WO2009101185A3 - A polymorphic form of a pyrazino [2, 3-h] [3] benzazepine derivative - Google Patents

A polymorphic form of a pyrazino [2, 3-h] [3] benzazepine derivative Download PDF

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Publication number
WO2009101185A3
WO2009101185A3 PCT/EP2009/051727 EP2009051727W WO2009101185A3 WO 2009101185 A3 WO2009101185 A3 WO 2009101185A3 EP 2009051727 W EP2009051727 W EP 2009051727W WO 2009101185 A3 WO2009101185 A3 WO 2009101185A3
Authority
WO
WIPO (PCT)
Prior art keywords
pyrazino
polymorphic form
benzazepine derivative
benzazepine
varenicline base
Prior art date
Application number
PCT/EP2009/051727
Other languages
French (fr)
Other versions
WO2009101185A2 (en
Inventor
Stephen Benedict David Winter
Original Assignee
Medichem, S.A.
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, S.A. filed Critical Medichem, S.A.
Priority to EP09709821A priority Critical patent/EP2260037A2/en
Publication of WO2009101185A2 publication Critical patent/WO2009101185A2/en
Publication of WO2009101185A3 publication Critical patent/WO2009101185A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Addiction (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

The invention relates generally to a crystalline polymorphic form of 7, 8, 9, 10-tetrahydro-6, 10-methano-6H-pyrazino[2, 3-h][3] benzazepine, varenicline base, i.e. a hydrate of varenicline base, designated herein as Form II, and to a method for preparing and obtaining the same.
PCT/EP2009/051727 2008-02-15 2009-02-13 A NEW POLYMORPHIC FORM OF A PYRAZINO[2,3-h][3] BENZAZEPINE DERIVATIVE WO2009101185A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP09709821A EP2260037A2 (en) 2008-02-15 2009-02-13 A polymorphic form of a pyrazino [2,3-h] [3] benzazepine derivative

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US6603208P 2008-02-15 2008-02-15
US61/066,032 2008-02-15

Publications (2)

Publication Number Publication Date
WO2009101185A2 WO2009101185A2 (en) 2009-08-20
WO2009101185A3 true WO2009101185A3 (en) 2009-12-03

Family

ID=40852121

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2009/051727 WO2009101185A2 (en) 2008-02-15 2009-02-13 A NEW POLYMORPHIC FORM OF A PYRAZINO[2,3-h][3] BENZAZEPINE DERIVATIVE

Country Status (2)

Country Link
EP (1) EP2260037A2 (en)
WO (1) WO2009101185A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11602537B2 (en) 2022-03-11 2023-03-14 Par Pharmaceutical, Inc. Varenicline compound and process of manufacture thereof
EP4241775A1 (en) 2022-03-11 2023-09-13 Par Pharmaceutical, Inc. Tablet comprising varenicline and process of preparation thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1157726A1 (en) * 2000-05-26 2001-11-28 Pfizer Products Inc. Reactive crystallization method to improve particle size
US6410550B1 (en) * 1997-12-31 2002-06-25 Pfizer Inc Aryl fused azapolycyclic compounds
US20030060624A1 (en) * 2001-04-20 2003-03-27 Singer Robert A. Process for the preparation of 1,3-substituted indenes and aryl-fused azapolycyclic componunds

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6410550B1 (en) * 1997-12-31 2002-06-25 Pfizer Inc Aryl fused azapolycyclic compounds
EP1157726A1 (en) * 2000-05-26 2001-11-28 Pfizer Products Inc. Reactive crystallization method to improve particle size
US20030060624A1 (en) * 2001-04-20 2003-03-27 Singer Robert A. Process for the preparation of 1,3-substituted indenes and aryl-fused azapolycyclic componunds

Also Published As

Publication number Publication date
EP2260037A2 (en) 2010-12-15
WO2009101185A2 (en) 2009-08-20

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