Abstract: The present invention relates to a small animal model useful in identifying novel therapies for treating pathogenic diseases. This flexible biotechnology tool is valuable for developing novel chemotherapeutics for a broad range of microbial pathogens.

Abstract: The present invention provides glycorandomaized structures and combinatorial methods for rapidly generating a diverse library of glycorandomized structures, comprising incubating one or more aglycons and a pool of NDP-sugars in the presence of a glycosyltransferase. The glycosyltransferase may be one that is associated with or involved in production of natural secondary metabolites, or one which is putatively associated with or involved in production of natural secondary metabolites. The glycosyltransferase may show significant flexibility with respect to its NDP-sugar donors and/or its aglycons. NDP-sugar donors may be commercially available, or may be produced by utilizing mutant or wild type nucleotidyltransferases significant flexibility with respect to their substrates.

Abstract: Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R1, R2 or R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein Q1 and Q2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: Compounds and methods for use in selectively inhibiting a lytic enzyme based on feedback inhibition are described. The conjugated compound serves as a substrate for a lytic enzyme. Cleavage of the conjugated compound by the lytic enzyme releases an inhibitor of the enzyme.

Abstract: Compounds that are adjuvants and immunoeffectors are described and claimed. The compounds augment antibody production in immunized animals as well as stimulate cytokine production and activate macrophages. Compositions and methods for using the compounds as adjuvants and immunoeffectors are also disclosed.

Abstract: The present invention concerns methods and compositions for delivery of therapeutic agents to target cells, tissues or organisms. In preferred embodiments, the therapeutic agents are delivered in the form of therapeutic-loaded polymers that may comprise many copies of one or more therapeutic agents. In more preferred embodiments, the polymer may be conjugated to a peptide moiety that contains one or more haptens, such as HSG. The agent-polymer-peptide complex may be delivered to target cells by, for example, a pre-targeting technique utilizing bispecific or multispecific antibodies or fragments, having at least one binding arm that recognizes the hapten and at least a second binding arm that binds specifically to a disease or pathogen associated antigen, such as a tumor associated antigen. Methods for synthesizing and using such therapeutic-loaded polymers and their conjugates are provided.

Abstract: A drug using the magnetic properties of a metal salen complex as represented by the following general formula in order to magnetize the intended drug by chemically binding the drug to a metal salen complex so that the drug can be delivered to the target diseased site. The drug can be delivered to the diseased site using the magnetic properties of the drug per se without using a carrier made of a magnetic substance as in the conventional methods.

Abstract: New devices and methods for diagnosis and compositions and methods for treatment of cancers use combinations of antimicrobial agents and agents that can reverse dormancy and hibernation pathways. We unexpectedly found that surprisingly low doses of anti-hibernation compounds can substantially inhibit cancer cell growth in vitro and can successfully treat cancers, including metastatic cancer. We also unexpectedly found that antimicrobial agents and anti-HDS compounds together can increase the degree of inhibition of cancer cell growth in a synergistic fashion. We conclude that combination therapy with antimicrobial agents and anti-HDS compounds can be effective in treating human patients with cancer.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: An antibacterial agent having high antibacterial activity against Mycobacterium avium subsp. paratuberculosis is provided. Specifically, the antibacterial agent of the present invention having high antibacterial activity against Mycobacterium avium subsp. paratuberculosis is a caprazamycin derivative represented, for example, by the following general formula (II): wherein Me is a methyl group; and R1 is a straight or substantially straight chain alkyl group having 5 to 21 carbon atoms, a straight or substantially straight chain alkenyl group having 5 to 21 carbon atoms, a cycloalkyl group having 5 to 12 carbon atoms, or a phenyl group substituted at the para-position with a straight chain alkyl group having 1 to 14 carbon atoms, a straight chain alkoxy group having 1 to 9 carbon atoms or a cycloalkyl group having 5 to 12 carbon atoms.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Z1, Z2, Z3, Z4, R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: Disclosed are methods of treating bacterial infections including those caused by multidrug resistant bacteria using polyamine efflux pump inhibiting compounds, including for example N-benzylated polyazaalkanes, N-benzylated polyaminoalkanes, or mixed N-benzylated poly(aza/amino)alkanes, optionally in combination with other drugs such as antibiotics, as well as pharmaceutical compositions thereof.

