Abstract: The present invention provides zinc complexes for use in methods of providing zinc to subjects in need of treatment. The invention further provides improved dietary supplement formulations for improving and maintaining ocular nutrition. In particular, the improved dietary supplement formulations comprise the zinc complexes described herein, antioxidant vitamins, minerals and excipients.

Abstract: The present invention relates to a compound of formula (I) AA-AA-AA-X—Y—Z wherein, in any order, 2 of said AA (amino acid) moieties are cationic amino acids and 1 of said AA is an amino acid with a lipophilic R group, the R group having 14-27 non-hydrogen atoms; X is a N atom, which may be substituted by a branched or unbranched C1-C10 alkyl or aryl group which group may incorporate up to 2 heteroatoms selected from N, O and S; Y represents a group selected from —Ra—Rb—, —Ra—Rb—Rb— and —Rb—Rb—Ra— wherein Ra is C, O, S or N, and Rb is C; each of Ra and Rb may be substituted by C1-C4 alkyl groups or unsubstituted; and Z is a group comprising 1 to 3 cyclic groups each of 5 or 6 non-hydrogen atoms, 2 or more of the cyclic groups may be fused and one or more of the cyclic groups may be substituted; the Z moiety incorporates a maximum of 15 non-hydrogen atoms; and wherein the bond between Y and Z is a covalent bond between Ra or Rb of Y and a non-hydrogen atom of one of the cyclic groups of Z.

Abstract: To provide ACE inhibitory peptides which can effectively inhibit ACE by a small amount of ingestion and have no fear of causing side effects and which can be orally ingested easily during daily life by persons having high blood pressure, and compositions comprising the peptides. The peptides represented by the following structural formulae (1) to (9), and salts thereof are provided.

Abstract: The present invention provides an anti-hypertensive agent. The anti-hypertensive agent of the present invention contains, as an active ingredient, at least one peptide selected from the group consisting of peptides originally derived from globin proteolysate, each of which consists of one of the following amino acid sequences (1) to (6), or a globin proteolysate containing at least one of the peptides: (1) Val-Val-Tyr-Pro (SEQ ID: NO. 1); (2) Trp-Gly-Lys-Val-Asn (SEQ ID: NO. 2); (3) Trp-Gly-Lys-Val (SEQ ID: NO. 3); (4) Trp-Gly-Lys (SEQ ID: NO. 4); (5) Ala-Ala-Trp-Gly-Lys (SEQ ID: NO. 5); and (6) Phe-Glu-Ser (SEQ ID: NO. 6).

Abstract: A nanoparticle conjugate comprising a nanoparticle having one or more peptide-ol compounds and one or more polyethylene glycol (PEG) compounds attached thereto. A method of producing the nanoparticle conjugate is also described.

Abstract: The invention provides peptides that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the peptide not attached to the water-soluble oligomer.

Abstract: The present invention describes a protein hydrolysate which is rich in tripeptides whereby the tripeptides are rich in proline at one end of the peptide.

Abstract: A new class of neuramidase inhibitor prodrugs is provided characterized by a prodrug moiety of a carboxyl group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide or a carbonyl ethoxy tripeptide, a guanidine group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide, a carbonyl ethoxy tripeptide; a primary alcohol modified to form an esterified single amino acid, dipeptide or tripeptide of zanavimir of the unaltered therapeutic agent. Exemplary therapeutic agents so modified to form prodrugs include zanavimir, oseltamivir and peramivir. The prodrug has increased oral bioavailability relative to the unaltered neuraminidase inhibitor and is effective in the inhibition of viral infections involving neuraminidase in the viral reproductive cycle.

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: The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

Abstract: Described herein are a class of metal oligomers and polymers that contain both metals and organic groups. Said oligomers and polymers have utility in many applications including biomedical imaging, radiation therapy, drug delivery, and in vitro analytical techniques, such as fluorescence and phosphorescence.

Abstract: The present invention discloses compounds of formula Ia or Ib or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Abstract: The invention provides compounds and methods, for example, to carry out organocatalytic Michael additions of aldehydes to cyclically constrained nitroethylene compounds catalyzed by a proline derivative to provide cyclically constrained ?-substituted-?-nitro-aldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96 to >99% e.e.). The Michael adducts can bear a single substituent or dual substituents adjacent to the carbonyl. The Michael adducts can be efficiently converted to cyclically constrained protected ?-amino acid residues, which are essential for systematic conformational studies of ?-peptide foldamers. New methods are also provided to prepare other ?-amino acids and peptides. These new building blocks can be used to prepare foldamers, such as ?/?-peptide foldamers, that adopt specific helical conformations in solution and in the solid state.

