Abstract: In accordance with the present invention, there are provided novel chemical entities which have multiple utilities, e.g., as prodrugs of NSAIDs; as dual inhibitors of cyclooxygenase (COX) and 5-lipoxygenase (5-LO); as anticancer agents (through promoting apoptosis and/or inhibiting the matrix metalloproteinases (MMPs)), and the like. Invention compounds comprise a non-steroidal anti-inflammatory agent (NSAID), covalently linked to a hydroxamate. Invention compounds are useful for a variety of applications, such as, for example, treating inflammation and inflammation-related conditions; reducing the side effects associated with administration of anti-inflammatory agents; promoting apoptosis; inhibiting matrix metalloproteinases; and the like.

Abstract: A description is given of substituted 3-heteroaryl(amino- or oxy)pyrrolidin-2-ones of the formula (I), processes for preparing them, and their use as herbicides or as plant growth regulators.

Abstract: Compounds of formula (I) as defined herein, or a pharmaceutically acceptable salt, or an in-vivo-hydrolysable ester thereof, are useful as antibacterial agents. Processes for their manufacture and pharmaceutical compositions containing them are described.

Abstract: Disclosed are substituted heteroarylalkanoic acids acids of the following formula D-A-C(O)R′, where D, A, and R′ are defined herein. These compounds are useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.

Abstract: A process for preparing a heteroaromatic compound having a heteroaromatic nucleus substituted with one or more ether groups comprising the step of: condensing at least one hydroxy-group of a compound having said heteroaromatic nucleus, said at least one hydroxy group (—OH) being substituted at &agr;- or &bgr;-positions with respect to a heteroatom of said heteroaromatic nucleus, with an alcohol containing one or more primary or secondary alcohol groups, optionally substituted with nitro, amide, ester, halogen, cyano or (hetero)aromatic groups, using the redox couple of a triaryl- or trialkylphosphine and an azodioxo-compound at a temperature between −40° C. and 160° C.

Abstract: A NK1 antagonist having the formula (I), 1

Abstract: Novel compounds are disclosed which inhibit the activity of phospholipase enzymes in a mammal, particularly cytosolic phospholipase A2. Pharmaceutical compositions comprising such compounds and methods of treatment using such compositions are also disclosed.

Abstract: The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.

Abstract: This invention is directed to lipoxin A4 analogs of the following formula (I) and (II): 1

Abstract: A peroxisome proliferator activated receptor regulator containing a compound of formula (I) (wherein all symbols are as defined in the specification), or a salt thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diabetes or syndrome X.

Abstract: Described herein are compounds related to lactacystin and lactacystin &bgr;-lactone, pharmaceutical compositions containing the compounds, and methods of use.

Abstract: This invention relates aryl substituted thiazolidinones of Formula I: 1

Abstract: A compound of the formula: 1

Abstract: Heterocyclic substituted compounds having the general structure: which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes.

Abstract: Zwitterionic imide compounds are provided according to the formula: R1—SO2—N−—SO2—R2+, where R1 and R2+are any suitable groups. Typically R1 is a highly fluorinated alkane and R2+contains a quaternary ammonium group or a heteroatomic aromatic group having an cationic nitrogen, such as: pyridiniumyl, pyridaziniumyl, pyrimidiniumyl, pyraziniumyl, imidazoliumyl, pyrazoliumyl, thiazoliumyl, oxazoliumyl, or triazoliumyl. Zwitterionic liquids are provided, typically having melting points of less than 100 ° C. and typically having a solubility in water of less than 5% by weight.

Abstract: This invention relates to compounds having the Formula I: 1

Abstract: The invention relates to novel substituted heteroaryloxyacetanilides of the general formula (I), in which n, R, X, and Z are to intermediates for their preparation and to their use as herbicides.

Abstract: The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazolidinedione analogs that have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds that have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester-containing thiazolidinedione analogs are also taught.

Abstract: This invention relates to monoalkyl phosphoric esters, dialkyl phosphoric esters, and, in small amounts, trialkyl phosphoric esters or salts thereof, which are preferably based on &bgr;-branched fatty alcohols, particularly Guerbet alcohol, which are effective in lowering the surface tension of both polar and also nonpolar liquids, and which have high stability, even at elevated temperatures, and low sensitivity to electrolytes and acids. The invention further relates to the use of such mixtures as emulsifiers in cosmetic and pharmaceutical formulations, and to the resulting products.

Abstract: This invention relates to a process for the production of an aryl thiol, which comprises hydrogenating an aryl sulfonyl chloride in a solvent in the presence of a palladium catalyst and a base whose conjugate acid has a pKa of about 2 or greater, wherein the base is selected from the group consisting of ionic bases soluble in water and tertiary amines soluble in the solvent, the tertiary amines not having a methyl group attached to the amine nitrogen.

