Solid forms of ceftolozane and processes for preparing
AssigneeMerck Sharp & Dohme Corp.
InventorsKevin Matthew Maloney, Eric M. Sirota, Richard J. Varsolona, Donald R. Gauthier, Jr., Hong Ren
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Abstract
The instant invention is related to a novel solid form of ceftolozane sulfate (the DMAc solvate of ceftolozane sulfate (Form 3)), compositions comprising ceftolozane sulfate DMAc solvate (Form 3), synthesis of Form 3 and an improved crystallization process using Form 3 to prepare ceftolozane sulfate Form 2. Novel compositions also include ceftolozane sulfate solid Form 3 and/or other crystalline and amorphous solid forms of ceftolozane.
Claims20
A solid form of ceftolozane sulfate DMAc solvate that produces an X-ray powder diffraction (XRPD) pattern having diffractions at angles (2 theta±0.2) of 12.8, 17.5, 21.7, 24.0 and 24.6.
A solid form of ceftolozane sulfate DMAc solvate that produces an X-ray powder diffraction (XRPD) pattern having diffractions at angles (2 theta±0.2) of 11.0, 21.0, 22.5 and 24.0.
A process for preparing wet solids of ceftolozane sulfate DMAc solvate comprising the steps of:
- a) combining ceftolozane TFA, water, DMAc and a first co-solvent to form a slurry;
- b) filtering the slurry to produce a filtrate;
- c) combining the filtrate and a sulfate source;
- d) adding a second co-solvent and DMAc solvate seeds to produce a product;
- and
- e) filtering the product to obtain wet solids of ceftolozane sulfate DMAc solvate.
Dependencies are inferred from the claim text.