Abstract: This invention relates to the synthesis for a precursor of E6020, compound 26, via a ?-keto amide alcohol intermediate, compound 22. The synthesis reacts compound 22 with compound 25 and the resultant intermediate is oxidized to produce compound 26, the precursor to E6020. Compounds 22 and 25, and their crystalline forms, represent separate embodiments of the invention. The invention also relates to compounds of formulas (3) and (4) and processes for their preparation. The ?-keto amide alcohol intermediate compound 22 is a compound of formula (3). Compound 25 is a compound of formula (4).

Abstract: The invention provides compounds for use in photochemotherapy or diagnosis, said compounds being branched alkyl esters or substituted alkyl esters of 5-aminolevulinic acid, or derivatives or pharmaceutically acceptable salts thereof. In particular, the invention provides compounds of formula (I): R22N—CH2COCH2CH2CO—OR1 (wherein R1 represents an optionally substituted branched alkyl (e.g.

Abstract: The invention relates to low extractable coatings, varnishes, adhesives or inks obtained with a radiation curable composition comprising amino(meth)acrylates obtained from the reaction of a primary and/or secondary amine (A) with a (methacrylated ethoxylated and/or propoxylated polyol (B) having a degree of alkoxylation of at least 4.

Abstract: A polymer film includes: a wavelength dispersion regulator represented by formula (I): wherein R1 and R2 each independently represents a hydrogen atom, an alkyl group or an aryl group, provided that both R1 and R2 are not hydrogen atoms at the same time; and R3 and R4 each independently represents an electron-withdrawing substituent, and R1 and R2, or R3 and R4 may be bonded together to form a ring, and wherein the polymer film has a retardation value that satisfies the following formulae (1) and (2): 70 nm?Rth(548)?300 nm??Formula (1) Rth(628)<Rth(548)<Rth(446)??Formula (2) wherein Rth(?) represents a retardation value expressed in nm in a film thickness direction measured at a wavelength of ? nm.

Abstract: Synthesis methods for the preparation of intermediates which are suitable for the preparation of statin derivatives, and especially to synthesis methods for the intermediate of formula (VI) wherein Ra? and Rc? are each independently of the other hydrogen or hydroxy-protecting group, or together are a bridging hydroxy-protecting group; and Rb is a carboxy-protecting group.

Abstract: Provided are compounds and a process for preparing benzyl pentahydroxyhexylcarbamoylundecanoate (I) and uses thereof.

Abstract: Provided are compounds of formula A and formula I: A compound of formula A: wherein n is an integer from 6 to 17 and a compound of formula I:

Abstract: The invention provides pharmaceutical compositions comprising primary N-hydroxylamines and related therapeutic, prophylactic, diagnostic and screening methods. The pharmaceutical compositions generally comprise a pharmaceutical composition comprising an orally administrable effective unit solid dosage of a primary N-hydroxylamine or a pharmaceutically acceptable salt thereof and substantially free of a nitrone corresponding to the hydroxylamine.

Abstract: An ionic liquid is disclosed A precursor composition that comprises at least one ionic liquid and at least one energetic material is also disclosed, as is a method of synthesizing an ionic liquid and a method of desensitizing an explosive composition.

Abstract: The invention relates to compounds of formula (I) provided in the form of racemic compounds, mixtures of diastereomers or essentially pure diastereomers, wherein R1 represents a hydrogen atom or C1-C4-alkyl, and at least one secondary phosphine depicts an unsubstituted or substituted cyclic phosphine group, or phosphonium salts thereof having one or two monovalent anions or a divalent anion.

Abstract: The present invention relates to a process for preparing 2-dihaloacyl-3-aminoacrylic esters of the formula (I) by reacting acid halides of the formula (II) with dialkylaminoacrylic esters of the formula (III) in which R, R1, R2, X1, X2 and Hal are each as defined in the disclosure in a water-immiscible organic solvent in the presence of a base, to the novel 2-dihaloacyl-3-aminoacrylic esters of the formula (I) themselves, to their use for preparing 3-dihalomethylpyrazoles, to a process for preparing 3-dihalo-methylpyrazoles, and to novel 3-dihalomethylpyrazoles.

Abstract: The invention relates to a method for the synthesis of two isomers, at function OH, alone or in mixtures, of amino acids ? or the derivatives thereof, having general formula (B), wherein: linkage C—O of the 4-position carbon (represented by symbol) denotes one or other of isomers III or IV, or mixtures thereof. Moreover, R1 and R2 represent: a hydrogen atom; or either R1 or R2 represents a hydrogen atom and the other substituent is a radical Ra, an acyl group —CORa, such as acetyl, or a functional group —COORa, —SO2Ra, —N (Ra, Rb), Ra and Rb, which are identical or different, representing a C1-C12 linear or branched alkyl radical, optionally substituted, an aryl group with one or more aromatic rings and heterocycles, comprising between 5 and 8C, optionally substituted, or aralkyl, the alkyl substituent and the aryl group being as defined above; or R1 and R2 both represent a substituent as defined above. R3 represents a hydrogen atom or Ra and R4 has the significance of Ra.

