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CO5200767A1 - NEW CRYSTAL FORM OF THE DISODIC ACID SALT N- [4- [2- (2- AMINO 4,7-DIHIDRO-4-OXO-3H-PIRROLO [2,3-D] - PIRIMIDIN-5-IL] ETIL] BENZOIL] -L- GLUTAMIC AND PROCEDURE FOR THE SAME - Google Patents

NEW CRYSTAL FORM OF THE DISODIC ACID SALT N- [4- [2- (2- AMINO 4,7-DIHIDRO-4-OXO-3H-PIRROLO [2,3-D] - PIRIMIDIN-5-IL] ETIL] BENZOIL] -L- GLUTAMIC AND PROCEDURE FOR THE SAME

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Publication number
CO5200767A1
CO5200767A1 CO00062633A CO00062633A CO5200767A1 CO 5200767 A1 CO5200767 A1 CO 5200767A1 CO 00062633 A CO00062633 A CO 00062633A CO 00062633 A CO00062633 A CO 00062633A CO 5200767 A1 CO5200767 A1 CO 5200767A1
Authority
CO
Colombia
Prior art keywords
glutamic
oxo
amino
pirimidin
pirrolo
Prior art date
Application number
CO00062633A
Other languages
Spanish (es)
Inventor
Linda Marie Osborne
Van Den Berghe Snorek Sharon
Gregory Alan Stephenson
Anne Marie Warner
Erik Christopher Chelius
Original Assignee
Elililly And Company
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 Elililly And Company filed Critical Elililly And Company
Publication of CO5200767A1 publication Critical patent/CO5200767A1/en

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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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Un procedimiento para la preparación de un compuesto de fórmula I<EMI FILE="00062633_1" ID="1" IMF=JPEG >que comprende hacer reaccionar pirrolo[2,3-d]-pirimidina sustituida en la posición 5 de fórmula III, en la que R es un grupo protector de carboxi:<EMI FILE="00062633_2" ID="2" IMF=JPEG >con hidróxido sódico.Una nueva forma cristalina hidratada de la sal disódica delácido N-[4-[2-(2-amino-4,7-dihidro-4-oxo-3H-pirrolo[2,3-d]-pirimidin-5-il)etil]benzoil]-L-glutámico ("MTA disódico hidratado Forma I") que presenta un diagrama de difracción de rayos X que comprende los siguientes picos correspondientes al espaciamiento d: 18,66 + 0,04 obtenido a 22 + 2 ºC y a una humedad relativa, en %, ambiental a partir de una fuente de radiación de cobre.A process for the preparation of a compound of formula I <EMI FILE = "00062633_1" ID = "1" MFI = JPEG> comprising reacting pyrrolo [2,3-d] -pyrimidine substituted at position 5 of formula III, in which R is a carboxy protecting group: <EMI FILE = "00062633_2" ID = "2" MFI = JPEG> with sodium hydroxide. A new hydrated crystalline form of the disodium salt of the acid N- [4- [2- ( 2-amino-4,7-dihydro-4-oxo-3H-pyrrolo [2,3-d] -pyrimidin-5-yl) ethyl] benzoyl] -L-glutamic ("Hydrated disodium MTA Form I") presenting an X-ray diffraction diagram comprising the following peaks corresponding to the spacing d: 18.66 + 0.04 obtained at 22 + 2 ° C and at a relative humidity, in%, environmental from a copper radiation source.

CO00062633A 1999-08-23 2000-08-22 NEW CRYSTAL FORM OF THE DISODIC ACID SALT N- [4- [2- (2- AMINO 4,7-DIHIDRO-4-OXO-3H-PIRROLO [2,3-D] - PIRIMIDIN-5-IL] ETIL] BENZOIL] -L- GLUTAMIC AND PROCEDURE FOR THE SAME CO5200767A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15025499P 1999-08-23 1999-08-23
US18496400P 2000-02-25 2000-02-25

Publications (1)

Publication Number Publication Date
CO5200767A1 true CO5200767A1 (en) 2002-09-27

Family

ID=26847471

Family Applications (1)

Application Number Title Priority Date Filing Date
CO00062633A CO5200767A1 (en) 1999-08-23 2000-08-22 NEW CRYSTAL FORM OF THE DISODIC ACID SALT N- [4- [2- (2- AMINO 4,7-DIHIDRO-4-OXO-3H-PIRROLO [2,3-D] - PIRIMIDIN-5-IL] ETIL] BENZOIL] -L- GLUTAMIC AND PROCEDURE FOR THE SAME

Country Status (5)

