Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth:

Abstract: Disclosed are compounds of Formula (I) and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.

Abstract: The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.

Abstract: This invention relates to a process for the recovery of precious metal/s from a precious metal-containing material in an aqueous leach slurry or solution. The process includes the step of contacting the precious metal/s in the leach slurry or solution with a ligand selected from dithiooxamide (rubeanic acid), or a substituted dithiooxamide. The leaching of PGMs, gold and silver from their ores using the ligand of the present invention may take place under aqueous alkaline conditions, avoiding both corrosive acidic conditions and the use of cyanide.

Abstract: The invention provides high-yield protein dimerization methods using highly reactive bis-thioimidates that may be used in the manufacture of a highly potent anti-cancer peptide dimers.

Abstract: An object is to provide a thiazole derivative produced from easily available raw materials by a simplified production process. Provided are a process for producing a novel thiazole derivative represented by the general formula (I), which is characterized by adding a strong base to a thioamide represented by the general formula (II) and reacting the mixture with a thioformamide represented by the general formula (III), and a novel thiazole derivative.

Abstract: Methods for controlling atmospheric corrosion of a metallic surface including coating the metallic surface with a coating material containing at least one compound having at least one thioamide group.

Abstract: There is provided an organic sulfur compound having an excellent controlling effect on harmful arthropods represented by the formula (I): wherein, R1 represents a C1-C5 haloalkyl group having at least one fluorine atom, R2 represents a C1-C4 alkyl group optionally substituted with at least one halogen atom or the like, R3 represents a hydrogen atom or the like, R4 represents a cyano group or the like, R5 represents a hydrogen atom or the like, m represents an integer of 1 to 4, and n represents 0, 1 or 2.

Abstract: There is provided an organic sulfur compound having an excellent controlling effect on harmful arthropods which is represented by formula (I): wherein R1 represents a C3-C6 haloalkyl group having at least one fluorine atom and at least one atom selected from group consisting of a chlorine atom, a bromine atom and an iodine atom, R2 represents a cyano group and the like, R3 represents a hydrogen atom, a halogen atom or a C1-C4 alkyl group, R4 represents a C1-C5 fluoroalkyl group, and n represents 0, 1 or 2.

Abstract: The present invention is a phosphorylcholine-containing chemical compound represented by the following formula (1) or (2). (CH3)3N+CH2CH2PO4?CH2COOH??(1) (CH3)3N+CH2CH2PO4?CH2COONa??(2) The object of the present invention is to provide a new phosphorylcholine-containing compound that is useful as a surface treatment agent or a source material of a surface treatment agent. Another object is to provide a manufacturing method that has a high industrial utility value.

Abstract: Disclosed herein are methods of purifying a bis(thio-hydrazide amides) compounds of the following structural formula: wherein R1, R2, R3, R4, R7, R8, Z, and Y are defined herein.

Abstract: The disclosure provides, in part, compositions and methods for producing cellular labels for tracking cells by MRI. The disclosure provides, in part, methods for labeling, detecting and quantifying cell numbers in vivo.

Abstract: Poly(?-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer/polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings. A system for preparing and screening polymers in parallel using semi-automated robotic fluid delivery systems is also provided.

Abstract: Disclosed herein are novel binaphthol derivatives and methods for the optical resolution of amino acids or amino alcohols and for the optical transformation of D, L-forms of amino acids using the same.

Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.

Abstract: The present invention relates to novel phenyl-substituted 2-enamino-ketonitriles of the formula (I): in which Ar, X, Z, Y and K are each as defined in the description, to a plurality of processes for their preparation and to their use as herbicides and pesticides.

Abstract: Poly(?-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer/polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.

Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.

Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.

Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: ##STR1## or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.

Abstract: In a process for reducing the primary amine content of a composition comprising at least one polyol, in which a composition comprising at least one polyol is admixed with at least one isocyanate which contains only secondary and/or tertiary, aliphatically bound isocyanate groups, isocyanate is added in an amount of up to 5% by weight, based on the total composition, and a polyol preparation is obtained.

