Abstract: The present invention relates to implantable surgical medical devices having coatings comprising one or more compounds that inhibit TNF-&agr; converting enzyme (TACE), more particularly, stents having coatings comprising TACE inhibitors.

Abstract: This invention is directed to a class of compounds (Formula I) including succinoyl amino pyrazoles, succinoyl amino thiadiazoles, succinoyl amino acid esters, succinoyl amino acid amides, succinoyl amino alcohols, succinoyl amino ketones, succinoyl amino hydantoins, succinoyl anilines, and succinoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting &bgr;-amyloid peptide release and/or synthesis, a method for inhibiting &ggr;-secretase activity and a method for treating neurological disorders associated with &bgr;-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.

Abstract: Compounds of the formula (I) useful as metalloproteinase inhibitors, especially as inhibitors of MMP12, wherein R5 is a monocyclic group.

Abstract: The object of the present invention is to provide a compound having an anti-Helicobacter action.

Abstract: The invention relates to 2-thiohydantoin derivative compounds selected from compounds of general formula (I): 1

Abstract: This invention relates to compounds of the following formula: 1

Abstract: Compounds of the formula (I) useful as metalloproteinase inhibitors, especially as inhibitors of MMP12, wherein R5 is a bicyclic group.

Abstract: The present invention is to provide an imidazolidinedione derivative and oxazolidinedione derivative represented by the following general Formula (I) having the chymase and/or tryptase inhibition activity 1

Abstract: Compounds of the formula (I) wherein z —O— or —S—, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.

Abstract: Methods and compositions for the topical or transdermal treatment of neuropathy. More particularly, transdermal or topical compositions including a combination of ingredients that provide a surprising degree of effective relief from the symptoms of peripheral neuropathy and methods for administering the compositions to treat various neuropathies.

Abstract: The present invention provides a stable, low free formaldehyde, synergistic antimicrobial composition, and a method of inhibiting the growth of or reducing microorganisms by applying the composition. Preferably, the constituents are dimethylol dimethylhydantoin, monomethylol dimethylhydantoin, dimethyl hydantoin, and dehydroacetic acid or its salts thereof. The composition has a free formaldehyde content of less than 0.2% and is beneficial for controlling microbiological and fungal contamination in personal care products, household products and industrial products and systems.

Abstract: This invention relates to aryl substituted hydantoins of Formula I: 1

Abstract: Base on the anatomy and neurophysiology described in the Neurophysiologic Basis of Idiopathic Diseases, the categories of oral and parenteral medications can be used to manage and treat fibromyalgia and related diseases, disorders, syndromes and sequelae in a human. The target neurons involve in the genesis and perpetuation of fibromyalgia and related syndromes, diseases and disorders and sequelae in the peripheral nervous system and central nervous system are affected and modulated by the anticonvulsants, antidepressants and opioids.

Abstract: The present invention is related to azolidinedione-vinyl fused-benzene derivatives of formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.

Abstract: Microbiological control in aqueous media and/or eradication or reduction of biofilm on a surface in contact with such media is achieved by introducing into the aqueous medium a microbiocidally effective quantity of one or more 1,3-dibromo-5,5-dialkylhydantoins where one of the alkyls is methyl and the other is a C1-4 alkyl, wherein (i) the molar quantity of 1,3-dibromo-5,5-dialkylhydantoin introduced is less than the molar quantity of N,N′-bromochloro-5,5-dimethylhydantoin that would be required to effect the same degree of microbiological control in that medium, (ii) the molar quantity of the 1,3-dibromo-5,5-dialkylhydantoin introduced releases an amount of “free chlorine” that is greater than the amount of “free chlorine” that would be released in that medium by an equimolar quantity of N,N′-bromochloro-5,5-dimethylhydantoin, and (iii) the amount of “free chlorine” released by the quantity of the 1,3-dibromo-5,5-dialkylhydantoin introduced is greater than the

Abstract: Microbiological control is achieved by continuously and inexpensively dosing water in contact with biofilm, or that comes into contact with biofilm, using a highly effective biocide that provides very effective microbiocidal control of planktonic microorganisms and of biofilm species, even where the biofilm infestations have been in existence for long periods of time and thus have encased themselves in a substantial quantity of slimy defensive polysaccharide layers or films. In addition, the biocide used makes possible significant reduction in copper and/or iron surfaces in contact with the water as compared to N,N′-bromochloro-5,5-dimethyl hydantoin. Still other advantages are made possible by the described technology.

