MX2015016986A - Forma de cristal estable de clorhidrato de tipiracil, y metodo de cristalizacion del mismo. - Google Patents
Forma de cristal estable de clorhidrato de tipiracil, y metodo de cristalizacion del mismo.Info
- Publication number
- MX2015016986A MX2015016986A MX2015016986A MX2015016986A MX2015016986A MX 2015016986 A MX2015016986 A MX 2015016986A MX 2015016986 A MX2015016986 A MX 2015016986A MX 2015016986 A MX2015016986 A MX 2015016986A MX 2015016986 A MX2015016986 A MX 2015016986A
- Authority
- MX
- Mexico
- Prior art keywords
- same
- crystal
- crystallization method
- tipiracil hydrochloride
- stabilized crystal
- Prior art date
Links
- 239000013078 crystal Substances 0.000 title abstract 4
- KGHYQYACJRXCAT-UHFFFAOYSA-N tipiracil hydrochloride Chemical compound Cl.N1C(=O)NC(=O)C(Cl)=C1CN1C(=N)CCC1 KGHYQYACJRXCAT-UHFFFAOYSA-N 0.000 title abstract 3
- 238000002425 crystallisation Methods 0.000 title 1
- 229960001740 tipiracil hydrochloride Drugs 0.000 title 1
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/7072—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 having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Saccharide Compounds (AREA)
Abstract
Un objetivo de la presente invención consiste en obtener una forma de cristal estable de clorhidrato de 5-cloro-6-(2-iminopirro lidin-1-il)metil-2,4(1H,3H)-pirimidinadiona. La presente invención provee un cristal estable de clorhidrato de 5-cloro-6-(2-iminopirrolidin-1-il)metil-2,4(1H,3H)-pirimidinadion a que presenta picos a dos o más ángulos seleccionados del grupo que consiste en 11.6°, 17.2°, 17.8°, 23.3°, 27.1°, y 29.3° como un ángulo de difracción (2? ± 0.1°) en difracción de rayos X de polvo.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2013126567 | 2013-06-17 | ||
PCT/JP2014/065985 WO2014203877A1 (ja) | 2013-06-17 | 2014-06-17 | チピラシル塩酸塩の安定形結晶及びその結晶化方法 |
Publications (1)
Publication Number | Publication Date |
---|---|
MX2015016986A true MX2015016986A (es) | 2016-07-21 |
Family
ID=52104609
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2015016986A MX2015016986A (es) | 2013-06-17 | 2014-06-17 | Forma de cristal estable de clorhidrato de tipiracil, y metodo de cristalizacion del mismo. |
Country Status (30)
Country | Link |
---|---|
US (3) | US9527833B2 (es) |
EP (2) | EP3305779A1 (es) |
JP (2) | JP6364409B2 (es) |
KR (1) | KR101806346B1 (es) |
CN (4) | CN106967051A (es) |
AU (2) | AU2014282281C1 (es) |
BR (1) | BR112015031619B1 (es) |
CA (2) | CA2985006C (es) |
CY (1) | CY1124868T1 (es) |
DK (1) | DK3012255T3 (es) |
ES (1) | ES2898408T3 (es) |
GE (2) | GEP20186875B (es) |
HK (1) | HK1203071A1 (es) |
HR (1) | HRP20211903T1 (es) |
HU (1) | HUE057352T2 (es) |
LT (1) | LT3012255T (es) |
MA (1) | MA38668B2 (es) |
MX (1) | MX2015016986A (es) |
MY (1) | MY173410A (es) |
NZ (1) | NZ714090A (es) |
PH (1) | PH12015502809B1 (es) |
PL (1) | PL3012255T3 (es) |
PT (1) | PT3012255T (es) |
RS (1) | RS62691B1 (es) |
RU (2) | RU2640417C2 (es) |
SG (4) | SG10201912293UA (es) |
SI (1) | SI3012255T1 (es) |
TW (1) | TWI639592B (es) |
UA (1) | UA112626C2 (es) |
WO (1) | WO2014203877A1 (es) |
