➤ Get the DrugPatentWatch Daily Briefing

Get Daily Updates on Generic Entry, Litigation, Biosimilars, and more …

Serving leading biopharmaceutical companies globally:

AstraZeneca
McKinsey
Mallinckrodt
Boehringer Ingelheim
Medtronic
Colorcon

Last Updated: September 21, 2021

DrugPatentWatch Database Preview

Claims for Patent: 8,735,392


Email this page to a colleague

« Back to Dashboard

Summary for Patent: 8,735,392
Title:Crystalline (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,- 9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt
Abstract: Provided herein are (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,- 9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt forms, including crystalline forms, and methods of their preparation. Pharmaceutical compositions comprising a (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,- 9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt are also provided, as are methods of using (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,- 9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt to treat a disease or condition, such as a cancer.
Inventor(s): Wang; Bing (San Jose, CA), Chu; Daniel (Santa Clara, CA), Liu; Yongbo (Shanghai, CN), Peng; Shichun (Shanghai, CN)
Assignee: BioMarin Pharmaceutical Inc. (Novato, CA)
Application Number:13/277,607
Patent Claims: 1. A crystalline form of (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,- 9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt, where the crystalline form exhibits at least one of: a solid state .sup.13C NMR spectrum with peaks at 143.2, 136.0, 131.8, 123.9, 112.2, 105.2, and 100.3 ppm.+-.0.2 ppm; a differential scanning calorimetry thermogram having an endotherm with a maximum at between about 320.degree. C. and about 335.degree. C.; a thermogravimetric analysis thermogram indicative of an unsolvated material; a dynamic vapor sorption isotherm plot which does not exhibit a significant weight change from 0 to 95% relative humidity; an X-ray powder diffraction pattern comprising characteristic peaks expressed in d-values (.ANG.) of about 11.9, 5.9, 4.9, 4.4, 4.3, 3.9, and 3.7; and an X-ray powder diffraction pattern comprising peaks at 2.theta. angle degrees.+-.0.2 2.theta. angle degrees of 7.4, 15.1, 18.1, 20.1, 20.4, 22.6, and 24.0.

2. The crystalline form of the (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,- 9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt of claim 1, where the crystalline form has a purity of at least about 99.5%.

3. The crystalline form of the tosylate salt of claim 1, where the crystalline form is substantially free of an amorphous form of (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,- 9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one or a salt or solvate thereof.

4. A pharmaceutical composition comprising the crystalline form of the tosylate salt according to claim 1 and a pharmaceutically acceptable excipient.

5. The pharmaceutical composition according to claim 4, where the composition is formulated for oral administration to a subject.

Make Better Decisions: Try a trial or see plans & pricing

Serving leading biopharmaceutical companies globally:

Merck
Medtronic
Harvard Business School
Moodys
Johnson and Johnson
McKesson

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 verification 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.