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

Last Updated: March 28, 2024

Claims for Patent: 9,725,455


✉ Email this page to a colleague

« Back to Dashboard


Summary for Patent: 9,725,455
Title:Crystalline forms of a bruton's tyrosine kinase inhibitor
Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pi- peridin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
Inventor(s): Purro; Norbert (Los Gatos, CA), Smyth; Mark Stephen (Foster City, CA), Goldman; Erick (Concord, CA), Wirth; David D. (Oak Ridge, NC)
Assignee: Pharmacyclics LLC (Sunnyvale, CA)
Application Number:15/497,896
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,725,455
Patent Claims: 1. A crystalline Form A of 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pi- peridin-1-yl)prop-2-en-1-one that has an X-ray powder diffraction (XRPD) pattern comprising 2-Theta peaks at 5.7.+-.0.1.degree., 18.9.+-.0.1.degree., and 21.3.+-.0.1.degree..

2. The crystalline form of claim 1, wherein the X-ray powder diffraction (XRPD) pattern further comprises a 2-Theta peak at 16.1.+-.0.1.degree..

3. The crystalline form of claim 1, wherein the X-ray powder diffraction (XRPD) pattern further comprises a 2-Theta peak at 13.6.+-.0.1.degree..

4. The crystalline form of claim 1, wherein the X-ray powder diffraction (XRPD) pattern further comprises a 2-Theta peak at 21.6.+-.0.1.degree..

5. The crystalline form of claim 1, wherein the X-ray powder diffraction (XRPD) pattern further comprises 2-Theta peaks at 13.6.+-.0.1.degree., 16.1.+-.0.1.degree., and 21.6.+-.0.1.degree..

6. The crystalline form of claim 1, wherein the X-ray powder diffraction (XRPD) pattern further comprises 2-Theta peaks at 13.6.+-.0.1.degree. and 16.1.+-.0.1.degree..

7. The crystalline form of claim 1, wherein the X-ray powder diffraction (XRPD) pattern further comprises 2-Theta peaks at 13.6.+-.0.1.degree. and 21.6.+-.0.1.degree..

8. The crystalline form of claim 1, wherein the X-ray powder diffraction (XRPD) pattern further comprises 2-Theta peaks at 16.1.+-.0.1.degree. and 21.6.+-.0.1.degree..

9. The crystalline form of claim 1, wherein the crystalline form has Infrared (IR) spectrum weak peaks at about 1584 cm.sup.-1, about 1240 cm.sup.-1, about 1147 cm.sup.-1, about 1134 cm.sup.-1, about 1099 cm.sup.-1, and about 1067 cm.sup.-1.

10. The crystalline form of claim 1, wherein the crystalline form has a melting temperature of about 155-156.degree. C.

11. The crystalline form of claim 1, wherein the crystalline form has a DSC thermogram with an endotherm having an onset at about 154.degree. C. and a peak at about 157.degree. C. and an exotherm at about 159.degree. C.

12. The crystalline form of claim 1, wherein the crystalline form is non-hygroscopic.

13. The crystalline form of claim 1, wherein the crystalline form has an observed aqueous solubility of about 0.013 mg/mL at about pH 8.

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.