Abstract: Provided herein are thiosuccinyl-crosslinked hemoglobin analogs useful as blood replacement agents, pharmaceutical compositions comprising the same and the methods of use and preparation thereof.

Abstract: The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof.

Abstract: The present invention pertains to substances of the formula (I) wherein X is O or S; and R1-R4 are defined in the claims as inhibitors of glyoxalase I and/or II, pharmaceutical compositions comprising one or more compounds according to formula (I) and the use of one or more compounds according to formula (I) for the treatment of diseases associated with increased glycolytic metabolism. In one embodiment, the disease is a bacterial infection.

Abstract: The invention relates to compounds having the general formula (I), the method of preparation thereof and the use thereof in organic radical synthesis. The invention also relates to compounds having the formula (II), the method of preparation thereof and a method for preparing compounds having the formula (VIII).

Abstract: Disclosed herein are carbonyl compounds of Formula: (I) as described herein. Compounds as modulators of his-tone deacetylase (HDAC), pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.

Abstract: Compounds of formula I wherein A is R3, OR3, SR3, and NR3R4; and R1, R2, R3 and R4 are as defined. The compounds of the invention are reversible inhibitors of acyl-CoA dehydrogenase, and are useful in treating disorders such as diabetes, heart diseases (including angina and congestive heart failure), and peripheral vascular disease in patients suffering from these diseases or conditions resulting thereof.

Abstract: Compounds of formula (I) wherein R4 is an ester or thioester group and R, R1, R2 and R3 are as defined in the specification, inhibit proliferation of tumor cells.

Abstract: Compounds having Formula 2 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: Compounds of the formula (I) and their salts as defined in claim 1, in which R1 is CO—Q—R8, where R8=H or R R2 and R3 are H or (C1-C4)alkyl, R4 is H, R, RO, OH, RCO, RSO2, PhSO2 R5 is RSO2, PhSO2, PhCO, RNHSO2, R2NSO2, RCO, CHO, COCOR′, CW—T—R9, CW—NR10R11, CW—N(R12)2 or R4 and R5 together are the chain (CH2)mB or —B1—(CH2)m1B— where B=SO2, m=3, 4; m1=2, 3; T and W=O, S; Q=O, S, NR13 where R13=H, R; R6=H, R, RO, RCO, ROCO, Hal, NO2, CN; R7=H, CH3; R9=R; R10, R11=H, R; N(R12)2=heterocycle A=pyrimidinyl and triazinyl radical or an analog thereof, where R=(substituted) aliphatic hydrocarbon radical, are suitable as selective herbicides. They are prepared by analogous processes via sulfonamides, some of which are new, of the formula (II) (see claim 4).

Abstract: Briefly, in one aspect, the present invention provides compositions of open-chain, .alpha.-branched fluoroalkylcarbonyl fluorides, and derivatives thereof.

Abstract: (Het)aryloxy-, -thio- and -aminocrotonates of the formula I ##STR1## where the substituents have the following meanings: U is oxygen, sulfur or amino;V is oxygen, sulfur, amino or alkylamino;X, Y and Z independently of one another are .dbd.N-- or .dbd.CR.sup.3 --;R.sup.1 and R.sup.2 independently of one another are alkyl;R.sup.3 is hydrogen, cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and haloalkylthio; andR.sup.4 is an organic radical which is bonded to the skeleton directly or via an oxy, mercapto, amino, carboxyl or carbonylamino group,process for their preparation, and their use.

Abstract: The invention comprises a novel pyruvate compound for the treatment of prevention of reperfusion injury following ischemia, diabetic effects, cholesterol levels, injured organs ethanol intoxication oras s foodstuff. The novel pyruvate compound is particularly a puruvate thiolester, a glucerol-pyruvate ester or a dihydoxyacetone-pyruvate ester.

