87 results about "Metabolic bone disease" patented technology

The invention relates to pharmaceutical compositions suitable for treating or curing clinical complications mediated by endotoxin, including sepsis. The compositions contain components suitable for detoxifying endotoxin rendering it less deleterious to mammals such as humans, in particular to patients with reduced host-defence resistance. The invention also relates to pharmaceutical compositions suitable for stimulating bone formation, e.g. for mending broken bone or for prophylaxis or therapy of metabolic bone diseases such as osteoporosis and osteomalacia and pharmaceutical compositions for decreasing or inhibiting undesired bone formation. The pharmaceutical compositions according to the invention are directed at modulating phosphatase activity in vivo.

Osteoporosis and the like metabolic bone diseases have a high frequency of causing lumbago and the like pains and bone fracture, due to lowering of the bone strength caused by the reduction of bone mass. Accordingly, great concern has been directed toward the creation of a drug which can increase the bone mass and bone strength by controlling the whole bone metabolism. The pharmaceutical composition or combination product of the invention comprising a non-living body-derived non-peptide osteoblast differentiation promoting compound and a bisphosphonate having a bone resorption inhibitory action is useful as a bone mass increasing inducer which can increase the bone mass and / or bone strength by controlling the bone metabolism.

The present invention relates to a pharmaceutical composition for the treatment of metabolic bone disease and the method of preparation thereof, and more particularly, to an improved pharmaceutical composition for the therapeutic treatment of metabolic disease and the method of preparation thereof, wherein said composition is prepared as a composite pharmaceutical agent which comprises calcitriol; which reduces the rate of spine fractures and increases bone density; alendronate, a bone resorption inhibitor, as two main active ingredients in an optimal mixing ratio to exert the greatest synergistic therapeutic effect; and adequate amount of other additives such as a resorption fortifier of alendronate. Thereof, the pharmaceutical composition according to the present invention can inhibit hypercalcemia caused when administered by calcitriol alone, compensate the inhibitory activity of bone remodeling caused by alendronate due to the presence of calcitriol, and improve drug compliance associated with the usual difficulty in administration as well as a side effect in esophagus, thus effectively preventing the occurence of osteoporosis.

Methods and formulations for the administration of a bone morphogenetic protein (BMP) anywhere along the alimentary canal of an individual are described for use in treating osteoporosis or other metabolic bone diseases.

This invention discloses (20S)-1α-hydroxy-2α-methyl-19-nor-vitamin D3 and (20S)-1α-hydroxy-2β-methyl-19-nor-vitamin D3 and pharmaceutical uses therefor. These compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. These compounds also have very significant calcemic activity and therefore may be used to treat immune disorders in humans as well as metabolic bone diseases such as osteoporosis.

This invention discloses (20S)-1α-hydroxy-2α-methyl-19-nor-vitamin D3 and (20S)-1α-hydroxy-2β-methyl-19-nor-vitamin D3 and pharmaceutical uses therefor. These compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. These compounds also have very significant calcemic activity and therefore may be used to treat immune disorders in humans as well as metabolic bone diseases such as osteoporosis.

As a result of an effort made by us for the purpose of developing a therapeutic agent having a bone formation-stimulating effect by promoting the functions of osteoblasts, the present inventors discovered that a certain nitrogen-containing heterocyclic compound exhibits a potent bone formation-stimulating effect on the osteoblast and thus can serve as an excellent prophylactic or therapeutic agent against a metabolic bone disease, whereby establishing the present invention. Thus, the present invention provides a 3,6-disubstituted 1,2,4-triazolo[4,3-b]pyridazine compound or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition comprising such a compound and a pharmaceutically acceptable carrier, especially a bone-forming agent.

