Abstract: This invention relates to the design, synthesis and use of synthetic vitamin D and other steroidal analogs. It further relates to the therapeutic use of such analogs and their manufacture.

Abstract: A new and versatile class of cyclic diazodicarboxamides that reacts efficiently and selectively with phenols and the phenolic side chain of tyrosine through an Ene-like reaction is reported. This mild aqueous tyrosine ligation reaction works over a broad pH range and expands the repertoire of aqueous chemistries available for small molecule, peptide, and protein modification. The tyrosine ligation reactions are shown to be compatible with the labeling of native enzymes and antibodies in buffered aqueous solution. This reaction provides a novel synthetic approach to bispecific antibodies. This reaction will find broad utility in peptide and protein chemistry and in the chemistry of phenol-containing compounds.

Abstract: The present invention relates to a process using Grignard reagents for providing thio-triazolo group-containing compounds.

Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.

Abstract: The present invention relates generally to the use of biological or chemical control agents with for controlling insects and nematodes and to methods particularly useful for combating insects or nematodes and/or increasing crop yield in plants that are at least partially resistant to one or more parasitic nematodes or insects.

Abstract: The present invention relates to novel cyclic N,N?-diarylureas and N,N?-diarylthioureas—androgen receptor antagonists, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of cancerous diseases, among them prostate cancer.

Abstract: The present invention relates to a process using Grignard reagents for providing thio-triazolo group-containing compounds.

Abstract: A new and versatile class of cyclic diazodicarboxamides that reacts efficiently and selectively with phenols and the phenolic side chain of tyrosine through an Ene-like reaction is reported. This mild aqueous tyrosine ligation reaction works over a broad pH range and expands the repertoire of aqueous chemistries available for small molecule, peptide, and protein modification. The tyrosine ligation reactions are shown to be compatible with the labeling of native enzymes and antibodies in buffered aqueous solution. This reaction provides a novel synthetic approach to bispecific antibodies. This reaction will find broad utility in peptide and protein chemistry and in the chemistry of phenol-containing compounds.

Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituent

Abstract: The present invention relates to selective-herbicidal compositions, characterized in that they contain an effective amount of the compound 2-(2-trifluoromethoxy-phenylsulphonylarninocarbonyl)-4-methyl-5-methoxy-2,4-dihydro-3H-1,2,4-triazol-3-one of the formula (I) and/or of salts of the compound of the formula (I), and to the use of these compositions for the selective control of weeds in crops of cereals, in particular crops of wheat, and to methods for the selective control of weeds in crops of cereals by applying the compositions together with surfactants and/or customary extenders.

Abstract: It is desirable to provide a method for easily removing catalyst-derived impurities from a product of a reaction by the catalysis of a compound having a dicarboximide skeleton and thereby efficiently yielding a target compound with high purity. Disclosed is a method for producing an organic compound through a reaction of a substrate in the presence of a catalyst, the catalyst including a compound having a dicarboximide skeleton represented by following Formula (i): wherein R represents hydrogen atom or a hydroxyl-protecting group. The method includes the step of treating a reaction product with hot water so as to decompose and remove an impurity derived from the catalyst. The temperature of the hot water is preferably 100° C. or higher.

Abstract: Compounds of formula I, wherein R1, R2, R3, R4, R5, X, Y, and Ar are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.

Abstract: A process for preparing phenyl iso(thio)cyanates of the formula I in which a compound of the formula II or its HCl adduct is reacted with a phosgenating agent where W is oxygen or sulfur and Ar and A are as defined in claim 1 is described. Moreover, the invention relates to the use of the phenyl iso(thio)cyanates for preparing crop protection agents.

Abstract: The invention relates to processes for the preparation of compounds of general formula (I) and salts thereof: in which Q1 represents O, Q2 represents O, R1 represents —CH3, R2 represents —CH3, R3 represents —OCH3, and R4 represents —CH3.

Abstract: The present invention relates to selective-herbicidal compositions, characterized in that they contain an effective amount of the compound 2-(2-trifluoromethoxy-phenylsulphonylaminocarbonyl)-4-methyl-5-methoxy-2,4-dihydro-3H-1,2,4-triazol-3-one of the formula (I) and/or of salts of the compound of the formula (I), and to the use of these compositions for the selective control of weeds in crops of cereals, in particular crops of wheat, and to methods for the selective control of weeds in crops of cereals by applying the compositions together with surfactants and/or customary extenders.

