Abstract: Provided herein are methods of treating or preventing pain and/or inflammation in a subject comprising administering to the subject a transient receptor potential (TRP) ion channel inhibitor.

Abstract: The invention relates to active compound combinations, in particular a fungicidal composition, comprising Iprovalicarb (1-methylethyl-[2-methyl-1-[[[(1S)-1-(4-methylphenyl)ethyl]amino]carbonyl]propyl]-carbamate, CAS No 140923-17-7) and Fosethyl Aluminium (aluminiumethylhydrogenphosphonate, CAS No 39148-24-8 (known from FR-A-2254276) and Propineb [[(1-methyl-1,2-ethanediyl)bis[carbamodithioato]](2-)]zinc homopolymer, CAS No. 12071-83-9 (known from BE 611960). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi and/or microorganisms of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.

Abstract: The present invention provides an environmentally compatible, pesticidal composition and method for the control of insect pests. The composition includes two components. The first component is a chelating agent, a metal complex of a chelating agent, and mixtures thereof, and the second component is preferably a carrier material.

Abstract: The present invention comprises compounds, compositions thereof, and methods capable of delivering modified inositol hexaphospahte (IHP) comprising an internal pyrophosphate ring to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering IHP to the cytoplasm of the red blood cells.

Abstract: A delivery device including at least one stinging capsule and methods of use are described.

Abstract: The invention is directed to a method of treating chronic spinal mechanical pain by intravenous administration to a subject in need of chronic spinal mechanical pain relief of an effective amount of bisphosphonate.

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 a new class of compounds having ?? T cells activating properties of Formula (I), a composition comprising these compounds and methods for regulating an immune response in a subject comprising the step of administering these compounds.

Abstract: Disclosed herein are compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof, compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.

Abstract: A composition and method for the treatment of Alzheimer's disease and related amyloid plaque development and reduction of amyloid plaque, amyloidosis and amyotrophic lateral sclerosis, includes an effective amount of a compound selected from the group consisting of phytic acid, a phytate salt, an isomer or hydrolysate of phytic acid or a phytate salt, or a mixture of any combination thereof, being administered to a person in an amount from about 0.5 grams to about 18.75 grams per day.

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: Compositions comprising one or more unsaturated fatty acids and one or more nitric oxide releasing compounds, and methods for using such compositions for enhancing cognitive function, reducing or preventing a decline of social interaction, reducing or preventing age-related behavioral changes, increasing trainability, maintaining optimal brain function, facilitating learning and memory, reducing memory loss, retarding brain aging, preventing or treating strokes, and preventing or treating dementia in an animal. Preferably, the compositions are food compositions useful for enhancing cognitive function in humans and companion animals.

Abstract: A method of treating otosclerosis in a human in need thereof by administering a bisphosphonate in a defined dosing schedule. The invention demonstrates an effective response and sustained benefit in the treatment of otosclerosis. Particularly, the method involves administration of a bisphosphonate in a stepped-up dosage amount, e.g., in a dose that is at least one and a half times the recommended dose for osteoporosis. It also includes administration of a time-dependent dose of more than one bisphosphonate, specifically, alternating administration of a first bisphosphonate with a second bisphosphonate. The inventive method further includes intravenous administration of a bisphosphonate, and optionally oral administration of a bisphosphonate. The present invention further contemplates a kit for facilitating the alternating bisphosphonate dosing schedule.

Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt, wherein W, X, Y, Z, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15 and R16 are as defined in the specification. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.

Abstract: Methods of treating metastatic cancer such as metastasized tumors include administering a compound of Structure I, a tautomer of the compound, a pharmaceutically acceptable salt of the compound, a pharmaceutically acceptable salt or the tautomer, or a mixture thereof to a subject. The compound, tautomer, salt of the compound, salt of the tautomer, or mixture thereof may be used to prepare medicaments for treating metastatic cancer. The variable A has the values defined herein.

Abstract: A method for treating inflammatory diseases through an anti-inflammatory type activation of monocytes, the method includes the administration to a patient in need thereof of an effective quantity of at least one dendrimer with mono- or biphosphonic terminations.

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 invention relates to mixed calcium/sodium salt of inositol tripyrophosphate, methods of preparing and methods of use. The mixed calcium/sodium salt may be a monocalcium tetrasodium salt of inositol tripyrophosphate. Methods of use include administering the above salts in an effective amount to treat diseases caused by hypoxia or other conditions associated with inadequate function of the lungs or circulatory system, such as various types of cancer and Alzheimer's disease.

