Abstract: A stereoselective process for the industrial synthesis of compounds of formula (I): wherein R represents linear or branched (C1-C6)alkyl, and application in the synthesis of perindopril and pharmaceutically acceptable salts thereof.

Abstract: The invention relates to a process for the preparation of an &ohgr;-benzyl ester of an amino diacid, characterized in that the amino diacid is reacted with a benzyl alcohol derivative of formula (I) 1

Abstract: Disclosed is a silver halide photographic light-sensitive material having one or more layers including a light-sensitive silver halide emulsion layer on a support, wherein any of the layers contains the specific fluorine compound. The silver halide photographic light-sensitive material can be stably produced and is imparted with antistatic property.

Abstract: An inner salt of L-carnitine is prepared by reduction, with a suitable reducing agent, of a compound of formula (I): 1

Abstract: The present invention provides biodegradable polyesters based on lower hydroxy acids and hydroxy fatty acids. The resulting polyesters are useful as cosmetic vehicles for sunscreens, skin lotions and by themselves are also useful as milder skin exfoliants.

Abstract: The present invention provides a method for preparing an amino acid monoester from an amino acid diester without the use of an enzyme. Particularly, the method involves hydrolysis of an amino acid diester in the presence of a non-enzyme additive and under reaction conditions that affect selective hydrolysis of the &agr;-ester group. The reaction conditions comprise a specific pH, temperature, and vapor pressure.

Abstract: The present invention involves a process for preparing protected amino acids. The process produces a di-tert-butyl amino ester or an N-protected di-tert-butyl amino ester by transesterification of an acidic amino acid or an N-protected acidic amino acid. By-products of the transesterification reaction may be recycled for use as part of the starting material. The N-protected di-tert-butyl amino ester may be hydrogenated to form a di-tert-butyl amino ester, which may subsequently form a di-tert-butyl ester hydrocholride salt.

Abstract: the present invention provides novel compounds represented by formula I: 1

Abstract: This invention relates to novel substituted succinic acid metallo-&bgr;-lactamase inhibitors which are useful potentiators of &bgr;-lactam antibiotics. Accordingly, the present invention provides a method of treating bacterial infections in animals or humans which comprises administering, together with a b-lactam antibiotic, a therapeutically effective amount of a compound of formula I: including pharmaceutically acceptable salts, prodrugs, anhydrides, and solvates thereof.

Abstract: The present invention is directed to novel dipeptides thereof, represented by the general Formula I: 1

Abstract: The invention relates to novel diazoketone derivatives. The invention also relates to processes for homologation of these diazoketone derivatives. The processes are useful for preparing compounds that are caspase inhibitors.

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: Methods for the preparation of an N-alkyl-N-bis-(2-( 1,2-dicarboxy-ethoxy)-ethyl)-amine derivative are described, products of the methods as well as uses of the products. The derivative is prepared by reacting an alkali or earth alkali metal salt of maleic acid with an N-substituted diethanolamine, the reaction taking place with the two ethanol groups of the diamine while the substituent group bound to the N atom remains unaffected, or alternatively by first reacting diethanolamine with an alkali or earth alkali metal salt of maleic acid to yield N-bis-(2-(1,2-dicarboxy-ethoxy)-ethyl)-amine, which is then reacted with a substitution reagent to obtain the final product. The derivative is useful as chelating agents, e.g., in the bleaching of chemical or mechanical pulp or in textile bleaches containing hydrogen peroxide or a peracid, or as a calcium binder in detergents and cleaning agents.

Abstract: Stereoselective process for the industrial synthesis of compounds of formula (I): 1

Abstract: A method for forming cascade polymers specifically utilizing the amine monomer of the formula 1

Abstract: The present invention provides biodegradable polyesters based on lower hydroxy acids and hydroxy fatty acids. The resulting polyesters are useful as cosmetic vehicles for sunscreens, skin lotions and by themselves are also useful as milder skin exfoliants.

