Patent SG-11201901131V-A (SG)
Title: Substituted pyrrolizine compounds and uses thereof
Inventor: DU JINFA
IPC: C07D519/00
Filed: 2017-08-25
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 1 MEM 0 11101 HOE HI 1 0 011111100111110111011 OE 11110 1111 011 Organization International Bureau (10) International Publication Number (43) International Publication Date .....0\"\" WO 2018/039531 Al 01 March 2018 (01.03.2018) W I PO I PCT (51) International Patent Classification: 94404 (US). WATKINS, William J.; c/o Gilead Sciences, CO7D 487/04 (2006.01) A61K 31/4192 (2006.01) Inc., 333 Lakeside Drive, Foster City, CA 94404 (US). CO7D 519/00 (2006.01) A61K 31/4245 (2006.01) (74) Agent: MARQUART, Timothy A. et al.; Gilead Sciences, A61K 31/407 (2006.01) A61K 31/4439 (2006.01) Inc., 333 Lakeside Drive, Foster City, California 94404 A61K 31/433 (2006.01) (US). (21) International Application Number: PCT/US2017/048565 (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, (22) International Filing Date: AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, 25 August 2017 (25.08.2017) 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, (25) Filing Language: English HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, (26) Publication Language: English KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, (30) Priority Data: 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, 62/380,063 26 August 2016 (26.08.2016) US November 2016 (01.11.2016) US 62/416,020 01 TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (71) Applicant: GILEAD SCIENCES, INC. [US/US]; 333 (84) Designated States (unless otherwise indicated, for every Lakeside Drive, Foster City, CA 94404 (US). kind of regional protection available): ARIPO (BW, GH, (72) Inventors: DU, Jinfa; 813 Bay Harbor Drive, Redwood GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, City, CA 94065 (US). KAPLAN, Joshua A.; _ c/o Gilead UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, CA 94404 TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, = Sciences, Inc., 333 Lakeside Drive, Foster City, Avenue, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, (US). KIRSCHBERG, Thorsten A.; 2230 Eaton Tetsuya; c/ MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, = San Carlos, CA 94070 (US). KOBAYASHI, Foster City, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, — o Gilead Sciences, Inc., 333 Lakeside Drive, c/o Gilead KM, ML, MR, NE, SN, TD, TG). = CA 94404 (US). LAZERWITH, Scott E.; = Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404 Inc., 333 Declarations under Rule 4.17: (US). LEE, Rick Andrew; c/o Gilead Sciences, = — Lakeside Drive, Foster City, CA 94404 (US). MEDLEY, — as to applicant's entitlement to apply for and be granted a Jonathan William; c/o Gilead Sciences, Inc., _ 333 Lake- patent (Rule 4.17(ii)) =side Drive, Foster City, CA 94404 (US). MITCHELL, = — as to the applicant's entitlement to claim the priority of the Michael L.; c/o Gilead Sciences, Inc., 333 Lakeside Drive, earlier application (Rule 4.17(iii)) Philip An- Published: Foster City, CA 94404 (US). MORGANELLI, Drive, Fos- = thony; c/o Gilead Sciences, Inc., 333 Lakeside — with international search report (Art. 21(3)) c/o Gilead PYUN, Hyung-Jung; = ter City, CA 94404 (US). CA 94404 Sciences, Inc., 333 Lakeside Drive, Foster City, = (US). SHEVICK, Sophia L.; 12627 Unit A, El Camino _ Real, San Diego, CA 92130 (US). SQUIRES, Neil H.; c/o = City, CA Gilead Sciences, Inc., 333 Lakeside Drive, Foster = = = AND USES THEREOF (54) Title: SUBSTITUTED PYRROLIZINE COMPOUNDS 1-1 A 1-1 en kin tz. RI 0 (I) Cr) \ N HN-R 4 © ---.... H QQ R 3 P S I © ei : This application relates to substituted fused pyrrole compounds of formula I, and pharmaceutical compositions com- 0 (57) prising them which inhibit HBV replication, and methods of making and using them. Formula (I) P''