SG11201806133UA - Intermediates in the synthesis of eribulin and related methods of synthesis - Google Patents

Intermediates in the synthesis of eribulin and related methods of synthesis

Info

Publication number
SG11201806133UA
SG11201806133UA SG11201806133UA SG11201806133UA SG11201806133UA SG 11201806133U A SG11201806133U A SG 11201806133UA SG 11201806133U A SG11201806133U A SG 11201806133UA SG 11201806133U A SG11201806133U A SG 11201806133UA SG 11201806133U A SG11201806133U A SG 11201806133UA
Authority
SG
Singapore
Prior art keywords
international
synthesis
tic
scan
rule
Prior art date
Application number
SG11201806133UA
Inventor
Phil Baran
Charles Chase
Francis Fang
Original Assignee
Eisai R&D Man Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Eisai R&D Man Co Ltd filed Critical Eisai R&D Man Co Ltd
Publication of SG11201806133UA publication Critical patent/SG11201806133UA/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/22—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains four or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis

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))
SG11201806133UA 2016-02-12 2017-02-10 Intermediates in the synthesis of eribulin and related methods of synthesis SG11201806133UA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662294538P 2016-02-12 2016-02-12
PCT/US2017/017501 WO2017139664A1 (en) 2016-02-12 2017-02-10 Intermediates in the synthesis of eribulin and related methods of synthesis

Publications (1)

Publication Number Publication Date
SG11201806133UA true SG11201806133UA (en) 2018-08-30

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201806133UA SG11201806133UA (en) 2016-02-12 2017-02-10 Intermediates in the synthesis of eribulin and related methods of synthesis

Country Status (10)

Country Link
US (1) US10676481B2 (en)
EP (1) EP3413887B1 (en)
JP (1) JP6786610B2 (en)
KR (1) KR20180107243A (en)
CN (1) CN108601760A (en)
IL (1) IL260717B (en)
MX (1) MX2018009794A (en)
RU (1) RU2732575C2 (en)
SG (1) SG11201806133UA (en)
WO (1) WO2017139664A1 (en)

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CA3028453C (en) 2004-06-03 2021-07-27 Eisai R&D Management Co., Ltd. Intermediates for the preparation of analogs of halichondrin b
CN101883763B (en) 2007-10-03 2016-04-20 卫材R&D管理有限公司 For the synthesis of intermediate and the method for halichondrin b analogs
WO2011094339A1 (en) 2010-01-26 2011-08-04 Eisai R&D Management Co., Ltd. Furo [3, 2 -b] pyrane derivatives useful in the synthesis of halichondrin b analogs
CN105683198B (en) 2013-11-04 2019-03-12 卫材R&D管理有限公司 Useful big cyclization and intermediate in the analog synthesis of halichondrin B
RU2676486C1 (en) 2013-12-06 2018-12-29 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Methods for synthesis of halichondrin b analogs
RU2739034C2 (en) 2015-05-07 2020-12-21 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Macrocyclisation reaction and intermediate compound and other fragments, useful in synthesis of macrolides of halichondrins
WO2018006031A1 (en) 2016-06-30 2018-01-04 Eisai R&D Management Co., Ltd. Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereof
SG11202005548WA (en) 2018-01-03 2020-07-29 Eisai R&D Man Co Ltd Prins reaction and compounds useful in the synthesis of halichondrin macrolides and analogs thereof
CN110568121A (en) * 2019-07-11 2019-12-13 山东省药学科学院 Eribulin and detection method of related substances in eribulin-containing preparation

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Also Published As

Publication number Publication date
CN108601760A (en) 2018-09-28
MX2018009794A (en) 2018-12-17
US10676481B2 (en) 2020-06-09
EP3413887A1 (en) 2018-12-19
JP2019504839A (en) 2019-02-21
RU2018132264A (en) 2020-03-12
RU2018132264A3 (en) 2020-04-15
US20190300542A1 (en) 2019-10-03
WO2017139664A1 (en) 2017-08-17
IL260717B (en) 2020-10-29
EP3413887B1 (en) 2021-04-07
KR20180107243A (en) 2018-10-01
EP3413887A4 (en) 2019-08-14
RU2732575C2 (en) 2020-09-21
JP6786610B2 (en) 2020-11-18
WO2017139664A8 (en) 2018-07-26

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