Abstract: The present application describes novel hydantoin derivatives of formula (I): 1

Abstract: A class of 1-phenyl imidazol-2-one biphenylmethyl compounds is described for use in treatment of circulatory disorders.

Abstract: Heterocyclic compound represented by the formula I 1

Abstract: The invention relates to novel biaromatic compounds which correspond to the general formula (I) below: 1

Abstract: The present invention relates to antimicrobial compositions including a critical, near critical, or supercritical (densified) fluid and an antimicrobial agent, to methods of forming these compositions, and to methods employing these compositions. An antimicrobial agent can be generated in the presence of a densified fluid, for example, by reacting an oxidizing agent with a precursor to the antimicrobial agent.

Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.

Abstract: The present invention provides a compound and a method of making a compound according to the following formula: 1

Abstract: The present invention provides compounds of formula (I), wherein X, Y, R1, R2, R3, and R4 are as defined in the description, and the preparation therof. The compounds of the formula bind to somatostatin receptiors and are useful as pharmaceuticals.

Abstract: A topical pharmaceutical composition is provided for the treatment of female sexual dysfunction, wherein the composition is formulated so as to contain a therapeutically effective amount of a phosphodiesterase inhibitor and a pharmaceutically acceptable carrier for topical administration. The phosphodiesterase inhibitor is generally selected from Type III, Type IV, Type V, and nonspecific phosphodiesterase inhibitors.

Abstract: The present invention relates to novel imidazolidine derivatives of formula I, wherein A, E, Z, R1, R2, R3, R4 and R5 have the meanings indicated in the claims. The compounds of formula I are valuable pharmaceutical active compounds which are suitable, for example, for the treatment of inflammatory diseases, including rheumatoid arthritis, or allergic diseases. The compounds of formula I are inhibitors of the adhesion and migration of leukocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the treatment of diseases which are caused by an undesired extent of leukocyte adhesion and/or leukocyte migration or are associated therewith or in which cell-cell or cell-matrix interactions which are based on the interactions of VLA-4 receptors with their ligands play a role.

Abstract: The dry blends comprise a powdery or finely-divided halogenated hydantoin, and a paraffin wax that is compatible with the halogenated hydantoin. The paraffin wax is a hydrocarbon paraffin wax and/or a chlorinated paraffin wax. Shape-retentive compacted compositions are formed by pressure compacting such blends. Preferred halogenated hydantoins are 1,3-dihalo-5,5-dialkylhydantoins.

Abstract: A method for the identification and treatment of pathogenic microorganism infections by inhibiting one or more enzymes in a metabolic pathway by inhibiting the conversion of substrate to produce the penultimate or ultimate product particularly by inhibiting the activity of one or more of the enzymes in the pathway, and compounds and pharmaceutical compositions for inhibiting infections of pathogenic microorganisms by inhibiting such enzymes.

Abstract: This invention is directed to a class of compounds (Formula I) including hydroxyalkanoyl amino pyrazoles, hydroxyalkanoyl amino thiadiazoles, hydroxyalkanoyl amino acid esters, hydroxyalkanoyl amino acid amides, hydroxyalkanoyl amino alcohols, hydroxyalkanoyl amino ketoes, hydroxyalkanoyl amino hydantoins, hydroxyalkanoyl anilines, and hydroxyalkanoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting &bgr;-amyloid peptide release and/or synthesis, a method for inhibiting &ggr;-secretase activity and a method for treating neurological disorders associated with &bgr;-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.

Abstract: The present invention relates to imidazolidine derivatives of the formula I, in which B, E, W, Y, R, R2, R3, R30, e and h have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds, which are suitable, for example, for the therapy and prophylaxis of inflammatory disorders, for example of rheumatoid arthritis, or of allergic disorders. The compounds of the formula I are inhibitors of the adhesion and migration of leukocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the therapy or prophylaxis of diseases which are caused by an undesired extent of leukocyte adhesion and/or leukocyte migration or are associated therewith, or in which cell-cell or cell-matrix interactions which are based on interactions of VLA-4 receptors with their ligands play a part.

