HRP20131090T4 - NOVI STABILNI KRISTALI 1-(2'-CIJANO-2'-DEOKSI-ß-D-ARABINOFURANOZIL) CITOZIN MONOHIDROKLORIDA - Google Patents
NOVI STABILNI KRISTALI 1-(2'-CIJANO-2'-DEOKSI-ß-D-ARABINOFURANOZIL) CITOZIN MONOHIDROKLORIDA Download PDFInfo
- Publication number
- HRP20131090T4 HRP20131090T4 HRP20131090TT HRP20131090T HRP20131090T4 HR P20131090 T4 HRP20131090 T4 HR P20131090T4 HR P20131090T T HRP20131090T T HR P20131090TT HR P20131090 T HRP20131090 T HR P20131090T HR P20131090 T4 HRP20131090 T4 HR P20131090T4
- Authority
- HR
- Croatia
- Prior art keywords
- arabinofuranosyl
- deoxy
- cyano
- type
- crystal
- Prior art date
Links
- OPTASPLRGRRNAP-UHFFFAOYSA-N cytosine Chemical compound NC=1C=CNC(=O)N=1 OPTASPLRGRRNAP-UHFFFAOYSA-N 0.000 title claims 10
- 239000013078 crystal Substances 0.000 title claims 8
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 title claims 5
- 229940104302 cytosine Drugs 0.000 title claims 5
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 238000010438 heat treatment Methods 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 238000002844 melting Methods 0.000 claims 2
- 230000008018 melting Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims 2
- 238000003756 stirring Methods 0.000 claims 2
- 238000001816 cooling Methods 0.000 claims 1
Classifications
-
- 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
-
- 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
- C07H19/16—Purine radicals
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
Claims (4)
1. Antitumorsko sredstvo, naznačeno time, što se sastoji od kristala tipa I 1-(2'-cijano-2'-deoksi-β-D- arabinofuranozil)citozin monohidroklorida koji ima karakteristične vršne vrijednosti na 13,7°, 15,7°, 16,0°, 18,6° 20,3° i 22,7° kao difrakcijske kutove (2θ ± 0,1°) izmjerene rendgenskom difrakcijom praha i imaju točku taljenja od 192°C do 197°C te farmaceutski prihvatljiv nosač.
2. Antitumorsko sredstvo, naznačeno time, što se sastoji od kristala tipa II 1-(2'-cijano-2'-deoksi-β-D- arabinofuranozil)citozin monohidroklorida koji ima karakteristične maksimume na 6,4°, 12,6°, 17,3° i 21,7 ° kao kutove difrakcije (2θ ± 0,1°) izmjerene rendgenskom difrakcijom praha i imaju točku taljenja od 192°C do 196°C te farmaceutski prihvatljiv nosač.
3. Postupak za proizvodnju kristala tipa I kako je definirano u patentnom zahtjevu 1, naznačeno time, što uključuje korake otapanja pod zagrijavanjem 1-(2'-cijano-2'-deoksi- β-D-arabinofuranozil)citozin monohidroklorida u etanolu i zatim dodavanja ove otopine kap po kap u dietil eter koji je ohlađen na 0- 5°C uz miješanje smjese, u svrhu dobivanja kristala tipa I.
4. Postupak za proizvodnju kristala tipa II definiranog u patentnom zahtjevu 2, naznačeno time, što uključuje korake otapanja pod zagrijavanjem 1-(2'-cijano-2'-deoksi- β-D-arabinofuranozil)citozin monohidroklorida ili kristala tipa I u etanolu, zatim hlađenja ove otopine na 40 ± 5°C a zatim dodavanja dietil etera kap po kap u otopinu uz miješanje smjese, u svrhu dobivanja kristala tipa II.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2009118726 | 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 |
| EP10774734.7A EP2431376B2 (en) | 2009-05-15 | 2010-05-14 | Novel stable crystal of 1-(2'-cyano-2'-deoxy-beta -d-arabinofuranosyl)cytosine monohydrochloride |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HRP20131090T1 HRP20131090T1 (hr) | 2013-12-20 |
| HRP20131090T4 true HRP20131090T4 (hr) | 2024-03-15 |
Family
ID=43084859
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20131090TT HRP20131090T4 (hr) | 2009-05-15 | 2013-11-14 | NOVI STABILNI KRISTALI 1-(2'-CIJANO-2'-DEOKSI-ß-D-ARABINOFURANOZIL) CITOZIN MONOHIDROKLORIDA |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US8377905B2 (hr) |
| EP (1) | EP2431376B2 (hr) |
| JP (2) | JP5801715B2 (hr) |
| KR (1) | KR101414888B1 (hr) |
| CN (1) | CN102414216B (hr) |
| DK (1) | DK2431376T4 (hr) |
| ES (1) | ES2426025T5 (hr) |
| FI (1) | FI2431376T4 (hr) |
| HR (1) | HRP20131090T4 (hr) |
| PL (1) | PL2431376T3 (hr) |
| PT (1) | PT2431376E (hr) |
| RU (1) | RU2538593C2 (hr) |
