Patent SG-11201906811W-A (SG)
Title: Solid fosmetpantotenate formulations
Inventor: MACIKENAS DAINIUS
IPC: A61K9/16
Filed: 2018-02-07
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 16 August 2018 (16.08.2018) WIP0 1 PCT omit °nolo DID mull oil mono oimIE (10) International Publication Number WO 2018/148313 Al 45.00% 40.00% 35.00% 30.00% 2500% 120.00% 15.00% I- 10.00% BB 5.00% r 0.00% (51) International Patent Classification: A61K 31/664 (2006.01) A61P 25/00 (2006.01) A61K 9/16 (2006.01) (21) International Application Number: PCT/US2018/017266 (22) International Filing Date: 07 February 2018 (07.02.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/456,077 07 February 2017 (07.02.2017) US 62/488,618 21 April 2017 (21.04.2017) US (71) Applicant: RETROPHIN, INC. [US/US]; 3721 Valley Centre Drive, Suite 200, San Diego, California 92130 (US). (72) Inventors: MACIKENAS, Dainius; 2945 Denver St., San Diego, California 92117 (US). RUBY, Kale; 1030 Saxony Road, Encinitas, California 92024 (US). (74) Agent: SARGEANT, Brooke et al.; Seed Intellectual Prop- erty Law Group LLP, Suite 5400, 701 Fifth Avenue, Seat- tle, Washington 98104-7064 (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, (54) Title: SOLID FOSMETPANTOTENATE FORMULATIONS drug only (2.696/week degradation) AA —11-75 mg drug Ethyl Acetate Capsules (2.546fweek degradation) BB 75 mg drug Lauryl Glycol 90 Capsules (2. 7 . 4 Jureek degradation) CC ad , 74anulation in MCC (1.8%/week deg DD • ^ 20.., of '-;•anutation in Mannitol (2.0%Aveek dein - add:, EE .1i.-25:75 (12 7, , rug HPMCAS-L SDD • 1.794(week degradation) FF 6 8 10 12 14 Time on Stability (weeks) MI FIG. 2 011 0 H3c., (i) 71' 1-1 1,13C0 (57) : Solid formulations comprising a compound having formula (I) or a pharmaceutically acceptable salt thereof, and their O use in the treatment of neurologic disorders (such as pantothenate kinase-associated neurodegeneration), are provided. O [Continued on next page] WO 2018/148313 Al MIDEDIMOMOIDEIREEMOMMIMMIOMMIDOMOVOIS TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(11)) as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) Published: — with international search report (Art. 21(3))