Abstract: A process for and intermediates in the preparation of canfosfamide and its salts. Some of the intermediates have anticancer activity.

Abstract: Disclosed is a novel synthetic method for isomeric peptides through an appropriate linkage of L-selenomethionine or Se-Methyl-L-selenocysteine with L-glutamic acid. The novel synthetic method produces isomeric peptides of L-selenomethionine or Se-Methyl-L-selenocysteine that exhibit (i) enhanced water solubility; (ii) enhanced rate of dissolution in water; (iii) enhanced bioavailability; (iv) excellent vascular endothelial growth factor promoting activity; (v) excellent anti-5-alpha-reductase activity; (vi) capabilities to prevent/reduce “hair fall” and promote “hair growth”, thereby maintaining a perfect homeostasis for “hair care”. Cosmeceutical and pharmaceutical compositions comprising the isomeric peptides obtained through an appropriate linkage of L-selenomethionine or Se-Methyl-L-selenocysteine with L-glutamic acid are also disclosed. Other dipeptides with several other amino acids and uses thereof are also disclosed.

Abstract: The present invention relates to novel cytotoxic molecules and their use for the treatment of cancer and other diseases.

Abstract: The invention provides a method of treating T-cell mediated diseases and a method of inhibiting the activation of T-cells using certain diketopiperazines. The invention also provides methods of synthesizing diketopiperazines and pharmaceutical compositions comprising certain diketopiperazines. The invention further provides methods of making improved pharmaceutical compositions of proteins and peptides by either increasing or decreasing the content of diketopiperazines in the compositions and the resultant improved pharmaceutical compositions.

Abstract: At least some embodiments of the invention relates to an implant having a coating that contains or is composed of a functionalized RGD peptidomimetic RGD-P1 having the formula (1) and/or a functionalized RGD peptidomimetic RGD-P2 having the formula (2), and an associated manufacturing method.

Abstract: S-t-butyl protected cysteine di-peptide analogs and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).

Abstract: At least some embodiments of the invention relates to an implant having a coating that contains or is composed of a functionalized RGD peptidomimetic RGD-P1 having the formula (1) and/or a functionalized RGD peptidomimetic RGD-P2 having the formula (2), and an associated manufacturing method.

Abstract: The present invention encompasses a method for screening for a kokumi-imparting substance by using the calcium receptor activity as an index, a composition containing a kokumi-imparting substance obtained by the screening method, a method for producing food or drink imparted with kokumi, and food or drink imparted with kokumi.

Abstract: An immunomodulatory compound is administered to treat, prevent, inhibit, or reduce melanoma in a subject.

Abstract: Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.

Abstract: A bortezomib composition includes bortezomib and boric acid in a mass ratio of boric acid to bortezomib is from 1:1 to 10:1. The composition is a solid, and may be prepared by forming a liquid mixture including a solvent, bortezomib and boric acid, and lyophilizing the liquid mixture.

Abstract: The subject invention provides therapeutic compositions, and uses thereof for the treatment or amelioration of injury to small intestine mucosa. In preferred embodiments, the composition comprises one or more nutrients and/or electrolytes that acquire or retain considerable absorptive capacity.

Abstract: Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described.

Abstract: This invention relates to the inhibition of a newly discovered growth-stimulating protein in an individual. Further, the invention relates to a method for preventing or treating a cancer, or preventing or treating cancer growth, invasion or metastasis, or preventing or treating other hyperproliferative diseases in an individual, by down regulating the expression of said growth-stimulating protein or by inactivating said protein. Still further, the invention concerns a method for diagnosing cancer or other hyperproliferative diseases in an individual based on said growth-stimulating protein.

Abstract: Smac mimetics that inhibit IAPs.

Abstract: The subject invention provides dipeptides useful in promoting healthy muscle tissues as well as effective immune responses. The dipeptides of the subject invention are particularly advantageous because they are stable, bioavailable, and can be formulated in an aqueous solution.

