Abstract: The present invention provides compositions and methods for inducing an immune response in a subject. In particular, the present invention provides compositions comprising immunostimulatory ligands (ISL) and methods of inducing an immune response in a subject therewith. Compositions and methods of the present invention find use in, among other things, clinical (e.g. therapeutic and preventative medicine (e.g., vaccination)) and research applications.

Abstract: The present invention features the local administration of complement inhibitors for treatment of complement-mediated disorders. In certain embodiments the invention features inhibiting activation of one or more locally produced complement proteins. The invention provides sustained release formulations and devices comprising a complement inhibitor and methods of use thereof.

Abstract: The present invention provides novel liposomal formulations of polymyxin B and pharmaceutical compositions thereof useful for the treatment of bacterial infections. The liposomal formulation comprises a lipid component formed as vesicles each having a minimum size of at least 500 nm and polymyxin B encapsulated in the vesicles. The present invention also provides a drug delivery system that comprises a plurality of liposomes encapsulating a polymyxin B therein, where the liposomes have a minimum vesicular size of at least 500 nm. The liposomes comprising the drug delivery system are useful to increase efficacy of a treatment for a bacterial infection by increasing bioavailability and distribution of the polymyxin B within the subject.

Abstract: Disclosed are compounds, compositions and methods for systemic and local delivery of biologically active molecules.

Abstract: Disclosed are methods of treating viral disorders via the administration of an inducing agent and an anti-viral agent. In one embodiment, the inducing agent and the anti-viral agent are administered for about five days, and the anti-viral agent is subsequently administered without the inducing agent for an additional period of about sixteen days for a total cycle of about 21 days.

Abstract: The present application teaches a coating having a biologically compatible compound conjugated to, or blended with, a polymer, wherein the polymer includes at least one olefin-derived unit and at least one unit derived from a vinyl alcohol, an allyl alcohol, or derivatives thereof.

Abstract: There is provided inter alia compounds of formula (I): for use in treatment of viral infection or as an immunosuppressant.

Abstract: A system for the protection against degradation during pelleting of one or more physiologically or pharmacologically active substances, comprising compositions in the form of micro particles or granules, particularly for use in the zootechnical and/or veterinary field. The micro particles include a core which contains one or more substances having a pharmacological action, food supplements or diagnostic media, said one or more substances being characterized by the presence, within their chemical structure, of a basic functional group, specifically including an amine functional group. The core comprises also one or more carboxylic acids and/or their salts and eventually one or more excipients. Said core is coated by an outer layer of fats or waxes, and preferably by a mixture of glyceride of fatty acids.

Abstract: The present invention relates to a composition comprising a Ninjurin1 expression or activity inhibitor for the prevention and treatment of inflammatory disease. Ninjurin1 protein is specifically expressed in macrophages around blood vessels, increases cell-cell adhesion and cell-matrix adhesion, increases expressions of Wnt7b (Wingless-type MMTV integration site family, member 7B) and Ang2 (angiopoietin-2), but reduces expression of Ang1 to induce apoptosis of vascular endothelial cells. In addition, Ninjurin1 protein is up-regulated when inflammation is induced and induces iNOS expression as well as increased NO generation. Therefore, the Ninjurin1 protein expression or activation inhibitor can be effectively used as an active ingredient of a composition for the prevention and treatment of inflammatory disease.

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 virus infections, particularly hepatitis C infections.

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 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: The present invention provides thermo-sensitive, mucoadhesive biopolymer formulations that enhance the penetration of therapeutics across the skin or mucosal surfaces. In a preferred embodiment, the biopolymer formulation comprises co-polymer of poloxamer 188 and propylene glycol, laurocapram and, optionally, one or more therapeutic agents. Also provided are uses of the biopolymer formulations for topical therapy of cancer including cervical cancer.

Abstract: A cyclic peptide capable of binding specifically to the ?2 I domain of a collagen binding integrin receptor may be conjugated to a drug containing particle via a linker moiety. The conjugate may be used to target a therapeutic drug to a cell expressing a collagen binding integrin receptor on its surface.

Abstract: Disclosed are nanoparticles, such as carbon nanotubes or other graphitic sheet materials having extended aromatic surfaces, which are used to deliver active agents such as drugs, labels or dyes (termed for convenience a “drug”) to the interior of cells. The nanoparticles are functionalized by a hydrophilic polymer or adsorption of an amphiphilic molecule to render them stable in suspension. The drug is therefore capable of release in the cell exterior. The drug is more rapidly released at lower pH, as found e.g., in tumor cells. The drug may also be linked to a branched chain hydrophilic polymer, so that each polymer molecule carries more than one drug bound by a cleavable linker.

Abstract: The present invention is directed to stable linaclotide compositions and methods of treating gastrointestinal disorders in patients in need thereof by providing the stable linaclotide compositions.

