152 results about "Bisphosphonate" patented technology

This invention relates to a method for prevention and treatment of aging and age-related disorders including atherosclerosis, peripheral vascular disease, coronary artery disease, osteoporosis, type 2 diabetes, dementia and some forms of arthritis and cancer in a subject comprising administering to said subject, separately, sequentially or simultaneously a therapeutically effective dosage of each component or combination of statins, bisphosphonates, cholesterol lowering agents or techniques, interleukin-6 inhibitor / antibody, interleukin-6 receptor inhibitor / antibody, interleukin-6 antisense oligonucleotide (ASON), gp130 protein inhibitor / antibody, tyrosine kinases inhibitors / antibodies, serine / threonine kinases inhibitors / antibodies, mitogen-activated protein (MAP) kinase inhibitors / antibodies, phosphatidylinositol 3-kinase (PI3K) inhibitors / antibodies, Nuclear factor κB (NF-κB) inhibitors / antibodies, IκB kinase (IKK) inhibitors / antibodies, activator protein-1 (AP-1) inhibitors / antibodies, STAT transcription factors inhibitors / antibodies, altered IL-6, partial peptides of IL-6 or IL-6 receptor, or SOCS (suppressors of cytokine signaling) protein, or a functional fragment thereof, administered separately, in sequence or simultaneously. Inhibition of the signal transduction pathway for Interleukin 6 mediated inflammation is key to the prevention and treatment of atherosclerosis, peripheral vascular disease, coronary artery disease, aging and age-related disorders including osteoporosis, type 2 diabetes, dementia and some forms of arthritis and tumors. Inhibition of Interleukin 6 mediated inflammation may be achieved indirectly through regulation of endogenous cholesterol synthesis and isoprenoid depletion or by direct inhibition of the signal transduction pathway utilizing interleukin-6 inhibitor / antibody, interleukin-6 receptor inhibitor / antibody, interleukin-6 antisense oligonucleotide (ASON), gp130 protein inhibitor / antibody, tyrosine kinases inhibitors / antibodies, serine / threonine kinases inhibitors / antibodies, mitogen-activated protein (MAP) kinase inhibitors / antibodies, phosphatidylinositol 3-kinase (PI3K) inhibitors / antibodies, Nuclear factor κB (NF-κB) inhibitors / antibodies, IκB kinase (IKK) inhibitors / antibodies, activator protein-1 (AP-1) inhibitors / antibodies, STAT transcription factors inhibitors / antibodies, altered IL-6, partial peptides of IL-6 or IL-6 receptor, or SOCS (suppressors of cytokine signaling) protein, or a functional fragment thereof. Said method for prevention and treatment of said disorders is based on inhibition of Interleukin-6 inflammation through regulation of cholesterol metabolism, isoprenoid depletion and / or inhibition of the signal transduction pathway.

This invention relates to a method for prevention and treatment of Atherosclerosis, Peripheral Vascular Disease, Coronary Artery Disease, and age-related disorders including Osteoporosis, Arthritis, Type II Diabetes, Dementia and Alzheimer's disease in a subject comprising administering to said subject a therapeutically effective dosage of each component or combination of statins, bisphosphonates, cholesterol lowering agents or techniques, interleukin-6 inhibitor / antibody, interleukin-6 receptor inhibitor / antibody, gp130 protein inhibitor / antibody, tyrosine kinases inhibitors / antibodies, STAT transcription factors inhibitors / antibodies, altered IL-6, partial peptides of IL-6 or IL-6 receptor, or SOCS (suppressors of cytokine signaling) protein, or a functional fragment thereof, administered separately, in sequence or simultaneously. Inhibition of the signal transduction pathway for Interleukin 6 mediated inflammation is key to the prevention and treatment of atherosclerosis, peripheral vascular disease, coronary artery disease, aging and age-related disorders including osteoporosis, type 2 diabetes, dementia and some forms of arthritis and tumors. Inhibition of Interleukin 6 mediated inflammation may be achieved indirectly through regulation of endogenous cholesterol synthesis and isoprenoid depletion or by direct inhibition of the signal transduction pathway including interleukin-6 inhibitor / antibody, interleukin-6 receptor inhibitor / antibody, gp130 protein inhibitor / antibody, tyrosine kinases inhibitors / antibodies, STAT transcription factors inhibitors / antibodies, altered IL-6, partial peptides of IL-6 or IL-6 receptor, or SOCS (suppressors of cytokine signaling) protein, or a functional fragment thereof. Said method for prevention and treatment of said disorders is based on inhibition of Interleukin-6 inflammation through regulation of cholesterol metabolism, isoprenoid depletion and inhibition of the signal transduction pathway.

