Abstract: There are provided an aromatic monoamine derivative having a fluorene structure-containing organic group and an aromatic hydrocarbon group-containing organic group, and an organic electroluminescent element containing an organic thin film layer composed of a single layer or plural layers while including at least a light emitting layer, the organic thin film layer being between a cathode and an anode, wherein at least one layer of the organic thin film layer, particularly a hole transport layer, contains the aromatic amine derivative alone or as a component of a mixture. An organic electroluminescent element which maintains high luminous efficiency even if exposed to a high temperature environment, and has a low driving voltage and a long emission lifetime, and an aromatic amine derivative capable of realizing the organic electroluminescent element are provided.

Abstract: A novel serine racemase inhibitor exhibits sufficient activity and specificity. The serine racemase inhibitor includes one or more compounds selected from compounds respectively represented by the following general formulas [MM_1], [DR_1], [DR?_1], [LW_1], and [ED_1] as an active ingredient.

Abstract: Provided is a screening method for a more effective Ras inhibitor. Further provided are amino acid residues at a site important for an interaction with a Ras inhibitor in a Ras polypeptide. By confirming a difference between structural information on the Ras polypeptide by NMR and structural information between a complex of the Ras polypeptide and a seed compound by NMR, a more effective lead compound than the seed compound can be selected. As a result of analysis based on the structural information on the Ras polypeptide by NMR, the amino acid residues capable of interacting with a Ras inhibitor candidate (a) are K5, E37, D38, S39, L56, E63, Y64, A66, M67, Q70, Y71, R73, and T74 with reference to an amino acid sequence set forth in SEQ ID NO: 1.

Abstract: The present invention provides a compound having a salty taste enhance activity, and a salty taste enhancer containing the compound, and the like. The present invention relates to a salty taste enhancer for a food or drink, which contains a compound represented by the following formula: wherein each symbol is as defined in the specification, or an edible salt thereof.

Abstract: Provided herein are small molecule inhibitors of Taspase1 and methods of using the small molecule inhibitors of Taspase1 to treat neoplasm in subjects in need thereof.

Abstract: The present invention relates to a method of making asymmetrical bis(thiosemicarbazones), compounds useful as synthetic intermediates in the method, new bis(thiosemicarbazones) that can be readily accessed by use of the method and methods of treatment and imaging utilising some of the new bis(thiosemicarbazones).

Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.

Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.

Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.

Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.

Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.

Abstract: Fuels, especially hydrocarbon fuels, and lubricants, especially lubricating oils, contain dithiocarbamyl ?-hydroxy fatty acid esters, a class of anti-corrosion, anti-wear, anti-fatigue, and extreme pressure additives that are derived from epoxidized fatty acid esters. The additives exhibit synergistic anti-wear activity in combination with phosphorus containing additives.

Abstract: The present invention provides compounds of Formula I: wherein Ar1 is aryl or heteroaryl, Ar2 is aryl or heteroaryl, and R is a suitable organic group. Herbicidal composition comprising such active compounds, and methods for controlling undesirable plants by applying such compounds, are also described.

Abstract: Compositions containing surfactant compounds according to formula (I) ROCH2CH(OH)CR1R2ZCR1R2CH(OH)CH2OR,??(I) wherein Z is S, SO, or SO2, can have a range of equilibrium and/or dynamic surface tensions and a range of foaming performance attributes, depending upon the particular values of Z, R, R1, and R2. The compounds of formula (I) may be prepared by a process that includes reaction of a sulfide source such as a metal sulfide or bisulfide with an alkyl glycidyl ether.

Abstract: The present invention relates to thio semicarbazone and semicarbazone inhibitors of cysteine proteases and methods of using such compounds to prevent and treat protozoan infections such as trypanosomiasis, malaria and leishmaniasis. The compounds also find use in inhibiting cysteine proteases associated with carcinogenesis, including cathepsins B and L.

Abstract: Reagents and methods are provided for crosslinking and immobilizing biomolecules, drugs and synthetic polymers. The reagents possess (i) a thiol or amino reactive group; and (ii) a hydrazino or oxyamino moiety. Conjugates and immobilized biomolecules are also provided.

