophene, or a pharmaceutically acceptable salt thereof, for the treatment of a tauopathy in a subject.

Abstract: Oral dosage forms of osteoclast inhibitors, such as zoledronic acid, in an acid or a salt form, can be used to treat or alleviate pain or related conditions.

Abstract: Oral dosage forms of osteoclast inhibitors, such as neridronic acid, in an acid form or a salt form can be used to treat or alleviate pain or related conditions, such as allodynia associated with complex regional pain syndrome.

Abstract: Oral dosage forms of osteoclast inhibitors, such as neridronic acid, in an acid or a salt form can be used to treat or alleviate pain or related conditions, such as arthritis.

Abstract: Osteoclast inhibitors, such as neridronic acid, in an acid or a salt form can be used to treat or alleviate pain or related conditions, such as complex regional pain syndrome.

Abstract: Oral dosage forms of osteoclast inhibitors, such as neridronic acid and zoledronic acid, in an acid or a salt form can be used to treat or alleviate pain or related conditions, such as joint pain.

Abstract: The present invention relates to a method for substituting for or acting with the hyperbaric oxygen therapy to improve hypoxia, comprising the step of: administrating a phthalide compound to a subject in need thereof, wherein the phthalide compound can increase the oxygen release efficiency of blood hemoglobin (Hb) in the subject and further increase the cellular oxygenation level, and when the phthalide compound substitutes for or act with the hyperbaric oxygen therapy, the common adverse side effects of the hyperbaric oxygen therapy, such as barotrauma, decompression sickness and oxygen poisoning, are prevented. The phthalide compound is used to substitute for or act with 2,3-BPG, to modulate and decrease the oxygen affinity of hemoglobin (Hb), to increase the oxygen release efficiency of hemoglobin (Hb) to tissue cells, thereby achieving a normal cellular oxygenation level and maintaining the cellular oxygenation level in a normal range.

Abstract: Oral dosage forms of osteoclast inhibitors, such as neridronic acid, in an acid or a salt form can be used to treat or alleviate pain or related conditions, such as complex regional pain syndrome.

Abstract: The invention relates to the treatment of bone disorders. In particular, the invention is directed to the use of a dosing holiday to help overcome the resistance to anti-sclerostin antibodies which develops over time when a plurality of doses of antibody are given to a subject. By giving the subject to be treated such a dosing holiday, the subject may subsequently display an increased response to a subsequent dose of the anti-sclerostin antibody. The subject may be given multiple cycles of a batch of at least two doses of anti-sclerostin antibody and a dosing holiday. In some instances, the subject may be monitored to help determine when to give the dosing holiday. Further, the subject may be given a different treatment for the bone disorder during the dosing holiday from the anti-sclerostin antibody.

Abstract: A method for bone regeneration which comprises administering a short term release composition into a bone area of a subject in need thereof, wherein the composition comprises a poly(lactic-co-glycolic acid) cross-linked alendronate (PLGA-ALN), wherein the composition releases the alendronate into the bone area, wherein the bone tissue of the bone area is exposed in situ to a therapeutically effective amount of the alendronate over 9 days.

Abstract: Oral, parenteral, and intravenous dosage forms of osteoclast inhibitors, such as neridronic acid, can be used to treat or alleviate pain or related conditions, such as knee pain.

Abstract: A method of treating TDP-43 proteinopathies such as Alzheimer's disease, amyotrophic lateral sclerosis, and fronto-temporal lobar dementia is presented herein. It was found that administering hexachlorophene to cells expressing endogenous TDP-43 or overexpressing wild-type TDP-43 reduced accumulation of TDP-43 in the cells.

Abstract: Oral dosage forms of osteoclast inhibitors, such as zoledronic acid, in an acid or a salt form can be used to treat or alleviate pain or related conditions, such as bone marrow lesions.

Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions such as complex regional pain syndrome.

Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions such as bone marrow lesion.

Abstract: This invention relates to a composition comprising an anti-HIV treatment and a treatment for side effects of said anti-HIV treatment in an HIV-infected patient. This invention is, for example, very useful in the treatment of side effects caused by certain anti-HIV treatments, for example premature aging and lipodystrophy, which can be caused by protease inhibitors or reverse transcriptase inhibitors. The composition of this invention includes at least one hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor, at least one farnesyl-pyrophosphate synthase inhibitor, and at least one anti-HIV agent. One of the processes for treating an HIV-infected patient includes, in any order, the following steps: (i) administration of a mixture including at least one hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor and at least one farnesyl-pyrophosphate synthase inhibitor and (ii) administration of an anti-HIV agent, in which the administrations are concomitant, successive or alternative.

Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.

Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.

Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.

Abstract: The present invention is directed to antiviral compositions that provide efficacy against non-envelope viruses such as noroviruses. The antiviral compositions comprise an alcohol and a synergistic combination of an aromatic carboxylic acid and an aromatic hydroxyamide. The composition may be used as a topical on human skin, as a hand sanitizer or as a hard surface cleaning composition.

Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.

Abstract: Novel peptides are described which comprise an amino acid motif selected from the group consisting of “PG”, “GP”, “PI” and “IG” and having up to 10 amino acids upstream and/or downstream of the amino acid motif, wherein “P” in the motif is proline or hydroxyproline and the peptide stimulates the development, maintenance and repair of bone, cartilage and associated connective tissue. The invention further relates to pharmaceutical compositions of these peptides, as well as therapeutic and prophylactic uses of such peptides.

Abstract: Described herein are dental compositions, articles of manufacture including such dental compositions, and methods of using such dental compositions. In some embodiments, the dental compositions include a combination of ascorbic acid with at least one of a hexametaphosphate and a beta glucans. In some instances, the dental compositions are included within an edible article, a chew, or an edible chew. Administration of the dental compositions to the oral cavity of a subject may reduce the gingival, plaque, and/or calculus scores of the subject over a defined time period.

Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.

Abstract: According to the invention there is provided a compound of formula (I): wherein R1, R2, R3 and n have meanings given in the description, or a pharmaceutically acceptable solvate, salt or prodrug thereof for use in the treatment of osteoporosis and/or osteopenia.

Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.

Abstract: The present invention relates to the field of osteoarthritis. More specifically, the present invention provides compositions and methods useful for treating or preventing osteoarthritis. In one embodiment, a method for treating or preventing osteoarthritis in a patient comprises the step of administering to the patient a therapeutically effective amount of a transforming growth factor beta (TGF-beta) inhibitor.

Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.

Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.

Abstract: Provided is a moisturizer having hygroscopicity and water retention ability, and also provided is a composition superior in antiseptic property and feeling on application, in addition to moisturizing property, and free of coloration and odorization. A moisturizer containing acylproline represented by the formula (1) wherein an acyl group represented by R1—CO— is an acyl group derived from a saturated or unsaturated fatty acid having 3-23 carbon atoms, or a salt thereof, and a composition containing (A) acylproline represented by the above formula (1) or a salt thereof and (B) bisphosphonate.

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: Disclosed herein are implantable medical devices comprising controlled release biodegradable block copolymers or coated with controlled release block copolymers and at least one drug releasable from the block copolymer. The controlled release block copolymers comprise least two blocks selected from the group consisting of polyesters, polyethers, and polyurethanes.

Abstract: Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions.

Abstract: The present invention provides phosphonate conjugates and methods of preparing the phosphonate conjugates so as to allow, for example, improved methods and compounds for modifying the surface of a nanoparticle to increase in vivo circulation times and targeted delivery performance.

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 characterized 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 invention relates to a complex of a bisphosphonate compound, methods of preparing such complex and uses thereof.

Abstract: The invention provides methods for treating fibrosis, as well as methods for modulating mitochondrial peroxide production in a cell, and methods for modulating the import of Rac1 into the mitochondria of a cell.

Abstract: A bone filler composition comprises a mixture of a curable calcium phosphate based bone filler which is formed from a liquid component and a calcium phosphate based powder component, and a formulation which comprises a bisphosphonate in particulate form. The particles of the bisphosphonate being embedded in particles of a polymeric material which resorbs when the formulation is implanted.

Abstract: The present invention relates to the regional delivery of therapeutic agents for the treatment of vascular diseases wherein regional delivery refers to delivery of a therapeutically effective amount of the therapeutic agent to an area of the vessel that includes not only afflicted tissue but non-afflicted tissue at the periphery of the afflicted tissue as well.

Abstract: This disclosure relates, at least in part, to a method of treatment. In one embodiment, the method of treatment comprises administering to a subject in need of such treatment a first therapeutic agent including compound (1): or a pharmaceutically acceptable salt thereof in combination with a second therapeutic agent, wherein the first therapeutic agent and the second therapeutic agent are administered either simultaneously or sequentially.

Abstract: The invention relates to a pharmaceutical composition and oral dosage forms comprising a bisphosphonate in combination with an enhancer to enhance intestinal delivery of the bisphosphonate to the underlying circulation. Preferably, the enhancer is a medium chain fatty acid or a medium chain fatty acid derivative having a carbon chain length of from 6 to 20 carbon atoms, and the solid oral dosage form is a controlled release dosage form such as a delayed release dosage form.

Abstract: Compounds, compositions, and methods of treatment and prevention of HIV infection are disclosed. The compounds are pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidine JAK inhibitors. Combinations of these JAK inhibitors and additional antiretroviral compounds, such as NRTI, NNRTI, integrase inhibitors, entry inhibitors, protease inhibitors, and the like, are also disclosed. In one embodiment, the combinations include a combination of adenine, cytosine, thymidine, and guanine nucleoside antiviral agents, optionally in further combination with at least one additional antiviral agent that works via a different mechanism than a nucleoside analog. This combination has the potential to eliminate the presence of HIV in an infected patient.

Abstract: The present invention provides a method of promoting local bone growth by administering a therapeutic amount of a Sost antagonist to a mammalian patient in need thereof. Preferably, the Sost antagonist is an antibody or FAB fragment selectively recognizing any one of SEQ ID NOS: 1-23. The Sost antagonist may be coadministered together or sequentially with a matrix conducive to anchoring new bone growth. Orthopedic and Periodontal devices comprising an implantable portion adapted to be permanently implanted within a mammalian body and bearing an external coating of a Sost antagonist are also disclosed, as it a method of increasing bone density by administering to a mammalian patient a therapeutic amount of a Sost antagonist together with an antiresorptive drug.

Abstract: A combination therapy for treating osteoarthritis is disclosed. The combination therapy includes the co-administration of a steroid and Zoledronic Acid. The coadministration of a steroid decreases the production of cytokines, and, therefore, decreases the pro-inflammatory effects of Zoledronic Acid. The co-administration of Zoledronic Acid with steroids treats osteoarthritis, and helps to prevent the onset of osteoarthritis in patients at risk for osteoarthritis.

Abstract: This invention relates to a composition that comprises inositol phosphates and/or bisphosphonates, and to the use thereof to prevent the loss of substances of biological interest in the body of patients subjected to dialysis and to maintain sufficient physiological levels of said substances to regulate physiological and/or pathological processes, these substances being inhibitors of pathological crystallisation.

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 flavoring 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 for methods and compositions for treating, reducing and/or preventing cardiac dysfunction by administering to subject a therapeutically effective amount of a bisphosphonate, prodrug thereof, functional analogue or a pharmaceutically effective salt thereof in an amount sufficient to increase activity of at least one kinase in heart tissue of the subject.