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.

The invention is directed to a method of inhibiting bone resorption. The method comprises administering to a human an amount of sclerostin inhibitor that reduces a bone resorption marker level for at least 2 weeks. The invention also provides a method of monitoring anti-sclerostin therapy comprising measuring one or more bone resorption marker levels, administering a sclerostin binding agent, then measuring the bone resorption marker levels. Also provided is a method of increasing bone mineral density; a method of ameliorating the effects of an osteoclast-related disorder; a method of treating a bone-related disorder by maintaining bone density; and a method of treating a bone-related disorder in a human suffering from or at risk of hypocalcemia or hypercalcemia, a human in which treatment with a parathyroid hormone or analog thereof is contraindicated, or a human in which treatment with a bisphosphonate is contraindicated.

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

The invention relates to a pharmaceutical composition and oral dosage forms comprising a bisphosphonate in combination with an enhancer to promote absorption of the bisphosphonate at the GIT cell lining. 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. Preferably, the solid oral dosage form is a controlled release dosage form such as a delayed release dosage form.

A method of treating acne in a human in need thereof comprising administering systemically to said human a tetracycline compound in an amount that is effective to treat acne but has substantially no antibiotic activity, without administering a bisphosphonate compound.

A composition is provided which contains calcium chelators, bisphosphonates, and / or citrate compounds and which may be used for treating and or reducing pathological calcifications, heavy metal poisoning, the growth of Nanobacterium Calcifying Nano-Particles and calcification-induced diseases in humans and animals. The method includes administering a therapeutic composition of calcium chelators, bisphosphonates, and / or citrate compounds which effectively inhibit or treat the development of calcifications in vivo. Typically, the administered composition includes about 0.1-10:1 parts by weight of calcium chelators, bisphosphonates, and / or citrate compounds.

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.

This invention relates to a method for prevention and treatment of Atherosclerosis, Peripheral Vascular Disease, Coronary Artery Disease, and age-related disorders including Osteoporosis, Arthritis, Type II Diabetes, Dementia and Alzheimer's disease in a subject comprising administering to said subject a therapeutically effective dosage of each component or combination of statins, bisphosphonates and / or cholesterol lowering agents or techniques, administered separately, in sequence or simultaneously. Cholesterol Metabolites (isoprenoids) are an integral component of the signaling pathway for Interleukin 6 mediated inflammation. Interleukin 6 inflammation is the common causative origin for Atherosclerosis, Peripheral Vascular Disease, Coronary Artery Disease, and age-related disorders including Osteoporosis, Arthritis, Type II Diabetes, Dementia and Alzheimer's disease. Said method for prevention and treatment of said disorders is based on inhibition of Interleukin-6 inflammation through regulation of cholesterol metabolism and isoprenoid depletion.

