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WO2016014864A1 - Hydroxy-(r)-2,2'-bisméthylnaltrexones et leurs utilisations - Google Patents

Hydroxy-(r)-2,2'-bisméthylnaltrexones et leurs utilisations Download PDF

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Publication number
WO2016014864A1
WO2016014864A1 PCT/US2015/041848 US2015041848W WO2016014864A1 WO 2016014864 A1 WO2016014864 A1 WO 2016014864A1 US 2015041848 W US2015041848 W US 2015041848W WO 2016014864 A1 WO2016014864 A1 WO 2016014864A1
Authority
WO
WIPO (PCT)
Prior art keywords
compound
formula
mntx
sample
hplc chromatogram
Prior art date
Application number
PCT/US2015/041848
Other languages
English (en)
Other versions
WO2016014864A8 (fr
Inventor
Cameron S. GIBB
Preston J. ABSHER
Darryl A. LEBLANC
Original Assignee
Salix Pharmaceuticals, Inc.
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 Salix Pharmaceuticals, Inc. filed Critical Salix Pharmaceuticals, Inc.
Publication of WO2016014864A1 publication Critical patent/WO2016014864A1/fr
Publication of WO2016014864A8 publication Critical patent/WO2016014864A8/fr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/02—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone

Definitions

  • Suzuki coupling is described in detail herein, other methods for coupling two aromatic compounds may also be used.
  • aromatic compounds may be coupled using oxidative coupling or Stille coupling, or coupling reactions reported by Negishi, Hiyama or Kumada. See, e.g. , Smith, M. and March, J.
  • methylating agent refers to a reactive species having electrophilic properties that is capable of introducing a methyl group at the nitrogen atom of naltrexone, so as to form a covalent bond therewith.
  • Illustrative methylating agents can be represented by the formula CH 3 Z, wherein "Z" is a leaving group which, upon its departure, enables a covalent bond to be formed between the methyl group and the nitrogen atom of naltrexone, forming MNTX.
  • Methylating agents arid leaving groups are well known to those of ordinary skill in the art and are described extensively in both the patent literature and in chemistry text books.

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne des composés de formule (I) dans laquelle R1 et X ont la signification indiquée dans la description, ainsi que des procédés de synthèse et d'utilisation de ceux-ci. La présente invention concerne également de la 10'-hydroxy-(R),(R)-2,2'-bisméhylnaltrexone, ainsi que des procédés de synthèse et d'utilisation de celle-ci.
PCT/US2015/041848 2014-07-23 2015-07-23 Hydroxy-(r)-2,2'-bisméthylnaltrexones et leurs utilisations WO2016014864A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462027852P 2014-07-23 2014-07-23
US62/027,852 2014-07-23

Publications (2)

Publication Number Publication Date
WO2016014864A1 true WO2016014864A1 (fr) 2016-01-28
WO2016014864A8 WO2016014864A8 (fr) 2016-03-24

Family

ID=55163804

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2015/041848 WO2016014864A1 (fr) 2014-07-23 2015-07-23 Hydroxy-(r)-2,2'-bisméthylnaltrexones et leurs utilisations

Country Status (1)

Country Link
WO (1) WO2016014864A1 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10799496B2 (en) 2018-07-13 2020-10-13 Alkermes Pharma Ireland Limited Naphthylenyl compounds for long-acting injectable compositions and related methods
US10807995B2 (en) 2018-07-13 2020-10-20 Alkermes Pharma Ireland Limited Thienothiophene compounds for long-acting injectable compositions and related methods
US10975099B2 (en) 2018-11-05 2021-04-13 Alkermes Pharma Ireland Limited Thiophene compounds for long-acting injectable compositions and related methods

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110190331A1 (en) * 2007-03-29 2011-08-04 Avey Alfred A Peripheral opioid receptor antagonists and uses thereof
US20130296570A1 (en) * 2008-02-06 2013-11-07 Progenics Pharmaceuticals., Inc. Preparation and use of (r),(r)-2,2'-bis-methylnaltrexone

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110190331A1 (en) * 2007-03-29 2011-08-04 Avey Alfred A Peripheral opioid receptor antagonists and uses thereof
US20130296570A1 (en) * 2008-02-06 2013-11-07 Progenics Pharmaceuticals., Inc. Preparation and use of (r),(r)-2,2'-bis-methylnaltrexone

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10799496B2 (en) 2018-07-13 2020-10-13 Alkermes Pharma Ireland Limited Naphthylenyl compounds for long-acting injectable compositions and related methods
US10807995B2 (en) 2018-07-13 2020-10-20 Alkermes Pharma Ireland Limited Thienothiophene compounds for long-acting injectable compositions and related methods
US10975099B2 (en) 2018-11-05 2021-04-13 Alkermes Pharma Ireland Limited Thiophene compounds for long-acting injectable compositions and related methods

Also Published As

Publication number Publication date
WO2016014864A8 (fr) 2016-03-24

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