Families Citing this family (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PL3012255T3 (pl) * | 2013-06-17 | 2022-01-24 | Taiho Pharmaceutical Co., Ltd. | Stabilna krystaliczna postać chlorowodorku typiracylu i sposób jej krystalizacji |
CN104744443A (zh) * | 2013-12-26 | 2015-07-01 | 江苏豪森药业股份有限公司 | 嘧啶二酮类化合物盐酸盐新晶型及其制备方法 |
CN103788075B (zh) * | 2014-02-19 | 2018-03-27 | 齐鲁制药有限公司 | 一种胸苷磷酸化酶抑制剂的结晶形式及其制备方法 |
CN104945385A (zh) * | 2014-03-31 | 2015-09-30 | 江苏豪森药业股份有限公司 | Tipracil盐酸盐的新晶型及其制备方法 |
CN106018573B (zh) * | 2016-03-16 | 2018-09-18 | 江苏悦兴药业有限公司 | 一种tas-102中盐酸替比拉西的纯度检测方法 |
CN105859691A (zh) * | 2016-04-07 | 2016-08-17 | 扬子江药业集团南京海陵药业有限公司 | 一种胸苷磷酸化酶抑制剂的新型结晶形式及其制备方法 |
WO2018039359A1 (en) * | 2016-08-23 | 2018-03-01 | Board Of Regents, The University Of Texas System | Methods for the treatment of cancer-associated bone disease |
WO2019002407A1 (en) * | 2017-06-28 | 2019-01-03 | Amneal Pharmaceuticals Company Gmbh | PROCESS FOR THE PREPARATION OF TIPIRACIL CHLORHYDRATE |
CN107216314A (zh) * | 2017-08-02 | 2017-09-29 | 国药心制药有限公司 | 一种盐酸替匹嘧啶的晶型及其制备方法 |
WO2019049174A1 (en) * | 2017-09-07 | 2019-03-14 | Msn Laboratories Private Limited, R&D Center | SOLID STATE FORMS OF 5-CHLORO-6 - [(2-IMINOPYRROLIDIN-1-YL) METHYL] PYRIMIDINE-2,4- (1H, 3H) -DIONE HYDROCHLORIDE AND METHODS OF PREPARATION THEREOF |
US20200283414A1 (en) * | 2017-09-14 | 2020-09-10 | Aurobindo Pharma Ltd | Process for preparing crystalline Tipiracil Hydrochloride |
JP7330180B2 (ja) * | 2017-11-02 | 2023-08-21 | プロコス ソシエタ ペル アチオニ | チピラシル塩酸塩結晶iii型の製造方法 |
US11730753B2 (en) | 2018-03-03 | 2023-08-22 | Natco Pharma Limited | Stable pharmaceutical compositions comprising trifluridine and tipiracil hydrochloride |
Family Cites Families (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2191340C (en) | 1995-03-29 | 2001-04-17 | Shingo Yano | Uracil derivatives, and antitumor effect potentiator and antitumor agent containing the same |
DE69731940T2 (de) | 1996-09-24 | 2005-05-25 | Taiho Pharmaceutical Co. Ltd. | Uracilderivate enthaltende krebsmetastasen inhibitoren |
JP4049477B2 (ja) * | 1999-03-23 | 2008-02-20 | 大鵬薬品工業株式会社 | 副作用軽減剤 |
JP4110347B2 (ja) | 1999-11-05 | 2008-07-02 | 大鵬薬品工業株式会社 | 抗hiv剤 |
US7799783B2 (en) * | 2005-01-26 | 2010-09-21 | Taiho Pharmaceutical Co., Ltd. | Method of administrating an anticancer drug containing α, α, α-trifluorothymidine and thymidine phosphorylase inhibitor |
CN101420957B (zh) | 2006-04-13 | 2011-04-13 | 大鹏药品工业株式会社 | 炎症性肠病治疗药 |
EP2036903B1 (en) * | 2006-06-30 | 2012-05-23 | Taiho Pharmaceutical Co., Ltd. | Potentiator of radiation therapy |
PL3012255T3 (pl) | 2013-06-17 | 2022-01-24 | Taiho Pharmaceutical Co., Ltd. | Stabilna krystaliczna postać chlorowodorku typiracylu i sposób jej krystalizacji |
CN103613877B (zh) * | 2013-11-20 | 2017-09-19 | 上海锦湖日丽塑料有限公司 | 适于吹塑成型的高耐热abs树脂组合物及其制备方法 |
CN104744443A (zh) | 2013-12-26 | 2015-07-01 | 江苏豪森药业股份有限公司 | 嘧啶二酮类化合物盐酸盐新晶型及其制备方法 |
CN103788075B (zh) * | 2014-02-19 | 2018-03-27 | 齐鲁制药有限公司 | 一种胸苷磷酸化酶抑制剂的结晶形式及其制备方法 |
CN104945384B (zh) | 2014-03-25 | 2018-10-16 | 江苏豪森药业集团有限公司 | 5-氯-6-[(2-亚氨基-1-吡咯烷)甲基]-2,4(1h,3h)-嘧啶二酮或其盐的制备方法 |
CN104945385A (zh) | 2014-03-31 | 2015-09-30 | 江苏豪森药业股份有限公司 | Tipracil盐酸盐的新晶型及其制备方法 |
CN103980253B (zh) | 2014-05-06 | 2015-07-08 | 济南百诺医药科技开发有限公司 | 一种5-氯-6-(2-亚氨基吡咯烷基-1-基)甲基-2,4-(1h, 3h)嘧啶二酮盐酸盐的合成方法 |
