Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.

Abstract: Described herein are CDP-therapeutic peptide conjugates, therapeutic delivery systems comprising CDP-therapeutic peptide conjugates, compositions comprising CDP-therapeutic peptide conjugates, dosage forms comprising CDP-therapeutic peptide conjugates, and kits comprising CDP-therapeutic peptide conjugates. Also disclosed are methods of using (e.g., to treat a disorder) the CDP-therapeutic peptide conjugates, therapeutic delivery systems comprising CDP-therapeutic peptide conjugates, compositions comprising CDP-therapeutic peptide conjugates, dosage forms comprising CDP-therapeutic peptide conjugates, and kits comprising CDP-therapeutic peptide conjugates.

Abstract: The present invention relates to a compound of the Formula (I)): or pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same, a method for treating or preventing viral infections, inflammation, dry eye, central nervous disorders, cardiovascular diseases, cancer, obesity, diabetes, muscular dystrophy, and hair loss.

Abstract: The present invention relates to peptidomimetics having a stable, internally constrained protein secondary structure, where the peptidomimetics contain a hydrogen bond surrogate in the internal constraint, and at least one beta amino acid. Methods for promoting cell death using peptidomimetics that inhibit p53/hDM2 are also disclosed.

Abstract: The present invention relates to pharmaceutical compositions having improved stability.

Abstract: The present invention relates to novel lipopeptide compounds, pharmaceutical compositions of these compounds and methods of using these compounds as antibacterial compounds. The compounds of the invention are particularly useful against a variety of bacteria, including resistant strains. The compounds are useful as antibacterial agents against Clostridium difficile.

Abstract: Provided are: a novel compound having a structure different from that of existing drugs; a novel microorganism capable of producing the novel compound; and further; a novel compound effective to a multiple-drug-resistant bacterium. To provide a novel compound having a high therapeutic effect which can be expected to have a low hurdle for practical realization by selecting an intended compound from many candidate compounds based not only on an antibacterial activity but also on evaluation including a therapeutic effect, a cyclic peptide compound shown by the following formula (1) or a pharmaceutically allowable salt thereof and a microorganism with Accession No. NITE BP-870 or a microorganism mutated naturally or artificially therefrom are provided. (In the formula (1), R1 represents an acyl group having 7, 8, or 9 carbon atoms and optionally containing a substituent group; R2 represents a methyl group or a hydrogen atom; and R3 represents an ethyl group or a methyl group.

Abstract: Disclosed herein are peptides which exhibit hepcidin activity and methods of making and using thereof.

Abstract: The invention relates to polypeptides of amino acid sequence SEQ ID NO: 1 according to formula (1), the use thereof for producing a medicament, and medicaments for the treatment of diseases related to monocyte recruitment.

Abstract: Use of urodilatin for preparing a medicament for the treatment of cardiovascular, renal, pulmonary and neuronal syndromes while avoiding a rebound, wherein said medicament for the delivery of urodilatin is suitable in a first quantity for a first period of at least 48 hours, followed by delivery over a second period of at least 12 hours with successive reduction of said first quantity continuously or gradually to 0 ng/kg/min.

Abstract: The invention provides a synthetic polypeptide of Formula I?: or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia.

Abstract: The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition including Crohn's disease and ulcerative colitis, and cancer.

Abstract: A composition useful as a PET and/or fluorescence imaging probe a compound a compound of Formula I, including salts, hydrates and solvates thereof: wherein R1-R7 may be independently selected from hydrogen, halogen, hydroxy, alkoxy, nitro, substituted and unsubstituted amino, cycloalkyl, carboxy, carboxylic acids and esters thereof, cyano, haloalkyl, aryl, X is selected from the group consisting of C and N; and A is selected of hydrogen, halogen, hydroxy, alkoxy, nitro, substituted and unsubstituted amino, alkyl, cycloalkyl, carboxy, carboxylic acids and esters thereof, cyano, haloalkyl, aryl, including phenyl and aminophenyl, and heteroaryl.

