WO2001014379A3 - Nouvelle forme cristalline de disodium n-[4-[2-(2-amino-4,7-dihydro-4-oxo-3h-pyrrolo[2,3-d]-pyrimidin-5-yl)ethyl]benzoyl]-l- sel d'acide glutamique et procedes de preparation - Google Patents

Nouvelle forme cristalline de disodium n-[4-[2-(2-amino-4,7-dihydro-4-oxo-3h-pyrrolo[2,3-d]-pyrimidin-5-yl)ethyl]benzoyl]-l- sel d'acide glutamique et procedes de preparation Download PDF

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Publication number
WO2001014379A3
WO2001014379A3 PCT/US2000/020777 US0020777W WO0114379A3 WO 2001014379 A3 WO2001014379 A3 WO 2001014379A3 US 0020777 W US0020777 W US 0020777W WO 0114379 A3 WO0114379 A3 WO 0114379A3
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WO
WIPO (PCT)
Prior art keywords
pyrrolo
pyrimidin
dihydro
benzoyl
oxo
Prior art date
Application number
PCT/US2000/020777
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English (en)
Other versions
WO2001014379A2 (fr
Inventor
Erik Christopher Chelius
Linda Marie Osborne
Sharon Van Den Berghe Snorek
Gregory Alan Stephenson
Anne Marie Warner
Original Assignee
Lilly Co Eli
Erik Christopher Chelius
Linda Marie Osborne
Sharon Van Den Berghe Snorek
Gregory Alan Stephenson
Anne Marie Warner
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
Application filed by Lilly Co Eli, Erik Christopher Chelius, Linda Marie Osborne, Sharon Van Den Berghe Snorek, Gregory Alan Stephenson, Anne Marie Warner filed Critical Lilly Co Eli
Priority to AU68908/00A priority Critical patent/AU6890800A/en
Priority to EP00957261A priority patent/EP1212325A2/fr
Publication of WO2001014379A2 publication Critical patent/WO2001014379A2/fr
Publication of WO2001014379A3 publication Critical patent/WO2001014379A3/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0031—Rectum, anus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/485—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Zoology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dispersion Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention relève du domaine de la chimie pharmaceutique et organique, et concerne un meilleur procédé de préparation de l'antifolique multicible N-[4-[2-(2-amino-4,7-dihydro-4-oxo-3H-pyrrolo[2,3-d]-pyrimidin-5-yl)éthyl]benzoyl]-L-acide glutamique et des cristaux de ce dernier.
PCT/US2000/020777 1999-08-23 2000-08-15 Nouvelle forme cristalline de disodium n-[4-[2-(2-amino-4,7-dihydro-4-oxo-3h-pyrrolo[2,3-d]-pyrimidin-5-yl)ethyl]benzoyl]-l- sel d'acide glutamique et procedes de preparation WO2001014379A2 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU68908/00A AU6890800A (en) 1999-08-23 2000-08-15 A novel crystalline form of disodium n-[4-[2-(2-amino-4,7-dihydro-4-oxo-3h-pyrrolo[2,3-D]- pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic acid salt and processes therefor
EP00957261A EP1212325A2 (fr) 1999-08-23 2000-08-15 Nouvelle forme cristalline de disodium n-[4-[2-(2-amino-4,7-dihydro-4-oxo-3h-pyrrolo 2,3-d]-pyrimidin-5-yl)ethyl]benzoyl]-l- sel d'acide glutamique et procedes de preparation

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US15025499P 1999-08-23 1999-08-23
US60/150,254 1999-08-23
US18496400P 2000-02-25 2000-02-25
US60/184,964 2000-02-25

Publications (2)

Publication Number Publication Date
WO2001014379A2 WO2001014379A2 (fr) 2001-03-01
WO2001014379A3 true WO2001014379A3 (fr) 2001-09-07

Family

ID=26847471

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/020777 WO2001014379A2 (fr) 1999-08-23 2000-08-15 Nouvelle forme cristalline de disodium n-[4-[2-(2-amino-4,7-dihydro-4-oxo-3h-pyrrolo[2,3-d]-pyrimidin-5-yl)ethyl]benzoyl]-l- sel d'acide glutamique et procedes de preparation

Country Status (5)

