Patent classifications
C07H17/08
SCALABLE SYNTHESIS OF REDUCED TOXICITY DERIVATIVE OF AMPHOTERICIN B
Disclosed is a simplified, readily scalable series of individual methods that collectively constitute a method for the synthesis of C2′epiAmB, an efficacious and reduced-toxicity derivative of amphotericin B (AmB), beginning from AmB. Also provided are various compounds corresponding to intermediates in accordance with the series of methods.
Azithromycin derivatives with epithelial barrier enhancement properties
The invention provides novel compounds that are derivatives of Azithromycin and that have been found by the current inventors to have low antimicrobial activity but significant epithelial barrier enhancement properties. The invention further provides use of the compounds as a medicament, in particular in the treatment or prophylaxis of a disease or condition that is caused by a defect in epithelial cells or tissue, or a disease or condition that benefits from enhancement or restoration of epithelial barrier function, for example diseases of the respiratory tract.
Azithromycin derivatives with epithelial barrier enhancement properties
The invention provides novel compounds that are derivatives of Azithromycin and that have been found by the current inventors to have low antimicrobial activity but significant epithelial barrier enhancement properties. The invention further provides use of the compounds as a medicament, in particular in the treatment or prophylaxis of a disease or condition that is caused by a defect in epithelial cells or tissue, or a disease or condition that benefits from enhancement or restoration of epithelial barrier function, for example diseases of the respiratory tract.
Tylosin derivatives and method for preparation thereof
The present invention relates to new macrolide derivatives, in particular new tylosin derivatives of the formula (IIa), 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. ##STR00001##
Tylosin derivatives and method for preparation thereof
The present invention relates to new macrolide derivatives, in particular new tylosin derivatives of the formula (IIa), 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. ##STR00001##
Hydrogen bond forming fluoro ketolides for treating diseases
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.
Hydrogen bond forming fluoro ketolides for treating diseases
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.
C-4" POSITION SUBSTITUTED MACROLIDE DERIVATIVE
A useful novel compound that shows superior antibacterial activity also against erythromycin resistant bacteria, for example, resistant pneumococci, streptococci, mycoplasmas, and the like, against which sufficient antibacterial activity cannot be obtained with conventional macrolide antibiotics, or a pharmaceutically acceptable salt thereof, or a hydrate or a solvate thereof.
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C-4" POSITION SUBSTITUTED MACROLIDE DERIVATIVE
A useful novel compound that shows superior antibacterial activity also against erythromycin resistant bacteria, for example, resistant pneumococci, streptococci, mycoplasmas, and the like, against which sufficient antibacterial activity cannot be obtained with conventional macrolide antibiotics, or a pharmaceutically acceptable salt thereof, or a hydrate or a solvate thereof.
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Anti-cancer compounds from invasive salvinias and methods of treating cancer
Compositions and methods related to anti-cancer terpenoid compounds isolated from plants in the Salviniaceae family, pharmaceutical compositions comprising the same, and methods of treating cancer.