Patent AU-2013203252-B2 (AU)
Title: Combination therapies using late sodium ion channel blockers and potassium ion channel blockers
Inventor: BELARDINELLI LUIZ
IPC: A61K31/00
Filed: 2013-01-25
Granted: 2015-08-20
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date W O 2013/112932 Al 1 August 2013 (01.08.2013) W I PO I P CT (51) International Patent Classification: AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, A61K31/00 (2006.01) A61K31/4545 (2006.01) BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, A61K 31/14 (2006.01) A61K 31/506 (2006.01) DO, DZ, EC, EE, EG, ES, Fl, GB, GD, GE, GH, GM, GT, A61K31/18 (2006.01) A61K31/553 (2006.01) HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, A61K31/439 (2006.01) A61P 9/06 (2006.01) KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, (21) International Application Number: NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, PCT/US2013/023291 RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, (22) International Filing Date: TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, 25 January2013 (25.01.2013) ZM, ZW. (25) Filing Language: English (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, (26) Publication Language: English GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, (30) Priority Data: UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, 61/591,734 27 January 2012 (27.01.2012) US TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, Fl, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, (71) Applicant: GILEAD SCIENCES, INC. [US/US]; 333 MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, Lakeside Drive, Foster City, California 94404 (US). TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, (72) Inventors: BELARDINELLI, Luiz; 205 Manzanita Ave., ML, MR, NE, SN, TD, TG). Palo Alto, California 94306 (US). RAJAMANI, Sridhar- Declarations under Rule 4.17: an; 8535 Mahogany Place, Newark, California 94560 _ as to the applicant's entitlement to claim the priority of the (US). earlier application (Rule 4.17(iii)) (74) Agents: TANNER, Lorna, L. et al.; Foley & Lardner - of inventorship (Rule 4.17(iv)) LLP, 3000 K Street N.W., Suite 600, Washington, DC 20007-5109 (US). Published: (81) Designated States (unless otherwise indicated, for every - with international search report (Art. 21(3)) kind of national protection available): AE, AG, AL, AM, (54) Title: COMBINATION THERAPIES USING LATE SODIUM ION CHANNEL BLOCKERS AND POTASSIUM ION --- CHANNEL BLOCKERS 'KACh + 'Na 70% Synergism s KACh Na 26% 23.5% Tertiapin (TO) Compound 1 TQ+Compound 1 (1 nM) (300 nM) (1 nM + 300 nM) O (57) Abstract: Described herein is a method for the treatment or prevention of atrial fibrillation and/or atrial flutter comprising ad ministration of an effective amount of one or more of a potassium channel blocker and an effective amount of one or more of a late sodium channel blocker. Also provided are methods for modulating ventricular and atrial rhythm and rate. Also provided are phar maceutical formulations that are suitable for such combined administration.