Abstract: The present invention relates to intermediate thiazole compounds and a process for preparing 2-chloro-5-chloromethylthiazole which is a known compound useful for the preparation of insecticides.

Abstract: The invention relates to epothilone analog represented by formula (I) wherein (i) R2 is absent or oxygen; “a” can be either a single or double bond; “b” can be either absent or a single bond; and “c” can be either absent or a single bond, with the proviso that if R2 is oxygen then “b” and “c” are both a single bond and “a” is a single bond; if R2 is absent then “b” and “c” are absent and “a” is a double bond; and if “a” is a double bond, then R2, “b” and “c” are absent; R3 is a radical selected from the group consisting of hydrogen; lower alkyl; —CH═CH2; —C≡CH; —CH2F; —CH2Cl; —CH2—OH; —CH2—O—(C1-C6-alkyl); and —CH2—S—(C1-C6-alkyl); R4 and R5 are independently selected from hydrogen, methyl or a protecting group; and R1 is as defined in the specification, or a salt of a compound of formu

Abstract: This invention relates to the synthesis of certain complexes of cysteine, N-acetylcysteine, N-(2-mercaptopropionyl)glycine, and L-2-oxothiazolidine-4-carboxylate and to the nutritional use of these and other related individual or complexed thiol-contributing glutathione predecessors. Clinical uses for these molecules and complexes in the beneficial modification of various physiological conditions and functions associated with aging, chronic glaucoma, diabetes mellitus, insulin resistance, macular degeneration, neurodegenerative diseases and vasoconstriction are described in particular.

Abstract: Thiazole esters are suitable for detecting the presence of leukocytes in urine. Such thiazole esters are suitable for use in compositions, diagnostic devices, and methods for detecting the presence of leukocytes. A thiazole ester of the invention is of the formula: or a salt or solvated salt thereof, in which A is an N-blocked amino acid residue or N-blocked peptide chain, preferably an alanine residue or polyalanine chain; and R1 and R2 are each independently hydrogen, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted alkoxy, amino, unsubstituted or substituted acyl, halo, nitro, cyano, —SO3H, or hydroxy, with the proviso that R1 and R2 are not both hydrogen. In one embodiment, at least one of R1 and R2 is methoxy, ethoxy, propoxy, or butoxy. In still another embodiment, R1 is hydrogen and R2 is methoxy, ethoxy, propoxy, or butoxy.

Abstract: The present invention provides compounds of Formula I shown below. The present invention also provides methods of treating or preventing 3 inflammation or atherosclerosis, and a pharmaceutical composition that contains a compound of Formula I.

Abstract: Novel benzotriazoles of the formula in which R, X1, X2, X3, X4 and Y have the meanings given in the description, and their acid addition salts and metal salt complexes, a process for the preparation of these substances and their use as microbicides in crop protection and in material protection.

Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; 1

Abstract: Compounds, compositions and methods are provided that are useful in the treatment of chemokine receptor-mediated conditions and diseases. In particular, the invention provides compounds which modulate CCR4 function or a CCR4-mediated response. The subject compounds and compositions are useful for the treatment or prevention of inflammatory conditions and diseases.

Abstract: Disclosed are compounds of the Formula I wherein: Z is C or nothing, provided that when Z is nothing, R3 and R4 are nothing; A is S, S═O or O═S═O; R1 and R2 are independently hydrogen, lower alkyl, halogen, hydroxy or lower alkoxy, (un)substituted aryl, (un)substituted arylalkyl, (un)substituted heteroaryl or(un)substituted heteroarylakyl; R3 and R4 independently represent hydrogen, lower alkyl, cycloalkyl, aminoalkyl, mono- or dialkylaminoalkyl, (un)substituted aryl or (un)substituted heteroaryl; R5 represents a (un)substituted carbocyclic group containing from 3-7 members, up to two of which members are optionally hetero atoms; or R5 is (CR6R7)—(CH2)n—XR8R9; X is S or N; R6, R7, R8, R9, and n are as defined in the specification. The compounds are useful in the treatment and prevention of the AIDS virus. Intermediates useful in the preparation of the final products, pharmaceutical compositions containing the final products are also taught.

Abstract: The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTP&agr;, LAR and HePTP or the like.

Abstract: Thiazolidinedione compounds, compositions, and methods of inhibiting telomerase activity in vitro and treatment of telomerase mediated conditions or diseases ex vivo and in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of conditions or diseases mediated by telomerase activity, such as in the treatment of cancer. Also disclosed are methods for assaying or screening for inhibitors of telomerase activity.

