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Last Updated: March 30, 2023

Claims for Patent: 8,247,416

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Summary for Patent: 8,247,416
Title:Phthalazinone derivative
Abstract: 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-p- hthalazin-1-one as crystalline Form A.
Inventor(s): Menear; Keith Allan (Cambridge, GB), Ottridge; Anthony Peter (Cambridge, GB), Londesbrough; Derek John (Sunderland, GB), Hallett; Michael Raymond (Sunderland, GB), Mulholland; Keith Raymond (Macclesfield, GB), Pittam; John David (Macclesfield, GB), Laffan; David Dermot Patrick (Macclesfield, GB), Ashworth; Ian Woodward (Macclesfield, GB), Jones; Martin Francis (Macclesfield, GB), Cherryman; Janette Helen (Macclesfield, GB)
Assignee: Kudos Pharmaceuticals Limited (London, GB)
Application Number:12/500,900
Patent Claims: 1. The compound 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-p- hthalazin-1-one as a crystalline form having the following characteristic peaks in a powder X-ray diffraction pattern: TABLE-US-00005 2.theta..degree. (.+-.0.1.degree.) Peak .lamda. = 1.5418.ANG.) 1 12.0 2 17.8 3 21.1 4 22.3 5 29.2.

2. The compound of claim 1 having the following additional characteristic peaks in a powder X-ray diffraction pattern: TABLE-US-00006 2.theta..degree. (.+-.0.1.degree.) Peak (.lamda. = 1.5418.ANG.) 6 10.5 7 14.0 8 21.7 9 24.3 10 26.1.

3. The compound of claim 1, which begins melting at 210.1.degree. C..+-.1.degree. C. when heated from 25.degree. C. to 325.degree. C. at 10.degree. C. per minute in differential scanning calorimetry.

4. A method of synthesising 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-p- hthalazin-1-one from 2-fluoro-5-(4-oxo-3,4-dihydro-phthalazin-1-ylmethyl)-benzoic acid comprising reacting 2-fluoro-5-(4-oxo-3,4-dihydrophthalazin-1-ylmethyl)-benzoic acid with 1-(cyclopropylcarbonyl)piperazine or a mineral acid salt thereof in the presence of an amide coupling agent and a base to form 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-p- hthalazin-1-one.

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Serving leading biopharmaceutical companies globally:

Boehringer Ingelheim
Express Scripts

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