JP2021512951A - ゲムシタビン誘導体の新規小分子薬物コンジュゲート - Google Patents

ゲムシタビン誘導体の新規小分子薬物コンジュゲート Download PDF

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Publication number
JP2021512951A
JP2021512951A JP2020564033A JP2020564033A JP2021512951A JP 2021512951 A JP2021512951 A JP 2021512951A JP 2020564033 A JP2020564033 A JP 2020564033A JP 2020564033 A JP2020564033 A JP 2020564033A JP 2021512951 A JP2021512951 A JP 2021512951A
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alkyl
substituted
compound
alkoxy
pharmaceutically acceptable
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JP2021512951A5 (https=
JPWO2019152911A5 (https=
Inventor
スティーブン アルバート エベレット
スティーブン アルバート エベレット
クレイグ アラン コーバン
クレイグ アラン コーバン
Original Assignee
メイベリックス オンコロジー インコーポレイテッド
メイベリックス オンコロジー インコーポレイテッド
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Publication of JP2021512951A publication Critical patent/JP2021512951A/ja
Publication of JP2021512951A5 publication Critical patent/JP2021512951A5/ja
Publication of JPWO2019152911A5 publication Critical patent/JPWO2019152911A5/ja
Priority to JP2024019158A priority Critical patent/JP2024073414A/ja
Pending legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/54—Medicinal 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
    • A61K47/545—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds 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
    • A61K31/7064—Compounds 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
    • A61K31/7068—Compounds 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/0004—Screening or testing of compounds for diagnosis of disorders, assessment of conditions, e.g. renal clearance, gastric emptying, testing for diabetes, allergy, rheuma, pancreas functions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/575—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/5758—Immunoassay; Biospecific binding assay; Materials therefor for cancer involving compounds serving as markers for tumours, cancers or neoplasias, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides or metabolites
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/90—Enzymes; Proenzymes
    • G01N2333/902—Oxidoreductases (1.)
    • G01N2333/90245—Oxidoreductases (1.) acting on paired donors with incorporation of molecular oxygen (1.14)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2440/00—Post-translational modifications [PTMs] in chemical analysis of biological material
    • G01N2440/24—Post-translational modifications [PTMs] in chemical analysis of biological material hydroxylation

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pathology (AREA)
  • Hematology (AREA)
  • Toxicology (AREA)
  • Rheumatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Endocrinology (AREA)
  • Cell Biology (AREA)
  • Diabetes (AREA)
  • Microbiology (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
JP2020564033A 2018-02-02 2019-02-04 ゲムシタビン誘導体の新規小分子薬物コンジュゲート Pending JP2021512951A (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2024019158A JP2024073414A (ja) 2018-02-02 2024-02-13 ゲムシタビン誘導体の新規小分子薬物コンジュゲート

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862625779P 2018-02-02 2018-02-02
US62/625,779 2018-02-02
PCT/US2019/016477 WO2019152911A1 (en) 2018-02-02 2019-02-04 Novel small molecule drug conjugates of gemcitabine derivatives

Related Child Applications (1)

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JP2024019158A Division JP2024073414A (ja) 2018-02-02 2024-02-13 ゲムシタビン誘導体の新規小分子薬物コンジュゲート

Publications (3)

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JP2021512951A true JP2021512951A (ja) 2021-05-20
JP2021512951A5 JP2021512951A5 (https=) 2022-02-14
JPWO2019152911A5 JPWO2019152911A5 (https=) 2022-02-14

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JP2020564033A Pending JP2021512951A (ja) 2018-02-02 2019-02-04 ゲムシタビン誘導体の新規小分子薬物コンジュゲート
JP2024019158A Pending JP2024073414A (ja) 2018-02-02 2024-02-13 ゲムシタビン誘導体の新規小分子薬物コンジュゲート

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Country Link
US (1) US20210380626A1 (https=)
EP (1) EP3746133A1 (https=)
JP (2) JP2021512951A (https=)
KR (1) KR20200118828A (https=)
CN (1) CN112135635A (https=)
AU (1) AU2019216514A1 (https=)
BR (1) BR112020015747A2 (https=)
CA (1) CA3090272A1 (https=)
EA (1) EA202091857A1 (https=)
IL (1) IL276442A (https=)
PH (1) PH12020551178A1 (https=)
SG (1) SG11202007381YA (https=)
WO (1) WO2019152911A1 (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2026009986A1 (ja) * 2024-07-05 2026-01-08 学校法人東京理科大学 化合物の製造方法及び化合物
WO2026009987A1 (ja) * 2024-07-05 2026-01-08 学校法人東京理科大学 化合物の製造方法、化合物、及びヌクレオチドプロドラッグ前駆体