Country Link
EP (1) EP1212325A2 (fr)
AU (1) AU6890800A (fr)
CO (1) CO5200767A1 (fr)
PE (1) PE20010489A1 (fr)
WO (1) WO2001014379A2 (fr)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA02008242A (es) * 2000-02-25 2002-11-29 Lilly Co Eli Nueva forma cristalina del acido n-[4- [2-(2-amino -4, 7- dihidro -4 -oxo-3h- pirrolo [2, 3-d]pirimidin -5-il) eitl]benzoil] -l-glutamico y procedimiento para su obtencion.
EP1579857A1 (fr) 2004-03-22 2005-09-28 Laboratoires Besins International Compositions stables a base de 4-hydroxy tamoxifene
EP2322526A1 (fr) 2006-08-14 2011-05-18 Sicor, Inc. Forme cristalline de diacide de pemetrexed et son procédé de préparation
EP1934226A2 (fr) 2006-08-14 2008-06-25 Sicor, Inc. Diacide de pemetrexed de haute pureté et ses procédés de préparation
US8629152B2 (en) 2006-08-14 2014-01-14 Sicor, Inc. Processes for the preparation of lyophilized pharmaceutically acceptable salts of pemetrexed diacid
TWI374886B (en) 2006-08-14 2012-10-21 Sicor Inc Processes for preparing intermediates of pemetrexed
WO2008124485A2 (fr) * 2007-04-03 2008-10-16 Dr. Reddy's Laboratories Ltd. Formes solides de pemetrexed
CN101417998B (zh) 2007-10-24 2012-10-24 重庆医药工业研究院有限责任公司 一种培美曲塞盐的纯化方法
EP2072518A1 (fr) * 2007-12-23 2009-06-24 Sun Pharma Advanced Research Company Limited Forme amorphe stable de Pemextred disodium
RS57035B1 (sr) * 2008-06-06 2018-05-31 Boehringer Ingelheim Int Farmaceutska kombinacija
WO2010028105A2 (fr) * 2008-09-08 2010-03-11 Dr. Reddy's Laboratories Ltd. Disodium de pemetrexed amorphe
WO2010030598A2 (fr) * 2008-09-11 2010-03-18 Dr. Reddy's Laboratories Limited Formulations pharmaceutiques comprenant du pemetrexed
CN101684121B (zh) 2008-09-22 2013-04-03 重庆医药工业研究院有限责任公司 培美曲塞二酸的新晶型及其制备方法
TW201118098A (en) * 2009-08-13 2011-06-01 Reddy S Lab Liimited Dr Processes for preparing pemetrexed
CN102050825B (zh) * 2009-11-05 2014-12-17 上海创诺制药有限公司 制备培美曲塞二钠2.5水结晶的方法
EP2504341A1 (fr) 2009-11-24 2012-10-03 Azad Pharmaceutical Ingredients AG Nouvelle forme cristalline du pemetrexed disodique
RU2552519C2 (ru) * 2010-08-02 2015-06-10 Неон Лэборэторис Лтд. Способ получения высокочистого диалкилпеметрекседа
KR101308767B1 (ko) 2011-01-20 2013-12-31 에스티팜 주식회사 고 순도 페메트렉세드 디에틸 에스테르의 제조방법 및 이 방법을 포함하는 페메트렉세드 이나트륨염의 제조방법
EP2675808A4 (fr) * 2011-02-15 2014-07-09 Hetero Research Foundation Procédé d'obtention de pemetrexed disodique
US9051322B2 (en) 2011-03-23 2015-06-09 Scinopharm Taiwan, Ltd. Process for the production of a pemetrexed salt
CA2827455C (fr) * 2011-03-25 2017-10-24 Scinopharm Taiwan Ltd Procede pour la production d'un sel de pemetrexed
WO2014060953A1 (fr) * 2012-10-17 2014-04-24 Shilpa Medicare Limited Procédé pour préparer du dipotassium de pémetrexed et ses hydrates
ZA201400898B (en) 2013-02-06 2015-12-23 Cipla Ltd Pemetrexed complexes and pharmaceutical compositions containing pemetrexed complexes
EP2997031A1 (fr) 2013-05-17 2016-03-23 Instytut Farmaceutyczny Procédé pour la préparation de pemetrexed disodique amorphe de haute pureté et formes cristallines de l'acide n-[4-[2-(2-amino-4,7-dihydro-4-oxo-3h-pyrrolo[2,3-d]pyrimidin-5-yl)éthyl]benzoyl]-l-glutamique
EP3021849B1 (fr) 2013-07-16 2019-10-09 Dr. Reddy's Laboratories Ltd. Nouvelles formes cristallines de sels de trométhamine de pemetrexed
NZ630292A (en) * 2013-11-25 2015-02-27 Shilpa Medicare Ltd Process for crystalline pemetrexed dipotassium salt
CN103784454B (zh) * 2014-01-22 2015-11-18 海南锦瑞制药有限公司 一种含有培美曲塞二钠化合物的药物组合物

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WO1999016742A1 (fr) * 1997-09-26 1999-04-08 Eli Lilly And Company Procedes et intermediaires pour la production d'antifoliques

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WO1999016742A1 (fr) * 1997-09-26 1999-04-08 Eli Lilly And Company Procedes et intermediaires pour la production d'antifoliques

Non-Patent Citations (2)

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Also Published As

Publication number Publication date
AU6890800A (en) 2001-03-19
WO2001014379A2 (fr) 2001-03-01
PE20010489A1 (es) 2001-04-27
EP1212325A2 (fr) 2002-06-12
CO5200767A1 (es) 2002-09-27

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