The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.

The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.

The present invention relates to novel cephalosporin derivatives represented by ##STR00001##
X, Y, L, R1, and R2 are as same as defined in the description of the invention. The present invention also relates to pharmaceutical antibiotic compositions comprising a novel celphalosporin derivative represented by Chemical Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient. According to the present invention, novel cephalosporin derivatives, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient for the broad spectrum of antibiotic resistant, low toxicity, particularly in Gram-negative bacteria, which can be useful with strong antimicrobial activity.

The present invention relates to novel cephalosporin derivatives represented by ##STR00001##
X, Y, L, R1, and R2 are as same as defined in the description of the invention. The present invention also relates to pharmaceutical antibiotic compositions comprising a novel celphalosporin derivative represented by Chemical Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient. According to the present invention, novel cephalosporin derivatives, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient for the broad spectrum of antibiotic resistant, low toxicity, particularly in Gram-negative bacteria, which can be useful with strong antimicrobial activity.

This disclosure provides multifunctional conjugate molecules in which at least one -lactam antibiotic is covalently attached to a cannabinoid by means of a linker. The disclosed conjugate molecules are designed to deliver therapeutic benefits as intact molecules, with release of the cannabinoid upon binding of the -lactam antibiotic to its target conveying further therapeutic benefits, and can be used to treat bacterial infections and other disorders.

This disclosure provides multifunctional conjugate molecules in which at least one -lactam antibiotic is covalently attached to a cannabinoid by means of a linker. The disclosed conjugate molecules are designed to deliver therapeutic benefits as intact molecules, with release of the cannabinoid upon binding of the -lactam antibiotic to its target conveying further therapeutic benefits, and can be used to treat bacterial infections and other disorders.

A compound of compound according to formula (I): ##STR00001##
wherein X is selected from the group consisting of CH, CCl and N, Z is selected from the group consisting of CH.sub.2COOH, CH(CH.sub.3)COOH, C(CH.sub.3).sub.2COOH and CH.sub.2F, D is a single bond connecting A and Ar or selected from the group consisting of CO, NHCO and N(C.sub.0-6)alkyl-CO, A is selected from the group consisting of a (C.sub.1-6)alkanediyl and a (C.sub.3-6)cycloalkanediyl or, if D is N(C.sub.0)alkyl-CO, A forms a 4- to 7-membered aliphatic heterocyclic ring with the nitrogen atom of N(C.sub.0)alkyl-CO in D, and Ar is a 6-membered aromatic ring with a first hydroxyl group in para-position to D, a second hydroxyl group in meta-position to D, and with at least one electron-withdrawing element and uses thereof.

A compound of compound according to formula (I): ##STR00001##
wherein X is selected from the group consisting of CH, CCl and N, Z is selected from the group consisting of CH.sub.2COOH, CH(CH.sub.3)COOH, C(CH.sub.3).sub.2COOH and CH.sub.2F, D is a single bond connecting A and Ar or selected from the group consisting of CO, NHCO and N(C.sub.0-6)alkyl-CO, A is selected from the group consisting of a (C.sub.1-6)alkanediyl and a (C.sub.3-6)cycloalkanediyl or, if D is N(C.sub.0)alkyl-CO, A forms a 4- to 7-membered aliphatic heterocyclic ring with the nitrogen atom of N(C.sub.0)alkyl-CO in D, and Ar is a 6-membered aromatic ring with a first hydroxyl group in para-position to D, a second hydroxyl group in meta-position to D, and with at least one electron-withdrawing element and uses thereof.

This disclosure provides multifunctional conjugate molecules in which at least one -lactam antibiotic is covalently attached to a cannabinoid by means of a linker. The disclosed conjugate molecules are designed to deliver therapeutic benefits as intact molecules, with release of the cannabinoid upon binding of the -lactam antibiotic to its target conveying further therapeutic benefits, and can be used to treat bacterial infections and other disorders.

This disclosure provides multifunctional conjugate molecules in which at least one -lactam antibiotic is covalently attached to a cannabinoid by means of a linker. The disclosed conjugate molecules are designed to deliver therapeutic benefits as intact molecules, with release of the cannabinoid upon binding of the -lactam antibiotic to its target conveying further therapeutic benefits, and can be used to treat bacterial infections and other disorders.