Abstract: The present application discloses angiogenic peptides that cause intracellular calcium release in target cells and thereby induce proliferation, migration, and capillary-like tube formation in primary cultured endothelial cells. The angiogenic peptides can be used for preventing and/or treating angiognesis-related conditions, especially wound healing, treating foot and leg ulcers in a subject, etc. In addition, the angiogenic peptides can be used for cosmetics a constituent of cosmetics for aged skin, for examples, anti-wrinkle and skin whitening.

Abstract: The invention relates to the modulation of gene expression in a cell, also called gene control, in particular in relation to the treatment of a variety of diseases. The invention provides a method for modulating expression of a gene in a cell comprising providing the cell with a signalling molecule comprising a peptide or functional analogue thereof. Furthermore, the invention provides a method for identifying or obtaining a signalling molecule comprising a peptide or functional derivative or analogue thereof capable of modulating expression of a gene in a cell comprising providing the cell with a peptide or derivative or analogue thereof and determining the activity and/or nuclear translocation of a gene transcription factor.

Abstract: The present invention provides compositions and methods for imaging tumor resections.

Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (GRLN, growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and/or variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as antagonists or inverse agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, obesity and obesity-associated disorders, appetite or eating disorders, addictive disorders, cardiovascular disorders, gastrointestinal disorders, genetic disorders, hyperproliferative disorders, central nervous system disorders and inflammatory disorders.

Abstract: The invention relates to methods for identifying compounds which modulate the interaction between STAT3 an SP1. A peptide is provided which is able to bind STAT3 and interfere with the interaction of STAT3 and SP1. The invention provides methods for identifying compounds which are capable of binding to the peptide and thus release interference with the interaction between STAT3 and SP1, as well as methods for identifying inhibitors and enhancers of the STAT3 SP1 interaction. Compounds identified by the methods of the invention are useful in the repression or stimulation of appetite in a patient, useful for the treatment of leptin resistance, obesity and anorexia.

Abstract: The present invention provides a method of improving the oral delivery of a parent peptide, comprising the step of linking the parent peptide to an added peptide to form a conjugate which has greater oral bioavailability than the parent molecule alone, the added peptide comprising a balance of hydrophobic and hydrophilic residues as defined herein. Conjugates for use in the method are also provided, as are pharmaceutical compositions comprising the conjugate and methods of treatment using the conjugate or pharmaceutical composition.

Abstract: The present invention provides a peptide and a composition which are suitable for oral ingestion, and which have a skin aging-inhibiting activity, a collagen-production promoting activity, an epidermal turnover promoting activity, and a cutaneous cell-proliferating effect. The present invention also provides a medicament and a functional food which have a skin aging-inhibiting activity, a collagen-production promoting activity, and a cutaneous cell-proliferation promoting activity. The present invention provides a composition including at least one peptide of Asn-Ile-Pro-Pro-Leu, Ile-Pro-Pro-Leu, Ile-Pro-Pro, Pro-Val-Val-Val-Pro-Pro, Val-Pro-Pro-Phe, Val-Pro-Pro, Phe-Pro-Pro-Gln, and Leu-Pro-Pro-Thr.

Abstract: A process for the manufacture of peptide Omiganan in solution phase. Novel intermediates in the process for the manufacture of Omiganan and processes for the manufacture of these intermediates.

Abstract: The subject of the present invention is to provide a fluorescent substance excitable under visible light, having higher photostability and a long fluorescence lifetime. Another subject is to provide a fluorescent substance consists of a non-natural amino acid applicable to peptide synthesis systems. Searching fluorescent substances, which are fluorescent amino acids and excitable under visible light, having the lowest possible molecular weight for a high photostability resulted in forming a condensed polycyclic aromatic compound by subjecting a compound having an acridone structure to substitution with an amino acid and further condensation with a benzene ring. Thus, the subject is achieved by the fluorescent substance consisting of amino acid-substituted benzoacridone derivative excitable under visible light.

Abstract: Conjugates of hydroxypropyl methacrylamide (HPMA)-derived copolymers having attached thereto TNP-470 and a high load (e.g., higher than 3 mol %) of alendronate (ALN), and processes of preparing same are disclosed. Conjugates of polymers or copolymers having attached thereto an anti-angiogenesis agent and an oligoaspartate bone targeting agent, and processes of preparing same, are further disclosed. Pharmaceutical compositions containing these conjugates and uses thereof in the treatment and monitoring of bone related disorders are also disclosed.

Abstract: Disclosed are compositions and methods related to clot-binding head groups. The disclosed targeting is useful for treatment of cancer and other diseases and disorders.

