Abstract: Controlled release compositions of matter are disclosed comprising complexes for treating a population of one or more aquatic organisms in a column of water. The complexes comprise at least one system wherein the system comprises at least one bioactive agent as a component selected for treating a population of aquatic organisms, at least one carrier component, and at least one coating component for regulating the controlled release rate and release profile of the bioactive agent in water or at least one bioactive agent and one joint-function component that can serve as both a carrier and coating to regulate the controlled release rate and release profile of the bioactive agent in water, with or without optional binder components and/or additional formulation materials. The components are selected to sink or float so that the complexes will permeate and/or remain in any planar or volumetric segment of a water column for a period of time that is sufficient to effectively treat a population of aquatic organisms.

Abstract: The invention is concerned with a pharmaceutical preparation for subcutaneous, parenteral administration, which contains bisphosphonic acids or their salts as the active substance, as well as the production of this preparation. By means of the preparation in accordance with the invention it is possible to administer locally relatively high concentrations of bisphosphonates without the occurrence of incompatibilities.

Abstract: The present invention relates to pharmaceutical treatment kits and to methods for administering a pharmaceutical active.

Abstract: An effervescent formulation of alendronate contains an acid source, a carbonate source, a binder, a lubricant and optionally, flavoring agents, colorants and sweeteners.

Abstract: The present invention is directed to particular bisphosphonate compounds, and in particular, to bisphosphonate conjugates that are useful in the treatment of soft tissues surrounding bone and bone-related diseases, such as bone cancer and osteoporosis.

Abstract: The present invention relates to novel pharmaceutical tablets useful for administering pharmaceutical active ingredients, such as bisphosphonates. These tablets have improved surface properties which can aid esophageal transit, thereby reducing the potential for adverse gesture intestinal effects. The present invention also relates to processes for making said novel pharmaceutical tablets.

Abstract: This invention relates to methods, pharmaceutical compositions and kits useful in promoting bone formation and/or preventing bone loss and/or treating atherosclerosis. The compositions are comprised of a polyphosphonate as a first active component and a statin as a second active component and a pharmaceutically acceptable vehicle, carrier or diluent.

Abstract: Methods are disclosed for treatment of patients suffering from accumulation of a metabolite within macrophages, such as in lysosomal storage diseases. The methods comprise treating the patient with a macrophage depleting amount of a bisphosphonate compound, such that apoptosis of macrophages is induced and the metabolite is released into circulation so that the metabolites may be eliminated from the patient. The methods may further include administration of a gene therapy vector for the treatment of lysosomal storage diseases.

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: Disclosed are methods for inhibiting bone resorption in mammals while minimizing the occurrence of or potential for adverse gastrointestinal effects. Also disclosed are pharmaceutical compositions and kits for carrying out the therapeutic methods disclosed herein.

Abstract: The present invention relates to methods for inhibiting bone resorption in a mammal comprising administering to a mammal in need thereof a therapeutically effective amount of an EP4 receptor subtype antagonist.

Abstract: The present invention relates to a parenteral composition comprising a bisphosphonic acid or a pharmaceutically acceptable salt thereof (bisphosphonate) as active component and a pharmaceutically acceptable chelating agent, processes of the preparation of this composition, and methods of their use in the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, hypercalcemia of malignancy, and metabolic bone disease. The compositions are especially useful for improving the local tolerance of the active component when administered parenterally.

Abstract: Pharmaceutical compositions of bisphosphonic acids, and salts thereof, are prepared by wet granulation tablet formulation. These pharmaceutical compositions are useful in the treatment of disturbances involving calcium or phosphate metabolism, in particular, the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, malignant hypercalcemia, and metastatic bone disease. These compositions are prepared without the addition of binder; instead, the drug itself acts as a binder.

Abstract: The inhibition of natural bone formation experienced in the prophylaxis and/or treatment of bone resorption disease with a bisphosphonic acid or a pharmaceutically acceptable salt thereof is overcome by the concommitant administration of an agent that binds to the androgen receptor.

