Abstract: The present invention covers zwitterionic, non-surface-active compounds in the form of carboxymethylated, short-chain dialkylaminoalkylamides and use thereof as therapeutic agent.

Abstract: The disclosure relates to engineered amidase polypeptides and processes of using the polypeptides for chiral resolution of amino acid amide compounds. The disclosure further relates to the polynucleotides that encode the engineered amidase polypeptides and related vectors, host cells, and methods for making the engineered amidase polypeptides.

Abstract: The present invention relates to compounds of azapeptide or azapeptidomimetic type of formula (I): in which R1, R2, R3, X1, X2, X3, X4 and Y are as defined in claim 1, to pharmaceutical compositions containing them and to such compounds as adjuvant for an anticancer or anti-infectious medicament.

Abstract: The subjects of the current invention are compounds, which exhibit arginase inhibiting activity (including difluoromethylornithine (DFMO) and L-norvaline, but not limited to them), and which can be used as therapeutically active agents for the treatment and prevention of depression and/or depression-related conditions. Other subjects of the present invention are the use of said arginase inhibiting compounds as therapeutically active agents for the manufacture of pharmaceutical compositions for human and veterinary application, pharmaceutical composition comprising said arginase inhibiting compound and a method for treatment and prevention of depression and/or depression-related conditions. Also, a method for identifying compounds suitable for use as therapeutically active agents for treatment and/or prevention of depression and/or depression-related conditions is disclosed.

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 invention relates to compounds having either agonist or antagonist activities for the neurotrophins NGF and BDNF and represented by monomeric or dimeric substituted dipeptides that are analogs of the exposed portions of loop 1 or loop 4 regions of these neurotrophins near or at a beta-turn of the respective loop. N-acylated substituents of these dipeptides are biostereoisomers of the amino acid residues preceding these dipeptide sequences in the neurotrophin primary structure. The dimeric structure is produced advantageously by using hexamethylenediamine to which dipeptides are attached via their carboxyl groups. The claimed compounds displayed neuroprotective and differentiation-inducing activities in cellular models and enhanced the amount of phosphorylated tyrosine kinase A and the heat shock proteins Hsp32 and Hsp70 in the concentration range of 10?9 to 10?5 M.

Abstract: A normal person (i.e. a control) and liver diseases such as drug induced liver injury, an asymptomatic hepatitis B carrier, an asymptomatic hepatitis C carrier, chronic hepatitis B, chronic hepatitis C, liver cancer, a nonalcoholic fatty liver disease (NAFLD), nonalcoholic steatohepatitis (NASH), and simple steatosis (SS) are identified by measuring the concentrations of ?-Glu-X (X represents an amino acid or an amine) peptides or the levels of AST or ALT in blood and carrying out, for example, a multiple logistic regression based on the measured value.

Abstract: Processes for making a diester compound of formula (B) and for converting it to pregabalin, especially via a compound of formula (2), can provide several advantages. The compound (B) can be converted to the compound (2) via reductive hydrogenation.

Abstract: A subject-matter of the invention is formulations comprising novel zwitterionic compounds and the use of these formulations as cosmetics.

Abstract: The invention provides derivative compounds of N-6-trimethyl-L-lysine (TML) for potential treatment of disorders resulting from deficiencies in the TML-carnitine pathway. The invention also provides a method of purification of TML and TML derivative compounds. The treatment of conditions of the diseases late infantile neuronal ceroid lipofuscinosis (LINCL) and neuronal ceroid lipofuscinosis (NCL) with TML were shown in the original parent application.

Abstract: An amino acid-modified organopolysiloxane is provided. It has an amino acid derivative bonded to at least one silicon atom of the organopolysiloxane segment constituting the backbone of the organopolysiloxane via an amide bond represented by the following general formula (1): wherein X and Y are independently a C1-10 divalent hydrocarbon group; m is an integer of 0 to 4; Ra is hydrogen atom, a monovalent hydrocarbon group containing 1 to 4 carbon atoms, or an organic group represented by the following general formula (2): (wherein Rb is hydrogen atom, a C1-7 monovalent hydrocarbon group, an alkaline metal, or an alkaline earth metal, and Rc is independently hydrogen atom, hydroxy group, or a C1-10 monovalent hydrocarbon group optionally containing oxygen atom, sulfur atom, or nitrogen atom); and Z is an organic group represented by the general formula (2).