Abstract: Stereoselective process for the industrial synthesis of compounds of formula (I): 1

Abstract: A process for preparing amino derivatives of C—H-acid compounds of the general formula I where R is an alkyl group, a cycloaliphatic radical, an aryl radical, an alkylaryl radical or an aralkyl radical, and X1 and X2 are identical or different electron-withdrawing groups, by reacting compounds of the general formula II with nitrous acid, where the nitrosation is carried out in the presence of from 1 to 10 mol of a carboxylic anhydride, and the reaction product is subjected to catalytic hydrogenation, where appropriate after removing the salts derived from the reaction. Compounds of the general formula I are useful intermediates for compounds which can be used in the pharmaceutical and agricultural sectors.

Abstract: Novel glucocorticoid and thyroid receptor ligands as provided which have the general formula (I): in which R1 is an aliphatic hydrocarbon, an aromatic hydrocarbon, carboxylic acid or ester thereof, alkenyl carboxylic acid or ester thereof, hydroxy, halogen, or cyano, or a pharmaceutically acceptable salt thereof. R2 and R3 are the same or different, and are hydrogen, halogen, alkyl of 1 to 4 carbons, or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen. X is carbonyl or methylene. R4 is an aliphatic, aromatic or heteroaromatic. Y is hydroxyl, methoxy, amino, or alkyl amino. n is an integer from 0 to 4. A method for treating diseases associated with metabolism dysfunction or which are dependent on the expression of a glucocorticoid or thyroid receptor gene such as diabetes, hypercholesterolemia, or obesity using these compounds is also disclosed.

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: Disclosed are prodrug compounds of a class of alkyl carboxy amino acid analogs of glutamic acid that act as specific regulators of the kainate EAA receptor cation channel. These compounds are useful for treating neurological, neuropsychological, neuropsychiatric, neurodegenerative, neuropsychopharmacological and functional disorders associated with excessive or insufficient activation of the kainate subtype of the ionotropic EAA receptors; treating cognitive disorders associated with deactivation, suboptimal activation or over-activation of the kainate receptor; alleviating pain and improving and enhancing memory, learning, and associated mental processes.

Abstract: A process for preparing compounds of the formula IIb  where R is C6-C30-alkyl or C6-C30-alkenyl, which may additionally have upto 5 hydroxyl groups, formyl groups, C1-C4-alkoxy groups, phenoxy groups or C1-C4-alkoxycarbonyl groups as substituents and may be interrupted by upto 5 nonadjacent oxygen atoms, or alkoxylate groups of the formula —(CH2)k—O—(A1O)m—(A2O)n—Y where A1 and A2 are, independently of one another, 1,2-alkylene groups having 2 to 4 carbon atoms, Y is hydrogen, C1-C12-alkyl, phenyl or C1-C4-alkoxycarbonyl, and k is 1, 2 or 3, and m and n are each numbers from 0 to 50, and the total of m+n must be at least 4, by reacting iminodiacetonitrile with aldehydes of the formula R—CHO and HCN or alkali metal cyanides, the process being carried out a) in the absence of an organic solvent and in the presence of a Lewis or Brönsted acid, or b) in the presence or absence of an organic solvent and in the presence of an emulsifier, or c)

Abstract: Polyacetylene compounds and process for the preparation thereof from a chiral dihydroxy amide are described. The compounds preferably have diacyl groups attached to the amide. The compounds are useful for making films which are electrically conductive, near infrared absorbing, polarizing, and have the characteristic optical and other properties of polyacetylenes.

Abstract: This invention features methods of biphasic synthesis for synthesizing combinatorial libraries and combinatorial libraries of chemical compounds utilizing the template, and combinatorial libraries of chemical compounds formed by the methods of this invention.

Abstract: Methods are disclosed for preparing partial and complete esters of poly-&ggr;-glutamic acid, and of the cross-linking of such esters by light of predetermined wavelength. The final products of the present invention are useful in local drug delivery in depot form, for guided tissue regeneration, and for inhibition of post-surgical adhesion.