The invention discloses a tanshinol lipidosome bone-targeting pharmaceutical preparation and a preparation method thereof. The preparation is prepared by jointing and carrying out surface modification on a lipidosome microparticle containing a tanshinol medicine molecule by using a bone-targeting jointer. The preparation method comprises the steps of jointing a bisphosphonate molecule with bone-targeting ability on one end of a polyethylene glycol molecule through synthetic reaction, and jointing a cholesterol molecule serving as a lipidosome raw material on the other end of the polyethylene glycol molecule through synthetic reaction to prepare a jointer with bone-targeting ability, namely bisphosphonate-polyethylene glycol-cholesterol (BP-PEG-CHOL); and then, preparing a lipidosome provided with the bone-targeting jointer on the surface from phospholipid, cholesterol and the bone-targeting jointer which serve as raw materials, adding tanshinol, and containing the tanshinol into the lipidosome to prepare the tanshinol lipidosome bone-targeting preparation. The preparation disclosed by the invention has the bone-targeting ability and can be used for remarkably increasing the concentration of medicines in a bone tissue, improving the curative effect and preventing and treating systemic metabolic bone diseases, osteoporosis and bone fracture.

The present invention relates to compounds of formula (1), and pharmaceutically acceptable salts thereof, A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof (I), wherein: one of R1 and R2 is H, and the other is selected from F and Cl, or R1 and R2 are both F; R3 is selected from cyclopentyl and cyclohexyl; R4 is an optionally substituted 5- or 6-membered monocyclic or an 8- to 10-membered bicyclic aryl or heteroaryl ring which includes up to four heteroatoms. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.

The invention is a treatment for increasing the bone mass or preventing bone loss in an individual afflicted with a bone disease which includes administering to the individual a morphogen in a therapeutically effective amount so as to maintain or stimulate bone formation.

A composition containing 1,4-dihydroxy-2-naphthoic acid at a high concentration is obtained by intracellularly and extracellularly producing 1,4-dihydroxy-2-naphthoic acid using a bacterium belonging to the genus Propionibacterium and collecting it. This composition is efficacious in improving intestinal flora, alleviating abdominal ailments in association with the intake of milk, and preventing metabolic bone diseases.

The present invention concerns methods for diagnosis and treatment of metabolic bone diseases and disorders using a novel member of the tumor necrosis factor (TNF) family of cytokines. In particular the invention provides methods of using the Endokine alpha protein and / or homomultimeric and / or heteromultimeric polypeptide complexes containing Endokine alpha, in the diagnosis, prognosis and treatment of metabolic bone diseases and disorders. Also provided by the invention are methods of using the Endokine alpha protein and / or homomultimeric and / or heteromultimeric polypeptide complexes containing Endokine alpha, in the diagnosis, prognosis and treatment of diseases and / or disorders associated with aberrant osteoclast development and / or activity. The present invention also provides isolated polynucleotides encoding polypeptides of the invention, antibodies thereto, and agonists and antagonists thereof, for use in the diagnosis, prognosis and treatment of metabolic bone diseases and disorders.

Disclosed is a pharmaceutical composition containing an extract of Schisandrae Fructus for preventing and treating metabolic bone diseases, oxidative stress-induced diseases and inflammatory diseases.The composition of the present invention contains the extract of Schisandrae Fructus showing increasing action on bone mineralization and protein biosynthesis, antioxidant action and anti-inflammation and analgesic actions, and can be used as a direct therapeutic agent or a therapeutic aide for metabolic bone diseases, oxidative stress-induced diseases and inflammatory diseases.A therapeutic agent of the present invention is of a natural medicament containing the extract of Schisandrae Fructus, that is, a kind of medicinal plants, and shows the above described actions without any adverse side effect shown in conventional synthetic medicaments, thereby preferably replacing the conventional synthetic medicaments.

Disclosed is a pharmaceutical composition for treating and preventing metabolic bone diseases, comprising a pharmaceutically effective amount of N-acylated lysophosphatidylcholine compound represented by Formula 1 (R is a saturated or unsaturated fatty acid of C14 to C20, and R′ is methoxycarbonyl or hydroxylmethyl group), and a pharmaceutically acceptable carrier. Also, the present invention discloses a method of preparing an N-acylated lysophosphatidylcholine compound represented by Formula 1, from serine. [Formula 1]

Novel remedies for metabolic bone diseases containing an IL-18 inhibitor as the active ingredient. These remedies exert a therapeutic effect by inhibiting the effect of overexpressed IL-18 which closely relates to the onset of osteoporosis. They are also useful as remedies for other metabolic bone diseases.

