Salt forms of ceftolozane

Patent metadata

Field	Value
Publication number	US-10000510-B2
Application number	US-201515504364-A
Country	US
Kind code	B2
Filing date	Aug 17, 2015
Priority date	Aug 18, 2014
Publication date	Jun 19, 2018
Grant date	Jun 19, 2018

Abstract

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.

First claim

What is claimed is:

1. An isolated solid ceftolozane salt, wherein the ceftolozane salt is a bromide salt.

2. An isolated solid ceftolozane salt, wherein the ceftolozane salt is an edisylate salt.

3. An isolated solid ceftolozane salt, wherein the ceftolozane salt is a chloride salt.

4. A pharmaceutical composition comprising the salt of claim 1 , and a pharmaceutically acceptable carrier.

5. A pharmaceutical composition comprising an isolated solid ceftolozane salt, wherein the ceftolozane salt is a chloride salt, and a pharmaceutically acceptable carrier, wherein the isolated solid ceftolozane salt is obtained by a process comprising the steps of:
(a) combining ceftolozane zwitterion in aqueous solution with a salt forming acid, wherein the acid is hydrochloric acid;
(b) incubating the solution of step (a);
(c) precipitating the ceftolozane salt by addition of a suitable solvent; and
(d) isolating the precipitate from the solution to yield the isolated solid ceftolozane salt.

6. The pharmaceutical composition of claim 5 , wherein the suitable solvent of step (c) is isopropanol.

7. The pharmaceutical composition of claim 5 , wherein the ceftolozane salt has a purity greater than or equal to 93% as measured by HPLC.

8. A pharmaceutical composition comprising the salt of claim 2 , and a pharmaceutically acceptable carrier.

9. A pharmaceutical composition comprising the salt of claim 3 , and a pharmaceutically acceptable carrier.

Assignees

• Merck Sharp & Dohme

Inventors

• Gu Jian-Qiao
• Jurkauskas Valdas
• Lopez Carlos
• Moshos Kristos Adrian
• Pathare Pradip M
• Garad Sudhakar
• Hwang You Seok

Classifications

• C07C309/04

  containing only one sulfo group · CPC title

• C07C309/05

  containing at least two sulfo groups bound to the carbon skeleton · CPC title

• C07C62/18

  Saturated compounds containing keto groups · CPC title

• C07D501/46 Primary

  with the 7-amino radical acylated by carboxylic acids containing hetero rings · CPC title

• C07C57/145

  Maleic acid · CPC title