Abstract: A low temperature process for preparing a methyl ester having formula (III) said process comprising reacting a carboxylic acid or salt thereof having formula (I) with dimethyl carbonate having formula (II) in the presence of a catalyst selected from the group consisting of 1,8 diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; and combinations thereof, wherein said process is conducted at a temperature of about 10° C. to less than 120° C.; R1 is selected from the group consisting of an alkyl, aryl, alkoxy, alkenyl, cycloalkyl, benzocycloalkyl, cycloalkylalkyl, aralkyl, heterocyclic, heteroaralkyl, alkoxyalkyl, carboxyalkyl, alkylcarbonyl, alkoxycarbonyl, alkoxycarbonylalkyl and haloalkyl; and M is selected from the group consisting of hydrogen, a monovalent metal and a monovalent fractional part of a polyvalent metal.

Abstract: Compounds of the formula 1

Abstract: Disclosed are novel NO-releasing compounds which comprise a stabilized S-nitrosyl group and a free alcohol or a free thiol group. Also disclosed is a method of preparing the NO-releasing compounds. The method comprises reacting a polythiol or a thioalcohol with a nitrosylating agent. Also disclosed are medical devices coated with the disclosed compounds, methods of delivering NO to treatments sites in a subject by utilizing the medical devices and methods of sterilizing surfaces.

Abstract: The invention comprises a novel lactate compound for two unique purposes: (1) cardiac energy resuscitation and the treatment or prevention of reperfusion injury following ischemia, and (2) the provision of a fuel energy source to humans and other mammals during exercise and recovery. The novel lactate compound is particularly a lactate thiolester. Preferably, the thiol is selected from a cysteine or a methionine amino acid. In a particularly preferred form, the compound is a lactate N-acetyl ethyl ester of the cysteine or methionine amino acid. The most preferred compound is lactate N-acetyl cysteine thiolester (LNACE): Further, the invention involves use of mixtures of lactate- and pyruvate compounds as well as hexoses (glucose and fructose), maltodextrins and electrolytes as adjutants to support LNACE in its specific purposes.

Abstract: Compositions containing a &agr;-sulfofatty acid ester and a hydrotrope. The &agr;-sulfofatty acid ester and the hydrotrope reduce the pH drift in the composition and solubilize the &agr;-sulfofatty acid ester in solution. Methods are also disclosed for making such compositions.

Abstract: One aspect of the present invention relates to 2-hydroxymethylglutamic acid and congeners thereof. A second aspect of the invention relates to a method of synthesizing 2-hydroxymethylglutamic acid and congeners thereof.

Abstract: The present invention relates to novel fatty acid analogous of the general forumla I: CH3—[CH2]m—[xi—CH2]n—COOR, as defined in the specification, which can be used for the treatment and/or prevention of obesity, fatty liver and hypertension. Further, the invention relates to a nutritional composition comprising such fatty acid analogues, and a method for reducing the total weight, or the amount of adipose tissue in an animal. The invention also relates to a method for improving the quality of product such as meat, milk and eggs.

Abstract: Novel brain targeted low molecular weight, hydrophobic antioxidants and use of antioxidants in treatment of central nervous system neurodegenerative disorders such as Parkinson's, Alzheimer's and Creutzfeldt-Jakob's diseases and in treatment of conditions of peripheral tissues, such as acute respiratory distress syndrome, amyotrophic lateral sclerosis, atheroscierotic cardiovascular disease and multiple organ dysfunction, in which oxidants are overproduced.

Abstract: A process for producing optically active cysteine derivatives with high optical purity and good quality which is economically advantageous and is high in productivity even on a commercial scale is provided.

Abstract: A method for enhancing the purity of a desired compound comprising: Step (a) treating a crude reaction product which contains at least one desired compound, unreacted starting materials and/or byproducts with at least one bifunctional quenching agent that is capable of selective covalent reaction with unwanted byproducts, or excess reagents; Step (b) allowing the quenching agent to covalently react with unreacted starting materials and/or byproducts to afford a derivatized compound of the quenching agent: and Step (c) isolating the desired compound is described as well as novel quenching agents and methods for their use in the rapid purification of synthetic intermediates and products in synthesis, combinatorial chemistry, and automated organic synthesis.

