Abstract: The invention relates to novel synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I wherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or —N(CH3)OCH3, Ra is a hydroxy-protecting group and Rb is a carboxy-protecting group, and, as well as to the compound of formula I, to further new intermediates and methods for their preparation by Friedel-Crafts acylation.

Abstract: Gelling agents which contain a specific N-acylamino acid monoamide monoalkyl ester have a melting temperature of about 100° C., are capable of solidifying a wide variety of oily base materials including silicones, and do not cause “sweating” while retaining a practical level of gel strength. When applied to skin, the resulting gels have a good feeling, good spreadability, and good fittability to skin.

Abstract: Processes for forming adducts of amines with acrylic macromonomers are provided. Also provided are processes for using ring-closing reactions of the adducts to form lactams. The adducts are useful, for example, for making adhesives, surfactants, viscosity modifiers, processing aids, and other products.

Abstract: Ester compounds of the formula I-a wherein R1 is selected from OH, NH2 and NH3+X?, wherein X is an inorganic anion, wherein R2 is a singly-branched saturated or unsaturated aliphatic hydrocarbon moiety selected from C7-C15, wherein R5 is selected from H, and a linear saturated or unsaturated aliphatic hydrocarbon moiety selected from C6-C14, and wherein R2 and R5 together have a total of 7 to 15 carbon atoms; that are useful as antibacterial or antifungal compounds in consumer products.

Abstract: The present invention refers to O-acyl salicylic acid derivatives (I) bearing a NO donor moiety, a process for their preparation and pharmaceutical compositions containing them. (I) wherein: D is ONO2 or (A).

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract: Corrosion and gas hydrate inhibitors having improved water solubility and increased biodegradability The invention thus 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, —CHR5—COO? or —O?, R4 is M, hydrogen or an organic radical which optionally contains heteroatoms and has from 1 to 100 carbon atoms, B is an optionally substituted C1- to C10-alkylene group, D is an ethylene group substituted by an organic radical having from 1 to 600 carbon atoms, X, Y are each independently O or NR6, R5, R6 are each independently hydrogen, C1- to C22-alkyl, C2- to C22-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, and M is a cation as corrosion and gas hydrate inhibitors, and also the compounds of formula 1.

Abstract: This invention relates to a stereoselective preparation of fluoroleucine alkyl esters.

Abstract: The instability of carbamate-protected alkyl imines has greatly hampered the development of catalytic asymmetric Mannich reactions suitable for the synthesis of optically active carbamate-protected chiral alkyl amines. A highly enantioselective Mannich reaction with in situ generation of carbamate-protected imines from stable ?-amido sulfones catalyzed by an organic catalyst has been developed. This reaction provides a concise and highly enantioselective route converting aromatic and aliphatic aldehydes into optically active aryl and alkyl ?-amino acids.

Abstract: This invention relates to newly identified ester-linked Gemini surfactant compounds of formula (I), where Y is either H or (Aa)x where (Aa) is a basic amino acid and x is 1 to 6, to the use of such compounds and to their production. The invention also relates to the use of the ester-linked Gemini surfactant compounds to facilitate the transfer of polynucleotide into cells.

Abstract: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.

Abstract: The invention relates to synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I wherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or N(CH3)OCH3, Ra is a hydroxy-protecting group, and Rb is a carboxy-protecting group, and, as well as to the compound of formula I, to further intermediates and methods for their preparation by Friedel-Crafts acylation.

Abstract: Phosphoramidites with the general formulae I to VI are claimed together with the use of these compounds as ligands of transition metal compounds, in particular in transition metal catalysts, in the hydrogenation, transfer hydrogenation, hydroboration, hydrocyanation, 1,4-addition, hydroformylation, hydrosilylation, hydrovinylation, and Heck reactions of prochiral olefins, ketones, or ketimines.

Abstract: The present invention provides methods for labeling One or two oxygen atom(s) in a carboxyl group of a carboxyl-containing compound with an oxygen isotope selected from oxygen-17 (17O) or oxygen-18 (18O). The methods of the present invention are characterized in that an activated ester of the carboxyl-containing compound (carboxylic acid) is reacted with H217O or H218O in the presence of an activator. In the methods of the present invention, the reaction between the activated ester of a carboxylic acid and H217O or H218O can be allowed to proceed without including drastic conditions such as strongly acidic conditions or alkaline hydrolysis because an activator is used.

