CA3007058C - Cytarabine conjugates for cancer therapy - Google Patents

Cytarabine conjugates for cancer therapy Download PDF

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Publication number
CA3007058C
CA3007058C CA3007058A CA3007058A CA3007058C CA 3007058 C CA3007058 C CA 3007058C CA 3007058 A CA3007058 A CA 3007058A CA 3007058 A CA3007058 A CA 3007058A CA 3007058 C CA3007058 C CA 3007058C
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CA
Canada
Prior art keywords
subject
acid
compound
cytarabine
administration
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CA3007058A
Other languages
English (en)
French (fr)
Other versions
CA3007058A1 (en
Inventor
Stela Gengrinovitch
Ruth BEN YAKAR
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Biosight Ltd
Original Assignee
Biosight 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 Biosight Ltd filed Critical Biosight Ltd
Publication of CA3007058A1 publication Critical patent/CA3007058A1/en
Application granted granted Critical
Publication of CA3007058C publication Critical patent/CA3007058C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542Carboxylic acids, e.g. a fatty acid or an amino acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Saccharide Compounds (AREA)
CA3007058A 2015-12-03 2016-01-25 Cytarabine conjugates for cancer therapy Active CA3007058C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562262428P 2015-12-03 2015-12-03
US62/262,428 2015-12-03
PCT/IL2016/050077 WO2017093993A1 (en) 2015-12-03 2016-01-25 Cytarabine conjugates for cancer therapy

Publications (2)

Publication Number Publication Date
CA3007058A1 CA3007058A1 (en) 2017-06-08
CA3007058C true CA3007058C (en) 2023-10-17

Family

ID=58796462

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3007058A Active CA3007058C (en) 2015-12-03 2016-01-25 Cytarabine conjugates for cancer therapy

Country Status (10)

Country Link
US (1) US11058701B2 (enExample)
EP (1) EP3383407B1 (enExample)
JP (3) JP7149183B2 (enExample)
CN (1) CN108289905A (enExample)
AU (2) AU2016362830B2 (enExample)
BR (1) BR112018011177A2 (enExample)
CA (1) CA3007058C (enExample)
IL (2) IL259631B (enExample)
RU (1) RU2708672C1 (enExample)
WO (1) WO2017093993A1 (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12071450B2 (en) 2015-12-03 2024-08-27 Biosight Ltd. Salts of conjugates for cancer therapy
IL259569B2 (en) 2015-12-03 2024-03-01 Biosight Ltd Salts of cytarabine-amino acids conjugates
US12064445B2 (en) 2015-12-03 2024-08-20 Biosight Ltd. Cytarabine conjugates for cancer therapy
WO2019012328A1 (en) * 2017-07-09 2019-01-17 Biosight Pharma ANTICANCER POLY THERAPY
CN110590862A (zh) * 2019-11-01 2019-12-20 南京师范大学 阿糖胞苷4-n位氨基酸衍生物及其制备方法与应用
WO2021156869A1 (en) * 2020-02-04 2021-08-12 Biosight Ltd. Aspacytarabine pharmaceutical compositions and uses thereof
JP2023522420A (ja) * 2020-04-23 2023-05-30 バイオサイト リミテッド 血液がんの治療のための方法及びレジメン
KR20230074156A (ko) * 2020-09-21 2023-05-26 바이오사이트 리미티드 아스파시타라빈의 결정질 형태
CN112409431B (zh) * 2020-12-07 2023-04-21 武汉伯瑞恒医药科技有限公司 阿糖胞苷结构类似物及其制备方法和用途
CA3239219A1 (en) * 2021-11-21 2023-05-25 Biosight Ltd. Cytarabine-amino acid based prodrug for the treatment of cancer
WO2023175622A1 (en) * 2022-03-17 2023-09-21 Biosight Ltd. Crystalline forms of aspacytarabine
WO2023228177A1 (en) * 2022-05-22 2023-11-30 Biosight Ltd. Compositions comprising aspacytarabine and additional compounds, and use thereof