Abstract: Purified soy phosphatidylserine is used to make cochleates. The cochleates contain at least about 75% soy phosphatidylserine and optionally a bioactive load. A preferred cochleate contains the antifungal agent amphotericin B.

Abstract: Hydroxamic and carboxylic acid derivatives having MMP and TNF inhibitory activity.

Abstract: Microbiological control in aqueous media and/or eradication or reduction of biofilm on a surface in contact with such media is achieved by introducing into the aqueous medium a microbiocidally effective quantity of one or more 1,3-dibromo-5,5-dialkylhydantoins where one of the alkyls is methyl and the other is a C1-4 alkyl, wherein (i) the molar quantity of 1,3-dibromo-5,5-dialkylhydantoin introduced is less than the molar quantity of N,N′-bromochloro-5,5-dimethylhydantoin that would be required to effect the same degree of microbiological control in that medium, (ii) the molar quantity of the 1,3-dibromo-5,5-dialkylhydantoin introduced releases an amount of “free chlorine” that is greater than the amount of “free chlorine” that would be released in that medium by an equimolar quantity of N,N′-bromochloro-5,5-dimethylhydantoin, and (iii) the amount of “free chlorine” released by the quantity of the 1,3-dibromo-5,5-dialkylhydantoin introduced is greater than the

Abstract: It is found out that compounds represented by the formula (I): 1

Abstract: The present invention provides a method of treating a visceral pain syndromes in a mammal. The method includes administering to the mammal an effective amount of a selective norepinephrine (NE)-serotonin (5-HT) reuptake inhibitor (NSRI), e.g., milnacipran.

Abstract: Microbiological control is achieved by continuously and inexpensively dosing water in contact with biofilm, or that comes into contact with biofilm, using a highly effective biocide that provides very effective microbiocidal control of planktonic microorganisms and of biofilm species, even where the biofilm infestations have been in existence for long periods of time and thus have encased themselves in a substantial quantity of slimy defensive polysaccharide layers or films. In addition, the biocide used makes possible significant reduction in copper and/or iron surfaces in contact with the water as compared to N,N′-bromochloro-5,5-dimethyl hydantoin. Still other advantages are made possible by the described technology.

Abstract: Combination therapy comprising RXR modulators and glucose reabsorption inhibitors useful for the treatment of diabetes and Syndrome X are disclosed.

Abstract: Peptide compositions and methods for inhibiting and controlling the growth of microbes using peptides possessing antimicrobial activity are described. The composition comprises at least one antimicrobial peptide in combination with at least one biocide, germicide, preservative or antibiotic. The method comprises administering an amount of the peptide composition effective for the prevention, inhibition or termination of microbes in industrial and clinical settings.

Abstract: Non-peptide somatostatin receptor ligands with conformationally restricted side chains exhibiting high binding affinity toward somatostatin receptors are provided. The compounds exhibit a high selectivity and act as agonists at human subtype 2 somatostatin receptors. The compounds are long acting for advantageous use as medicaments in peripheral diseases where somatostatinergic therapy is indicated. Furthermore, many of the compounds are lipophilic and are particularly useful for treating central nervous system and ophthalmic diseases where penetration of the blood brain and blood retinal barriers is required. It is a further object to describe the preferred stereoisomers of these somatostatin agonists and processes for their preparation. Further objects will become apparent from reading the following description.

Abstract: O-linked protein glycosylation of proteasome mediated by O-linked N-acetylglucosamine transferase (OGT) blocks proteasomal function. This blockade of proteasomal function results in accumulation of proapoptotic factors that lead to neuro-endocrine cell death in the pathogenesis of neurodegenerative diseases and diabetes. Thus, inhibiting OGT activity by structural analog of N-acetylglucosamine such as (Z)-1-[N-(3-Ammoniopropyl)-N-(n-propyl)amino]diazen-ium-1,2-diolate would provide new methods of preventing and/or treating late onset of Alzheimer's disease and diabetes.

