MA38668A1 - Cristal stabilisé de chlorhydrate de tipiracil, et son procédé de cristallisation - Google Patents

Cristal stabilisé de chlorhydrate de tipiracil, et son procédé de cristallisation

Info

Publication number
MA38668A1
MA38668A1 MA38668A MA38668A MA38668A1 MA 38668 A1 MA38668 A1 MA 38668A1 MA 38668 A MA38668 A MA 38668A MA 38668 A MA38668 A MA 38668A MA 38668 A1 MA38668 A1 MA 38668A1
Authority
MA
Morocco
Prior art keywords
crystal
crystallization process
tipiracil hydrochloride
stabilized crystal
stabilized
Prior art date
Application number
MA38668A
Other languages
English (en)
Other versions
MA38668B2 (fr
Inventor
Hideki Kazuno
Tomonobu Mutsumi
Original Assignee
Taiho Pharmaceutical Co Ltd
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=52104609&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MA38668(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Taiho Pharmaceutical Co Ltd filed Critical Taiho Pharmaceutical Co Ltd
Publication of MA38668A1 publication Critical patent/MA38668A1/fr
Publication of MA38668B2 publication Critical patent/MA38668B2/fr

Links

Classifications

    • 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (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

La présente invention aborde le problème de production d'un cristal stabilisé de monochlorhydrate de 5-chloro-6-[(2-iminopyrrolidin-1-yl)méthyl]- pyrimidine-2,4(1h,3h)-dione. Comme moyen pour résoudre le problème, il est proposé un cristal de monochlorhydrate de 5-chloro-6-[(2-iminopyrrolidin- 1-yl)méthyl]pyrimidine-2,4(1h,3h)-dione. Le cristal présente des pics caractéristiques à des angles de diffraction (2? ± 0,1°) de 11,6°, 17,2°, 17,8°, 23,3°, 27,1° et 29,3° dans la diffraction des rayons x sur poudre.
MA38668A 2013-06-17 2014-06-17 Cristal stabilisé de chlorhydrate de tipiracil, et son procédé de cristallisation MA38668B2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2013126567 2013-06-17
PCT/JP2014/065985 WO2014203877A1 (fr) 2013-06-17 2014-06-17 Cristal stabilisé de chlorhydrate de tipiracil, et son procédé de cristallisation

Publications (2)

Publication Number Publication Date
MA38668A1 true MA38668A1 (fr) 2018-05-31
MA38668B2 MA38668B2 (fr) 2019-09-30

Family

ID=52104609

Family Applications (1)

Application Number Title Priority Date Filing Date
MA38668A MA38668B2 (fr) 2013-06-17 2014-06-17 Cristal stabilisé de chlorhydrate de tipiracil, et son procédé de cristallisation

Country Status (31)

Country Link
US (3) US9527833B2 (fr)
EP (2) EP3012255B1 (fr)
JP (2) JP6364409B2 (fr)
KR (1) KR101806346B1 (fr)
CN (4) CN106967051A (fr)
AU (3) AU2014282281C1 (fr)
BR (1) BR112015031619B1 (fr)
CA (2) CA2985006C (fr)
CY (1) CY1124868T1 (fr)
DK (1) DK3012255T3 (fr)
ES (1) ES2898408T3 (fr)
GE (3) GEP20186875B (fr)
HK (1) HK1203071A1 (fr)
HR (1) HRP20211903T1 (fr)
HU (1) HUE057352T2 (fr)
LT (1) LT3012255T (fr)
MA (1) MA38668B2 (fr)
MX (2) MX383401B (fr)
MY (2) MY173410A (fr)
NZ (1) NZ714090A (fr)
PH (1) PH12015502809A1 (fr)
PL (1) PL3012255T3 (fr)
PT (1) PT3012255T (fr)
RS (1) RS62691B1 (fr)
RU (2) RU2640417C2 (fr)
SG (4) SG10202007643SA (fr)
SI (1) SI3012255T1 (fr)
SM (1) SMT202100689T1 (fr)
TW (1) TWI639592B (fr)
UA (1) UA112626C2 (fr)
WO (1) WO2014203877A1 (fr)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG10202007643SA (en) * 2013-06-17 2020-09-29 Taiho Pharmaceutical Co Ltd Stable crystal form of tipiracil hydrochloride and crystallization method for the same
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 (fr) * 2016-08-23 2018-03-01 Board Of Regents, The University Of Texas System Procédés de traitement d'une maladie osseuse associée à un cancer.
WO2019002407A1 (fr) 2017-06-28 2019-01-03 Amneal Pharmaceuticals Company Gmbh Procédé de préparation de 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
US11149026B2 (en) * 2017-09-07 2021-10-19 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 their processes for the preparation thereof
US20200283414A1 (en) * 2017-09-14 2020-09-10 Aurobindo Pharma Ltd Process for preparing crystalline Tipiracil Hydrochloride
US11344550B2 (en) * 2017-11-02 2022-05-31 Procos S.P.A. Process for the preparation of the crystalline form III of tipiracil hydrochloride
US11730753B2 (en) 2018-03-03 2023-08-22 Natco Pharma Limited Stable pharmaceutical compositions comprising trifluridine and tipiracil hydrochloride