Abstract: A shelf-stable consumable composition may comprise one or more Probiotic-Mimicking Elements (PMEs) wherein the median particle size of the one or more PMEs is less than the median particle size of a probiotic from which the one or more PMEs were derived. In some embodiments, the median particle size of the one or more PMEs may be less than about 0.2 microns. In some embodiments, the PMEs may comprise at least one of peptides, fatty acids, bacteriocins, cell surface proteins, phospholipids, teichoic acids, and nucleic acids, and may be combined with one or more prebiotics, such as oligosaccharides, inulin, short-chain fructo-oligosaccharides, xylooligosaccharides, galactooligosaccharides, soyoligosaccharides, and lactulose/lactitol. Methods for preparing and using a shelf-stable consumable composition for promoting digestive health in a subject are also described.

Abstract: The present invention provides a method of promoting bone growth in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I. The present invention also provides methods for the treatment of renal disease and cancer.

Abstract: This invention relates to pyrimidine compounds of formula (I), formula (I?), and formula (I?): and pharmaceutically acceptable salts, solvates, clathrates, and prodrugs thereof, wherein R1, R2, R3, R4, R5, U, V, W, X, Y, Z, and n are defined herein. This invention also relates to compositions comprising these compounds and methods for using them. The compounds and compositions of this invention are useful to treat or prevent disorders associated with excessive bone loss, including, without limitation periodontal disease, non-malignant bone disorders (such as osteoporosis, Pagers-disease of bone, osteogenesis imperfecta, fibrous dysplasia, and primary hyperparathyroidism) estrogen deficiency, inflammatory bone loss, bone malignancy, arthritis, osteopetrosis, and certain cancer-related disorders (such as hypercalcemia of malignancy (HCM), osteolytic bone lesions of multiple myeloma and osteolytic bone metastases of breast cancer and other metastatic cancers).

Abstract: Inositol derivatives are described that are represented by the structural formula I wherein X is a radical of scyllo-inositol wherein one or more of R1, R2, R3, R4, R5, and R6 are independently alkyl, alkenyl, alkynyl, alkylene, alkenylene, alkoxy, alkenyloxy, cycloalkyl, cycloalkenyl, cycloalkoxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, sulfoxide, sulfate, sulfonyl, sulfenyl, sulfonate, sulfinyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, seleno, silyl, silyloxy, silylthio, carboxyl, carbonyl, carbamoyl, or carboxamide and the other of R1, R2, R3, R4, R5, or R6 are hydroxyl, or pharmaceutically acceptable salts thereof. The compounds, compositions comprising same and methods using same are described for use in the prevention and/or treatment of diseases characterized by abnormal protein folding or aggregation or amyloid formation, desposition, accumulation or persistence.

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: A novel form of Ibandronate sodium which is particularly suitable for pharmaceutical applications, and a process for preparing said novel form.

Abstract: The invention provides, inter alia, novel bisphosphonate compounds and methods of making and using. In embodiments, the invention provides compounds and methods in connection with research and therapeutic applications, e.g., for tumor cell growth inhibition, activation of gammadelta T cells, inhibition of farnesyldiphosphate (FPPS) and/or undecaprenyldiphosphate synthase enzymes, bone resorption diseases, cancer, immune disorders, immunotherapy, and infectious diseases. In regards to certain embodiments, a surprising advance has been the recognition that certain structural features can significantly enhance the activity of the compounds. For example, the presence of particular cationic species e.g., phosphonium, sulfonium, and arsonium moieties can contribute to desirable functional activity when positioned near a bisphosphonate moiety. In other embodiments of non-nitrogen containing bisphosphonates, terphenyl and benzyl bisphosphonate compounds and methods are provided. Further variations are also provided.

Abstract: The present invention relates to a new class of compounds having ?? T cells activating properties referred to herein as angelyl or tiglyl phosphoesters, compositions comprising any of these compounds and methods for regulating an immune response in a subject comprising the step of administering these compounds.

Abstract: The present invention relates to depot formulations comprising a poorly water soluble salt of a bisphosphonate forming together with one or more biocompatible polymers. The depot formulation may be in the form of microparticles or implants. The depot formulations are useful for the treatment and prevention of proliferative diseases including cancer.