Abstract: Peptide compounds and methods for upregulating expression of a gene encoding an antioxidative enzyme, such as superoxide dismutase or catalase, to counteract harmful oxidative effects of reactive oxygen species and other free radicals are described. The peptide compounds may be used to treat or prevent diseases and conditions characterized by undesirable elevation of reactive oxygen species and other free radicals, to upregulate AP-1 gene expression, and to treat pain. The peptide compounds may be used as components of pharmaceuticals and dietary supplements.

Abstract: The present invention relates to the use of compounds selected from the group consisting of Lys-(D)Pro-Thr, N-acyl Lys-(D)Pro-Thr, C-amide Lys-(D)Pro-Thr, and C-esters of Lys-(D)Pro-Thr; or a pharmaceutically acceptable salt of said compound fort he treatment of inflammatory disorders. The invention also relates to the use of ?MSH for inducing tolerance.

Abstract: A process for making pure crystalline D-isoglutamyl-D-tryptophan is provided which includes the step of deprotecting essentially pure N-tert-butoxycarbonyl-D-isoglutamyl-D-tryptophan or its diester to yield essentially pure D-isoglutamyl-D-tryptophan. A process is also provided for the preparation of pure mono ammonium salt of D-isoglutamyl-D-tryptophan from essentially pure N-tert-butoxycarbonyl-D-isoglutamyl-D-tryptophan. D-isoglutamyl-D-tryptophan, ammonium salt (1:1) is a stable pharmaceutical solid.

Abstract: Compounds which inhibit the activity of signal transducer and activator of transcription 3 (STAT3) are provided together with methods of making and using the same. The compounds are designed to bind to the SH2 domain of STAT3, preventing STAT3 from binding to receptors for interleukin-6 family cytokines, growth factors such as the platelet-derived growth factor, the epidermal growth factor, vascular endothelial growth factor, and other signaling molecules such as leptin. Blocking these interactions prevents STAT3 from being phosphorylated on Tyr705, which is required for the dimerization of STAT3, translocation to the nucleus, binding to STAT3 response elements on promotors, and transcription of genes. In addition to these activities, binding to the SH2 domain of STAT3 breaks up pre-formed dimmers, thereby preventing the transcriptional activity of the inhibitor.

Abstract: A calcium receptor activator and compositions containing at least one of the following: ?-Glu-Cys-Gly, ?-Glu-Cys(SNO)-Gly, ?-Glu-Ala, ?-Glu-Gly, ?-Glu-Cys, ?-Glu-Met, ?-Glu-Thr, ?-Glu-Val, ?-Glu-Orn, Asp-Gly, Cys-Gly, Cys-Met, Glu-Cys, Gly-Cys, Leu-Asp, D-Cys, ?-Glu-Met(O), ?-Glu-Val-Val, ?-Glu-Val-Glu, ?-Glu-Val-Lys, ?-Glu-?-Glu-Val, ?-Glu-Val-NH2, ?-Glu-Val-ol, ?-Glu-Ser, ?-Glu-Tau, ?-Glu-Cys(S-Me)(O), ?-Glu-Leu, ?-Glu-Ile, ?-Glu-t-Leu, ?-Glu-Cys(S-allyl)-Gly, ?-Glu-Gly-Gly, ?-Glu-Val-Phe, ?-Glu-Val-Ser, ?-Glu-Val-Pro, ?-Glu-Val-Arg, ?-Glu-Val-Asp, ?-Glu-Val-Met, ?-Glu-Val-Thr, ?-Glu-Val-His, ?-Glu-Val-Asn, ?-Glu-Val-Gln, ?-Glu-Val-Cys, ?-Glu-Val-Orn, ?-Glu-Ser-Gly, ?-Glu-Cys(S-Me), ?-Glu-Abu-Gly, ?-Glu-Cys(S-Me)-Gly, and ?-Glu-Val-Gly.

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 provides a hair growth agent having novel action mechanism and a hair growth composition containing the agent. Specifically, the present invention provides a novel hair growth composition containing one or more kinds of epsilon-N-(gamma-glutamyl)lysine or a salt thereof.

