Abstract: A bis-alkoxyl amide alkyl cationic peptide lipid has a chemical structure as below: wherein the bis-alkoxyl amide alkyl cationic peptide lipid is dispersed in water to obtain the cationic peptide liposome which are high in stability and uniform in dispersion and have about 120 nm of average grain diameter and Zeta electric potential between 30 and 50 mV. The liposome can effectively compress the plasmids DNA and siRNA, can efficient transfection both in-vitro and in-vivo, and almost does not have toxicity to cells and mice, so that the liposome can be widely applied in gene delivery as a gene vector.

Abstract: Embodiments of the present invention provide for efficient methods and processes for preparing ionic amino acid esters from a specific synthesis route. The disclosed embodiments consist of a single reaction step: reacting a natural or synthetic unprotected amino acid with an aliphatic, branched or aromatic fatty alcohol of even or odd number of carbon atoms from 6 to 20 with or without unsaturation(s), in stoichiometric amounts, in the presence of an organic acid (HX) like carboxylate, mesylate, tosylate or sulfonate, employed as catalyst and under conventional heating (CC) of 1 to 3 hours at a temperature in the range of approximately 60 to 150° C. and pressure the range of approximately 0 to approximately 250 psi; the product obtained is cooled and recrystallized from ethanol.

Abstract: A method for concentrating and crystallizing fermentable carboxylic acids, salts, and mixtures thereof may involve the use of carboxylic acids that have a defined temperature dependence of the solubility and of the osmotic pressure. The carboxylic acids may be concentrated by a membrane method and subsequently crystallized out by a cooling crystallization and isolated. In some examples, the membrane method may involve nanofiltration, reverse osmosis, and/or membrane distillation for separation into a concentrate and a permeate. Similarly, an apparatus for implementing such methods may include a nanofiltration, reverse osmosis, and/or membrane distillation unit for concentrating the carboxylic acid, and at least one cooling crystallization unit for crystallizing the carboxylic acid.

Abstract: The present invention relates to MRI contrasting agent for contrasting cancer cell which contains ultrafine nanoparticles. More particularly, the present invention is directed to a self-assembled ligand composition comprising a ligand A, which is separated at a specific pH range, and a ligand B of which surface charge changes at a specific pH range, MRI contrast agent for contrasting cancer cell comprising said ligand composition and MRI contrasting nanoparticles, and the methods for preparing them.

Abstract: Provided herein are compositions including diastereomers in substantially diastereomerically pure form and enantiomers in substantially enantiomerically pure form, and processes for preparing them and converting them to metyrosine.

Abstract: An aqueous oral spray designed to treat mouth guards against bacterial infection comprising: 1. A naturally derived di-basic amino acid derivative, 2. A natural sweetener which inhibits the adhesion of bacteria to the oral cavity and, 3. Optionally a natural flavor and/or natural dye 4. Optionally a mouth guard surface modified to absorb specific components of above oral aqueous solution so as to render mouth guard more effective overtime in inhibiting microorganism growth on surface and in contact with mouth surfaces compared with unmodified mouth guard surface.

Abstract: A process for preparing amino acid-modified siloxanes that can be carried out under mild conditions is provided as well as organically modified silicones for care formulations for skin, hair and textiles that are toxicologically unobjectionable.

Abstract: The present application relates to functionalized nanodiamonds, to complexes comprising a functionalized nanodiamond reversibly bound to a nucleic acid and to compositions comprising such functionalized nanodiamonds and complexes. In particular, the functionalized nanodiamonds comprise at least one naturally occurring basic amino acid, or analogs or derivatives thereof, covalently linked to a nanodiamond. The present application also includes methods and uses of the complexes and compositions, for example for delivering a nucleic acid to a cell.

Abstract: The invention provides compositions for stimulating the formation of one or more extracellular matrix components that contain a lipoaminoacid derivative of the tripeptide carnosine such as N-Octanoyl Carnosine. Also provided are compositions containing N-Octanoyl Carnosine in combination with selected tripeptide and/or tetrapeptides as well as pharmaceutical and/or cosmetic compositions containing such compositions. The invention further provides methods of using the compositions and compositions of the invention to treat, alleviate, and/or ameliorate a symptom, condition, disorder, or disease of the skin or mucosa, wherein the symptom, condition, disorder, or disease is associated with changes in extracellular matrix components.

Abstract: The present invention relates to novel drug conjugates, where in two drugs are linked together through an appropriate linker having at least two functional groups capable of forming covalent bond with drugs D1 and D2. The invention also relates to developing novel compositions, methods for their preparation and their use in treating various disease conditions.

Abstract: Dipeptide compounds containing a histidine residue proved to have interesting blocking activity on secondary products from lipid oxidative stress, in particular on unsaturated aldehydes such as malondialdehyde and hydroxynonenal, which are known to contribute to the inset of quite a number of chronic pathologies such as neurodegenerative, inflammatory chronic, cardiovascular diseases, diabetes complications and cataract.

