Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.

Abstract: The present invention discloses novel depeptidized compounds which have HCV protease inhibitory activity as well as pharmaceutical compositions comprising such compounds and methods of using them to treat disorders associated with the HCV protease.

Abstract: The present invention relates to a combination comprising: (a) an angiotensin II receptor blocker (ARB), or a pharmaceutically acceptable salt thereof; (b) a calcium channel blocker (CCB), or a pharmaceutically acceptable salt thereof; and (c) one of the two active agents selected from (i) a rennin inhibitor, or a pharmaceutically acceptable salt thereof; and (ii) a neutral endopeptidase (NEP) inhibitor, or a pharmaceutically acceptable salt thereof; for the prevention of, delay the onset of and/or treatment of cardiovascular disorders, which method comprises administering to a warm-blooded animal, in need thereof, a therapeutically effective amount of a combination of the present invention.

Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.

Abstract: Treating of localized bacterial infection, comprising locally applying Taurolidine to the infection. A device for insertion into the body, the device comprising Taurolidine to render the device infection resistant. A medication for treating bacterial infections, comprising Taurolidine carried by one of: gels, liquid, thixotropic gels, colloidal mixtures, dispensal suspensions, injectable polymers, or a microparticle. A method for treating blood, comprising: removing blood from the body; treating the blood with Taurolidine; and returning the treated blood.

Abstract: A method of treating a patient with breast cancer includes administering to the patient a breast cancer cell proliferation-inhibiting amount of a methylol-containing compound such as taurolidine, taurultam or a mixture thereof.

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: wherein R1, R2, R3A, R3B, R4, R5, R6, R7, R8, and X are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, and intermediates are also disclosed.

Abstract: The invention relates to carboxamidine derivatives to pharmaceutical compositions containing the same and the use thereof in the preparation of pharmaceutical compositions for the treatment of vascular diseases.

Abstract: The invention relates to a bilayer pharmaceutical tablet comprising a first layer containing 3 to 50 wt. % of telmisartan dispersed in a dissolving tablet matrix and a second layer containing a diuretic in a disintegrating tablet matrix as well as a processes for producing same.

Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.

Abstract: This invention relates to a solid pharmaceutical composition containing valsartan particles characterized in that the D50 of said valsartan particles is 150 ?m or below and that the valsartan particles have a maximum diameter of no more than 1100 ?m, as determined by electron microscopy.

Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is

Abstract: N-(Substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides are inhibitors of HIV integrase and inhibitors of HIV replication. The naphthyridine carboxamides are of Formula (I): wherein R1?, R2? and R3? are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are described.

Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.

Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R6 is hydrogen or phenylmethyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical.

Abstract: The present invention discloses novel depeptidized compounds which have HCV protease inhibitory activity as well as pharmaceutical compositions comprising such compounds and methods of using them to treat disorders associated with the HCV protease.

Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.

Abstract: Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.

Abstract: Taurolidine and/or taurultam is administered during and after surgical removal of a cancerous tumor to treat abdominal cancer.

Abstract: Compound of the Formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein: X is CH or N, Y is C or S, Z is —SO2— or —(CRaRb)r—, n is 1 or 2, R2 is aryl or heteroaryl, and R1, R3, R4, R5, R6, R7, R8, R9, Ra, Rb, m, p, q and r, are as defined herein. The compounds are modulators of the 5-HT6 receptor and are useful for treatment of central nervous system disorders. Also provided are methods for preparing, compositions comprising, and methods for using Compounds of Formula I.

Abstract: The invention relates to methods for preventing and treating disseminating cancers. Inhibition metastases of a primary tumor to a liver tissue is carried out by directly contacting a liver tissue with Taurolidine.

Abstract: A compound having the general formula and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.

Abstract: Disclosed are a series of heteroaryl-?-alanine derivatives, compositions containing them, processes for their preparation and their use in medicine.

