Abstract: The present invention provides methods and pharmaceutical compositions for treating or inhibiting urinary stone disease that involve administering to an individual with urinary stone disease or at risk of developing urinary stone disease an amount effective of pyridoxamine to reduce urinary oxalate concentrations.

Abstract: Phenylacetic acid derivatives of the formula I where the variables are as disclosed herein, their salts, processes and intermediates for their preparation, and their use for controlling harmful fungi and animal pests.

Abstract: Treatment with a cyclooxygenase-2 inhibitor and a leukotriene A4 hydrolase inhibitor is described as being useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune diseases.

Abstract: The present invention provides a compound containing at least one sulfhydryl group and at least one NO donor group, wherein said compound is a) a compound containing one or more sulfhydryl groups linked to at least one aromatic ring or a heteroaromatic ring with a nitrogen in the ring structure, which ring is substituted by one or more substituents bearing a terminal —ONO2 group; b) a 5-membered ring heterocyclic compound containing a sulfur atom and a nitrogen atom, which ring is substituted by one or more substituents bearing a terminal —ONO2 group; c) a 5-membered ring compound containing two conjugate S-atoms, which ring is linked to one or more substituents bearing a terminal —ONO2 group; or d) a compound containing an acyclic —S—S group, linked to at least one aromatic ring or a heteroaromatic ring with a nitrogen in the ring structure, which ring is substituted by one or more substituents bearing a terminal —ONO2 group.

Abstract: Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR1R2  I  in which A, R1 and R2 are as defined in the description, and b) compounds of the formula II, their N-oxide or one of their salts  where the substituents R12 to R18 are as defined in the description, and/or c) compounds of the formula III  where the substituents X1 to X5 and R19 to R22 are as defined in the description, in a synergistically effective amount.

Abstract: Compounds of the formula which is explained more fully in the specification, may be prepared by conventional methods and used therapeutically in conventional galenic preparations.

Abstract: The invention relates to use of substituted aromatic polycyclic tertiary-heteroalkylamine compounds as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred substituted aromatic polycyclic tertiary-heteroalkylamine compounds are substituted N-benzyl-N-phenyl aminoalcohols.

Abstract: Derivatives of phenyl pyridinone are useful for the treatment of patients having precancerous lesions. These compounds are also useful to inhibit the growth of neoplastic cells.

Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted cycloalkyl aminoalcohols.

Abstract: An aryloxyaniline derivative represented by the formula: wherein Ar1 and Ar2 are the same or different, and are each a substituted or unsubstituted phenyl group, a substituted or unsubstituted pyridyl group or a naphthyl group, provided that Ar1 and Ar2 are not both phenyl or both naphthyl and are not phenyl and naphthyl, R1 is a hydrogen atom, a substituted or unsubstituted alkyl group having 1 to 10 carbon atoms, an alkoxy group having 1 to 10 carbon atoms, a substituted or unsubstituted phenyl group or a group of the formula: —NR2(R3) (wherein R2 and R3 are the same or different, and are each a hydrogen atom or an alkyl group having 1 to 10 carbon atoms, X1 is a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, a phenoxy group, a halogen atom, a trifluoromethyl group, a carbamoyl group or an aminosulfonyl group, Y1 is a branched or unbranched alkylene group having 1 to 6 carbon atoms or a single bond; and pharmaceutically acceptabl

Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not require a &bgr;-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: The present invention relates to a method of treating Multiple Sclerosis, other demyelinating disorders and peripheral neuropathy in a mammal by administering to the mammal a neurotransmitter-inducing or precursor agent in combination with an (SRI) antidepressant or an anxiolytic agent with improvement in efficiency. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a neurotransmitter-inducing or precursor agent, and an SRI antidepressant or anxiolytic agent.

Abstract: A compound of the formula (I): 1

Abstract: This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl.

Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenoxy-N-phenyl aminoalcohols.

Abstract: The present invention is concerned with 3-(amino- or aminoalkyl)pyridinone derivatives which inhibit the reverse transcriptase of the Human Immunodeficiency Virus (HIV). It relates moreover to the use of such compounds for treating HIV-related diseases. Furthermore it relates to a process for the preparation of these compounds.

Abstract: Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof aryloxyalkylamines, including pyridyloxylalkylamines and phenoxyalkylamines, such as (3-(3-pyridyloxy)propyl)methylamine and (3-(5-bromo(3-pyridyloxy))propyl)methylamine.

Abstract: Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof aryloxyalkylamines, including pyridyloxylalkylamines and phenoxyalkylamines.

