Abstract: The present invention relates to tyrosine-specific functionalized insulin analogs and processes of making such tyrosine-specific functionalized insulin analogs using R-3H-1,2,4-triazoline-3,5-(4H)diones (PTAD).

Abstract: Systems and methods are provided for generating a print job archive optimized for searching by a specific server. The system includes a memory and an indexing controller. The indexing controller generates an archive for print jobs, by determining a number of Central Processing Unit (CPU) cores that access the archive, and generating table files in the archive equal to the number of CPU cores. The indexing controller also populates the archive by detecting print jobs, generating records that describe the print jobs, and distributing the records such that each table file includes a different set of records. Further, the indexing controller searches the archive by triggering multiple processing threads that each utilize a different CPU core to review a different table file of the archive based on the search request, and reporting a set of records in the archive that match the request.

Abstract: Quantification of vitamin D2, vitamin D3, and the monohydroxy and diihydroxy metabolites of vitamin D2 and vitamin D3, can comprise labeling analytes with mass spectrometry (MS) tagging reagents and performing LC-MSMS analysis of the labeled analytes. The labeled analytes can include a labeled standard and can have distinct retention times on a reversed phase column, as well as distinct masses. Under high energy collisions, reporter groups can be generated. The intensity or the peak area detected for each reporter group can be used for quantitation. In some embodiments, a one-step tagging reagent is used that is a dienophile-containing, labeled m Diels Alder reagent.

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: The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders.

Abstract: The present disclosure features a strain-promoted [2+2+2] reaction that can be carried out under physiological conditions. In general, the reaction involves reacting a pi-electrophile with a low lying LUMO with a quadricyclane on a biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo and in vitro. The reaction is compatible with modification of living cells. In certain embodiments, the pi-electrophile can comprise a molecule of interest that is desired for delivery to a quadricyclane-containing biomolecule via [2+2+2] reaction.

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: Providing a novel control agent for soft rot and a novel control method for the same. A compound having no antibacterial activity against Erwinia carotovora but having a control activity against fungi on soil surface, specifically containing, as the active ingredient, a fungicide comprising any of a strobilurin compound such as azoxystrobin and kresoxim-methyl, an azole compound such as triflumizol, cyazofamid, amisulbrom, and thiophanate-methyl, a carboxamide compound such as penthiopyrad and boscalid, a sulfonamide compound such as flusulfamide, an organic chlorine compound such as chlorothalonil, a dicarboximide compound such as pro-cymidone and iprodione, a phenylpyrrole compound such as fludioxonil, an anilinopyrimidine compound such as mepanipyrim, and a guanidine compound such as iminoctadine is the control agent for plant soft rot, which is applied to plant cultivation soil.

Abstract: The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders.

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 provides compounds of formula (I), or pharmaceutically acceptable derivatives thereof wherein the variables Z, Q, Ring A, V, X, Y and Y? are as defined herein, and pharmaceutical compositions comprising these compounds. The compounds of formula (I) and pharmaceutical compositions comprising them are useful for treating a disorder for which a V1a antagonist is indicated, in particular, dysmenorrhoea.

Abstract: The invention relates to triazole salts, to their preparation and to applications thereof. The salts have at least one anionic triazolium group which carries at least one chlorosulphonyl, fluorosulphonyl or alkoxyfluorosulphonyl group, each of the anionic groups being combined with a proton or a cation that has a valency of less than or equal to 4. The salts are useful as synthesis reagents, as chemical-reaction or polymerization catalysts, and as ion-conducting materials for electrochemical generators, supercapacitors and electrochromic devices.

Abstract: The invention relates to triazole salts, to their preparation and to applications thereof. The salts have at least one anionic triazolium group which carries at least one chlorosulphonyl, fluorosulphonyl or alkoxyfluorosulphonyl group, each of the anionic groups being combined with a proton or a cation that has a valency of less than or equal to 4. The salts are useful as synthesis reagents, as chemical-reaction or polymerization catalysts, and as ion-conducting materials for electrochemical generators, supercapacitors and electrochromic devices.

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 triazole salts, to their preparation and to applications thereof. The salts have at least one anionic triazolium group which carries at least one chlorosulphonyl, fluorosulphonyl or alkoxyfluorosulphonyl group, each of the anionic groups being combined with a proton or a cation that has a valency of less than or equal to 4. The salts are useful as synthesis reagents, as chemical-reaction or polymerization catalysts, and as ion-conducting materials for electrochemical generators, supercapacitors and electrochromic devices.

Abstract: Methods and kits which utilize a conjugate, preferably an adduct, of ergosterol for determining the presence or level of a broad spectrum of ergosterol-containing organisms (e.g., fungi) in various substrates are disclosed. These methods and kits can be used to accurately and efficiently diagnose a subject having a fungal infection, particularly invasive fungal infection, and to accurately and efficiently detect the presence of fungi and other ergosterol-containing organisms in other substrates. Antibodies and other compounds (e.g., molecularly imprinted polymers) that are capable of selectively binding to ergosterol or to an ergosterol-containing conjugate and methods of producing same are also disclosed.

