Abstract: Compounds comprising peptides capable of binding C3 protein and inhibiting complement activation are disclosed. The compounds comprise compstatin analogs in which the N-terminus and/or C-terminus contains an added component that improves (1) the peptide's solubility at physiological pH; (2) the peptide's plasma half-life; (3) the peptide's intraocular retention; and/or (4) the peptide's binding affinity to C3 or its fragments as compared to an unmodified compstatin peptide under equivalent conditions. Pharmaceutical compositions and methods of using the compounds are also disclosed.

Abstract: The present invention relates to formulations and methods for treatment of sexual dysfunction in females diagnosed with both sexual dysfunction and controlled hypertension.

Abstract: A compound of Formula I, and its analogs are provided. Compositions that include Formula I can be used to inhibit human equilibrative nucleoside transporter 1, increase adenosine signaling and produce effects that include increasing antiviral activity, increasing antiparasitic activity, increasing alcohol tolerance, decreasing pain protecting from ischemia as well as many other conditions.

Abstract: Methods of inhibiting the growth or metastasis of a cancer in a subject by inhibiting a Ral GTPase in the subject, and small molecule inhibitors of Ral GTPases useful in the methods of the invention. Pharmaceutical compositions containing the compounds of the invention, and methods of using the same.

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: There is described herein imidopiperidine compounds as inhibitors of human polynucleotide kinase phosphatase.

Abstract: The present subject matter provides pH triggered peptides, as well as compositions methods, devices, and systems comprising the same. The pH triggered peptides include cyclic and short linear peptides, and may have higher affinity to a membrane lipid bilayer at low pH than at neutral or high pH.

Abstract: The present invention provides scaffolds that include a polymer and a cyclic peptide ligand. The peptide ligand increases the attachment of endothelial cells and/or progenitor cells to the scaffold. The present invention also provides engineered tissues that include the provided scaffolds. The present invention also provides coatings that include a coating polymer and a cyclic peptide ligand. The present invention also provides methods of improving endothelialization and vascularization of endothelial cells and/or progenitor cells for tissue regeneration in a subject and of repairing bone defects in a subject, by implanting a provided scaffold.

Abstract: Embodiments of compositions and methods for the treatment of blood disorders and malignancies in a subject are described herein. In one embodiment, a composition for the treatment of a blood disorder or a malignancy in a subject comprises decitabine, tetrahydrouridine, and an excipient. In another embodiment, a method for the treatment of a blood disorder or a malignancy in a subject comprises the oral administration of a composition comprising decitabine and tetrahydrouridine. In some examples, the composition may be administered 1-3 times weekly.

Abstract: The invention provides compositions that increase the mobilization, homing, expansion, and/or differentiation of stem cells and methods of using the same for the treatment of mammals.

Abstract: Novel peptide analogs of a ?-defensin have been developed that provide a biphasic effect in treating infection and/or sepsis. These analogs are active at concentrations below those needed to provide a bactericidal or bacteriostatic effect, and function by initially recruiting effector cells of the immune system to address the infective organism followed by regulation of the immune system to down regulate the inflammatory response characteristic of sepsis and septic shock. These novel ?-defensin analogs are protective at concentrations where naturally occurring ?-defensins have no apparent effect, and include a core set of structural and sequence features not found in native ?-defensin.

Abstract: The invention provides methods and compositions for treating various degenerative diseases (e.g., AMD) with a factor D inhibitor (e.g., anti-factor D antibody or antigen-binding fragment thereof). Also provided are methods of selecting or identifying patients for treatment with a factor D inhibitor. Methods include the use of prognostic and/or predictive biomarkers.

Abstract: The present invention relates to improved pharmaceutical formulations, uses and methods for the oral delivery of peptide drugs with advantageously high bioavailability, safety and costeffectiveness. In particular, the invention provides a peptide drug having a molecular weight of equal to or less than 5 kDa for use as a medicament, wherein said peptide drug is to be administered orally in combination with a pharmaceutically acceptable copper salt/complex and/or a pharmaceutically acceptable zinc salt/complex and/or a pharmaceutically acceptable iron salt/complex, and with a pharmaceutically acceptable complexing agent. The invention also provides a pharmaceutical composition comprising: a peptide drug having a molecular weight of equal to or less than 5 kDa; a pharmaceutically acceptable copper salt/complex and/or a pharmaceutically acceptable zinc salt/complex and/or a pharmaceutically acceptable iron salt/complex; and a pharmaceutically acceptable complexing agent.