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

Abstract: The dimerization of HIV RNA is a key step in the virus replication cycle. Based on RNA DIS crystal structures, a novel kind of compounds, dimeric or not, based on neamine was designed and synthesized. Biological studies showed that such compounds bind and interfere with the targeted RNA sequence, opening a new anti-HIV approach. The crystal structures and bio-chemical experiments showed that the DIS of HIV-1 genomic RNA is a target for new anti-HIV drugs and that those drugs could be derived from aminoglycosides. The results revealed that binding of aminoglycosides to the DIS is specific regarding both the aminoglycoside family and the RNA subtype.

Abstract: Disclosed is a method of diagnosing irritable bowel syndrome, fibromyalgia, chronic fatigue syndrome, depression, attention deficit/hyperactivity disorder, autoimmune diseases, such as multiple sclerosis and systemic lupus erythematosus, or Crohn's disease, which involves detecting the presence of small intestinal bacterial overgrowth (SIBO) in a human subject having at least one symptom associated with a suspected diagnosis of any of those diagnostic categories. Also disclosed is a method of treating these disorders, and other disorders caused by SIBO, that involves at least partially eradicating a SIBO condition in the human subject. The method includes administration of anti-microbial or probiotic agents, or normalizing intestinal motility by employing a prokinetic agent. The method improves symptoms, including hyperalgesia related to SIBO and disorders caused by SIBO.

Abstract: The present invention relates to a diaryl hepatonoid-based compound of formula (1) having viral inhibitory activity; its pharmaceutically acceptable salt; or a hydrate, a solvate or a prodrug of any of the foregoing, and a pharmaceutical composition comprising the same, and the use thereof therapeutic agents. The diaryl hepatonoid-based compounds according to present invention have an excellent effect of inhibiting viral activity, and thus will be useful as therapeutic agents against virus-related diseases.

Abstract: An oligo-aminosaccharide compound formed by binding 3 to 6 saccharides, such as 2,6-diamino-2,6-dideoxy-?-(1?4)-D-glucopyranose oligomers, or a salt thereof, which has high affinity to a double-stranded nucleic acid.

Abstract: We describe the functional cloning and the use of a non-fungal inositol phosphoryceraminde synthase (IPC synthase) in a screening assay for the identification of agents that target and antagonize the activity of IPC synthase.

Abstract: An aqueous or powder composition includes anti-gram-negative antibiotic or salt thereof being present at an amount ranging from about 100 mg/ml to about 200 mg/ml. Another aqueous or powder composition includes anti-gram-positive antibiotic or salt thereof being present at a concentration ranging from about 0.6 to about 0.9 of the water solubility limit, at 25° C. and 1.0 atmosphere, of the anti-gram-positive antibiotic or salt thereof. Other embodiments include unit doses, kits, and methods.

Abstract: This present provides kaempferol-3-(2-E,3-Z-di-p-coumaroyl)-rhamnoside, kaempferol-3-(2-Z-3-E-di-p-coumaroyl)-rhamnoside, and kaempferol-3-(2,3-di-Z-p-coumaroyl)-rhamnoside compounds useful as a new class of anti-bacterial agents. These compounds are extracted from Platanus occidentalis or Laurus nobilis. These compounds were found to exhibit anti-bacterial activity against methicillin resistant Staphylococcus aureus (MRSA).

Abstract: The present invention provides aminoglycosides and pharmaceutical compositions that include the aminoglycosides. The aminoglycosides are useful to treat or prevent infectious diseases (e.g., bacterial infections) in a mammal (e.g., human).

Abstract: A dicarboxylic acid compound obtainable by oxidative degradation of pradimicin antibiotics, which are antibiotics consisting of the benzonaphthacene skeleton, a D-amino acid side chain and a sugar chain, for the second saccharide residue of the sugar chain, and use thereof utilizing a specific microorganism binding property thereof are provided. The dicarboxylic acid compound has significantly improved water-solubility compared with the raw material antibiotics, whist maintaining the specific microorganism binding property.

Abstract: The present invention provides compounds characterized by the formula (I), where each of the substituent radicals is described in the specification. The invention also describes the use of said compounds in the treatment of various diseases, including: cancer or tumoral processes in general, Paget's disease, hypercalcaemia, hypercalciuria and neurological diseases (inter alia, Parkinson's, Alzheimer's, Huntington's).

Abstract: Spinetoram is selectively produced in excellent yields by hydrogenating a mixture of 3?-O-ethyl spinosyn J and 3?-O-ethyl spinosyn L in a water miscible organic solvent using hydrogen gas and a heterogeneous catalyst.

Abstract: This invention describes processes for the convergent synthesis of calicheamicin derivatives, and similar analogs using bifunctional and trifunctional linker intermediates.

