Patent SG-11201806133U-A (SG)
Title: Intermediates in the synthesis of eribulin and related methods of synthesis
Inventor: BARAN PHIL
IPC: C07D493/22
Filed: 2017-02-10
Abstract: International Patent Classification: A61K 31/35 (2006.01) C07D 493/04 (2006.01) A61K 31/357 (2006.01) C07D 493/22 (2006.01) C07D 307/20 (2006.01) (21) International Application Number: PCT/US2017/017501 (22) International Filing Date: 10 February 2017 (10.02.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/294,538 12 February 2016 (12.02.2016) US (71) Applicant: EISAI & R&D MANAGEMENT CO., LTD. [JP/JP]; 6-10, Koishikawa 4-chome, Bunkyo-ku, 112-8088 (JP). (72) Inventors; and (71) Applicants US only): BARAN, Phil, S. [US/US]; 5160 Great Meadow Drive, San Diego, CA 92130 (US). CHASE, Charles, E. [US/US]; 18 Devonshire Lane, Lon- donderry, NH 03053 (US). FANG, Francis, G. [US/US]; 16 Greybirch Road, Andover, MA 01810 (US). (74) Agents: MCDONALD, J., Cooper et al.; Clark & Elbing LLP, 101 Federal Street, 15th Floor, Boston, MA 02110 (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). arations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(ii)) as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) of inventorship (Rule 4.17(iv)) Decl [Continued on next page] (54) Title: INTERMEDIATES IN THE SYNTHESIS OF ERIBULIN AND RELATED METHODS OF SYNTHESIS HG. 1 94155_197_00 . 0 020 0.40 ' 070 0.80 1 00 7.90 1.40 100 1.90 m1513_197_01 2.20 2.40 2.50 2.80 3.00 2 48 0 6:7 - 411.W•6'''768' , Fi , iTo 23 .ia. .FLO e 40155_197_02 . 0 2.00 . 2.20 2.40 ' 2.50 0 2.25 6. 2 . . . -0.00 0.20 0.40 0.50 0.80 1.00 1.20 1.40 1.50 45155_197_03 (III) -4 , j I \" 1:20 1 1 80 1 80 . 40 ,.._ 2.60 „_ 2 : 00 .,,_3.00.., (57) : The invention relates to methods and intermediates useful in the synthesis of eribulin. W O 20 17 / 13966 4 Al .80 2.00 W 220 2.40 2.89 2.80 9. 229 1. Scan ES+ TIC 7.90e8 1. Scan ES+ TIC 6.08e8 1. Scan ES+ TIC 5.68e8 1. Scan ES+ TIC 6.00e8 (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 2017/139664 Al 17 August 2017 (17.08.2017) WIPO I PCT 111111111111110111011111111111010111110 011101111101111111001111111111111110111111 WO 2017/139664 Al MIDEDIM000101011101010M011110H011101100IM1110VOIMIE Published: — with international search report (Art. 21(3))