The invention discloses a novel adenine bisphosphonate, a preparation method and the application in the preparation of pharmaceutical preparations for the treatment of the metabolic bone diseases. A compound is (2-(6-amino-purine-9-yl)-1-hydroxy-phosphono-ethyl)phosphonate and 3-((6-amino-purine-9-yl)-1-hydroxy-phosphono-propyl)phosphonate. The compound can be used for the treatment of hypercalcemia, bone pains and other metabolic bone diseases caused by osteoporosis, osteitis deformans and bone metastasis of the malignant tumor, and the invention has an anti-cancer effect at the same time.

The present invention relates to a pharmaceutical composition for preventing and / or treating metabolic bone disease. The pharmaceutical composition comprises an effective dose of an N-acyl lysophosphatidylcholine compound (chemical formula 1) and a carrier thereof that can be used in pharmaceutical preparations . Furthermore, the present invention relates to a preparation method for preparing the N-acyl lysophosphatidylcholine compound of Chemical Formula 1 from serine.

The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.

A composition comprising bone marrow cells (BMC) and demineralized bone matrix (DBM) and / or mineralized bone matrix (MBM) and optionally comprising bone morphogenetic protein / s (BMP) and / or other active agents, particularly for use in the transplantation of mesenchymal progenitor cells into a joint and / or a cranio-facial maxillary bone, for restoring and / or enhancing the formation of a new hyaline cartilage and subchondral bone structure. The composition of the invention and method of treatment employing the same may be used for the treatment of hereditary or acquired bone disorders, hereditary or acquired cartilage disorders, malignant bone or cartilage disorders, metabolic bone diseases, bone infections, conditions involving bone or cartilage deformities and Paget's disease. The composition and method may further be used for the correction of complex fractures, bone replacement and formation of new bone in plastic or sexual surgery, for support of implants of joints, cranio-facial-maxillary bones, or other musculoskeletal implants, including artificial implants. The method of the invention may further be used for treating damaged joints or degenerative arthropathy associated with malformation and / or dysfunction of cartilage and / or subchondral bone. A kit is provided for performing transplantation into a joint or a cranio-facial-maxillary bone of a mammal of the composition of the invention.

Disclosed is a bone formation enhancing agent comprising an RANKL-acting molecule which can enhance the differentiation, maturation or calcification of an osteoblast or a cell capable of being differentiated into an osteoblast. Specifically disclosed is a pharmaceutical composition for the treatment or prevention of a metabolic bone disease accompanied by the decrease in bone mass, which comprises, as an active ingredient, a compound which can act on an RANKL located on an osteoblast or a cell capable of being differentiated into an osteoblast to accelerate the differentiation, proliferation,maturation or calcification of the osteoblast or the cell capable of being differentiated into an osteoblast.

Described are medicaments and methods of treating or preventing metabolic bone diseases, such as Critical Illness Related Metabolic Bone Disease or of critical illness induced Osteopenia secondary to ICU Admission by sufficient autophagy inducing compound to inhibit or suppress critical illness enhanced osteoclastogenesis or increased osteoclast differentiation. The methods include administering of an autophagy activating compound to a mammal to: treat or prevent a bone degenerative disorder; slow bone deterioration; restore lost bone; maintain bone mass and / or bone quality or inhibit bone resorption in particularly by inhibiting or reducing a process by which osteoclasts break down bone and release the minerals resulting in a transfer of calcium from bone fluid to the blood. Also described are methods for administering the autophagy activating compound to treat a bone disorder of hyperresorption of bone and / or enhanced activation of osteoclasts.