Abstract: Reagents and methods are provided for crosslinking and immobilizing biomolecules, drugs and synthetic polymers. The reagents possess (i) a thiol or amino reactive group; and (ii) a hydrazino or oxyamino moiety. Conjugates and immobilized biomolecules are also provided.

Abstract: Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the “good” cholesterol and as such may be useful for treating diseases such as atherosclerosis.

Abstract: Halogenated derivatives of two synthetic anti-tuberculosis agents, thioacetazone and p-aminosalicylic acid, have been synthesized. In general, the halogenated compound has the structure of Structure I: wherein X1 is a halogen and X2 is a second halogen or hydrogen, and Y is sulfur or oxygen; or, has the structure of Structure IV: wherein X1 is a halogen and X2 is a second halogen or hydrogen. Alternatively, the halogenated compounds may be pharmaceutically acceptable salts of these compounds. These halogenated derivatives possess anti-mycobacterial activity and are particularly useful for the treatment of Mycobacterium tuberculosis infections. In particular, fluorinated analogs of thioacetazone and p-amino-salicylic acid have been synthesized for use as anti-tuberculosis therapeutic agents either alone or in combination with other conventional anti-tuberculosis therapeutic agents.

Abstract: The present invention relates to novel, non-peptidic small organic compounds having an affinity for cyclophilin (CyP)-type immunophilin proteins. In the compounds of this invention, at least two carbo- or heterocyclic groups are attached to a central saturated, partially saturated, or aromatic 5-6 membered carbocyclic ring by a combination of straight or branched linker chains. The invention further relates to pharmaceutical compositions comprising one or more of the said compounds, and to the uses of these compounds and compositions for binding CyP-type proteins, inhibiting their peptidyl-prolyl isomerase activity, and for research, development, and therapeutic applications in a variety of medical disorders, such as neurological disorders, hair loss disorders, ischemic disorders, and disorders caused by viral or protozoan infection.

Abstract: According to a novel process, it is possible to prepare triazolinethione derivatives of the formula in which R1 and R2 are each as defined in the description by a) reacting hydrazine derivatives of the formula  or their acid addition salts with an inorganic or organic acid with thiocyanate of the formula Y-SCN  (III)  in which Y represents sodium, potassium or ammonium in the presence of a diluent and, if appropriate, in the presence of a catalyst and b) reacting the resulting thiosemicarbazide derivatives of the formula  with formic acid, if appropriate in the presence of a catalyst and if appropriate in the presence of a diluent. The thiosemicarbazide derivatives of the formula (IV) are novel.

Abstract: Compounds of the formula: are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpes virus.

Abstract: Radionuclide chelating compounds are provided for conjugation to targetting molecules such as proteins, peptides or antibodies. The resulting labelled targetting molecules may be used in diagnosis and therapy.

Abstract: Linker compounds for formation of stably-linked conjugates are disclosed. Such linker compounds are semicarbazide-containing linker compounds useful in forming conjugates having stable semicarbazone linkages. The stably-linked conjugates have utility in a variety of immunodiagnostic and separation techniques.

Abstract: A method for producing 3-amino-5-mercapto-1,2,4-triazole, useful as an intermediate compound for a medicine or pesticide, or the intermediate thereof, a salt of N-guanidino thiourea from aminoguanidine thiocyanate or a thiocyanate and an aminoguanidine compound in the presence of an acid in a polar solvent, or even from hydrazine and cyanamide is disclosed.

Abstract: This invention relates to chelating agents useful for coupling metal ions to biologically active molecules. In particular, substantial thioureas for chelating metals such as technetium are provided that can be conjugated to a targeting molecule such as an antibody, a peptide or a protein.

