Abstract: The invention discloses 20,23-modified novel derivatives of 16-membered demycarosyltylonolide antibiotics, which are useful against bacterial and mycoplasmic pathogens in humans and animals. Also claimed are pharmaceutical compositions of such derivatives and their use in treating bacterial and mycoplasmic infections in humans and animals.

Abstract: Provided are novel methods and formulations for orally controlling bot larvae in the gastrointestinal tract of equine animal using a spinosyn.

Abstract: The invention provides novel compounds and compositions and methods for making and using the compounds and compositions. In particular, the use of organic acid salts promotes solubility. These more soluble forms are suitable for use in various diseases, notably diseases of lung, muscle, metabolism and eyesight.

Abstract: Disclosed herein is an acrylic resin film having excellent heat resistance and mechanical strength, less fish-eyes, and high transparency. The acrylic resin film is obtained by molding a resin composition containing a glutarimide acrylic resin (G) and a (meth)acrylic resin (F) obtained by polymerization of a vinyl group-containing compound in the presence of alkyl acrylate-based cross-linked elastic particles having an average particle size of less than 80 nm.

Abstract: A method for changing a condition of an eyelid of a hairless animal, a model animal for evaluating a therapeutic or prophylactic effect against an eyelid disease obtained by the method, a method for producing the model animal, a method of screening using the model animal and a substance having a therapeutic or prophylactic effect against an eyelid disease selected by the method of screening, and a therapeutic or prophylactic agent against an eyelid disease containing the substance as an active ingredient.

Abstract: The present invention relates to a calixarene-based glycosylated compound (I) having the formula: (I) wherein D is independently selected in the group comprising a —CH2-group, an oxygen atom, a sulphur atom, a sulfinyl group or a sulfonyl group, E is independently selected in the group comprising a hydrogen, an alkyl having from 1 to 10 carbon atoms, an aryl having from 6 to 20 carbon atoms, a nitrogen dioxide group, an azide group, an amino group, a guanidinium group, a halogen atom, a —CH2 R group wherein R is a hydroxyl, a halogen, an amino group, a N(alkyl)2 group, a NH(alkyl) group, or E represents a —CO—R? wherein R? is a hydrogen atom, a hydroxyl group or an amino, B represents a A-C group wherein A is independently selected in the group comprising an oxygen atom, a sulfur atom, a NH group or a (CH2)i group, i being an integer from 1 to 10, C is independently selected in the group comprising a hydrogen, an alkyl, an alkenyl, an alkynyl, or C is a group of formula (II).

Abstract: The present invention relates to new macrolide derivatives, in particular new tylosin derivatives of the formula (I); a pharmaceutical or veterinary composition comprising the derivatives; a method for preparation thereof; a method for treating and/or preventing bacterial infections in an animal, wherein the method comprises administering the derivatives or the composition; and a use of the derivatives for the manufacture of medicaments for treating and/or preventing bacterial infections in an animal.

Abstract: The invention relates to novel forms of compounds displaying broad spectrum antibiotic activity, especially crystalline polymorphic forms and amorphous forms of such compounds, compositions comprising such crystalline polymorphic forms and amorphous forms of such compounds, processes for manufacture and use thereof. The compounds and compositions of the invention are useful in the pharmaceutical industry, for example, in the treatment or prevention of diseases or disorders associated with the use of antibiotics, chemotherapies, or antiviral therapies, including, but not limited to, colitis, for example, pseudo-membranous colitis; antibiotic associated diarrhea; and infections due to Clostridium difficile (“C. difficile”), Clostridium perfringens (“C. perfringens”), Staphylococcus species, for example, methicillin-resistant Staphylococcus, or Enterococcus including Vancomycin-resistant enterococci.

Abstract: The invention relates to macrolide compounds of formula (I), the use of said compounds as medicaments, in particular for the treatment or prevention of inflammatory and allergic diseases, pharmaceutical compositions containing said compounds and to processes for their preparation. The invention relates in particular to macrolide compounds with antiinflammatory activity mediated primarily through inhibition of phosphodiesterase 4 (PDE4) which makes them useful for the treatment and/or prevention of inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, atopic dermatitis or inflammatory bowel disease or proliferative diseases such as cancer.

Abstract: The invention relates to novel forms of compounds displaying broad spectrum antibiotic activity, especially crystalline polymorphic forms and amorphous forms of such compounds, compositions comprising such crystalline polymorphic forms and amorphous forms of such compounds, processes for manufacture and use thereof. The compounds and compositions of the invention are useful in the pharmaceutical industry, for example, in the treatment or prevention of diseases or disorders associated with the use of antibiotics, chemotherapies, or antiviral therapies, including, but not limited to, colitis, for example, pseudo-membranous colitis; antibiotic associated diarrhea; and infections due to Clostridium difficile (“C. difficile”), Clostridium perfringens (“C. perfringens”), Staphylococcus species, for example, methicillin-resistant Staphylococcus, or Enterococcus including Vancomycin-resistant enterococci.

