Abstract: The invention relates to a method for synthesizing 9-aminononanoic acid or the esters thereof from natural unsaturated fatty acids, comprising at least one step of metathesis of the natural fatty acid and an oxidation step by oxidative cleaving. Said synthetic method uses widely available renewable starting materials and hence economical.

Abstract: A lipid particle can include a cationic lipid. Synthesis of the cationic lipid can include a ylide-based reaction, such as a Wittig reaction or sulfur ylide reaction. In some cases, the synthesis can also include a Michael addition or a related addition reaction.

Abstract: The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of a specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.

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 relates to a method for synthesizing ?-amino-alkanoic acids or the esters thereof from mono-unsaturated natural fatty acids comprising at least one step of forming the unsaturated diacid corresponding to the original fatty acid.

Abstract: Provided is an enantioselective, palladium-catalyzed method for the preparation of ?-amino-?,?-unsaturated carboxylic acid derivatives having the formulas II, III, VII and VIII:

Abstract: The invention relates to a series of novel chiral phosphorus ligands of formulae (Ia) and (Ib): wherein R, 1-rR>4 and X are as defined herein. The invention also relates to chiral metal complexes prepared with these chiral phosphorus ligands. The chiral metal complexes are useful as catalysts for carrying out asymmetric hydro genation.

Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

Abstract: The present invention discloses an optically active quarternary ammonium salt having axial asymmetry and a method for producing an ?-amino acid and a derivative thereof using the same. The optically active quarternary ammonium salt having axial asymmetry of the present invention is a chiral phase-transfer catalyst that has a simple structure and that can be produced in a smaller number of process steps. The compound of the present invention is very useful as a phase-transfer catalyst in the synthesis of an ?-alkyl-?-amino acid and a derivative thereof as well as an ?,?-dialkyl-?-amino acid and a derivative thereof. Therefore, the compound of the present invention can be used in the development of novel foods and pharmaceuticals.

Abstract: The present invention provides a method for producing an optically active N-(halopropyl)amino acid derivative, wherein the method comprises the steps of obtaining a compound represented by formula (III) by reacting an optically active alanine ester represented by formula (I) or a salt thereof (hereinafter sometimes simply referred to as an “alanine ester”) with a halogenated propane represented by formula (II); and obtaining an optically active N-(halopropyl)amino acid derivative represented by formula (IV) by introducing a protecting group onto the nitrogen atom of the compound represented by formula (III). The present invention provides a method for efficiently producing an optically active N-(halopropyl)amino acid derivative.

Abstract: It is intended to provide a drug which is efficacious in treating and preventing diseases wherein ischemia or an inflammatory substance associated with ischemia participates in the onset or worsening thereof. Because of containing as the active ingredient a substance selected from among farnesol, a farnesol derivative, a tocopherol derivative, a tocotrienol derivative, pharmacologically acceptable salts thereof and solvates thereof, the above-described inhibitor of ischemic disorders can exert therapeutic and preventive effects on diseases wherein ischemia or an inflammatory substance associated with ischemia participates in the onset or worsening thereof (for example, brain infarction, brain edema, cardiac infarction, etc.) not only by the administration in the acute ischemic stage but also by the therapeutic administration in subacute and/or chronic stages after ischemia-reperfusion. It is also intended to provide a farnesol carboxylic acid ester derivative and a method of producing the same.

Abstract: The present invention relates to imidazolo-containing phosphinoborane compounds, to optically active ligands prepared using them, to transition metal complexes which comprise such ligands, and to catalysts which comprise such transition metal complexes. The present invention further relates to the particular processes for preparing the phosphinoborane compounds, the optically active ligands, the transition metal complexes and the catalysts, and to the use of the catalysts for organic transformation reactions. The present invention further relates to a process for preparing optically active ligands comprising imidazolo-containing phosphorus compounds using imidazolo-containing phosphinoborane compounds.

Abstract: The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of a specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.

Abstract: To provide a production method of phosphates of amino acids, typified by ?-aminolevulinic acid phosphate, or esters thereof. A method for producing phosphates of an amino acid or an ester thereof, which comprises allowing an amino acid, an ester thereof or a salt thereof to coexist with phosphoric acids and a basic nitrogen-containing compound.