Methods and compositions are provided which contains preparations of calcium chelators, bisphosphonates, antibiotics, antimicrobial agents, cytostatic agents, calcium ATPase and pyrophosphatase pump inhibitors, calcium phosphate-crystal dissolving agents, agents effective against calcium phosphate-crystal nucleation and crystal growth, and / or a combination of supportive agents and which may be used for treating and or reducing pathological calcifications, the growth of Nanobacterium and calcification-induced diseases including, but not limited to, Arteriosclerosis, Atherosclerosis, Coronary Heart Disease, Chronic Heart Failure, Valve Calcifications, Arterial Aneurysms, Calcific Aortic Stenosis, Transient Cerebral Ischemia, Stroke, Peripheral Vascular Disease, Vascular Thrombosis, Dental Plaque, Gum Disease (dental pulp stones), Salivary Gland Stones, Chronic Infection Syndromes such as Chronic Fatigue Syndrome, Kidney and Bladder Stones, Gall Stones, Pancreas and Bowel Diseases (such as Pancreatic Duct Stones, Crohn's Disease, Colitis Ulcerosa), Liver Diseases (such as Liver Cirrhosis, Liver Cysts), Testicular Microliths, Chronic Calculous Prostatitis, Prostate Calcification, Calcification in Hemodialysis Patients, Malacoplakia, Autoimmune Diseases. Erythematosus, Scleroderma, Dermatomyositis, Antiphospholipid Syndrome, Arteritis Nodosa, Thrombocytopenia, Hemolytic Anemia, Myelitis, Livedo Reticularis, Chorea, Migraine, Juvenile Dermatomyositis, Grave's Disease, Hypothyreoidism, Type 1 Diabetes Mellitus, Addison's Disease, Hypopituitarism, Placental and Fetal Disorders, Polycystic Kidney Disease, Glomerulopathies, Eye Diseases (such as Corneal Calcifications, Cataracts, Macular Degeneration and Retinal Vasculature-derived Processes and other Retinal Degenerations, Retinal Nerve Degeneration, Retinitis, and Iritis), Ear Diseases (such as Otosclerosis, Degeneration of Otoliths and Symptoms from the Vestibular Organ and Inner Ear (Vertigo and Tinnitus)), Thyroglossal Cysts, Thyroid Cysts, Ovarian Cysts, Cancer (such as Meningiomas, Breast Cancer, Prostate Cancer, Thyroid Cancer, Serous Ovarian Adenocarcinoma), Skin Diseases (such as Calcinosis Cutis, Calciphylaxis, Psoriasis, Eczema, Lichen Ruber Planus), Rheumatoid Arthritis, Calcific Tenditis, Osteoarthritis, Fibromyalgia, Bone Spurs, Diffuse Interstitial Skeletal Hyperostosis, Intracranial Calcifications (such as Degenerative Disease Processes and Dementia), Erythrocyte-Related Diseases involving Anemia, Intraerythrocytic Nanobacterial Infection and Splenic Calcifications, Chronic Obstructive Pulmonary Disease, Broncholiths, Bronchial Stones, Neuropathy, Calcification and Encrustations of Implants, Mixed Calcified Biofilms, and Myelodegenerative Disorders (such as Multiple Sclerosis, Lou Gehrig's and Alzheimer's Disease) in humans and animals. The method comprises administering the various classes of compositions of the present invention, which together effectively inhibit or treat the development of calcifications in vivo.

Novel methods for the medical treatment and / or inhibition of the development of hypercholesterolemia in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator particularly compounds having the general structure: and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3β,17β-diol and compounds converted in vivo to one of the foregoing precursor. Further administration of bisphosphonates in combination with selective estrogen receptor modulators and / or sex steroid precursor is disclosed for the medical treatment and / or inhibition of the development of osteoporosis. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.

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.

The present invention relates to novel compositions comprising an excision-inhibiting bisphosphonate and a nucleoside reverse transcriptase inhibitor. The present invention also relates to methods for preventing or treating retrovirus-related diseases using a composition comprising a bisphosphonate and a nucleoside reverse transcriptase inhibitor. In a specific embodiment, the invention provides methods for preventing or treating AIDS by administering a bisphosphonate-based compound in combination with 3′-azido-3′-deoxythymidine (AZT) to patients infected with AZT-resistant HIV to improve the effectiveness of AZT therapy.

The present invention provides a method of treating or preventing osteoporosis comprising administering to a patient in need thereof an effective amount of pharmaceutical composition comprising benzamidine derivative or its salt, and bisphosphonate for the purpose of using simultaneously, separately, or sequentially as active ingredients. As a prophylactic or therapeutic composition for osteoporosis, the combination treatment of the benzamidine derivative and the bisphosphonate compound exhibits excellent inhibitory effect on osteoclast differentiation than the total effect of each individual treatment, thereby being used for the prevention or treatment of osteoporosis.

A bisphosphonate for treatment of osteoporosis is formulated with an amount of an antifoaming agent effective for reducing foaming in the stomach, leading to reduced reflux and oesophageal irritation in use and increased patient compliance.

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.

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.

A therapeutically effective amount of an antibody for a compound selected from the group consisting of PTHrp, TGFα, IL-1α, IL-1β, IL-6, Lymphotoxin, TNF, PGE; 1,25 dihydroxy vitamin D3 and an antigenic fragment thereof used in the treatment of cancer metastasis to bone and cancer cell growth in bone as well as osteolysis and symptomatic sequelae thereof. An antibody immunoreactive with parathyroid hormone-related protein (PTHrp) is particularly preferred. Antibodies with human characteristics are included in the invention for application of the invention method to human subjects. Also, the antibody can be administered in an injectable is formulation in combination with a therapeutically effective amount of a bisphosphonate or pyrophosphate having the general structure formula wherein X is a linking moiety allowing for the interconnection of the phosphonate groups, and pharmaceutically acceptable salts, hydrates and partial hydrates thereof. The antibody and bisphosphonate act synergistically in the treatment of cancer metastases to bone and symptomatic sequelae thereof and particularly as regards bone resorption.

