Cocrystal of olaparib and urea and preparation method thereof

A technology of eutectic crystal form and constant temperature, which is applied in the preparation of organic compounds, preparation of urea derivatives, chemical instruments and methods, etc., can solve the problem of low solubility of free base crystal form, simplify the preparation and post-treatment process, facilitate Long-term storage, the effect of improving drug absorption efficiency
CN105753789BActive Publication Date: 2018-09-25CRYSTAL PHARMATECH CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
CRYSTAL PHARMATECH CO LTD
Publication Date
2018-09-25

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Abstract

Disclosed are a co-crystal of olaparib and urea and a preparation method therefor. Specifically disclosed is a co-crystal form A, and an X-ray powder diffraction pattern of this crystal form has characteristic peaks at points where 2theta value is 17.4°±0.2°, 20.7°±0.2°, 10.5°±0.2°. The disclosed co-crystal has better stability, lower hygroscopicity and higher solubility as compared to existing olaparib free alkali crystal forms.
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Description

technical field

[0001] The invention relates to a co-crystal of olaparib and urea, a preparation method and application thereof. Background technique

[0002] Olaparib was first developed by the British biotechnology company KuDOS (Kudos) Pharmaceutical Co., Ltd. After AstraZeneca acquired KuDOS in 2005, it continued to develop Olaparib for the treatment of ovarian cancer. On December 19, 2014, Olaparib was approved by the FDA for marketing in the United States. It is the first targeted drug approved by the FDA for ovarian cancer patients with BRCA mutations, and is suitable for patients who have previously undergone chemotherapy. It has been demonstrated in preclinical models that olaparib is a first-in-class oral poly ADP ribose polymerase (PARP) inhibitor that exploits defects in the DNA repair pathway to preferentially kill cancer cells. The chemical name of olaparib is 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one, and its str...

Claims

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