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2014
- 2014-06-17 PL PL14814354T patent/PL3012255T3/pl unknown
- 2014-06-17 US US14/896,748 patent/US9527833B2/en active Active
- 2014-06-17 SG SG10201912293UA patent/SG10201912293UA/en unknown
- 2014-06-17 RU RU2016100972A patent/RU2640417C2/ru active
- 2014-06-17 SG SG11201509189SA patent/SG11201509189SA/en unknown
- 2014-06-17 LT LTEPPCT/JP2014/065985T patent/LT3012255T/lt unknown
- 2014-06-17 CN CN201610818347.6A patent/CN106967051A/zh active Pending
- 2014-06-17 HR HRP20211903TT patent/HRP20211903T1/hr unknown
- 2014-06-17 MY MYPI2015002887A patent/MY173410A/en unknown
- 2014-06-17 BR BR112015031619-0A patent/BR112015031619B1/pt active IP Right Grant
- 2014-06-17 CN CN201480000562.4A patent/CN104395307A/zh active Pending
- 2014-06-17 PT PT148143548T patent/PT3012255T/pt unknown
- 2014-06-17 SG SG10202007643SA patent/SG10202007643SA/en unknown
- 2014-06-17 KR KR1020167001279A patent/KR101806346B1/ko active IP Right Grant
- 2014-06-17 JP JP2015522923A patent/JP6364409B2/ja active Active
- 2014-06-17 UA UAA201600333A patent/UA112626C2/uk unknown
- 2014-06-17 CA CA2985006A patent/CA2985006C/en active Active
- 2014-06-17 AU AU2014282281A patent/AU2014282281C1/en active Active
- 2014-06-17 SG SG10201710916YA patent/SG10201710916YA/en unknown
- 2014-06-17 MA MA38668A patent/MA38668B2/fr unknown
- 2014-06-17 GE GEAP201414034A patent/GEP20186875B/en unknown
- 2014-06-17 CN CN201910111208.3A patent/CN109912573A/zh active Pending
- 2014-06-17 DK DK14814354.8T patent/DK3012255T3/da active
- 2014-06-17 CA CA2914999A patent/CA2914999C/en active Active
- 2014-06-17 NZ NZ714090A patent/NZ714090A/en unknown
- 2014-06-17 CN CN201910933531.9A patent/CN110746403A/zh active Pending
- 2014-06-17 ES ES14814354T patent/ES2898408T3/es active Active
- 2014-06-17 GE GEAP201414225A patent/GEP20186841B/en unknown
- 2014-06-17 RU RU2017124790A patent/RU2674441C1/ru active
- 2014-06-17 HU HUE14814354A patent/HUE057352T2/hu unknown
- 2014-06-17 EP EP17204730.0A patent/EP3305779A1/en active Pending
- 2014-06-17 TW TW103120948A patent/TWI639592B/zh active
- 2014-06-17 EP EP14814354.8A patent/EP3012255B1/en active Active
- 2014-06-17 MX MX2015016986A patent/MX2015016986A/es active IP Right Grant
- 2014-06-17 WO PCT/JP2014/065985 patent/WO2014203877A1/ja active Application Filing
- 2014-06-17 SI SI201431915T patent/SI3012255T1/sl unknown
- 2014-06-17 RS RS20211505A patent/RS62691B1/sr unknown
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2015
- 2015-04-10 HK HK15103542.0A patent/HK1203071A1/xx unknown
- 2015-12-17 PH PH12015502809A patent/PH12015502809B1/en unknown
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2016
- 2016-11-16 US US15/352,858 patent/US10138223B2/en active Active
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2018
- 2018-05-02 US US15/969,434 patent/US10457666B2/en active Active
- 2018-07-02 JP JP2018126102A patent/JP6526883B2/ja active Active
- 2018-08-20 AU AU2018219967A patent/AU2018219967C1/en active Active
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2021
- 2021-12-07 CY CY20211101073T patent/CY1124868T1/el unknown
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