Abstract: The invention provides a method of inhibiting tumor growth in a mammal, by administering to the mammal composition containing taurolidine, taurultam, or a biologically active derivative thereof. The composition is administered to directly contact a tumor cell at a dose sufficient to induce cell death by apoptosis.

Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.

Abstract: The invention provides a method of inhibiting tumor growth in a mammal, by administering to the mammal composition containing methylol-containing compound. The composition is administered to directly contact a tumor cell at a dose sufficient to induce cell death by apoptosis.

Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) in which X represents hydrogen, halogen or alkyl, m represents integers from 2 to 10, n represents 0, 1 or 2. y represents unsubstituted or substituted methylene and p represents 1, 2 or 3, and to processes for their preparation and to their use as pesticides.

Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a

Abstract: The use of mitochondrial KATP channel openers, particularly compounds of general formula (I), for the treatment or prevention of inflammation by inducing apoptosis of inflammatory cells.

Abstract: Complex compounds or adducts of xanthine derivatives, for example propentofylline or pentoxyfylline, or phenazone derivatives, for example phenazone, propylphenazone and aminophenazone, and acesulfame-H, in which the components are present in a molar ratio of 1:1 or 1:2, have a pleasantly sweet taste and are suitable for numerous applications, for example in pharmaceuticals. The compounds can be prepared from the dissolved components by simple reaction.

Abstract: The present invention provides certain thiadiazinone derivatives of oxazolidinones of the following formula I: or pharmaceutically acceptable salts thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.

Abstract: The present invention provides a hetrodiazinon compound having 2-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor antagonistic action, which is represented by the following formula (I), a pharmacologically acceptable salt thereof or hydrates thereof. Wherein A represents O, S or a group represented by the formula NR3 (wherein R3 represents hydrogen atom or a lower alkyl group); R1 and R2 are the same as or different from each other and each represents an optionally substituted (hetero)aryl group etc.; and R4 and R5 are the same as or different from each other and each represents hydrogen atom, hydroxy, a halogen atom, nitrile group, nitro group, a lower alkyl group, a (hetero)aryl group etc.

Abstract: A taurolidine composition includes an aqueous solution containing about 1.5-3% by weight taurolidine, the solution containing a stability-enhancing effective amount of at least one physiologically acceptable electrolyte, such that the solution is substantially isotonic.

Abstract: Reaction products of taurultam and glucose are useful as antineoplastic agents. They are produced by reacting an aqueous solution of taurultam and glucose at about 100 degrees Celsius for about 30 minutes, yielding a reaction product which has a melting point of 168 to 170 degrees Celsius.

Abstract: The present invention relates to modified amino acids of general formula 1

Abstract: The present invention contemplates the addition of 0.5% to 4% taurolidine into solutions used peritoneal dialysis. The taurolidine is intended to prevent or reduce the incidence of infection within the abdomen and/or in the vicinity of an implanted dialysis port. The invention also includes methods using solutions of taurolidine in the flushing and locking of catheters and fluid lines used in peritoneal dialysis.

Abstract: The invention relates to a compositions useful in the field of agricultural chemistry and methods for making and using the compositions. The compositions include (i) a permeabilizing agent, and (ii) a active component, for example, a pesticide or plant growth regulator, and can include additional components as well, for example, flow agents. The permeabilizing agent, or a mixture of permeabilizing agents, acts as an adjuvant to the active component or chemicals to improve the degree of efficacy of the active component or speed of action of the active component. The permeabilizing agents are typically one or more chelating agents, cationic materials, anionic materials, and zwitterionic materials, and include polyphosphate salts. Examples of cationic materials include polyamines such as ethylenediamine and quaternary ammonium salts. The active components can be pesticides, herbicides, insecticides, fungicides, virucides, bacteriocides, and acaricides.

Abstract: The invention relates to methods for preventing and treating disseminating cancers. Inhibition metastases of a primary tumor to a liver tissue is carried out by directly contacting a liver tissue with Taurolidine.

