DrugPatentWatch Database Preview
« Back to Dashboard
Summary for Patent: 8,247,416
|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)|
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.
For more information try a trial or see the plans and pricing
Serving hundreds of leading biopharmaceutical companies globally:
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.