Abstract: According to the present invention, a tumor diagnostic agent which carries out early stage detection, monitoring of therapeutic effect and prognostic diagnosis of all tumors The tumor diagnostic agent of the present invention is a tumor diagnostic agent comprising ?-aminolevulinic acid represented by formula (I), a derivative thereof and a salt thereof: R2R1NCH2COCH2CH2COR3 ??(I) wherein R1 and R2 each independently represents hydrogen, alkyl, acyl, alkoxycarbonyl, aryl or aralkyl; and R3 represents hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, aryloxy, aralkyloxy or amino, which is used for diagnoses by measuring porphyrins in a sample collected from the inside or outside of the body after its administration.

Abstract: The present invention provides an acid addition salt of 5-aminolevulinic acid (5-ALA) or of a 5-ALA derivative (e.g. a 5-ALA ester) with an acid which has a pKa of about 5 or less, preferably about 3 or less, with the proviso that the acid is other than hydrochloric acid. Particularly preferred salts are those derived from acids selected from the group comprising sulphonic acid and its derivatives, hydrobromic acid, sulfuric acid, nitric acid and phosphoric acid. The salts in accordance with the invention are particularly suitable for use as photosensitizing agents in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body.

Abstract: The present invention relates to 5-azido levulinic acid, a process for its preparation, its use. Using 5-azido levulinic acid as starting material for the synthesis of 5-amino levulinic acid hydrochloride it is possible to obtain the latter in good yield an in pharmaceutical acceptable quality. 5-Azido levuliniv acid is synthesized in that methyl 5-bromo levulinate and/or methyl 5-chloro levulinate is converted with aqueous hydrochloric acid and as a result of an incomplete bromine/chlorine exchange at the C-5-postion a mixture of 5-chloro levulinic acid and 5-bromo levulinic acid is obtained, and the obtained 5-chloro levulinic acid, a mixture of 5-chloro levulinic acid and 5-bromo levulinic acid and the pure 5-bromo levulinic acid is transferred into 5-azido levulinic acid by conversion with a nucleophilic azide.

Abstract: The invention relates to novel synthesis methods for the preparation of the intermediates, which are suitable for the preparation of statin derivatives, especially to novel synthesis methods of the intermediate of formula VI wherein Ra? and Rc? are each independently of the other hydrogen or a hydroxy-protecting group or together are a bridging hydroxy-protecting group, and Rb is a carboxy-protecting group, which methods are carried out by conversion of the intermediate of formula XVI wherein Ra? and Rc? are each independently of the other hydrogen or a hydroxy-protecting group, R* and R** are each independently of the other hydrogen or an amide-protecting group, and Rb is a carboxy-protecting group; which methods proceed to further new intermediates and methods for their preparation

Abstract: Disclosed is a process for the manufacture of pseudo proline dipeptides of the formula wherein R1 is a side chain of an alpha amino acid, R2 is an amino protecting group and R3 and R4 are independently either hydrogen or C1-4-alkyl, and R5 is hydrogen or methyl starting from an amino acid derivative of the formula wherein R1 and R2 are as defined above. Pseudo proline dipeptides can be used as reversible protecting groups for Ser, Thr and Cys and thus are versatile tools in peptide chemistry.

Abstract: Initiators for atom transfer radical polymerizations are described. The initiators have an azlactone or ring-opened azlactone moiety to provide telechelic (co)polymers.

Abstract: The invention relates to a novel process for hydroxymethylating noncyclic ?,?-dialkylcarboxylic acid derivatives with formaldehyde using amide bases at temperatures of from ?40° C. up to the boiling point of the solvent or solvent mixture used.

Abstract: The invention provides anti-apoptotic compositions containing lysophosphatidic acids and methods for making and using the compositions. Such compositions may also contain LPA potentiating agents, including proteins, lipid membrane structures and polymers such as polyethylene glycols. The compositions can additionally contain other pharmaceutically effective agents such as drugs, antibiotics, wound healing agents and antioxidants.

Abstract: The invention relates to the compound of the formula 1 and to its physiologically acceptable salts. The compound is suitable, for example, as a hypolipidemic.

Abstract: The present invention is directed to the use of compounds of the formula: for treating pain, in particular neuropathic pain, bipolar disease and migraine headaches.

Abstract: The present invention is directed to the use of compounds of the formula: for treating pain, in particular neuropathic pain, bipolar disease and migraine headaches.

Abstract: Hydroxy-amino acids are provided and are prepared by contacting a substituted ?-ketodiester having a ketone group and two ester functional groups with a ketoreductase under conditions permitting the reduction of the keytone group to an alcohol. Only one of the ester functional groups is regioselectively hydrolyzed to the corresponding carboxylic acid, whereby a non-hydrolyzed ester functional group remains. The carboxylic acid is converted to an amine to produce a hydroxy-amino acid.

