This invention pertains generally to prostacyclin formulations and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing

The present invention relates to compounds of formula (Ia) and the use thereof as inhibitors of P. aeruginosa virulence factor LasB. Formula (Ia). These compounds are useful in the treatment of bacterial infections, especially caused by P. aeruginosa.

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The present invention relates to a pharmaceutically acceptable salt of alkylcarbamoyl naphthalenyloxy octenoylhydroxyamide or of a derivative thereof and a method for preparing same, and can improve moisture stability while maintaining the characteristics, such as the efficacy and effective dose, of a pharmaceutically acceptable salt of alkylcarbamoyl naphthalenyloxy octenoylhydroxyamide or of a derivative thereof. In addition, the present invention can simplify the production and manufacturing process of a formulation by improving hygroscopicity.

The invention relates to hydrazide compounds and their use in medicine, particularly in treating and/or preventing infections caused by a fungus.

The invention relates to hydrazide compounds and their use in medicine, particularly in treating and/or preventing infections caused by a fungus.

The present disclosure is related to the field of enzyme inhibitors, and in particular to a hydroxamic acid derivative, a method for producing the same and use thereof. The hydroxamic acid group of the hydroxamic acid derivative can be chelated with zinc ions in the LpxC active area, and the derivative has a hydrophobic side chain which can bind to hydrophic channels in the enzyme LpxC. These guarantee that the hydroxamic acid derivative has good bactericidal activity against Gram-negative bacteria and low toxicity. The present disclosure also provides a method for producing the hydroxamic acid derivative, which requires a shorter reaction time and can provide the derivative with a high yield.

The present disclosure is related to the field of enzyme inhibitors, and in particular to a hydroxamic acid derivative, a method for producing the same and use thereof. The hydroxamic acid group of the hydroxamic acid derivative can be chelated with zinc ions in the LpxC active area, and the derivative has a hydrophobic side chain which can bind to hydrophic channels in the enzyme LpxC. These guarantee that the hydroxamic acid derivative has good bactericidal activity against Gram-negative bacteria and low toxicity. The present disclosure also provides a method for producing the hydroxamic acid derivative, which requires a shorter reaction time and can provide the derivative with a high yield.

This invention pertains generally to prostacyclin formulations and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing

This invention pertains generally to prostacyclin formulations and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing

New chelators such as H.sub.3L1, H.sub.3L2, H.sub.3L3, H.sub.3L26 and derivatives were synthesized for the complexation of {Al.sup.18F}.sup.2+. These new chelators are able to complex {AI.sup.18F}.sup.2+ with good radiochemical yields using a labeling temperature of 37° C. The stability of the new Al.sup.18F-complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum. AI.sup.18F-L3 and AI.sup.18F-L26 showed a stability comparable to that of the previously reported Al.sup.18F-NODA. Moreover, the biodistribution of Al.sup.18F-L3 and AI.sup.18F-L26 showed absence of in vivo demetallation since only very limited bone uptake was observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestine due to hepatobiliary clearance of the radiolabeled ligand. The chelators H.sub.3L3 and Al.sup.18F-L26 demonstrated to be a good lead candidates for the labeling of heat sensitive biomolecules with .sup.18F-fluorine and derivatives have been synthesized. We have explored the complexation of {AI.sup.18F}.sup.2+ with new chelators and obtained very favourable radiochemical yields (>85%) using a labeling temperature of 37° C. The stability of the new Al.sup.18F-complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum at 37° C., where AI.sup.18F-L3 and AI.sup.18F-L26 showed a stability comparable to that of the previously reported Al.sup.18F-NODA. Moreover, the biodistribution of Al.sup.18F-L3 and Al.sup.18F-L26 showed high stability, since only very limited bone uptake—which would be an indication of release of fluorine-18 in the form of fluoride—was observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestines due to hepatobiliary clearance of the radiolabeled ligand. The chelators H.sub.3L3 and H.sub.3L26 demonstrated to be good lead candidates for the labeling of heat sensitive biomolecules with .sup.18F-fluorine and several derivatives have been synthesized.