Abstract: Methods, processes and materials for the production and recovery of Tiacumicins produced by culturing a microorganism belonging to the species Dactylosporangium aurantiacum subspecies hamdenensis having the ability to produce and accumulate one or more Tiacumicin in a nutrient medium comprising a carbon source, a nitrogen source, trace elements such as inorganic salts, and an adsorbent, wherein said nitrogen source comprises fish powder, and wherein said Tiacumicin is produced in a yield greater than about 50 mg/L broth.

Abstract: The present invention relates to the use of avermectin derivative as a drug for the treatment of parasitic infections. The avermectin derivative is represented by the formula (I) wherein: (i) R1 is chosen from the group constituted of —CH(CH3)2, —CH(CH3)CH2CH3, or cyclohexyle, (ii) X represents —CH2CH2—, or —CH?CH—, (iii) R2 is chosen from the group constituted of or —OH group, (iv) R3 is OH or NOH, (v) represents a single bond when R3 is OH, or a double bond when R3 is NOH, as an inhibitor of a membrane-bound protein which transports exogenous compounds out of target cells.

Abstract: The present invention provides a highly safe pharmaceutical composition for preventing and/or treating bone disease, a pharmaceutical preparation comprising thereof, a health food comprising thereof, a functional food comprising thereof. Since the present invention comprises the arylheptanoid compound shown in the following formula (I) and the derivatives thereof, it enables to prevent and/or treat the bone disease. (In the formula (I), R1 and R5 are a functional group selected from the group consisting of a hydrogen atom, alkyl group having carbon numbers 1 to 3, monosaccharide and disaccharide; R2, R3, and R4 are a functional group selected from the group consisting of a hydrogen atom, an oxygen atom, alkyl group having carbon numbers 1 to 3, monosaccharide and disaccharide; R5 may be bound on meta-position against heptylene group of another aryl group to form a ring.

Abstract: The present invention provides compositions, systems and methods for demulsifying an emulsion including an aqueous phase and an organic phase by adding an effective amount of a composition comprising at least one quaternary organopolysiloxane or salt thereof to the emulsion, the composition optionally including at least one of quaternary epihalohydrin/polyamine copolymers or salts, and/or (poly)diallyldimethylammonium halides.

Abstract: A method for reducing alcohol consumption in a subject includes a step of identifying a subject exhibiting at least one symptom of alcoholism and then administering a therapeutically effective amount of an Ivermectin analogue-containing composition to the subject. A method of screening Ivermectin analogues for reducing alcohol consumption is also provided.

Abstract: Disclosed are levoisovalerylspiramycin I, II or III, preparations, preparing methods and uses thereof. The preparations comprise levoisovalerylspiramycin I, II or III and pharmaceutically acceptable carrier and/or adjuvant, wherein the purity of levoisovalerylspiramycin I, II or III is above 90 wt %. The levoisovalerylspiramycin I, II or III has a good antibacterial activity, and the preparations include solution for injection, powder for injection or lyophilized powder for injection.

Abstract: The present invention relates to a prodrug, comprising a pharmaceutically and/or diagnostically active compound, and one or more bisphosphonate groups, to a process for producing such a prodrug, and to a pharmaceutical composition comprising said prodrug, to be used for the treatment of bone-related disorders such as bone cancer.

Abstract: The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

Abstract: The present invention provides solid state forms of Fidaxomycin, processes for preparing the solid state forms, as well as pharmaceutical compositions and formulations comprising one or more of the solid state forms of Fidaxomycin, and processes for the preparation of the compositions and formulations. The solid state forms of the present invention exhibit advantageous properties such as improved reliability and reproducibility in manufacturing and processing and stability in formulations.

Abstract: A method of treating a disease or disorder caused by the presence of a bacterium selected from the group consisting Clostridium species, Staphylococcus species, Enterococcus species and combinations thereof comprising administering to a patient in need an effective amount of a mixture, which comprises tiacumicin B, lipiarmycin A4, and at least one of other macrocyclic compounds:

Abstract: The present invention provides triazole macrocyclic compounds useful as therapeutic agents. More particularly, these compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.

Abstract: The invention provides, biologically active spinosyns, hybrid spinosyn polyketide synthases capable of functioning in Saccharopolyspora spinosa to produce the spinosyns, and methods of controlling insects using the spinosyns.