Abstract: Specific template-fixed ?-hairpin peptidomimetics of the general formula (I) wherein the single elements T or P are ?-amino acid residues connected from the carbonyl (C?O) point of attachment to the nitrogen (N) of the next element in clockwise direction and wherein said elements, depending on their positions in the chain, are defined in the description and the claims have the property to act on the receptor CXCR7. Thus, these ?-hairpin peptidomimetics can be useful in the treatment or prevention of diseases or conditions in the area of dermatological disorders, metabolic diseases, inflammatory diseases, fibrotic diseases, infectious diseases, neurological diseases, cardiovascular diseases, respiratory diseases, gastro-intestinal tract disorders, urological diseases, ophthalmic diseases, stomatological diseases, haematological diseases and cancer; or the mobilization of stem cells.

Abstract: Hydrophobic weak base compounds such as hydrophobic weak base chemotherapeutic agents (which are not an anthracycline) for use in the treatment of medical conditions such as proliferative disease or disorder in a subject, in combination with illumination of a region in a body of the subject which is characterized by the presence of proliferating cells, are disclosed. The hydrophobic weak base compound and a wavelength of illumination are selected such that the hydrophobic weak base compound acts as a therapeutically effective photosensitizer when exposed to the illumination.

Abstract: The present invention relates to compounds of the Formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, X1, X2, X3 and X4 have the meanings indicated in the claims, and which are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb), and are suitable, for example, for the therapy and prophylaxis of athero-thrombotic diseases. The invention furthermore relates to processes for the preparation of compounds of the Formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.

Abstract: The invention concerns the use of cyclophilin inhibitors in the treatment of Hepatitis B and Hepatitis D virus infections.

Abstract: The present invention provides antiviral compounds of formula (I), as well as pharmaceutical compositions comprising these compounds, methods for synthesizing these compounds and methods of using these compounds for treating a viral infection.

Abstract: The present invention discloses the structure, preparation methods and uses of a series of novel polyheterocyclic based compounds (Ia-Ib and IIa-IIb) that are highly effective for inhibiting hepatitis C virus (HCV): where the structural variables are defined herein. The present invention is also provides a method of treating HCV infection by the polyheterocyclic based HCV inhibitory compounds, compositions and therapeutic methods.

Abstract: A cyclosporin derivative of general Formula (I) or a pharmaceutically compatible salt thereof, which have a pharmaceutical effectiveness, for example in the case of chronic inflammatory diseases. The cyclosporin derivatives are preferably free from a peptide section capable of passing through the membrane of a biological cell.

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 subject application pertains to a compound of structure IX or X: or a pharmaceutically acceptable salt thereof, wherein: X is —C(?O)N(R10)— or —CH(OPr3) —; R7, R9 and R10 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid; Pr1 and Pr2 are the same or different and represent hydrogen or a thiol protecting group; Pr3 is hydrogen or an alcohol protecting group; R1, R2, R5 and R6 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid, or R1 and R2 and/or R5 and R6, taken together with the carbon atom to which they are attached, form a spirocyclic moiety, with the proviso that: each of R1 and R2 is not hydrogen, or each of R5 and R6 is not hydrogen.

Abstract: Provided are methods and compositions for the prevention and/or treatment of viral conditions, virally-induced conditions and inflammatory conditions. The methods can comprise administering to a subject a viral inducing agent with an antiviral agent, and optionally an additional agent. The viral inducing agent can be a HDAC inhibitor administered orally.

Abstract: The invention discloses highly purified daptomycin and to pharmaceutical compositions comprising this compound. The invention discloses a method of purifying daptomycin comprising the sequential steps of anion exchange chromatography, hydrophobic interaction chromatography and anion exchange chromatography. The invention also discloses a method of purifying daptomycin by modified buffer enhanced anion exchange chromatography. The invention also discloses an improved method for producing daptomycin by fermentation of Streptomyces roseosporus. The invention also discloses high pressure liquid chromatography methods for analysis of daptomycin purity. The invention also discloses lipopeptide micelles and methods of making the micelles. The invention also discloses methods of using lipopeptide micelles for purifying lipopeptide antibiotics, such as daptomycin. The invention also discloses using lipopeptide micelles therapeutically.

Abstract: Methods and compositions for treating bedwetting are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising one or more analgesic agents.

Abstract: In some aspects, the present invention provides methods treating a subject in need of treatment for chronic rhinosinusitis or nasal polyposis, the methods comprising administering a complement inhibitor such as a compstatin analog to the subject. In some embodiments, the complement inhibitor is administered intranasally, e.g., in a nasal spray.

Abstract: The present invention relates to a new compound useful as a modulator of melanocortin receptors. In particular, the present invention relates to a compound WS727713, a process for production of the compound by culturing, in a culture medium, a WS727713-producing strain belonging to Pseudonocardia and recovering the compound from a culture broth, a pharmaceutical composition containing the compound, and uses of the compound.

Abstract: A class of macrocyclic compounds of formula (I), wherein R1, R3, R4, Ra, Rb, A, B, Z, M, W and n are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection.

Abstract: The present invention provides inventive stitched polypeptides, pharmaceutical compositions thereof, and methods of making and using inventive stitched polypeptides.