This invention relates to: a method for differentiating osteoclast precursor cells (preosteoclasts) into osteoclasts, which comprises culturing the preosteoclasts in the absence of accessory cells; a method for isolating preosteoclasts, which comprises culturing peripheral blood or joint fluid in the absence of cytokine for 1 to 3 weeks; an preosteoclasts, which is obtainable by the above method; a method for differentiating the preosteoclasts obtained by the above method into osteoclasts, which comprises culturing the preosteoclasts in the absence of accessory cell; an osteoclast, which is obtainable by the above method; a method for screening agents for treating metabolic bone diseases, which comprises using the preosteoclasts or the osteoclasts as described above; and agents for treating metabolic bone diseases, which is obtainable by the above screening method.

The invention relates to the technical field of calcitriol, in particular to an oral solution containing calcitriol and a preparation method of the oral solution, and the oral solution containing calcitriol comprises the following components in parts by weight: 0.290-0.305 part of calcitriol; 29.7 to 30.3 parts of butyl hydroxy anisole; 29.8 to 30.2 parts of butylated hydroxytoluene (BHM); and 299987 to 300012 parts of medium chain triglycerides. The preparation method of the oral solution containing calcitriol comprises the following steps: S100, weighing: turning on a yellow light lamp in a weighing room, weighing calcitriol, medium chain triglyceride, butylated hydroxyanisole and butylated hydroxytoluene according to parts by weight, and carrying out double-person rechecking; compared with the prior art, the oral solution containing calcitriol has the following beneficial effects that the oral solution containing calcitriol can make up the blank in the field of treating secondary hyperparathyroidism of patients with moderate to severe chronic renal failure before dialysis and follow-up metabolic bone diseases and hypoparathyroidism in domestic children medication, and the clinical requirements are met.

The present invention relates to a Eupatorium spp. extract having anti-obesity effects as a result of decreasing adipocytes and increasing osteoblasts, as well as the effects of preventing bone disease or fractures by increasing osteoblasts and of preventing osteoporosis by decreasing adipocytes and increasing osteoblasts by the same proportion in mesenchymal stem cells. DCM fraction layers of a Eupatorium spp. stem extract collected on a monthly basis and Eupatorium spp. stem extract collected only in September may inhibit the activity of PPARγ, AP2, CD36, adiponectin C / EBPα, and LPL, which serve as significant factors for adipocyte differentiation in C3H10T1 / 2 cells and primary mesenchymal stem cells, which are pluripotent stem cell lines, and may increase the activity of ALP, osterix, CO1I and RUNX2, which serve as significant factors for osteoblast differentiation. The Eupatorium spp. extract of the present invention exhibits the effects of increasing bone mineral density (BMD) and decreasing adipocytes in bone marrow in an osteoporosis animal model experiment involving an ovariectomy, and therefore may be used as a useful material for preventing and treating osteoporosis.

This invention relates to: a method for differentiating osteoclast precursor cells (preosteoclasts) into osteoclasts, which comprises culturing the preosteoclasts in the absence of accessory cells; a method for isolating preosteoclasts, which comprises culturing peripheral blood or joint fluid in the absence of cytokine for 1 to 3 weeks; an preosteoclasts, which is obtainable by the above method; a method for differentiating the preosteoclasts obtained by the above method into osteoclasts, which comprises culturing the preosteoclasts in the absence of accessory cell; an osteoclast, which is obtainable by the above method; a method for screening agents for treating metabolic bone diseases, which comprises using the preosteoclasts or the osteoclasts as described above; and agents for treating metabolic bone diseases, which is obtainable by the above screening method.

Provided is a compound showing a bone formation promoting action (and / or bone resorption suppressive action). A compound of the formula (I) or a pharmacologically acceptable salt:[wherein each substituent is as defined in the DESCRIPTION], has low toxicity, shows good pharmacokinetics, has an action to promote bone formation, and is useful for the prophylaxis or To treatment of metabolic bone diseases (osteoporosis, fibrous osteitis (hyperparathyroidism), osteomalacia, Paget's disease that influences the systemic bone metabolism parameter etc.) associated with a decrease in the bone formation ability as compared to the bone resorption capacity.