Abstract: The present invention relates to the preparation and biological activity of 3-deoxy-D-myo-inositol ether lipid analogs as inhibitors of phosphatidylinositol-3-kinase signaling and cancer cell growth. The compounds of the present invention are useful as anti-tumor agents which effectively inhibit the growth of mammalian cells.

Abstract: Inositol derivatives, compositions comprising inositol derivatives, and methods for using compositions comprising inositol derivatives as agents for inhibiting superoxide anion production are described. The inositol derivatives are obtainable via conventional organic synthesis. The inositol derivatives inhibit superoxide anion produced by neutrophils and macrophages which cause tissue damage.

Abstract: The present invention relates to conjugates of 3-carboxy-4,4′-dihydroxyphosphorylbutenoic acids with alkylating agents, derivatives are endowed with marked antitumor activity, especially against multiple myeloma. The present invention relates as well to a process for the preparation thereof and to pharmaceutical compositions containing them.

Abstract: A low volatile organic compound co-solvent system is disclosed for preparing emulsion concentrates of low melting organophosphorous insecticides wherein the bioefficacy of the insecticide active is significantly enhanced. The co-solvent system comprises a water-soluble ethoxylated fatty acid/rosin acid-nonionic surfactant composition.

Abstract: Pharmaceutical compositions of bisphosphonic acids, and salts thereof, are prepared by direct compression/dry mix tablet formulation. These pharmaceutical compositions are useful in the treatment of disturbances involving calcium or phosphate metabolism, in particular, the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, malignant hypercalcemia, and metastatic bone disease.

Abstract: The present invention relates to a method of treating angiogenesis in tumor tissue, such as glioma and glioblastama tissue. The method comprises administering to a mammal, including, man an effective amount at an isomer of inositol trisphosphate, such as D-myo-inositol-1,2,6-trisphosphate, or a pharmaceutically acceptable salt thereof.

Abstract: This invention relates to prostaglandin-bisphosphonate conjugates. These conjugates are effective for treating or preventing bone diseases such as osteoporosis. These conjugates simultaneously deliver a prostaglandin agent for increasing bone formation and a bisphosphonate agent for inhibiting bone resorption.

Abstract: Tissue-destructive conditions related to excess protemase activity in a biological system are treated or prevented by administering to the system a composition which combines a tetracycline and a bisphosphonate in synergistic proteinase inhibiting amounts.

Abstract: A method is provided by blocking or preventing the prenylation of CAAX box containing proteins including ras oncogene products thereby preventing and/or treating ras-related tumors which includes the step of administering a therapeutically effective amount of a protein-prenyl transferase inhibitor.

Abstract: The invention relates to a method of treating the navicular disease in horses, which comprises treating the navicular disease in horses with an effective amount of at least one compound of formula (I), ##STR1## wherein R.sub.1 is hydrogen, hydroxy, amino or halogen, and R.sub.2 is hydrogen, halogen or a radical which is bound through C, N, S or O, or of a C.sub.1 -C.sub.4 tetraalkyl ester thereof, each in the free form or in the form of the salt and/or in the hydrate form; to a compound of formula (I) for use in a method of treating the navicular disease, to a composition for use in a method of treating the navicular disease, which comprises one or more than one compound of formula (I), as well as to the use of a compound of formula (I) for the preparation of a veterinary composition for treating the navicular disease.

Abstract: To reduce the toxic effect of carboplatin, particularly myelosuppression and emesis, a dithioether having the formula R.sub.1 -(CH.sub.2).sub.n --S--S--(CH.sub.2).sub.m --R.sub.2 (I) wherein:each of R.sub.1 and R.sub.2 individually is SO.sub.3 H or PO.sub.3 H.sub.2 ; andeach of m and n is individually 1, 2, 3 or 4;or a pharmaceutically acceptable salt thereof, preferably disodium 2,2'-dithiobis(ethane sulfonate) (dimesna), is administered in combination with carboplatin to a patient, at substantially the same time or sequentially, whereby the dithioether and the carboplatin become co-present in the blood of the patient. Compositions comprising carboplatin and the dithioether are included in the invention.