Abstract: Therapeutic compounds having the formula: ##STR1## in which R.sub.2 and R.sub.3 independently denote H, C.sub.1 -C.sub.4 alkoxy or OH and (A, B)=(oxygen, oxygen) in which case one out of R and R.sub.1 denotes OH, halogen, secondary amino or tertiary amine and the other denotes NHNHCONHR.sub.4 or R and R.sub.1 together denote .dbd.N--NH--CX--NHR.sub.5, .dbd.N--NH--CX--N(phenyl).sub.2, .dbd.N--NH--CX--NH--NH--R.sub.5, .dbd.N--NH--C(SCH.sub.3).dbd.N--R.sub.6 or .dbd.N--N.dbd.C(SCH.sub.3)--NH--R.sub.6 ; or (A, B)=(N--OH, oxygen) in which case R and R.sub.1 together form .dbd.N--NH--CX--NHR.sub.5 or .dbd.N--NH--CX--N(phenyl).sub.2 ; or (A, B)=(N--NH--CX--NHR.sub.5, oxygen) in which case R and R.sub.1 together form .dbd.N--NH--CX--NHR.sub.5 ; or (A, B)=(N--OH, N--OH) in which case R and R.sub.1 together form .dbd.N--NH--CX--NHR.sub.5 or .dbd.N--NH--CX--N(phenyl).sub.2.

Abstract: A method for producing 3-amino-5-mercapto-1,2,4-triazole, useful as an intermediate compound for a medicine or pesticide, or the intermediate thereof, a salt of N-guanidino thiourea from aminoguanidine thiocyanate or a thiocyanate and an aminoguanidine compound in the presence of an acid in a polar solvent, or even from hydrazine and cyanamide is disclosed.

Abstract: The present invention relates to a hydrazinecarboxamide derivative of the general formula (I) shown below: ##STR1## wherein the substituents are as defined in the specification, which has a wide insecticidal spectrum at a low dosage, a process for producing said derivative, and utilization of said derivative as an insecticide.

Abstract: This invention relates to the preparation and use of novel open-chain or cyclic polypeptide constructs in which two or more polypeptide chains, in an open-chain construct, or one or more chains, in a cyclic construct, are chemically derivatized such that the resulting construct exhibits both metal-binding capability and tissue-, organ- or cell-targeting selectivity. In particular, the polypeptide constructs of the present invention comprise compounds of the formula (I): ##STR1## in which, "B" is a hydrocarbon backbone, "P" is a polypeptide capable of targeting particular cells, tissues or organs of the body, "A" may be the group --NR'--NR"-- or the group --NR'--NR"--L-- in which L may be an aliphatic or aromatic linker group, R, R' and R" may be the same or different and may be hydrogen or an aliphatic group, m is an integer .gtoreq.2, provided that the groups R, R', R', L and "P" of a given chain may be the same or different from the groups R, R', R", L and "P" of another chain, n is an integer .gtoreq.

Abstract: Compounds having the structural formula ##STR1## where X, Y, R and Z are defined in the specification are disclosed. The compounds of this invention are effective for controlling mites, nematodes, rice planthopper, tobacco budworm, and southern corn rootworm. Methods for making these compounds are also set forth.

Abstract: The present invention provides novel N-substituted hydrazine bifunctional compounds, novel N-substituted hydrazone derivatives of a cytotoxic reagent incorporating the bifunctional compounds, novel conjugates containing at least one cytotoxic reagent molecule reacted with the bifunctional compound and bound to a molecule reactive with a target cell population, methods for their production, and pharmaceutical compositions and methods for delivering cytotoxic reagents to a target population of cells. The hydrazone bonds of the conjugates of the invention permit the release of free cytotoxic reagent from the conjugates in the acidic external or internal environment of the target cells. The bifunctional compounds, derivatives, conjugates and methods of the invention are useful in antibody-or ligand-mediated drug delivery systems for the preferential killing of a target cell population to treat diseases such as cancers, infections and autoimmune disorders.

Abstract: This invention relates to chelating agents useful for coupling metal ions to biologically active molecules. In particular, isothiocyanate derived thiocarbonyls for chelating metals such as technetium are provided that can be conjugated to a targeting molecule such as an antibody, a peptide or a protein.

Abstract: Bifunctional chemicals useful for linking aldehyde containing moieties to moieties containing functionalities which are or can be reactive with sulfhydryl are claimed and have the formula:L--S--(CH.sub.2).sub.n1 --CONH--SPACER--NH--XwhereinL is a leaving group selected from --H or --S--Ar, wherein Ar represents optionally substituted phenyl or pyridyl;n.sub.1 =2-4;X is selected from: ##STR1## wherein Y is alkylene or oxaalkylene and Z is alkylene or a polypeptide residue briding the N-terminal amino group and C-terminal carboxy group thereof;the SPACER is oxaalkylene or oxaalkylene substituted with hydroxyl and specifically includes residues having formulas selected from--(CH.sub.2).sub.n2 --O--(CH.sub.2).sub.n2 --O--(CH.sub.2).sub.n2 --a)wherein each n2 is independently 2-4 and ##STR2## wherein n3 is 2-6. Also claimed are hydrazides, semicarbazides, and thiosemicarbazides of .omega.-mercaptocarboxylic acids which lack SPACER diamine.

