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

Abstract: The present invention relates to compounds that are cationic vancomycin analogues and their compositions. Method of making the compounds and their use as medicament for the treatment of bacterial infection are also disclosed.

Abstract: The present invention relates to cyclic cationic peptides and their use in the treatment of microbial infections.

Abstract: Provided herein are methods of treating a superbug infection in a subject that include administering to the subject a therapeutically effective dose of ramoplanin in combination with a therapeutically effective dose of one or more rhamnolipids, thereby treating the superbug infection. The superbug may be vancomycin-resistant Enterococcus, Clostridium difficile, or multidrug-resistant Clostridium difficile. The one or more rhamnolipids may include monorhamnolipid Rha-C10-C10, dirhamnolipid Rha-Rha-C10-C10, or monorhamnolipid Rha-C10-C10 and dirhamnolipid Rha-Rha-C10-C10. Also disclosed are pharmaceutical compositions that include ramoplanin, one or more rhamnolipids, and a pharmaceutically acceptable carrier, as well as formulations for preventing superbug infection.

Abstract: The invention discloses silaanalogs of oxazolidinone compounds, to pharmaceutical compositions and to the synthesis of the oxazolidinone derivatives of formula I. The invention further relates to methods of treating a subject suffering with gram positive pathogens including those resistant to methicillin and vancomycin using the compound(s) or modulation of coagulation properties of blood-clotting cascade or compositions of the oxazolidinone derivatives of the invention.

Abstract: Embodiments include methods for generating a metabolite profile of a stool sample and methods of assessing the status of a subject using the metabolic profile derived from a stool sample.

Abstract: The present invention relates to crystalline and crystal-like forms of lipopeptides, including daptomycin, a lipopeptide antibiotic with potent bactericidal activity against gram-positive bacteria, including strains that are resistant to conventional antibiotics. The present invention relates to methods of purifying lipopeptides, including daptomycin, a lipopeptide antibiotic with potent bactericidal activity against gram-positive bacteria, including strains that are resistant to conventional antibiotics. The present invention also relates to pharmaceutical compositions comprising the purified form of the lipopeptide and methods of using these compositions.

Abstract: Compositions that include antimicrobial agents and biodegradable delivery vehicles adapted to enter a cell and release the antimicrobial agents in the cell as they biodegrades. Also provided are compositions that include first and second delivery vehicles including first and second antimicrobial agents, wherein the first delivery vehicles are adapted to release the first antimicrobial agents at a rate that differs from that at which the second delivery vehicles release the second antimicrobial agents, articles of manufacture that include one or more biodegradable delivery vehicles, and methods of making and using the compositions to treat intracellular and/or extracellular infections are disclosed.

Abstract: The present disclosure provides novel powder daptomycin formulations which have improved chemical stability and faster reconstitution times when in the solid state. Some examples of the compositions comprise daptomycin and sucrose.

Abstract: Modified green tea polyphenols and methods of their use are provided. One aspect provides compounds and compositions containing green tea polyphenols with one on more ester-linked fatty acids.

Abstract: A hydrogel (I), comprising a polymer backbone wherein an aqueous solution of the hydrogel comprises a first lower critical solution temperature, and wherein the hydrogel is configured to be converted in vivo into a modified hydrogel, and wherein an aqueous solution of the modified hydrogel comprises a second lower critical solution temperature, and wherein the second lower critical solution temperature is greater than the first lower critical solution temperature.

Abstract: Novel peptoid oligomers are disclosed that have a formula represented by the following formula I: The peptoids demonstrate antimicrobial activity and may be prepared as pharmaceutical compositions and used for the prevention or treatment of a variety of conditions in mammals including humans where microbial invasion is involved. The present cyclic and linear peptoids are particularly valuable as their effect is rapid, broad in spectrum and mostly indifferent to resistance provoked by standard antibiotics.

