BR112020015747A2 - Conjugados de fármaco de moléculas pequenas de derivados de gemcitabina - Google Patents

Conjugados de fármaco de moléculas pequenas de derivados de gemcitabina Download PDF

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Publication number
BR112020015747A2
BR112020015747A2 BR112020015747-3A BR112020015747A BR112020015747A2 BR 112020015747 A2 BR112020015747 A2 BR 112020015747A2 BR 112020015747 A BR112020015747 A BR 112020015747A BR 112020015747 A2 BR112020015747 A2 BR 112020015747A2
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BR
Brazil
Prior art keywords
alkyl
compound
halo
alkoxy
ester
Prior art date
Application number
BR112020015747-3A
Other languages
English (en)
Portuguese (pt)
Inventor
Steven Albert Everett
Craig Alan COBURN
Original Assignee
Maverix Oncology, Inc.
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 Maverix Oncology, Inc. filed Critical Maverix Oncology, Inc.
Publication of BR112020015747A2 publication Critical patent/BR112020015747A2/pt

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    • 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
    • A61K47/545Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • C07H19/10Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • 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
    • A61K49/00Preparations for testing in vivo
    • A61K49/0004Screening or testing of compounds for diagnosis of disorders, assessment of conditions, e.g. renal clearance, gastric emptying, testing for diabetes, allergy, rheuma, pancreas functions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/575Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/5758Immunoassay; 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
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/90Enzymes; Proenzymes
    • G01N2333/902Oxidoreductases (1.)
    • G01N2333/90245Oxidoreductases (1.) acting on paired donors with incorporation of molecular oxygen (1.14)
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2440/00Post-translational modifications [PTMs] in chemical analysis of biological material
    • G01N2440/24Post-translational modifications [PTMs] in chemical analysis of biological material hydroxylation

Landscapes

  • 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)
BR112020015747-3A 2018-02-02 2019-02-04 Conjugados de fármaco de moléculas pequenas de derivados de gemcitabina BR112020015747A2 (pt)

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
BR112020015747A2 true BR112020015747A2 (pt) 2020-12-08

Family

ID=65494546

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112020015747-3A BR112020015747A2 (pt) 2018-02-02 2019-02-04 Conjugados de fármaco de moléculas pequenas de derivados de gemcitabina

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=)

Families Citing this family (5)

* 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
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
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

Family Cites Families (8)

* 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
GB0317009D0 (en) * 2003-07-21 2003-08-27 Univ Cardiff Chemical compounds
GB0907551D0 (en) * 2009-05-01 2009-06-10 Univ Dundee Treatment or prophylaxis of proliferative conditions
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
WO2015134334A1 (en) * 2014-03-03 2015-09-11 Suo Zucai Gemcitabine analogs
CN105001291B (zh) * 2014-04-15 2018-12-04 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
US20180044368A1 (en) * 2015-02-25 2018-02-15 Ligand Pharmaceuticals, Inc. Gemcitabine derivatives

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
IL276442A (en) 2020-09-30
CN112135635A (zh) 2020-12-25
CA3090272A1 (en) 2019-08-08
WO2019152911A1 (en) 2019-08-08

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Legal Events

Date Code Title Description
B350 Update of information on the portal [chapter 15.35 patent gazette]
B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 5A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2760 DE 28-11-2023 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.