HRP20161293T1 - Rnki-molekula za sintezu timidilata i njezina uporaba - Google Patents

Rnki-molekula za sintezu timidilata i njezina uporaba Download PDF

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Publication number
HRP20161293T1
HRP20161293T1 HRP20161293TT HRP20161293T HRP20161293T1 HR P20161293 T1 HRP20161293 T1 HR P20161293T1 HR P20161293T T HRP20161293T T HR P20161293TT HR P20161293 T HRP20161293 T HR P20161293T HR P20161293 T1 HRP20161293 T1 HR P20161293T1
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Croatia
Prior art keywords
rnai
pharmaceutical composition
antitumor agent
molecule
vector
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HRP20161293TT
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English (en)
Inventor
Hiromi Wada
Cheng Long HUANG
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Delta-Fly Pharma, Inc.
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Application filed by Delta-Fly Pharma, Inc. filed Critical Delta-Fly Pharma, Inc.
Publication of HRP20161293T1 publication Critical patent/HRP20161293T1/hr

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    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
    • C12N15/1137—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing against enzymes
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/63—Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y201/00—Transferases transferring one-carbon groups (2.1)
    • C12Y201/01—Methyltransferases (2.1.1)
    • C12Y201/01045—Thymidylate synthase (2.1.1.45)
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/10—Type of nucleic acid
    • C12N2310/14—Type of nucleic acid interfering N.A.
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2320/00—Applications; Uses
    • C12N2320/30—Special therapeutic applications
    • C12N2320/31—Combination therapy

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Physics & Mathematics (AREA)
  • Plant Pathology (AREA)
  • Microbiology (AREA)
  • Biophysics (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Saccharide Compounds (AREA)

Claims (12)

1. RNKi-molekula, naznačena time, da je sposobna za obuzdavanje ekspresije sinteze timidilata pomoću RNKi-djelovanja, te koja obuhvaća RNK-domenu dvostruke konfiguracije sastavljenu od sens-konfiguracije koja se sastoji od nukleotidne sekvence predstavljene sa SEQ ID NO:1, hibridizirane na antisens-konfiguraciju koja se sastoji od nukleotidne sekvence predstavljene sa SEQ ID NO:2, pri čemu je sens-konfiguracija povezana na antisens-konfiguraciju preko područja povezivača.
2. RNKi-molekula prema zahtjevu 1, naznačena time, da se sastoji od nukleotidne sekvence predstavljene sa SEQ ID NO:8.
3. Vektor, naznačen time, da obuhvaća matricu DNK od RNKi-molekule prema zahtjevu 1 ili zahtjevu 2, te je sposoban za ekspresiju RNKi-molekule.
4. Farmaceutski sastav, naznačen time, da obuhvaća RNKi-molekulu prema zahtjevu 1 ili zahtjevu 2, i/ili vektor prema zahtjevu 3, u kombinaciji s antitumorskim sredstvom 5-FU.
5. Farmaceutski sastav prema zahtjevu 4, naznačen time, da antitumorsko sredstvo 5-FU je kombinirani lijek koji sadrži tegafur.
6. Farmaceutski sastav prema zahtjevu 5, naznačen time, da antitumorsko sredstvo 5-FU je kombinirani lijek koji sadrži tegafur, gimeracil i oteracil-kalij.
7. Farmaceutski sastav prema zahtjevu 6, naznačen time, da sadrži tegafur, gimeracil i oteracil-kalij u molarnom omjeru od 1:0,4:1.
8. Farmaceutski sastav prema bilo kojem od zahtjeva 4 do 7, naznačen time, da je svaki od RNKi-molekule prema zahtjevu 1 ili zahtjevu 2, i/ili vektora prema zahtjevu 3, i antitumorskog sredstva 5-FU, takav pripravak koji je jednostruko djelotvoran sastojak.
9. Farmaceutski sastav prema bilo kojem od zahtjeva 4 do 7, naznačen time, da RNKi-molekula prema zahtjevu 1 ili zahtjevu 2, i/ili vektor prema zahtjevu 3, i antitumorsko sredstvo 5-FU, imaju oblik formulacije u garnituri.
10. Sredstvo, naznačeno time, da sadrži RNKi-molekulu prema zahtjevu 1 ili zahtjevu 2, i/ili vektor prema zahtjevu 3, te time, da se upotrebljava u postupku medicinskog liječenja.
11. Sredstvo prema zahtjevu 10, naznačeno time, da se upotrebljava u liječenju i/ili prevenciji raka i/ili se upotrebljava za pojačavanje antitumorskih učinaka od antitumorskog sredstva 5-FU.
12. Sredstvo za uporabu prema zahtjevu 11, naznačeno time, da antitumorsko sredstvo 5-FU je kombinirani lijek koji sadrži tegafur.
HRP20161293TT 2009-03-31 2016-10-07 Rnki-molekula za sintezu timidilata i njezina uporaba HRP20161293T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2009086463 2009-03-31
PCT/JP2010/055521 WO2010113844A1 (ja) 2009-03-31 2010-03-29 チミジル酸合成酵素に対するＲＮＡｉ分子およびその用途
EP10758615.8A EP2415870B1 (en) 2009-03-31 2010-03-29 Rnai molecule for thymidylate synthase and use thereof