Abstract: The compounds of the present invention are non-immunosupressive cyclosporine analogue molecules that are able to bind cyclophilin. Said compounds include a modified side chain of amino acid I of cyclosporin A, consisting of an oxyalkyl having substituents R?, R1 and R2, where R? is H or Acetyl; R1 is a saturated or unsaturated straight chain or branched aliphatic carbon chain; and R2 may be a hydrogen; a unsubstituted, N substituted or NN disubstituted amide; a N substituted or unsubstituted acyl protected amine; a carboxylic acid; a N substituted or unsubstituted amine; a nitrile; a ester; a ketone; a hydroxy, dihydroxy, trihydroxy or polyhydroxy alkyl; or a substituted or unsubstituted aryl.

Abstract: ?-Hairpin peptidomimetics of the general formula Cyclo (-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-), enantiomers and pharmaceutically acceptable salts thereof, with Xaa1-Xaa14 being amino acid residues of certain types which are defined in the description and the claims, have anti-infective activity, e.g. to selectively inhibit the growth of or to kill microorganisms such as Bacillus subtilis and/or Shigella boydii. They can be used as medicaments to treat or prevent infections or as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

Abstract: The present invention relates to radiopharmaceutical imaging in vivo of apoptosis. The invention provides imaging agents which target apoptotic cells via selective binding to the aminophospholipid phosphatidylethanolamine (PE), which is exposed on the surface of apoptotic cells. The radiopharmaceuticals comprise radiometal complexes of chelator conjugates of PE-binding peptides. Also provided are pharmaceutical compositions, kits and methods of in vivo imaging.

Abstract: A melanocortin receptor agonist cyclic peptide of the formula where R, x and y are as defined in the specification, compositions and formulations including the peptide of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes, including sexual dysfunction such as male erectile dysfunction and female sexual dysfunction.

Abstract: The invention relates to cyclic peptide agonists that bind to the mu (morphine) opioid receptor and their use in the treatment of acute and/or chronic pain. Embodiments of the invention are directed to cyclic pentapeptide and hexapeptide analogs of endomorphin that have (i) a carboxy-terminal extension with an amidated hydrophilic amino acid and (ii) a substitution in amino acid position 2, and a 2?,6?-dimethyltyrosine (Dmt) residue in place of the N-terminal tyrosine residue a position 1. These peptide analogs exhibit increased solubility compared to similar tetrapeptide analogs while maintaining favorable or improved therapeutic ratios of analgesia to side effects.

Abstract: The present invention provides macrocyclic compounds of Formula (I): pharmaceutically acceptable salts thereof; and pharmaceutical compositions thereof, wherein R1, R2, R3, R4, RE, RF, RG, RH, RI, f, g, h, n, and m are as defined herein. The present invention further provides methods of synthesizing these macrocyclic compounds, and methods of their use and treatment. Certain aspects of the present invention relate to modulation of kinase activity, and in the treatment of kinase-associated diseases or disorders.

Abstract: A novel cyclic heptapeptide that is useful as a preadipocyte differentiation-inhibitory agent or an adipocyte fat accumulation-inhibitory agent, and the use of such agents, are provided. A novel cyclic heptapeptide represented by the following formula is provided. wherein R is CH3, CH2CH(CH3)2, CH2OCH2C6H5, CH(OH)CH3, or CH2OH.

Abstract: The present invention is drawn to cyclic RGD peptides linked via a disulfide bond, where the terminal cysteines are preferably in the D configuration. These peptides target ?v?3 integrin on tumor cells and neovasculatures and function as targeting agents for tumor diagnostic imaging and therapy. Compared with the commonly used RGD ligands, compounds of the present invention have improved targeting efficacy and lower nonspecific binding to normal organs. Moreover, the compounds of the present invention can be functionalized to conjugate imaging payload without decreasing binding strength.

Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases.

Abstract: The disclosed invention relates to peptides incorporating 3-aminoadamantane-1-carboxylic acids. These peptides are disclosed as surprisingly possessing neurogenic and neurotrophic properties. These pharmacological activities can advantageously be utilized for restoring or maintaining neuronal function in the CNS. In particular, the compounds can be used for treatment and prophylaxis of neurodegenerative diseases, e. g., Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, as well as in post-acute traumatic brain injury, or cerebral ischemia.

