C07D501/46

Tetrazolones as a Carboxylic Acid Bioisosteres
20180002297 · 2018-01-04 ·

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.

SIDEROPHORE CEPHALOSPORIN CONJUGATES 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.

SIDEROPHORE CEPHALOSPORIN CONJUGATES 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.

CEPHALOSPORIN ANTIBACTERIAL COMPOUND AND PHARMACEUTICAL APPLICATION THEREOF
20230121689 · 2023-04-20 ·

Provided are a cephalosporin compound represented by formula I-1, I-2, or I-3, a pharmaceutical composition comprising same, and use thereof as an antibacterial agent.

##STR00001##

CEPHALOSPORIN ANTIBACTERIAL COMPOUND AND PHARMACEUTICAL APPLICATION THEREOF
20230121689 · 2023-04-20 ·

Provided are a cephalosporin compound represented by formula I-1, I-2, or I-3, a pharmaceutical composition comprising same, and use thereof as an antibacterial agent.

##STR00001##

A SALT OF CEPHALOSPORIN DERIVATIVE, ITS CRYSTALLINE SOLID AND A METHOD OF MANUFACTURING THEREOF

The present invention provides an acid addition salt or a sodium salt of a compound represented by the formula (IA):

##STR00001##

or their hydrate or a stable crystalline solid thereof. The salt or the crystalline solid is extremely useful as an active ingredient for the production of a pharmaceutical product.

SALT FORMS OF CEFTOLOZANE

This disclosure relates to salt forms of ceftolozane, processes for making these salt forms, and compositions comprising the same. Also disclosed are stabilized compositions of ceftolozane. Provided herein are salt forms of ceftolozane, processes for making these salt forms and compositions comprising the same. The salt forms provided herein include ceftolozane bromide, ceftolozane edisylate, ceftolozane mesylate, ceftolozane chloride, ceftolozane sulfate, ceftolozane maleate, ceftolozane phosphate, and ceftolozane ketoglutarate.

SALT FORMS OF CEFTOLOZANE

This disclosure relates to salt forms of ceftolozane, processes for making these salt forms, and compositions comprising the same. Also disclosed are stabilized compositions of ceftolozane. Provided herein are salt forms of ceftolozane, processes for making these salt forms and compositions comprising the same. The salt forms provided herein include ceftolozane bromide, ceftolozane edisylate, ceftolozane mesylate, ceftolozane chloride, ceftolozane sulfate, ceftolozane maleate, ceftolozane phosphate, and ceftolozane ketoglutarate.

Beta-Lactam-Cannabinoid Conjugate Molecules
20220257778 · 2022-08-18 ·

This disclosure provides multifunctional conjugate molecules in which at least one β-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 β-lactam antibiotic to its target conveying further therapeutic benefits, and can be used to treat bacterial infections and other disorders.

Beta-Lactam-Cannabinoid Conjugate Molecules
20220257778 · 2022-08-18 ·

This disclosure provides multifunctional conjugate molecules in which at least one β-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 β-lactam antibiotic to its target conveying further therapeutic benefits, and can be used to treat bacterial infections and other disorders.