Abstract: Diacyl-substituted guanidines of the formula I are described where X(1) and X(2) are as defined herein. The compounds are suitable for use as antiarrhythmic pharmaceuticals possessing a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris, in connection with which they also inhibit or strongly reduce, in a preventitive manner the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the elicitation of ischemically induced cardiac arrhythmias.

Abstract: Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR1R2  I in which A, R1 and R2 are as defined in the description, and b) dimethomorph or flumetover, and/or c) a valinamide of the formula III  in which R13 is C3-C4-alkyl and R14 is naphthyl or phenyl, where the phenyl radical is substituted in the 4-position by a halogen atom, a C1-C4-alkyl or C1-C4-alkoxy group, and/or d) benalaxyl, ofurace, metalaxyl, furalaxyl or oxydixyl, and/or e) 1-(2-cyano-2-methoxyiminoacetyl)-3-ethylurea in a synergistically effective amount.

Abstract: The present invention provides improved dialysis compositions and methods for dialysis comprising utilizing the disclosed AGE inhibitors, together with methods to reduce dialysis-related complications and disorders.

Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.

Abstract: The invention relates to the manipulation of enzymatic pathways, such as poly (ADP-ribose) polymerase pathways, which are dependent upon NAD as a substrate. By administering pro-NAD compounds, cell death caused by necrosis and/or apoptosis can be reduced. Further, by inhibiting one or more of these enzymes, the process of cell death can be accelerated, in conditions such as cancer, where acceleration of cellular necrosis and/or apoptosis is desired. Various inhibitors are described.

Abstract: The invention provides methods which are useful for treating diseases (e.g., cancer) where PKC&dgr; is implicated, and modulation (e.g, inhibition) of its activity is desired.

Abstract: Substituted 2-(2′-pyridyloxy)phenylacetamides I, where R1 is fluorine, chlorine, CH3 or halomethyl; R2 is fluorine, bromine, alkyl or halomethyl; R3 is hydrogen or one of the radicals mentioned under R2; and R2 is 6-chloro if R3 is hydrogen, R3 is 5-chloro if R2 is fluorine and the compound in which R1, R2 and R3 are each chlorine with the proviso that R1 may not be chlorine if R2 is 5-trifluoromethyl and R3 is hydrogen, and processes for their preparation and their use for controlling harmful fungi and animal pests are described.

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract: Substituted 4-phenyl-pyridine compounds with activity as antagonists of Neurokinin 1 receptors, methods of making these compounds and preparing.

Abstract: The present invention provides a phthalic acid diamide derivative represented by the general formula (I) (wherein R1, R2 and R3 are each H, C3-C6 cycloalkyl group, group of the formula —A1—Ql or the like; X may be the same or different and are each halogen atom, nitro group, phenyl group, group of the formula —A2—R7 or the like; n is 1 to 4; Y may be same or different and are each halogen atom, cyano group, phenyl group, group of the formula —A2—R7 or the like; m is 1 to 5; Z1 and Z2 are each 0 or S), fluorine-containing aniline compound represented by the general formula (ST-I) as starting material for said phthalic acid diamide derivative (wherein Ra is halogen atom, C1-C6 alkyl group or the like and Rb, Rc and Rd is H or C2-C6 perfluoroalkyl group), and an agricultural and horticultural insecticide containing said phthaldiamide derivative, as well as to provide a method for use of said insecticide.

Abstract: There is provided a pharmaceutical composition suitable for topical administration to an eye which contains a selective COX-2 inhibitory drug or nanoparticles of a drug of low water solubility, in a concentration effective for treatment and/or prophylaxis of a disorder in the eye, and one or more ophthalmically acceptable excipients that reduce rate of removal from the eye such that the composition has an effective residence time of about 2 to about 24 hours. Also provided is a method of treating and/or preventing a disorder in an eye, the method comprising administering to the eye a composition of the invention.

Abstract: Heteroaryl aminobenzophenones of general formula I inhibit interleukin-1&bgr; and TNF-&agr; and may therefore be useful in the therapy of inflammatory diseases and conditions.