Abstract: The present invention provides an orally ingestible composition and a method for regulating an autonomic nervous activity. In particular, the present invention provides an orally ingestible composition capable of suppressing an increase in a sympathetic nervous activity, and an orally ingestible composition capable of promoting a parasympathetic nervous activity. The present invention is a composition for regulating an autonomic nervous activity, comprising, as an active ingredient, Tyr-Pro or a salt thereof.

Abstract: The invention relates to a peptide combination characterized by peptides each having the same sequence length (SEQL), that can be produced from a mixture (A) comprising a number x of amino acids having a protected acid group or a number z of peptides having an acid group protected by means of a protecting group and an activated amino group, wherein the amino acids are present in the mixture (A) in particular adjustable molar ratios, and a mixture (B) comprising a number y of amino acids having an amino group protected by means of a protecting group, wherein the amino acid molar ratios of the mixture (B) are equal to the amino acid molar ratios of the mixture (A), and wherein the number x=y.

Abstract: The present invention is directed to compositions and methods for pain management, and for treating inflammation or an inflammation-associated disorder in a subject comprising administering to the subject a therapeutically effective amount of a COX-2 inhibitor and a therapeutically effective amount of a prostacyclin analog, such as treprostinil, a pharmaceutically acceptable salt thereof, or a treprostinil derivative described herein.

Abstract: The present invention relates generally to the use of ?-glutamyl antioxidants, particularly ?-glutamyl-cysteine, as cytoprotective agents to prevent reperfusion injury (i.e., hemorrhagic transformation) of the blood-brain barrier during reperfusion following an ischemic stroke. The ?-glutamyl antioxidants can be used alone or used in combination with an agent which inhibits the reverse movement of Na/Ca exchange in the blood-brain barrier such as 2-[2-[4-(4-nitrobenzyloxy)phenyl]ethyl]isothiourea methanesulphonate (KB-R7943).

Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.

Abstract: This invention is related to a peptides mixture. Without the need to consider the patients' genetic background, it can interfere with MHC-pathogenic peptide-TCR formation, which includes the interference with pathogen peptide binding with MHC and pMHC binding with specific TCR, suppression of the immune synapse formation when the specific T cell immune response occurs, reduction of the number and density of the MHC-specific immune response mediated pathogenic peptide-TCR in the immune synapse, and suppression of the highly activated signal transduction in the immune synapse. Hence it can negatively regulate the T cell specific immune response, reduce the specific immune cell activation, proliferation and effect, and make the radical T cell specific immune response more stable and last longer. It can be used to treat diseases with excessive T cell-specific immune reaction, such as severe flu, SARS, hand-foot-and-mouth disease, viral pneumonia, bacterial infections, severe autoimmune disease and etc.

Abstract: The present invention describes compounds comprising new and useful peptides and peptidomimetics that can bind to CD23. They are capable of reducing inflammatory responses associated with auto-immune diseases, chronic inflammatory diseases, allergies and other inflammatory conditions such as those mediated by the mammalian immune system. Compounds of the present invention relate to a CD23-binding peptide wherein said peptide comprises an amino-acid sequence of X1—X2—X3—X4—X5—X6—X7—X8, wherein: X1 is Phe, or is absent; X2 is His or Ala; X3 is Glu, Ser, Ala, Asn, Lys, or Cys; X4 is Asn, Phe, Gln, Pro, Ser, or Ala; X5 is Trp; X6 is Pro, Arg, Glu, Gly, Cys, or Lys; X7 is Ser, Pro, Leu, Thr Ala, Gly, Asn, or absent; and X8 is Phe, Gly, or is absent.

Abstract: Provided are compositions comprising beta-alanylhistidine peptides and/or beta-alanines, and methods for administering these peptides and amino acids. In one aspect, the compositions and methods cause an increase in the blood plasma concentrations of beta-alanine and/or creatine.

Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.

Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.

Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and ophthalmic diseases, disorders and conditions.

Abstract: This invention relates to novel 2-amino-3-hydroxypropanoic acid derivatives and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an NMDA glycine-site antagonist.