Abstract: Provided is a solid dispersion comprising vitamin D or a derivative thereof and a cyclodextrin; a complex formulation for the prevention or treatment of osteophorosis, which includes the solid dispersion and a bisphosphonate; and a method for preparing said complex formulation. The complex formulation 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.

Abstract: The invention relates to a solid oral dosage form comprising a pharmaceutically active ingredient in combination with an enhancer which enhances the bioavailability and/or the absorption of the active ingredient. Accordingly, a solid oral dosage form comprises a drug and an enhancer wherein the enhancer is a medium chain fatty acid ester, ether or salt or a derivative of a medium chain fatty acid, which is, preferably, solid at room temperature and which has a carbon chain length of from 6 to 20 carbon atoms. Preferably, the solid oral dosage form is controlled release dosage form such as a delayed release dosage form.

Abstract: The present invention relates to mixed calcium/sodium salt of inositol tripyrophosphate, methods of preparing and methods of use. The mixed calcium/sodium salt may be a monocalcium tetrasodium salt of inositol tripyrophosphate. Methods of use include administering the above salts in an effective amount to treat diseases caused by hypoxia or other conditions associated with inadequate function of the lungs or circulatory system, such as various types of cancer and Alzheimer's disease.

Abstract: The invention relates to a foamed polymer composite product incorporating several fillers and/or fibres and several pores characterized by the fact that it shows two distinct gradients, namely a filler and/or fibre density gradient and a pore density gradient. The polymer composite according to the invention may advantageously be used in tissue engineering, bone replacement, consumer goods, transportation or in any other suitable field. The invention also includes a process for manufacturing said polymer composite.

Abstract: The present invention comprises compounds, compositions thereof, and methods capable of delivering modified inositol hexaphosphate (IHP) comprising an internal pyrophosphate ring to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering IHP to the cytoplasm of the red blood cells.

Abstract: The invention relates to a combination which comprises (a) a bisphosphonate, a platinum compound or a vasculostatic compound and (b) an epothilone derivative of formula I wherein A represents O or NRN, wherein RN is hydrogen or lower alkyl, R is hydrogen or lower alkyl and Z is O or a bond, in which the active ingredients (a) and (b) are present in each case in free form or in the form of a pharmaceutically acceptable salt and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use, in particular for the delay of progression or treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition, a commercial package or product comprising such a combination; the use of such a combination for the preparation of a medicament for the delay of progression or treatment of a proliferative disease and to a method of treatment of a warm-blooded animal.

Abstract: The present invention comprises compounds, compositions thereof, and methods capable of delivering modified inositol hexaphospahte (IHP) comprising an internal pyrophosphate ring to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering IHP to the cytoplasm of the red blood cells.

Abstract: The invention relates to a combination which comprises (a) a bisphosphonate, a platinum compound or a vasculostatic compound and (b) an epothilone derivative of formula I wherein A represents O or NRN, wherein RN is hydrogen or lower alkyl, R is hydrogen or lower alkyl, and Z is O or a bond, in which the active ingredients (a) and (b) are present in each case in free form or in the form of a pharmaceutically acceptable salt and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use, in particular for the delay of progression or treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition, a commercial package or product comprising such a combination; the use of such a combination for the preparation of a medicament for the delay of progression or treatment of a proliferative disease and to a method of treatment of a warm-blooded animal.

Abstract: The present invention relates to stable aqueous oral formulation of bisphosphonic acid or its pharmaceutically acceptable salts. More particularly, the present invention relates to stable aqueous oral formulation of alendronate sodium. The present invention also relates to a process for the preparation of stable aqueous oral formulation of alendronate sodium.

Abstract: The present invention relates to novel dihydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.

Abstract: The present invention provides novel bisphosphonate conjugates, pharmaceutical compositions comprising bisphosphonate conjugates and methods of using such analogs in the treatment of bone cancer, bone-related diseases, bone infection, bone inflammation, and diseases of the soft tissues surrounding bones.

Abstract: Methods of using compatible solutes cyclic 2,3-diphosphoglycerate (cDPG), 1,-di-glyccrol phosphate (DGP), firoin and firoin-A, and/or derivatives of these compounds or combinations thereof, for treating skin conditions such as dermatoses and age spots. The methods include the application to the skin of a cosmetic and/or dermatological preparation containing the compatible solutes.