Abstract: The present invention provides a process for preparing 3-amino-2-hydroxypropionic acid derivatives (1) which does not use dangerous reagents, is economically advantageous, and is suitable for an industrial production, which process comprises: treating N-protected-3-amino-2-hydroxypropionic acid derivatives (2) having a steric configuration at 2-position carbon reverse to that of derivatives (1) with a leaving group-introducing agent to convert into N-protected-3-aminopropionic acid derivatives (3), then treating the derivatives with a basic substance to convert into substituted-3-amino-2-hydroxypropionic acid derivatives (4) having an inverted steric configuration at 2-position carbon, and then converting the derivatives into 3-amino-2-hydroxypropionic acid derivatives (1).

Abstract: The instant invention discloses a process for the preparation of compounds of the formula I: wherein the general symbols are as defined in claim 1, which process comprises reacting a compound of formula II: wherein the general symbols are as defined in claim 1, with a compound of the formula III: wherein R5 is as defined in claim 1. The compounds of the formula II are new and useful as stabilizers for protecting organic materials, in particular synthetic polymers, reprographic materials or coating materials against oxidative, thermal or light-induced degradation.

Abstract: Initiators for atom transfer radical polymerizations are described. The initiators have an azlactone or ring-opened azlactone moiety to provide telechelic (co)polymers.

Abstract: Compounds of the formula I, in which R1, R2, R3, R4, R5, and R6 have the meanings given in the description, and their physiologically acceptable salts. The compounds are suitable for use, for example, as hypolipidemics.

Abstract: The invention provides anti-apoptotic compositions lysophosphatidic acids and methods for making and using the compositions. Such compositions can also contain LPA potentiating agents, including proteins, lipid membrane structures and polymers such as polyethylene glycols. The compositions can additionally contain other pharmaceutically effective agents such as drugs, antibiotics, wound healing agents and antioxidants.

Abstract: The present invention is directed to the use of compounds of the formula: for treating pain, in particular neuropathic pain, bipolar disease and migraine headaches.

Abstract: The invention includes selected novel optically active ?-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.

Abstract: A methods for producing a hydroxy-amino acid or derivative thereof, such as statine, phenylstatine or isostatine, is provided. A substituted &bgr;-ketodiester having a ketone group and two ester functional groups is contacted with a ketoreductase under conditions permitting the reduction of the ketone group to an alcohol. Only one of the ester functional groups is regioselectively hydrolyzed to the corresponding carboxylic acid, whereby a non-hydrolyzed ester functional group remains. Either the carboxylic acid or the non-hydrolyzed ester functional group is converted to an amine or a derivative thereof to produce a hydroxy-amino acid or derivative thereof.

Abstract: Provided is a method of preparing a hydroxyamino acid derivative, particularly in an optically active form thereof with high efficiency.

Abstract: R or S aminocarnitine, R or S phosphonium aminocarnitine and R and S 3,4 diaminobutanoic acid, and their derivatives are prepared using starting from aspartic acid with the same configuration as the desired compounds. This process is advantageous from the industrial point of view in terms of the type of reactants used, the reduced volumes of solvents and the possibility of avoiding purification of the intermediate products.

Abstract: The present invention relates to a method for producing a saturated organic compound bearing at least one functional group from a mixture which comprises this saturated organic compound containing at least one functional group and also one or more other organic compounds, which comprises

Abstract: Glyceric acid compounds of the formula (I)

Abstract: A methods for producing a hydroxy-amino acid or derivative thereof, such as statine, phenylstatine or isostatine, is provided. A substituted &bgr;-ketodiester having a ketone group and two ester functional groups is contacted with a ketoreductase under conditions permitting the reduction of the ketone group to an alcohol. Only one of the ester functional groups is regioselectively hydrolyzed to the corresponding carboxylic acid, whereby a non-hydrolyzed ester functional group remains. Either the carboxylic acid or the non-hydrolyzed ester functional group is converted to an amine or a derivative thereof to produce a hydroxy-amino acid or derivative thereof.

Abstract: Perfluoroalkyl-substituted amines, acids, amino acids and thioether acid compounds containing a perfluoroalkyl-iodoalkyl or perfluoroalkyl-alkene group as well as derivatives thereof, are described. They are useful as surfactants in a variety of applications where low surface tensions are required, including coating formulations for glass, wood, metal, cement, paper, textiles, as foam control agents in polyurethane foams and especially in aqueous fire-fighting formulations.