Abstract: The present invention discloses the signaling pathway involved in erythroid repression by iron deficiency. Further disclosed is a non-toxic small-molecule compound which potently reverses the erythroid repression caused by iron deficiency. The present invention further encompasses novel compounds for inhibition of red cell production, useful, for example, in the treatment of polycythemia vera, a malignancy causing uncontrolled red cell production. These inhibitory compounds also promote megakaryocytic lineage commitment and may therefore be useful for augmentation of platelet production. The present invention further discloses isocitrate reversal of iron deprivation.

Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols, to a plurality of processes for their preparation and to their use as pesticides as herbicides.

Abstract: The present invention comprises a compound of a compound of Formula 1 wherein Rf is a C2 to C12 perfluoroalkyl optionally interrupted by one to four moieties each independently selected from the group consisting of —CH2—, —O—, —S—, —S(O)—, and —S(O)2—; n is 1 to 6; m is 0 to 2, provided that m is less than or equal to n. X and Y are each independently O or NR, R is hydrogen or C1 to C6 alkyl; R1, and R2 are each independently C1 to C6 alkyl, optionally containing one or more oxygen atoms and may form a ring selected from the group of piperidine, pyrrolidine, and morpholine; and R3 is O?, (CH2)pC(O)O?, (CH2)pCH(OH)(CH2)SO3?, and (CH2)qSO3?; p is 1 to 4; and q is 2 to 4 which is useful as a surfactant.

Abstract: Methods to convert biobased oils, oil derivatives, and modified oils to highly functionalized esters, ester polyols, amides, and amide polyols. The products can be used to make polyurethane and polyester films and foams.

Abstract: The present invention relates to an active ingredient-peptide construct for extracellular concentration, a process for the concentration of active ingredients in an extracellular space of a multicellular object, the use of the active ingredient-peptide construct according to the invention for the production of a medicinal product and a pharmaceutical composition containing the active ingredient-peptide construct according to the invention.

Abstract: Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described.

Abstract: Disclosed are UV absorbers that contain a labile functional group capable of initiating free radical polymerization.

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: Provided are compositions comprising beta-alanylhistidine peptides and/or beta-alanines, and methods for administering these peptides and amino acids. In one aspect, the compositions and methods cause an increase in the blood plasma concentrations of beta-alanine and/or creatine.

Abstract: The present invention is a process for producing optically active aminophosphinylbutanoic acids represented by the formula (2), comprising asymmetrically hydrogenating a compound represented by the formula (1) in the presence of a ruthenium-optically active phosphine complex, a process for the production thereof, and a compound useful in a herbicide such as L-AHPB that can be produced with good efficiency and high asymmetric yield.

Abstract: The invention relates to a method for synthesizing ?-aminoalkanoic acids or esters thereof from unsaturated natural fatty acids, passing through a monounsaturated dinitrile intermediate compound. The method of the invention is simple to carry out and, compared to other known methods, avoids the environmental constraints and economic disadvantages due to reaction by-products.

Abstract: The present invention relates to a photolabile compound including a coumarin family caging group covalently bound to an organic moiety containing a carboxyl group, an amino group, a sulfhydryl group, and/or a hydroxyl group. The photolabile compound, upon absorbing visible light, releases the organic moiety. Also disclosed is a method of making a photolabile compound that releases a biologically active compound upon absorbing visible light by providing an organic moiety and binding a coumarin family caging group to the organic moiety under conditions effective to make the photolabile compound. The present invention also relates to a method of obtaining a biologically active compound in a sample. The method involves adding to a sample a photolabile compound including a coumarin family caging group covalently bound to an organic moiety. The sample is then illuminated with visible light under conditions effective to obtain a biologically active compound including the organic moiety.

Abstract: Compounds having stable isotopes 13C and/or 2H were synthesized from precursor compositions having solid phase supports or affinity tags.

Abstract: The present invention discloses certain novel prodrugs of chloramphenicol or thiamphenicol, or of an analog of either, including prodrugs of pharmaceutically acceptable salts of chloramphenicol or thiamphenicol or of their analogs, including nitrogen-containing esters of both alcohol groups of such compounds. In certain embodiments these novel prodrugs are sufficiently water-soluble to serve the functions needed of a prodrug of chloramphenicol or thiamphenicol or of an analog of either. In one embodiment, a certain subclass of the compounds also possesses the hydrolytic stability needed to maintain the prodrug in solution in the subject's system until appropriate conditions exist when the prodrug can hydrolyze, releasing the active compound in question.

Abstract: The present invention describes a process for the synthesis of an amino acid methyl ester comprising the following steps: (a) refluxing a reaction mixture comprising a free amino acid, methanol and a strong acid; (b) concentrating the mixture; (c) adding methanol; (d) repeating steps a-c one or more times.