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20210367A1 (es) * 2018-02-02 2021-02-26 Maverix Oncology Inc Conjugados de farmacos de molecula pequena de monofosfato de gemcitabina
CN114349816B (zh) * 2021-11-30 2024-08-30 潍坊博创国际生物医药研究院 一种基于氨肽酶n/cd13的小分子偶联分子及其制备方法和应用
CN119708099B (zh) * 2024-12-23 2025-10-24 中国药科大学 吉西他滨前药及其医药用途

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006528162A (ja) * 2003-07-21 2006-12-14 ユニバーシティ、カレッジ、カーディフ、コンサルタンツ、リミテッド 化合物
JP2012525364A (ja) * 2009-05-01 2012-10-22 ユニバーシティー コート オブ ジ ユニバーシティー オブ ダンディー 増殖性状態の処置または予防
WO2015134334A1 (en) * 2014-03-03 2015-09-11 Suo Zucai Gemcitabine analogs
CN105001291A (zh) * 2014-04-15 2015-10-28 上海知萌生物医药科技有限公司 吉西他滨化学传递前药及其制备方法和应用

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2531599A (en) 1998-02-12 1999-08-30 De Montfort University Hydroxylation activated drug release
US7148226B2 (en) 2003-02-21 2006-12-12 Agouron Pharmaceuticals, Inc. Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same
JP6212831B2 (ja) * 2013-12-04 2017-10-18 杭州源昶医薬科技有限公司 ゲムシタビン誘導体、該誘導体を含む組成物及び該誘導体の製薬用途
US20180044368A1 (en) * 2015-02-25 2018-02-15 Ligand Pharmaceuticals, Inc. Gemcitabine derivatives

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006528162A (ja) * 2003-07-21 2006-12-14 ユニバーシティ、カレッジ、カーディフ、コンサルタンツ、リミテッド 化合物
JP2012525364A (ja) * 2009-05-01 2012-10-22 ユニバーシティー コート オブ ジ ユニバーシティー オブ ダンディー 増殖性状態の処置または予防
WO2015134334A1 (en) * 2014-03-03 2015-09-11 Suo Zucai Gemcitabine analogs
CN105001291A (zh) * 2014-04-15 2015-10-28 上海知萌生物医药科技有限公司 吉西他滨化学传递前药及其制备方法和应用

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
JARKKO RAUTIO ET AL.: "Prodrugs:design and clinical applications", NATURE REVIEWS DRUG DISCOVERY, vol. 7巻, JPN6023001299, 2008, pages 255 - 270, ISSN: 0005169954 *
MAGDALENA SLUSARCZYK; ET AL: "APPLICATION OF PROTIDE TECHNOLOGY TO GEMCITABINE: A SUCCESSFUL APPROACH TO OVERCOME 以下備考", JOURNAL OF MEDICINAL CHEMISTRY, vol. VOL:57, NR:4, JPN5021006337, 14 February 2014 (2014-02-14), pages 1531 - 1542, ISSN: 0005169953 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2026009986A1 (ja) * 2024-07-05 2026-01-08 学校法人東京理科大学 化合物の製造方法及び化合物
WO2026009987A1 (ja) * 2024-07-05 2026-01-08 学校法人東京理科大学 化合物の製造方法、化合物、及びヌクレオチドプロドラッグ前駆体

Also Published As

Publication number Publication date
KR20200118828A (ko) 2020-10-16
US20210380626A1 (en) 2021-12-09
SG11202007381YA (en) 2020-08-28
EP3746133A1 (en) 2020-12-09
EA202091857A1 (ru) 2020-12-04
PH12020551178A1 (en) 2021-06-07
AU2019216514A1 (en) 2020-09-24
JP2024073414A (ja) 2024-05-29
BR112020015747A2 (pt) 2020-12-08
IL276442A (en) 2020-09-30
CN112135635A (zh) 2020-12-25
CA3090272A1 (en) 2019-08-08
WO2019152911A1 (en) 2019-08-08

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