RU2011146144A - Новые стабильные кристаллы моногидрохлорида 1-(2'-дезокси-бета-d-арабинофуранозил)цитозина - Google Patents

Новые стабильные кристаллы моногидрохлорида 1-(2'-дезокси-бета-d-арабинофуранозил)цитозина Download PDF

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RU2011146144A
RU2011146144A RU2011146144/02A RU2011146144A RU2011146144A RU 2011146144 A RU2011146144 A RU 2011146144A RU 2011146144/02 A RU2011146144/02 A RU 2011146144/02A RU 2011146144 A RU2011146144 A RU 2011146144A RU 2011146144 A RU2011146144 A RU 2011146144A
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arabinofuranosyl
deoxy
crystals
cytozine
beta
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RU2011146144/02A
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RU2538593C2 (ru
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Сотаро ВАТАНАБЕ
Такахиро ХАТАКЕЯМА
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Дельта-Флай Фарма, Инк.
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    • 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
    • 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
    • C07H19/16Purine 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

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  • General Chemical & Material Sciences (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Abstract

1. Кристаллы моногидрохлорида 1-(2′-циано-2′-дезокси-β-D-арабинофуранозил)цитозина, имеющие характеристические пики при 13,7°, 15,7°, 16,0°, 18,6°, 20,3° и 22,7° в виде углов дифракции (2θ±0,1°), измеренных при порошковом рентгеноструктурном анализе, и имеющие температуру плавления 192-197°С.2. Кристаллы моногидрохлорида 1-(2′-циано-2′-дезокси-β-D-арабинофуранозил)цитозина, имеющие характеристические пики при 6,4°; 12,3°; 17,3° и 21,7° в виде углов дифракции (2θ±0,1°), измеренных при порошковом рентгеноструктурном анализе, и имеющие температуру плавления 192-197°С.3. Фармацевтическая композиция, содержащая кристаллы по п.1 или 2.4. Противоопухолевое средство, содержащее кристаллы по п.1 или 2.

Claims (4)

1. Кристаллы моногидрохлорида 1-(2′-циано-2′-дезокси-β-D-арабинофуранозил)цитозина, имеющие характеристические пики при 13,7°, 15,7°, 16,0°, 18,6°, 20,3° и 22,7° в виде углов дифракции (2θ±0,1°), измеренных при порошковом рентгеноструктурном анализе, и имеющие температуру плавления 192-197°С.
2. Кристаллы моногидрохлорида 1-(2′-циано-2′-дезокси-β-D-арабинофуранозил)цитозина, имеющие характеристические пики при 6,4°; 12,3°; 17,3° и 21,7° в виде углов дифракции (2θ±0,1°), измеренных при порошковом рентгеноструктурном анализе, и имеющие температуру плавления 192-197°С.
3. Фармацевтическая композиция, содержащая кристаллы по п.1 или 2.
4. Противоопухолевое средство, содержащее кристаллы по п.1 или 2.
RU2011146144/04A 2009-05-15 2010-05-14 НОВЫЕ СТАБИЛЬНЫЕ КРИСТАЛЛЫ МОНОГИДРОХЛОРИДА 1-(2-β-D-АРАБИНОФУРАНОЗИЛ)ЦИТОЗИНА RU2538593C2 (ru)

Applications Claiming Priority (3)

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JP2009118726 2009-05-15
JP2009-118726 2009-05-15
PCT/JP2010/003261 WO2010131475A1 (ja) 2009-05-15 2010-05-14 1-(2'-シアノ-2'-デオキシ-β-D-アラビノフラノシル)シトシン・一塩酸塩の新規安定形結晶

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RU2011146144A true RU2011146144A (ru) 2013-06-20
RU2538593C2 RU2538593C2 (ru) 2015-01-10

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US (1) US8377905B2 (ru)
EP (1) EP2431376B2 (ru)
JP (2) JP5801715B2 (ru)
KR (1) KR101414888B1 (ru)
CN (1) CN102414216B (ru)
DK (1) DK2431376T4 (ru)
ES (1) ES2426025T5 (ru)
FI (1) FI2431376T4 (ru)
HR (1) HRP20131090T4 (ru)
PL (1) PL2431376T3 (ru)
PT (1) PT2431376E (ru)
RU (1) RU2538593C2 (ru)
WO (1) WO2010131475A1 (ru)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0625283D0 (en) 2006-12-19 2007-01-24 Cyclacel Ltd Combination
WO2013146833A1 (ja) * 2012-03-28 2013-10-03 富士フイルム株式会社 1-(2-デオキシ-2-フルオロ-4-チオ-β-D-アラビノフラノシル)シトシンの塩

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* Cited by examiner, † Cited by third party
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JP2559917B2 (ja) 1990-06-15 1996-12-04 三共株式会社 ピリミジンヌクレオシド誘導体
CA2079413C (en) * 1991-09-30 2003-09-09 Masakatsu Kaneko Pyrimidine nucleoside derivatives having anti-tumor activity, their preparation and use
US5637688A (en) * 1994-12-13 1997-06-10 Eli Lilly And Company Process for preparing 1-(2'-deoxy-2'-difluoro-d-ribofuranosyl)-4-aminopyrimidin-2-one hydrochloride
GB0526419D0 (en) * 2005-12-23 2006-02-08 Cyclacel Ltd Formulation

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CN102414216B (zh) 2015-01-21
KR101414888B1 (ko) 2014-07-03
ES2426025T3 (es) 2013-10-18
HRP20131090T4 (hr) 2024-03-15
PT2431376E (pt) 2013-09-17
JP5801715B2 (ja) 2015-10-28
HRP20131090T1 (hr) 2013-12-20
EP2431376B1 (en) 2013-08-14
US20120029182A1 (en) 2012-02-02
ES2426025T5 (es) 2024-06-13
EP2431376B2 (en) 2024-02-07
CN102414216A (zh) 2012-04-11
US8377905B2 (en) 2013-02-19
JP2015157867A (ja) 2015-09-03
FI2431376T4 (fi) 2024-03-13
EP2431376A4 (en) 2012-08-01
WO2010131475A1 (ja) 2010-11-18
JPWO2010131475A1 (ja) 2012-11-01
JP6307045B2 (ja) 2018-04-04
DK2431376T3 (da) 2013-09-02
RU2538593C2 (ru) 2015-01-10
KR20120022940A (ko) 2012-03-12
PL2431376T3 (pl) 2014-01-31
DK2431376T4 (da) 2024-02-26
EP2431376A1 (en) 2012-03-21

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