Abstract: The present invention relates to novel inhibitors of aminoglycoside 6?-N-acetyltransferases, more specifically, AAC(6?)-li and AAC(6?)-ly, as well as compositions and uses thereof. Furthermore, the present invention relates to synthetic methodologies for preparing the inhibitors of aminoglycoside 6?-N-acetyltransferases.

Abstract: An aqueous or powder composition includes anti-gram-negative antibiotic or salt thereof being present at an amount ranging from about 100 mg/ml to about 200 mg/ml. Another aqueous or powder composition includes anti-gram-positive antibiotic or salt thereof being present at a concentration ranging from about 0.6 to about 0.9 of the water solubility limit, at 25° C. and 1.0 atmosphere, of the anti-gram-positive antibiotic or salt thereof. Other embodiments include unit doses, kits, and methods.

Abstract: Disclosed is a method of diagnosing irritable bowel syndrome, fibromyalgia, chronic fatigue syndrome, depression, attention deficit/hyperactivity disorder, autoimmune diseases, such as multiple sclerosis and systemic lupus erythematosus, or Crohn's disease, which involves detecting the presence of small intestinal bacterial overgrowth (SIBO) in a human subject having at least one symptom associated with a suspected diagnosis of any of those diagnostic categories. Also disclosed is a method of treating these disorders, and other disorders caused by SIBO, that involves at least partially eradicating a SIBO condition in the human subject. The method includes administration of anti-microbial or probiotic agents, or normalizing intestinal motility by employing a prokinetic agent. The method improves symptoms, including hyperalgesia related to SIBO and disorders caused by SIBO.

Abstract: The present invention relates to media containing purified antimicrobial polypeptides, such as defensins, and/or cell surface receptor binding proteins. The media may also contain buffers, macromolecular oncotic agents, energy sources, impermeant anions, ATP substrates. The media find use for the storage and preservation of internal organs prior to transplant.

Abstract: An antibacterial agent having high antibacterial activity against Mycobacterium avium subsp. paratuberculosis is provided. Specifically, the antibacterial agent of the present invention having high antibacterial activity against Mycobacterium avium subsp. paratuberculosis is a caprazamycin derivative represented, for example, by the following general formula (II): wherein Me is a methyl group; and R1 is a straight or substantially straight chain alkyl group having 5 to 21 carbon atoms, a straight or substantially straight chain alkenyl group having 5 to 21 carbon atoms, a cycloalkyl group having 5 to 12 carbon atoms, or a phenyl group substituted at the para-position with a straight chain alkyl group having 1 to 14 carbon atoms, a straight chain alkoxy group having 1 to 9 carbon atoms or a cycloalkyl group having 5 to 12 carbon atoms.

Abstract: A conjugate of formula: V—(Y)a-Z-T??(I), T-X—B—(Y)a-Z-T???(II), V—(Y)a-Z-(Y?)a—V???(III), T-X—B—(Y)a-Z-(Y?)a—X?—B?-T???(IV), V—(Y)a-Z-(Y?)a—X—B-T??(V), V—(Y)a-Z-X—B-Z?-(Y?)a—(V?)b??(VI), or (W)a—(Y)b-[(Z)c-(Y?)d—(X—B)e—(Y?)f-(Z?)g]h-(Y??)i—(W?)j??(VII), in which W and W? are independently a DNA intercalator or terminal subunit, V and V? are independently a DNA intercalator, X and X? are independently a DNA alkylator, B and B? are the same or different and each is a heteroaromatic residue that is attached to the N-terminus of an alkylator subunit (X or X?), Y, Y?, Y? and Y?? are independently a linker, T and T? are independently terminal subunits, Z and Z? are independently a polyamide group that binds to the minor groove of DNA, a, b, c, d, f, g, i, and j are independently 0 to 5, and e and h are independently 1 to 5, a composition comprising a conjugate of any of formulae (I)-(VII) and a carrier, and a method for treating cancer in a mammal comprising administering an effective amount of

Abstract: Caprazene and caprazol could be synthesized by hydrolysis of a caprazamycin. There could be synthesized a caprazene-1??-amide derivative of the formula (II) and a caprazene-1??-ester derivative of the formula (III) from caprazene. Further, there could be synthesized a caprazol-1??-amide derivative of the formula (V) and a caprazol-1??-amide-3??-ester derivative and a caprazol-3??-ester derivative, etc. from caprazol. Furthermore, an imidazolidinone derivative could be synthesized from the ring-opened product of the 1,4-diazepinone ring of caprazol. The novel caprazene derivative, novel caprazol derivative and novel imidazolidinone derivative now synthesized exhibit excellent antibacterial activities against a variety of bacteria, including acid-fast bacteria.