Abstract: The present invention is directed to presqualene diphosphate (PSDP) analogs having an active region of natural PSDP and a metabolic transformation region resistant to rapid intracellular inactivation in vivo. For example, PSDP and its stable analogs can inhibit neutrophil signal transduction events in cellular activation that result in the generation of active oxygen species, regulation of leukocyte adherence, both homotypic (leukocyte-leukocyte) or heterotypic adherence with leukocytes and epithelial cells of mucosal origin or endothelial cells of vascular origin. These analogs can also be used to regulate leukocyte-dependent tissue injury.

Abstract: Tissue-destructive conditions related to excess proteinase activity in a biological system are treated or prevented by administering to the system a composition which combines a tetracycline and a bisphosphonate in synergistic proteinase inhibiting amounts.

Abstract: Use of 1-amino-3-N,N-dimethylamino)-propyliden-1,1-bisphosphonic acid of the structural formula: ##STR1## or of its monosodium or other pharmaceutically acceptable salt, as a biological carrier for bone active substances or for the preparation of a medicament for the diagnosis, prophylaxis and/or treatment of bone and/or mineral metabolism disorders.

Abstract: The freshness of meat, vegetables and fruits in a refrigerator or food storage box can be retained for a long period of time by using (1) a freshness retaining gel composition which comprises a freshness retainer component comprising an isothiocyanic acid compound and an aliphatic carboxylic acid or (2) a freshness retaining gel composition which comprises a freshness retainer component comprising an isothiocyanic acid compound, a nonionic surfactant or a fatty acid ester, and a gelling agent.

Abstract: The invention relates to the use of certain methanebisphosphonic acid derivatives (for the manufacture of a pharmaceutical composition) for the prevention and treatment of prosthesis loosening and prosthesis migration in mammals including man.

Abstract: There are described compounds of the formula I ##STR1## in which R.sup.1 is (C.sub.1 -C.sub.10)-alkyl, (C.sub.1 -C.sub.8)-alkanoyl, (C.sub.6 -C.sub.10)-aryl or Het, each of which can be substituted by halogen, --OH, --NH.sub.2, --NH--CO--R.sup.7, --O--CO--R.sup.7 and --N--(R.sup.8).sub.2 where R.sup.7 =(C.sub.1 -C.sub.6)-alkyl and R.sup.8, independently of one another, is hydrogen or (C.sub.1 -C.sub.2)-alkyl or in which R.sup.1 is the radical of the formula II ##STR2## in which n is an integer from 3 to 10, m is zero to 3, R.sup.6, independently of one another, is (C.sub.1 -C.sub.6)-alkyl which is optionally substituted by halogen or --NH--CO--R.sup.7, where R.sup.7 =(C.sub.1 -C.sub.6)-alkyl, and X is absent or is (C.sub.1 -C.sub.10)-alkyl, and R.sup.2, R.sup.3, R.sup.4 or R.sup.5, independently of one another, are hydrogen, (C.sub.1 -C.sub.5) -alkyl, lithium, sodium, potassium or Si(R), where R=(C.sub.1 -C.sub.

Abstract: The present invention provides methods for bone mass anabolic preservation or augmentation in human or other animal subjects affected by osteoporosis or other metabolic bone disorder characterized by systemic or regional bone loss, using bisphosphonates formulations, wherein the bone mass anabolic composition contains effective non-toxic doses of ?3-(N,N-dimethylamine)-1-hydroxypropylidene!-bisphosphonic acid or olpadronate or the monosodium or other pharmaceutically acceptable salt thereof.

Abstract: Novel carbocyclic compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.

