BR112015010941A2 - pró-fármacos de gemcitabina e suas utilizações - Google Patents

pró-fármacos de gemcitabina e suas utilizações

Info

Publication number
BR112015010941A2
BR112015010941A2 BR112015010941A BR112015010941A BR112015010941A2 BR 112015010941 A2 BR112015010941 A2 BR 112015010941A2 BR 112015010941 A BR112015010941 A BR 112015010941A BR 112015010941 A BR112015010941 A BR 112015010941A BR 112015010941 A2 BR112015010941 A2 BR 112015010941A2
Authority
BR
Brazil
Prior art keywords
substituted
group
cycloheteroalkyl
formula
compounds
Prior art date
Application number
BR112015010941A
Other languages
English (en)
Inventor
I Wu Laurence
Original Assignee
Boyen Therapeutics 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 Boyen Therapeutics Inc filed Critical Boyen Therapeutics Inc
Publication of BR112015010941A2 publication Critical patent/BR112015010941A2/pt

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Classifications

    • 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
    • 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
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Dermatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

resumo “pró-fármacos de gemcitabina e suas utilizações” a presente invenção proporciona compostos de acordo com a fórmula i e seus sais farmaceuticamente aceitáveis. para os compostos de fórmula i, r1 e r2 são independentemente selecionados a partir do grupo que consiste em h, -c(=o)(ch2)2-arilo, e c(=o)(ch2)n-c(=o)nh-arilo . o índice n é de 2 a 6. r3 é selecionado a partir do grupo que consiste em h e -c(=o)-o-r4; e r4 é selecionado a partir do grupo que consiste em alquilo, alquilo substituído, alcenilo, alcenilo substituído, alcinilo, alcinilo substituído, arilalquilo, arilalquilo substituído, ciclo-heteroalquilo, ciclo-heteroalquilo substituo, heteroalquilo substituo e heteroalquilo. os compostos são fornecidos em que pelo menos um de r1 e r2 é diferente de h. composições farmacêuticas, métodos para a inibição do crescimento de células cancerosas, e métodos para o tratamento do cancro são também fornecidos.
BR112015010941A 2012-11-13 2013-11-12 pró-fármacos de gemcitabina e suas utilizações BR112015010941A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261725643P 2012-11-13 2012-11-13
PCT/US2013/069640 WO2014078295A1 (en) 2012-11-13 2013-11-12 Gemcitabine prodrugs and uses thereof

Publications (1)

Publication Number Publication Date
BR112015010941A2 true BR112015010941A2 (pt) 2017-07-11

Family

ID=50681903

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112015010941A BR112015010941A2 (pt) 2012-11-13 2013-11-12 pró-fármacos de gemcitabina e suas utilizações

Country Status (10)

Country Link
US (3) US8956613B2 (pt)
EP (1) EP2919790B1 (pt)
JP (1) JP6420247B2 (pt)
KR (1) KR20150082606A (pt)
CN (1) CN104968353B (pt)
AU (1) AU2013345007B2 (pt)
BR (1) BR112015010941A2 (pt)
CA (1) CA2891124A1 (pt)
SG (1) SG11201503773SA (pt)
WO (1) WO2014078295A1 (pt)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8956613B2 (en) 2012-11-13 2015-02-17 BoYen Therapeutics, Inc. Gemcitabine prodrugs and uses thereof
EP3125920B1 (en) 2014-04-04 2020-12-23 Del Mar Pharmaceuticals Dianhydrogalactitol, diacetyldianhydrogalactitol or dibromodulcitol to treat non-small-cell carcinoma of the lung and ovarian cancer
WO2016078397A1 (zh) * 2014-11-17 2016-05-26 常州方圆制药有限公司 新型胞苷衍生物及其应用
WO2016078163A1 (zh) * 2014-11-17 2016-05-26 常州方圆制药有限公司 新型胞苷衍生物二聚体及其应用
WO2016078160A1 (zh) * 2014-11-17 2016-05-26 常州方圆制药有限公司 胞苷衍生物及其应用
WO2016078399A1 (zh) * 2014-11-17 2016-05-26 常州方圆制药有限公司 新型胞苷衍生物二聚体及其应用
ITUB20159671A1 (it) * 2015-12-22 2017-06-22 Maurizio Ceruti Carbammati lipidici di farmaci antitumorali
HUE050290T2 (hu) * 2015-12-23 2020-11-30 NuCana plc Kombinált terápia
CN106946960A (zh) * 2017-03-29 2017-07-14 郑州泰基鸿诺医药股份有限公司 一种吉西他滨前药的晶型、制备方法、用途和药物组合物
CN110831605A (zh) 2017-04-26 2020-02-21 托马斯·I.·卡尔曼 多靶标的核苷衍生物
CN108329371B (zh) * 2018-03-06 2021-04-09 沈阳药科大学 白蛋白结合型吉西他滨前药及其合成和应用
WO2019204869A1 (en) * 2018-04-26 2019-10-31 NanoMed Holdings Pty Ltd Gemcitabine amphiphile prodrugs
GR1009958B (el) * 2019-04-24 2021-03-18 ΕΝΟΡΑΣΙΣ ΑΝΩΝΥΜΗ ΕΜΠΟΡΙΚΗ ΕΤΑΙΡΕΙΑ ΦΑΡΜΑΚΕΥΤΙΚΩΝ ΚΑΙ ΙΑΤΡΙΚΩΝ ΥΛΙΚΩΝ ΚΑΙ ΜΗΧΑΝΗΜΑΤΩΝ με δ.τ. "ΕΝΟΡΑΣΙΣ Α.Ε." Παραγωγα γεμσιταβινης και μεθοδοι δημιουργιας παραγωγων γεμσιταβινης
CN114011581B (zh) * 2021-11-09 2023-03-24 昆明理工大学 一种弱酸性条件下铜硫分离的抑制剂制备方法及其应用

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US4814438A (en) 1986-12-24 1989-03-21 Eli Lilly And Company Immunoglobulin conjugates of 2',2'-difluronucleosides
US4994558A (en) 1986-12-24 1991-02-19 Eli Lilly And Company Immunoglobulin conjugates
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CN103130854A (zh) 2013-01-31 2013-06-05 华东师范大学 维生素e琥珀酸酯化吉西他滨前药及应用

Also Published As

Publication number Publication date
US9890189B2 (en) 2018-02-13
SG11201503773SA (en) 2015-06-29
US20140134160A1 (en) 2014-05-15
JP6420247B2 (ja) 2018-11-07
EP2919790B1 (en) 2018-04-04
CA2891124A1 (en) 2014-05-22
JP2016503414A (ja) 2016-02-04
US8956613B2 (en) 2015-02-17
WO2014078295A8 (en) 2015-05-21
WO2014078295A1 (en) 2014-05-22
US20170107245A1 (en) 2017-04-20
AU2013345007B2 (en) 2018-08-30
EP2919790A4 (en) 2016-04-06
US9540410B2 (en) 2017-01-10
EP2919790A1 (en) 2015-09-23
CN104968353B (zh) 2017-12-22
US20150132298A1 (en) 2015-05-14
KR20150082606A (ko) 2015-07-15
CN104968353A (zh) 2015-10-07
AU2013345007A1 (en) 2015-05-21

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Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]
B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]