Abstract: The present invention provides a process for preparing 3-amino-2-hydroxypropionic acid derivatives (1) which does not use dangerous reagents, is economically advantageous, and is suitable for an industrial production, which process comprises:

Abstract: An inner salt of L-carnitine is prepared by reduction, with a suitable reducing agent, of a compound of formula (I): where X1 and X2, which may be the same or different, are hydroxy, C1-C4 alkoxy, phenoxy, halogen, or X1 and X2, when taken together are an oxygen atom and the resulting compound is a derivative of succinic anhydride; Y is halogen, the mesyloxy or the tosyloxy group: and subsequent treatment with water, then with a base and then with trimethylamine.

Abstract: A method for transferring amino acid into ketone acid (ester) may obtain ketone acid (ester) at low cost. The method uses sodium hypochlorous acid as oxidizing agent and proceeds oxidation reaction with amino acid or its derivatives so as to obtain ketone acid and its derivatives. The sodium hypochlorous acid is easily to get with low cost and the conditions of the reaction are mild so that the method meets the needs of the industry.

Abstract: The invention provides a process for the preparation of compounds of the formula (1) 1

Abstract: Seryl-lysyl-based peptide and peptidomimetic compounds are described as inhibitors of the enzyme N-myristoyl transferase to provide selective control of the fungal organism Candida albicans. Peptidomimetic compounds of particular interest are those of the formula: wherein R1 is selected form aminoalkyl, p-aminoalkylphenylalkyl, imidazolylalkylphenylalkyl, 2-alkylimidazolylalkylphenylalkyl, benzimidazolylalkylphenylalkyl and 2-alkylbenzimidazolylalkylphenylalkyl; wherein R2 is selected from hydrido, alkyl, cycloalkyl, akenyl, alkynyl, haloalkyl, benzyl, alkylphenylalkyl, alkoxyphenylalkyl, halophenylalkyl, phenethyl, cycloalkylalkyl, halocycloalkylalkyl, alkylcycloalkylalkyl, alkoxycycloalkylalkyl and naphthylalkyl; wherein Y is selected from carboxylic acid, hydroxamic acid, phosphonic acid and tetrazolyl; or a pharmaceutically-acceptable salt, amide or ester thereof. Compounds of the formula are species-specific inhibitors of C.

Abstract: The instant invention is improved gamma amino butyric acid analogs, processes for their preparation, and methods of using them as agents for treating epilepsy and other neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal damage, and inflammation.

Abstract: A synthetic reaction to produce [2-(2-aminoethoxy)ethoxy] acetic acid (AEEA) derivatives. This synthetic reaction does not require isolation and purification of intermediates. The AEEA derivatives can be used to synthesize high load polystyrene-polyethylene glycol-like resins having excellent swelling characteristics.

Abstract: A 6-aminocarbonylmethyl-4H-2,3-dioxin-4-one compounds can be produced by reacting a 6-halomethyl-4H-2,3-dioxin-4-one compound with a primary or secondary amine and carbon monoxide. The reaction may be carried out in the presence of a catalyst comprising a platinum group metal. 3-oxopentanedicarboxylic acid monoamides and 3-oxopentanedicarboxylic acid amide esters can be are produced by reacting 6-aminocarbonylmethyl-4H-2,3-dioxin-4-one compound with an alcohol or water. Using such intermediates, 6-aminocarbonylmethyl-4H-2,3-dioxin-4-one compound, 3-oxopentanedicarboxylic acid amide esters can provide in an easy and simple and efficient manner.

Abstract: An improved process is described for the industrial preparation of L-carnitine or alkanoyl L-carnitine mucate, which allows operations in a homogeneous phase in conditions of greater dilution, in a normal chemical reactor with stirring, in a batch process.

Abstract: Complexes of hyaluronic acid and carnitine of its derivatives and the simple combinations of them are useful in therapeutics and cosmetics. They have pharmacological activity, that is protective activity on tissues and cell plasma membrane, anti-inflammatory, radical scavenging activities and the like, was well as cosmetic activity, such as restoring or maintaining cutaneous elasticity.

Abstract: A process of preparing an acid addition salt of delta-aminolevulinc acid comprising: a) dissolving a lower alkyl 5-bromolevulinate and hexamethylenetetramine in a solvent selected from the group consisting of water, ethyl acetate, chloroform, acetone, ethanol, tetrahydrofuran and acetonitrile, to form a quaternary ammonium salt of the lower alkyl 5-bromolevulinate; and b) hydrolyzing the quaternary ammonium salt with an inorganic acid to form an acid addition salt of delta-aminolevulinic acid.

