Abstract: The invention relates to a method for the production of acetylsalicylic acid lysinate, optionally lysine acetylsalicylate.

Abstract: The present invention generally relies on a process for the preparation of chelated compounds, comprising the selective interaction between a solid matrix and a chelating agent. In more details, the present invention enables the preparation of chelated compounds useful as diagnostic agents, in high yields and in a reliable way.

Abstract: Using NMR/MS based metabonomics and targeted lipidomics approaches the inventors have explored the metabolic phenotypes of aging and longevity in a cohort compromising centenarians, elderly and young adults. The inventors have identified biomarkers for a reduced risk of developing ageing related chronic inflammatory disorders and propose an in vitro method of diagnosing a lifestyle that allows delaying and/or avoiding ageing related chronic inflammatory disorders using phenylacetylglutamine (PAG) as biomarker.

Abstract: The present invention relates to an improved process for the purification of polyaminocarboxylates such as DOTA, DTPA, DO3A-butrol, BOPTA.

Abstract: The present invention relates to the use of oligohydroxybenzoic acid derivatives in washing and cleaning agents in order to improve washing or cleaning performance with respect to bleachable stains.

Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, —C(?O), —S(?O)2—, —C(?O)O—, —C(O)NR3—, —C(?S)—NR3, —C(?NH)NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n and p are independently 0 or 1, Q is (i) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, or (ii), in the case where both m and p are 0, a divalent radical of formula —X2-Q1- or -Q1-X2— wherein X2 is —O—, S— or NRA— wherein RA is hydrogen or optionally substituted C1-C3 alkyl, and Q1 is an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic r

Abstract: The present invention is directed to Mannich condensation product sequestering agents or mixtures of Mannich condensation product sequestering agents for use in fuels and lubricating oils. The present invention is also directed to a process for preparing the Mannich condensation product sequestering agents. The present invention is also directed to a product formed by combining, under reaction conditions, a polyisobutyl-substituted hydroxyaromatic compound, an aldehyde, an amino acid or ester thereof, and an alkali metal base to form the Mannich condensation product sequestering agent. The present invention is also directed to a lubricating oil composition, a lubricating oil concentrate, a fuel composition, and a fuel concentrate having the Mannich condensation product sequestering agents of the present invention.

Abstract: This invention provides stable, lyophilized formulations of canfosfamide as well as the methods of preparation of those stable lyophilized formulations.

Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one aromatic amine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one alkylated amine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.

Abstract: The present invention relates to a novel compound, 3-amino-2-hydroxy-4-phenylbutanoyl-valyl-isoleucine with structure showed below. The compound is prepared from fermentation culture Streptomyces parvus CGMCC No. 4027 and is active as inhibitor of aminopeptidase. It can be used for preparation of aminopeptidase inhibitor.

Abstract: The present invention provides an iron chelating agent which can selectively chelate iron ions. The iron chelating agent of the present invention includes a compound represented by the following formula (1) or a salt thereof (wherein, ring Z represents an aromatic hydrocarbon ring or an aromatic heterocyclic ring; R1 represents an alkylene group; R2 and R3 each independently represent a hydrogen atom, a hydrocarbon group or a group having chelating ability; and the total coordination number of the groups represented by R2 and R3 is 1 or 2.

Abstract: The invention provides crystalline solid forms of (S)-4-((2S,3S)-7-carbamoyl-1,1-diethyl-3-methoxy-1,2,3,4-tetrahydronaphthalen-2-ylamino)-2-cyclohexylmethyl-butyric acid. The invention also provides pharmaceutical compositions comprising such crystalline solid forms, methods of using such crystalline solid forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline solid forms.

Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.

