Abstract: The present invention provides compositions and methods for protecting cells and tissues from damage associated with therapeutic treatments of cancers and other diseases and conditions where reactive oxygen species are produced. The present invention also provides compositions useful as research reagents.

Abstract: Lysine mimetic compounds having useful pharmacological activity such as antiarrhythmic activity and desirable bioavailability properties are disclosed.

Abstract: A method of supplementing a diet and ameliorating oxidative stress in a mammal includes administering a pharmaceutically effective amount of lipid soluble, hydrophobic active compounds having a chemical structure: wherein R1 is an aromatic backbone and R2 is a sulfur containing ligand. Through formation of disulfide linkages other moieties can be attached to R2 converting the hydrophobic base into a water soluble entity, for ease of delivery, which can be reconverted back to the original compound by biochemical reduction in the blood stream.

Abstract: The present invention is directed to a dietary supplement comprising palatinose or a derivative thereof. The dietary supplement may be a nutritional product, a sports performance product, a weight loss product or a meal replacement product. The present invention is also directed to a method of increasing the absorption of a compound into the bloodstream, cells and tissue comprising administering palatinose, or a derivative thereof, in combination with the compound.

Abstract: Disclosed is a protein hydrolysate having DPP-IV inhibiting activity, the hydrolysate being enriched in peptides having a length of 2-8 amino acids comprising at least one proline residue, an isolated peptide derivable from such a protein hydrolysate, or a mixture thereof, and the use of such protein hydrolysate or isolated peptide for the manufacture of a medicament, food supplement, beverage or food product for prophylaxis and/or treatment of a DPP-IV mediated condition, in particular chosen from the group of obesity, type 2 diabetes mellitus and an immunological disorder.

Abstract: A problem that the present invention is to solve is to provide: a main body of a peptide molecule which is effective for inhibition of various maladies such as osteoporosis, osteoarthritis and pressure ulcer, particularly, a dipeptide which is easy to absorb into a body in an intestine; a collagen peptide which comprises the dipeptide as an essential dipeptide; and a malady inhibitor which comprises the dipeptide as an essential effective component. As a means of solving such a problem, a collagen peptide according to the present invention is characterized by comprising a dipeptide having a structure of Hyp-Gly as an essential dipeptide. A dipeptide according to the present invention is characterized by having a structure of Hyp-Gly. A malady inhibitor according to the present invention is characterized by comprising a dipeptide having a structure of Hyp-Gly as an essential effective component.

Abstract: Disclosed herein are opioid peptide conjugates (for example, opioid peptide esters). In some embodiments, the disclosed conjugates include an opioid peptide consisting of two to six amino acids and a moiety conjugated to the opioid peptide by an ester bond. In some examples, the moiety is an alcohol, a sugar, a lipid, or dehydroascorbic acid. Also disclosed are methods of altering nociception including administering an effective amount of one or more disclosed opioid peptide conjugates to a subject (such as a human subject).

Abstract: The present disclosure provides drug-ligand conjugates that are potent cytotoxins, wherein the drug is linked to the ligand through either a peptidyl, hydrazine, or disulfide linker. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.

Abstract: The invention provides a cationic lipid comprising: (i) one head group, comprising one or more amino acids, in which at least one amino acid has a side chain that comprises a cationic moiety or a cationic precursor; (ii) a linking moiety of formula (5): —(HNR5)2NC(O)R3C(O)—??(5), wherein: each R5 is independently an optionally substituted C1-4 alkylene moiety; and R3 is an optionally substituted alkylene or alkenylene moiety; and (iii) two lipophilic moieties, wherein the head group and each of the lipophilic moieties are connected to the linking moiety through amide linkages.

Abstract: Pyrrolobenzodiazepine dimers I having a C2-C3 double bond and an aryl group at the C2 position on one monomer unit, and a C2-C3 double bond and either a conjugated double or triple bond at the C2 position or an alkyl group at the C2 position on the other monomer unit, and conjugates of these compounds.

Abstract: The disclosure provides compositions and methods relating to aromatic-cationic peptides. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to subjects in need thereof. For example, the peptides may be administered to subjects in need of a mitochondrial-targeted antioxidant.

Abstract: A composition for promoting lacrimal secretion which can be used safely and effectively in the lacrimal secretion promoting therapy, not in the conventional supplemental therapy of lacrimal fluid components is provided. The composition for promoting lacrimal secretion comprising a peptide derivative represented by the formula (I): and a contact lens which retains and/or contains the composition are provided.