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: The invention provides (i) a method of treating metabolic syndrome in an animal, (ii) a method of suppressing the appetite of an animal, (iii) a method of treating obesity in an animal, (iv) a method of reducing the weight of an animal in need thereof, (v) a method of reducing a blood lipid level in an animal in need thereof, (vi) a method of treating non-alcoholic steatohepatitis in an animal, and (vii) a method of inhibiting adipogenesis. The methods comprise administering an effective amount of an active ingredient, wherein the active ingredient comprises a diketopiperazine, a prodrug of a diketopiperazine or a pharmaceutically-acceptable salt of either of them to the animal. The invention also provides a kit comprising a container holding a diketopiperazine, a prodrug of a diketopiperazine or a pharmaceutically-acceptable salt of either of them; and instructions for administration of the diketopiperazine, the prodrug or the pharmaceutically-acceptable salt according to a method of the invention.

Abstract: The present invention relates to novel peptides and to topical and food compositions comprising them. The novel peptides have applications in skin lightening and immunomodulation when applied topically and to immunomodulation and modulation of body mass when consumed in food compositions.

Abstract: Cyclic constructs with an N-terminus and a C-terminus which bind to a natriuretic peptide receptor and include a plurality of amino acid residues, at least one amino acid surrogate of formula I: where R, R?, Q, Y, W, Z, J, x and n are as defined in the specification, and optionally at least one prosthetic group, pharmaceutical compositions including such cyclic constructs, and methods of treating congestive heart failure or other conditions, syndromes or diseases for which induction of anti-hypertensive, cardiovascular, renal or endocrine effects are desired.

Abstract: Melanocortin receptor-specific cyclic peptides of the formula where R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the specification, compositions and formulations including the peptides of the foregoing formula or salts thereof, and methods of preventing, ameliorating or treating melanocortin-1 receptor-mediated or responsive diseases, indications, conditions and syndromes.

Abstract: A composition comprising from about 0.001% to about 0.4% cyclosporin A, a surfactant, and an oil having a specific gravity from 0.8 to 0.95 is disclosed herein.

Abstract: Methods for use of a melanocortin receptor agonist cyclic peptide of the formula where R, x and y are as defined in the specification, and compositions and formulations including the peptide of the foregoing formula, for preventing, ameliorating or treating female sexual dysfunction.

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: The invention provides tight junction protein modulators, compositions comprising the same, and uses thereof. In particular, the invention provides tight junction protein modulators that modulate the second extracellular loop of tight junction proteins, such as occludin or claudin.

Abstract: Compositions are provided which stimulate bone growth. Also provided are methods for utilizing the compositions for filling in bone defects, promoting rapid fusion of bone fractures, grafts, and bone-prostheses, and promoting strengthening of osteoporotic bones.

Abstract: A composition is disclosed herein comprising from about 0.001% to about 0.

Abstract: Provided herein are peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.

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 provides peptides and peptide conjugates for treating inflammatory bowel diseases, including ulcerative colitis and Crohn's disease. The peptides are derived from annexin-1, can be acetylated or conjugated to fatty acids, may be linear or cyclic, and may comprise D amino acids. Pharmaceutical compositions and methods of use are also disclosed.

Abstract: The invention relates to tumour therapy. In one aspect, the present invention relates to conjugates of an amatoxin and a target-binding moiety, e.g. an antibody, connected by a linker comprising a urea moiety, which are useful in the treatment of cancer. In a further aspect the invention relates to pharmaceutical compositions comprising such conjugates.

Abstract: The present invention relates to novel octapeptide compounds of general formula (I), R-AA1-cyclo(AA2-Tyr3-D-Trp4-AA5-Val6-Cys7)-Thr8-NH2??(I) As these products have a good affinity for certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) of the somatostatin receptors is (are) involved. The invention also relates to pharmaceutical compositions containing said products and their use for the preparation of a medicament.

Abstract: A composition comprising a therapeutically effective amount of cyclosporin A, a blend of oils having a specific gravity of from 0.90 to 1.07, and a surfactant is disclosed herein.

Abstract: Oligonucleotide analogues are provided that incorporate 5-aza-cytosine in the oligonucleotide sequence, e.g., in the form of 5-aza-2?-deoxycytidine (decitabine) or 5-aza-cytidine. In particular, oligonucleotide analogues rich in decitabine-deoxyguanosine islets (DpG and GpD) are provided to target the CpG islets in the human genome, especially in the promoter regions of genes susceptible to aberrant hypermethylation. Such analogues can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position. Methods for synthesizing these oligonucleotide analogues and for modulating nucleic acid methylation are provided. Also provided are phosphoramidite building blocks for synthesizing the oligonucleotide analogues, methods for synthesizing, formulating and administering these compounds or compositions to treat conditions, such as cancer and hematological disorders.

Abstract: Methods for treating cancer (e.g., metastatic cancer to the lung or chronic lymphocytic leukemia) in patients are described that include administrating an aerosolized granulocyte macrophage colony stimulating factor to the patients. Methods for stimulating an immune response in patients also are described.