Abstract: The presently disclosed and claimed inventive concepts include inhibitors of antiplasmin cleaving enzyme (APCE) and fibroblast activation protein alpha (FAP) which can be used in various therapies related to disorders of fibrin and ?2-antiplasmin and abnormal cell proliferation. The presently disclosed and claimed inventive concepts also include substrates of APCE and FAP, which may be used, for example, in screening methods for identifying such inhibitors. The presently disclosed and claimed inventive concepts further include, but are not limited to, methods of treating or inhibiting atherosclerosis and thrombus disorders by altering the ratios of types of plasma ?2-antiplasmin and to methods of treating conditions involving abnormal cell proliferation such as cancers.

Abstract: A method is provided for the parallel identification of one or more metabolite species within a biological sample. The method comprises analyzing the sample to produce a spectrum containing individual spectral peaks representative of the one or more metabolite species contained within the sample; subjecting each of the individual spectral peaks to a statistical pattern recognition analysis to identify the one or more metabolite species contained within the sample; and identifying the one or more metabolite species contained within the sample by analyzing the individual spectral peaks of the spectra.

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: There has been a demand in the marketplace for medicines, functional foods and so on which can relieve subjective symptoms of fatigue in persons having these subjective symptoms, and enabling the persons to have productive days. That is, an object of the present invention is to provide a composition for relieving subjective symptoms of fatigue. According to the present invention, a safe and effective composition for relieving subjective symptoms of fatigue which contains ornithine or a salt thereof as an active ingredient can be provided.

Abstract: A process for reacting, in the presence of a particular calcium containing catalyst, an amine having an active hydrogen and one or more of a fatty acid ester or a fatty acid.

Abstract: The present invention provides a method of suppressing the nonspecific interaction between molecules, characterized in that in a process to immobilize a molecule onto a solid phase carrier and analyze the specific interaction between the molecule and a molecule that specifically interacts with the molecule on the solid phase, the hydrophobic property of the solid phase surface in the solid phase carrier is regulated, particularly a hydrophilic spacer is interlaid at the time of immobilization of the molecule onto the solid phase carrier, which method makes it possible to suppress the nonspecific interaction between the molecules, and to reduce nonspecific adsorption to the solid phase.

Abstract: The present invention discloses compounds with a carboxyl acid group and an amide group which also containing the tertiary amino groups. The carboxyl acid group having a partial negative charge can attract the tertiary amino group with each other to form a quaternary ammonium salt structure, so that the compounds are easy to dissolve in water. Moreover, these compounds having a mushroom tyrosinase-inhibition effect and have the potential to use in the cosmetics for skin whitening.

Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a drug linker conjugate D-L, wherein -D is an amine containing biologically active moiety; and -L is a non-biologically active linker moiety -L1 represented by formula (I), wherein the dashed line indicates the attachment to the amine of the biologically active moiety and wherein R1, R1a, R2, R2a, R3, R3a, X, X1, X2, X3 have the meaning as indicated in the description and the claims and wherein L1 is substituted with one to four groups L2-Z and optionally further substituted, provided that the hydrogen marked with the asterisk in formula (I) is not replaced by a substituent; wherein L2 is a single chemical bond or a spacer; and Z is a carrier group. The invention also relates to A-L, wherein A is a leaving group, pharmaceutical composition comprising said prodrugs and their use as medicaments.

Abstract: The object of the present invention is analogues of peptides or parent proteins, these peptide analogues, comprising at least one aza-?3 aminoacyl residue, and also their uses in pharmaceutical compositions or for the diagnosis of pathologies wherein the aforesaid peptides or parent proteins are involved.

Abstract: Ligand functionalized substrates, methods of making ligand functionalized substrates, and methods of using functionalized substrates are disclosed.

Abstract: The present invention relates to novel arginine analogs, and methods for their synthesis and use. Such analogs are designed to provide a protected or free thiol (—SH) group, thereby providing a convenient linkage chemistry for coupling to a suitable group on a target such as a protein, polypeptide, detectable label or solid phase, and at a site distal to the guanidino group. Arginine analog conjugates are useful for generating antibodies that can bind specifically with dimethylarginine, which can be detected using such antibodies in immunoassays.

Abstract: Disclosed herein is a composition for promoting proline recycling, and more particularly, to a composition for external application to skin or cosmetic food comprising theanine as an active ingredient for promoting expression or activity of prolidase, which is an enzyme to promote proline recycling, thereby increasing collagen synthesis and restoring wrinkle.