Abstract: The present invention is directed to novel methadone derivatives which are synthesized for the covalent attachment to antigens (proteins or polypeptides) for the preparation of antibodies or receptors to methadone and methadone metabolites. The resulting novel antigens may be used for the production of antibodies or receptors using standard methods. Once generated, the antibodies or receptors and the novel derivatives which are covalently attached to proteins, polypeptides or labels may be used in the immunoassay process.

Abstract: The present invention provides a simple and inexpensive method for producing .alpha.-hydroxy-.beta.-aminocarboxylic acids and their esters. An ester of an N-protected .alpha.-amino acid ester is converted into a .beta.-ketosulfoxide, which is then processed with an acid to give an .alpha.-ketohemimercaptal. Next, this is acylated and then processed with a base to obtain an N-protected .alpha.-acyloxy-.beta.-amino-thioester, which is then saponified to obtain an intended compound. According to the method of the present invention, it is possible to produce .alpha.-hydroxy-.beta.-aminocarboxylic acid derivatives, which are intermediates in producing various HIV protease inhibitors, renin inhibitors and carcinostatics, from a-amino acids. The method comprises reduced reaction steps, the selectivity in the method to give the intended product is high, and the yield of the product obtained is high.

Abstract: The present invention provides metal chelating compounds, to chelates and chelate-targeting agent conjugates formed from the chelating compounds, and to methods for making and using these compositions. The chelating compounds incorporate two nitrogen atoms and three sulfur atoms ("N.sub.2 S.sub.3 "), two nitrogen atoms and four sulfur atoms ("N.sub.2 S.sub.4 "), or three nitrogen atoms and three sulfur atoms ("N.sub.3 S.sub.3 "). Metals, and metal oxides, capable of being chelated by the compounds include those that are radionuclides, such as .sup.99m Tc and .sup.186/188 Re.The targeting agent portion of the chelate-targeting agent conjugates provided includes antibodies, peptides, hormones, enzymes and biological response modifiers. Methods for making the conjugates are provided and encompass the addition of a metal, or metal oxide, to a chelating compound prior to attachment to a targeting agent as well as subsequent to the attachment.

Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes and 3-aminochromanes which exhibit binding activity at the serotonin 1A receptor.

Abstract: A derivative of p-guanidinobenzoic acid of the general formula (IA): ##STR1## wherein Y represents an oxygen atom or a sulfur atom and (a) when Y is an oxygen atom, (R.sup.1).sub.m is selected from the group consisting of:5-(4-guanidinobenzoyloxy)-3-methoxymethyl, 3,5-dicarboxy, 3,5-bis(isopropoxycarbonyl), 3,5-bistrifluoromethyl, 3-acetyl, 3,5-bis(N-ethylcarbamoyl), and 3,5-bis(N-propylcarbamoyl);(b) when Y is a sulfur atom, (R.sup.1).sub.m is selected from the group consisting of:2-methyl, 3-methyl, 4-fluoro, 2-chloro, 3-chloro, 2,5-dichloro 2,6-dichloro, 3,4-dichloro, 2-bromo, 2-methoxycarbonyl, and 4-(N,N-diethylaminosulfonyl);or an acid addition salt of said derivative. A method for the treatment or prevention of diseases induced by abnormal enhancing of degradation of proteins by the action of elastase in mammals subject to or suffering therefrom, including the step of administering an effective amount of a p-guanidinobenzoic acid as described herein, is also disclosed.

Abstract: The present invention is directed to an oil-soluble lubricating oil additive comprising at least one adduct of (A) a polyolefin of 700 to 5,000 number average molecular weight substituted nitrogen- or ester-containing ashless dispersant and (B) a bis-keto/thioketo compound.

Abstract: KS-506a, KS-506x and KS-506g having an activity to inhibit cyclic nucleotide phosphodiesterase and KS-506m and KS-506h having an activity to inhibit histamine release are produced by culturing a microorganism belonging to the genus Mortierella.

Abstract: The present invention is directed to an oil-soluble lubricating oil additive comprising at least one adduct of (A) a polyolefin of 700 to 5,000 number average molecular weight substituted with carboxylic acid producing moieties (preferably acid or anhydride moieties), and (B) a monoepoxy thiol.