Abstract: Process for the hydrolytic ring cleavage of thiazolidine derivatives to give 2-aminomercaptan derivatives and carbonyl compounds, which comprises bringing an aqueous solution of the thiazolidine derivative into contact with an acidic cation exchanger in the H+ form, giving a solution L1 which contains the carbonyl compound and eluting the cation exchanger with a suitable eluent, giving a solution L2 which contains the 2-aminomercaptan derivative.

Abstract: Novel mixtures of perfluoroalkyl halides and derivatives thereof are described. These mixtures contain some compounds with a straight perfluoroalkyl group and some with a branched perfluoroalkyl group. Methods of preparation and use are also described.

Abstract: Reactions of ring systems, such as aziridines, oxetanes and oxiranes with carboxylic acids, anhydrides, imides, lactones and carbonate esters are catalyzed by C3-C60, substituted or unsubstituted, straight or branched-chained, alkyl, aryl, or aralkyl carboxylate Cr+3 salts, preferably chromium +3 octoate. The catalysts also accelerate the reaction of hydroxy compounds with anhydrides, and of thiiranes with anhydrides. The catalysts selectively enhance the conversion of ring systems to form monomers, prepolymers, copolymers, functional end-group monomers, functional end-group prepolymers, and functional end-group polymers rather than forming homopolymers. By varying the catalyst concentration, molar ratios, and reaction temperatures, the reaction time required to form the desired product can be controlled.

Abstract: Disclosed are novel NO-releasing compounds which comprise a stabilized S-nitrosyl group and a free alcohol or a free thiol group. Also disclosed is a method of preparing the NO-releasing compounds. The method comprises reacting a polythiol or a thioalcohol with a nitrosylating agent. Also disclosed are medical devices coated with the disclosed compounds, methods of delivering NO to treatments sites in a subject by utilizing the medical devices and methods of sterilizing surfaces.

Abstract: The present invention includes methods for treatment and prophylaxis of eye disorders and injuries, particularly treatment and prophylaxis of ocular neovascularization and disorders, especially a vasculopathy that affects retinal or chorodial vessels. The methods of the invention in general comprise administration of a therapeutically effective amount of a compound that inhibits farnesyl-protein transferase to a subject suffering from or susceptible to ocular neovascularization or associated disorder.

Abstract: Heteroatom-interrupted HETE derivatives and methods of their use for treating dry eye are disclosed.

Abstract: A cationic dyeability modifier for incorporation into polyesters and polyamides to increase their affinity for basic dyes, said cationic dyeability modifier having the following formula: R1OOC—(CH2)n—CH(CH2CH2SO3X)—(CH2)m—COOR2 where n is an integer from 1 to 10, m is an integer from 1 to 10, X is an alkali metal selected from the group consisting of lithium, sodium and potassium, and R1 and R2 are independently selected from hydrogen and alkyl groups having one to four carbon atoms is disclosed. Basic dyeable copolyesters and copolyamides containing the cationic dyeability modifier incorporated into the polymer chain of the copolymer are also disclosed. A process for preparing a basic dyeable copolyester by combining poly(alkylene terephthalate)-forming monomers or polyoxyalkylene glycol oligomers with the cationic dyeability modifier, and mixing and heating at a temperature sufficient to cause copolymerization to form a copolyester is also disclosed.

Abstract: Esters of formula: HS—X—COOR in which X denotes a C1-C4 alkylene radical and R a C1-C18 alkyl radical, are prepared by reaction of a hydrosulphide with the corresponding halocarboxylic ester: Y—X—COOR where Y denotes a chlorine or bromine atom. The reaction is performed under a hydrogen sulphide pressure of at least 10 bars absolute, and preferably in an anhydrous or substantially anhydrous alcoholic medium.

Abstract: It has been discovered that compounds of the formula: and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4 and are useful in treating inflammation associated with chronic inflammatory diseases such as rheumatoid arthritis (RA), multiple sclerosis, (MS), asthma, and inflammatory bowel disease (I BD).

Abstract: An alkyl 3-oxoalkanoate, a process for preparation and use for the synthesis of fatty hydroxylated amino acids, fatty amino alcohols and ceramides.