Abstract: The invention provides compositions, pharmaceutical preparations and methods for inhibition of cystic fibrosis transmembrane conductance regulator protein (CFTR) that are useful for the study and treatment of CFTR-mediated diseases and conditions. The compositions and pharmaceutical preparations of the invention may comprise one or more thiazolidinone compounds, and may additionally comprise one or more pharmaceutically acceptable carriers, excipients and/or adjuvants. The methods of the invention comprise, in certain embodiments, administering to a patient suffering from a CFTR-mediated disease or condition, an efficacious amount of a thiazolidinone compound. In other embodiments the invention provides methods of inhibiting CFTR that comprise contacting cells in a subject with an effective amount of a thiazolidinone compound.

Abstract: The invention provides a method of inhibiting tumor growth in a mammal, by administering to the mammal composition containing taurolidine, taurultam, or a biologically active derivative thereof. The composition is administered to directly contact a tumor cell at a dose sufficient to induce cell death by apoptosis.

Abstract: The invention relates to the area of erythropoiesis, in particular to the use of tetrahydroquinolinyl-6-methyldihydrothiadiazinones of general formula (I) for treating anaemia. The invention also relates to novel tetrahydroquinolinyl-6-methyldihydrothiadiazinone derivatives and to the production thereof.

Abstract: The invention relates to the use of mitochondrial KATP channel openers, particularly compounds of general formula (1), for the treatment or prevention of inflammation by inducing apoptosis or inflammatory cells.

Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule in an amount sufficient to control the aberrant growth state e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. The present invention further makes available methods and reagents for ameliorating to consequences of hedgehog loss-of-function, ptc gain-of-function, or smoothened loss-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule, in an amount sufficient to ameliorate the In certain embodiments, the subject compounds, e.g., a cAMP analog, adenylate cyclase agonist, or cAMP phosphodiesterase inhibitor, regulate cAMP levels, which in turn modulates activity of the hedgehog pathway.

Abstract: The invention relates to novel guanidine derivatives of the formula (I) in which A, R1, R2, R3 and Z are as defined in the description, to a process for their preparation and to their use for controlling animal pests.

Abstract: The present invention provides certain thiadiazinone derivatives of oxazolidinones of the following formula I: 1

Abstract: Implanted catheters are locked with a solution comprising a lower alcohol, typically ethanol, propanol, or butanol, most preferably isopropanol, and an additive, the additive comprising an anti-microbial, typically taurolidine or triclosan, or an anti-coagulant, typically riboflavin, sodium citrate, ethylene diamine tetraacetic acid, or citric acid. The use of an alcohol and additive solution can effectively reduce fouling of the catheter, particularly clotting and thrombus in intravascular catheters, as well as reduce the risk of infection. The risk of infection can be further reduced by employing a catheter body which is sufficiently porous to permit the anti-microbial solution of a lower alcohol and another anti-microbial or anti-coagulant compound to penetrate into the catheter body and preferably through the catheter into tissue surrounding the implanted catheter.

Abstract: The present invention contemplates the addition of 0.5% to 4% taurolidine into solutions used peritoneal dialysis. The taurolidine is intended to prevent or reduce the incidence of infection within the abdomen and/or in the vicinity of an implanted dialysis port. The invention also includes methods using solutions of taurolidine in the flushing and locking of catheters and fluid lines used in peritoneal dialysis.

Abstract: The present invention relates, e.g., to a method and application for the treatment and/or prophylaxis of tumors and/or infections in the central nervous system and/or other parenchymal organs in mammalian subjects. In preferred embodiments, a microdialysis device is used to provide an effective dose of taurolidine and/or its metabolites and/or other chemotherapeutic and/or immunotherapeutic and/or antibiotic and/or virostatic and/or fungistatic agents is administed to a mammalian subject suffering from or at risk to growth of tumors of the central nervous system and/or other parenchymal organs.

Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.