Abstract: Novel diphenylethylene compounds and derivatives thereof containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. The compounds are disclosed as useful for a variety of treatments including the treatment of inflammation, inflammatory and immunological diseases, insulin resistance, hyperlipidemia, coronary artery disease, cancer and multiple sclerosis.

Abstract: The present invention provides a compound of formula (1), or pharmaceutical acceptable salts thereof wherein R1 is C4-12 alkyl, C4-12 alkenyl, C4-12 alkynyl, —(CH2)h-C3-8 cycloalkyl, substituted and unsubstituted —(CH2)h-aryl, substituted and unsubstituted-(CH2)h-het, R2 is substituted and unsubstituted C1-12 alkyl, substituted and unsubstituted C2-12 alkenyl, substituted and unsubstituted C2-12 alkynyl, substituted and unsubstituted-(CH2)h-C3-8 cycloakyl, substituted and unsubstituted —(CH2)h-C3-8 unsubstituted-(CH2)h-C3-8 cycloakyl, substituted and unsubstituted —(CH2)h-C3-8 cycloalkenyl, substituted and unsubstituted-(CH2)h-aryl, substituted and unsubstituted-(CH2)h-heterocyclic ring, substituted and unsubstituted —(CH2)i-X—R4 (X is —O—, —S(═O)j-, —NR7-, —S(═O)2NR8-, or —C(═O)—), and —(CH2)iCHR5R6.

Abstract: Enamine derivatives of formula (1) are described: wherein R1 is a group Ar1 L2Ar2Alk- in which Ar1 is an aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Cy is a cycloaliphatic or heterocycloaliphatic ring in which X is a N atom or a C(Rw) group; Rx is a oxo, thioxo, or imino group; Rw and Rz is each a hydrogen atom or optional substituent; provided that Cy is not a cyclobutenedione group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.

Abstract: The object of the present invention is to provide a microbicidal deodorant in a tractable liquid form that has excellent long-term storage stability.

Abstract: The compounds have a structure according to the following Formula (I): 1

Abstract: Therefore, it is critical that the roles these enzymes play in biological processes outside of extracellular matrix degradation or remodeling be understood in order to assess their potential as targets for therapeutic intervention, and to design safe, conveniently produced, orally active inhibitors.

Abstract: Compounds of formula (I) wherein R is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl or heterocyclyl; R1 is bicyclyl or heterobicyclyl; R2 is aryl, heteroaryl, heterocyclyl, alkoxy, alkyl, hydroxy or optionally substituted amino and n is from 0 to 3; with the provisos than when n is 0 R2 is alkyl or when n is from 1 to 3 R2 is not alkyl, are useful in the treatment and prophylaxis of conditions mediated by CD23 or TNF.

Abstract: Erodible, gastric-retentive dosage forms are provided that are formulated using the in vitro drug release profile obtained with USP Disintegration test equipment rather the USP Dissolution Apparatus. The invention is premised on the discovery that the USP Disintegration Test and modified versions thereof are far more predictive of the in vivo release profile for a controlled release dosage form than is the standard USP Dissolution Test, particularly controlled release dosage forms of the swellable, erodible type. The dosage forms generally comprise particles of a biocompatible, hydrophilic polymer having the active agent incorporated therein, wherein the particles are optionally but preferably compacted into a tablet or loaded into a capsule. The dosage forms can be used to deliver water-insoluble or sparingly soluble drugs as well as water-soluble drugs, providing that the latter are coated with a protective coating or contained in a protective vesicle.

Abstract: The present application describes novel hydantoin derivatives of formula (I): 1

Abstract: A highly stable liquid formulation having broad spectrum preservative properties which constitutes an admixture of an alkanol-substituted DMH, an iodopropynyl compound, a stabilizer of a hydantoin, urea or derivative thereof, and a hydroxyl solvent. Preferably the constituents are dimethyloldimethylhydantoin, 3-iodo-2-propynyl-butyl carbamate, dimethylhydantoin, and a glycol solvent. The preservative preferably has a total formaldehyde content of 5% and less than 0.2% of free formaldehyde. The composition is prepared by successively admixing the alkanol-substituted dimethyl-hydantoin and the stabilizer, the hydroxyl solvent, and the iodopropynyl compound. Also described is a stabilized iodopropynyl compound preferably containing dimethylhydantoin as the stabilizer.