Abstract: The present invention provides novel N-substituted hydrazine bifunctional compounds, novel N-subhstituted hydrazone derivatives of a cytotoxic reagent incorporating the bifunctional compounds, novel conjugates containing at least one cytotoxic reagent molecule reacted with the bifunctional compound and bound to a molecule reactive with a target cell population, methods for their production, and pharmaceutical compositions and methods for delivering cytotoxic reagents to a target population of cells. The hydrazone bonds of the conjugates of the invention permit the release of free cytotoxic reagent from the conjugates in the acidic external or internal environment of the target cells. The bifunctional compounds, derivatives, conjugates and methods of the invention are useful in antibody-or ligand-mediated drug delivery systems for the perferential killing of a target cell population to treat diseases such as cancers, infections and autoimmune disorders.

Abstract: A group of functionalized triamine chelants and their derivatives that form complexes with radioactive metal ions are disclosed. The complexes can be covalently attached to a protein or an antibody or antibody fragment and used for therapeutic and/or diagnostic purposes.

Abstract: TCH is produced by a process which does not require expensive measures to remove hydrazine. In this process, hydrazinium dithiocarbazinate is reacted with an amine other than hydrazine or a strong base, optionally in the presence of water. It is preferred that a sulfur suppressing compound also be included in the reaction mixture. The precipitated TCH is removed from the reaction mixture to leave a mother liquor. Hydrazinium-dithiocarbazinate may then be added to the mother liquor. TCH precipitates and may be readily recovered.

Abstract: Thiocarbohydrazide (TCH) is made by reacting carbon disulfide and hydrazine in the presence of a mercaptan at an elevated temperature. The TCH is removed from the reaction mixture, the mother liquor is further treated to form HDTC which is further reacted to form TCH and the mother liquor is recycled. A major advantage of this process is the recyclability of the mother liquor without reduction in TCH yield.

Abstract: TCH is produced in two stages. In the first stage, carbon disulfide and excess hydrazine are reacted in the presence of a mercaptan and optionally a strong base or an amine other than hydrazine. Carbon disulfide and a strong base (if none was present during the first stage) are then added to the reaction mixture which is further reacted to complete the formation of TCH.

Abstract: The present invention relates to a process for the preparation of alkyl semicarbazides by reaction of a dithiocarbamate and hydrazine in a weakly basic reaction media using a metal rearrangement catalyst.

Abstract: New semicarbazide derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen,R.sup.2 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkenyl or aryl,R.sup.3 is lower alkyl, ar(lower)alkyl, lower alkenyl or aryl, orR.sup.2 and R.sup.3 are taken together to form (C.sub.2 -C.sub.6)alkylidene group optionally substituted with aryl or taken together with the adjacent nitrogen atom to form a saturated or unsaturated, 5- or 6-membered heterocyclic group optionally substituted with aryl; orR.sup.1 and R.sup.2 are taken together with the adjacent nitrogen atoms to form a saturated or unsaturated, 5- or 6-membered heterocyclic group or 1,2-diazaspiroalkane-1,2-diyl group,R.sup.3 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkenyl or aryl;R.sup.4 is aryl which may have substituent(s) selected from lower alkyl, halogen, lower alkoxy, lower alkylamino, halo(lower)alkyl, hydroxy, lower alkanoyl, esterified carboxy and carboxy,R.sup.

Abstract: To produce thiosemicarbazide hydrazine is reacted with hydrogen cyanide and sulfur to form hydrazine thiocyanate, and this is then converted into the thiosemicarbazide at an elevated temperature. Advantageously, the reaction is carried out in a polar solvent.