Abstract: The present invention relates to compounds of formula (I), wherein Ar1 represents (A) and (B) or (C); R12 and R13 are independently hydrogen or C1-4alkyl; Ar2 is phenyl or heteroaryl; p is 0 or 1; Ar3 is phenyl, pyridinyl, pyridazinyl, pyrimidyl or pyrazynyl, the ring being substituted on ring carbon atoms by R2 and —(CH2)nR3, and wherein Ar3 is attached to Ar1C(R12)R13CH(Ar2)O— by a ring carbon atom; R2 is a group of formula (2), or R2 represents a lactone of formula (3), the group of formula (2) or (3) having L or D configuration at the chiral alpha carbon in the corresponding free amino acid; n is 0, 1 or 2; R3 is phenyl or heteroaryl; and R5-R9, m and n are as defined in the specification; or a pharmaceutically acceptable salt, prodrug or solvate thereof. Processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them. A particular use in cancer therapy.

Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.

Abstract: The present invention is directed to methods of using pro-NAD agents capable of enhancing the dermal and epidermal skin cell NAD content. These pro-NAD agents may be administered topically, orally, or parenterally to enhance DNA repair and other protective responses to DNA damage. The invention further relates to pharmaceutical compositions comprising pro-NAD agents that effectively elevate intracellular NAD content. Finally, the invention relates to the method of using the pro-NAD agents to treat disorders such as sunburn and other skin deterioration that results from DNA damage in skin cells.

Abstract: An antioxidant composition is isolated and purified from natural sources including yeast (S. carlsbergenesis, S. cerevisiae, or commercial yeast extract), and saltbush (Atriplex halimus), or synthesized chemically, by processes that improve the potency of the product. Compositions containing natural and synthetic compounds, with or without chromium, possessing antioxidant activity are formulated for use in animals and humans. Methods for use of the natural and synthetic antioxidants, alone or in combination with other antioxidant agents, for regulating oxidative conditions are presented.

Abstract: There is provided a method for controlling flies, that live in or come flying to livestock pens or poultry houses, by using a compound or salt thereof with an affinity for a nicotinic acetylcholine receptor of insects. Since having a very high activity against flies, the compound or salt thereof helps quickly and efficiently to control flies that live in or come flying to livestock pens or poultry houses. Also, since having an excellent control effect on flies that are resistant to conventional chemicals including a organo-phosphoric pesticide and a pyrethroid, the compound or salt thereof helps to prevent propagation, caused by flies, of various diseases to livestock, poultry and humans, and reduce discomfort of workers engaged in the livestock and poultry farming and a community. Still, it is possible with the present invention to keep livestock pens or poultry houses in a hygienic condition, which may greatly contribute to the development of the livestock and poultry farming.

Abstract: The present invention is directed to a series of substituted pyridine compounds, a method for selectively controlling neurotransmitter release in mammals using these compounds, and pharmaceutical compositions containing these compounds. Preferred compounds are 3′-(5′- and/or 6′-substituted) pyridyl ethers.

Abstract: The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds with (derivatised) hydroxyalkyl substituents on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at least one of the 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds as the active ingredient.

Abstract: This invention relates to a series of substituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules that bind to neutral sphingomyelinase and inhibit its activity.

Abstract: Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof aryloxyalkylamines and arylthioalkylamines, including pyridyloxylalkylamines, phenoxyalkylamines, pyridylthiolalkylamines and phenylthioalkylamines. Exemplary compounds include (2-(5-bromo(3-pyridylthio))ethyl)methylamine, (2-(5-bromo(3-pyridylthio))isopropyl)methylamine, (2-(5-bromo(3-pyridylthio))propyl)methylamine, (3-(5-bromo(3-pyridylthio))propyl)methylamine, 3-((3S)-3-pyrrolidinyloxy)pyridine, 3-(4-piperidinyloxy)pyridine, 3-(1-methyl-4-piperidinyloxy)pyridine, (3-benzo[3,4-d]1,3-dioxolan-5-yloxypropyl)methylamine, and methyl(3-tricyclo[7.3.1.0<5,13>]tridec-2-yloxypropyl)amine.

Abstract: Blood cholesterol levels are correlated with production of amyloid &bgr; protein (A&bgr;), and are predictors of populations at risk of developing AD. Methods for increasing HDL-cholesterol levels, HDL-apoA-I levels, or HDL function, can be used to decrease production of A&bgr;, thereby decreasing the risk of developing AD. Compounds which function as HDL include synthetic HDL which contains lipid such as phosphotidyl choline, phosphatidyl serine, phosphatidyl ethanolamine, and other phospholipids. Compounds which enhance HDL function include HDL associated proteins such as apo A1 or variants thereof including apo AI-Milano and biologically active peptides derived therefrom, reverse lipid transport (RLT) peptides, apoE, enzymes associated with HDL such as paraoxonase, and LCAT, alone or, more preferably, formulated in combination with liposomes or emulsions.