Abstract: The invention relates to tri- and tetracarboxylic acid ester of the formula (1) wherein R1 and R2 independently of one another are C1- to C22-alkyl, C2- to C22-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, and A is a C2- to C4-alkylene group, B is an arbitrarily substituted organic group having 3-100 carbon atoms, n is a number from 1 to 30, m is 3 or 4, whereby the structural units —NR1-R2 are partly or completely quaternized and the use thereof as a gas hydrate inhibitor.

Abstract: The invention concerns a method for preparing (meth)acrylic esters or anhydrides from acrylic acid of formulae (I), where R is H or Me, and R? is alkyl and R? is alkyl or ethyl substituted by dialkylamino whereof the alkyls can form with the nitrogen atom, a 5- or 6-membered heterocycle, capable of bearing one or several alkyl substituents. OII or ?O, or R? is H and R? is alkyl, the alcohol R?—OH being primary or secondary; or (II) wherein R? is H or Me, functioning preferably in the presence of at least one catalyst, wherein is performed a reaction in a reaction R2 with constant equilibrium displacement provided with a first reactor R1 designed for prior dehydration of the reagents to be involved in the reaction.

Abstract: The invention provides a process for preparing amino acid esters and/or their acid addition salts from monomeric or polymeric amino acids, peptides, proteins and alcohols, which comprises carrying out the reaction in supercritical alcohols, preferably at pressures and temperatures which are at least 5% above the critical parameters, the alcohols serving both as the solvent and as reactants.

Abstract: The invention provides novel compounds of Formula (I), pharmaceutical compositions and methods of synthesis thereof.

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: One aspect of the invention relates to hexafluoroleucine and congeners thereof, and methods of making the compounds. Another aspect of the invention relates to the synthesis of protein cores comprising hexafluoroleucine and congeners thereof. Certain peptides comprising hexafluoroleucine and congeners thereof have been characterized using comparative biophysical studies. In general, the fluorinated peptides show higher thermal stability and enhanced resistance to chemical denaturation. Further, mixed hydrocarbon-fluorocarbon cores self-sort into homogeneous bundles, suggesting new avenues for the design and manipulation of protein-protein interfaces.

Abstract: In accordance with the disclosure, one aspect of the present application is directed to a dispersant compound comprising the reaction product of (i) a hydrocarbyl carbonyl compound, (ii) a polycarbonyl compound having at least three carbonyl acylating functions, and (iii) a primary amine moiety of a polyamine. Methods of making and methods of using the dispersant compound are also disclosed.

Abstract: The present invention is to provide a method for producing the desired optically active ?-amino acid derivatives of high optical purities in high yields, without requiring a step of deprotection. More particularly, the present invention relates to a method for producing an optically active ?-amino acid derivative or a salt thereof represented by the formula (2): which comprises reacting an ?,?-unsaturated carboxylic acid derivative or a salt thereof represented by the formula (1): with an amines or a salt thereof in the presence of a chiral catalyst and in the presence or absence of an acid.

Abstract: A process for amino acid derivatives shown by the below general formula (I): (wherein R1 means a hydrogen atom or a straight chain or branched chain alkyl group with 1-5 carbon atoms.) having an object to provide a process of the amino acid derivatives of the formula (I) and their synthetic intermediate, t-butoxycarbonylamino-ethylamine, whereby it requires no tedious procedure and is also good in yield, and its application to a mass production is easy, and to provide novel amino acid derivatives of the formula (IV), their synthetic intermediates, and a process thereof, characterized in that it comprises a step to obtain the amino acid derivatives shown by the general formula (I) by hydrolysis of compounds shown by the below formula (II): (wherein R1 has the same meaning as described above, and R2 means a straight chain or branched chain alkyl group with 1-4 carbon atoms.

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, —CHR5—COO? or —O?, R4 is M, hydrogen or an organic radical which optionally contains heteroatoms and has from 1 to 100 carbon atoms, B is an optionally substituted C1- to C30-alkylene group, D is an organic radical which optionally contains heteroatoms and has from 1 to 600 carbon atoms, X, Y are each independently O or NR6, R5, R6 are each independently hydrogen, C1- to C22-alkyl, C2- to C22-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, and M is a cation as gas hydrate inhibitors.

Abstract: The present invention discloses novel dual prodrug compositions of Formula 1, wherein A is a single bond, —O—, or —CH2—; m and n vary from 0 to 15; p and q vary from 0 to 4; B is a single bond or —CR3R4; D is selected from the group consisting —CO2R5, —OR6, —OCOR7, —SO3R8, —SO2NH2, —OPO(OR9)(OR10), —OPO(OR9)(NH2), —OPO(OR9)—O—PO(OR10)(OR11), R1 to R11 are various substituents selected to optimize the physicochemical and biological properties such as, lipophilicity, toxicity, bioavailability, and pharmacokinetics of compounds of Formula 1. These compounds are useful for the treatment of various cardiovascular and neurological disorders.