Abstract: Novel 4-chloro-4,4-difluorothiobutyric acid derivatives of the formula I ##STR1## in which R.sub.1 and R.sub.2 are, independently of one another, hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 halogenoalkyl and R.sub.3 is hydrogen or an organic radical can be employed as pest-control agents. Control of insects and arachnids is possible and preferable.

Abstract: Protein conjugated chelated metal radionuclides are provided for use in vivo. Intermediates are provided for preparing the polypeptide compositions efficiently.

Abstract: Ammonium salt of methyl 4,4,4-trifluoro-3-oxobutanethioate (TMTFAA).

Abstract: Novel .omega.-mercaptopropanamides and their homologs of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and ##STR2## R.sub.1 ' is selected from the group consisting of alkyl of 1 to 5 carbon atoms and aryl optionally substituted with at least one member of the group consisting of --OH, alkyl and alkoxy of 1 to 5 carbon atoms, --NO.sub.2 and halogen, n is an integer from 1 to 5, R.sub.2 is selected from the group consisting of hydrogen alkyl of 1 to 5 carbon atoms and aryl and aralkyl of 6 to 15 carbon atoms optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, --OH, halogen and --CF.sub.3, R.sub.3 is selected from the group consisting of a) hydrogen, b) phenyl optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, --OH, --NO.sub.2, halogen, --CF.sub.

Abstract: Described herein is a process for preparation of substituted piperidine dicarbothioate compounds.

Abstract: Lubricants are stablized against oxidative degradation by the incorporation therein of hydroxylamines substituted with thioalkanoic acid residues of the formula ##STR1## wherein R and R.sub.1 are independently H, alkyl or aryl, X is independently OR.sub.2 SR.sub.2 or NR.sub.3 R.sub.4 wherein Rhd 2 is H, alkyl, cycloalkyl or aralkyl, and R.sub.3 and R.sub.4 are independently H, alkyl or aryl and n is 1 or 2.

Abstract: Borated glycerol hydroxyesters are effective friction reducing additives when incorporated into lubricating compositions.

Abstract: A plant metabolism regulating agent comprising as an active ingredient an alpha,beta or beta,gamma-un-saturated carboxylic acid or its derivative. It is useful for controlling the metabolism of a plant, facilitating the growth of a beneficial plant such as cereals by inhibiting the growth of undesirable plants or eradicating them, regulating the growth of a plant and dwarfing a plant.

Abstract: Disclosed herein is 4,4,4-trifluoro-3-oxo-butanethioate, a useful starting material in the preparation of pyridinedicarboxylate herbicides.

Abstract: 5-2-chloro-4-trifluoromethylphenoxy)-2-nitro-.alpha.-substituted-acetopheno nes and oxime derivatives thereof represented by the formula ##STR1## wherein R.sup.1 and Y are as defined in the disclosure, process for the preparation thereof, herbicidal composition and method for the destruction of undesirable weeds. The herbicides comprising the above compounds are capable of selectively controlling undesirable weeds among desirable crop plants.

Abstract: A collector composition for use in froth flotation processes comprises two collectors. One of the collectors is preferably an omega-(hydrocarbylthio)alkylamine, S-(omega-aminoalkyl) hydrocarbyl thioate, N-(hydrocarbyl)-alpha, omega-alkanediamine, (omega-aminoalkyl) hydrocarbon amide, omega-(hydrocarbyloxy)alkylamine, omega-aminoalkyl hydrocarbonoate or mixture thereof. The second collector is a thiocarbonate, a thionocarbamate, a thiophosphate, thiocarbinilide, thiophosphinate, mercaptan, xanthogen formate, xanthic ester or mixture thereof. The collector composition floats a broad range of metal-containing minerals.