Abstract: The inventions discloses a process for preparation of compounds of Formula (IX), Wherein, R is C1-C6 alkyl, R1 is hydrogen or a hydroxyl protecting group, and R2 is hydrogen or fluorine.

Abstract: Provided are: a novel monoalkylamino intermediate (I); and a production method for a compound represented by the formula (III), which is an animal antibacterial agent, via the novel monoalkylamino intermediate.

Abstract: The inventors of the present invention have succeeded in acquiring a compound having excellent antibacterial activities against pathogens of respiratory tract infections in animals through the use of josamycin as a lead scaffold.

Abstract: The present invention provides glycorandomized 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: Described herein are novel macrolides, the preparation of novel macrolides, the use of novel macrolides for preventing, treating, or ameliorating various conditions, and the use of novel macrolides as antibacterial agents.

Abstract: The present invention provides solid state forms of Fidaxomycin, processes for preparing the solid state forms, as well as pharmaceutical compositions and formulations comprising one or more of the solid state forms of Fidaxomycin, and processes for the preparation of the compositions and formulations. The solid state forms of the present invention exhibit advantageous properties such as improved reliability and reproducibility in manufacturing and processing and stability in formulations.

Abstract: The present invention provides gas-induced method for phase-transforming organic solids, such as pharmaceutical crystals. The inventive method subjects the polymorphs of pharmaceutical agents to various pressures of gases (such as CO2, N2O, and CH4) to induce phase transform with ease.

Abstract: The present invention relates to an improved process for the purification of tiacumicin B. Specifically, the invention relates to a simplified, optimised process for the purification of tiacumicin B from a fermentation broth, using chromatography techniques. In particular, the invention relates to a method for purifying tiacumicin B which comprises subjecting a liquid containing tiacumicin B to at least one hydrophobic interaction chromatography step. The process according to the invention is simpler than the processes according to the prior art, and can easily be used on a large scale for commercial production.

Abstract: The present invention relates generally to the 18-membered macrocyclic antimicrobial agents called Tiacumicins, specifically, OPT-80 (which is composed almost entirely of the R-Tiacumicin B), pharmaceutical compositions comprising OPT-80, and methods using OPT-80. In particular, this compound is a potent drug for the treatment of bacterial infections, specifically C. difficile infections.

Abstract: The present invention relates to a calixarene-based glycosylated compound (I) having the formula: (I) wherein D is independently selected in the group comprising a —CH2-group, an oxygen atom, a sulphur atom, a sulfinyl group or a sulfonyl group, E is independently selected in the group comprising a hydrogen, an alkyl having from 1 to 10 carbon atoms, an aryl having from 6 to 20 carbon atoms, a nitrogen dioxide group, an azide group, an amino group, a guanidinium group, a halogen atom, a —CH2R group wherein R is a hydroxyl, a halogen, an amino group, a N(alkyl)2 group, a NH(alkyl) group, or E represents a —CO—R? wherein R? is a hydrogen atom, a hydroxyl group or an amino, B represents a A-C group wherein A is independently selected in the group comprising an oxygen atom, a sulfur atom, a NH group or a (CH2)i group, i being an integer from 1 to 10, C is independently selected in the group comprising a hydrogen, an alkyl, an alkenyl, an alkynyl, or C is a group of formula (II).

Abstract: The invention encompasses an active metabolite of the 18-membered macrocyclic antimicrobial agents, specifically, a metabolite of tiacumicin B and in certain embodiments, R-Tiacumicin B or and its related compounds. In particular, the invention encompasses a compound that acts as a potent antibiotic agent for the treatment of bacterial infections, specifically GI infections caused by toxin producing strains of Clostridium difficile (C. difficile) and Clostridium perfringens (C. perfringens).

Abstract: The invention relates to novel forms of compounds displaying broad spectrum antibiotic activity, especially crystalline polymorphic forms and amorphous forms of such compounds, compositions comprising such crystalline polymorphic forms and amorphous forms of such compounds, processes for manufacture and use thereof. The compounds and compositions of the invention are useful in the pharmaceutical industry, for example, in the treatment or prevention of diseases or disorders associated with the use of antibiotics, chemotherapies, or antiviral therapies, including, but not limited to, colitis, for example, pseudo-membranous colitis; antibiotic associated diarrhea; and infections due to Clostridium difficile (“C. difficile”), Clostridium perfringens (“C. perfringens”), Staphylococcus species, for example, methicillin-resistant Staphylococcus, or Enterococcus including Vancomycin-resistant enterococci.