Abstract: The present invention relates to compounds being esters of 5-aminolevulinic acids or pharmaceutically acceptable salts thereof, including compounds of formula (I) R22N—CH2COCH2-CH2CO—OR1 (wherein R1 may represent alkyl optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and optionally interrupted by oxygen, nitrogen, sulphur or phosphorus atoms; and R2 represents a hydrogen atom or a group R1, and both R2 groups may be the identical or different), and their use in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.

Abstract: Betaine ester quaternary ammonium compounds with reduced toxicity and improved biodegradability are formed by esterification of a haloacetic acid with an alcohol containing at least 4 carbon atoms, followed by quaternization of the halo-acetate with a tertiary amine containing at least 4 carbon atoms. In one non-limiting embodiment the alkyl substituents on the nitrogen of the tertiary amine have at least 2 carbon atoms, and in another non-limiting embodiment are each n-butyl.

Abstract: Presented are compounds represented by the following general formulas (I) and (II), for inhibiting cysteine protease legumain for modulating associated disease states in subjects

Abstract: Astaxanthin derivatives of the general formula (I) wherein R is in each case group —NH—CH(R1)—COOR2, —OR3 or —(Y)n-Z and R1, R2, R3, Y, Z and n are significances given in detail in the description, are novel compounds with improved stability during extrusion at the elevated temperatures as required in feed manufacture and during the storage of the manufactured feed and which accordingly are useful as pigmenting carotinoids for feed for aquatic animals. The derivatives are produced by reacting astaxanthin with the pertinent acid RCOOH as such or as its acid chloride RCOC1 or acid anhydride (RCO)2O, or, in the cases where R signifies a group —NH—CH(R1)—COOR2, with the appropriate N-carbonyl-amino acid ester of the formula OCNCH(R1)COOR2.

Abstract: The present invention relates to compounds being esters of 5-aminolevulinic acids or pharmaceutically acceptable salts thereof, including compounds of formula (I) R22N—CH2COCH2—CH2CO—OR1 (wherein R1 may represent alkyl optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and optionally interrupted by oxygen, nitrogen, sulphur or phosphorus atoms; and R2 represents a hydrogen atom or a group R1, and both R2 groups may be the identical or different), and their use in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.

Abstract: The invention is a method for producing ?-aminopentadienoate derivatives of formula (1), the method comprising reacting a streptocyanine derivative of formula (2) with an ester derivative of formula (3) in the presence of an organic base.

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: Cyclic ?-(acylamino)acrylate derivatives were hydrogenated using Ru-chiral phosphine ligand catalysts and thereafter converted to the corresponding cyclic ?-aminoacids in high yield and enantioselectivity according to the reaction scheme:

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, —CHR5—COO? or —O?, R4 is M, hydrogen or an organic radical which optionally contains heteroatoms and has from 1 to 100 carbon atoms, B is an optionally substituted C1- to C30-alkylene group, D is an organic radical which optionally contains heteroatoms and has from 1 to 600 carbon atoms, X, Y are each independently O or NR6, R5, R6 are each independently hydrogen, C1- to C22-alkyl, C2- to C22-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, and M is a cation as gas hydrate inhibitors.

Abstract: The present invention relates to processes for the preparation of any of the intermediate 1,3-substituted indenes of the formulae (Ia), (Ib) and (Ic) or a mixture thereof: wherein R1, R2, R3, R4, and R5 are defined herein. Compounds of formulae (Ia), (Ib) and (Ic) or mixtures thereof are useful in the preparation of compounds of formula (II): wherein R2, R3 and R6 are also defined herein.

Abstract: Novel urea and urethane derivatives of general formula (I) in which R1, R2, R3, R5, R5?, X, Y, B, m, n and o are as defined in Patent Claim 1, and physiologically acceptable salts or solvates thereof are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart disease, arteriosclerosis, inflammation, tumors. Osteoporosis, infections and restenosis after angioplasty or in pathological processes maintained or propagated by antiogenesis.