| WO (1) | WO2010131475A1 (hr) |
Families Citing this family (2)
| 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 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
-
2010
- 2010-05-14 RU RU2011146144/04A patent/RU2538593C2/ru active
- 2010-05-14 EP EP10774734.7A patent/EP2431376B2/en active Active
- 2010-05-14 KR KR1020117027019A patent/KR101414888B1/ko active IP Right Grant
- 2010-05-14 PT PT107747347T patent/PT2431376E/pt unknown
- 2010-05-14 ES ES10774734T patent/ES2426025T5/es active Active
- 2010-05-14 PL PL10774734T patent/PL2431376T3/pl unknown
- 2010-05-14 DK DK10774734.7T patent/DK2431376T4/da active
- 2010-05-14 CN CN201080017920.4A patent/CN102414216B/zh active Active
- 2010-05-14 FI FIEP10774734.7T patent/FI2431376T4/fi active
- 2010-05-14 JP JP2011513251A patent/JP5801715B2/ja active Active
- 2010-05-14 US US13/264,111 patent/US8377905B2/en active Active
- 2010-05-14 WO PCT/JP2010/003261 patent/WO2010131475A1/ja active Application Filing
-
2013
- 2013-11-14 HR HRP20131090TT patent/HRP20131090T4/hr unknown
-
2015
- 2015-06-10 JP JP2015117232A patent/JP6307045B2/ja active Active
Also Published As
| Publication number | Publication date |
|---|---|
| CN102414216B (zh) | 2015-01-21 |
| KR101414888B1 (ko) | 2014-07-03 |
| ES2426025T3 (es) | 2013-10-18 |
| PT2431376E (pt) | 2013-09-17 |
| RU2011146144A (ru) | 2013-06-20 |
| 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 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HRP20160208T4 (hr) | Polimorfi dasatiniba i postupak za njihovu pripremu | |
| HRP20211903T1 (hr) | Stabilni kristalni oblik tipiracil hidroklorida i postupak kristalizacije istog | |
| ES2621664T3 (es) | Cristal de ácido 7-{(3S,4S)-3-[(ciclopropilamino)metil]-4-fluoropirrolidin-1-il}-6-fluoro-1-(2-fluoroetil)-8-metoxi-4-oxo-1,4-dihidroquinolin-3-carboxílico | |
| JO3178B1 (ar) | النموذج السادس البلوري الجديد من مركب الاغوميلاتين وطريقة تحضيره وتحضير المركبات الصيدلانية المحتوية عليه | |
| MX347841B (es) | Procedimiento para preparar derivados de antranilamida sustituidos con tetrazoles y polimorfos cristalinos novedosos de estos derivados. | |
| JP2012176975A5 (hr) | ||
| JP2006151999A5 (hr) | ||
| HRP20171041T1 (hr) | Nova sol abeksinostata, s njome povezani kristalni oblik, postupak pripreme i farmaceutske tvari koje ih sadrže | |
| HRP20151344T1 (hr) | Kristalni oblik slobodne baze bifenilnog spoja | |
| PH12015501877B1 (en) | Suspension for oral administration comprising amorphous tolvaptan | |
| MY143557A (en) | Beta-crystalline form of perindopril arginine salt, process for its preparation, and pharmaceutical compositions containing it | |
| HRP20131090T4 (hr) | NOVI STABILNI KRISTALI 1-(2'-CIJANO-2'-DEOKSI-ß-D-ARABINOFURANOZIL) CITOZIN MONOHIDROKLORIDA | |
| JP2011105685A (ja) | フェネチルアミン化合物の結晶 | |
| RU2015113277A (ru) | Кристаллическтие соединения | |
| RU2014104991A (ru) | Полиморфные формы натриевой соли 4-трет-бутил-n-[4-хлор-2-(1-окси-пиридин-4-карбонил)-фенил]-бензолсульфонамида | |
| MD20120130A2 (en) | Delta crystalline form of the L-arginine salt of perindopril, a process for its preparation and pharmaceutical compositions containing it | |
| HRP20110712T1 (hr) | Novi postupak za dobivanje kristalnog oblika agomelatina | |
| CN104628743B (zh) | 头孢硫脒化合物的新晶型及其结晶制备方法 | |
| RU2016132469A (ru) | S-кристаллическая форма хлористоводородного ивабрадина, способ ее получения и фармацевтическая композиция на основе этой формы | |
| CO5780134A1 (es) | Forma polimorfica de descetoprofeno trometamol, su preparacion y composiciones que lo contienen | |
| RU2017102321A (ru) | Новая поликристаллическая форма пролекарства тенофовира и способ ее получения и ее применение | |
| RU2017117890A (ru) | Стабильный кристаллический моногидрат эпирубицина гидрохлорида и способ его получения | |
| MY160337A (en) | Agomelatine hydrobromide hydrate and preparation thereof | |
| JP2010520273A5 (hr) | ||
| RU2014127478A (ru) | Кристаллические формы[(s)-1-карбамоил-2-(фенилпиримидин-2-иламино)этил]амида 2-(2-метиламинопиримидин-4-ил)-1н-индол-5-карбоновой кислоты |