Abstract: The present invention relates to novel fluorobutenic acid hydrazides of the formula (I) ##STR1## in which Y represents C.dbd.O, C.dbd.S or SO.sub.2,R.sup.1 represents hydrogen or halogen andR.sup.2 represents alkyl, halogenoalkyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, alkenyl, alkenyloxy, alkoxy, cycloalkyloxy, alkylthio or respectively optionally substituted aryl, aralkyl, aralkyloxy or hetaryl,to processes for their preparation and to their use for controlling animal pests.

Abstract: Novel compounds of Formula I and methods of making and using the compounds which are useful as fungicides, particularly in the agricultural field: ##STR1## wherein C.sub.1 and C.sub.2 are carbon atoms which are part of an aromatic ring; W is alkoxyimino, alkoxymethylene or alkylthiomethylene; R.sub.1 is independently selected from the group consisting of halogen, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, wherein the alkyl or alkoxy are optionally substituted by halogen, and p is 0, 1, or 2; Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, NR.sub.2 wherein R.sub.2 is hydrogen or a lower aliphatic group, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 S(O)--, --OCH.sub.2 --, --SCH.sub.2 --, --S(O)CH.sub.2 --, --CH.sub.2 ON.dbd.C(R.sub.3)-- or --CH.dbd.NB wherein B is --O--CO--, --N.dbd.CR.sub.3, or --CR.sub.3 R.sub.4 -- wherein R.sub.3 and R.sub.4 are independently hydrogen or C.sub.1 -C.sub.

Abstract: A process for preparing an aliphatic thioamide entails reacting a nitrile compound of the general formulaR.sub.1 R.sub.2 R.sub.3 C--CN,wherein R.sub.1 denotes a hydrogen atom, an alkyl radical containing from 1 to 5 carbon atoms or an aryl radical and R.sub.2 and R.sub.3 each denotes a hydrogen atom containing from 1 to 5 carbon atoms, with hydrogen sulphide, in the presence as catalyst of an aliphatic amine of the general formulaR.sub.4 R.sub.5 R.sub.6 N,wherein R.sub.4 denotes an alkyl radical containing 1 to 5 carbon atoms and R.sub.5 and R.sub.6 each denotes a hydrogen atom or an alkyl radical containing 1 to 5 carbon atoms, in a water-miscible polar solvent.

Abstract: Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops, these compounds having the structure: ##STR1## where Q is --(C.dbd.S)--R.sub.1 and R.sub.1 is --OR.sub.5, --SR.sub.5, halogen, --NHOH or --NR.sub.5 R.sub.6. Each of R.sub.5 and R.sub.6 is independently hydrogen; an aliphatic or an aromatic group; a C.sub.1 -C.sub.12 aliphatic amine group; a C.sub.2 -C.sub.12 aliphatic carboxylic acid group; or R.sub.5 and R.sub.6 when taken together with the N of R.sub.1 are a protein amino acid or a cyclic group. Polar compounds are particularly useful for systemic control of pests.

Abstract: A novel and simple method is proposed for the synthetic preparation of an N,N-disubstituted .beta.-ketothioamide compound represented by the general formulaR.sup.1 R.sup.2 N--CS--CH.sub.2 --CO--R.sup.3,in which R.sup.1 and R.sup.2 are each a monovalent hydrocarbon group or each a divalent hydrocarbon group jointly forming a cyclic structure together with the nitrogen atom and R.sup.3 is a hydrogen atom, a monovalent hydrocarbon group or a divalent hydrocarbon group forming a cyclic structure jointly with R.sup.1, R.sup.1 being a divalent hydrocarbon group and R.sup.2 being a monovalent hydrocarbon group. The method comprises:(a) mixing an N,N-disubstituted amide compound represented by the general formulaR.sup.1 R.sup.2 N--CO--R.sup.3,and a bis(trialkylsilyl)thioketene compound represented by the general formula(R.sub.3 Si).sub.2 C.dbd.C.dbd.

Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof.These compounds are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, and as anti-viral and anti-fungal agents or pro-drugs of such agents. Illustrative of the disclosed compounds are fatty acid amino acid analogs of the structure ##STR1## in which X is the ethyl or t-butyl ester of an amino acid such as Gly, L-Ala, L-Ile, L-Phe, L-Trp, L-Thr or an amide such as NHCH.sub.2 C.sub.6 H.sub.5 or NH(CH.sub.2).sub.2 C.sub.6 H.sub.5.