Abstract: The present invention provides 2-azetidinone derivatives, or pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof, comprising formula (I): wherein the substituents are as herein defined. The compounds possess cholesterol absorption inhibitory activity and are accordingly of value in the treatment of disease states associated with hyperlipidaemic conditions.

Abstract: Disclosed herein are crystalline forms of L-ornithine phenyl acetate and methods of making the same. The crystalline form may, in some embodiments, be Forms I, II, III and V, or mixtures thereof. The crystalline forms may be formulated for treating subjects with liver disorders, such as hepatic encephalopathy. Accordingly, some embodiments include formulations and methods of administering L-ornithine phenyl acetate.

Abstract: This invention deals with a novel straight chain compound, namely, 1,6-diamino alkanoic acid having a straight chain of six carbon atoms with two terminal amino groups and accompanying —COOH group, which is capable of effecting controlled formation of new blood vessels in ischaemic tissues, and their pharmaceutically acceptable salts and/or derivatives thereof. The compounds may be in laevo, dextro, activated laevo, activated dextro or oligomeric form. The invention also pertains to a process for preparing the aforesaid novel compound, which is illustrated by the accompanying drawing.

Abstract: Provided herein are methods for synthesis of peptides. In particular, provided herein are methods of synthesis for therapeutic antiviral peptides.

Abstract: The present invention relates to a process for producing an N-carbamoyl-tert-leucine, characterized in mixing tert-leucine with an isocyanic acid compound while a pH of the mixture is kept at not less than 8.0 and not more than 13.5, wherein an amount of the isocyanic acid compound is not less than 0.9 times by mole and not more than 1.1 times by mole relative to an amount of the tert-leucine. According to the present invention, it becomes possible to easily produce an N-carbamoyl-tert-leucine with high efficiency, while the generation of by-products such as a dipeptide-like compound and a urea compound is prevented.

Abstract: The present invention relates to glutamic acid N,N-diacetic amide, potassium or sodium glutamate N,N-diacetic amide, glutamic acid N-acetic amide N-acetonithle, potassium or sodium glutamate N-acetic amide N-acetonitrile, to processes to prepare such compounds and the use thereof.

Abstract: Methods of production for Tricreatine Hydroxycitrate are disclosed. Tricreatine hydroxycitrate can be used as supplemental dietary ingredient for the purposes of reducing adiposity, suppression of appetite, improvement of muscle and exercise performance and recovery. The salts are useful in the dietetic, food supplement and food industries.

Abstract: The present invention provides crystals of L-ornithine and a process for producing the crystals of L-ornithine including the steps of (i) exposing L-ornithine or a salt thereof, a composition comprising L-ornithine or a salt thereof, or a solution containing L-ornithine, a salt thereof, or the composition to a cation exchange resin to adsorb L-ornithine onto the cation exchange resin; (ii) eluting L-ornithine from the cation exchange resin on which L-ornithine is adsorbed with an aqueous alkaline solution, and removing an alkaline component from the resulting eluate to prepare an aqueous L-ornithine solution; and (iii) mixing the aqueous L-ornithine solution with a hydrophilic organic solvent, and crystallizing L-ornithine from the resulting mixed solution.

Abstract: A nutrient composition comprises an essential nutrient in which at least one exchangeable H atom is 2H and/or at least one C atom is 13C. The nutrient is thus protected from, inter alia, reactive oxygen species.

Abstract: This invention relates to non-natural desamino amino acid compounds, methods of making, and peptides containing these compounds as their N-terminus moieties. A preferred example is neurotensin (8-13) in which the N terminus is an alpha desamino N,N dimethyl homolysine residue.

Abstract: In one aspect, the present invention provides a composition of a covalent conjugate of an eflornithine analog with an anti-inflammatory drug. In another aspect, the present invention provides a composition of an eflornithine prodrug. In another aspect, the present invention provides a composition of an eflornithine or its derivatives aspirin salt. In another aspect, the present invention provides methods for treating or preventing cancer using the conjugates or salts of eflornithine analogs or eflornithine prodrugs.

Abstract: A moisturizing agent comprising one or more than one compound selected from the group consisting of lysyl-?-alanine represented by the following general formula (1) and a salt thereof:

Abstract: The invention relates to compounds of the formula I as defined herein, which are inhibitors of activated thrombin-activatable fibrinolysis inhibitor. The compounds of the formula I are suitable for manufacturing medicaments for the prophylaxis, secondary prevention and therapy of one or more disorders which are associated with thromboses, embolisms, hypercoagulability or fibrotic changes.