Abstract: The present invention relates to the use of an ester of inositoltrisphosphate for the preparation of a medicament for preventing, alleviating or combatting inflammatory conditions in mammals including man.Injury or destruction of tissues should be understood as damage to an aggregation of specialized cells with a particular function both internally and externally in the body, such as different organs or parts of these, vessels, skin etc.Tissue damage involves a complex series of events such as dilatation of vessel walls e.g. arterioles, capillaries and venules, increased permeability of fluids including e.g. plasma proteins and increased blood flow. Increased vascular leakage often results in extravasation and oedema formation which characterize the damage of different tissues.Often tissue damage and inflammatory conditions are characterized by signs of pain, heat, redness, swelling and loss of function.

Abstract: The invention provides a method for inhibiting protein isoprenylation by administration of a polyisoprenyl pyrophosphate analogue. The polyisoprenyl pyrophosphate analogue may have formula 1, ##STR1## wherein: Pren represents a C.sub.10 -C.sub.30 terpenoid group or a derivative thereof;A.sup.1, A.sup.2, A.sup.3 and A.sup.4 independently represent a direct bond or a C.sub.1 -C.sub.4 alkylene or alkenylene group, optionally having substituents selected from methyl, hydroxy, methoxy, mercapto, methylthio, amino, methylamino, dimethylamino, halogen and a group having formula --X.sup.5 --A.sup.5 --P(.dbd.Z.sup.2)Y.sup.2 Y.sup.3 ; A.sup.5 represents a direct bond or a C.sub.1 -C.sub.4 alkylene or alkenylene group;X.sup.1, X.sup.2, X.sup.3, X.sup.4 and X.sup.5 independently represent a direct bond, oxygen, sulphur, imino or methylimino;Y.sup.1, Y.sup.2 and Y.sup.

Abstract: Compounds of the formula ##STR1## where m and n are integers 0 to 10 and m+n equals 0 to 10, (a) X is O or S(b) Z is a covalent bond; a monocyclic or polycyclic carbocycle ring moiety; or a monocyclic or polycyclic heterocyclic ring moiety containing one or more heteroatoms selected from O, S, or N;(c) Q is covalent bond; O; or S;(d) R is COOH, SO.sub.3 H, PO.sub.3 H.sub.2, or P(O)(OH)R.sup.4, wherein R.sup.4 is C.sub.1 -C.sub.8 alkyl;(e) R.sup.1, R.sup.2 and R.sup.5 are as defined in the claims.are useful in the treatment of calcium and phosphate elated disorders, such as arthritis and the like.

Abstract: The subject invention relates to compositions which are useful for improving the visual appearance of skin, especially facial skin. The composition contains certain primary actives including at least one cyclic polyanionic polyols at least one sulfhydryl compound and at least one zwitterionic surfactant. The subject invention further relates to methods of improving the visual appearance of skin.

Abstract: Alendronate, a bisphosphonate, when administered daily over a substantial period of time, can reduce the rate of non-vertebral fractures, in post-menopausal women.

Abstract: This invention encompasses a pharmaceutical composition comprising an effective amount of alendronate salt for reducing calcium loss and an effective amount of a gastric propulsive agent, preferably cisapride, to prevent gastric reflux caused by the alendronate salt.

Abstract: The present invention provides novel methods of treating or preventing osteoporosis comprising administering to a mammal in need of such treatment an effective amount of a compound of formula I ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different provided that, when R.sup.1 and R.sup.2 are the same, each is a methyl or ethyl group, and, when R.sup.1 and R.sup.2 are different, one of them is a methyl or ethyl group and the other is hydrogen or a benzyl group; or a pharmaceutically acceptable salt thereof; together with a bone resorption inhibiting polyphosphonate.