Abstract: This invention relates to pentaerythritol lipid derivatives which are useful for the intracellular delivery of polynucleotides. These cationic lipids are useful in the preparation of liposomes and other lipid vesicles for the delivery of nucleic acids into mammalian cells.

Abstract: New water-soluble polyperfluoroalkyl surfactants derived from functional polycarboxylic polymers, characterized by the fact they have alco-oleophobic properties, to be used in the make-up of protein or synthetic foam for extinguishing fires caused not only by hydrocarbons, but also by polar liquids (alcohol, ethers, esters, etc.) without requiring the use of thickening agents, such as polysaccharides.

Abstract: Iodopropargylamine compound of the general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 each independently represent a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, or R.sup.1 and R.sup.2 combine with each other to form a tetramethylene group or a pentamethylene group, R.sup.3 represents a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, and X and Y each independently represent a cyano group, an alkoxycarbonyl group having 2 to 7 carbon atoms, an alkylcarbonyl group having 2 to 7 carbon atoms, an alkylsulfonyl group having 1 to 6 carbon atoms, a phenylcarbonyl group or a phenylsulfonyl group, provided that the phenyl group of a phenylcarbonyl group or a phenylsulfonyl group may be optionally substituted by halogen atoms, alkyl groups having 1 to 3 carbon atoms, alkoxy groups having 1 to 3 carbon atoms, nitro groups or trifluoromethyl groups.

Abstract: This invention relates to pentaerythritol lipid derivatives which are useful for the intracellular delivery of polynucleotides. These cationic lipids are useful in the preparation of liposomes and other lipid vesicles for the delivery of nucleic acids into mammalian cells.

Abstract: The present invention relates to a novel intermediate compound for preparing optionally substituted 1,2,4-triazolinones and a process for preparing that intermediate compound.

Abstract: The invention relates to amphiphilic compounds of the general formula I ##STR1## with at least two hydrophilic and at least two hydrophobic groups based on alkoxylated amines and/or alkoxylated fatty acid amides and di-, oligo- or polycarboxylic acids (spacer A). Y and Z are hydrogen or functional groups. The amphiphilic compounds according to this invention are usually surface-active and are suitable as emulsifiers, demulsifiers, detergents, dispersants and hydrotropes in industry and domestically, for example in the areas of metal processing, ore production, surface treatment, washing and cleaning hard surfaces, such as, for example, the manual cleaning of crockery, washing and cleaning skin and hair, cosmetics, medicine and food processing and preparation.

Abstract: A process for making derivatized polymers of maleic anhydride containing maleamic acid and its corresponding cyclic imide repeat units, in alcohol solution, at a temperature of about 60-160.degree. C., during a reaction period of about 1-25 hours. The product is a polymer having a predetermined ratio of the above repeat units.

Abstract: The present invention relates to mixtures of .alpha.-amino acids and/or derivatives thereof and cyclopentane-.beta.-amino acids and/or derivatives thereof, dipeptides of the abovementioned .alpha.-amino acids and cyclopentane-.beta.-amino acids and mixtures of the abovementioned mixtures and dipeptides which have an improved tolerability in warm-blooded animals compared with the pure cyclopentane-.beta.-amino acids.

Abstract: The present invention provides a process to prepare a pyridine-2,3-dicarboxylate derivative via the reaction of a dailkyl alkoxy(or alkylthio)oxalacetate with an appropriately substituted acrolein compound in the presence of an ammonia source and a solvent.The present invention also provides useful intermediate compounds of formula IV.

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: Compounds of formula I: ##STR1## wherein R.sub.a, R.sub.b, .PHI., B and R are as defined in the disclosure, have antagonistic activity on osteoclast hyper-reactivity.

