Solid forms of ceftolozane

Provided are solid forms of ceftolozane sulfate. Ceftolozane is also known as ((6R,7R)-3-[(5-amino-4-{ [(2-aminoethyl)carbamoyl]amino} -1-methyl-1H-pyrazol-2-ium-2-yl)methyl]-7-({ (2Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-[(1-carboxy-1-methylethoxy)imino]acetyl} amino)-8-oxo-5-thia-1-azabicyclo[4.2.0...

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Main Authors SANJAY MUDUR, JASON WOERTINK, VALDAS JURKAUSKAS, LISA DUONG, ASLI OVAT, YOU SEOK HWANG, JOSEPH TERRACCIANO, KRISTOS ADRIAN MOSHOS, NICOLE MILLER DAMOUR
Format Patent
LanguageEnglish
Published 29.04.2016
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:Provided are solid forms of ceftolozane sulfate. Ceftolozane is also known as ((6R,7R)-3-[(5-amino-4-{ [(2-aminoethyl)carbamoyl]amino} -1-methyl-1H-pyrazol-2-ium-2-yl)methyl]-7-({ (2Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-[(1-carboxy-1-methylethoxy)imino]acetyl} amino)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate). Form 1 has diffractions at angles (2 theta ±0.2) of 12.4, 16.4, 22.6, 25.1, and 28.0. In a preferred embodiment the solid form is Form 2 which has diffractions at angles (2 theta ±0.2) of 4.4, 8.8, 11.0, 14.9, and 17.7. Additionally provided are pharmaceutical compositions comprising the solid forms and involving the process of lyophilising the solid forms. The pharmaceutical compositions can additionally contain tazobactam. Ceftolozane is an antibacterial agent.
Bibliography:Application Number: NZ20140631761