Abstract: Disclosed are novel NO-releasing compounds which comprise a stabilized S-nitrosyl group and a free alcohol or a free thiol group. Also disclosed is a method of preparing the NO-releasing compounds. The method comprises reacting a polythiol or a thioalcohol with a nitrosylating agent. Also disclosed are medical devices coated with the disclosed compounds, methods of delivering NO to treatments sites in a subject by utilizing the medical devices and methods of sterilizing surfaces.

Abstract: Disclosed are novel NO-releasing compounds which comprise a stabilized S-nitrosyl group and a free alcohol or a free thiol group. Also disclosed is a method of preparing the NO-releasing compounds. The method comprises reacting a polythiol or a thioalcohol with a nitrosylating agent. Also disclosed are medical devices coated with the disclosed compounds, methods of delivering NO to treatments sites in a subject by utilizing the medical devices and methods of sterilizing surfaces.

Abstract: The present invention relates to chemically stable, polyfunctional, perfluorinated polyorganosiloxanes (POS) comprising on the one hand fluorinated lateral grafts resulting from the hydrosilylation of perfluorinated olefins with SiH units and having alkyl and/or alkyl ester linkages but not ether linkages, and on the other hand other, non-perfluorinated functional units E capable of giving them diverse and varied physical and chemical properties and opening up avenues in numerous applications. Examples of these POS according to the invention are those of the following formula: According to another of its features, the invention relates to a process for the preparation of these polyfunctional perfluorinated POS. Applications: antifoams, agents for lowering surface tension, dirt repellents, antiadhesives, lubricants, oleophobic and/or hydrophobic agents, coatings etc.

Abstract: The present invention is directed to polymeric- prodrug transport forms of the formula: ##STR1## wherein: B is a leaving group, OH, a residue of a hydroxyl-containing moiety or ##STR2## wherein B.sub.1 is a leaving group, OH or a residue of a hydroxyl-containing moiety;Y.sub.1-2 are independently O or S;M is selected from either X or Q; wherein X is an electron withdrawing group and Q is a moiety containing a free electron pair positioned three to six atoms from C(.dbd.Y.sub.2); R.sub.2-5 are independently selected from the group consisting of hydrogen, C.sub.1-6 alkyls, C.sub.3-12 branched alkyls, C.sub.3-8 cycloalkyls, C.sub.1-6 substituted alkyls, C.sub.3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C.sub.1-6 heteroalkyls and substituted C.sub.1-6 heteroalkyls;(m) is zero or one;(n) is a positive integer;(p) is zero or a positive integer;Z is an electron withdrawing group; andR.sub.

Abstract: This invention relates to matrix metalloproteinase (MMP) inhibiting compounds of the formula: ##STR1## where R.sup.1 is C.sub.1 -C.sub.12 alkyl, straight or branched and optionally substituted by halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, carboxamido, nitrile, mono- or di-(C.sub.1 -C.sub.6)alkylamino, thio, C.sub.1 -C.sub.6 alkylthio, aryl, --Oaryl or --OCH.sub.2 aryl where aryl is optionally substituted with C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, carboxy, halogen, cyano, nitro, carboxamido, or hydroxy; and C.sub.1 -C.sub.6 alkanesulfonyloxy. R.sup.2 is .alpha.-OH or .beta.-OH and R.sup.6 is H or R.sup.2 and R.sup.6 together are carbonyl; the chemical intermediates; and processes for the preparation of these compounds and the intermediates thereto.Matrix metalloproteinases (MMP) are a family of zinc-containing calcium dependent proteinases, including stromelysins, collagenases, and gelatinases.

Abstract: The compounds of Formula I are useful as immunosuppressive agents.

Abstract: The present invention is directed to novel propoxyphene derivatives which are synthesized for the covalent attachment to antigens (proteins or polypeptides) for the preparation of antibodies or receptors to propoxyphene and propoxyphene 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: Novel substantially odor-free polymeric thiol-containing antioxidant compounds suitable for preventing light induced brightness reversion or yellowing of pulps and papers and polymeric materials are described. The novel compounds are based on a polymeric backbone having thiolactate or thioglycolate groups grafted onto the ends thereof and are soluble in water or alcohol.