Abstract: Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and m is 1 or 2, R.sup.1 is hydrogen, C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, phenyl, naphthyl, C.sub.1-10 alkyl-phenyl, C.sub.2-10 alkenyl-phenyl or C.sub.2-10 alkynyl-phenyl, said phenyl and naphthyl groups being optionally substituted, R.sup.2 is hydrogen or a protecting group, and Q is an acidic group; or a salt or ester thereof.

Abstract: The invention relates to a process for the preparation of aminomalonic acid esters and optionally their salts by the catalytic hydrogenation of a substituted malonic acid ester in an inert solvent, and optionally by the addition of an acid to the hydrogenation mixture. The process comprises carrying out the hydrogenation in the presence of a solid dehydrating agent and a solvent or solvent mixture in which the aminomalonic acid ester salt is substantially insoluble.

Abstract: Glycine-N, N-diacetic acid derivatives are prepared by reacting corresponding 2-substituted glycines, 2-substituted glycinonitriles, doubled glycines, or precursors of the glycine derivatives with formaldehyde and alkali metal cyanide. The reaction is conducted in an aqueous medium at a pH of 8 to 14. From 0, 5 to 30% of the amount of alkali metal cyanide required for the reaction are added to the glycine derivatives or precursors thereof Subsequently, the remaining amount of alkali metal cyanide and the formaldehyde are simultaneously metered in over a period of from 0.5 to 12 hours.

Abstract: Hydroxamic acids and hydroxamic acid ethers I and II ##STR1## where Z.sup.1 and Z.sup.2 are --NH --OY, --NR.sup.1 --OY or --OX, where in the case of (I) at least one of Z.sup.1 or Z.sup.2, and in the case of (II) Z.sup.1 is --NH --OY or --NR.sup.1 --OY, andR.sup.1 is C.sub.1 -C.sub.18 -alkyl,X is hydrogen, alkali metal, ammonium or substituted ammonium, andY is hydrogen, alkali metal, ammonium, substituted ammonium or C.sub.1 -C.sub.18 -alkyl, andL is a C.sub.1 -C.sub.100 linker which can also carry oxygen and nitrogen functional groups,with the exception of N,N-bis(carboxymethyl)-2-aminoacetohydroxamic acid.

Abstract: A star-like or comb-like branched aliphatic polyamino compound for use as a basic catalyst or a curing agent, as an effective thixotropic agent or viscosity adjusting agent for an aqueous medium, as a component for any one of a coating-forming agent, a sealing agent, a molding material and an adhesive resin, or as a substantially solvent-free coating composition, molding material or adhesive resin. The process for the production of the above compound comprises (a) forming an adduct of ammonia or an aliphatic amino compound having an amino group (compound A) with methyl acrylate, adding an alkylenediamine having 2 to 12 carbon atoms to the adduct to carry out an ester-amide exchange reaction (b), thereby obtaining a polyamino compound (B) having a total of 2 to 100 aliphatic primary amino and secondary amino groups per molecule and having a number average molecular weight of 170 to 10,000, and forming an adduct of the polyamino compound (B) with an acrylic acid ester (C) of the formula (1),CH.sub.2 =CHCOO--R.

Abstract: Lysine derivatives, the salts of the derivatives, their optical isomers of D or L configuration, or their mixtures, the derivatives containing an N.sup..epsilon. -alkoxy or N.sup..epsilon. -alkenoxycarbonyl group of formula: ##STR1## in which: R represents a linear or branched C.sub.13 -C.sub.24 alkyl radical, the C.sub.16 radical being branched, or a linear or branched C.sub.8 -C.sub.24 alkenyl radical. The lysine derivatives are used in cosmetic, pharmaceutical hygiene or food compositions.

Abstract: Linear oligomer polychelant compounds and chelates formed therewith have alternating chelant and linker moieties bound together by amide or ester moieties. The compounds have between 3 and 100 chelant moieties, at least one of which complexes a paramagnetic metal ion. The polychelants and especially their paramagnetic metal polychelates are particularly suitable for diagnostic imaging.