Abstract: The invention provides bipartite inhibitors of bacterial RNA polymerase having the general structural formula (I): X-?-Y (I) wherein X is an moiety that binds to the rifamycin binding site of a bacterial RNA polymerase, Y is a moiety that binds to the GE23077 binding site of a bacterial RNA polymerase, and is a linker. The invention also provides compositions comprising such compounds, methods of making such compounds, and methods of using said compounds. The invention has applications in control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, and antibacterial therapy.

Abstract: The present invention relates to cyclic cationic peptides and their use in the treatment of microbial infections.

Abstract: The invention describes a pharmaceutical composition to combat multiple-drug-resistant bacteria in non-ocular infective conditions. Compositions comprising glycopeptides, in particular vancomycin, and cephalosporins, in particular ceftriaxone, are disclosed. Such compositions are found to be useful for parenteral administration for hospitalized patients with serious infections. Specifically, this invention also discloses a pharmaceutical composition further including an excipient such as CVMC agent and is available in dry powder form for reconstitution before injection with a suitable solvent. The pharmaceutical compositions of this invention have been found normally to enhance resistance to precipitation in solutions to be administered parenterally. The invention also gives details of the dosage forms stored in sealed containers to be reconstituted before use.

Abstract: The present invention relates generally to novel depsipeptides, to methods for the preparation of these novel depsipeptides, to pharmaceutical compositions comprising the novel depsipeptides; and to methods of using the novel depsipeptides to treat or inhibit various disorders.

Abstract: A compound having the general structure R1, R2, R3 and R4 being selected from the group consisting of a hydrogen atom (H) and a C1-C20 alkyl, and R5 being a phenyl radical.

Abstract: A composition suitable for application to the skin comprising at least one lantibiotic, an acidic external phase aqueous solution, at least one pharmaceutically acceptable internal phase carrier material, and a combination thereof. A method for preventing or treating mastitis, comprising administering to a human in need of such treatment a topical composition comprising a therapeutically-effective amount of at least one lantibiotic, an acidic aqueous solution, and at least one pharmaceutically acceptable carrier material.

Abstract: The invention relates to a compound of the general structure (I), where R is a hydrogen atom (II) or an unsubstituted, monosubstituted or polysubstituted C1-C20-alkyl, wherein the alkyl is straight, branched, cyclic and/or partially unsaturated, or an unsubstituted, monosubstituted or polysubstituted phenyl group.

Abstract: The present disclosure provides compositions comprising fatty acids, or derivatives thereof (e.g., C1-C4 esters) including, for example, DGLA, 15-OHEPA and/or 15-HETrE, used alone or in combination with one or more antibiotic agents for the treatment of disease and/or disorders such as a skin infection or wound healing.

Abstract: The invention features vancomycin class compounds modified to be suitable for oral delivery or to possess increased antimicrobial potency, formulations for the oral administration of vancomycin class compounds, and synthetic methods for making vancomycin class compounds.

Abstract: The invention provides compounds of formula (I): and salts thereof, wherein X and Y have any of the values defined herein. The compounds inhibit bacterial RNA polymerase, inhibit bacterial growth, and have applications in, analysis of RNA polymerase structure and function, control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, antibacterial therapy, and drug discovery.

Abstract: The invention provides bipartite inhibitors of bacterial RNA polymerase that contain: (i) a first moiety that binds to the salinamide binding site of a bacterial RNA polymerase; (ii) a second moiety comprising a nucleoside analog; and (iii) a linker connecting said first and second moieties.

Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

Abstract: The present invention relates to novel anti-TB cyclic peptides from Nonomuraea sp. MJM5123, a process for the production of the anti-Tuberculosis peptide and a pharmaceutical composition for the prevention and treatment of mycobacterial infection comprising the same. The composition of the present invention is highly active against replicating/non-replicating M. tuberculosis, including MDR and XDR strains, so that it can be effectively used as a therapeutic agent for tuberculosis.