Abstract: This invention relates to a process for the Heck coupling reaction where heterogeneous palladium catalysts are used to activate aryl halides for a carbon-carbon coupling with olefins in the presence a base and an aprotic solvent to produce aryl-olefin compounds. The process, in particular, provides for the use of aryl chlorides substituted with electron-withdrawing or electron-donating group for the cross coupling with olefins.

Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.

Abstract: Compound represented by the structural formula 1

Abstract: The present invention provides a compound of the formula: and methods for using the same, wherein R1, R2, R3, R4 and X are those defined herein.

Abstract: 3-(Substituted phenyl)-5-(substituted heterocyclyl)-1,2,4-triazole compounds are useful as insecticides and acaricides. New synthetic procedures and intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects and mites using the compounds are also provided.

Abstract: This invention provides compounds of Formula I having the structure wherein: A, X, Y, Z, R1, R2, R3, R4, R5, and R6 are as defined hereinbefore or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.

Abstract: The present invention describes novel nitrosated and/or nitrosylated H2 receptor antagonist compounds, and novel compositions comprising at least one H2 receptor antagonist compound that is optionally substituted with at least one NO and/or NO2 group, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase. The present invention also describes methods for treating and/or preventing gastrointestinal disorders; improving gastroprotective properties of H2 receptor antagonists; decreasing the recurrence of ulcers; facilitating ulcer healing; preventing and/or treating inflammations and microbial infections, ophthalmic diseases and disorders, multiple sclerosis, and viral infections; and decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds.

Abstract: The present invention relates to a compound of the formula (I) 1

Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.

Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Abstract: Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.

Abstract: The Invention relates to a process for the preparation of a compound of the formula wherein Q, Y, Z, R1, R2, R3, R4 and R5 are as defined in the specification, which comprises a) reacting a compound of the formula  with a halogenating agent to form a compound of the formula b) converting a compound of formula (II) by means of a halogenating agent into a compound of the formula  optionally c) converting the compound of formula (IV) into a compound of formula (III); d) converting a compound of formula (III) by means of a compound of the formula e) converting a compound (IV) by means of a compound (V) into a compound (VI); and f) converting a compound (VI) by means of a chlorinating agent into a compound (I); a compound (IV); to a process for the preparation of a compound (III) and to a process for the preparation of a compound (IV).

Abstract: The present invention is concerned with novel pharmaceutical compositions of lipid lowering agents which can be administered to a mammal suffering from hyperlipidemia, obesitas or atherosclerosis, whereby a single such dosage form can be administered once daily, and in addition at any time of the day independently of the food taken in by said mammal. These novel compositions comprise particles obtainable by melt-extruding a mixture comprising a lipid lowering agent and an appropriate water-soluble polymer and subsequently milling said melt-extruded mixture.

Abstract: Compounds of the formula: 1

Abstract: A novel 3-hydroxypyridin-4-one compound of formula I is provided wherein R is hydrogen or a group that is removed by metabolism in vivo to provide the free hydroxy compound, R1 is an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by a hydroxy group or a carboxylic acid ester, sulpho acid ester or a C1-6 alkoxy, C6-aryloxy or C7-10aralkoxy ether thereof, R3 is selected from hydrogen and C1-6alkyl; and R4 is selected from hydrogen, C1-6alkyl and a group as described for R2; characterised in that R2 is selected from groups —CONH—R5  (i) —CH2NHCO—R5  (ii) —SO2NH—R5  (iii) —CH2NHSO2—R5  (iv) —CR6R6OR7  (v) —CONHCOR5  (viii)  wherein R5 is selected from hydrogen and optionally hydroxy, alkoxy, or aralkoxy substituted C1-13 alkyl, aryl and C71-13 aralkyl, R6 is independently selected from hydrogen, C1-13 alkyl, aryl and C7-13 aralkyl,

Abstract: This invention relates to novel N-heteorocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and neurodengenerative diseases, for treating alopecia and promoting hair growth, for treating vision disorders and/or improving vision, and for treating memory impairment and/or enhancing memory performance by administering such compounds.

Abstract: A compound represented by the formula (I) or its salt and herbicidal and desiccant use thereof: wherein X, Y are independently hydrogen, halogen, cyano, nito, or (C1-6)haloalkyl; Z is oxygen or sulfur; and

Abstract: A triazole compound having the formula: wherein Ar1 represents a phenyl group which may be substituted, Ar2 represents a heterocyclic group which may be substituted, R0 represents a hydrogen atom or a lower alkyl; R1 represents a lower alkyl; R2 to R5 each represent a hydrogen atom or an unsubstituted or halo substituted alkyl; n represents 0 to 2; p represents 0 or 1; q, r and s each represent 0 to 2; A represents a 4- to 7-membered carbon ring or a 4- to 7-membered heterocyclic group. The compound of the present invention exhibits an excellent antifungal activity.

Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.