Abstract: Imidobisphosphoric acids, process for their preparation, and use thereof.There are described compounds of the formula I ##STR1## in which R.sup.1 is (C.sub.1 -C.sub.10)-alkyl, (C.sub.1 -C.sub.8)-alkanoyl, (C.sub.6 -C.sub.10)-aryl or Het, each of which can be substituted by halogen, --OH, --NH.sub.2, --NH--CO--R.sup.7, --O--CO--R.sup.7 and --N--(R.sup.8).sub.2 where R.sup.7 =(C.sub.1 -C.sub.6)-alkyl and R.sup.8, independently of one another, is hydrogen or (C.sub.1 -C.sub.4)-alkyl or in which R.sup.1 is the radical of the formula II ##STR2## in which n is an integer from 3 to 10, m is zero to 3, R.sup.6, independently of one another, is (C.sub.1 -C.sub.6)-alkyl which is optionally substituted by halogen or --NH--CO--R.sup.7, where R.sup.7 =(C.sub.1 -C.sub.6)-alkyl, and X is absent or is (C.sub.1 -C.sub.10)-alkyl, and R.sup.2, R.sup.3, R.sup.4 or R.sup.5, independently of one another, are hydrogen, (C.sub.1 -C.sub.5)-alkyl, lithium, sodium, potassium or Si(R), where R=(C.sub.1 -C.sub.

Abstract: A method is provided for preventing and/or treating hypertriglyceridemia, and/or atherosclerosis and/or pancreatitis resulting from hypertriglyceridemia, employing a squalene synthetase inhibitor.

Abstract: An insecticide composition is enhanced from the standpoint of its ability to be absorbed by insects, such as red fire ants, particularly dithiophosphate ester pesticides by the addition of a small amount of a water soluble non-aromatic polyorganic acid or salt form thereof such as polyaspartic acid, particularly preferred with a molecular weight in the range of about 3000 to 40,000.

Abstract: The present invention relates to methods of inhibiting alveolar bone resorption or the undesirable movement of teeth of a human or other animal comprising:a) administering a reservoir to the gingival tissue of the oral cavity such that the reservoir is in contact with the exposed tissue nearest to the alveolar bone to be treated wherein the reservoir is a composition having a pH which maintains an active compound in a negatively charged state and comprises a safe and effective amount of the active compound having the structure: ##STR1## wherein: n is an integer from 0 to 7 (preferably from 0 to 3, more preferably 1); R.sup.1 is hydrogen, chloro, amino, or hydroxy (preferably hydrogen or hydroxy); X is --NH--, quaternary amine, oxygen, sulfur, or a single bond (preferably --NH-- or single bond); R.sup.

Abstract: An insecticide composition is enhanced from the standpoint of its ability to be absorbed by insects, such as red fire ants, particularly dithiophosphate ester pesticides by the addition of a small amount of a water soluble non-aromatic polyorganic acid or salt form thereof such as polyaspartic acid, particularly preferred with a molecular weight in the range of about 3000 to 40,000.

Abstract: This invention is directed to a method for stimulating the proliferation of V.gamma.2V.delta.2 T cells comprising contacting V.gamma.2V.delta.2 T cells with a V.gamma.2V.delta.2 T cell proliferation stimulating amount of a compound selected from the group consisting of a monoalkyl phosphate and an alkenyl pyrophosphate.

Abstract: There is provided a squalene inhibitory composition containing a 1,1-bisphosphonic acid compound, a lower alkyl ester thereof, or a salt thereof, which is useful for treating hypercholesterolemia. There are also provided novel compounds having squalene synthetase inhibitory activity and a pharmaceutical composition for treating hypercholesterolemia containing a 1,1-bisphosphonic compound, a lower alkyl ester thereof or a salt thereof.

Abstract: Bisphosphonate, particularly alendronate, can prevent or treat bone loss associated with immunosuppressive therapy, whether or not the immunosuppressive therapy is associated with an organ transplant.

Abstract: This invention relates to bisphosphoryl hydrazine compounds and to compositions thereof which are useful as pesticides. The compounds of this invention are effective against soil insects, especially the corn rootworm.

Abstract: This invention relates to bisphosphoryl hydrazine compounds and to compositions thereof which are useful as pesticides. The compounds of this invention are effective against soil insects, especially the corn rootworm.