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: 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: 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: 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: 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: Bisimino-substituted phenyl compounds of the formula I where the substituents have the following meanings: X is a group A or B  where # denotes the bond with the phenyl ring and Ra is halogen, alkyl or alkoxy; Y is halogen, alkyl, haloalkyl or alkoxy; n is 0, 1 or 2, it being possible for the radicals Y to be different if n=2; R1 is alkyl; R2 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl; R3 is hydrogen, alkyl, haloalkyl or substituted or unsubstituted phenyl; R4 is ═CRbRc or ═N—ORd where Rb, Rc independently of one another are hydrogen, alkyl or substituted or unsubstituted phenyl; and Rd is one of the radicals mentioned under R2. Processes and intermediates for their preparation, and their use.

Abstract: Triazolone derivatives represented by the formula wherein R1 represents optionally substituted C1-10 alkyl, A1—L1—, A1—ON═CA2, etc.; R2 represents hydrogen, C1-6 alkyl, etc.; R3 represents C1-6 alkoxy, etc.; one of T, U, and V represents CR4, another represents CH or nitrogen, and the remaining one represents CR5 or nitrogen; and W represents CR6 or nitrogen.

Abstract: Compounds of formula 1 wherein: Y signifies halogen, C1-C4-alkoxy, C1-C4-alkylthio or hydroxy; R1 signifies methyl, ethyl or cyclopropyl; R2 signifies C1-C6-alkyl or C1-C6-alkyl substituted by 1 to 5 fluorine atoms; R3 is C1-C6-alkyl, C1-C6-alkoxy, C3-C6-cycloalkyl, C3-C6-cycloalkoxy, C2-C6-alkenyl, C2-C6-alkenyloxy, C2-C6-alkinyl, C2-C6-alkinyloxy, C1-C6-alkoxycarbonyl or CN, whereby, with the exception of CN, the above-mentioned groups may be substituted by identical or different substituents; or R3 is aryl, heteroaryl, heterocyclyl, aryloxy, heteroaryloxy or heterocyclyloxy, whereby the above-mentioned groups may be substituted by identical or different substituents, R5 signifies hydrogen or methyl; have microbicidal, insecticidal and acaricidal activity and may be used to control insects and plant-pathogenic fungi in agriculture, horticulture and in the field of hygiene.

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: A process for preparing alkoxytriazolinones of general formula (1): in which R1 and R2 independently represent an alkyl group, an aryl group, an arylalkyl group or cycloalkyl group. The alkoxytriazolinones are prepared by reacting, in a first stage, water-dissolved iminocarboxylic acid diesters in the presence of a mineral acid or by reacting a mixture of water with a water-miscible polar organic solvent and a carboxylic acid ester, yielding hydrazine carboxylic acid ester; and in a second stage, by further reacting the thus obtained reaction product with an amine, a polar organic solvent or mixtures thereof in the presence of water.

Abstract: The present invention relates to a process for manufacturing substituted triazolinones, which are intermediates in the preparation of herbicidally active compounds. In particular, this invention relates to the reaction of an isothiocyanate with an alkanol to produce a thionocarbamate intermediate product; alkylation of the intermediate product, reaction of the alkylated intermediate with and alkoxycarbobyl or aryloxycarbonyl hydrazine and reaction of the resultant compound with a base to produce a substituted triazolinone. In this context the terms “alkanol” and “alkylation” represent generic terms and thus, include the use of alkanols and alkylating agents having an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkylalkyl group, an aryl group or an arylalkyl group.

Abstract: 2-[1′,2′,4′-Triazol-3′-yloxymethylene]anilides of the formula I where the index and the substituents have the following meanings: n is 0, 1, 2, 3, or 4; X is a direct bond, O or NRa; Ra is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl; R1 is nitro, cyano, halogen, unsubstituted or substituted alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy or alkynyloxy; R2 is hydrogen, nitro, cyano, halogen, alkyl, haloalkyl, alkoxy, alkylthio or alkoxycarbonyl; R3 is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, heteocyclyl, aryl or heteroaryl; R4 is hydrogen, unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkylcarbonyl or alkoxycarbonyl; R5 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, processes and intermediates for their preparation and their use are described.

Abstract: The invention relates to novel arylalkyl compounds of the general formula (I) in which m represents the numbers 0 to 5, n represents the numbers 0 to 4, Q represents O, S, SO or SO2, R1 represents hydrogen or optionally substituted alkyl, R2 represents hydrogen or optionally substituted alkyl, X represents hydroxyl, mercapto, amino, hydroxyamino, nitro, formyl, carboxyl, cyano, carbamoyl, thiocarbamoyl, halogen, or represents an in each case optionally cyano-, halogen- or alkoxy-substituted radical from the series alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino, dialkylamino, alkylcarbonyl or alkoxycarbonyl, Y represents nitro, carboxyl, cyano, carbamoyl, thiocarbamoyl, halogen, or represents an in each case optionally cyano-, halogen- or alkoxy-substituted radical from the series alkyl, alkoxy, alkylthio, alkylsulphinyl or alkylsulphonyl, and Z represents one of the groupings below in which R3, R4, R5, R6 and R7 are each as defined in the desc

Abstract: The present invention relates to a process for manufacturing substituted triazolinones, which are intermediates in the preparation of herbicidally active compounds. In particular, this invention relates to the alkylation of a non-alkylated triazolinone intermediate product, wherein the improvement comprises conducting the alkylation reaction under pH controlled conditions. In a preferred embodiment, the invention relates to the preparation of a 5-alkoxy(or aryloxy)-2,4-dihydro-3H-1,2,4-triazol-3-one, and the alkylation of this non-alkylated triazolinone intermediate product, to produce a 5-alkoxy(or aryloxy)-4-alkyl-2,4-dihydro-3H-1,2,4-triazol-3-one.