Abstract: Solid state forms of Linaclotide, processes for their preparation, compositions comprising them and medical uses thereof are provided. The solid state forms of Linaclotide are useful in the preparation of other solid state forms of Linaclotide, particularly the amorphous form.

Abstract: A method for preparing a cyclopeptide, which includes the following steps: (A) providing compounds represented by the following formulas (II-1) or (II?-1) and (II-2); (B) performing a reaction between the compounds of formulas (II-1) or (II?-1) and (II-2), to obtain a compound represented by the following formula (II-3) and (II?-3), respectively; (C) performing a reaction between the compound of formula (II-3) or (II?-3) and a compound represented by the following formula (II-4) or (II?-4), respectively, is performed, to obtain a compound represented by the following formula (II-5), and (II?-5), respectively; (D) performing a cyclization reaction of the compound of formula (II-5) or (II?-5) with a catalyst of formula (III), to obtain a compound represented by the following formula (I) or (I?), respectively. The formulas (I), (I?), (II-1) to (II-5), (II?-1) to (II?-5) and (III) are shown in the specification.

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: The present invention relates to stable pharmaceutical compositions comprising linaclotide or pharmaceutically acceptable salts thereof, as well as to various methods and processes for the preparation and use of the compositions.

Abstract: The present invention relates to stable pharmaceutical compositions comprising linaclotide or pharmaceutically acceptable salts thereof, as well as to various methods and processes for the preparation and use of the compositions.

Abstract: The present disclosure describes methods for preventing or treating periodontitis or diseases associated with periodontitis. The present disclosure also describes methods of screening for compounds that can be used to prevent or treat periodontitis or diseases associated with periodontitis.

Abstract: The invention relates to methods, uses, compositions and formulations including a melanocortin receptor-4 agonist and a glucagon-like peptide-1 receptor agonist for treatment of obesity, diabetes, metabolic syndrome and related indications, diseases or disorders.

Abstract: The invention relates to thioether monomer and dimer peptide molecules which inhibit binding of ?4?7 to the mucosal addressing cell adhesion molecule (MAdCAM) in vivo.

Abstract: Peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production are described.

Abstract: The invention relates to preparations comprising amorphous emodepside in a polyvinylpyrrolidone matrix, pharmaceuticals comprising such preparations, and their use against endoparasites in animals or humans.

Abstract: Template-fixed ?-hairpin peptidomimetics of the general formulae wherein Z is a chain of 11 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or Pro(4NHCOPhe), or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to inhibit proteases, in particular serine proteases, especially Cathepsin G or Elastase or Tryptase. These ?-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.

Abstract: Peptide inhibitors of the interleukin-23 receptor, and related compositions and methods of using these peptide inhibitors to treat or prevent a variety of diseases and disorders, including inflammatory bowel disease, are disclosed.

Abstract: Use of a subcutaneously administered dose of between about 1.0 mg and 1.75 mg of bremelanotide or a pharmaceutically acceptable salt of bremelanotide for the treatment of female sexual dysfunction in women while reducing or minimizing undesirable side effects.

Abstract: Peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production are described.

Abstract: The invention relates to the use of the Peptide of the formula Cyclo-(Arg-Gly-Asp-DPhe-NMe-Val) and/or the pharmaceutically acceptable derivatives, solvates and/or salts thereof, for the manufacture of a medicament for the treatment of breast cancer and/or bone metastases in humans, wherein the medicament is optionally to be used in combination with one or more cancer cotherapeutic agents, preferably selected from a) hormone modulating agents, b) osteoclast activity modulating agents, c) cancer chemotherapeutic agents, and/or d) radiotherapy, alone, concurrently or not in the dosage regime of the present invention.

Abstract: Peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production are described.

