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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
Authority
WO
WIPO (PCT)
Prior art keywords
pyrrolo
pyrimidin
dihydro
benzoyl
oxo
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US2000/020777
Other languages
English (en)
Other versions
WO2001014379A2 (fr
Inventor
Erik Christopher Chelius
Linda Marie Osborne
Sharon Van Den Berghe Snorek
Gregory Alan Stephenson
Anne Marie Warner
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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 Eli Lilly and Co filed Critical Eli Lilly and Co
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
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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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
    • 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
    • A61K9/485—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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Zoology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Inorganic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Dispersion Chemistry (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (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 Ceased 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 Ceased 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
AU777047B2 (en) * 2000-02-25 2004-09-30 Eli Lilly And Company A novel crystalline form of N-(4-(2-(2-amino-4,7-dihydro-4- oxo-3H-pyrrolo(2,3-d)pyrimidin-5-YL)ethyl)benzoyl)-L- glutamic acid and process therefor
US20050208139A1 (en) 2004-03-22 2005-09-22 Ascend Therapeutics, Inc. Chemically stable compositions of 4-hydroxy tamoxifen
EP1934226A2 (fr) 2006-08-14 2008-06-25 Sicor, Inc. Diacide de pemetrexed de haute pureté et ses procédés de préparation
KR101045616B1 (ko) * 2006-08-14 2011-07-01 시코르, 인크. 페메트렉세드 이산의 결정형 및 이의 제조 방법
ES2555154T3 (es) 2006-08-14 2015-12-29 Sicor, Inc. Procesos para la preparación de intermedios del pemetrexed
DE602007011384D1 (de) 2006-08-14 2011-02-03 Sicor Inc Verfahren zur herstellung lipophiler pharmazeutisch akzeptabler salze aus pemetrexed-disäure
JP2010523589A (ja) * 2007-04-03 2010-07-15 ドクター レディズ ラボラトリーズ リミテッド ペメトレキセドの固体形
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
MX338047B (es) * 2008-06-06 2016-03-31 Boehringer Ingelheim Int Combinacion farmaceutica útil para el tratamiento fr enfermedades que involucran proliferación celular, migración o apoptosis de células de mieloma, angiogéneisis o fibrosis.
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
WO2011064256A1 (fr) 2009-11-24 2011-06-03 Azad Pharmaceutical Ingredients Ag Nouvelle forme cristalline du pemetrexed disodique
WO2012017443A1 (fr) * 2010-08-02 2012-02-09 Neon Laboratories Ltd. Procédé pour la préparation de pemetrexed dialkylé de haute pureté
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
ES2639639T3 (es) * 2011-03-25 2017-10-27 Scinopharm Taiwan, Ltd. Proceso para la producción de pemetrexed disódico
NZ705994A (en) * 2012-10-17 2015-08-28 Shilpa Medicare Ltd Process for preparing pemetrexed di potassium and its hydrates
WO2014122460A2 (fr) 2013-02-06 2014-08-14 Cipla House Complexes de pémétrexed et compositions pharmaceutiques contenant des complexes de pémétrexed
WO2014185797A1 (fr) 2013-05-17 2014-11-20 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
JP2016527227A (ja) 2013-07-16 2016-09-08 ドクター レディズ ラボラトリーズ リミテッド ペメトレキセドトロメタミン塩の新規な結晶形
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
EP3749317A4 (fr) 2018-02-07 2022-06-22 L.E.A.F Holdings Group LLC Pémétrexed alpha-polyglutamaté et utilisations associées
EP3749311A4 (fr) 2018-02-07 2022-07-06 L.E.A.F Holdings Group LLC Compositions de pémétrexed polyglutamaté gamma et leurs utilisations

Citations (1)

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

Patent Citations (1)

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

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