Abstract: Organic dicarboxylic acid compounds, salts and preparation methods thereof are described. The compounds have activity of resisting oxidation damage to crystalline lens of eyes. The structures of the above organic dicarboxylic acid compounds are shown as wherein R is a hydrogen atom, a C1-3 alkyl group, a C1-3 alkoxyl group, or a halogen atom.

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 relates to method for treating skin diseases and skin conditions in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, or enantiomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals.

Abstract: Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R?, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.

Abstract: This invention discloses a method of preservation of a food product comprising the step of adding 1) a first component comprising between 10 ppm and 1% of a biocidal salt of N?—(C1-C22) alkanoyl di-basic amino acid alkyl (C1-C22) ester cationic biocidal molecule with an anionic counterion, and 2) a second component comprising from 10 ppm to 1% by weight an acyl monoglyceride, directly to a food product. The preferred cationic biocidal molecule comprises N?-lauroyl-L-arginine ethyl ester (“LAE”). The invention also discloses the method of preservation of a food product using salts of a N?—(C1-C22) alkanoyl di-basic amino acid alkyl (C1-C22) ester cationic biocidal molecule and an anionic counterion with or without a monoglyceride of a fatty acid, whereby the packaging film is compounded with the salts and the optional monoglyceride of a fatty acid.

Abstract: The present invention generally relates to methods and systems relating to the selection of substrates comprising crystalline templates for the controlled crystallization of molecular species. In some embodiments, the methods and systems allow for the controlled crystallization of a molecular species in a selected polymorphic form. In some embodiments, the molecular species is a small organic molecule (e.g., pharmaceutically active agent).

Abstract: A monitoring test for recurrent breast cancer with a high degree of sensitivity and specificity is provided that detects the presence of a panel of multiplicity of biomarkers that were identified using metabolite profiling methods. The test is capable of detecting breast cancer recurrence about a years earlier than current available monitoring diagnostic tests. The panel of biomarkers is identified using a combination of nuclear magnetic resonance (NMR) and two dimensional gas chromatography-mass spectrometry (GC×GC-MS) to produce the metabolite profiles of serum samples. The NMR and GC×GC-MS data are analyzed by multivariate statistical methods to compare identified metabolite signals between samples from patients with recurrence of breast cancer and those from patients having no evidence of disease.

Abstract: Disclosed is an agent for use in the treatment or prevention of inflammatory bowel disease. Also disclosed is an agent for inhibiting the production of TNF-?. A therapeutic or prophylactic agent for inflammatory bowel disease comprising at least one amino acid selected from the group consisting of lysine, histidine, phenylalanine, methionine, tryptophan, glutamine, glycine, cysteine, cystine and threonine, the amino acid being administered at a dose of 0.1 to 4000 mg/kg per day; and a TNF-? production inhibitor comprising an amino acid selected from the group consisting of histidine, phenylalanine and tryptophan, the amino acid being administered at a dose of 0.1 to 4000 mg/kg per day.

Abstract: Organic dicarboxylic acid compounds, salts and preparation methods thereof. The said compounds have activity of resisting oxidation damage to crystalline lens of eyes. The structures of the above organic dicarboxylic acid compounds are shown as formula (1).

Abstract: The present invention is related to methods for preventing or retarding (i.e., inhibiting) yellow color or peroxide formation in a composition. The present invention is also related to methods of reducing or decreasing the amount of yellow color or peroxide in a composition. More specifically, the present invention relates to the use of an antioxidant, an oxygen scavenger, pH, a chelating agent, and/or at least two factors in the methods of the invention. The present invention is also related to methods for predicting the rate of yellow color or peroxide formation in a composition.

Abstract: The present invention relates to method of lowering intraocular pressure in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising a ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, of enantiomers thereof, of tautomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals.

Abstract: The present invention relates to method for treating skin diseases and skin conditions in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, or enantiomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals.

Abstract: The present invention relates to novel compounds, ester pro-drugs of [3-(1-1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals in the treatment of conditions mediated by adrenergic receptors.

Abstract: The present invention relates to a process for producing 2-[1-(S)-carboxy-2(S)-[3-(3,5-dichloro-benzyl)-3H-imidazol-4-yl]-ethylamino]-4-methyl-pentanoic acid, as well as novel salts, including hydrates and solvates thereof, and novel crystalline and amorphous forms thereof.

Abstract: A stable aqueous composition containing follicle-stimulating hormone, which comprises follicle-stimulating hormone and histidine as a stabilizing agent.