Abstract: The invention relates to an antibiotic substances of microbial origin, arbitrarily denominated antibiotic GE 81112 factor A, factor B1 and factor B, which is produced by fermentation of Streptomyces sp. DSMZ 14386, the pharmaceutically acceptable salts and compositions thereof, and their use as an antibacterial agent having inhibitory activity versus susceptible microbes.

Abstract: The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.

Abstract: A medicament for treating cancer for use in combination therapy with an anti-HER2 antibody, which comprises amrubicin or a pharmaceutically acceptable salt thereof as an active ingredient.

Abstract: Disclosed are processes for preparing glycopeptide phosphonate derivatives having an amino-containing side chain. Several of the process steps are conducted in a single reaction vessel without isolation of intermediate reaction products, thereby generating less waste and improving the overall efficiency and yield of the process.

Abstract: A monosaccharide compound of formula I as shown in the specification. Processes for the preparation of the compound of formula I and methods of screening for antibacterial or antibiotic compounds involving the compound of formula I.

Abstract: The invention relates to an antibiotic substances of microbial origin, arbitrarily denominated antibiotic GE 81112 factor A, factor B1 and factor B, which is produced by fermentation of Streptomyces sp. DSMZ 14386, the pharmaceutically acceptable salts and compositions thereof, and their use as an antibacterial agent having inhibitory activity versus susceptible microbes.

Abstract: This invention relates to a new class of polyene polyketides, their pharmaceutically acceptable salts and derivatives, and to methods for obtaining the compounds. One method of obtaining these compounds is by cultivation of novel strains of Streptomyces aizunensis; another method involves expression of biosynthetic pathway genes in transformed host cells. The present invention further relates to the novel strains of Streptomyces aizunensis used to produce these compounds, to the use of these compounds and their pharmaceutically acceptable salts and derivatives as pharmaceuticals, in particular to their use as inhibitors of fungal cell growth and cancer cell growth. The invention also relates to pharmaceutical compositions comprising these novel polyketides or a pharmaceutically acceptable salts or derivatives thereof. Finally, the invention relates to novel polynucleotide sequences and their encoded proteins, which are involved in the biosynthesis of these novel polyketides.

Abstract: The invention relates to novel paranmycin compounds that have activity against gram positive and gram negative bacteria, preferably bacteria that are resistant to other antibiotics.

Abstract: The inventive polypeptide is embodied in the form of a similar fragment of the epidermal growth factor of aminoacid ranging from 21 to 31 and capable of efficiently binding with the receptor of the epidermal growth factor as a vector for the directed supply of anticancer agent to tumour cells. The inventive conjugate of said polypeptide contains doxorubicine and has a selective action on cancer tumours and can substantially reduce the resistance of tumour cells with respect to the anticancer agents, the conjugated parts of said agents being binded with the aid of a chemical bond which is unstable in relation to acid hydrolysis. The inventive pharmaceutical composition comprises an efficient quantity of conjugate and a carrier which is fit for intravenous injection. Said invention can be used for medicine for treating cancer patients.

Abstract: The invention relates to a method for the antibiotic coating of bodies with interconnecting microcavities as well as bodies coated this way and their usage.

Abstract: The present invention provides vancomycin analogs and methods related to synthesis of these analogs via chemoenzymatic techniques.

Abstract: The present invention relates to aminoglycoside compounds having antibiotic activity. Moreover, the present invention relates to L-aminoglycoside compounds and diastereomers thereof which posses antibiotic activity and are not susceptible to development of resistant bacterial strains. The present invention also relates to methods of treatment and pharmaceutical compositions that utilize or comprise one or more of aminoglycoside compounds provided by the invention.

Abstract: The present invention relates to glycosyl-etoposide prodrugs, a process for the preparation thereof and the use thereof in combination with functionalized tumor-specific enzyme conjugates for treating cancers.

Abstract: The present invention provides aminoglycosides and pharmaceutical compositions that include the aminoglycosides. The aminogylcosides are useful to treat or prevent infectious diseases (e.g., bacterial infections) in a mammal (e.g., human).

Abstract: Screening procedures are disclosed for identifying compounds useful for inhibiting infection or pathogenicity. Methods are also disclosed for identifying pathogenic virulence factors.