51 results about "Hypercalcinemia" patented technology

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.

The present invention relates to novel, non-secosteroidal, hydroxyl substituted, carbon-linked diaryl compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1?,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.

The present invention provides a method for treating diseases caused by either an excess or diminution of Vitamin D3. It provides pharmaceutical compositions for the treatment of such diseases and the methods by which these compositions are to be used. Also provided are methods for testing the activity of both 24(OH)ase and CCAATT / Enhancer Binding Protein β (C / EBPβ), as well as, for testing the effect of a compound on 24(OH)ase and C / EBPB activity activity. In particular embodiments, a method is provided for reducing the risk of hypercalcemia when administering 1,25(OH)2D3 or its analogs for the treatment of vitamin D diseases. Methods for both enhancing and diminishing 24(OH)ase activity are also provided.

Disclosed are methods of inhibiting bone resorption and / or promoting bone formation using GLP-2 and related Compounds. The invention has a wide spectrum of important uses including hyperparathyroidism, Paget's disease, hypercalcemia of malignancy, osteolytic lesions produced by bone metastasis, bone loss due to immobilisation or sex hormone deficiency, osteomalacia, hyperostosis and osteopetrosis.

The pharmaceutical composition comprising the compound of the invention having 8-azaprostaglandin skeleton represented by formula (I) (wherein, all the symbols have the same meanings as that of the specification.) a salt thereof, a solvate thereof or a cyclodextrin clathrate thereof, or a prodrug thereof and them as active ingredient have EP4 agonistic action and thus are considered useful for the prevention and / or treatment of immunological diseases, asthma, neuronal cell death, arthritis, lung failure, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, liver damage, acute hepatitis, nephritis, renal insufficiency, hypertension, myocardial ischemia, systemic inflammatory response syndrome, sepsis, hemophagous syndrome, macrophage activation syndrome, Still's disease, Kawasaki disease, burn, systemic granulomatosis, ulcerative colitis, Crohn's disease, hypercytokinemia at dialysis, multiple organ failure, shock and glaucoma, etc. Furthermore, the compounds also have an action of accelerating bone formation, so it is expected to be useful for the prevention and / or treatment of diseases associated with loss in bone mass, for example, primary osteoporosis, secondary osteoporosis, bone metastasis of cancer, hypercalcemia, Paget's disease, bone loss, osteonecrosis, bone formation after bone operation, alternative treatment for bone grafting.

Provided are compositions and methods for the identification and treatment of ovarian cancers, such as small cell ovarian cancers, in particular small cell carcinoma of the ovary, hypercalcemic type (SCCOHT), which ovarian cancers are characterized by reduced SMARCA4 gene expression and / or protein function and, as a consequence, are sensitive to growth and / or survival inhibition by one or more compounds that restore SMARCA4 gene expression and / or protein function.

Novel pharmaceutical gallium compositions, including gallium complexes having increased oral bioavailability relative to uncomplexed gallium salts are disclosed. Such compositions are useful in the treatment of conditions and diseases in which inhibition of abnormally increased calcium resorption is desired, including cancer, hypercalcemia, osteoporosis, osteopenia and Paget's disease. Methods for preparation and treatment are also provided.

The present invention is directed to novel pyrido[4,3-d]pyrimidin-4(3H)-one derivatives and pharmaceutically acceptable salts thereof of structural formula Iwherein the variables R1, R2, R3, R4 and R5 are as described herein. Also provided are pharmaceutical compositions comprising the compounds of formula I as well as methods of treatment employing compounds of formula I to treat a disease or disorder characterized by abnormal bone or mineral homeostasis such as hypoparathyroidism, osteoporosis, osteopenia, periodontal disease, Paget's disease, bone fracture, osteoarthritis, rheumatoid arthritis, and humoral hypercalcemia of malignancy.

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.

Compounds expressed by the following general formula (1), [wherein, R01 and R02 are each independently a hydrogen atom or a protecting group for a hydroxyl group; Z is one out of the following formulae (1-1) to (1-5)]. The compounds can be used as active ingredients of treating agents for inflammatory respiratory diseases, malignant tumors, rheumatoid arthritis, osteoporosis, diabetes mellitus, hypertension, alopecia, acne, psoriasis, dermatitis, hypercalcemia, hypoparathyroidism and metabolic disorder of cartilage.