Abstract: The present invention relates to crystalline forms of the mono-sodium salt of D-isoglutamyl-D-tryptophan, pharmaceutical compositions comprising them, their use in the treatment of various diseases and conditions, and processes for their preparation. In particular, the present invention relates the crystal modification 2 (polymorphic form I) of the mono-sodium salt of D-isoglutamyl-D-tryptophan.

Abstract: The present invention relates to crystalline forms of the mono-sodium salt of D-isoglutamyl-D-tryptophan, pharmaceutical compositions comprising them, their use in the treatment of various diseases and conditions, and processes for their preparation. In particular, the present invention relates the crystal modification 1 (polymorphic form F) of the mono-sodium salt of D-isoglutamyl-D-tryptophan.

Abstract: The present invention relates to an amino acid solution for the parenteral nutrition of pediatric patients. The amino acid solution provides for an increased concentration of glutamine, tyrosine, cysteine and taurine, while the concentrations of phenylalanine and methionine is small. Glutamine and tyrosine are provided in the form of oligopeptides.

Abstract: The invention relates to novel cell-binding agent-cytotoxic agent conjugate having a peptide linkers and more specifically to conjugates of formula (I). The invention also provides novel cytotoxic agents of formula (II), linker compounds represented by formula (III), and drug-linker compounds represented by formula (IV). The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

Abstract: Disclosed herein are tablets comprising ezatiostat hydrochloride wherein the ezatiostat hydrochloride comprises from about 75 to about 82 percent by weight of the tablet.

Abstract: The present invention is directed in particular to dipeptide-like compounds derived from functionally substituted amino acids, having fatty acid chains bound thereto through amidification of the amine functional groups of said dipeptide-like compounds, one end portion of which bears an accessory functional side chain spacer, with the other end portion being an acid group either in neutral or charged state. Compounds of the present invention have immunomodulating properties like adjuvants. In addition, compounds of the invention can be grafted on a given antigen in order to modulate or tune the immune response or can be equally grafted on a pharmaceutical carrier to enhance the therapeutic effect or targeting thereof. Accordingly, compounds of the invention find use in human and veterinary medicine both as immunogens and diagnostic tools.

Abstract: The present invention is directed to a compound of the formula: or pharmaceutically acceptable salts thereof and use of such compounds for treating proliferative diseases such as cancer, in mammals.

Abstract: The invention provides a composition used for promoting glucose uptake, which comprises a peptide having an effect of promoting glucose uptake as the active ingredient, as well as a composition comprising a dipeptide containing leucine and/or isoleucine as the active ingredient. The composition is effective in preventing or treating diabetes mellitus or an elevation of blood glucose level, in promoting glycogen storage, or in enhancing physical strength, enhancing athletic ability, improving endurance performance or relieving fatigue.

Abstract: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as opioid agonists.

Abstract: The present invention is directed to the use of a class of peptide compounds for treating pain in trigeminal neuralgia.

Abstract: Embodiments of the invention disclosed herein relate to compositions comprising carnosine and N-acetyl-histitidine in a pharmaceutically acceptable carrier. Other embodiments disclosed herein relate to preventing and/or ameliorating one or more symptoms associated with an eye disease such as dry eye syndrome, cataracts of the eye and nuclear sclerosis of the eye lens. Kits for preventing and/or ameliorating one or more symptoms associated with an eye disease by administering a pharmaceutical composition comprising N-acetyl-histidine are also disclosed.

Abstract: Disclosed are compressed tablets containing atazanavir sulfate, optionally with another active agents, e.g., anti-HIV agents, granules that contain atazanavir sulfate and an intragranular lubricant that can be used to make the tablets, compositions comprising a plurality of the granules, processes for making the granules and tablets, and methods of treating HIV.

Abstract: A composition and treatment method are disclosed for one or more of alpha, beta, and gamma-Cyclodextrin and a natural molecule or fragment thereof wherein the natural molecule is sometimes Glutathione, is non-acetylated, non-Esterified, and non-fatty acid attached, and the composition is administered parenterally and non-interveneously.

Abstract: The invention provides methods for treating muscle loss in an individual. In one embodiment, the invention includes administering to an individual an effective amount of a branched chain amino acid (BCAA), a BCAA precursor, a BCAA metabolite, a BCAA-rich protein, a protein manipulated to enrich the BCAA content or any combination thereof. The invention further provides nutritional products for such administration, including orally-administrable nutritional products.

Abstract: This invention describes an ICE inhibitor prodrug (I) having good bioavailability. Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.

