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WO2011039369A3 - Amorphous forms of a 2-amino-4-(4-fluorobenzylamino)phenylcarbamate derivative - Google Patents

Amorphous forms of a 2-amino-4-(4-fluorobenzylamino)phenylcarbamate derivative Download PDF

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Publication number
WO2011039369A3
WO2011039369A3 PCT/EP2010/064694 EP2010064694W WO2011039369A3 WO 2011039369 A3 WO2011039369 A3 WO 2011039369A3 EP 2010064694 W EP2010064694 W EP 2010064694W WO 2011039369 A3 WO2011039369 A3 WO 2011039369A3
Authority
WO
WIPO (PCT)
Prior art keywords
fluorobenzylamino
amino
amorphous forms
phenylcarbamate derivative
same
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/EP2010/064694
Other languages
French (fr)
Other versions
WO2011039369A2 (en
Inventor
Monica Benito Velez
Ernesto Duran Lopez
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.)
Medichem SA
Original Assignee
Medichem SA
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 Medichem SA filed Critical Medichem SA
Publication of WO2011039369A2 publication Critical patent/WO2011039369A2/en
Anticipated expiration legal-status Critical
Publication of WO2011039369A3 publication Critical patent/WO2011039369A3/en
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/26—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
    • C07C271/28—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a non-condensed six-membered aromatic ring
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/27—Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682—Processes
    • A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
    • 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
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

The invention relates to a stable amorphous solid mixture of retigabine and at least one pharmaceutically acceptable carrier, to processes for preparing the same, to solid pharmaceutical formulations comprising the same, and to said mixture or formulation stabilized in a container or packaging.
PCT/EP2010/064694 2009-10-02 2010-10-01 Amorphous forms of a 2-amino-4-(4-fluorobenzylamino)phenylcarbamate derivative Ceased WO2011039369A2 (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US24822409P 2009-10-02 2009-10-02
US61/248,224 2009-10-02
US25793009P 2009-11-04 2009-11-04
US61/257,930 2009-11-04
US30619610P 2010-02-19 2010-02-19
US61/306,196 2010-02-19

Publications (2)

Publication Number Publication Date
WO2011039369A2 WO2011039369A2 (en) 2011-04-07
WO2011039369A3 true WO2011039369A3 (en) 2013-03-28

Family

ID=43032933

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2010/064694 Ceased WO2011039369A2 (en) 2009-10-02 2010-10-01 Amorphous forms of a 2-amino-4-(4-fluorobenzylamino)phenylcarbamate derivative

Country Status (1)

Country Link
WO (1) WO2011039369A2 (en)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102009013611A1 (en) * 2009-03-17 2010-09-23 Ratiopharm Gmbh Solid retigabine in non-crystalline form
CN102241608A (en) * 2011-05-12 2011-11-16 天津市汉康医药生物技术有限公司 Retigabine compound and composition thereof
WO2013008250A2 (en) * 2011-07-01 2013-01-17 Dr.Reddys Laboratories Limited. Crystalline form of retigabine and processes for mixture of retigabine crystalline modifications
CN107049979B (en) * 2011-09-30 2020-08-14 持田制药株式会社 Easily administrable solid preparation
WO2014023270A1 (en) 2012-08-09 2014-02-13 Zentiva, K.S. Salts or co-crystals of ethyl n-[2-amino-4-[(4-fluorophenyl)methylamino]-phenyl]carbamate
CN102964273B (en) * 2012-12-06 2014-04-02 北京英科博雅科技有限公司 Novel retigabine crystal form F and preparation method thereof
US20190038754A1 (en) 2017-08-07 2019-02-07 SE Tylose, USA, Inc. Pharmaceutical composition in solid extruded form
PH12022551176A1 (en) * 2019-12-02 2023-12-04 Xenon Pharmaceuticals Inc Pediatric immediate-release formulation of the potassium channel opener ezogabine

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020001573A1 (en) * 2000-06-14 2002-01-03 Alain Martin Immunostimulator anti-cancer compounds
US20060160892A1 (en) * 2001-04-04 2006-07-20 Wyeth Methods for treating hyperactive gastric motility
WO2010105823A1 (en) * 2009-03-17 2010-09-23 Ratiopharm Gmbh Solid retigabine in non-crystalline form

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4200259A1 (en) 1992-01-08 1993-07-15 Asta Medica Ag NEW 1,2,4-TRIAMINOBENZOL DERIVATIVES AND METHOD FOR THE PRODUCTION THEREOF
DE19701694A1 (en) 1997-01-20 1998-07-23 Asta Medica Ag New modifications of the 2-amino-4- (4-fluorobenzylamino) -l-ethoxycarbonyl-aminobenzen and processes for their preparation

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020001573A1 (en) * 2000-06-14 2002-01-03 Alain Martin Immunostimulator anti-cancer compounds
US20060160892A1 (en) * 2001-04-04 2006-07-20 Wyeth Methods for treating hyperactive gastric motility
WO2010105823A1 (en) * 2009-03-17 2010-09-23 Ratiopharm Gmbh Solid retigabine in non-crystalline form

Also Published As

Publication number Publication date
WO2011039369A2 (en) 2011-04-07

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