CN112135635A - 吉西他滨衍生物的新型小分子药物偶联物 - Google Patents

吉西他滨衍生物的新型小分子药物偶联物 Download PDF

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Publication number
CN112135635A
CN112135635A CN201980024089.6A CN201980024089A CN112135635A CN 112135635 A CN112135635 A CN 112135635A CN 201980024089 A CN201980024089 A CN 201980024089A CN 112135635 A CN112135635 A CN 112135635A
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alkyl
compound
alkoxy
substituted
ester
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Pending
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CN201980024089.6A
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English (en)
Chinese (zh)
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S·A·艾弗雷特
C·A·科伯恩
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Marfurix Oncology Co ltd
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Marfurix Oncology Co ltd
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Publication of CN112135635A publication Critical patent/CN112135635A/zh
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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)
CN201980024089.6A 2018-02-02 2019-02-04 吉西他滨衍生物的新型小分子药物偶联物 Pending CN112135635A (zh)

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

Publications (1)

Publication Number Publication Date
CN112135635A true CN112135635A (zh) 2020-12-25

Family

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CN201980024089.6A Pending CN112135635A (zh) 2018-02-02 2019-02-04 吉西他滨衍生物的新型小分子药物偶联物

Country Status (13)

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
CN114349816A (zh) * 2021-11-30 2022-04-15 青岛博创生物科学研究院 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
CN119708099A (zh) * 2024-12-23 2025-03-28 中国药科大学 吉西他滨前药及其医药用途

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
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

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102458394A (zh) * 2009-05-01 2012-05-16 邓迪大学管理会 增殖性疾病状态的治疗或预防
CN104693256A (zh) * 2013-12-04 2015-06-10 杭州民生药业有限公司 吉西他滨衍生物、含该衍生物的组合物及所述衍生物的制药用途
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
CN106459130A (zh) * 2014-03-03 2017-02-22 纽科利制药公司 吉西他滨类似物
CN107295800A (zh) * 2015-02-25 2017-10-24 配体药物公司 吉西他滨衍生物

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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
GB0317009D0 (en) * 2003-07-21 2003-08-27 Univ Cardiff Chemical compounds

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102458394A (zh) * 2009-05-01 2012-05-16 邓迪大学管理会 增殖性疾病状态的治疗或预防
CN104693256A (zh) * 2013-12-04 2015-06-10 杭州民生药业有限公司 吉西他滨衍生物、含该衍生物的组合物及所述衍生物的制药用途
CN106459130A (zh) * 2014-03-03 2017-02-22 纽科利制药公司 吉西他滨类似物
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
CN107295800A (zh) * 2015-02-25 2017-10-24 配体药物公司 吉西他滨衍生物

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
MAGDALENA SLUSARCZYK ET AL.: "Application of ProTide Technology to Gemcitabine: A Successful Approach to Overcome the Key Cancer Resistance Mechanisms Leads to a New Agent (NUC-1031) in Clinical Development", JOURNAL OF MEDICINAL CHEMISTRY, no. 57, pages 1531 - 1542 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114349816A (zh) * 2021-11-30 2022-04-15 青岛博创生物科学研究院 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
CN119708099A (zh) * 2024-12-23 2025-03-28 中国药科大学 吉西他滨前药及其医药用途
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

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
JP2021512951A (ja) 2021-05-20
BR112020015747A2 (pt) 2020-12-08
IL276442A (en) 2020-09-30
CA3090272A1 (en) 2019-08-08
WO2019152911A1 (en) 2019-08-08

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