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: The invention relates to a method for the synthesis of ?-amino alkanoic acids or esters thereof starting from unsaturated natural fatty acids passing through an ?-unsaturated nitrile intermediate compound.

Abstract: Hyperbranched polymers and methods for preparing the same are disclosed. The polymers are obtained based on monomers synthesized via reacting a substituted or unsubstituted cyclic anhydride with a bifunctional amine.

Abstract: Methods to convert biobased oils, oil derivatives, and modified oils to highly functionalized esters, ester polyols, amides, and amide polyols. The products can be used to make polyurethane and polyester films and foams.

Abstract: Provided is an anti-inflammatory composition which has a high efficacy, causes no concern about side effects, is easy to ingest, and can also be administered for a long period of time because of its low cost and high safety. The present invention relates to a peptide comprising an amino acid sequence represented by pyroGlu-(X)n-A or a salt thereof, wherein X is independently Gln, Asn, or Pro; A represents Gln, Asn, Leu, Ile, Met, Val, or Phe; and n represents an integer of 0 to 2, and an anti-inflammatory composition comprising the same.

Abstract: A support comprising functional groups supported therein that specifically react with an aldehyde group of a sugar chain, and a polymer particle and a glycochip to which the support is applied, and uses thereof.

Abstract: The present invention relates to a process for the preparation of 1-alkyl- or 1-aryl-substituted 5-pyrazolecarboxylic acid derivatives comprising the reaction of substituted 1,3-dioxolanes and 1,4-dioxanes with alkyl- or arylhydrazines to give 1-alkyl- or 1-aryl-substituted dihydro-1H-pyrazoles, and their further reaction to give 1-alkyl- or 1-aryl-substituted 5-pyrazolecarboxylic acid derivatives, which can be used as valuable intermediates for producing insecticidally effective anthranilamides.

Abstract: The invention describes compounds useful for labelling molecules of interest (i.e. analytes), particularly biomolecules such as peptides, proteins, oligonucleotides and nucleic acids, and also methods for analysing, detecting and/or isolating these labelled molecules using mass spectrometry. The compound in one aspect is a mass marker for labelling of an analyte detectable by mass spectrometry such as neutral loss mass spectroscopy, in which the mass marker comprises a neutral loss mass modifier linked via a first collision cleavable linker to a reactive group having reactive functionality for attachment to the analyte. The neutral loss mass modifier upon cleavage from the analyte during mass spectroscopy is uncharged.

Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.

Abstract: A hair growth regulating agent containing, as an active ingredient, a compound represented by the following formula (I): [wherein R1 represents a substituted or unsubstituted, linear or branched C2 to C25 alkyl group; a group represented by the following formula (II): (wherein R1? represents a substituted or unsubstituted, linear or branched C2 to C20 alkylene group, or —(CH2)n-{O—(CH2)m}o-O—(CH2)p- in which each of n, m, o, and p is an integer from 1 to 6; X? represents —CO—NH—, —O—CO—O—, —NH—CO—, —CO—O—, —O—CO—, or —O—; Y? represents a substituted or unsubstituted C1 to C4 alkylene group; R2? represents a hydrogen atom or a C1 to C4 alkyl group; R3? represents a C1 to C4 alkyl group; and when R2? and R3? each represent a C1 to C4 alkyl group, the two alkyl groups may be identical to or different from each other); or a group represented by the following formula (III): (wherein R1?, X?, and Y? have the same meanings as defined above; R4?, R5?, and R6?, which may be identical to or different from one another,

Abstract: Compounds of the formula (I), in the form of mixtures comprising predominantly one diastereomer or in the form of pure diastereomers, Z1-Q-P*R0R1 (I) in which Z1 is a C-bonded, secondary phosphine group —P(R)2; in which R is in each case independently hydrocarbon radicals or heterohydrocarbon radicals, or Z1 is the —P*R0R1 group; Q is a bivalent, achiral, aromatic base skeleton, a bivalent, achiral ferrocene base skeleton, an optionally substituted bivalent cycloalkane or heterocycloalkane skeleton, or a C1-C4-alkylene skeleton, and in which base skeletons a secondary phosphine group Z1 is bonded directly to a carbon atom, or, in the case of cyclic base skeletons, directly to a carbon atom or via a C1-C4-alkylene group, and in which base skeletons a P-chiral group —P*R0R1 is bonded directly to a carbon atom, or, in the case of cyclic base skeletons, directly to a carbon atom or via a C1-C4-alkylene group to a carbon atom such that the phosphorus atoms are linked via 1 to 7 atoms of a carbon chain optionally i