Abstract: Compounds of formula (IV) and pharmaceutical compositions comprising the same are described, wherein X1 and X2, R3, L, Ar1, p and Z have the values disclosed herein.

Abstract: The present disclosure relates to pyrazine compounds of formula I: wherein L, n, R1, and R2 are as described in the specification. These compounds are useful as inhibitors of ATR protein kinase. The disclosure also relates to pharmaceutically acceptable compositions comprising the compounds of the disclosure; methods of treating of various diseases, disorders, and conditions using the compounds of the disclosure; processes for preparing the compounds of the disclosure; intermediates for the preparation of the compounds of the disclosure; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.

Abstract: The present invention relates to crystalline and crystal-like forms of lipopeptides, including daptomycin, a lipopeptide antibiotic with potent bactericidal activity against gram-positive bacteria, including strains that are resistant to conventional antibiotics. The present invention relates to methods of purifying lipopeptides, including daptomycin, a lipopeptide antibiotic with potent bactericidal activity against gram-positive bacteria, including strains that are resistant to conventional antibiotics. The present invention also relates to pharmaceutical compositions comprising the purified form of the lipopeptide and methods of using these compositions.

Abstract: The present invention relates to the field of bacteriology. In particular, the present invention provides compositions (e.g., comprising a lantibiotic and mupirocin or gentamicin) and methods of treating (e.g., killing or inhibiting growth of) bacteria. For example, the present invention provides pharmaceutical compounds (e.g., comprising a lantibiotic and mupirocin or gentamicin) and methods of using the same in research, therapeutic and drug screening applications.

Abstract: Glycopeptide antibiotics, such as oritavancin, demonstrate significant activity against both a vegetative form of C. difficile and C. difficile spores. Methods for the treatment, prophylaxis and prevention of C. difficile infection and disease in animals, including humans, are described.

Abstract: The present invention concerns novel lantibiotic compounds, processes for the isolation and preparation thereof, pharmaceutical compositions containing the same, pharmaceutical acceptable salts thereof, and methods of use of the lantibiotics as antibacterial agents.

Abstract: Provided herein are inventive enopeptin compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Further provided are methods of preparation, use, and treatment.

Abstract: The present invention provides novel cyclosporin analogue compounds, pharmaceutical compositions comprising these compounds and methods of using these compounds for the treatment of disorders and diseases, including immune disorders, inflammatory disorders and viral infections.

Abstract: The present invention relates to a polymyxin derivative wherein R1, R2 and R3 are optional and R1, R2, R3, R5, R8 and R9 are cationic or neutral amino acid residues selected so that the total number of positive charges at physiological pH is at least two but no more than three; and to a combination product comprising at least two such derivatives.

Abstract: Provided herein are novel compounds and novel protected compounds that can be derived from polymyxin, including, e.g., polymyxin A. The novel compounds have antibacterial properties against a diverse range of Gram negative bacteria and reduced toxicity compared to polymyxins such as polymyxin A. Also provided are antibacterial pharmaceutical compositions containing the novel compounds and novel protected compounds, as well as methods for preparing the antibacterial compounds and protected compounds.

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: A tissue adhesive including cyanoacrylate and polyethylene glycol (PEG), wherein the PEG remains a polyether and wherein the tissue adhesive is bioabsorbable. A tissue adhesive including cyanoacrylate bulk monomer and cyanoacrylate nanoparticles containing a therapeutic therein. A kit for applying tissue adhesive, including the tissue adhesive described above and an applicator. Methods of accelerating degradation of a cyanoacrylate tissue adhesive applying a tissue adhesive, closing an internal wound, administering a therapeutic to tissue, treating cancer, and preventing infection in a wound. Methods of method of making a bioabsorbable tissue adhesive and making a therapeutic tissue adhesive.

Abstract: A product comprising at least one given antibiotic and a calixarene for use as medicament.

