Patent SG-11201807569W-A (SG)
Title: Elimination of hepatitis b virus with antiviral agents
Inventor: SCHINAZI RAYMOND F
IPC: C07D207/34
Filed: 2017-03-09
Abstract: WO 17 / 15 6 255 Al (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 WO 2017/156255 Al 14 September 2017 (14.09.2017) WIPO I PCT (51) International Patent Classification: CO7D 207/34 (2006.01) A61K 31/454 (2006.01) CO7D 249/04 (2006.01) A61K 31/427 (2006.01) CO7D 401/12 (2006.01) A61K 31/4192 (2006.01) CO7D 403/12 (2006.01) A61P 31/20 (2006.01) A61K 31/4025 (2006.01) (21) International Application Number: PCT/US2017/021551 (22) International Filing Date: 9 March 2017 (09.03.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/305,865 9 March 2016 (09.03.2016) US (71) Applicant: EMORY UNIVERSITY [US/US]; 1599 Clifton Road NE, 4th Floor, Mailstop 1599/001/1AZ, At- lanta, Georgia 30322 (US). (72) Inventors: SCHINAZI, Raymond F.; 3630 Peachtree Road, NE, Apt. 3402, Atlanta, Georgia 30326 (US). BOUCLE, Sebastien; 3824 Cline Drive SE, Smyrna, Georgia 30082 (US). AMBLARD, Franck; 2975 Wind- field Circle, Tucker, Georgia 30084 (US). SARI, Ozkan; 3131 N. Druid Hills Rd., Apt. 7304, Decatur, Georgia 30033 (US). BASSIT, Leda; 3691 Cedar Ridge Dr. SE, Smyrna, Georgia 30080 (US). (74) Agent: BRADIN, David; ANDREWS KURTH KENYON LLP, 4505 Emperor Blvd., Suite 330, Durham, North Car- olina 27703 (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, 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)) [Continued on next page] (54) Title: ELIMINATION OF HEPATITIS B VIRUS WITH ANTIVIRAL AGENTS Monitoring HBV Capsid Assembly using Electron Microscopy Capsid Formation Assay HBV Cp149 Incubate with 25 pM Induce Assembly 10 pM Compound for 1 h, 4°C HBV > Cp149 500 mM NaCI, 4°C Capsid overnight GLS4 Incomplete hollow spheres -Fully-formed hollow spheres -Misassemmed ilogew spheres -Low abundance -Diameter < 20nrn Figure 1 (57) : The present invention is directed to compounds, compositions and methods for preventing, treating or curing Hepatit- is B (HBV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prod - rugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment, prevention or eradication of HBV in - fection. 111111111111110111011111111111010111110111011111111111110111111111111111111111110111111 Vehicle WO 2017/156255 Al MIDEDIMOMMIDIIMMEOMOMEIMMIMIOVOIMIE — 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))