Abstract: This invention relates to a method comprising reacting an amino acid derivative of the following general formula (I); ##STR1## (wherein R.sup.1 represents an amino-protective group; R.sup.0 represents hydrogen or, taken together with R.sup.1, represents an amino-protecting group; R.sup.2 represents a carboxy-protecting group; X represents a leaving group) with a thiol compound of the following general formula (II) :R.sup.3 SH (II)(wherein R.sup.3 represents an alkyl group of 1 to 7 carbon atoms, an aryl group of 6 to 10 carbon atoms, or an aralkyl group of 7 to 10 carbon atoms) to give a cysteine derivative of the following general formula (III): ##STR2## (wherein R.sup.0, R.sup.1, R.sup.2, and R.sup.3 are as defined above), wherein the reaction is conducted in the presence of a base and water in an organic reaction solvent.

Abstract: Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, m and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described.The compounds of formula I are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.

Abstract: A method of inhibiting bacterial sialidase comprising administering to a subject an inhibiting effective amount of a compound of formula I: ##STR1## wherein A is CO.sub.2 H, PO.sub.2 H, or SO.sub.2 H; B is N; R.sub.1 and R.sub.2 are H; R.sub.3 and R.sub.4 are, independently, H, OH, NO.sub.2, guanidino, or alkyl or alkenyl of from 1 to 3 carbons where the alkyl or alkenyl is unsubstituted or is substituted, independently, with one or more of OH, NH2, or halide; R.sub.5 is H; and R.sub.6 is COCH.sub.3, or COCI.sub.3 ; or an analog, pharmaceutically acceptable salt, derivative, or mixture thereof. A method of preventing a bacterial or trypanosomal infection using the compounds of formula I. A method of treating a bacterial or trypanosomal infection using the compounds of formula I. A pharmaceutical composition comprising a pharmaceutically acceptable carrier admixed with an inhibiting effective amount of a compound of formula I.

Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.

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: Disclosed are detergent compositions comprising:(a) an .alpha.-sulfonated alkyl ester of a fatty acid having an average of about 12-14 carbon atoms;(b) an anionic surfactant; and(c) a nonionic surfactant, and methods for preparing such compositions.

Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.

Abstract: The present invention provides compounds with antioxidant activity effective in treating free radical mediated diseases.

Abstract: The invention provides a method of synthesis of a image-dye forming coupler of formula (I) ##STR1## wherein X is a substituent linked to the coupler by an atom of oxygen, sulfur or nitrogen R.sup.1 is an alkyl or aryl group, R.sup.2 is a hydrogen atom or an alkyl group; R.sup.3 to R.sup.7 are the same or different and selected from a hydrogen atom and substituent groups;which method comprises the reaction of a compound of formula (II) ##STR2## wherein R and R.sup.1 are the same or different and are as defined above for R.sup.1 and X is as defined above with a compound of formula (III) ##STR3## wherein R.sup.2 to R.sup.7 are as defined above, in the presence of an inert organic solvent.

Abstract: A method for the continuous production of esters of thermally unstable acids by the esterification, with or without a catalyst, of the acids with alcohols is provided. The method involves esterification at temperatures of approximately 80.degree. C. to approximately 130.degree. C., essentially in a single reaction zone, to which the acid and an excess of alcohol are continuously supplied and from which a vapor stream containing alcohol and water produced by the esterification reaction are removed, while at the same time removing an ester-rich liquid reaction mixture from the single reaction zone, from which the ester is obtained.

Abstract: Novel brain targeted low molecular weight, hydrophobic antioxidants and use of antioxidants in treatment of central nervous system neurodegenerative disorders such as Parkinson's, Alzheimer's and Creutzfeldt-Jakob's diseases and in treatment of conditions of peripheral tissues, such as acute respiratory distress syndrome, amyotrophic lateral sclerosis, atheroscierotic cardiovascular disease and multiple organ disfunction, in which oxidants are overproduced.

Abstract: Compounds of formula (I) wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, m and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described. The compounds of formula (I) are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.