Abstract: New crystalline forms of macrolide compounds, and pharmaceutical compositions thereof, are described herein. In addition, processes for preparing the crystalline forms are described herein.

Abstract: The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit superior antibacterial properties, particularly against Haemophilus influenzae. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

Abstract: The invention relates to novel forms of compounds displaying broad spectrum antibiotic activity, especially crystalline polymorphic forms and amorphous forms of such compounds, compositions comprising such crystalline polymorphic forms and amorphous forms of such compounds, processes for manufacture and use thereof. The compounds and compositions of the invention are useful in the pharmaceutical industry, for example, in the treatment or prevention of diseases or disorders associated with the use of antibiotics, chemotherapies, or antiviral therapies, including, but not limited to, colitis, for example, pseudo-membranous colitis; antibiotic associated diarrhea; and infections due to Clostridium difficile (“C. difficile”), Clostridium perfringens (“C. perfringens”), Staphylococcus species, for example, methicillin-resistant Staphylococcus, or Enterococcus including Vancomycin-resistant enterococci.

Abstract: Described are methods for making macrolides, and, in particular, a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, among other uses, may be used to make macrolides. Also described are solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.

Abstract: A novel compound that has antimicrobial activity against penicillin-resistant Streptococcus pneumoniae, and an anti-penicillin resistant pneumococci agent that includes the compound as an active ingredient are provided. Thus, an anti-penicillin resistant pneumococci agent is provided that includes as an active ingredient a compound represented by the following formula (I) or a pharmacologically acceptable salt thereof, or hydrates thereof: wherein, in the formula (I), R represents any one of a halogen atom, an azido group, Ra-Wa-, Rb-Wb-, Rc-Wc-, and RdRd?N—.

Abstract: The present invention concerns a process for the preparation of the compound of formula The compound of formula (1) is the key intermediate in the synthesis of some antibacterial agents of the triamilide class, such as Tulathromycin, useful to treat bacterial and protozoa infections.

Abstract: The invention described herein pertains to a novel macrolide antibacterial agent of formula (I): A-L-Q, as defined herein, and pharmaceutically acceptable salts, solvates, and hydrates thereof. Inter alia, the new macrolide antibacterial agent is active against a number of bacterial species, including resistant species.

Abstract: The present invention discloses compounds of formula I, II or X, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

Abstract: Described are methods for making macrolides, and, in particular, a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, inter alia, may be used to make macrolides. Also described are solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.

Abstract: The invention encompasses an active metabolite of the 18-membered macrocyclic antimicrobial agents, specifically, a metabolite of tiacumicin B and in certain embodiments, R-Tiacumicin B or and its related compounds. In particular, the invention encompasses a compound that acts as a potent antibiotic agent for the treatment of bacterial infections, specifically GI infections caused by toxin producing strains of Clostridium difficile (C. difficile) and Clostridium perfringens (C. perfringens).

Abstract: Methods, processes and materials for the production and recovery of Tiacumicins produced by culturing a microorganism belonging to the species Dactylosporangium aurantiacum subspecies hamdenensis having the ability to produce and accumulate one or more Tiacumicin in a nutrient medium comprising a carbon source, a nitrogen source, trace elements such as inorganic salts, and an adsorbent, wherein said nitrogen source comprises fish powder, and wherein said Tiacumicin is produced in a yield greater than about 50 mg/L broth.

Abstract: The invention relates to solid pharmaceutical or veterinary compositions comprising substantially pure Tulythromycin A in form of an addition salt with one or more acids, and to methods for preparing them. Following reconstitution with an aqueous solvent, the resulting solutions of Tulathromycin A may be administered to a mammal in order to treat bacterial or protozoal infections.

Abstract: Disclosed are levoisovalerylspiramycin I, II or III, preparations, preparing methods and uses thereof. The preparations comprise levoisovalerylspiramycin I, II or III and pharmaceutically acceptable carrier and/or adjuvant, wherein the purity of levoisovalerylspiramycin I, II or III is above 90 wt %. The levoisovalerylspiramycin I, II or III has a good antibacterial activity, and the preparations include solution for injection, powder for injection or lyophilized powder for injection.

Abstract: The present invention provides triazole macrocyclic compounds useful as therapeutic agents. More particularly, these compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.

Abstract: The invention described herein pertains to processes for the preparation of macrolide antibacterial agents. In particular, the invention pertains to processes for preparing macrolides and ketolides from erythromycin A.

Abstract: The invention relates to fatty and macrolide derivatives; compositions comprising an effective amount of fatty acid macrolide derivative; and methods for treating or preventing an autoimmune disorders and diseases with inflammation as the underlying etiology comprising the administration of an effective amount of a fatty acid macrolide derivative.