Abstract: The invention relates to processes for the preparation of compounds of general formula (I) and salts thereof: in which Q1 represents O, Q2 represents O, R1 represents —CH3, R2 represents —CH3, R3 represents —OCH3, and R4 represents —CH3.

Abstract: The present invention relates to selective-herbicidal compositions, characterized in that they contain an effective amount of the compound 2-(2-trifluoromethoxy-phenylsulphonylaminocarbonyl)-4-methyl-5-methoxy-2,4-dihydro-3H-1,2,4-triazol-3-one of the formula (I) and/or of salts of the compound of the formula (I), and to the use of these compositions for the selective control of weeds in crops of cereals, in particular crops of wheat, and to methods for the selective control of weeds in crops of cereals by applying the compositions together with surfactants and/or customary extenders.

Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.

Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.

Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.

Abstract: The invention relates to novel substituted thiene-3-ylsulphonylamino(thio)carbonyl-triazolin(ethi)ones of the general formula (I) in which Q1, Q2, R1, R2 R3 and R4 are as defined in the description, except for prior-art compounds. The invention also relates to the preparation of the compounds, to their use as herbicides and to herbicidal compositions comprising the novel compounds.

Abstract: Aminocarbonyl-substituted thiensulfonylamino(thio)carbonyl-triazolin(ethi)ones, processes for their preparation and their use The invention relates to novel substituted thien-3-ylsulfonylamino(thio)carbonyl-triazolin(ethi)ones of the formula (I), in which Q1, Q2, R1, R2, R3, R4 and R5 are as defined in the description, and also to salts of compounds of the formula (I), to processes for their preparation and to their use as herbicides.

Abstract: It is desirable to provide a method for easily removing catalyst-derived impurities from a product of a reaction by the catalysis of a compound having a dicarboximide skeleton and thereby efficiently yielding a target compound with high purity. Disclosed is a method for producing an organic compound through a reaction of a substrate in the presence of a catalyst, the catalyst including a compound having a dicarboximide skeleton represented by following Formula (i): wherein R represents hydrogen atom or a hydroxyl-protecting group. The method includes the step of treating a reaction product with hot water so as to decompose and remove an impurity derived from the catalyst. The temperature of the hot water is preferably 100° C. or higher.

Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.

Abstract: 2-[Pyrazolyl- and triazolyl-3?-oxymethylene]phenylisoxazolones, -triazolones and -tetrazolones of formula I where: X is a group A, B or C, ?where # denotes the bond with the phenyl ring, Ra is hydrogen, halogen, alkyl or alkoxy, Rb is alkyl; Y is N or CRc, where Rc is hydrogen, halogen or alkyl; n is 0, 1, 2, 3 or 4, where the substituents R1 may be different if n is greater than 1; R1 is nitro, cyano, halogen, alkyl with or without substitution or alkoxy with or without substitution or is additionally, if n is 2, an optionally substituted 3 or 4 membered bridge which forms together with the ring to which it is attached a bicyclic partially unsaturated or aromatic radical; R2 is hydrogen, nitro, cyano, halogen, alkyl, haloalkyl, alkoxy, alkylthio or alkoxycarbonyl; R3 is optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted hetaryl, their preparation and their use for controlling unwanted animal pests or harmful fungi.

Abstract: Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent such as a cyano group; A is a substituent such as a 4-pyrazolyl or thiazolyl group; and B is a substituent such as an alkylcarbonyl group. Agricultural chemicals and agents for preventing the attachment of aquatic organisms containing one or more such ethylene derivatives.

Abstract: The invention relates to novel substituted benzoylcyclohexenones of the formula (I), in which n, A, R1, R2, R3, R4, Y and Z are each as defined in the description, and also to processes for their preparation and to their use as herbicides.

Abstract: The invention relates to novel substituted thien-3-yl-sulphonylamino(thio)carbonyl-triazolin(ethi)ones of the general formula (I) in which Q1, Q2, R1, R2, R3 and R4 are each as defined in the description, and to salts of the compounds according to formula (I), to processes and to novel intermediates for their preparation and to their use as herbicides.