Publications (1)

Publication Number Publication Date
HRP20161293T1 true HRP20161293T1 (hr) 2016-11-18

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HRP20161293TT HRP20161293T1 (hr) 2009-03-31 2016-10-07 Rnki-molekula za sintezu timidilata i njezina uporaba

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Country Link
US (1) US8524876B2 (hr)
EP (1) EP2415870B1 (hr)
JP (1) JP5687188B2 (hr)
KR (1) KR101579638B1 (hr)
CN (2) CN107090454A (hr)
DK (1) DK2415870T3 (hr)
ES (1) ES2599153T3 (hr)
HR (1) HRP20161293T1 (hr)
HU (1) HUE029171T2 (hr)
PL (1) PL2415870T3 (hr)
PT (1) PT2415870T (hr)
RU (1) RU2535993C2 (hr)
TW (1) TWI526211B (hr)
WO (1) WO2010113844A1 (hr)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120301537A1 (en) 2011-05-23 2012-11-29 Delta-Fly Pharma, Inc. LIPOSOME CONTAINING shRNA MOLECULE TARGETING A THYMIDYLATE SYNTHASE AND USE THEREOF
US8592572B2 (en) 2011-05-23 2013-11-26 Delta-Fly Pharma, Inc. Liposome containing shRNA molecule targeting a thymidylate synthase and use thereof
US20140255471A1 (en) * 2013-03-11 2014-09-11 Wake Forest University Health Sciences Method of treating brain tumors
PT2992874T (pt) 2013-04-30 2018-11-09 Delta Fly Pharma Inc Lipossoma para administração tópica e aplicação do mesmo
ES2809460T3 (es) 2014-10-30 2021-03-04 Delta Fly Pharma Inc Nuevo método de producción de lipoplejo para administración local y fármaco antitumoral que utiliza lipoplejo
JP2023167428A (ja) 2022-05-12 2023-11-24 コニカミノルタ株式会社 光学フィルムの製造方法、光学フィルム、偏光板及び液晶表示装置

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JPS4910510B1 (hr) 1968-01-26 1974-03-11
JP2614164B2 (ja) 1991-05-27 1997-05-28 大鵬薬品工業株式会社 抗腫瘍効果増強のための及び腫瘍治療のための組成物
RU2279277C2 (ru) * 2000-03-31 2006-07-10 Энджиоджен Фармасьютикалз Лтд. Лечение разделенными дозами агентов с сосудоразрушающей активностью
EP1511769A2 (en) * 2002-05-15 2005-03-09 Birgit Luber Egf receptor antagonists in the treatment of gastric cancer
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JP4543188B2 (ja) 2004-03-10 2010-09-15 学校法人日本医科大学 ヒトチミジル酸合成酵素に対するＲＮＡｉとして作用するＲＮＡ配列
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Publication number Publication date
DK2415870T3 (en) 2016-10-10
RU2011143753A (ru) 2013-05-10
CN107090454A (zh) 2017-08-25
TW201038278A (en) 2010-11-01
KR20110135980A (ko) 2011-12-20
US20120016012A1 (en) 2012-01-19
PL2415870T3 (pl) 2017-01-31
JPWO2010113844A1 (ja) 2012-10-11
HUE029171T2 (hu) 2017-02-28
WO2010113844A1 (ja) 2010-10-07
JP5687188B2 (ja) 2015-03-18
PT2415870T (pt) 2016-10-25
RU2535993C2 (ru) 2014-12-20
ES2599153T3 (es) 2017-01-31
EP2415870A9 (en) 2012-07-11
EP2415870A1 (en) 2012-02-08
EP2415870B1 (en) 2016-07-20
CN102369283A (zh) 2012-03-07
US8524876B2 (en) 2013-09-03
EP2415870A4 (en) 2012-11-28
KR101579638B1 (ko) 2015-12-22
TWI526211B (zh) 2016-03-21

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