Abstract: A therapeutic agent for prostate cancer and malignant lymphoma containing FK228 or a salt thereof as an active ingredient, and a method for evaluating an antitumor effect of a histone deacetylase inhibitor which includes at least a step of treating a test cell with a histone deacetylase inhibitor, a step of measuring change in the expression amount of a specific gene in the test cell before and, after the treatment with the inhibitor, comparing the both expression amounts.

Abstract: The present application provides biligand and triligand protein-catalyzed capture (PCC) agents that specifically bind VEGF, as well as the use of these capture agents as detection, diagnosis, and treatment agents.

Abstract: The present invention relates to diagnostic imaging and in particular to the diagnostic imaging of fibrosis. More particularly, the present invention provides a polypeptides, cyclic polypeptides and pharmaceutical compositions suitable for the non-invasive visualization of fibrosis. The polypeptide of the invention may comprise an amino acid sequence consisting of: X1-X2-M-H-G-L-X7-L-X9-X10-D-E (SEQ ID NO: 1) wherein amino acid X1 is R, F or P; amino acid X2 is F or V; amino acid X7 is Q, H or L; amino acid X9 is W or G and amino acid X10 is A or D.

Abstract: The present invention relates to imaging agent compositions comprising radiolabelled c-Met binding peptides suitable for positron emission tomography (PET) imaging in vivo. The c-Met binding peptides are labelled with the radioisotope 18F. Also disclosed are pharmaceutical compositions, methods of preparation of the agents and compositions, plus methods of in vivo imaging using the compositions, especially for use in the management of cancer.

Abstract: A therapeutic combination comprises an antibacterially effective amount of daptomycin, and an amount of protein synthesis inhibitor antibiotic effective to prevent the development of daptomycin non-susceptibility in bacteria. Related combination therapies and methods are also included.

Abstract: Peptides having a structure characterized by the presence of two loops constrained in cyclic structure by the presence of covalent bonds between amino acid side chains, the amino acid sequences of the first and the second loop being substantially homologues to that of loop 1 (residues 29-38) and of loop 4 (residues 92-97) of NGF, respectively, displaying nerve growth factor (NGF) agonist or partial agonist activity.

Abstract: The present invention relates to a method for the production of a compound of interest by microbial fermentation, wherein the microbial host cell used has been modified in its genome such that it results in a deficiency in the production of at least one non-ribosomal peptide synthase. The present invention further relates to a microbial host cell that has been modified in its genome such that it results in a deficiency in the production of at least one non-ribosomal peptide synthase. The invention further relates to a compound of interest.

Abstract: Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

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 peptide not attached to the water-soluble oligomer.

Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as 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, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.

Abstract: The present invention provides a cyclic peptide containing RRXR motif. The present invention also provides a composition comprising the said cyclic peptide and a pharmaceutical acceptable carrier. The present invention further provides a method for treating cancer.

Abstract: Various embodiments of the invention relate to a cRGD peptide derivative and an associated manufacturing method, and to an implant having a coating containing a cRGD peptide derivative. One aspect of the invention is the provision of a cRGD peptide derivative having the formula (1): wherein x=0-8, in particular 4-8, and R is a hydrophobic group.

Abstract: Depsipeptides and congeners thereof are disclosed having structure (I), wherein m, n, p, q, X, R1, R2 and R3 are as defined herein. These compounds, including FR901228, have activity as, for example, immunosuppressants, as well as for the prevention or treatment of patients suffering or at risk of suffering from inflammatory, autoimmune or immune system-related diseases including graft-versus-host disease and enhancement of graft/tissue survival following transplant. Also provided are methods for inhibiting lymphocyte activation, proliferation, and/or suppression of IL-2 secretion.

Abstract: Described herein are methods for forming two or more dicarba bridges, as well as new compounds containing dicarba bridges.

Abstract: The present invention discloses a crystal of a peptide substance and the preparation method as well as the use thereof. Said crystal B possesses peaks at the following 2? angles in the X-ray diffraction pattern (XRPD): 3.2±0.2°, 5.4±0.2°, 6.2±0.2°, and 9.3±0.2°.

Abstract: The present invention relates generally to receptor-selective variants of the low-density lipoprotein receptor-associated protein (RAP) and compositions thereof, methods of generating such variants and methods of using such receptor-selective RAP variant compositions for therapeutic purposes.