Abstract: The present invention features the use of compstatin and complement inhibiting analogs thereof for treating and/or preventing age related macular degeneration and other conditions involving macular degeneration, choroidal neovascularization, and/or retinal neovascularization. The invention also provides compositions comprising compstatin or a complement inhibiting analog thereof and a second therapeutic agent. The invention also provides compositions comprising compstatin or a complement inhibiting analog thereof and a gel-forming material, e.g., soluble collagen, and methods of administering the compositions.

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: This invention relates to methods and compositions for treating carcinoid syndrome and other adverse symptoms associated with tumor-producing neuroendocrine tumors, said methods comprising administering a therapeutically effective amount of a vascular disrupting agent, or a pharmaceutically acceptable salt thereof, to a subject having a hormone producing neuroendocrine tumor. In preferred implementations, the vascular disrupting agent is combretastatin A-4 phosphate, combretastatin A-1 diphosphate, or a pharmaceutical acceptable salt thereof.

Abstract: Disclosed are compositions comprising crosslinked hyaluronic acid gels, preferably vinyl sulfone cross-linked hyaluronic acid known as hylan B gel, for use in topical cosmetic and dermatological formulations. The hylan B gel in these formulations provides prolonged delivery of incorporated substances to the surface of the skin, to provide a hydrated film on the surface of the skin, and to provide a substantive and compatible film on the skin.

Abstract: Solid, stable formulations of linaclotide suitable for oral administration are described herein as are methods for preparing such formulations. The formulations described herein contain a polypeptide consisting of the amino acid sequence Cys Cys Glu Tyr Cys Cys Asn Pro Ala Cys Thr Gly Cys Tyr (“linaclotide”; SEQ ID NO:1) or a pharmaceutically acceptable salt thereof. The linaclotide formulations described herein are stable and have a sufficient shelf life for manufacturing, storing and distributing the drug.

Abstract: Disclosed are compositions comprising crosslinked hyaluronic acid gels, preferably vinyl sulfone cross-linked hyaluronic acid known as hylan B gel, for use in topical cosmetic and dermatological formulations. The hylan B gel in these formulations provides prolonged delivery of incorporated substances to the surface of the skin, to provide a hydrated film on the surface of the skin, and to provide a substantive and compatible film on the skin.

Abstract: Cross-linked proteins and peptides, and methods of making and uses of such cross-linked proteins and peptides. The cross-linked proteins and peptides have rigid, distance-matching bismethylene aryl cross-linking moieties. Compositions comprising the cross-linked proteins and peptides can be used as pharmaceutical delivery formulations. The cross-linked proteins and peptides can have improved properties, such as cell permeability, as compared to the parent protein or peptide.

Abstract: Compounds of formula (I), salts thereof, and compositions and uses thereof are described. The compounds are useful as V1a vasopressin agonists, for the treatment of e.g., complications of cirrhosis, including bacterial peritonitis, HRS2 and refractory ascites.

Abstract: Novel peptoid oligomers are disclosed that have a formula represented by the following formula Ia or Ib: The peptoid oligomers are prepared as modulators of androgen receptor (AR), and may be prepared as pharmaceutical compositions and used for the prevention or treatment of a variety of conditions in mammals, including humans, associated with unwanted or aberrant AR activity. The present peptoid oligomers are particularly valuable for the treatment of subjects with cancer.

Abstract: The present invention relates generally to tissue differentiation factor (TDF) analogs. More specifically, the invention relates to structure-based methods and compositions useful in designing, identifying, and producing molecules, which act as functional modulators of TDF-like receptors. The invention further relates to methods of detecting, preventing, and treating TDF-associated disorders.

Abstract: A method and formulation for preparing spray dried vancomycin. In various embodiment, the formulation includes vancomycin HCl (10-20%) and one or more of the following PEG (0-5%), mannitol (0-5%), ethanol (0-10%), and a citrate buffer. Spray dried vancomycin has favorable reconstitution times and water content.

Abstract: The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production. Macrocycles of the invention include triazole moieties that crosslink amino acid side chains. The cross links can stabilize a secondary structure of a peptidomimetic macrocycle, such as an ?-helix.

Abstract: Disclosed are compounds and methods relating to a chemical transformation for the conjugation of unprotected peptide biomolecules via a SNAr process between highly fluorinated aryl moieties and thiols (“fluoroaryl-thiol-click”).

