Abstract: Various compounds can be administered orally to humans or animals for the purpose of enhancing nitric oxide production. Enhancing nitric oxide production is beneficial for those looking to increase lean body mass or enhance exercise performance. Such administration can also be used for the purpose of enhancing nutrient transport for purposes of athletic performance and controlling bodyweight and body fat levels. L-Arginine and alpha amino n-Butryate work synergistically to enhance nitric oxide production and may further be coupled with either and/or a) an inhibitor of nitric oxide breakdown or b) a nitric oxide potentiators or other precursor and serve to accomplish this goal of enhance nitric oxide. The composition may be administered in a variety of ways including capsules, tablets, powdered beverages, bars, gels or drinks.

Abstract: Disclosed herein are various novel oxazolidinone, imidazolidinone, and thiazolidinone analogs and methods of treating cancer and/or microbial infection using these analogs. Particular 4-oxazolidinone compounds are shown to have anti-cancer and anti-microbial activity.

Abstract: The present invention relates to compounds particularly asymmetric urea compounds which are labeled with one or more radioisotopes and which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors which express NAALADase and/or PSMA. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled compounds of the invention, particularly tissues, organs, or tumors which express NAALADase and/or PSMA to which the compounds of the invention have an affinity.

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 oxime, carbonyl, dicarbonyl, and/or hydroxylamine 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 oxime, carbonyl, dicarbonyl, and/or hydroxylamine 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: A process of producing dicreatine malate with high purity, includes the steps of providing a predetermined amount of malic acid, agitating a predetermined amount of anhydrous alcohol to the malic acid to obtain a first solution, filtering the first solution to form a clear solution, agitating a predetermined amount of creatine to the clear solution to obtain a second solution, centrifuging the second solution to obtain a wet dicreatine malate and a separated alcohol, and drying the wet dicreatine malate to produce a dicreatine. Because of its low energy consumption, this process produces dicreatine malate effectively.

Abstract: A compound or a salt thereof having the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, said atoms constitute the pharmacophore represented by the following formula: and inhibits the activity of transcription factor AP-1 and is useful as an agent for preventing and treating the diseases into which over expression of AP-1 participates and as an AP-1 inhibitor.

Abstract: Disclosed are creatine salts having the general formula wherein A is a member of a group consisting of an anion of ketoglutaric acid and succinic acid.

Abstract: This invention relates to a novel compound, dicreatine malate, comprising approximately two moles of creatine cations per one mole of malate anion. The creatine salt of this invention has been found to increase the bioavailability of both the creatine and malic acid moieties over and above the individual bioavailabilities of creatine monohydrate and malic acid base. Dicreatine malate vastly improves the production of Adenosine TriPhosphate (ATP) beyond the level of creatine monohydrate or any other creatine derivative. It also has a much greater efficacy in uses such as increasing muscle mass, increasing cell volumization, decreasing adipose stores, and for increasing overall strength and endurance.

Abstract: Disclosed are pharmaceutical compositions containing: extracts of Tribulus terrestris, Turnera diffusa and Cinnamon cassia in the weight ratio of 1.5–3.5:1–2:0.1–0.4 respectively; Ginkgo biloba extract, and optionally arginine or a physiologically equivalent esters salts or precursor thereof. The compositions according to the invention are useful in the treatment of male and female sexual dysfunctions.

Abstract: Disclosed are creatine salts having the general formula wherein A represents an anion of a dicarboxylic acid, and a process of making such salts.

Abstract: Compounds of formula (I) wherein: Q represents an amidino group, a cyano group or a group of formula XYN—, (where X and Y are hydrogen or various groups); Ra represents alkylene; Rb and Rc each represents alkylene, the total number of carbon atoms in said straight chains of Rb and Rc being 7); R2 and R3 each represents hydrogen, or a group of formula R, RCO—, ROCO—, or RNHCO—, where R represents alkyl or aryl; the chiral carbon atom indicated by the asterisk is in the L configuration; Z is an aromatic amino acid residue; n is 0 or 1; R1 represents hydrogen, alkyl or aryl; and W represents hydrogen, alkyl or aryl; and pharmaceutically acceptable salts thereof have the ability to protect against the neuronal damage which may be caused by an ischemic event.

Abstract: Compounds of the formula I, in which R1, R2, R3, R4, R5, and R6 have the meanings given in the description, and their physiologically acceptable salts. The compounds are suitable for use, for example, as hypolipidemics.

Abstract: A kit of parts containing (a) a pharmaceutical formulation including a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative thereof, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier, and (b) a pharmaceutical formulation including a prodrug of a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative of that prodrug, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier. Components (a) and (b) are each provided in a form that is suitable for administration in conjunction with the other. The kit is useful in the treatment of conditions in which inhibition of thrombin is required or desired.

Abstract: The present invention is directed to a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: R2 is selected from the group consisting of H and methyl; and R2 is selected from the group consisting of H and methyl. The compounds possess useful nitric oxide synthetase inhibiting activity, and are expected to be useful in the treatment or prophylaxis of a disease or condition in which the synthesis or over synthesis of nitric oxide forms a contributory part.