To provide a compound having an excellent cysteine protease inhibitory effect, and to provide a drug for treatment or prevention of the disease selected from the group consisting of osteoporosis, osteoarthritis, chronic rheumatoid arthritis, Paget's disease of bone, hypercalcemia, bone metastasis of cancer, and ostealgia. A compound represented by formula (1) or a pharmaceutically acceptable salt thereof, or a drug or pharmaceutical composition containing the same as an effective component.

Compounds expressed by the following general formula (1), [wherein, R01 and R02 are each independently a hydrogen atom or a protecting group for a hydroxyl group; Z is one out of the following formulae (1-1), (1-2), (1-3), (1-4) and (1-5)]. The compounds can be used as active ingredients of treating agents for inflammatory respiratory diseases, malignant tumors, rheumatoid arthritis, osteoporosis, diabetes mellitus, hypertension, alopecia, acne, psoriasis, dermatitis, hypercalcemia, hypoparathyroidism and metabolic disorder of cartilage.

Disclosed is a tape-type transdermally absorptive preparation which has excellent transdermal absorption, high safety and high usability, and which is suitable for the treatment of a disorder of bone / calcium metabolism, such as osteoporosis, osseous Paget's disease and hypercalcemia associated with a malignant tumor. Specifically disclosed is a tape-type transdermally absorptive preparation characterized by containing a bisphosphonate or a derivative thereof. Preferably, the tape-type transdermally absorptive preparation comprises a support sheet and an adhesive layer laminated on one surface of the support sheet, wherein the adhesive sheet comprises: 100 parts by weight of an acrylic copolymer which comprises 50 to 88 wt% of acrylic acid, 8 to 40 wt% of 2-ethylhexyl acrylate and 1 to 42 wt% of a polar monomer (excluding acrylic acid); 150 to 600 parts by weight of a polyhydric alcohol; and a pharmaceutically effective amount of a bisphosphonate.

The present invention relates to an agent for increasing BMD characterized by use of a cathepsin K inhibitor as a bone resorption inhibitor in combination with a type of PTH as a bone formation stimulator. This agent for increasing BMD is useful for the treatment of osteoporosis, bone fracture, arthritis, rheumatoid arthritis, osteoarthritis, hypercalcemia, osteometastasis of carcinoma, periodontal disease, bone Paget's disease and other bone metabolic diseases. For example, as the cathepsin K inhibitor, there can be mentioned a compound of formula (W) and a salt thereof, etc.

A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof,wherein: one of R1 and R2 is H, and the other is selected from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; orR1 and R2 are both H;one of R3 and R4 is H, and the other is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; orR3 and R4 are joined together with the adjacent backbone carbon atom to form a spiro-C5-C6 cycloalkyl group;R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl; orR6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached;R8 is C1-8-alkyl or C3-8-cycloalkyl;R9 is a para-substituted 6-membered monocyclic aryl or heteroaryl ring which includes up to five 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 present disclosure provides a method of treating malignant rhabdoid tumor in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of an enhancer of zeste homolog 2 (EZH2) inhibitor. In certain embodiments of the method, the malignant rhabdoid tumor is small cell carcinoma of the ovary with hypercalcemia (SCCOHT), and the EZH2 inhibitor is tazemetostat (also known as Tazemetostat).

The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof,wherein:X is CH or N; andR4 is optionally substituted C3-8 alkyl or optionally substituted C3-8 cycloalkyl.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 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.

The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof,wherein:X is CH or N;one of R1 and R2 is H, and the other is selected from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8;R3 is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl;R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl;R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl, or R6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; andR8 is C1-8-alkyl or C3-8-cycloalkyl.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.

A compound represented by the following Formula (1) that is effective for the treatment of Paget's disease of bone or hypercalcemia or a medically acceptable solvate thereof; [wherein R1 refers to hydrogen atom, C1-C6 alkyl group optionally substituted with hydrogen group or C1-C6 alkoxy group optionally substituted with hydroxyl group, R2a and R2b refer to hydrogen atom, C1-C10 alkyl group optionally substituted with hydroxyl group, C6-C10 aryl group optionally substituted with hydroxyl group or C7-C12 aralkyl group optionally substituted with a hydroxyl group, or are combined to represent ethylene group. However, a compound in which R1 is a hydrogen atom or a methyl group and R2a and R2b are hydrogen atoms is excluded].