Abstract: This invention relates to matrix metalloproteinase (MMP) inhibiting compounds of the formula: ##STR1## where R.sup.1 is C.sub.1 -C.sub.12 alkyl, straight or branched and optionally substituted by halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, carboxamido, nitrile, mono- or di-(C.sub.1 -C.sub.6)alkylamino, thio, C.sub.1 -C.sub.6 alkylthio, aryl, --Oaryl or --OCH.sub.2 aryl where aryl is optionally substituted with C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, carboxy, halogen, cyano, nitro, carboxamido, or hydroxy; and C.sub.1 -C.sub.6 alkanesulfonyloxy. R.sup.2 is .alpha.-OH or .beta.-OH and R.sup.6 is H or R.sup.2 and R.sup.6 together are carbonyl; the chemical intermediates; and processes for the preparation of these compounds and the intermediates thereto.Matrix metalloproteinases (MMP) are a family of zinc-containing calcium dependent proteinases, including stromelysins, collagenases, and gelatinases.

Abstract: N-?Mercaptoacyl(amino acid or peptide)! compounds and S-lipophilic aliphatic carbonyl derivatives thereof, and pharmaceutical compositions comprising such compounds, as well as the use of these compounds as antihypertensives by the inhibition of neutral endopeptidase and/or peptidyldipeptidase A are disclosed. Methods for preparing such compounds and derivatives are disclosed also.

Abstract: Esters of formula:HS--X--COORin which X denotes a C.sub.1 -C.sub.4 alkylene radical and R a C.sub.1 -C.sub.18 alkyl radical, are prepared by reaction of a hydrosulphide with the corresponding halocarboxylic ester:Y--X--COORwhere Y denotes a chlorine or bromine atom. The reaction is performed under a hydrogen sulphide pressure of at least 10 bars absolute, and preferably in an anhydrous or substantially anhydrous alcoholic medium.

Abstract: The present invention relates to glutathione monoester sulfonate represented by formula (I): ##STR1## (wherein R.sup.1 represent lower alkyl, and R.sup.2 represents lower alkyl, or substituted or unsubstituted aryl) which readily crystallizes and has high stability, and a simple process for producing the same. According to the process, the product having high purity can be obtained in high yields.

Abstract: An acetamide derivative having the general formula (I): ##STR1## or a pharmacologically acceptable salt thereof; a synthetic intermediate of the above-mentioned acetamide derivative; a treating agent for peptic ulcer and for gastritis which comprises the above-mentioned compound having the general formula (I) as an effective ingredient, and a process for treating peptic ulcer and gastritis using the above-mentioned compound having the general formula (I), are disclosed.

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: The invention relates to an improved process for the preparation of thioglycolic acid alkyl esters by heating a reaction mixture which essentially comprises thioglycolic acid, an alcohol and an acid catalyst, the water formed being removed by distillation using a water separator, in which the resulting product mixture is passed over a basic ion exchanger, if appropriate after removal of the acid catalyst.

Abstract: A process comprises contacting, in the presence of a catalyst, hydrogen sulfide or a mercaptan such as, for example, n-dodecyl mercaptan with an .alpha.,.beta.-unsaturated carbonyl or .alpha.,.beta.-unsaturated cyano compound such as, for example, methyl acrylate wherein the catalyst comprises a pyridine derivative such as, for example, 4-(dimethylamino)pyridine or an ion exchange resin such as, for example, "AMBERLYST A-21" to produce a 3-hydrocarbylthio derivative of the .alpha.,.beta.-unsaturated carbonyl or .alpha.,.beta.-unsaturated cyano compound such as, for example, methyl 3-(dodecylthio)propionate.

Abstract: This invention relates to compounds and methods for use in determining renal function by means of scintigraphic urography. More specifically, this invention relates to radionuclide complexes of ester-substituted diaminethiols, radiopharmaceutical compositions comprising said complexes, kits for the preparation of said compositions, and a method of using said compositions for examining renal function. Compounds of this invention have the formula: ##STR1## wherein the various groups are as defined herein.

Abstract: The hair shaping composition for permanent shaping of hair contains a cysteine ester of the formula (I):HS--CH.sub.2 --CH(NH.sub.2)--COO--CH.sub.2 --CH.sub.2 --R (I)as a keratin-reducing material, wherein R is a hydroxy group, alkoxy groups, a poly(alkoxy) group or a hydroxypoly(alkoxy) group, or one of its acid additional salts. Cysteine ester compounds and their methods of preparation are also described. Preferred embodiments of the hair shaping composition have a pH of from 4.5 to 9.0 and contain from 4 to 30% by weight of the cysteine ester or its acid addition salt and provide a safe and uniform shaping of hair without allergic or sensitizing reactions.