Abstract: A process for removing .beta.-hydroxy groups from .beta.-hydroxy-containing compounds is disclosed. The process involves the use of a retro-aldol-promoting reagent selected from the group of trimethylamine-N-oxide, triethylamine-N-oxide, trimethylamine-N-oxide-hydrate, and trimethylamine-hydrate and requires dissolution of the substrate in an aprotic solvent and reaction under elevated temperatures. The process is broadly applicable to a variety of substrates including complex cyclic peptides, linear peptides, and non-peptides.

Abstract: This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.

Abstract: Reaction products of amino-alkylenecarboxylic acids with polyoxyalkylene compounds are used as paraffin dispersants for mineral oil middle distillates.

Abstract: The present invention relates to a process for the preparation of quaternary diesters of the formula: ##STR1## wherein X.sup.- represents a halogen atom, R.sub.1 and R.sub.2 are the same or different and are selected from an alkyl group having 1 to 3 carbon atoms or a hydroxyethyl group, or may be linked together to form an alkylene group having 4 to 6 carbon atoms which may be interrupted by an N atom or O atom, and R.sub.3 and R.sub.4 are the same or different and are selected from an alkyl group or alkenyl group having 8 to 22 carbon atoms, or may be linked together to form an alk(en)ylene group having 8 to 22 carbon atoms. In the processa) a secondary amine of the formula R.sub.1 --NH--R.sub.2 is gradually added to and converted with one or more liquid compounds of the formula ##STR2## a molar ratio in the range of 1.0:1.0 and 1.0:1.

Abstract: To provide an aqueous fabric softener composition, which is excellent in softening performance, elasticity and storage stability, and a quaternary ammonium salt which is useful as a softening base of this composition and nondetrimental to the natural environment because of its excellent biodegradability, and a process for the preparation of this salt.The aqueous fabric softener composition of the present invention comprises from 8 to 40% by weight of a quaternary ammonium salt represented by the following formula (I), a quaternary ammonium salt represented by the following formula (II) or a mixture thereof, and water: ##STR1## wherein R.sup.1 and R.sup.2 represent each a C.sub.1-4 alkyl group, etc.; R.sup.3 and R.sup.4 represent each a C.sub.7-35 alkyl group, etc.; and X.sup.- represents an anion group; and ##STR2## wherein R.sup.5 and R.sup.6 represent each a C.sub.1-4 group, etc.; R.sup.7 and R.sup.8 represent each a C.sub.1-5 alkylene group, etc.; R.sup.9 and R.sup.10 represent each a C.sub.

Abstract: Dendritic derivatives of 3,5-bis(aminomethyl)benzene and aminomethyl benzene core groups are disclosed. In each derivative, termed an "amplifier" because the dendritic structure on each molecule terminates with multiple termini to each of which an "active group" can be attached, the desired effect of the active group per mole is amplified compared to conventional compounds having only one active group per molecule. Amplifier molecules can include a targeting group permitting the molecules to preferentially attach to a particular anatomical or physiological situs. Active groups are any of various pharmacologically or therapeutically active moieties, including moieties useful for magnetic-resonance contrast enhancement. The dendritic structures comprise linkers and branch groups covalently bonded to each other in any of various structural combinations. The amplifiers can be prepared as a solution or mixture with a physiologically compatible carrier for administration to a warm-blooded animal subject.

Abstract: The present invention relates to hyperbranched polyaspartate esters containing repeating structural units corresponding to the formula I and/or II ##STR1## The present invention also relates to a process for the preparation of these hyperbranched polyaspartate esters by self condensing, via a transesterification reaction, at least a portion of the hydroxy and ester groups of the hydroxy aspartates corresponding to the above formula at a temperature of 60.degree. to 240.degree. C. to form hyperbranched polyaspartate esters and eliminating alcohols having the formula R.sub.1 --OH and/or R.sub.2 --OH.