Abstract: The invention relates to compounds, in particular MMP inhibitors. The compounds of the invention have formula (1). The invention can be used in particular in the pharmaceutical field. The present invention also relates to labeled compounds of formula (2), and to the use thereof as contrast agents for detecting extracellular matrix metalloproteinases.

Abstract: Compounds of Formula II wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10 alkyl chain, C2-C4haloalkyl or —CH2C3-C7 cycloalkyl; R4? is C1-C6alkyl, C1-C6haloalkyl or oxetany-3-yl. for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.

Abstract: The present invention discloses compounds of formula I and II 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: A composition comprising a material at least partially enclosed by a tubular, spherical or planar nanostructure composed of a plurality of peptides, wherein each of the plurality of peptides includes no more than 4 amino acids and whereas at least one of the 4 amino acids is an aromatic amino acid.

Abstract: It is an object of the present invention to provide improved pharmacological properties to molecules which bind to a target with low affinity (hereinafter referred to as a “ligand moiety”) through linkage of such molecules to a metal binding moiety, thereby generating a combination molecule commonly referred to as a “metallodrug” or “metallotherapeutic.” The metal binding domain of metallodrugs typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, resulting in modification of proteins and nucleic acids that are in close proximity due to binding of the ligand moiety to its target.

Abstract: The invention relates to compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 as defined herein. The invention also relates to pharmaceutical compositions and methods of treating bacterial infections using compounds of formula (I).

Abstract: Compounds based around tetrapeptide, tripeptide and dipeptide moeties and corresponding peptiod moeties. Related methods and pharmaceutical compositions for use in treatment of cancer, inflammatory diseases, and other disorders.

Abstract: A substance capable of imparting a kokumi having CaSR agonist activity is described. This substance is able to impart kokumi in a superior manner, in particular, at the initial taste, and is also highly stable and can easily be produced at a low cost. The present invention thus provides a kokumi-imparting composition which includes such a substance as well as a complex kokumi-imparting composition which includes the substance and other substances possessing the CaSR agonist activities in combination. More particularly, the present invention herein provides a kokumi-imparting composition including ?-Glu-Nva (L-?-glutamyl-L-norvaline), and a complex kokumi-imparting composition including the foregoing substance and another substance having a CaSR agonist activity, in combination.

Abstract: The present invention relates to the field of protein misfolding diseases and thus to diseases which are associated with or induced by abnormal or pathogenic three-dimensional folding of proteins and/or peptides or which are linked to pathogenic conformational changes of proteins and/or peptides, such as Alzheimer's disease. Particularly, the present invention provides novel trimeric pyrazole compounds, which exhibit a therapeutic effectiveness in regard to the aforementioned protein misfolding diseases, and refers to their use for the treatment of such protein misfolding diseases, especially neurodegenerative diseases as well as to medicaments or pharmaceutical compositions comprising these compounds.

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: A problem that the present invention is to solve is to provide: a main body of a peptide molecule which is effective for inhibition of various maladies such as osteoporosis, osteoarthritis and pressure ulcer, particularly, a dipeptide which is easy to absorb into a body in an intestine; a collagen peptide which comprises the dipeptide as an essential dipeptide; and a malady inhibitor which comprises the dipeptide as an essential effective component. As a means of solving such a problem, a collagen peptide according to the present invention is characterized by comprising a dipeptide having a structure of Hyp-Gly as an essential dipeptide. A dipeptide according to the present invention is characterized by having a structure of Hyp-Gly. A malady inhibitor according to the present invention is characterized by comprising a dipeptide having a structure of Hyp-Gly as an essential effective component.

Abstract: The invention provides methods of making and using compounds of the formula: or a pharmaceutically acceptable salt thereof; wherein n is an integer between 1 and 2 inclusively; m is an integer between 0 and 2 inclusively; X is selected from the group consisting of CH or N; R1 is selected from the group consisting of —CH2NH2, and R2 is selected from the group consisting of —H, —OH, —NH2 and acetyl; R3 is selected from the group consisting of —H, benzyloxycarbonyl and benzylsulfonyl; and R4 is selected from the group consisting of —OH, wherein p is an integer between 0 and 2 inclusively, Y is selected from the group consisting of —O—, —S—, —S(?O)—, —SO2—, methylene, —CH(OH)—, —CH(NH2)—, —CH(CH2—OH)—, —CH(CH2—NH2)— or —N(R6)—, R5 is selected from the group consisting of —H or a simple (C1-C3) alkyl and R6 is selected from the group consisting of —H, a simple (C1-C3) alkyl or a simple (C1-C3) acyl.