Abstract: The present invention relates to 2-amino-2-alkyl-5 heptenoic and heptynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.

Abstract: Polyoxometalate compounds which exhibit anti-retroviral activity are disclosed. Compounds with anti-retroviral activity include those having the following general molecular formulas: M7PW11O39 M8SiW11O39 M9HSiW9O34 M8HPW9O34 M10(TM)4(PW9O34)2 M16(TM)4(P2W15O56)2 M14[NaP5W30O110] M12(TM)3(PW9O34)2 M6P2W18O62 wherein M is an alkali metal, NH4+ or other common monocation or soluble dication, or any combination of the above provided adequate water solubility is exhibited, or histidinium ion, argininium ion, or lysinium ion or any dication of a dipeptide or oligopeptide with 2 protonated basic amino acid residues, or any combination of these monocations or dications with each other or with any common inorganic cation, and TM is a divalent transition metal ion, such as Mn, Fe, Co, Ni, Cu and Zn.

Abstract: The present invention relates to improved chelator conjugates with biological targeting molecules, suitable for forming metal complexes with radiometals. The radiometal complexes, especially with the radiometal99mTc, are useful as radiopharmaceuticals.

Abstract: The present invention relates to 2-amino-2-alkyl-3 hexenoic and hexynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.

Abstract: The present invention pertains to specific peptides obtainable from cocoa beans and giving rise to a particular and distinct savor when subjected to a Maillard reaction with reducing sugars. In particular, the present invention pertains to the use of one or more of these specific peptides for the preparation of a chocolate flavor, specifically a cocoa and a caramel flavor, a floral or specifically, a bonbon flavor, a bready flavor, a roasted flavor or a meat flavor.

Abstract: This invention relates to a novel compound, dicreatine malate, comprising approximately two moles of creatine cations per one mole of malate anion. The creatine salt of this invention has been found to increase the bioavailability of both the creatine and malic acid moieties over and above the individual bioavailabilities of creatine monohydrate and malic acid base. Dicreatine malate vastly improves the production of Adenosine TriPhosphate (ATP) beyond the level of creatine monohydrate or any other creatine derivative. It also has a much greater efficacy in uses such as increasing muscle mass, increasing cell volumization, decreasing adipose stores, and for increasing overall strength and endurance.

Abstract: This invention relates to a process for the synthesis and method of use of an effective amount of a creatine heterocyclic acid salt for the regulation athletic function in humans.

Abstract: Compounds of formula (I) wherein: Q represents an amidino group, a cyano group or a group of formula XYN—, (where X and Y are hydrogen or various groups); Ra represents alkylene; Rb and Rc each represents alkylene, the total number of carbon atoms in said straight chains of Rb and Rc being 7); R2 and R3 each represents hydrogen, or a group of formula R, RCO—, ROCO—, or RNHCO—, where R represents alkyl or aryl; the chiral carbon atom indicated by the asterisk is in the L configuration; Z is an aromatic amino acid residue; n is 0 or 1; R1 represents hydrogen, alkyl or aryl; and W represents hydrogen, alkyl or aryl; and pharmaceutically acceptable salts thereof have the ability to protect against the neuronal damage which may be caused by an ischemic event.

Abstract: The present invention provides compositions and their use in the treatment of inflammatory diseases caused by T-cell proliferation such as sepsis, inflammatory bowel diseases, autoimmune encephalomyelitis, or lupus.

Abstract: A process for the production of (R)— or (S)-aminocarnitine starting respectively from (R)— or (S)-nitryloxycarnitine, through the formation and hydrogenation of the azidocarnitine intermediate with the same absolute configuration is described. (R)— aminocarnitine inner salt is obtained after purification, which is then converted into non-deliquescent salts. A further subject of the present invention is a process for the preparation of derivatives of (R)— and (S)-aminocarnitine, in particular acylated or ureic derivatives, having known pharmacological properties, starting from (R)— and (S)-aminocarnitine salts, releasing the aminic function in situ.

Abstract: A composition for an infant formula which comprises a low threonine content; a method of producing the composition; use of the composition in the manufacture of a medicament or nutritional product for addressing the nutritional needs and providing healthy growth of an infant; and a method of addressing the nutritional needs and providing healthy growth of an infant which comprises administering an effective amount of the composition. A preferred embodiment of the composition comprises all of: i) acid whey protein or sweet whey protein from which caseino-glyco-macropeptide has been removed; and ii) free arginine; and iii) free histidine; and iv) free tyrosine or free tryptophan or tryptophan rich milk protein or a mixture thereof.

Abstract: (2S,5Z)-2-amino-7-(ethanimidoylamino)-2-methylhept-5-enoic acid is crystallized as an anhydrous, stoichiometric 1.5 HCl salt and a scaleable crystallization method is disclosed. The salt form was characterized and the absolute configuration of the chiral center was confirmed as “S”. (2S,5Z)-2-amino-7-(ethanimidoylamino)-2-methylhept-5-enoic acid was high melting and appears acceptably non-hygroscopic for use in a pharmaceutical composition.