Abstract: The invention provides the use of compounds of the formula (1) where R1, R2 are each independently C1- to C22-alkyl, C2- to C22-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, R3 is C1- to C22-alkyl, C2- to C22-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, —CHR6COO? or —O?, A is a C2- to C4-alkylene group, B is a C1- to C10-alkylene group, X is O or NR7 R6, R7 are each independently hydrogen, C1- to C22-alkyl, C2- to C22-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, R4 is a C1- to C50-alkyl, C2- to C50-alkenyl radical, C6- to C50-aryl or C7- to C50-alkylaryl, R5 is hydrogen, —OH or a C1- to C4-alkyl radical, n, m are each independently a number from 0 to 30, x is a number from 1 to 6, as corrosion and gas hydrate inhibitors, and also the compounds of formula 1.

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: A method for producing a hydroxy-amino ester, or derivative thereof, is provided. A substituted ?-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. The carboxylic acid is converted to an amine or a derivative thereof to produce a hydroxy-amino ester or derivative thereof. A number of novel hydroxy-amino esters are prepared by the method.

Abstract: The invention provides compounds for use in photochemotherapy or diagnosis, said compounds being branched alkyl esters or substituted alkyl esters of 5-aminolevulinic acid, or derivatives or pharmaceutically acceptable salts thereof. In particular, the invention provides compounds of formula (I): R22N—CH2COCH2CH2CO—OR1 (wherein R1 represents an optionally substituted branched alkyl (e.g.

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 XIX wherein Ra and Rc are each independently of the other hydrogen or a hydroxy-protecting group, and Rb is a carboxy-protective group

Abstract: The present invention relates to an additive, and its use for inhibiting nucleation, growth and agglomeration of gas hydrates by adding an effective amount of an inhibitor to a multiphasic mixture which tends to hydrate formation and consists of water, gas and optionally condensate, or to a drilling fluid which tends to form gas hydrates. Said inhibitor comprising dialkoxylated quaternary ammonium compounds of the formula 1 where R1, R2 are each independently radicals of the formulae—(B)—(O—A)n—O—CO—R5 or —(A—O)n—(C)—CO—O—R5, R3 is C1- to C30-alkyl or C2- to C30-alkenyl, R4 is an organic radical which optionally contains heteroatoms and has from 1 to 100 carbon atoms, R5 is an alkyl or an alkenyl, n is a number from 1 to 20, A is an alkylene group, B is an alkylene group, C is a C1- to C6-alkylene group and X is an anion, are used as gas hydrate inhibitors.

Abstract: The invention relates to an additive and to a method of corrosion inhibition on devices for the recovery and transportation of hydrocarbons in crude oil recovery and processing by adding an effective amount of an inhibitor. The inhibitor comprises an alkoxylated quaternary compounds of the formula 1 where R1, R2 are independently groups of the formula —(B)—(O—A)n—O—CO—R5 or —(A—O)n—(C)—CO—O—R5, R3 is C1— to C30-alkyl or C2— to C30-alkenyl, R4 is an organic radical with 1 to 100 carbon atoms optionally containing heteroatoms, R5 is an alkyl or an alkenyl, n is a number from 1 to 20, A is an alkylene group, B is an alkylene group, C is a C1— to C6-alkylene group and X is an anion, used as corrosion inhibitors.

Abstract: The present invention provides compounds which inhibit serine protease activity of matriptase or MTSP1. Also provided are pharmaceutical compositions comprising those compounds and methods of using the compounds and pharmaceutical compositions to treat conditions ameliorated by inhibition of matriptase or MTSP1.

Abstract: The present invention relates to improved processes for the production of compounds of formula I:

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: The present invention provides a compound of formula I; R22N—CH2COCH2—CH2CO—OR1??(I) wherein R1 represents (a) an optionally substituted branched C6-30 alkyl group, comprising a straight chain C4-29 alkyl group, branched by substitution with one or more C1-6 alkyl groups, wherein said site of substitution is at C2 or a higher C atom, (b) a non-heteroaromatic aryl substituted alkyl group, wherein said aryl group is substituted, or (c) an alkoxy substituted alkyl group, wherein said alkoxy group is substituted by a methoxy group or an alkoxy group substituted with an alkoxy group, wherein in (a) and (b) said substituents are selected from hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, nitro, oxo or fluoro groups, and said alkyl group is optionally interrupted or terminated by one or more —O—, NR3—, —S— or PR3— groups; R2, each of which may be the same or different, represents a hydrogen atom or a group R1, wherein R1 represents (a) an optionally substituted branched C5-30 alkyl group, comprising a

Abstract: A process for synthesizing L and D-5,5,5,5?,5?,5?-hexafluoroleucine and protected analogs is disclosed. These compounds have utility in the preparation of fluorous peptides and proteins, which display interesting and unusual properties including strong self-association and an affinity for lipid bilayers.

Abstract: Provided is a zwitterionic lipid compound represented by formula (I) given below: In formula (I), m and n are independently integers of 1 to 4, p is an integer of 7 to 21, one R is NH3+, and each other R is H.

