C07D499/00

High penetration prodrug compositions of antimicrobials and antimicrobial-related compounds
10233197 · 2019-03-19 · ·

The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

Compounds and their use

Described herein are compounds and their use in the treatment of infections. The compound of formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, solvates, pharmaceutically acceptable salts and pharmaceutical compositions described herein are also useful as ?-lactamase inhibitors, which restore or enhance the antibiotic spectrum of a suitable antibiotic agent. The compounds of formula (I) act as inhibitors of ?-lactamases. These compounds restore/potentiate the activities of ?-lactam antibiotics against carbapenemases. These compounds find use in diagnostic method for detecting ?-lactamases. Formula (I) ##STR00001##

Compounds and their use

Described herein are compounds and their use in the treatment of infections. The compound of formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, solvates, pharmaceutically acceptable salts and pharmaceutical compositions described herein are also useful as ?-lactamase inhibitors, which restore or enhance the antibiotic spectrum of a suitable antibiotic agent. The compounds of formula (I) act as inhibitors of ?-lactamases. These compounds restore/potentiate the activities of ?-lactam antibiotics against carbapenemases. These compounds find use in diagnostic method for detecting ?-lactamases. Formula (I) ##STR00001##

PLATFORM DRUG DELIVERY SYSTEM UTILIZING CRYSTAL ENGINEERING AND THEANINE DISSOLUTION

A platform drug delivery system and a method of improving the delivery of low solubility pharmaceuticals utilizing crystal engineering and Theanine dissolution resulting in enhanced bioactivity, dissolution rate, and solid state stability.

Platform drug delivery system utilizing crystal engineering and theanine dissolution

A platform drug delivery system and a method of improving the delivery of low solubility pharmaceuticals utilizing crystal engineering and Theanine dissolution resulting in enhanced bioactivity, dissolution rate, and solid state stability.

Platform drug delivery system utilizing crystal engineering and theanine dissolution

A method of making a water-soluble doxorubicin-theanine cocrystal composition. The method includes the steps of providing a quantity of doxorubicin, adding a quantity of a theanine enantiomer to the quantity of doxorubicin to form a mixture of the quantity of doxorubicin and the enantiomer of theanine, wetting the mixture, and grinding the mixture for a length of time sufficient to produce a dried crystalline mass.

Platform drug delivery system utilizing crystal engineering and theanine dissolution

A method of treating Hodgkin's disease in a subject. The method involves administering to the subject an effective amount of a water-soluble composition which includes a cocrystal composition containing doxorubicin and a theanine enantiomer.

Optically-Detectable Enzyme Substrates and Their Method of Use

The present invention relates to compounds that are substrates for an enzyme, and upon reaction with the enzyme provide a detectable response, such as an optically detectable response. In particular, the compounds have utility in detecting the presence of a -lactamase in a sample. In addition to the compounds, methods are disclosed for analyzing a sample for the presence of a -lactmase, for example, as an indicator of expression of a nucleic acid sequence including a sequence coding for a -lactmase. Kits are disclosed that include the disclosed compounds and additional components, for example, cells, antibodies, a -lactmase or instructions for using the components in an assay.

Platform drug delivery system utilizing crystal engineering and theanine dissolution

A platform drug delivery system and a method of improving the delivery of low solubility pharmaceuticals utilizing crystal engineering and Theanine dissolution resulting in enhanced bioactivity, dissolution rate, and solid state stability.

Platform drug delivery system utilizing crystal engineering and theanine dissolution

A platform drug delivery system and a method of improving the delivery of low solubility pharmaceuticals utilizing crystal engineering and Theanine dissolution resulting in enhanced bioactivity, dissolution rate, and solid state stability.