Abstract: Disclosed are creatine salts having the general formula 1

Abstract: A process for the preparation of creatine or creatine monohydrate by reaction of sodium or potassium sarcosinate with cyanamide at a temperature from 20 to 150° C. and a pH from 7.0 to 14.0 comprises carrying out the pH adjustment with carbonic acid.

Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.

Abstract: The present invention relates to 2-amino-2-alkyl-4 hexenoic and hexynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.

Abstract: A process for producing 4-bromo-2-oxyimino butyric acid, predominantly as the (Z)-isomer of formula (I), 1

Abstract: New spisulosine derivatives of use in treating tumors are of the formula (I) wherein: each X is the same or different, and represents H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, CN, halogen, C(═O)H, C(═O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic, or two groups X may together form ═O; Y is NR1, OR1, PR1, SR1, or halogen, wherein the number of substituents R1 is selected to suit the valency and each R1 is independently selected of H, OH, C(═O)R′, P(═O)R′R″, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, and wherein the dotted line indicates an optional double bond; each Z is the same different, and represents H, OH,

Abstract: A chemical composition and method of use of the composition is described. The chemical composition includes an aza-enediyne, aza-enyne allene, or an aza-diallene. These compound are preferably non-hydrolyzable, cationic compounds that bind to nucleic acids. In addition it is believed that these compounds may undergo chemical reactions in the presence of a nucleic acid to generate reactive intermediates that cleave nucleic acids.

Abstract: A method of preparing a 2-alkyl amino acid involves the aziridination of an alkylacrylate and the opening of the aziridine ring by addition of a side chain. This method can result in the preparation of enantiomeric excess of a 2-alkyl amino acid. The invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.

Abstract: Derivatives of active ingredients with creatine and ornithine are disclosed having enhanced nutritional and/or therapeutic effects which favorably lend themselves to the preparation of orally administrable solid compositions.

Abstract: The present invention relates to a process for the preparation of 4-halogeno-2-substitutedimino-3-oxo-butyric acid of formula (I) 1

Abstract: Novel molecules without intramolecular peptidic bonds, able to mimic the RGD peptide, containing ARG-GLY-ASP motif “arginine-glycine-aspartic acid” (that is a potent inhibitor, in vivo and in vitro, of cellular adhesion) In vitro experimentation demonstrated that said molecules are efficient inhibitors of RASMC adhesion, proliferation and migration.

Abstract: The invention provides compounds that are useful for the treatment of bacterial infections in mammals.

Abstract: There are disclosed &bgr;-sheet mimetics and methods relating to the same for imparting or stabilizing the &bgr;-sheet structure of a peptide, protein or molecule. In one aspect, the &bgr;-sheet mimetics are covalently attached at the end or within the length of the peptide or protein. The &bgr;-sheet mimetics have utility as protease inhibitors generally, including activity as serine protease inhibitors such as thrombin, elastase and Factor X.

Abstract: The invention concerns a perfusion and/or preservation and/or re-perfusion solution during organ transplant, in particular the cardiac organ, containing the following elements: K+ in the range of about 4 to about 7 mM; Ca2+ in the range of about 0.2 to about 0.3 mM; Mg2+ in the range of about 13 to about 16 mM; glutamate in the range of about 18 to about 22 mM; arginine in the range of about 2 to about 4 mM; adenosine in the range of about 0.5 to 1 mM.

Abstract: The present invention is directed to nitrosated or nitrosylated &agr;-adrenergic receptor antagonists, compositions comprising &agr;-adrenergic receptor antagonists that are optionally substituted with at least one NO or NO2 moiety and compounds that donate, transfer or release nitric oxide or elevate levels of endogenous endothelium-derived relaxing factor, and methods for treating sexual dysfunctions in males and females.

Abstract: A process for preparing guanidine derivatives, in particular creatine, is described and entails continuously combining a cyanamide derivative and a primary or secondary amine in the presence of crystals of the guanidine derivative.

Abstract: Chelating agents (chelants) of the general structure: 1

Abstract: The present invention contains halogenated 2-amino-4,5 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.

Abstract: The present invention discloses halogenated 2-amino-5,6 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.

Abstract: The present invention contains novel compounds useful as nitric oxide synthase inhibitors.

Abstract: A chemical composition and method of use of the composition is described. The chemical composition includes an aza-enediyne, aza-enyne allene, or an aza-diallene. These compound are preferably non-hydrolyzable, cationic compounds that bind to nucleic acids. In addition it is believed that these compounds may undergo chemical reactions in the presence of a nucleic acid to generate reactive intermediates that cleave nucleic acids.

Abstract: The present invention relates to 2-amino-2-alkyl-5 heptenoic and heptynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.

Abstract: The present invention relates to 2-amino-2-alkyl-4 hexenoic and hexynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.

Abstract: Novel molecules without intramolecular peptidic bonds, able to mimic the RGD peptide, containing ARG-GLY-ASP motif “arginine-glycine-aspartic acid” (that is a potent inhibitor, in vivo and in vitro, of cellular adhesion) In vitro experimentation demonstrated that said molecules are efficient inhibitors of RASMC adhesion, proliferation and migration.