Patent SG-11201811255W-A (SG)
Title: Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
Inventor: FERDOUS ABU J
IPC: A61K9/50
Filed: 2017-06-29
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 04 January 2018 (04.01.2018) W I PO I PCT oimitia °nolo olon Emmoilmionio oimIE (10) International Publication Number WO 2018/005849 Al (51) International Patent Classification: A61K 9/50 (2006.01) A61K 31/00 (2006.01) (21) International Application Number: PCT/US2017/040075 (22) International Filing Date: 29 June 2017 (29.06.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/356,345 29 June 2016 (29.06.2016) US (71) Applicant: PRINCIPIA BIOPHARMA INC. [US/US]; 400 East Jamie Court, Suite 302, South San Francisco, Cal- ifornia 94080 (US). (72) Inventors: FERDOUS, Abu J.; 610 Masonic Way, #3, Belmont, California 94002 (US). MASJEDIZADEH, Mo- hammad R.; 5341 Elrose Ave., San Jose, California 95124 (US). LIN, Wu; 31 Archer Crescent, Nottingham NG8 1HB (GB). (74) Agent: CHEN, Wei-Chuan; Finnegan, Henderson, Farabow, Garrett & Dunner, LLP, 901 New York Avenue NW, Washington, DC, District of Columbia 20001-4413 (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, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, 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, SA, 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, ST, 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: MODIFIED RELEASE FORMULATIONS OF 24344-AMINO-3-(2-FLUOR0-4-PHENOXY- PHENYL)PYRAZOLO[3,4-D]PYRIMIDIN-1-YLPIPERIDINE-1-CARBONYL]-4-METHYL-4-[4-(OXETAN-3-Y = L)PIPERAZIN-1-YL]PENT-2-ENENITRILE FIG. 1 (57) : Modified release formulations, such as solid oral dosage forms comprising a core composition comprising Compound (I) and/or a pharma- ceutically acceptable salt thereof; a sub-coating layer coating the core com- position, said sub-coating layer comprising a polyvinyl alcohol and/or a hy- droxypropyl methyl cellulose; and an enteric coating layer encapsulating the sub-coating layer and the core composition, said enteric coating layer comprising at least one polymer selected from an acrylic/methacrylic/ethacr ylic acid homopolymer and copolymers thereof, a cellulose derivative, and a polyvinylpyrrolidone, and methods of administration of a Bruton's tyrosine kinase (BTK) inhibitor using said formulations. W O 20 18/005 8 49 Al Enteric coat Subcoat