Abstract: Succinoylamino hydroxyethylamino sulfamic acid derivative compounds which are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: The .beta.-oxo-.beta.-benzenepropanethioamide derivative of the present invention has potassium channel opening action and is useful for treatment of hypertension, asthma, hypersensitive colon syndrome, and enteritis through pharmacological actions including blood vessel dilation, bronchial tract dilation, relaxation of gastrointestinal tract smooth muscle, and the like. The present invention also includes a pharmaceutical composition containing, as the active ingredient, the compound of the present invention and a method for producing the same.

Abstract: Pesticidal compositions for use against insects and acarines comprising a compound of Formula (I):R.sup.1 --(CA.dbd.CA').sub.n C(.dbd.S)NR.sup.2 R.sup.3 (I)whereinR.sup.1 is: C.sub.1-14 alkyl optionally substituted by C.sub.1-6 alkoxy, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.2-6 alkenyloxy, C.sub.2-6 alkynyloxy, aryl, aryloxy or aryl (C.sub.1-6) alkoxy; aryloxy or aryl (C.sub.1-6) alkoxy; any of which groups may be substituted by halo,n is 1 or 2,each A and A' is independently hydrogen, halo, C.sub.1-4 alkyl or halo (C.sub.1-4) alkyland R.sup.2 and R.sup.3 are independently hydrogen, C.sub.1-6 alkyl or C.sub.3-6 cycloalkyl, either of which may be substituted by one or more of halo, C.sub.2-6 alkenyl, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkenyl, C.sub.1-6 alkoxy, C.sub.2-6 alkynyl or cyano, except that, when n is 1 and R.sup.2 is alkyl and R.sup.3 is hydrogen and A and A' are both hydrogen then R.sup.1 is not substituted alkyl.

Abstract: Pesticidal compositions for use against insects and acarines comprising a compound of Formula (I):R.sup.1 --(CA.dbd.CA').sub.n C(.dbd.S)NR.sup.2 R.sup.3 (I)wherein R.sup.1 is: C.sub.1-14 alkyl optionally substituted by C.sub.1-6 alkoxy, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.2-6 alkenyloxy, C.sub.2-6 alkynyloxy, aryl, aryloxy or aryl (C.sub.1-6) alkoxy; aryloxy or aryl (C.sub.1-6) alkoxy; any of which groups may be substituted by halo,n is 1 or 2,each A and A' is independently hydrogen, halo, C.sub.1-4 alkyl or halo (C.sub.1-4) alkyl and R.sup.2 and R.sup.3 are independently hydrogen, C.sub.1-6 alkyl or C.sub.3-6 cycloalkyl, either of which may be substituted by one or more of halo, C.sub.2-6 alkenyl, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkenyl, C.sub.1-6 alkoxy, C.sub.2-6 alkynyl or cyano, except that, when n is 1 and R.sup.2 is alkyl and R.sup.3 is hydrogen and A and A' are both hydrogen then R.sup.1 is not substituted alkyl.Most of the compounds of Formula (I) are novel.

Abstract: An amide is thiated to the corresponding thioamide by reacting it with phosphorus pentasulfide in the presence of a Group IIA metal fluoride as an adjuvant.

Abstract: Ammonium hydroxide is used in the recovery of a thiono compound prepared by reacting an organic carbonyl compound with phosphorus pentasulfide to improve the product yield.

Abstract: An amide is thiated to the corresponding thioamide by reacting it with phosphorus pentasulfide in the presence of an adjuvant selected from diatomaceous earth, zeolites, and molecular sieves.

Abstract: A compound of the general formula (I): ##STR1## wherein R is C.sub.2 -C.sub.4 alkenyl or C.sub.2 -C.sub.4 alkynyl, both optionally substituted by lower alkyl, halogen or trialkylsilyl; E is CN or CSNH.sub.2 ; and Y is C.sub.1 -C.sub.4 alkoxy, C.sub.3 -C.sub.4 alkenyloxy, C.sub.3 -C.sub.4 alkynyloxy, 1-pyrazolyl or 2-furyl. The compounds have fungicidal and plant growth regulating activity.