Abstract: A probe for imaging EGFR expressing cells includes an EGFR targeting moiety, a reporter moiety, and a hydrophilic linker that links the EGFR targeting moiety to the reporter moiety. The hydrophilic linker enhances solubility of the probe in an aqueous media as well as binding affinity of the probe to EGFR expressing cells.

Abstract: The new pure vancomycin hydrochloride substantially free of impurities known in commercially available products is described. The term “substantially free of impurities” designates a purity of vancomycin hydrochloride between about 97% and about 99%, particularly between about 98% and about 99%, preferably about 99%, as determined by HPLC analytical method as directed in U.S.P., NF 27th revision, 22 (2004). The new pure vancomycin hydrochloride (vancomycin B hydrochloride) contains less than 0.7% of total impurities, namely, only one impurity exceeds 0.3%. The new process for the purification of crude vancomycin by displacement chromatography is described by which the desired pure antibiotic according to the present invention is produced, based on the finding that high purity of the vancomycin hydrochloride is obtained using low selected pH values of the mobile phase between 3.9 and 4.2.

Abstract: Provided are a cyclic peptide compound or a pharmacologically acceptable salt thereof capable of inhibiting parakeratosis of skin, and a method for producing the same.

Abstract: The invention relates to peptide derivatives (peptides and pseudo-peptides) and the use thereof as vectors for molecules of interest. The invention also relates to conjugates containing a peptide derivative of the invention bound to a molecule of interest. The peptides of the invention can be used, in particular, to vectorize, generally in the form of prodrug conjugates, molecules of pharmaceutical or diagnostic interest such as, for example, therapeutic molecules, imaging or diagnostic agents, or molecular probes, across cell membranes of different tissues or organs, healthy or pathologic, and in particular to enable their transport across physiological barriers of the nervous system such as the Blood brain barrier (BBB), Blood-spinal cord barrier (BSCB), or Blood-retinal barrier (BRB).

Abstract: The present invention relates to labelled cMet binding peptides suitable for optical imaging in vivo. The peptides are labelled with a benzopyrylium dye suitable for imaging in the red to near-infrared region. Also disclosed are pharmaceutical compositions and kits, as well as in vivo imaging methods, especially of use in the detection, staging, diagnosis, monitoring of disease progression or monitoring of treatment of colorectal cancer (CRC).

Abstract: Depsipeptides and congeners thereof are disclosed having structure (I), wherein m, n, p, q, X, R1, R2 and R3 are as defined herein. These compounds, including FR901228, have activity as, for example, immunosuppressants, as well as for the prevention or treatment of patients suffering or at risk of suffering from inflammatory, autoimmune or immune system-related diseases including graft-versus-host disease and enhancement of graft/tissue survival following transplant. Also provided are methods for inhibiting lymphocyte activation, proliferation, and/or suppression of IL-2 secretion.

Abstract: The present application relates to cyclic depsipeptides of Formula I: or derivatives thereof, wherein X, A1, A2, A3, A4, A5, A6 and A7 are defined herein. The cyclic depsipeptides of Formula I are inhibitors of kallikrein 7 and thus can be employed for the treatment of kallikrein-7 dependent diseases.

Abstract: A process for manufacturing a cyclic peptide which comprises providing a cyclic peptide bonded to a Merrifield-type resin and cleaving the cyclic peptide from the Merrifield type resin by transesterification.

Abstract: The present invention relates to the clinical application of BBP, alone or in combination with other growth factors, for use in bone healing applications, such as spinal surgery. Additional applications include use in orthopedic implantable prostheses and implantation into other surgical sites (e.g., surgical reconstruction, regional osteopenia, etc.) where bone is desired.

Abstract: The invention relates to new peptide-based compounds for use as diagnostic imaging agents or as therapeutic agents wherein the agents comprise a targeting vector which binds to receptors associated with integrin receptors.

Abstract: A cyclic organic compound which comprises 16 amino acids or 17 amino acids and has no carboxyl group C-terminally and/or no amino group N-terminally. Optionally, one of the amino acids is a normatural amino acid. The ring closure is formed between a side chain of one amino acid and the C-terminus of another amino acid, or the ring closure is effected with the aid of a normatural amino acid. A process for producing and using the compound for regulating vectorial ion channels, for treating diseases associated with the lung function and for treating oedemas is provided.