Abstract: The present invention relates to a casein hydrolysate containing free amino acids and in vivo indigestible peptides having minimally suppressed in vivo enzymatic digestibility, and expected to express functions, such as hypotensive effect, in living organism, and to a method for preparing such a hydrolysate, and use thereof. The casein hydrolysate of the present invention contains free amino acids and peptides, such as in vivo indigestible peptides including Xaa-Pro and Xaa-Pro-Pro, obtained by hydrolyzing animal milk casein to have an average chain length of not longer than 2.1 in terms of the number of amino acid residues, and has ACE inhibitory activity or hypotensive effect.

Abstract: Processes using Allium tissue homogenates and extracts in a simple and cost-effective manner to maximize the yields and recovery of thiosulfinates from Allium tissues and related organisms possessing alliinase, LF synthase and/or S-alk(en)yl-L-cysteine sulfoxides are disclosed.

Abstract: Compounds of the following general formula (I): are provided. The compounds can be used as modulators of the proteasome activity, in the preparation of a medicament useful for the prevention or treatment of diseases wherein the proteasome is involved, such as diseases of inflammatory processes, various hematological and solid tumor cancers, immunological and autoimmune diseases, cardiac pathologies, myopathies, AIDS, cystic fibrosis, Alzheimer's and Parkinson's disease, or in the preparation of cosmetic compositions or phytosanitary compositions.

Abstract: The present invention provides compound having the general structure A or pharmaceutically acceptable salts thereof: Het-L-P??(A) wherein Het is an aromatic moiety comprising a heterocyclic structure mimicking ATP, P is a docking site derived peptide or a docking site peptide mimetic, and L is a linking moiety, wherein L links the ATP mimetic to the docking site peptide moiety. The compounds having the general structure A can serve as inhibitors of kinases, such as the kinases JNK, Erk and p38.

Abstract: The present invention relates to compounds of Formula I, IA, II, HA, III, or IHA and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more caspases. Also described are methods where the compounds of Formula I, IA, II, IIA, III, or IIIA are used in the prevention and/or treatment of various diseases and conditions in subjects, including caspase-mediated diseases such as sepsis, myocardial infarction, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative disease (e.g. multiple sclerosis (MS) and Alzheimer's, Parkinson's, and Huntington's diseases).

Abstract: Sulfur-containing ligands and methods of their utilization for binding metals and/or main group elements and removing them from fluids, solids, gases and/or tissues are disclosed.

Abstract: A method and medical composition for the treatment and/or prevention of a functional Vitamin B12 deficiency in an individual that is brought about as a consequence of oxidative stress on biochemical pathways. The functional Vitamin B12 deficiency may eventually present as dementia, other neuropsychiatric abnormality and/or vascular disease. The method involves the administration of a medical composition that supplies a cobalt-sulphur bond in the upper ?-ligand of an intracellular cobalamin molecule thereby facilitating intracellular processing of cobalamin. The cobalt-sulphur bond may he provided directly by administration of a thiolatocohalamin, such as glutathianyl-cobalamin or indirectly by the co-administration of Vitamin B12 (or a derivative thereof) with a sulphur-containing molecule, such as glutathione or a precursor thereof.

Abstract: A novel class of antimicrobial polymeric agents, which include a plurality of amino acid residues, such as positively charged amino acid residues, and at least one hydrophobic residue linking therebetween, such as an omega-amino-fatty acid residue, 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: The present invention provides a method of preparing an intermediate for LHRH antagonists, which requires fewer steps than conventional methods and provides the intermediate in high yield and high purity.

Abstract: The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein R1 represents a —CO—(CH2)n—COR2 group (wherein n is an integer of 1 to 4, and R2 is (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxo-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.

Abstract: The invention provides 4-amino-4-oxobutanoyl peptide compounds of Formula I and the pharmaceutically salts and hydrates thereof. The variables R1-R9, R16, R18, R19, n, M, n, M, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain 4-amino-4-oxobutanoyl peptide compounds disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptide compounds and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain 4-amino-4-oxobutanoyl peptide compound as the only active agent or may contain a combination of 4-amino-4-oxobutanoyl peptide containing peptides compound and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in mammals.

Abstract: A method of treating a patient for a condition wherein the bioactive agent of choice is DRUG, wherein DRUG is a substrate that is effluxed by the P-gp transporter, is provided, the method comprising administering to the patient an effective amount of a compound of formula (I): DRUG-X—Y(n)—Z(n?)—Z?(n?)—R??(I) wherein each X, Y, Z, and Z? is independently Met, Val, Thr, Tyr, Trp, Ser, Ala, or Gly; R is H or an amino-protecting group; n is 1, and each n?, or n? is independently 0 or 1; or a pharmaceutically acceptable salt thereof, with the proviso that DRUG is not acyclovir or ganciclovir and that DRUG is non-peptidyl.