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: The present invention relates to a peptide or peptidomimetic for use in the treatment of a biofilm-associated infection in a subject, wherein said peptide or peptidomimetic a) carries a net positive charge, b) is 1 to 6 amino acids in length or is an equivalently sized peptidomimetic; and c) is amphipathic in nature, having one or more lipophilic groups, one of said lipophilic groups comprising at least 7 non-hydrogen atoms.

Abstract: The present invention relates to structural studies of dipeptidyl peptidase I (DPPI) proteins, modified dipeptidyl peptidase I (DPPI) proteins and DPPI co-complexes. Included in the present invention is a crystal of a dipeptidyl peptidase I (DPPI) and corresponding structural information obtained by X-ray crystallography from rat and human DPPI. In addition, this invention relates to methods for using structure co-ordinates of DDPI, mutants hereof and co-complexes, to design compounds that bind to the active site or accessory binding sites of DPPI and to design improved inhibitors of DPPI or homologues of the enzyme.

Abstract: This invention discloses drug-delivery compositions, methods of making prodrugs, and methods of drug delivery using a self-assembled gelator. The backbone of the gelator can contain a drug or prodrug, such as acetaminophen or salicin. Additional drugs or agents can be encapsulated in the gelator. Enzymatic or hydrolytic cleavage can be used to release the drugs.

Abstract: Described herein are peptide derivatives and peptidomimetics as inhibitors for transglutaminases, methods for their preparation, pharmaceutical compositions containing said compounds as well as uses of said transglutaminase inhibitors in particular for the treatment of coeliac disease and transglutaminase dependent diseases.

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: 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: 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: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers thereof, wherein each variable has specific definitions. Pharmaceutical compositions containing compounds (I) and process for preparing compounds (I) are also provided. Bioavailable combinations of the inhibitors of HCV of Formula (I) with ritonavir are also provided.

Abstract: Isolated DJ-1 related peptides are disclosed and pharmaceutical compositions comprising same for treating oxidative stress-related disorder.

Abstract: Inhibitors of HCV of formula (I). and the N-oxides, salts, and stereoisomers thereof, wherein the dashed line represents an optional double bond between atoms C7 and C8; R1 is hydrogen or C1-6alkyl; R2 is hydrogen or C1-6alkyl; and n is 3, 4, 5, or 6; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I) are provided. Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.

Abstract: The present invention provides compounds of formula M-L-M? (where M and M? are each independently a monomeric moiety of Formula (I) and L is a linker). The dimeric compounds have been found to be effective in promoting apoptosis in rapidly dividing cells.

Abstract: The present invention relates to the use of a composition comprising at least one cell membrane fraction or parts thereof, for the reduction of lipolytic activity and/or to retard fat digestion, suppress appetite, body weight and/or lower blood lipids. The invention also relates to the use of said hydrophobic peptide in a pharmaceutical as well as a food composition and methods of treating a mammal with said composition.

Abstract: Disclosed is a novel synthetic method for isomeric peptides through an appropriate linkage of L-selenomethionine or Se-Methyl-L-selenocysteine with L-glutamic acid. The novel synthetic method produces isomeric peptides of L-selenomethionine or Se-Methyl-L-selenocysteine that exhibit (i) enhanced water solubility; (ii) enhanced rate of dissolution in water; (iii) enhanced bioavailability; (iv) excellent vascular endothelial growth factor promoting activity; (v) excellent anti-5-alpha-reductase activity; (vi) capabilities to prevent/reduce “hair fall” and promote “hair growth”, thereby maintaining a perfect homeostasis for “hair care”. Cosmeceutical and pharmaceutical compositions comprising the isomeric peptides obtained through an appropriate linkage of L-selenomethionine or Se-Methyl-L-selenocysteine with L-glutamic acid are also disclosed. Other dipeptides with several other amino acids and uses thereof are also disclosed.

Abstract: The invention provides an orally-administrable nutritional product comprising a dipeptide including a branched chain amino acid (BCAA). In one embodiment, the nutritional product comprises a dipeptide selected from at least one of the following: alanyl-leucine, alanyl-isoleucine, alanyl-valine, glycyl-leucine, glycyl-isoleucine, and glycyl-valine.