Abstract: Substituted 3-hydrazinopropionates comprising compounds of the general fola: ##STR1## wherein R.sup.1, R.sup.2 =H, an alkyl, a substituted alkyl, hydroxycarbonyl, alkoxycarbonyl, an aryl, an aralkyl, an unsaturated alkyl, a substituted aryl or a substituted aralkyl: ##STR2## wherein R.sup.7, R.sup.8 =H, an alkyl, an unsaturated alkyl, an aralkyl, an aryl, a substituted alkyl,R.sup.9 =OH, an alkoxy, an aralkoxy, an alkyl, an unsaturated alkyl, an aryl, a substituted aryl, an aralkyl;R.sup.4 is --C.tbd.N, --COR.sup.10, wherein R.sup.10 =OR.sup.11, NR.sup.12 R.sup.13, where R.sup.11 is H, an alkyl, an aralkyl and an alkali metal, R.sup.11 and R.sup.12 are each H, an alkyl, an aralkyl, an aryl;R.sup.5, R.sup.6 = an alkyl, an aryl, an aralkyl.

Abstract: Hydrazinecarboxamides and carbothioamides of the formula ##STR1## wherein R.sub.1 is selected from alkyl, cyanoalkyl, hydroxyalkyl, and benzyl, R.sub.2 is hydrogen or alkyl, Y is oxygen or sulfur, n is 0-5, and Z is substituted for hydrogen and independently selected from halogen, alkyl, alkoxy, phenoxy, trifluoromethyl, and nitro are useful as nematicides when applied to or incorporated into nematode-infested soil.

Abstract: Disclosed is a process for making carbohydrazide by reacting a di(lower alkyl) carbonate with hydrazine in two-stages with an intermediate step of removing the corresponding lower alkanol formed as a co-product in the first stage. The two reaction stages are carried out at relatively low temperatures (i.e. below about 80.degree. C.).

Abstract: A process for preparing semicarbazide hydrochloride comprising the steps:(a) reacting an aqueous hydrazine solution with urea at a temperature from about 80.degree. C. to about 130.degree. C. and at a mole ratio of hydrazine to urea from about 0.9:1 to about 1.2:1 to form a reaction mixture comprising semicarbazide, water and alcohol-insoluble by-products;(b) removing substantially all of the water from the reaction mixture;(c) mixing a sufficient amount of an alcohol with the water-deleted reaction mixture to dissolve the semicarbazide and to precipitate said alcohol-insoluble by-products from the resulting alcohol solution;(d) removing said precipitated alcohol-insoluble by-products from said alcohol solution;(e) adding a sufficient amount of anhydrous hydrogen chloride to said alcohol solution to form and precipitate semicarbazide hydrochloride; and(f) recovering said semicarbazide hydrochloride from said alcohol solution.

Abstract: Compounds of the formula: ##STR1## wherein R is lower alkyl or lower alkenyl are fungicidal.

Abstract: The present invention is directed to a class of novel 1-benzoyl-3-thiosemicarbazides which are useful as plant growth regulants. The present invention is also directed to methods and formulations for plant growth regulation.

Abstract: Compounds of the formula ##STR1## wherein R is H or C.sub.1-5 straight or branched chain alkyl; R.sub.1 is H, C.sub.1-10 straight or branched chain alkyl, allyl or phenyl; and R.sub.2 is phenyl or phenyl substituted with F, Cl, C.sub.1-5 straight or branched chain alkyl, di-F, di-Cl or di-Br; and the pharmaceutically acceptable acid addition salts thereof; are useful as muscle relaxants, anticonvulsants and analgesics.

Abstract: In the production of thiocarbohydrazide by reacting hydrazine hydrate with carbon disulphide in the presence of water to form in a first stage hydrazinium dithiocarbazinate, subsequently thermally decomposing the hydrazinium dithiocarbazinate in a second stage to form thiocarbohydrazide, and recovering the thiocarbohydrazide from the reaction medium, the improvement which comprises effecting the entire reaction in the mother liquor of a preceding batch, carrying out the first reaction stage at a temperature between about 25.degree. C. and 45.degree. C., with injection of carbon disulphide below the surface of the reaction mixture; carrying out the second stage at about 62.degree. to 65.degree. C. without prior isolation of the intermediate product; filtering off the thiocarbohydrazide formed after cooling, separating the amount of mother liquor in excess of that required for the next batch, and feeding the balance of the mother liquor to the next batch.