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3088757B2 (ja) * 1995-03-29 2000-09-18 大鵬薬品工業株式会社 ウラシル誘導体並びにそれを含有する抗腫瘍効果増強剤及び抗腫瘍剤
EP0884051B1 (fr) 1996-09-24 2004-12-15 Taiho Pharmaceutical Company Limited Inhibiteurs de metastases cancereuses contenant des derives d'uracile
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
ATE554770T1 (de) 2006-04-13 2012-05-15 Taiho Pharmaceutical Co Ltd Therapeutisches mittel gegen entzündliche darmerkrankungen
CN101484443B (zh) 2006-06-30 2012-11-21 大鹏药品工业株式会社 放射线治疗增强剂
SG10202007643SA (en) * 2013-06-17 2020-09-29 Taiho Pharmaceutical Co Ltd Stable crystal form of tipiracil hydrochloride and crystallization method for the same
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

Also Published As

Publication number Publication date
SG11201509189SA (en) 2016-02-26
LT3012255T (lt) 2021-12-27
SG10201710916YA (en) 2018-02-27
CA2914999A1 (fr) 2014-12-24
HRP20211903T1 (hr) 2022-03-04
RU2640417C2 (ru) 2018-01-09
HUE057352T2 (hu) 2022-05-28
EP3012255A4 (fr) 2017-02-08
MY173410A (en) 2020-01-22
AU2017208215B2 (en) 2018-07-19
AU2018219967C1 (en) 2024-06-13
BR112015031619B1 (pt) 2023-01-17
AU2014282281B2 (en) 2017-09-07
JP2018145204A (ja) 2018-09-20
SG10202007643SA (en) 2020-09-29
US10138223B2 (en) 2018-11-27
CY1124868T1 (el) 2022-11-25
JPWO2014203877A1 (ja) 2017-02-23
CN110746403A (zh) 2020-02-04
US9527833B2 (en) 2016-12-27
US20160145241A1 (en) 2016-05-26
SG10201912293UA (en) 2020-02-27
MA38668B2 (fr) 2019-09-30
TW201534601A (zh) 2015-09-16
US20170057949A1 (en) 2017-03-02
PT3012255T (pt) 2021-11-30
GEP20186841B (en) 2018-04-10
KR20160020560A (ko) 2016-02-23
GEP20186875B (en) 2018-07-10
AU2017208215A1 (en) 2017-08-10
HK1203071A1 (en) 2015-10-16
PL3012255T3 (pl) 2022-01-24
AU2014282281C1 (en) 2024-06-27
KR101806346B1 (ko) 2017-12-07
CN104395307A (zh) 2015-03-04
RU2016100972A (ru) 2017-07-21
NZ714090A (en) 2017-05-26
EP3305779A1 (fr) 2018-04-11
AU2018219967A1 (en) 2018-09-13
SMT202100689T1 (it) 2022-01-10
US10457666B2 (en) 2019-10-29
CA2985006C (fr) 2022-02-22
CN109912573A (zh) 2019-06-21
BR112015031619A8 (pt) 2021-10-26
PH12015502809B1 (en) 2016-03-14
MX383401B (es) 2025-03-13
GEAP201814034A (en) 2018-03-12
WO2014203877A1 (fr) 2014-12-24
RS62691B1 (sr) 2022-01-31
TWI639592B (zh) 2018-11-01
PH12015502809A1 (en) 2016-03-14
EP3012255A1 (fr) 2016-04-27
MX2015016986A (es) 2016-07-21
US20180291005A1 (en) 2018-10-11
MY205261A (en) 2024-10-10
JP6526883B2 (ja) 2019-06-05
JP6364409B2 (ja) 2018-07-25
CA2914999C (fr) 2018-03-20
AU2018219967B2 (en) 2019-01-03
ES2898408T3 (es) 2022-03-07
RU2674441C1 (ru) 2018-12-10
BR112015031619A2 (pt) 2017-07-25
EP3012255B1 (fr) 2021-10-13
AU2014282281A1 (en) 2015-11-19
CA2985006A1 (fr) 2014-12-24
AU2017208215C1 (en) 2024-07-11
UA112626C2 (uk) 2016-09-26
SI3012255T1 (sl) 2022-01-31
CN106967051A (zh) 2017-07-21
DK3012255T3 (da) 2021-12-06

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