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: The present invention relates to methods of treating or preventing retinal ganglion cell (RGC) death and/or glaucoma using modulators of neurotrophic receptors that comprise ?-turn peptidomimetic cyclic compounds or derivatives thereof. The neurotrophic receptor modulators can be used alone, in combination and/or in conjunction with one or more other compounds, molecules or drugs that treat or prevent ocular hypertension, RGC death and/or glaucoma.

Abstract: The present invention relates to a polymyxin derivative wherein the derivative has a total of three positive charges at physiological pH and wherein the terminal moiety (D) of the derivative comprises a total of 1 to 5 carbon atoms. The invention also relates to a method of treating a subject for a gram-negative bacterial infection by administering a polymyxin derivative of the invention in combination with a second antibacterial agent. Finally, the invention relates to a process for preparing such polymyxin derivatives.

Abstract: Disclosed are a novel strain with antibacterial activity, identified as Streptomyces sp. AN1542 strain (Accession No.: KCTC 12113BP), an antibacterial composition comprising a compound represented by Chemical Formula 1 or 2, or a strain producing the same as an active ingredient, and a method for producing the same. Exhibiting potent antibacterial activity against pathogenic microbes and antibiotic-resistant microbes, particularly, MRSA, QRSA, VRSA and VRE, the compound or the strain of the present invention can be applied to the treatment of infectious diseases caused by superbacteria.

Abstract: A method of treatment of inflamed, pre-cancerous or cancerous tissue or polyps in a mammalian subject is disclosed. The treatment involves administration of a composition of at least one peptide agonist of a guanylate cyclase receptor and/or other small molecules that enhance intracellular production of cGMP. The at least one peptide agonist of a guanylate cyclase receptor may be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The inhibitor may be a small molecule, peptide, protein or other compound that inhibits the degradation of cGMP. Without requiring a particular mechanism of action, this treatment may restore a healthy balance between proliferation and apoptosis in the subject's population of epithelial cells, and also suppress carcinogenesis.

Abstract: The present invention relates to crystalline and crystal-like forms of lipopeptides, including daptomycin, a lipopeptide antibiotic with potent bactericidal activity against gram-positive bacteria, including strains that are resistant to conventional antibiotics. The present invention relates to methods of purifying lipopeptides, including daptomycin, a lipopeptide antibiotic with potent bactericidal activity against gram-positive bacteria, including strains that are resistant to conventional antibiotics. The present invention also relates to pharmaceutical compositions comprising the purified form of the lipopeptide and methods of using these compositions.

Abstract: Glycopeptide antibiotics, such as oritavancin, demonstrate significant activity against both a vegetative form of C. difficile and C. difficile spores. Methods for the treatment, prophylaxis and prevention of C. difficile infection and disease in animals, including humans, are described.

Abstract: Provided herein are novel compounds and novel protected compounds that can be derived from polymyxin, including, e.g., polymyxin B1 and [Ile7] polymyxin B1. The novel compounds have antibacterial properties against a diverse range of gram negative bacteria and reduced toxicity compared to polymyxins such as polymyxin B. Also provided are antibacterial pharmaceutical compositions containing the novel compounds and novel protected compounds, as well as methods for preparing the antibacterial compounds and protected compounds.

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: There is described a composition comprising a therapeutically active imidazole, and derivatives thereof, and an agent active on a bacterial cell surface selected from the group consisting of one or more of colistin, nisin, D-cycloserine, fosfomycin, fosfomycin trometamol, fosfomycin disodium and polymixin B, and derivatives thereof.

Abstract: This disclosure relates to methods for differentiating between mammals having active and latent Tuberculosis disease, by determining the percentage of polyfunctional CD4+ T-cells expressing TNF-alpha, IFN-gamma, and IL-2, or by determining expression of IL-17.

Abstract: Cyclic peptides having a random alternation of L-?-aminoacyl residues and aza-?3-aminoacyl residues and their uses.