Abstract: Compounds that provide for sustained systemic concentrations of GABA analogs following oral administration to animals are disclosed. Pharmaceutical compositions including, and methods using, such compounds are also disclosed.

Abstract: A method for producing 3-(2,2,2-trimethylhydrazinium)propionate dihydrate by saponification of salts of 3-(2,2,2-trimethylhydrazinium)propionate esters with subsequent purification step using saturation with carbon dioxide or sulphur dioxide in alcoholic solution.

Abstract: PEG linker compounds and biologically active conjugates thereof having mixed functional group linkages attached to at least one PEG moeity, and a coupling group for attaching a biologically active molecule. The PEG mixed linkages can be the combinations of stable, or labile, or releasable, or stable and labile, or stable and releasable, or releasable and labile covalent linkages. The mixed functional linkages of the PEG linker compounds consist of different organic functional groups, which have non-equivalent half-life in plasma and, hence, they have different release rates in blood. The present invention also provides for attachment of novel PEG linker compounds with mixed functional linkages for Pegylation of biologically active molecules to produce Probiomolecule-PEG constructs. The Probiomolecule-PEG construct is the prodrug of biomolecule-PEG conjugate or biomolecule.

Abstract: This invention relates to novel 4-dimethylaminobutyric acid derivatives of the formula wherein A1, A2, R1, m and n are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit carnitine palmitoyl transferase (CPT) activity, in particular CPT2 activity, and can be used as medicaments in methods for the treatment of diseases modulated by CPT2 inhibitors.

Abstract: This invention relates to novel 4-trimethylammoniobutyrates of the formula wherein A1, R1, m and n are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit carnitine palmitoyl transferase (CPT) activity, in particular CPT2 activity, and can be used as medicaments.

Abstract: This application relates to methods and compositions for treating rheumatoid arthritis by administering a combination therapy comprising methotrexate and an antibody to alpha-4 integrin or an immunologically active antigen binding fragment in therapeutically effective amounts. The application also relates generally to methods and compositions for treating rheumatoid arthritis by administering a combination therapy comprising methotrexate and small molecule alpha-4 integrin antagonist that inhibits the alpha-4 integrin (?4 integrin) interaction with VCAM-1. The invention further relates to methods of preparing the compounds and methods of using the compounds and compositions.

Abstract: Disclosed is a process for the enzymatic preparation of a gamma-glutamyl compound. The process comprises a step of contacting a gamma-glutamyl donor and a gamma-glutamyl acceptor with an aqueous medium comprising a gamma glutamyl transpeptidase enzyme. The enzyme is derived from a plant belonging to the Graminaceae or Leguminaceae family, or from Camellia sinensis.

Abstract: Disclosed is a method of coupling an amino or hydroxyl compound with the amino portion of a sulfonamide via condensation with a cyclic thioanhydride. The reaction of cyclic thioanhydrides with amines affords amides functionalized with thioacids, which can be trapped in situ with preferably electron deficient arylsulfonamides. In this manner the cyclic thioanhydride serves as a linchpin in a three component coupling sequence.

Abstract: The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

Abstract: The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

Abstract: The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

Abstract: Modified clay minerals obtained by treating a clay mineral with a particular acylarginine derivative are useful for stabilizing emulsion compositions, inter alia, W/O emulsion composition, while hardly causing skin irritation, and providing moisture retention properties.

Abstract: The novel salt creatine glycinate and compositions (dietary supplements, energy drinks, and dietetic or pharmaceutical products containing the same are described.

Abstract: The present invention provides crystals of L-ornithine and a process for producing the crystals of L-ornithine including the steps of (i) exposing L-ornithine or a salt thereof, a composition comprising L-ornithine or a salt thereof, or a solution containing L-ornithine, a salt thereof, or the composition to a cation exchange resin to adsorb L-ornithine onto the cation exchange resin; (ii) eluting L-ornithine from the cation exchange resin on which L-ornithine is adsorbed with an aqueous alkaline solution, and removing an alkaline component from the resulting eluate to prepare an aqueous L-ornithine solution; and (iii) mixing the aqueous L-ornithine solution with a hydrophilic organic solvent, and crystallizing L-ornithine from the resulting mixed solution.