PE20010489A1 - NEW CRYSTALLINE FORM OF THE DISODE SALT OF N- [4- [2- [2-AMINO-4,7-DIHYDRO-4-OXO-3H-PYRROLO [2,3-D] -PYRIMIDIN-5-IL) ETHYL ] BENZOIL] -L-GLUTAMIC AND PROCEDURES FOR SAME - Google Patents

NEW CRYSTALLINE FORM OF THE DISODE SALT OF N- [4- [2- [2-AMINO-4,7-DIHYDRO-4-OXO-3H-PYRROLO [2,3-D] -PYRIMIDIN-5-IL) ETHYL ] BENZOIL] -L-GLUTAMIC AND PROCEDURES FOR SAME

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Publication number
PE20010489A1
PE20010489A1 PE2000000850A PE0008502000A PE20010489A1 PE 20010489 A1 PE20010489 A1 PE 20010489A1 PE 2000000850 A PE2000000850 A PE 2000000850A PE 0008502000 A PE0008502000 A PE 0008502000A PE 20010489 A1 PE20010489 A1 PE 20010489A1
Authority
PE
Peru
Prior art keywords
ethyl
salt
benzoil
pyrrolo
pyrimidin
Prior art date
Application number
PE2000000850A
Other languages
Spanish (es)
Inventor
Gregory Alan Stephenson
Erik Christopher Chelius
Linda Marie Osborne
Anne Marie Warner
Den Berghe Snorek Sharon Van
Original Assignee
Lilly Co Eli
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 filed Critical Lilly Co Eli
Publication of PE20010489A1 publication Critical patent/PE20010489A1/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)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Inorganic Chemistry (AREA)
  • Dispersion Chemistry (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION DE UN COMPUESTO DE FORMULA I QUE COMPRENDE HACER REACCIONAR PIRROLO [2,3-d]PIRIMIDINA SUSTITUIDA EN LA POSICION 5 DE FORMULA III CON HIDROXIDO DE SODIO; R ES UN GRUPO PROTECTOR DE CARBOXI TAL COMO ESTER METILICO O ETILICO. TAMBIEN SE REFIERE A LA SAL ACIDA DEL ACIDO N-[4-[2-(2-AMINO-4,7-DIHIDRO-4-OXO-3H-PIRROLO[2,3-d]PIRIMIDIN-5-IL)ETIL]BENZOIL]-L-GLUTAMICO QUE SE CARACTERIZA POR SU DIAGRAMA DE DIFRACCION DE RAYOS X. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION QUE COMPRENDE LA CRISTALIZACION DE LA SAL DISODICA DEL COMPUESTO I EN UN DISOLVENTE ADECUADO, AJUSTANDO EL pH DE 7,5 A 8,0 DE LA SOLUCION ACUOSA. EL CRISTAL DEL COMPUESTO ES UN INHIBIDOR DE DIVERSAS ENZIMAS QUE REQUIERENPUEDE SER UTIL PARA EL TRATAMIENTO DE CANCER DE MESOTELIOMAIT REFERS TO A PROCEDURE FOR THE PREPARATION OF A COMPOUND OF FORMULA I WHICH INCLUDES REACTING PIRROLO [2,3-d] PYRIMIDINE SUBSTITUTED IN POSITION 5 OF FORMULA III WITH SODIUM HYDROXIDE; R IS A PROTECTIVE GROUP OF CARBOXY SUCH AS METHYL OR ETHYL ESTER ALSO REFERS TO ACID SALT OF ACID N- [4- [2- (2-AMINO-4,7-DIHYDRO-4-OXO-3H-PYRROLO [2,3-d] PYRIMIDIN-5-IL) ETHYL] BENZOIL] -L-GLUTAMIC WHICH IS CHARACTERIZED BY ITS X-RAY DIFFRACTION DIAGRAM. ALSO REFERS TO A PROCEDURE FOR THE PREPARATION THAT INCLUDES THE CRYSTALLIZATION OF THE DISODIC SALT OF COMPOUND I IN A SUITABLE SOLVENT, ADJUSTING THE pH OF 7.5 A 8.0 OF THE AQUEOUS SOLUTION. THE CRYSTAL OF THE COMPOUND IS AN INHIBITOR OF VARIOUS ENZYMES THAT REQUIRE, MAY BE USEFUL FOR THE TREATMENT OF MESOTHELIOMA CANCER

PE2000000850A 1999-08-23 2000-08-22 NEW CRYSTALLINE FORM OF THE DISODE SALT OF N- [4- [2- [2-AMINO-4,7-DIHYDRO-4-OXO-3H-PYRROLO [2,3-D] -PYRIMIDIN-5-IL) ETHYL ] BENZOIL] -L-GLUTAMIC AND PROCEDURES FOR SAME PE20010489A1 (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
PE20010489A1 true PE20010489A1 (en) 2001-04-27

Family

ID=26847471

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000000850A PE20010489A1 (en) 1999-08-23 2000-08-22 NEW CRYSTALLINE FORM OF THE DISODE SALT OF N- [4- [2- [2-AMINO-4,7-DIHYDRO-4-OXO-3H-PYRROLO [2,3-D] -PYRIMIDIN-5-IL) ETHYL ] BENZOIL] -L-GLUTAMIC AND PROCEDURES FOR 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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EA004684B1 (en) * 2000-02-25 2004-06-24 Эли Лилли Энд Компани NOVEL CRYSTALLINE FORM OF N-[4-[2(2-AMONO-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
ES2354843T3 (en) * 2006-08-14 2011-03-18 Sicor, Inc. CRYSTALLINE FORMS OF PEMETREXED DIÁCIDE AND PROCEDURES FOR THE PREPARATION OF THE SAME.
US8629152B2 (en) 2006-08-14 2014-01-14 Sicor, Inc. Processes for the preparation of lyophilized pharmaceutically acceptable salts of pemetrexed diacid
KR20090052355A (en) 2006-08-14 2009-05-25 시코르, 인크. Highly pure pemetrexed diacid and processes for the preparation thereof
US7994180B2 (en) 2006-08-14 2011-08-09 Sicor Inc. Processes for preparing intermediates of pemetrexed
CA2681829A1 (en) 2007-04-03 2008-10-16 Dr. Reddy's Laboratories Ltd. 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
DK2985025T3 (en) * 2008-06-06 2018-03-19 Boehringer Ingelheim Int PHARMACEUTICAL COMPOSITION
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
WO2011064256A1 (en) 2009-11-24 2011-06-03 Azad Pharmaceutical Ingredients Ag A new crystalline form of pemetrexed disodium
UA105580C2 (en) * 2010-08-02 2014-05-26 Неон Лабораторіс Лтд. 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
EP2675808A4 (en) * 2011-02-15 2014-07-09 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
CA2888611A1 (en) * 2012-10-17 2014-04-24 Shilpa Medicare Limited Process for preparing pemetrexed dipotassium and its hydrates
ZA201400898B (en) 2013-02-06 2015-12-23 Cipla Ltd 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
US9688682B2 (en) 2013-07-16 2017-06-27 Dr. Reddy's Laboratories Limited 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

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CN1213998C (en) * 1997-09-26 2005-08-10 伊莱利利公司 Processes and intermediates useful to make antifolates

Also Published As

Publication number Publication date
WO2001014379A2 (en) 2001-03-01
EP1212325A2 (en) 2002-06-12
WO2001014379A3 (en) 2001-09-07
AU6890800A (en) 2001-03-19
CO5200767A1 (en) 2002-09-27

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