Abstract: Among other things, the present invention provides novel compounds capable of effectively inhibiting inflammatory responses that are mediated by G-proteins or GPCRs in neutrophils, macrophages and platelets. In particular, compounds of the present invention act as inhibitors of edema, inhibitors of erythema and inhibitors of MPO (myeloperoxidase), pharmaceutical compositions containing the same compounds and the use thereof for the treatment of diseases that may benefit from edema, erythema and MPO inhibition, such as inflammation (acute or chronic), asthma, autoimmune diseases, and chronic obstructive pulmonary disease (COPD) (e.g., emphysema, chronic bronchitis and small airways disease, etc.), inflammatory responses of the immune system, skin diseases (e.g., reducing acute skin irritation for patients suffering from rosacea, atopic dermatitis, seborrheic dermatitis, psoriasis), irritable bowel syndrome (e.g., Chron's disease and ulcerative colitis, etc.), and central nervous system disorders (e.g.

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: Disclosed is 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. The method includes subjecting an enamine to an asymmetric hydrogenation.

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 provides novel stabilized crosslinked compounds having secondary structure motifs, libraries of these novel compounds, and methods for the synthesis of these compounds libraries thereof. The synthesis of these novel stabilized compounds involves (1) synthesizing a peptide from a selected number of natural or non-natural amino acids, wherein said peptide comprises at least two moieties capable of undergoing reaction to promote carbon-carbon bond formation; and (2) contacting said peptide with a reagent to generate at least one crosslinker and to effect stabilization of a secondary structure motif. The present invention, in a preferred embodiment, provides stabilized p53 donor helical peptides. Additionally, the present invention provides methods for disrupting the p53/MDM2 binding interaction comprising (1) providing a crosslinked stabilized ?-helical structure; and (2) contacting said crosslinked stabilized ?-helical structure with MDM2.

Abstract: The invention relates to a coordination complex system comprising a ligand having the formula: R1—SO2—NH—P (XR2)2 (1a); or R1—SO2—N?PH (XR2)2 (1b); or R1—SO(OH)?N—P(XR2)2 (1c); wherein X is independently O, S, NH, or a bond; R1 and R2 are independently selected from hydrogen and substituted or unsubstituted alkyl or aryl; wherein at least one equivalent of the ligand is complexed to an equivalent of a metal selected from a transition metal and lanthanide. The invention also relates to the use of said coordination complexes as catalysts in the hydroformylation, hydrogenation, transfer hydrogenation, hydrocyanation, polymerization, isomerization, carbonylation, cross-coupling, metathesis, CH activation, allylic substitution, aldol condensation, or Michael addition.

Abstract: The invention includes a method of increasing the substantivity of a personal care composition to hair, skin or nails by preparing a composition of an aqueous phase, a non-aqueous phase and a neutralized amino acid ester that is a reaction product of a neutral amino acid having a non-polar side chain with a long chain fatty alcohol and is represented by formula (I): wherein R1 is an alkyl group; R2 is a linear or branched carbon chain; and the amine group of the amino acid is neutralized with an acid. The composition is substantially free of petrochemicals and/or derivatives of petrochemical materials. The aqueous phase and the non-aqueous phase are emulsified by the neutralized amino acid ester. Other methods and an emulsifiers that is the neutralized amino acid ester are included. Because the neutralized amino acid ester and the compositions do not contain petrochemical-derived ingredient, the products are natural.

Abstract: The present invention relates to a cell, which has been genetically modified relative to its wild type, so that in comparison with its wild type it is able to produce more ?-aminocarboxylic acids, more ?-aminocarboxylic acid esters or more lactams derived from ?-aminocarboxylic acids, starting from carboxylic acids or carboxylic acid esters. Furthermore, the present invention relates to a method for the production of a genetically modified cell, the cells obtainable by this method, a method for the production of ?-aminocarboxylic acids, of ?-aminocarboxylic acid esters or of lactams derived from ?-aminocarboxylic acids, the ?-aminocarboxylic acids, ?-aminocarboxylic acid esters or lactams derived from ?-aminocarboxylic acids obtainable by this method, a method for the production of polyamides based on ?-aminocarboxylic acids or based on lactams and the polyamides obtainable by this method.

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: 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.