Abstract: A collector composition useful for the recovery of metal values from metal ores in a froth flotation process comprises two collectors. One collector is an organic compound containing at least 4 carbon atoms and one or more monosulfide units, wherein the carbon atoms to which the sulfur atoms are bound are aliphatic or cycloaliphatic carbons. The other collector is preferably an omega-(hydrocarbylthio)alkylamine, S-(omega-aminoalkyl)hydrocarbyl thioate, N-(hydrocarbyl)-alpha, omega-alkanediamine, N-(omega-aminoalkyl)hydrocarbon amide, omega-(hydrocarbyloxy)alkalamine, omega-aminoalkyl hydrocarbonate or mixture thereof. The collector composition floats a broad range of metal values including sulfide ores, oxide ores and precious metals.

Abstract: A process for preparing cyclopentenone derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl or lower alkenyl, R.sup.2 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted ar(lower)alkyl and A is the residue of a nucleophilic agent from which a hydrogen atom is excluded, which comprises reacting a 3-hydroxy-4-cyclopentenone compound of the formula: ##STR2## wherein R.sup.1 and R.sup.2 are each as defined above with a nucleophilic agent of the formulaA--H (III)wherein A is as defined above.The cyclopentenone derivatives of the formula (I) are useful as pharmaceuticals, agricultural chemicals, perfumes and as intermediates for the preparation of agricultural chemicals, pharmaceuticals and perfumes.

Abstract: Certain novel aryl sulfonyl fluorides, their preparation, and their use in inhibiting serine proteases with chymotrypsin-like and elastase-like specificity.

Abstract: The invention relates to novel phenoxyphenylamino acid derivatives of the formula I ##STR1## wherein X is hydrogen, chlorine, fluorine or bromine,R.sup.1 is hydrogen, nitroso, or C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.1 -C.sub.4 alkylcarbonyl or C.sub.2 -C.sub.4 alkenylcarbonyl, each of which is unsubstituted or substituted by one or more halogen atoms,Q is a straight chain or branched aliphatic radical of 1 to 5 carbon atoms ##STR2## in which A', E', G', L' and M' are hydrogen or C.sub.1 -C.sub.4 alkyl, or two adjacent substituents A', E', G', L' and M' together are also a bond between the two carbon atoms to which they are attached; A, E, G, L and M are hydrogen or one or two of A, E, G, L and M are also --OR.sup.2, --SR.sup.3, --COOR.sup.4, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkyl substituted by --OR.sup.5, --SR.sup.6 or --COOR.sup.7, where R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are hydrogen or C.sub.1 -C.sub.4 alkyl; a, b, c and d are 0 or 1; or R.sup.

Abstract: Provided are antihypertensive compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl, and may be the same or different,m is an integer from 0 to 2 inclusive,n is an integer from 0 to 4 inclusive,M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycycloalkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cycloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl.Y is hydroxy, alkoxy, amino, or substituted amino, aminoalkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is alkyl, aryl, aralkyl, cycloalkyl, cycloalkyl-alkyl, heterocyclic, --CO--SR, --CS--SR, ##STR2## CH.sub.2 CO.sub.2 R, --CHM--CO.sub.2 R, --CH.sub.2 --CO--SR, --CN, ##STR3## --CO--NH--CH.sub.2 CO.sub.2 R, ##STR4## or --CO--CO.sub.

Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: m is an integer selected from 1 to 4;n is zero or an integer selected from 1 to 4;X are selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, alkylthio, sulfamoyl, substituted sulfamoyl, amino, substituted amino, the group --(CH.sub.2).sub.p C(.dbd.A)Z in which p is zero or one A is oxygen or sulfur, and Z is hydrogen, hydroxy, alkoxy, alkylthio, alkyl, substituted alkyl, amino or substituted amino, the group --NHC(.dbd.B)NR.sup.7 R.sup.8 in which B is oxygen or sulfur and R.sup.7 and R.sup.8 are hydrogen or alkyl;R.sup.1 is selected from hydrogen, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl;R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl, and phenyl; andR.sup.4 is selected from hydrogen, halogen, alkyl, cyano and alkoxycarbonyl.