Abstract: The invention relates to novel substituted benzoyl ketones of the formula (I) in which n represents 0, 1, 2 or 3, A represents a single bond or represents alkanediyl (alkylene), R1 represents hydrogen or represents in each case optionally substituted alkyl or cycloalkyl, R2 represents hydrogen, cyano, carbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkoxycarbonyl, alkylthio, alkylsulphinyl or alkylsulphonyl, R3 represents hydrogen, nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino, dialkylamino or dialkylaminosulphonyl, R4 represents nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino, dialkyiamino or dialkylaminosulphonyl, and Z represents an optionally substituted 4- to 12-membered, saturated or u

Abstract: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy.

Abstract: The invention relates to novel substituted aryl ketones of the general formula (I) in which n, A, R1, R2, R3, R4 and Z are each as defined in the description, to processes for their preparation and to their use as herbicides.

Abstract: The present invention relates to the derivatives of specially substituted azole compounds which have improved antifungal activity as compared with presently available agents in this class and the processes for the preparation thereof. This invention also relates to pharmaceutical preparations containing the compounds of the present invention and their use in treating and/or preventing the fungal infections in mammals, preferably humans.

Abstract: The invention relates to novel sulfonylamino(thio)carbonyl compounds of the formula (I), in which n represents the numbers 0, 1 or 2, A represents a single bond, or oxygen or sulfur, or the grouping N—R, in which R represents hydrogen, alkyl, alkenyl, alkinyl or cycloalkyl, Q represents oxygen or sulfur, R1 represents hydrogen or formyl, or represents respectively optionally substituted alkyl, alkoxy, alkylamino, alkoxyamino, dialkylamino, N-alkoxy-N-alkyl-amino, alkylcarbonyl, alkoxycarbonyl, alkylsulfonyl, alkenyl, alkinyl, cycloalkyl, cycloalkylcarbonyl or cycloalkylsulfonyl, R2 represents cyano or halogen, or represents respectively optionally substituted alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, dialkylaminosulfonyl, alkenyl, alkinyl, alkenyloxy or alkinyloxy, and R3 represents respectively optionally substituted heterocyclyl having 5 ring members of which at least one is oxygen, sulfur or nitrogen and from one to three further ring members can be nitrogen, an

Abstract: The invention relates to novel substituted benzoylcyclohexenones of the formula (I), 1

Abstract: The invention relates to novel substituted aryl ketones of the general formula (I) 1

Abstract: The invention relates to novel substituted N-aryl nitrogen-containing heterocyclic compounds of the general formula (I) 1

Abstract: The invention relates to novel substituted N-aryl nitrogen-containing heterocyclic compounds of the general formula (I) 1

Abstract: A process is described for preparing 1-aryltriazolinones of formula I useful in the production of commercial herbicides: by (i) carbonylating an amidrazone of formula (A) with one or more carbonylating agent, or by (ii) condensing a hydrazonoyl derivative of formula (A) with one or more ring-forming agent, wherein formula (A) is where W, X, Y, Z, and R1 are fully described herein. Preferred are those where W is halogen or —NHR where R is hydrogen or haloalkyl; X and Y are independently selected from hydrogen, chloro, or fluoro; Z is hydrogen, bromo, iodo, nitro, amino, or methylsulfonylamino; and R1 is methyl. Certain compounds of formula (A) are novel compositions of matter. The process as described herein has utility in providing compounds of formula I in unexpectedly high yield and purity.

Abstract: The present invention relates to compounds of formula I and to pharmaceutically acceptable salts, hydrates and prodrugs thereof, wherein R1, R2, R3, R4, R5, R10, R11, b, m, n, p and v are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and methods of treating hyperproliferative disorders in mammals by administering the above compounds.

Abstract: The invention relates to novel substituted heterocyclyl-2H-chromenes of the general formula (I) in which R1, R2, R3, R4, R5 Z are each as defined in the description, and to a process for their preparation and to their use as herbicides.

Abstract: A process is described for preparing 1-aryltriazolinones of formula I useful in the production of commercial herbicides: by (i) carbonylating an amidrazone of formula (A) with one or more carbonylating agent, or by (ii) condensing a hydrazonoyl derivative of formula (A) with one or more ring-forming agent, wherein formula (A) is where W, X, Y, Z, and R1 are fully described herein. Preferred are those where W is halogen or —NHR where R is hydrogen or haloalkyl; X and Y are independently selected from hydrogen, chloro, or fluoro; Z is hydrogen, bromo, iodo, nitro, amino, or methylsulfonylamino; and R1 is methyl. Certain compounds of formula (A) are novel compositions of matter. The process as described herein has utility in providing compounds of formula I in unexpectedly high yield and purity.

Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.

Abstract: The invention relates to novel substituted N-aryl nitrogen-containing heterocyclic compounds of the general formula (I) and to the compounds isomeric to the substituted N-aryl nitrogen-containing heterocyclic compounds of the formula (I), of the formulae (Ia) and (Ib) in which Q1, Q2, R1, R2 and Ar have the meanings given in the description, processes for their preparation and their use as herbicides.

Abstract: The invention relates to novel thienylsulphonylamino(thio)carbonyl compounds of the formula (I), in which Q represents oxygen or sulphur, R1 represents cyano, halogen or in each case optionally cyano-, halogen- or C1-C4-alkoxy-substituted alkyl, alkenyl, alkinyl, alkoxy, alkenyloxy or alkinyloxy having in each case up to 6 carbon atoms, R2 represents cyano, halogen or in each case optionally cyano-, halogen- or C1-C4-alkoxy-substituted alkyl, alkenyl, alkinyl, alkoxy, alkenyloxy or alkinyloxy having in each case up to 6 carbon atoms, and R3 represents in each case optionally substituted heterocyclyl having 5 ring members, at least one of which represents oxygen, sulphur or nitrogen and one to three others may represent nitrogen, and salts of compounds of the formula (I), to processes and novel intermediates for preparing the novel compounds and to their use as herbicides.

Abstract: &bgr;-sheet mimetics and methods relating to the same are disclosed. The &bgr;-sheet mimetics have utility as protease and kinase inhibitors, as well as inhibitors of transcription factors and protein-protein binding interactions. Methods of the invention include administration of a &bgr;-sheet mimetic, or use of the same for the manufacture of a medicament for treatment of a variety of conditions associated with the targeted protease, kinase, transcription factor and/or protein-protein binding interaction.

Abstract: The invention relates to new substituted phenyltriazolin(thi)one of the general formula (I), in which Q1, Q2, R1, R2, R3, R4 and R5have the meanings given in the description, and to a process for their preparation and to their use as herbicides.

Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula (T)xA—B—D—E—G wherein A is an aryl or heteroaryl rings; B is an aryl or heteroaryl ring or a bond; each T is a substituent group; x is 0, 1, or 2; the group D represents the group E represents a two or three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and the group G represents and with the proviso that when G is each of the substituents on E is an independent substituent; and include pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to novel heterocyclic compounds and their agronomically suitable salts, methods for the use of these compounds in controlling unwanted plant species, and the use of herbicidal compositions containing these compounds. In particular, the present invention pertains to substituted and unsubstituted triazoles, imidazoles and pyrazoles linked to a heterocyclic substituted benzene group. Such compounds are useful as pre-emergent and post-emergent herbicides.

Abstract: The present invention relates to the use of partly known N-aryl-1,2,4-triazolin-5-ones of the formula (I) in which A, R1, R2, R3, R4 and R5 are each as defined in the description for controlling animal pests.

Abstract: The invention relates to novel sulphonylamino(thio) carbonyl compounds of the formula (I), in which A represents a single bond, oxygen, sulphur or the group N—R, in which R represents hydrogen, alkyl, alkenyl, alkinyl or cycloalkyl, Q represents oxygen or sulphur, R1 represents hydrogen or formyl or represents in each case optionally substituted alkyl, alkenyl, alkinyl, alkylcarbonyl, alkoxycarbonyl, alkylsulphonyl, cycloalkyl, cycloalkylcarbonyl or cycloalkylsulphonyl, R2 represents cyano or halogen or represents in each case optionally substituted alkyl, alkenyl, alkinyl, alkoxy, alkenyloxy or alkinyloxy, and R3 represents in each case optionally substituted heterocyclyl having 5 ring members of which at least one is oxygen, sulphur or nitrogen and from one to three further ring members can be nitrogen, and salts of compounds of the formula (I), the previously known compounds 4,5-dimethoxy-2-(2,5-dimethoxy-phenylsulphonylaminocarbonyl)-2,4-dihydro-3H-1,2,4-triazol-3-one, 4,5-diethoxy-2-(2,5-dimetho