Patent SG-11201408067Y-A (SG)
Title: Crystalline forms of a bruton's tyrosine kinase inhibitor
Inventor: SMYTH MARK
IPC: A61P29/00
Filed: 2013-06-03
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 12 December 2013 (12.12.2013) WIPOIPCT (10) International Publication Number WO 2013/184572 A1 (51) International Patent Classification: A61K 47/38 (2006.01) A61P 35/00 (2006.01) A61K 47/30 (2006.01) A61P 29/00 (2006.01) A61K 9/48 (2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/US2013/043888 3 June 2013 (03.06.2013) English (30) Priority Data: 61/655,381 4 June 2012 (04.06.2012) English US (71) Applicant: PHARMACYCLICS, INC. [US/US]; 995 East Arques Avenue, Sunnyvale, CA 94085 (US). (72) Inventor; and (71) Applicant : PURRO, Norbert [US/US]; 15460 Corinne Drive, Los Gatos, CA 95032 (US). (72) Inventors: SMYTH, Mark; 211 Rock Harbor Lane, Foster City, CA 94404 (US). GOLDMAN, Erick; 1137 Keith Drive, Concord, CA 94518 (US). WIRTH, David, D.; 5906 Tarleton Drive, Oak Ridge, NC 27310 (US). (74) Agent: HOSTETLER, Michael, J.; Wilson Sonsini Goodrich & Rosati, 650 Page Mill Road, Palo Alto, CA 94304 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available)'. AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available)'. ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Published: — with international search report (Art. 21(3)) (54) Title: CRYSTALLINE FORMS OF A BRUTON'S TYROSINE KINASE INHIBITOR CJ l> oo 16000- 15000- 14000- 13000- 12000- 11000- 10000- 9000- 8000- 7000- 6000- 5000- 4000- 3000- 2000- 1000- o- FIG. 1 XRPD Pattern of Form A 20 2-Theta - Scale i-H o CJ (57) Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor l-((R)-3-(4-amino-3-(4-phenoxyphenyl)-lH- pyrazolo[3,4-d]pyrimidin-l-yl)piperidin-l-yl)prop-2-en-l-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 in­ hibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroim- mune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.