Abstract: The invention concerns peptoid-peptide hybrids that may act as protein interaction inhibitors (PPIIs). Another aspect of the invention concerns a method for treating a disorder (e.g., an oncologic disorder) in a human or animal subject, comprising administering an effective amount of a peptoid-peptide hybrid (a peptoid body) of the invention, or a composition comprising a peptoid-peptide hybrid, to the subject in need thereof. Another aspect of the subject invention concerns a method for killing or inhibiting the growth of cells (e.g., cancer cells or malaria-infected cells), comprising contacting a cancer cell in vitro or in vivo with an effective amount of a peptoid-peptide hybrid, or a composition comprising the peptoid-peptide hybrid. Another aspect of the invention concerns a method for producing a peptoid-peptide hybrid.

Abstract: A high purity cyclopeptide crystal has a structure shown by Formula I. R represents H or a cation forming a pharmaceutically acceptable salt. Also disclosed are a preparation method and a use of the high-purity cyclopeptide crystal.

Abstract: The present invention relates to compositions forming a low viscosity mixture of: a) 20-50 wt. % of at least one diacyl glycerol; b) 20-54 wt. % of at least one phosphatidyl choline (PC); c) 5-15 wt. % of at least one biocompatible, organic mono-alcoholic solvent; d) 1 to 20 wt. % polar solvent e) 5 to 150 mg/ml of at least one peptide somatostatin receptor agonist comprising pasireotide; f) optionally at least one antioxidant; wherein the ratio of components a:b is in the range 40:60 to 54:46; wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with excess aqueous fluid. The invention further relates to methods of treatment comprising administration of such compositions, and to pre-filled administration devices and kits containing the formulations.

Abstract: Provided herein are methods or reactivating a latent Human Immunodeficiency Virus (HIV) infection in a cell. The methods comprise modulating a level of NF-?B activity in the cell by contacting the cell with an agent that produces a transient first increase in the level of NF-?B activity without a second delayed increase in NF-?B activity. Optionally, a second agent is used to prime the reactivation. Also provided herein is an isolated Massilia bacterium or population thereof capable of producing a HIV-1 reactivating factor (HRF). Also provided are methods of culturing the Massilia bacteria. Further provided are methods of reactivating a latent Human Immunodeficiency Virus-1 (HIV-1) infection in a subject comprising administering to the subject a HIV-1 reactivating factor produced by Massilia bacteria, optionally with a priming agent.

Abstract: The present invention provides, among other things, novel peptides and compositions for treating disease.

Abstract: Described are lantibiotic-based compounds, pharmaceutical compositions comprising the same and use of the compounds and said compositions, for the treatment of microbial infection, for example Clostridium difficile or Micrococcus luteus infection. The lantibiotic-based compounds have antimicrobial activity and in comparison to one or more of actagardine, actagardine B, deoxyactagardine B and deoxyactagardine have retained activity or improved activity.

Abstract: The present invention features peptides, compositions, and related methods for treating gastrointestinal disorders and conditions, including but not limited to, irritable bowel syndrome (IBS), gastrointestinal motility disorders, functional gastrointestinal disorders, gastroesophageal reflux disease (GERD), duodenogastric reflux, Crohn's disease, ulcerative colitis, inflammatory bowel disease, functional heartburn, dyspepsia, visceral pain, gastroparesis, chronic intestinal pseudo-obstruction (or colonic pseudo-obstruction), disorders and conditions associated with constipation, and other conditions and disorders are described herein. using peptides and other agents that activate the guanylate cyclase C (GC-C) receptor.

Abstract: The present invention features peptides, compositions, and related methods for treating gastrointestinal disorders and conditions, including but not limited to, irritable bowel syndrome (IBS), gastrointestinal motility disorders, functional gastrointestinal disorders, gastroesophageal reflux disease (GERD), duodenogastric reflux, Crohn's disease, ulcerative colitis, inflammatory bowel disease, functional heartburn, dyspepsia, visceral pain, gastroparesis, chronic intestinal pseudo-obstruction (or colonic pseudo-obstruction), disorders and conditions associated with constipation, and other conditions and disorders are described herein, using peptides and other agents that activate the guanylate cyclase C (GC-C) receptor.