Patent SG-11201900910T-A (SG)
Title: RNAi AGENTS FOR HEPATITIS B VIRUS INFECTION
Inventor: LI ZHEN
IPC: C07H21/02
Filed: 2017-08-04
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 08 February 2018 (08.02.2018) WIPO I PCT 011111010 n °nolo oio 11o1 IIII 11111°1111°111 (10) International Publication Number WO 2018/027106 A3 (51) International Patent Classification: C07H 21/02 (2006.01) A61K 48/00 (2006.01) (21) International Application Number: PCT/US2017/045446 (22) International Filing Date: 04 August 2017 (04.08.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/370,754 04 August 2016 (04.08.2016) US 62/534,733 20 July 2017 (20.07.2017) US 62/540,639 03 August 2017 (03.08.2017) US (71) Applicant: ARROWHEAD PHARMACEUTICALS, INC. [US/US]; 225 South Lake Avenue, Suite 1050, Pasadena, CA 91101 (US). (72) Inventors: LI, Zhen; Arrowhead Pharmaceuticals, Inc., 502 S. Rosa Road, Madison, WI 53719 (US). ZHU, Rui; Arrowhead Pharmaceuticals, Inc., 502 S. Rosa Road, Madi- son, WI 53719 (US). WOODDELL, Christine I.; Arrow- head Pharmaceuticals, Inc., 502 S. Rosa Road, Madison, WI 53719 (US). GIVEN, Bruce D.; Arrowhead Pharma- ceuticals, Inc., 502 S. Rosa Road, Madison, WI 53719 (US). PEI, Tao; Arrowhead Pharmaceuticals, Inc., 502 S. Rosa Road, Madison, WI 53719 (US). LEWIS, David L.; 2930 Lakeland Avenue, Madison, WI 53704 (US). ALMEIDA, Lauren J.; 490 Togstad Glenn, Madison, WI 53711 (US). ROZEMA, David B.; 4361 Gils Way, Cross Plains, WI 53528 (US). WAKEFIELD, Darren H.; 5236 Stoneman Drive, Fitchburg, WI 53711 (US). (74) Agent: TEIGEN, Robert Michael; Arrowhead Pharma- ceuticals, Inc., 502 S. Rosa Road, Madison, WI 53719 (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). Declarations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(ii)) 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)) with sequence listing part of description (Rule 5.2(a)) (88) Date of publication of the international search report: 15 March 2018 (15.03.2018) Cr) O 1-1 (54) Title: RNAi AGENTS FOR HEPATITIS B VIRUS INFECTION \" (57) : Described are compositions and methods for inhibition of Hepatitis B virus gene expression. RNA interference (RNAi) agents for inhibiting the expression of Hepatitis B virus gene are described. The HBV RNAi agents disclosed herein may be targeted to cells, such as hepatocytes, for example, by using conjugated targeting ligands. Pharmaceutical compositions comprising one or more HBV RNAi agents optionally with one or more additional therapeutics are also described. Delivery of the described HBV RNAi agents N to infected liver in vivo provides for inhibition of HBV gene expression and treatment of diseases and conditions associated with HBV C infection.