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2949451A (en) 1959-04-21 1960-08-16 Hoffmann La Roche Preparation of thymidine and deoxyfluorouridine, and intermediates therefor
US3041335A (en) 1959-04-21 1962-06-26 Hoffmann La Roche Mercury salts of nitrogen heterocyclics and preparation thereof
US4179337A (en) 1973-07-20 1979-12-18 Davis Frank F Non-immunogenic polypeptides
US4296105A (en) 1978-08-03 1981-10-20 Institut International De Pathologie Cellulaire Et Moleculaire Derivatives of doxorubicine, their preparation and use
US4348522A (en) 1980-01-23 1982-09-07 Starks Associates, Inc. N-(phosphonacetyl)-L-aspartic acid salts with piperazine, cyclohexylamine and calcium
EP0329184A3 (en) 1988-02-19 1990-05-23 Neorx Corporation Antimers and antimeric conjugation
RU2085557C1 (ru) 1991-09-30 1997-07-27 Санкио Компани Лимитед Производные нуклеозидов пиримидина или их фармацевтически приемлемые соли и способ их получения
US5643957A (en) 1993-04-22 1997-07-01 Emisphere Technologies, Inc. Compounds and compositions for delivering active agents
EP0737077A1 (en) * 1994-01-11 1996-10-16 Targetech, Inc. Hepatocyte-targeted drug conjugates
ATE380559T1 (de) 1994-08-19 2007-12-15 Wallone Region Konjugate enthaltend ein antitumorales mittel und deren verwendung
JPH0859688A (ja) 1994-08-25 1996-03-05 Mitsui Toatsu Chem Inc 5’−チオノエステル置換トリフルオロチミジン誘導体およびそれを有効成分とする制癌剤
US6001347A (en) 1995-03-31 1999-12-14 Emisphere Technologies, Inc. Compounds and compositions for delivering active agents
US5650386A (en) 1995-03-31 1997-07-22 Emisphere Technologies, Inc. Compositions for oral delivery of active agents
AU2595697A (en) 1996-03-29 1997-10-22 Emisphere Technologies, Inc. Compounds and compositions for delivering active agents
US6258774B1 (en) 1998-03-19 2001-07-10 University Of Medicine And Dentistry Of New Jersey Carrier for in vivo delivery of a therapeutic agent
JP2003518000A (ja) 1998-12-11 2003-06-03 コールター ファーマシューティカル,インコーポレイティド プロドラッグ化合物およびその調製方法
EP1556398B1 (en) 2002-10-31 2009-09-09 Metabasis Therapeutics, Inc. Novel cytarabine monophosphate prodrugs
EP1718145A4 (en) 2004-02-02 2012-03-07 Biosight Ltd CONJUGATES FOR CANCER THERAPY AND DIAGNOSIS
JP5410295B2 (ja) 2006-12-13 2014-02-05 ジボダン ネーデルランド サービシーズ ビー.ヴイ. カルボン酸およびプリン、ピリミジン、ヌクレオシドまたはヌクレオチドのフレーバー調節誘導体
CN101812105A (zh) 2009-02-25 2010-08-25 沈阳药科大学 阿糖胞苷5’-o-氨基酸酯和其盐类及其制备方法
JP5873656B2 (ja) * 2011-06-13 2016-03-01 株式会社Ihi 金属サレン錯体化合物、局所麻酔薬剤及び抗悪性腫瘍薬剤
WO2013058294A1 (ja) 2011-10-18 2013-04-25 味の素株式会社 膵臓癌及び/又は胆道癌治療薬
WO2014097318A2 (en) * 2012-12-18 2014-06-26 Godavari Biorefineries Limited Agents for eliminating tumour-initiating cells
WO2015178265A1 (ja) 2014-05-23 2015-11-26 日本化薬株式会社 新規なグルタミン酸誘導体およびその用途

Also Published As

Publication number Publication date
IL259631B (en) 2021-10-31
CA3007058A1 (en) 2017-06-08
JP2020183419A (ja) 2020-11-12
JP7417658B2 (ja) 2024-01-18
US11058701B2 (en) 2021-07-13
WO2017093993A1 (en) 2017-06-08
AU2022204373A1 (en) 2022-07-28
JP2018535989A (ja) 2018-12-06
IL287644A (en) 2021-12-01
EP3383407A1 (en) 2018-10-10
JP2022097619A (ja) 2022-06-30
RU2708672C1 (ru) 2019-12-11
AU2016362830B2 (en) 2022-07-14
US20180369265A1 (en) 2018-12-27
AU2022204373B2 (en) 2024-01-25
BR112018011177A2 (pt) 2018-11-21
IL259631A (en) 2018-07-31
EP3383407B1 (en) 2023-12-06
JP7149183B2 (ja) 2022-10-06
AU2016362830A1 (en) 2018-07-12
CN108289905A (zh) 2018-07-17
EP3383407A4 (en) 2019-07-17

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