The invention relates to a porous active artificial bone. In the porous active artificial bone, a calcium phosphate-based biological ceramic material is used as a matrix, and the porous active artificial bone comprises small pores, dense parts and directional pore channels and chelates with diphosphonate. A preparation method of the porous active artificial bone comprises the steps of preparing calcium phosphate precursor powder, compression molding a ceramic blank by using a pore-foaming agent, polyester fiber and the precursor powder, high temperature sintering into a calcium phosphate-based ceramic sintered body and forming the dense parts, the small pores distributed alternately; and immersing calcium phosphate-based ceramic sintered body in a diphosphonate solution to chelate with the diphosphonate so as to obtain the drug-loaded porous active artificial bone. The artificial bone provided by the invention has longitudinal directional pores and a porous structure suitable for osteoblast migration, propagation and growth metabolism, can slowly release small molecular drugs capable of promoting the growth of the osteoblast and inhibiting osteoclast, and is particularly suitable for the fields of treating bone defects of osteoporosis patients, dental restoration, and the like.

The present invention relates to methods and compositions for inhibiting, treating, and preventing dental diseases in human and non-human animals, particularly domesticated companion animals. More particularly, the present invention relates to the unexpected discovery that the combination of micron-sized particulate bioactive glass and a topical bisphosphonate yields a composition that is capable of treating and / or preventing dental problems such as periodontal disease, tooth decay and tooth resorption in animals, particularly small mammals such as cats.

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.

The present invention relates to a solid dispersion comprising vitamin D or a derivative thereof and a cyclodextrin; a complex formulation for the prevention or treatment of osteophorosis, which comprises said solid dispersion and a bisphosphonate; and a method for preparing said complex formulation. The complex formulation of the present invention comprising vitamin D or a derivative thereof and a bisphosphonate can maintain a constant therapeutic level of vitamin D or a derivative thereof through its improved drug stability, while enhancing the patient compliance by minimizing inconvenience and adverse effects when administered to patients. Therefore, the complex formulation of the present invention can be advantageously used for preventing and treating osteophorosis.

In a method for making bisphosphonates by reacting a carbonyl compound with a phosphorus halide, the reaction is carried out in a solvent / carrier system which is a mixture of an amine hydrochloride, phosphorous acid and optionally phosphoric acid.

Novel bisphosphonate cyclic acetal compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating bone metabolism disorders, such as abnormal calcium and phosphate metabolism.

The invention relates to a bisphosphonate (BP) compound, or a pharmaceutically acceptable salt or solvate or prodrug thereof, for use as a cytoprotectant for protecting non-cancerous cells of a subject against radiation-induced damage and / or damage induced by a chemical agent.

The invention discloses a double phosphonate medicine and a method for the isolation analysis of the ion chromatography for impurity negative ions thereof; the method includes steps of the base line mapping, the sample injection, the ion exchange, the elution and the detection and analysis of the restraining electric conduction; the method can be used to measure the contents of the double phosphonate and the impurity negative ions in double phosphonate medicines, plasmas, normal saline substrates and glucose substrates.

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.

An activated antigen-presenting cell capable of inducing an immunocompetent cell including a disease antigen-specific CD8+CTL and / or a gamma delta T cell in vivo and / or in vitro with good efficiency; a pharmaceutical comprising the activated antigen-presenting cell; a therapeutic / prophylactic method using the activated antigen-presenting cell; a method for induction of an immunocompetent cell including a disease antigen-specific CD8+CTL and / or a gamma delta T cell which is induced by using the activated antigen-presenting cell; an immunocompetent cell induced by the method; a pharmaceutical comprising the immunocompetent cell; and a therapeutic / prophylactic method using the immunocompetent cell. An antigen-presenting cell is sensitized with a disease antigen and also co-sensitized with bisphosphonate, thereby producing an increased number of a disease antigen-specific CD8+CTL and / or a gamma delta T cell at a higher ratio compared to a method without co-sensitization with bisphosphonate.