Abstract: The present invention provides the use of pelorol analogs of Formula, (I) and pharmaceutical compositions thereof as modulators of SHIP 1 activity. A compound or a pharmaceutical composition of the present invention may be used for the treatment or prophylaxis of an inflammatory, neoplastic, hematopoetic or immune disorder or condition in addition to other disorders and conditions.

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: 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 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 novel class of antimicrobial polymeric agents which are designed to exert antimicrobial activity while being stable, non-toxic and avoiding development of resistance thereto and a process of preparing same are disclosed. Further disclosed are pharmaceutical compositions containing same and a method of treating medical conditions associated with pathological microorganisms, a medical device, an imaging probe and a food preservative utilizing same. Further disclosed are conjugates of an amino acid residue and a hydrophobic moiety residue and a process of preparing same.

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: Histidine and/or a derivative thereof. In some embodiments, the histidine and/or a derivative thereof is used in maintaining and/or improving barrier function of the skin of a subject. In some embodiments, the histidine and/or a derivative thereof is used for the prevention and/or treatment of an inflammatory skin disease.

Abstract: The present invention provides the use of prodrugs of pelorol and homopelorol, related compounds and pharmaceutical compositions thereof as modulators of SHIP1 activity. A compound or a pharmaceutical composition of the present invention may be used for the treatment or prophylaxis of an inflammatory, neoplastic, hematopoetic or immune disorder or condition in addition to other disorders and conditions.

Abstract: The invention relates to compouns derived from betulin, and to the use thereof as antibacterial agents in pharmaceutical and cosmetic applications.

Abstract: A biofilm-removing agent which effectively removes biofilms is provided. A biofilm-removing agent containing a basic amino acid derivative represented by the following formula (1) or a salt thereof: (wherein R1 represents a linear- or branched-alkyl group having 4 to 18 carbon atoms or a linear- or branched-alkenyl group having 4 to 18 carbon atoms; X and Y each represent a group selected from the groups represented by the following formulas: and m represents an integer from 1 to 5).

Abstract: A controlled release biocidal salt of a first component comprises a cation of a N?—(C1-C22)alkanoyl di-basic amino acid alkyl(C1-C22)ester cationic biocidal molecule and a second component comprising an anion of a monomeric anionic molecule having insignificant biocidal activity. The salt is characterized such that when the salt is exposed to an aqueous medium, the salt partially dissolves thereby releasing biocidal ions in an amount sufficient to exceed the MIC or MBC of a target bacteria being controlled, and further characterized as leaving a residual reservoir of undissolved salt capable of releasing more biocidal ions as the salt is consumed or otherwise removed from the environment encompassing the target bacteria. The preferred cationic biocidal molecule comprises N?-lauroyl-L-arginine ethyl ester (“LAE”).

Abstract: An object of the present invention is to provide a cerebral infarction suppressant which is effective for brain tissue necrosis after long-time ischemia as in actual cerebral infarction and has fewer side effects. The cerebral infarction suppressant of the present invention is characterized in that histidine is contained and the cerebral infarction is attributed to long-time ischemia.

Abstract: The present invention herein provides, for instance, a stable isotope-labeled phenylalanine wherein a carbon atom of the phenyl group linked to an amino acid residue is 13C, 2 to 4 carbon atoms of the remaining 5 carbon atoms constituting the phenyl group are 12C atoms to which deuterium atoms are bonded, and the remaining carbon atoms are 13C atoms to which hydrogen atoms are linked, and a stable isotope-labeled tyrosine wherein a carbon atom of the phenyl group linked to an amino acid residue is 13C, the carbon atom bonded to the hydroxyl group (OH group) of the phenyl group is 12C or 13C, 2 to 4 carbon atoms of the remaining 4 carbon atoms constituting the phenyl group are 12C atoms to which deuterium atoms are bonded, and the remaining carbon atoms are 13C atoms to which hydrogen atoms are linked.

Abstract: Novel compounds, compositions comprising compounds, and methods for methods for preparing and using compounds are described herein. Methods of treating or ameliorating various conditions, including insulin resistance, pancreatic beta cell apoptosis, obesity, pro-thrombotic conditions, myocardial infarction, hypertension, dyslipidemia, manifestations of Syndrome X, congestive heart failure, inflammatory disease of the cardiovascular system, atherosclerosis, sepsis, type 1 diabetes, liver damage, and cachexia, by administering compounds described herein. Compounds presented herein may be used to modulate serine palmitoyl transferase activity.

Abstract: Novel compounds, compositions comprising compounds, and methods for preparing and using compounds are described herein. Methods of treating or ameliorating various conditions, including insulin resistance, pancreatic beta cell apoptosis, obesity, pro-thrombotic conditions, myocardial infarction, hypertension, dyslipidemia, manifestations of Syndrome X, congestive heart failure, inflammatory disease of the cardiovascular system, atherosclerosis, restenosis, sepsis, type 1 diabetes, liver damage, and cachexia, by administering compounds described herein. Compounds presented herein may be used to modulate serine palmitoyltransferase activity.

