Patent SG-11201407970V-A (SG)
Title: Modulation of hepatitis b virus cccdna transcription
Inventor: GUO JU-TAO
IPC: C07K5/00
Filed: 2013-05-31
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 5 December 2013 (05.12.2013) WIPOIPCT (10) International Publication Number WO 2013/181584 A3 (51) International Patent Classification: A61K38/12 (2006.01) A01N 47/34 (2006.01) C07K 5/00 (2006.01) C07D 245/00 (2006.01) (21) International Application Number: PCT/US2013/043691 (22) International Filing Date: 31 May 2013 (31.05.2013) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 61/654,374 1 June 2012 (01.06.2012) US (71) Applicant: DREXEL UNIVERSITY [US/US]; 3141 Chestnut Street, Philadelphia, PA 19104 (US). (72) Inventors: GUO, Ju-Tao; 1426 Oxford Circle, Lansdale, Pennsylvania 19446 (US). CHANG, Jinhong; 101 Bar­ berry Court, Chalfont, Pennsylvania 18914 (US). BLOCK, Timothy M.; 90 Foxcroft Drive, Doylestown, Pennsylvania 18902 (US). KINNEY, William A.; 16 Thompson Mill Road, Newtown, Pennsylvania 18940 (US). ALMOND, Harold, R.; 1330 Hanover Place, Maple Glen, PA 19002 (US). (74) Agents: CALDWELL, John W. et al.; Woodcock Wash­ burn LLP, Cira Centre, 12th Floor, 2929 Arch Street, Phil­ adelphia, Pennsylvania 19104 (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). [Continued on next page] (54) Title: MODULATION OF HEPATITIS B VIRUS CCCDNA TRANSCRIPTION NT 1 o © o- o us ^ ^ !%S! m ll © o is-; O O O O O is> c-s r-i — ^ 11' (57) Abstract: The present disclosure per­ tains to the discovery of new family of a \"first in class\" small molecular inhibitors of hepatit­ is B virus (HBV) covalently closed circular (ccc) DNA for use as therapeutics in the man­ agement of chronic HBV. Provided are agents that provide epigenetic modification of the cccDNA, histone modifying agent, and inhib­ itors of histone deacetylace activity that in turn modulate HBV cccDNA, which has nev­ er been achieved with a pharmacological agent. Also provided are methods for modu­ lating HBV cccDNA, for treating or prevent­ ing HBV in a subject, and for modulating cccDNA transcription of hepatitis B in a sub­ ject. WO 2013/181584 A3 I lllll llllllll II llllll III lllll lllll III III III lllll lllll lllll lllll lllll llll lllllll llll llll llll Published: — with international search report (Art. 21(3)) — before the expiration of the time limit for amending the claims and to be republished in the event of receipt of amendments (Rule 48.2(h)) (88) Date of publication of the international search report: 13 February 2014