Abstract: An amide derivative of the formula (I): ##STR1## or a tautomeric form thereof, wherein R is a phenyl group substituted in the 4-position by a group of R.sup.1 XCH.sub.2--, where R.sup.1 is C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, C.sub.1 -C.sub.4 alkynyl, C.sub.1 -C.sub.4 alkylcarbonyl, or H, and X is oxygen or sulphur; E is CN, or CSNH.sub.2, or CONH.sub.2 ; and Y is C.sub.1 -C.sub.4 alkoxy, C.sub.3 -C.sub.4 alkenyloxy, C.sub.3 -C.sub.4 alkynyloxy, 1-pyrazolyl or 2-furyl. Compositions and processes for using these derivatives to combat plant fungi are also disclosed.

Abstract: An amide derivative of the formula (I): ##STR1## or a tautomeric form thereof, wherein R is a phenyl group substituted in the 4-position by a group of R.sup.1 XCH.sub.2-, where R.sup.1 is C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, C.sub.3 -C.sub.4 alkynyl, C.sub.1 -C.sub.4 alkylcarbonyl, or H, and X is oxygen or sulphur;E is CN, or CSNH.sub.2, or CONH.sub.2 ; andY is 1-pyrazolyl or 2-furyl. Compositions and processes for using these derivatives to combat plant fungi are also disclosed.

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: Herbicidal and fungicidal benzamide derivatives of the formula (I) ##STR1## wherein R.sup.1 is an optionally substituted alkyl, alkenyl, aryl, heterocyclyl, benzyl, or heterocyclylmethyl radical;R.sup.2 is hydrogen, or an optionally substituted alkyl, alkenyl, benzyl, or heterocyclylmethyl, radical;X is oxygen, sulphur, or an --NH-- group;R.sup.3 is an optionally substituted alkyl or alkenyl radical when X is oxygen or sulphur, or is an optionally substituted alkanoyl radical when X is --NH--;and E is a --CN, --CONH.sub.2, --CSNH.sub.2, or --CONR.sup.4 R.sup.5 group wherein each R.sup.4 and R.sup.5 is an optionally substituted alkyl or alkenyl group.

Abstract: Useful thionamide compounds are prepared by reacting sulfur with imines of the structural formula: ##STR1## where R is an alkyl group of 1 to 18 carbon atoms and is other than a phenyl or cyclohexyl group, R.sub.1 and R.sub.2 are alkyl or phenyl groups of 1 to 18 carbon atoms, and R.sub.3 is a phenyl group of 6 to 18 carbon atoms or is hydrogen, in the presence of a diol or triol compound. The total number of carbons in R, R.sub.1, R.sub.2, and R.sub.3 does not exceed 36 in number.

Abstract: Disclosed are selected 2-acyl- or 2-thioacyl-1-trichloroacetimidoylhydrazines having the formula: ##STR1## wherein X is an atom selected from the group consisting of oxygen and sulfur; and R is a hydrogen, lower alkyl or lower alkoxy group having 1 to 4 carbon atoms, or an unsubstituted or substituted phenyl group. These compounds are disclosed to be agricultural fungicides.

Abstract: The title compounds are prepared by the reaction of a 2-alkyl-2-oxazoline with hydrogen sulfide in a continuous process wherein both reactants are maintained in the liquid phase throughout the reaction by the use of superatmospheric pressure. This continuous process reduces the reaction time substantially compared to prior art process and also reduces the quantity of by-products.

Abstract: The use of oxythioamido substituted arylhydrazides in producing images in silver halide photographic elements is disclosed. The oxythioamido substituted arylhydrazide can be incorporated in photographic silver halide emulsions. The oxythioamido substituent is capable of promoting adsorption of the arylhydrazide to silver halide grain surfaces. In negative working surface latent image forming emulsions the oxythioamido substituted arylhydrazides permit higher speeds to be achieved. In direct positive internal latent image forming emulsions increased nucleation activity can be achieved.

Abstract: Poly(?-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer/polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings. A system for preparing and screening polymers in parallel using semi-automated robotic fluid delivery systems is also provided.