Abstract: The invention provides monomeric and oligomeric amyloid beta peptide isomers that are resistant towards fibrillogenesis and their use as screening reagents or antigens in methods and pharmaceutical preparations for the treatment of Alzheimer's disease and other conditions related to protein misfolding. The alanines at positions 21 and 30, in wild type amyloid beta peptide amino acid sequence, are according to the invention replaced by cysteins, which results in an intra molecular disulphide bond. The invention further provides transgenic animals expressing modified amyloid precursor proteins or amyloid beta peptides.

Abstract: The invention provides 4-amino-4-oxobutanoyl peptide compounds of Formula I and the pharmaceutically salts and hydrates thereof. The variables R1-R9, R16, R18, R19, n, M, n, M, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain 4-amino-4-oxobutanoyl peptide compounds disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptide compounds and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain 4-amino-4-oxobutanoyl peptide compound as the only active agent or may contain a combination of 4-amino-4-oxobutanoyl peptide containing peptides compound and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in mammals.

Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.

Abstract: The present invention relates to a peptide for the treatment or prophylaxis of an autoimmune disease, a nucleic acid molecule coding for said peptide, a pharmaceutical composition comprising the peptide and/or the nucleic acid molecule, and to a method for the treatment and/or prophylaxis of an autoimmune disease.

Abstract: The present invention provides a mineral-peptide chelate comprising a peptide consisting of 2˜18 amino acids and a mineral chelated to the peptide, wherein the peptide can be a hydrolysate obtained by hydrolyzing soybean or other protein materials with proteases, or a product obtained by hydrolyzing soybean or other protein material with proteases and fermentation. The mineral-peptide chelate of the present invention may further comprise a carrier which covers the peptide and the mineral which is chelated to the peptide.

Abstract: The present invention is directed to an inventive polymeric carrier molecule according to generic formula (I) and variations thereof, which allows for efficient transfection of nucleic acids into cells in vivo and in vitro, a polymeric carrier cargo complex formed by a nucleic acid and the inventive polymeric carrier molecule, but also methods of preparation of this inventive polymeric carrier molecule and of the inventive polymeric carrier complex. The present invention also provides methods of application and use of this inventive polymeric carrier and the inventive polymeric carrier cargo complex as a medicament, for the treatment of various diseases, and in the preparation of a pharmaceutical composition for the treatment such diseases.

Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula (I), and G, X1, X2, R1, R2, R3, R4, R4?, R5, Ra, Rb, and Rc are as described herein.

Abstract: The present invention relates to a multi-conjugate of small interfering RNA (siRNA) and a preparing method of the same, more precisely a multi-conjugate of siRNA prepared by direct binding of double stranded sense/antisense siRNA monomers or indirect covalent bonding mediated by a cross-linking agent or a polymer, and a preparing method of the same. The preparing method of a siRNA multi-conjugate of the present invention is characterized by simple and efficient reaction and thereby the prepared siRNA multi-conjugate of the present invention has high molecular weight multiple times the conventional siRNA, so that it has high negative charge density, suggesting that it has excellent ionic interaction with a cationic gene carrier and high gene delivery efficiency.

Abstract: An immunopeptide containing a T cell epitope from the tumor associated antigen L6 (TAL6) and a nucleic acid encoding the immunopeptide. The immunopeptide and its encoding nucleic acid can be used as a component of an immune composition for enhancing immune response against cancer cells that express TAL6.

Abstract: A method of making a fluorogenic peptide with an acridone fluorophor is provided, the method comprising the steps of: (a) providing an acridone derivative, said acridone derivative having first and second reactive groups (or precursors thereof), (b) providing a solid phase support provided with reactive species for reacting with the first reactive group of the acridone derivative (c) causing the solid phase support and acridone derivative to react so that the acridone derivative is attached to the solid phase support (d) providing the peptide or reagents for the formation of the peptide, and (e) subsequent to step (c), causing the reaction of the second acridone reactive group with the peptide or one or more of the reagents for the formation of the peptide.

Abstract: The invention relates to pharmaceutical compounds and compositions comprised of a chemical moiety attached to oxycodone in a manner that substantially decreases the potential for overdose. When delivered at the proper dosage the pharmaceutical composition provides therapeutic activity similar to that of oxycodone and may also provide sustained release characteristics and/or reduced side-effects. Further the compounds and compositions of the invention are useful in preventing addiction and susceptibility to addiction of oxycodone.

Abstract: Peptide aldehydes or ketone derivatives are particularly efficient for stabilizing subtilisin-type proteases in aqueous compositions such as liquid detergents, including peptide compounds with OH-substituted phenylalanine aldehyde as the C-terminal residue.