Abstract: The invention is directed to radiolabelled MMP selective compounds, a processes for the preparation thereof, and uses thereof. The derivatives of the invention have formula (I) wherein Y represents O, CH2, (CH2)2, S, NH, or C(?O)NH; X represents 1-5 substituents, wherein said substituents can be the same or different and wherein at least one of said substituents comprises a radioisotope suitable for PET and/or SPECT and/or a ?-emitter; Z is S; Q is chosen from the group consisting of 3-pyridyl and carboxyl; and R is chosen from the group consisting of C(?O)—NH—OH, (II), (III, (IV). The MMP selective compounds of the invention are selective for MMPs and can be used for the identification and treatment of unstable atherosclerotic plaques.

Abstract: Formulations of canfosfamide and their preparation.

Abstract: The invention relates to a method for producing crystalline 3,6,9-triaza-3,6,9-tris(carboxymethyl)-4-(4-ethoxybenzyl)undecanedioic acid of the formula I by saponifying 3,6,9-triaza-3,6,9-tris(tert-butoxycarbonylmethyl)-4-(4-ethoxybenzyl)-undecanedioic acid di-tert-butyl ester of the formula II in an aqueous alkali metal hydroxide solution and using 3,6,9-triaza-3,6,9-tris(carboxymethyl)-4-(4-ethoxybenzyl)undecanedioic acid of the formula I for producing the gadolinium complex of 3,6,9-triaza-3,6,9-tris(carboxymethyl)-4-(4-ethoxybenzyl)undecanedioic acid [(Gd-EOB-DTPA)=Primovist®].

Abstract: The present invention is directed to Mannich condensation product sequestering agents or mixtures of Mannich condensation product sequestering agents for use in fuels and lubricating oils. The present invention is also directed to a process for preparing the Mannich condensation product sequestering agents. The present invention is also directed to a product formed by combining, under reaction conditions, a polyisobutyl-substituted hydroxyaromatic compound, an aldehyde, an amino acid or ester thereof, and an alkali metal base to form the Mannich condensation product sequestering agent. The present invention is also directed to a lubricating oil composition, a lubricating oil concentrate, a fuel composition, and a fuel concentrate having the Mannich condensation product sequestering agents of the present invention.

Abstract: This invention relates to tryptophan hydroxylase inhibitors, compositions comprising them, and methods of their use for the treatment, management and/or prevention of metastatic bone disease.

Abstract: The invention relates to a process for the preparation of N,N?-bis(2-hydroxybenzyl)-ethylenediamine-N,N?-diacetic acid and its derivatives of general formula (I), wherein both R have the same meaning and are selected from H, C1-C4alkyl, CH2OH, SO3M, and COOM; and all M have the same meaning and represent hydrogen atom, Na, K or NH4; which comprises reductive amination of glyoxylic acid with a salan compound of general formula (II), in the presence of an amine proton acceptor. The compounds of formula (I) can be used as chelating agents for micronutrients in fertilizer preparations for plants.

Abstract: A medicament having an excellent CaSR agonist action which enables the prevention or treatment of diabetes or obesity is provided by a composition comprising the compound represented by general formula (I) as defined, or a salt thereof.

Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The invention relates to the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein n, G, W, X, Y, and R1 are defined in the detailed description and claims. The compounds of formula I bind to or associate with VLA-4 and can be used in delivery formulations to deliver drugs, nucleic acids, or other therapeutic compounds to tissues or cells expressing VLA-4.

Abstract: Polymeric polyamine is produced by polymerizing polyoxyalkylene-amine and a linker. The polyoxyalkylene-amine has a structural formula H2N—R—NH2, wherein R is selected from the group consisting of dianhydride, diacid, epoxy, diisocyanate and poly(styrene-co-maleic anhydride) copolymers (SMA). The linker can be anhydride, carboxylic acid, epoxy, isocyanate or poly(styrene-co-maleic anhydride) copolymers (SMA). The polymeric polyamine so produced can be used as a stabilizer or dispersant of the Ag nanoparticles.

Abstract: The instant invention relates to peptides obtained from the enzymatic hydrolysis of yellow pea seed proteins that are capable of lowering the blood pressure and reducing the effects of kidney disease in a subject b\ inhibiting or reducing the affinity of the enzymes in the renin-angiotensin system for their substrates, specifically renin, to compositions comprising said peptides and to uses thereof.