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

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MXPA02008242A (en) * 2000-02-25 2002-11-29 Lilly Co Eli 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.
EP1579857A1 (en) 2004-03-22 2005-09-28 Laboratoires Besins International Chemically stable compositions of 4-hydroxy tamoxifen
WO2008021411A2 (en) 2006-08-14 2008-02-21 Sicor Inc. Processes for the preparation of lyophilized pharmaceutically acceptable salts of pemetrexed diacid
US7994180B2 (en) 2006-08-14 2011-08-09 Sicor Inc. Processes for preparing intermediates of pemetrexed
KR20090052355A (en) 2006-08-14 2009-05-25 시코르, 인크. Highly pure pemetrexed diacids and methods for their preparation
US8088919B2 (en) * 2006-08-14 2012-01-03 Sicor Inc. Crystalline forms of pemetrexed diacid and processes for the preparation thereof
MX2009010568A (en) * 2007-04-03 2009-10-22 Reddys Lab Ltd Dr Solid forms of pemetrexed.
CN101417998B (en) 2007-10-24 2012-10-24 重庆医药工业研究院有限责任公司 Purification method of pemetrexed salt
US20090181990A1 (en) * 2007-12-23 2009-07-16 Patel Nileshkumar S Stable amorphous form of pemetrexed disodium
SI2985025T1 (en) * 2008-06-06 2018-04-30 Boehringer Ingelheim International Gmbh Pharmaceutical combination
EP2334685A4 (en) * 2008-09-08 2011-10-26 Reddys Lab Ltd Dr Amorphous pemetrexed disodium
WO2010030598A2 (en) * 2008-09-11 2010-03-18 Dr. Reddy's Laboratories Limited Pharmaceutical formulations comprising pemetrexed
CN101684121B (en) 2008-09-22 2013-04-03 重庆医药工业研究院有限责任公司 New crystal form of pemetrexed diacid and method for preparing same
TW201118098A (en) * 2009-08-13 2011-06-01 Reddy S Lab Liimited Dr Processes for preparing pemetrexed
CN102050825B (en) * 2009-11-05 2014-12-17 上海创诺制药有限公司 Method for preparing pemetrexed disodium 2.5 water crystal
US9174991B2 (en) 2009-11-24 2015-11-03 Azad Pharmaceutical Ingredients Ag Crystalline form of pemetrexed disodium
WO2012017443A1 (en) * 2010-08-02 2012-02-09 Neon Laboratories Ltd. Process for preparation of highly pure dialkyl pemetrexed
KR101308767B1 (en) 2011-01-20 2013-12-31 에스티팜 주식회사 Preparation method of Pemetrexed diethyl ester with high purity and the preparation method of pemetrexed disodium salt comprising the thereof
WO2012111027A2 (en) * 2011-02-15 2012-08-23 Hetero Research Foundation Process for pemetrexed disodium
US9051322B2 (en) 2011-03-23 2015-06-09 Scinopharm Taiwan, Ltd. Process for the production of a pemetrexed salt
AU2011363636B2 (en) 2011-03-25 2016-03-17 Scinopharm Taiwan Ltd Process for the production of a pemetrexed salt
EP2909208A4 (en) * 2012-10-17 2016-07-13 Shilpa Medicare Ltd PROCESS FOR PREPARING DIPOTASSIUM OF PEMETREXED AND ITS HYDRATES
US20150359898A1 (en) 2013-02-06 2015-12-17 Cipla Limited Pemetrexed Complexes and Pharmaceutical Compositions Containing Pemetrexed Complexes
WO2014185797A1 (en) 2013-05-17 2014-11-20 Instytut Farmaceutyczny Process for the preparation of high purity amorphous pemetrexed disodium and crystalline forms of n-[4-[2-(2-amino-4,7-dihydro-4-oxo-3h-pyrrolo[2,3- d] pyrimidin-5-yl)ethyl] benzoyl]-l-glutamic acid
WO2015008221A1 (en) 2013-07-16 2015-01-22 Dr. Reddy’S Laboratories Limited Novel crystalline forms of pemetrexed tromethamine salts
NZ630292A (en) * 2013-11-25 2015-02-27 Shilpa Medicare Ltd Process for crystalline pemetrexed dipotassium salt
CN103784454B (en) * 2014-01-22 2015-11-18 海南锦瑞制药有限公司 A kind of pharmaceutical composition containing pemetrexed disodium compound
CN111954531A (en) 2018-02-07 2020-11-17 L.E.A.F.控股集团公司 Alpha polyglutamate pemetrexed and uses thereof
JP7490239B2 (en) 2018-02-07 2024-05-27 エル．イー．エー．エフ． ホールディングス グループ エルエルシー Gamma polyglutamylated pemetrexed and uses thereof

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Also Published As

Publication number Publication date
EP1212325A2 (en) 2002-06-12
AU6890800A (en) 2001-03-19
PE20010489A1 (en) 2001-04-27
WO2001014379A2 (en) 2001-03-01
WO2001014379A3 (en) 2001-09-07

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