Abstract: Lysine mimetic compounds having useful pharmacological activity such as antiarrhythmic activity and desirable bioavailability properties are disclosed.

Abstract: The present disclosure generally relates to crystalline forms of N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-((7-chloro-4-methoxy-1-isoquinolinyl)oxy)-N-((1R,2S)-1-((cyclopropylsulfonyl)carbamoyl)-2-vinylcyclopropyl)-L-prolinamide. The present disclosure also generally relates to a pharmaceutical composition comprising one or more of the crystalline forms, as well of methods of using the crystalline forms in the treatment of Hepatitis C virus (HCV) and methods for obtaining such crystalline forms.

Abstract: Compounds of formula (I) or formula (II) have dopaminergic activity: wherein: R1 is a carboxyl, carboxyl ester, or carboxamide group; R2 is a group —C(?O)—NR3R4, or —S(?O)2—NR3R4; R3 and R4 are independently selected from hydrogen, optionally substituted C1-C6 alkyl, (C1-C5 fluoroalkyl)-CH2—, -Q, and —CH2Q, wherein Q is an optionally substituted monocyclic carbocyclic or heterocyclic ring of (3) to (6) ring atoms; or R3 and R4 together with the nitrogen to which they are attached form an optionally substituted monocyclic cycloalkyl or non-aromatic heterocyclic ring of (3) to (8) ring atoms; R5 is hydrogen, or a natural or non-natural alpha amino acid residue linked via a peptide bond; R6 is hydrogen or a group R7C(?O)—; and R7 is C1-C6 alkyl, C1-C6 fluoroalkyl or cyclopropyl.

Abstract: The present invention provides a new prodrug technology and new prodrugs in order to increase the solubility, to modulate plasma protein binding or to enhance the biovailability of a drug. In the present invention the prodrugs are conjugates of a therapeutic compound and a peptide (eg tetrapeptide or hexapeptide) wherein the conjugate is cleavable by dipeptidyl-peptidases, more preferably by CD26, also known as DPPIV (dipeptidyl aminodipeptidase IV). The present invention furthermore provides a method of producing the prodrugs, to enhance brain and lymphatic delivery of drugs and/or to extend drug half-lives in plasma.

Abstract: A method to predict which patients will respond to a IAP inhibiting compound comprising administering an IAP inhibitor compound to a patient/and measuring IL1B, Lymphotoxin alpha (LTa), TWEAK, LIGHT, Fas, TNF alpha or TRAIL levels.

Abstract: A problem that the present invention is to solve is to provide: a main body of a peptide molecule which is effective for inhibition of various maladies such as osteoporosis, osteoarthritis and pressure ulcer, particularly, a dipeptide which is easy to absorb into a body in an intestine; a collagen peptide which comprises the dipeptide as an essential dipeptide; and a malady inhibitor which comprises the dipeptide as an essential effective component. As a means of solving such a problem, a collagen peptide according to the present invention is characterized by comprising a dipeptide having a structure of Hyp-Gly as an essential dipeptide. A dipeptide according to the present invention is characterized by having a structure of Hyp-Gly. A malady inhibitor according to the present invention is characterized by comprising a dipeptide having a structure of Hyp-Gly as an essential effective component.

Abstract: Pharmaceutical compositions and kits useful for the treatment of cancer include certain alkyl esters of cystine and certain alkyl-substituted cystamine derived esters, including, for example, cystine dimethyl ester and a di-alkyl peptidyl cystamine ester, among others. These compounds may be employed in methods of treating cancers or methods of determining sensitivity of certain cancer cells to apoptosis alone, or in combination with other chemotherapeutic, radiological or apoptotic agents.

Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.

Abstract: Disclosed are compounds having at least one quaternary alkyl ammonium functionality. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.

Abstract: Smac mimetics that inhibit IAPs.

Abstract: In accordance with the present invention, novel multifunctional compounds have been developed which have orthogonal reactive groups thereon, thereby facilitating preparation of compounds having multiple functional properties (e.g., a targeting moiety and a biologically active moiety). Such constructs are useful for a variety of applications, e.g., for the delivery of biologically compatible materials, and release thereof in active form. Therefore, in accordance with the present invention, there are provided multifunctional linkers of defined structure, as well as various derivatives thereof bearing one or more biologically active components thereon. Also provided in accordance with the present invention are methods for the preparation of such constructs, as well as various uses thereof.