Abstract: A novel process for producing an optically active amide excellent in chemical selectivity and enantioselectivity by asymmetric hydrogenation of an ?,?-unsaturated amide and also allowing the reaction to proceed efficiently even when a trace amount of a catalyst is used relative to the substrate as compared with the amount in a conventional process. An optically active amide is produced by asymmetric hydrogenation of an ?,?-unsaturated amide derivative in the presence of a transition metal complex containing a specific phosphine-phosphorane compound.

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: 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: Compounds of the formula wherein R, R1, COOR2, R3-R7, alk, and X have meaning as defined, such being useful as dual inhibitors of angiotensin converting enzyme and neutral endopeptidase, as well as inhibitors of endothelin converting enzyme.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: A process for preparing N-acyl derivatives of the formula I, in which the substituents independently of one another have the following meanings: X is CH(OR3)2, COOR3; R1 is hydrogen, C1-C12-alkyl, aryl, unsubstituted or substituted; R2 is hydrogen, C1-C12-alkyl, aryl, unsubstituted or substituted; R3 is C1-C12-alkyl, which comprises reacting a carboxamide R1—CONH2 of the formula II with a glyoxal monoacetal derivative of the formula III, in the presence of a carboxylic acid R4—COOH of the formula IV where R4=C1-C12-alkyl, where the substituents R1 to R3 are as defined above, is described.

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: The invention is directed primarily to compounds of Formula I: wherein: R1 is a polymeric residue; L1 is a bifunctional linking group; Y1 and Y2 are independently O, S or NR7; R2-7 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; D is a moiety that is a leaving group or a residue of a compound to be delivered into a cell; Z is selected from the group consisting of: a moiety that is actively transported into a target cell, a hydrophobic moiety, and combinations thereof; Ar is a moiety which when included in Formula (I) forms a multi-substituted aromatic hydrocarbon or a multi-substituted heterocyclic group; and (y) is a positive integer greater than or equal to 1. Methods of making and using the same are also disclosed.

Abstract: A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal alkoxide is reacted with a &bgr;-lactam.

Abstract: The present invention relates to blocked polyisocyanate cross-linking agents and their use in one-component stoving lacquers, in particular in solvent-containing or predominantly water-based plastics coatings having a soft-feel effect.

Abstract: Aminobutylic acid derivatives of the formula (I) wherein the symbols are as defined in specification; and non-toxic salts thereof. Because of inhibiting matrix metalloproteinase, the compounds of the formula (I) are useful for prevention and/or treatment of diseases, for example, rheumatoid diseases, arthrosteitis, osteoarthritis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, cornea ulcer, metastasis, invasion or growth of tumor cells, autoimmune disease, disease caused by vascular emigration or infiltration of leukocytes, arterialization, multiple sclerosis, arota aneurysm, endometriosis, restenosis after PTCA, unstable angina, acute myocardial infarction, transient ischemic attack.

Abstract: The invention concerns alkoxyamines derived from &bgr;-phosphorous nitroxides corresponding to formula (I). Said compounds can be used as (co)polymerization initiators of at least a monomer polymerizable by radical polymerization.

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: 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: The invention relates to cycloalkyl derivatives, a process for their preparation and their use.

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: The present invention provides novel and useful ester group-containing tertiary amine compounds which, when used as additives in chemical amplification photolithography, can yield photoresists having a high resolution and an excellent focus margin. Specifically, the present invention provides ester group-containing tertiary amine compounds represented by the following general formula (1).

Abstract: The present invention is directed to novel substituted &agr;-hydroxy acid thereof, represented by the general Formula I: where R1-R5, X and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.

Abstract: Enantiomerically enriched N-acylated &bgr;-amino acids are synthesized by catalytic enantioselective hydrogenation of E-isomers and Z-isomers of 3-amino acrylic acid derivatives in the presence of a catalysts of formula (I)

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: Perfluorinated esters of alkanoyl-L-carnitine of the formula (I): are useful as cationic lipids for the intracellular delivery of pharmacologically active compounds.

Abstract: A compound of the following formula (II) and a process for preparing of the compound of the following formula (I) its preparation wherein R1 is carboxy or protected carboxy; R2 is lower alkoxy or higher alkoxy; A1 is a divalent aromatic ring, a divalent heterocyclic group or a divalent cyclo(lower)alkane; and A2 is a divalent aromatic ring, a divalent heterocyclic group or a divalent cyclo(lower)alkane, or a salt thereof. The process comprises, reacting a compound of the formula (III): wherein R1, R2, A1 and A2 are each as defined above or a salt thereof, with an acid ammonium salt to give a compound of the formula (II).

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

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: Compounds formed by reacting a protected amino acid with an alkali metal enolate of an alkyl acetate are reacted with a halogenating agent for halogenation of the 2-position, or a protected amino acid is reacted with an alkali metal enolate of an alkyl halogenoacetate, to form a 4-amino-3-oxo-2-halogenobutanoic acid ester derivative, and hydrolysis and decarboxylation are conducted to produce a 3-amino-2-oxo-1-halogenopropane derivative or its salt. The present method is a useful process for producing a 3-amino-2-oxo-1-halogenopropane derivatives which can easily be converted to a 3-amino-1,2-epoxypropane.