You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: April 19, 2024

Claims for Patent: 10,414,748

✉ Email this page to a colleague

« Back to Dashboard

Summary for Patent: 10,414,748

Title:	Crystalline forms of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyan- ophenyl)urea maleate
Abstract:	This invention relates to a crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyan- ophenyl)urea maleate, and to pharmaceutical compositions thereof, to intermediates and methods for the production and isolation of such crystalline forms and compositions, and to methods of using such crystalline forms and compositions in the treatment of abnormal cell growth in mammals, especially humans.
Inventor(s):	Seadeek; Christopher Scott (West Lafayette, IN)
Assignee:	Pfizer Inc. (New York, NY)
Application Number:	15/567,433
Patent Claims:	1. A crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyan- ophenyl)urea maleate, having the structure: ##STR00007## and having a powder X-ray diffraction pattern comprising peaks at 2.theta. values of: 11.6, 12.1 and 19.6.degree. 2.theta..+-.0.2.degree. 2.theta.. 2. The crystalline form of claim 1, having a powder X-ray diffraction pattern comprising peaks at 2.theta. values of: 11.6, 12.1, 17.0, 17.7 and 19.6.degree. 2.theta..+-.0.2.degree. 2.theta.. 3. The crystalline form of claim 1, having a Raman spectrum comprising a wavenumber (cm.sup.-1) value of: 2219 cm.sup.-1.+-.2 cm.sup.-1. 4. The crystalline form of claim 1, having a Raman spectrum comprising a wavenumber (cm.sup.-1) value of: 1612 cm.sup.-1.+-.2 cm.sup.-1. 5. The crystalline form of claim 1, having a Raman spectrum comprising wavenumber (cm.sup.-1) values of: 1612 and 2219 cm.sup.-1.+-.2 cm.sup.-1. 6. The crystalline form of claim 1, having a Raman spectrum comprising wavenumber (cm.sup.-1) values of: 1534, 1612 and 2219 cm.sup.-1.+-.2 cm.sup.-1. 7. The crystalline form of claim 1, having a Raman spectrum comprising wavenumber (cm.sup.-1) values of: 1175, 1534, 1612 and 2219 cm.sup.-1.+-.2 cm.sup.-1. 8. The crystalline form of claim 1, having a .sup.13C solid state NMR spectrum comprising a resonance (ppm) value of: 148.3 ppm.+-.0.2 ppm. 9. The crystalline form of claim 1, having a .sup.13C solid state NMR spectrum comprising resonance (ppm) values of: 57.8, 134.8 and 148.3 ppm.+-.0.2 ppm. 10. The crystalline form of claim 1, having a .sup.13C solid state NMR spectrum comprising resonance (ppm) values of: 57.8, 134.8, 144.7 and 148.3 ppm.+-.0.2 ppm. 11. A crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyan- ophenyl)urea maleate, having the structure: ##STR00008## and having: (a) a powder X-ray diffraction pattern comprising peaks at 2.theta. values of: 11.6 and 12.1.degree. 2.theta..+-.0.2.degree. 2.theta.; and (b) a Raman spectrum comprising wavenumber (cm.sup.-1) values of: 1612 and 2219 cm.sup.-1.+-.2 cm.sup.-1. 12. A crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyan- ophenyl)urea maleate, having the structure: ##STR00009## and having: (a) a powder X-ray diffraction pattern comprising peaks at 2.theta. values of: 11.6 and 12.1.degree. 2.theta..+-.0.2.degree. 2.theta.; (b) a Raman spectrum comprising wavenumber (cm.sup.-1) values of: 1612 and 2219 cm.sup.-1.+-.2 cm.sup.-1; and (c) a .sup.13C solid state NMR spectrum comprising a resonance (ppm) value of: 148.3 ppm.+-.0.2 ppm. 13. The crystalline form of claim 1, having: (a) a Raman spectrum comprising wavenumber (cm.sup.-1) values of: 1612 and 2219 cm.sup.-1.+-.2 cm.sup.-1; and (b) a .sup.13C solid state NMR spectrum comprising a resonance (ppm) value of: 148.3 ppm.+-.0.2 ppm. 14. A crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyan- ophenyl)urea maleate, having the structure: ##STR00010## and having: (a) a powder X-ray diffraction pattern comprising peaks at 2.theta. values of: 11.6 and 12.1.degree. 2.theta..+-.0.2.degree. 2.theta.; and (b) a .sup.13C solid state NMR spectrum comprising a resonance (ppm) value of: 148.3 ppm.+-.0.2 ppm. 15. A pharmaceutical composition comprising the crystalline form of claim 1, and a pharmaceutically acceptable carrier or excipient. 16. A pharmaceutical composition comprising the crystalline form of claim 11, and a pharmaceutically acceptable carrier or excipient. 17. A pharmaceutical composition comprising the crystalline form of claim 12, and a pharmaceutically acceptable carrier or excipient. 18. A pharmaceutical composition comprising the crystalline form of claim 14, and a pharmaceutically acceptable carrier or excipient.

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

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.