Abstract: The invention relates to methods of synthesizing 2-substituted azole compunds of formula (I): The invention is also relates to compounds of formula (I) and to intermediate compounds in the synthesis method.

Abstract: Urea derivatives of formula I are disclosed: The compounds are inhibitors of ?-secretase, and hence useful in the treatment or prevention of Alzheimer's Disease

Abstract: ACE-2 inhibitors for the treatment of body weight and related disorders are disclosed. ACE-2 inhibitors include peptides and small molecules. Examples of small molecule ACE-2 inhibitors include compounds of formula (I): Z-???(I) Wherein Z is a zinc coordinating moiety and ? is an amino-acid mimicking moiety, and pharmaceutically acceptabale salts thereof. Methods of using the inhibitors and pharmaceutical compositions containing the inhibitors to treat a body weight disorder, to decrease appetite, to increase muscle mass, to decrease body fat, to treat diabetes and to treat a state associated with altered lipid metabolism, are also described.

Abstract: The present invention provides a process for efficiently producing an optically active ?-amino acid and an optically active ?-amino acid amide. After contacting with cells or processed cells thereof having an ability to asymmetrically hydrolyse, a water solvent is substituted with at least one solvent selected from the group consisting of linear, branched, or cyclic alcohol having 3 or more carbon atoms and the optically active ?-amino acid is preferentially precipitated from the alcohol solution. The addition of basic compounds, particularly potassium compounds to the alcohol solution containing the optically active ?-amino acid amide, which is obtained after the separation of the optically active ?-amino acid, enables the purification of the amide without the inclusion of amino acid into amino acid amide. Thus, the amide is subjected to the step of racemization and then recycled.

Abstract: ?-alaninamides of the general formula Wherein R1 is hydrogen or C1-6 alkyl which is unsubstituted or substituted with hyroxy, amino, carboxy, carbamoyl, methylmercapto, guanidino, unsubstituted or substituted aryl or heteroaryl, and R2 is hydrogen, or R1 and R2 together form a group of the formula —(CH2)n— where n is 3 or 4, and R3 is hydrogen, a negative charge compensated by an equivalent of an inorganic or organic cation or is C1-6 alkyl, are prepared, without using an amino-protective group, by reacting the corresponding ?-amino acid or the corresponding ?-amino acid ester with a cyanoacetic ester to give a cyanoacetamide and by subsequent catalytic hydrogenation. The method is particularly suitable for preparing carnosine (?-alanyl-L-histidine, R1=imidazol-4-yl-methyl, R2=R3=H), a naturally occurring dipeptide which used as a dietary supplement with antioxidative action.

Abstract: This invention relates to a novel use of cationic preservatives and preparations according to this novel use. A cationic preservative derived from lauric acid and arginine, in particular, the ethyl ester of the lauramide of the arginine monohydrochloride, hereafter named LAE, can be used for the protection against the growth of microorganisms. The chemical structure of LAE is described in formula (I). LAE and related compounds are particularly suitable to be used in the preservation of all perishable food products. It is preferred to dissolve the compound directly before use in one of the following preferred solvents of food grade: water, ethanol, propylene glycol, isopropyl alcohol, other glycols, mixtures of glycols and mixtures of glycols and water. If the treatment shall be performed at a specific pH value the use of a corresponding buffer solution may be recommendable. The composition optionally comprises auxiliary components and excipients.

Abstract: Process for the separation of enantiomers comprising at least one free functional group, in which process a reagent based on an enantiopure amino acid is reacted in basic medium with a mixture comprising enantiomers.

Abstract: The invention concerns novel derivatives of 3,3-diphenylpropylamines, methods for their preparation, pharmaceutical compositions containing the novel compounds, and the use of the compounds for preparing drugs. More particularly, the invention relates to novel prodrugs of antimuscarinic agents with superior pharmacokinetic properties compared to existing drugs such as oxybutynin and tolterodine, methods for their preparation, pharmaceutical compositions containing them, a method of using said compouds and compositions for the treatment of urinary incontinence, gastrointestinal hyperactivity (irritable bowel syndrome) and other smooth muscle contractile conditions.

Abstract: A method for inhibiting and/or ameliorating the occurrence of diseases associated with reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals in a subject whereby a subject is administered a carotenoid structural analog, either alone or in combination with another carotenoid analog, or co-antioxidant formulation. The analog or analog combination is administered such that the subject's risk of experiencing diseases associated with reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals may be thereby reduced. The analog or analog combination may be administered to a subject for the inhibition and/or amelioration of ischemia-reperfusion injury. The analog or analog combination may be administered to a subject for the inhibition and/or amelioration of liver disease. The analog or analog combination may be administered to a subject for the inhibition and/or amelioration of cancer.