Abstract: One aspect of the invention relates to hexafluoroleucine and congeners thereof, and methods of making the compounds. Another aspect of the nvention relates to the synthesis of protein cores comprising hexafluoroleucine and congeners thereof. Certain peptides comprising hexafluorleucine and congeners thereof have been characterized using comparative biophysical studies. In general, the fluorinated peptides show higher thermal stability and enhanced resistance to chemical denaturation. Further, mixed hydrocarbonfluorocarbon cores self-sort into homogeneous bundles, suggesting new avenues for the design and manipulation of protein-protein interfaces.

Abstract: The present invention relates to processes for the preparation of any of the intermediate 1,3-substituted indenes of the formulae (Ia), (Ib) and (Ic) or a mixture thereof: wherein R1, R2, R3, R4, and R5 are defined herein. Compounds of formulae (Ia), (Ib) and (Ic) or mixtures thereof are useful in the preparation of compounds of formula (II): wherein R2, R3 and R6 are also defined herein.

Abstract: The present invention relates to a method for introducing an amino group into an organic acid or an organic ester by reacting an organic salt or an organic ester and ammonia under high-temperature and high-pressure water conditions, a method for synthesizing an amino acid or an amino ester by the above method, and a method for manufacturing an amino acid compound by synthesizing an amino acid or an amino ester by the above method and separating and refining it with an ion exchange resin.

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 invention relates generally to a novel type of arginine mimetics which are inhibitors of factor Xa; to pharmaceutical compositions which comprise these mimetics; and to the use of these arginine mimetics for producing compositions for antithrombotic therapy.

Abstract: The present invention relates to novel retinol derivatives, the methods of preparation and the uses thereof. According to the present invention, retinol derivatives comprise carboester linkage between di-, tri-, polypeptide having functional group of COOH and retinol. Retinol derivatives in the present invention comprise carboester linkage between amino acid having functional group of di-COOH and retinol. Retinol derivatives comprise carboester linkage between retinol and the compounds having the function group of COOH and multiple double bonds on carbon chain. Retinol derivatives in the present invention comprise carboester linkage between retinol and the compounds having the functional group of di-COOH and one double bond. Retinol derivatives in the present invention comprise ether linkage between the compounds with OH functional group and retinol.

Abstract: Compounds having the formula are useful for treating conditions which arise from or are exacerbated by angiogenesis. Also disclosed are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.

Abstract: To provide a producing method of an optically active ?-amino acid useful as intermediate for the production of medicines, agricultural chemicals and physiologically active substances, by means of a catalytic and asymmetric synthesis method of high performance and a high enantiomeric excess, without requiring additional procedures such as introduction and removal of protecting group and so on. A producing method of an optically active ?-amino acids which comprises subjecting an enamine to an asymmetric hydrogenation.

Abstract: Compositions including a conjugate of ?-difluoromethylornithine can be applied topically to reduce hair growth.

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: Provided is a compound having one or more structures of the formula: wherein X is a primary carbamate group, Y is a hydroxy or halide group, n is an integer of 2 or more, n? is an integer of 1 or more, and R0, R1, R2, R3, R4 and R5 may be H or a group selected from alkyl groups, aliphatic groups, cycloaliphatic groups, aromatic groups and mixtures thereof, with the provisos that at least one R1 or R2 group is selected from the group consisting of aliphatic groups, cycloaliphatic groups, and aromatic groups, and in substantially all structures primary carbamate group X is attached to a carbon atom having a lower degree of substitution than a carbon atom to which functional group Y is attached. The invention provides a method of making the claimed compound.

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: Nordihydroguaiaretic acid derivatives and methods of use thereof for the treatment of tumors.

Abstract: The compound O-(2-[18F]fluoroethyl)-L-tyrosine has proven to be particularly suitable for positron emission tomography and has already been tested in clinical practice. Until now, the compound has been prepared according to a relatively laborious method (Wester H. J. et al., J. Nucl. Med. 1999; 40: 205-212). The invention relates to L-tyrosine derivatives of the formula (1) whereby R1 represents a suitable protective group for the carboxy group, R2 a suitable protective group for the amino group and R3 a suitable leaving group, R1 represents a methylthiomethyl group, a tetrahydrofuranyl group, a diphenylmethyl group, a para-methoxybenzyl group, a piperonyl group or a tert-butyl group, R2 an alkyl- or an arylalkyl group and R3 a p-tosyloxy, methanesulfonyloxy, trifluoromethanesulfonyloxy or bromine. The invention also relates to a method for preparing O-(2-[18F]-fluoroethyl)-L-tyrosine from the initial compounds of formula (1) and method for the preparation of these initial compounds.