Abstract: The invention concerns new guanidine derivatives of formula (I), methods of preparing them and their use in drugs containing such compounds.

Abstract: A compound having formula (I), wherein A is selected from the group consisting of: (i) phenyl, wherein said phenyl is optionally substituted by one or more halogen atoms, C1-6alkyl, C1-3alkoxy, C1-3fluoroalkoxy, nitrile, or —NR7R8 where R7 and R8 are independently hydrogen or C1-3alkyl; (ii) a 5- or 6-membered hetrocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur; and (iii) a fused bicyclic ring (a), wherein ring C represents a heterocyclic group as defined in point (ii) above, which bicyclic ring is attached to group B via a ring atom of ring C; B is selected from the group consisting of: (iv) C1-6alkylene; (v) —MC1-6alkylene or C1-6alkyleneMC1-6alkylene, wherein M is O, S, or —NR2 wherein R2 represents hydrogen or C1-3alkyl; (vi) a 5- or 6-membered heterocyclic group containing at least one nitrogen heteroatom and optionally at least one further heteroatom selected from oxygen, nitrogen and sulfur and optionally substituted by C1-3alkyl; and (vii) H

Abstract: A natural method for promoting fat, and weight loss while decreasing food cravings comprising administrating to an individual in need thereof L-carnitine, chromium, coenzyme Q10, creatine, lipoic acid, niacin, pyruvate, riboflavin, and thiamine. Pyruvate is a major promoter of the oxidation of dietary fuels like carbohydrates and fatty acids in the citric acid cycle. L-carnitine allow the transport of fatty acids into the mitochondria were they can be degraded in the citric acid cycle. Lipoic acid is a major intracellular antioxidant, and component of key enzymes in the citric acid cycle. Niacin, riboflavin, and thiamine are key components of enzymes that lead to the breakdown of dietary fuel molecules such as fatty acids, amino acids, and carbohydrates that enter the citric acid cycle. The breakdown of these dietary fuels leads to the production of high energy hydrogen atoms. Coenzyme Q10 accepts these hydrogen atoms and utilizes them for cellular energy production.

Abstract: Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof aryloxyalkylamines, including pyridyloxylalkylamines and phenoxyalkylamines.

Abstract: Patients susceptible to or suffering from central nervous system disorders (e.g., Alzheimer's disease, Parkinson's disease, Tourette's syndrome, attention deficit disorder or schizophrenia) are treated by administering an effective amount of an aryl substituted olefinic amine compound. Exemplary compounds include, (E)-N-methyl-4-[3-(5-isopropoxypyridin)yl]-3-buten-1-amine, and (E)-N-methyl-4-[3-(5-methoxymethylpyridin)yl]-3-buten-1-amine.

Abstract: A frozen nutritional food product and method for oral delivery of nutrients, medicinal substances and other active ingredients via absorption through the oral mucosa for systemic effect. The frozen product includes at least one active ingredient, at least one flavoring agent, preservatives, food coloring, and a balance of water as a delivery liquid. The water is subjected to a magnetic treatment process and an ozonation process to enhance delivery of the active ingredients. More particularly, a first portion of the water is magnetized to neutralize the pH, increase oxygenation, and to improve the solubility of the ingredients mixed with the water. The remaining portion of the water is sterilized by ozonation, causing oxidation of undesirable metallic ions, odor and taste producing agents, and a wide variety of organics. Ozonation further increases the dissolved oxygen content of the water.

Abstract: Compounds having fungicidal activities and represented by general formula (I) and salts and hydrates thereof wherein R1 represents an optionally substituted aryl, an optionally substituted alkyl or the like; R2 represents an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted aryl, an optionally substituted heterocyclic group or the like; R3 represents an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted arylsulfonyl, an optionally substituted heterocyclic group or the like; R4 and R5, which may be the same or different, represent each a hydrogen atom, an optionally substituted alkyl, or an optionally substituted alkoxy, or R4 and R5 may form together with the adjacent nitrogen atom an optionally substituted monocycle or polycycle; X and Y, which may be the same or different, represents each an oxygen atom or NR6 wherein R6 represents a hydroge

Abstract: Patients susceptible to, or suffering from chronic and/or female-specific pain are treated by administering an effective amount of a metanicotine-based compound.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: The instant invention provides compositions and methods for modeling post-Amadori AGE formation and the identification and characterization of effective inhibitors of post-Amadori AGE formation, and such identified inhibitor compositions.