Abstract: The present invention describes a process for the industrial production of L-carnitine, comprising the enantioselective reduction of an alkyl 4-chloro-3-oxobutyrate or 4-chloro-3-oxobutyramide. The optically active 3-hydroxy derivative thus obtained is reacted with trimethylamine, obtaining crude L-carnitine, which is then finally purified. The catalyst used for the reduction is a complex of ruthenium bound to a penta-atomic bis-heteroaromatic system. The reduction reaction, performed in controlled conditions of hydrogen pressure, substrate concentration, temperature, and substrate: catalyst molar ratio, enables 4-chloro-3-hydoxybutyrate or 4-chloro-hydroxybutyamide to be obtained in a high yield. The process described, which leads to L-carnitine being obtained, is easily applicable on an industrial scale.

Abstract: Carnitine derivatives of formula (I) are described in racemic and/or optically active form, as well as the process for their preparation and their use as pharmaceutical anti-angina active ingredients for the treatment of ischaemic heart disease. Also described is a process for producing the (R)-carnitine enantiomer from (S)-carnitine (or vice versa), using the derivatives of formula (I).

Abstract: The invention includes selected novel optically active &agr;-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.

Abstract: A pharmaceutical product which comprises admixed or separately packaged (A) L-Carnitine or an alkanoyl L-canitine and (B) a trihydroxy- or tetrahydroxystilbene such as resveratrol is useful for the prevention and treatment of pathological neuronal or cerebral disorders.

Abstract: Non-hygrocopic salts of L-carnitine and of the lower alkanoyl L-carnitines with pamoic acid are described, which are used to prepare solid compositions suitable for oral administration. Solid compositions containing such salts are also described.

Abstract: Inhibitors of phosphoserine- or posphothreonine-specific peptidyl prolyl isomerases are described. Such inhibitors include molecules that mimic the structure and conformation of the pSer/pThr-Pro peptide moiety of the isomerase substrate when the substrate is bound into the active site of the isomerase. For example, a protein, peptide or peptide mimetic including xSer/ThrY where x is a negatively charged tetra or pentavalent moiety and Y is a Pro or a Pro analog. Methods of inhibiting cell growth and methods of identifying phosphoserine- or phosphothreonine-proline specific peptidyl-prolyl isomerase inhibitors are also included in the invention.

Abstract: The invention relates to dipeptide compounds having formula (I): The compounds having formula (I) have a high antifungal activity and are used for the control of phytopathogens in the agronomic field.

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

Abstract: A silver halide photographic material is described, which contains the compound represented by the following formula (I): wherein R1 represents a substituted or unsubstituted alkylene group having from 1 to 5 carbon atoms; X represents a water-soluble group; and R represents a substituted or unsubstituted alkyl group having the sum total of from 14 to 40 carbon atoms, an alkenyl group, an aryl group, an alkoxyl group, —NR3R4 (R3 and R4 each independently represents an alkyl group having from I to 40 carbon atoms, a hydrogen atom, or an aryl group), a bicycloalkyl group, a bicycloalkenyl group, a cycloalkyl group, a cycloalkenyl group or a heterocyclic group, provided that when X represents a quaternary ammonium salt structure, R2 does not represent an alkyl group having from 14 to 17 carbon atoms.

Abstract: A compound of the formula (I): wherein R1 represents an amino group which may be substituted; R2 represents a carboxy group which may be esterified or amidated; R3, R4, R5 and R6 each represent a hydroxy group which may be protected; Q represents an aryl group which may be substituted; or a salt thereof is disclosed. The compound (I) possesses ant-Helicobacter pylori activity, and is useful in the prevention or treatment of various diseases associated with Helicobacter bacteria, such as duodenal ulcer, gastric ulcer, chronic gastritis and cancer of the stomach.

Abstract: A process is described for the stereoselective synthesis of R-(−)-carnitine in which the characterizing step is condensation of glycerol with an amine of (−)camphorsulfonic acid.

Abstract: Embodiments include reagents to modify a bioactive species for incorporating a bifunctional boronic compound complexing moiety for subsequent conjugation to a different or same bioactive species having pendant phenylboronic acid moieties of General Formula I, wherein group R is an electrophilic or nucleophilic moiety suitable for reaction of the putative bifunctional boronic compound complexing reagent with a bioactive species, wherein group R2 is selected from one of H and OH moieties, and wherein group R3 is selected from one of an alkyl and a methylene bearing an electronegative substituent. Group Z is a spacer selected from (CH2)n and CH2O(CH2CH2O)n2, wherein n is an integer of from 1 to 5, and wherein n2 is an integer of from 1 to 4. Group Z2 and Z3 is a spacer and need not be the same.

Abstract: A process for the combinatorial preparation of a substance library from n different compounds in an array of n different reaction solutions at n spatially separate reaction sites, in which at each of the n reaction sites