Abstract: The present invention provides a chemical compound or a salt thereof having the chemical formula of: wherein said R is H or citrate and wherein at least one R is citrate. The salt of the chemical compound is the Na+, K+, Mg2+, or Ca2+ salt of said chemical compound. The chemical compound is a chelator which chelates sodium, potassium or lithium, magnesium, calcium, copper, iron, lead, zinc, aluminum, mercury, cadmium, or chromium. It is also be used as an artery plaque dissolver and/or to treat age-related degenerative disorders, such as Alzheimer's disease. The present invention also provides a method for producing the phytic citrate compound and/or its salt.

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 disclosure provides methods and compositions using Syk inhibitory compounds for treating degenerative bone disorders and as prophylactic treatment to prevent bone loss. These treatments may reduce the fracture risk associated with bone loss and compromised bone strength.

Abstract: The present invention relates to the use of myo-inositol hexaphosphate or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the prevention or treatment of a disease associated with the dissolution of crystals of calcium salts, in particular osteoporosis. These compounds may be utilized in the manufacture of functional foods, dietetic supplements, vitamin supplements, nutritional supplements, food supplements, or phytotherapeutic products having properties of inhibition of dissolution of crystals of calcium salts.

Abstract: The present invention provides a chemical compound or a salt thereof having the chemical formula of: wherein said R is H or citrate and wherein at least one R is citrate. The salt of the chemical compound is the Na+, K+, Mg2+, or Ca2+ salt of said chemical compound. The chemical compound is a chelator which chelates sodium, potassium or lithium, magnesium, calcium, copper, iron, lead, zinc, aluminum, mercury, cadmium, or chromium. It is also be used as an artery plaque dissolver and/or to treat age-related degenerative disorders, such as Alzheimer's disease. The present invention also provides a method for producing the phytic citrate compound and/or its salt.

Abstract: A method of treating otosclerosis in a human in need thereof by administering a bisphosphonate in a defined dosing schedule. The invention demonstrates an effective response and sustained benefit in the treatment of otosclerosis. Particularly, the method involves administration of a bisphosphonate in a stepped-up dosage amount, e.g., in a dose that is at least one and a half times the recommended dose for osteoporosis. It also includes administration of a time-dependent dose of more than one bisphosphonate, specifically, alternating administration of a first bisphosphonate with a second bisphosphonate. The inventive method further includes intravenous administration of a bisphosphonate, and optionally oral administration of a bisphosponate.

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: This invention discloses a process for producing a polymer by controlled polymerization which comprises polymerizing at least one monomer in the presence of a free radical control agent of the structural formula: (Z)-(R1)n, wherein n represents an integer from 1 to about 6; wherein Z represents an aromatic or aliphatic moiety containing from 1 to about 20 carbon atoms; wherein R1 represents a moiety of the structural formula: wherein R2 represents a moiety selected from the group consisting of alkyl groups, alkenyl groups, alkynyl groups, aryl groups, heteroaryl groups, and alkaryl groups; wherein the alky groups, alkenyl groups, alkynyl groups, aryl groups, heteroaryl groups, and alkaryl groups can be substituted, unsubstituted, linear, branched or cyclic; and wherein Ar represents a p-alkoxyphenyl group having an alkoxy moiety that contains from 1 to 8 carbon atoms.

Abstract: The invention provides a method of inhibiting cell death in a mammal. The method comprises administering to a mammal an effective amount of a composition comprising a cell protection factor covalently linked to a bone targeting agent via a linkage that is cleaved under physiological conditions, whereby the cell protection factor is released from the bone targeting agent in vivo to inhibit cell death. The invention further provides a compound comprising a cell protection factor covalently attached to a bone targeting agent via a linker that is cleaved under physiological conditions.

Abstract: 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.

Abstract: This invention discloses a process for producing a polymer by controlled polymerization which comprises polymerizing at least one monomer in the presence of a free radical control agent of the structural formula: (Z)-(R1)n, wherein n represents an integer from 1 to about 6; wherein Z represents an aromatic or aliphatic moiety containing from 1 to about 20 carbon atoms; wherein R1 represents a moiety of the structural formula: wherein R2 represents a moiety selected from the group consisting of alkyl groups, alkenyl groups, alkynyl groups, aryl groups, heteroaryl groups, and alkaryl groups; wherein the alky groups, alkenyl groups, alkynyl groups, aryl groups, heteroaryl groups, and alkaryl groups can be substituted, unsubstituted, linear, branched or cyclic; and wherein Ar represents a p-alkoxyphenyl group having an alkoxy moiety that contains from 1 to 8 carbon atoms.