Abstract: Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.

Abstract: The invention relates to growth hormone compounds with a protracted profile. The effect is obtained by linking an albumin binding residue via a hydrophilic spacer to growth hormone variants. Further described are methods of preparing and using such compounds. These growth hormone compounds are based on there altered profile considered particular useful in therapy.

Abstract: This invention provides stable, lyophilized formulations of canfosfamide as well as the methods of preparation of those stable lyophilized formulations.

Abstract: The present invention is directed to biphenyl derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.

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: A conjugate comprising L-DOPA covalently linked to at least one ?-aminobutyric acid (GABA) moiety, an ester and/or an addition salt thereof are disclosed, as well as uses thereof for treating a neurodegenerative disease or disorder.

Abstract: A process for producing a peptide product having cholecystokinin secretion promoting effect, said process comprising hydrolyzing soybean residues with one or more proteases so that the peptide product having cholecystokinin secretion promoting effect is obtained. Also disclosed is the composition containing the peptide product and the use thereof.

Abstract: The present invention is directed to Mannich condensation product sequestering agents or mixtures of Mannich condensation product sequestering agents for use in fuels and lubricating oils. The present invention is also directed to a process for preparing the Mannich condensation product sequestering agents. The present invention is also directed to a product formed by combining, under reaction conditions, a polyisobutyl-substituted hydroxyaromatic compound, an aldehyde, an amino acid or ester thereof, and an alkali metal base to form the Mannich condensation product sequestering agent. The present invention is also directed to a lubricating oil composition, a lubricating oil concentrate, a fuel composition, and a fuel concentrate having the Mannich condensation product sequestering agents of the present invention.

Abstract: The present invention discloses a process for the preparation of gadobenate dimeglumine complex in a solid form. In particular, said solid form is conveniently obtained by spray-drying a corresponding liquid suspension at a given temperature and concentration. The present invention is particularly advantageous for the industrial scale as the solid form may be obtained by employing water as a solvent, which is a non-toxic solvent, easy to handle and basically not requiring troublesome health or safety precautions.

Abstract: The present invention concerns prodrugs of mexiletine (and mexiletine's active metabolite) pharmaceutical compositions containing such prodrugs. Methods for treating myotonic conditions, while reducing the inherent adverse GI side effects associated with mexiletine, increasing the bioavailability of mexiletine, and improving the pharmacokinetic reproducibility of mexiletine with the aforementioned prodrugs are also provided.

Abstract: A method for detecting ?-amyloid using an amino acid dimer instead of a secondary antibody binding to the ?-amyloid primary antibody in an immunoassay based on an antigen-antibody reaction, and a kit for detecting ?-amyloid including the dimer. The method is advantageous in that the dimer has good properties in stability, availability, and storage compared to antibodies and that it can detect various ?-amyloids by using one kind of antibody, and thus may be effectively used in early diagnosis and research of Alzheimer's disease.

Abstract: [Problem] A compound which is useful as an anti-obesity agent is provided. [Means for Solution] The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases, and as a result, they have found that the diacylethylenediamine compound of the present invention has an excellent DGAT1 inhibitory action, thereby completing the present invention. That is, the diacylethylenediamine compound of the present invention has a DGAT1 inhibitory action, and can be therefore used as an agent for preventing and/or treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases.

Abstract: The present invention relates to novel acid-free quaternized nitrogen compounds, to the preparation thereof and to the use thereof as a fuel and lubricant additive, more particularly as a detergent additive, as a wax antisettling additive (WASA) or as an additive for reducing internal diesel injector deposits (IDID); to additive packages which comprise these compounds; and to fuels and lubricants thus additized. The present invention further relates to the use of these acid-free quaternized nitrogen compounds as a fuel additive for reducing or preventing deposits in the injection systems of direct-injection diesel engines, especially in common-rail injection systems, for reducing the fuel consumption of direct-injection diesel engines, especially of diesel engines with common-rail injection systems, and for minimizing power loss in direct-injection diesel engines, especially in diesel engines with common-rail injection systems.

Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.

Abstract: The present invention relates to compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7 and R8 are defined as stated hereinafter, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.

Abstract: The present invention relates to a novel compound having excellent antioxidant activity, isolated from Ramalina terebrata, and more particularly to a novel compound, Ramalin, having excellent antioxidant activity, isolated from the Antarctic lichen Ramalina terebrata, a method for preparing the Ramalin, and a pharmaceutical composition, a functional food and a functional cosmetic composition, which contain the Ramalin as an active ingredient. The Ramalin according to the invention has significantly excellent antioxidant effects compared to commercially available antioxidants, and thus can be widely used in agents for treating oxidation-related diseases, anti-aging functional foods, functional cosmetic products for skin whitening and wrinkle reduction, etc.

Abstract: The present invention provides an iron chelating agent which can selectively chelate iron ions. The iron chelating agent of the present invention includes a compound represented by the following formula (1) or a salt thereof (wherein, ring Z represents an aromatic hydrocarbon ring or an aromatic heterocyclic ring; R1 represents an alkylene group; R2 and R3 each independently represent a hydrogen atom, a hydrocarbon group or a group having chelating ability; and the total coordination number of the groups represented by R2 and R3 is 1 or 2.

Abstract: The present invention provides methods and therapeutic agents for lowering or increasing serum serotonin levels in a patient in order to increase or decrease bone mass, respectively. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis and the agents are TPH1 inhibitors or serotonin receptor antagonists.

Abstract: The present invention provides novel phenoxyacetic acids useful for the prevention and treatment of inflammatory disorders, including those affecting the respiratory system and skin.

Abstract: The present invention relates to dephenolic compounds, an example of which is shown below, which are functionalized, and polymers formed from the same. Polymers formed from the functionalized diphenolics are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.

Abstract: In one aspect, the present invention provides a contrast enhancement agent comprising an iron chelate having structure I wherein R1 is independently at each occurrence a hydroxy group, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R2-R7 are independently at each occurrence hydrogen, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R1-R7 is a hydroxy group or a C1-C3 hydroxyalkyl group; and wherein Q is a charge balancing counterion. Also provided is a metal chelating ligand having structure IX and medical formulations comprising the contrast enhancement I.

Abstract: The invention provides compounds formula (I), their preparation, and their use as pharmaceutically active immuno-suppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SIP receptors.

Abstract: The present invention concerns prodrugs of mexiletine (and mexiletine's active metabolite) with amino acids or peptides and pharmaceutical compositions containing such prodrugs. Methods for providing pain relief, treating arrhythmia, decreasing the adverse GI side effects associated with mexiletine, increasing the bioavailability of mexiletine, and improving the pharmacokinetic reproducibility of mexiletine with the aforementioned prodrugs are also provided. Oligopeptides incorporating lysine or arginine residues attached directly or indirectly through a glycine residue are also described herein.

Abstract: The present invention includes methods of making and methods of using peptidomimetics compositions that mimic ?-helical BH3 sequences in cells. The peptidomimetics can be used to mimic ?-helical BH3 sequences and kill cancer cells.

Abstract: The present invention relates to biaryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.

Abstract: The invention relates to a process for the preparation of N,N?-bis(2-hydroxybenzyl)-ethylenediamine-N,N?-diacetic acid and its derivatives of general formula (I), wherein both R have the same meaning and are selected from H, C1-C4alkyl, CH2OH, SO3M, and COOM; and all M have the same meaning and represent hydrogen atom, Na, K or NH4; which comprises reductive amination of glyoxylic acid with a salan compound of general formula (II), in the presence of an amine proton acceptor. The compounds of formula (I) can be used as chelating agents for micronutrients in fertilizer preparations for plants.