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WO2016125190A3 - Novel crystalline forms of vortioxetine, premixes, and processes for the preparation thereof - Google Patents

Novel crystalline forms of vortioxetine, premixes, and processes for the preparation thereof Download PDF

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Publication number
WO2016125190A3
WO2016125190A3 PCT/IN2016/050041 IN2016050041W WO2016125190A3 WO 2016125190 A3 WO2016125190 A3 WO 2016125190A3 IN 2016050041 W IN2016050041 W IN 2016050041W WO 2016125190 A3 WO2016125190 A3 WO 2016125190A3
Authority
WO
WIPO (PCT)
Prior art keywords
preparation
vortioxetine
crystalline forms
premixes
processes
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/IN2016/050041
Other languages
French (fr)
Other versions
WO2016125190A2 (en
Inventor
Ramakoteswara Rao Jetti
Asharani GORANTLA
Satish BEERAVALLI
Sureshbabu JAYACHANDRA
Rathinapandian JEBARAJ
Anjaneyaraju Indukuri
Bommareddy AGGIRAMIREDDY
Amit Singh
Soumyajit GHOSH
Attanti Veera Venkata SRINIVASARAO
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.)
Mylan Laboratories Ltd
Original Assignee
Mylan Laboratories Ltd
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 Mylan Laboratories Ltd filed Critical Mylan Laboratories Ltd
Publication of WO2016125190A2 publication Critical patent/WO2016125190A2/en
Publication of WO2016125190A3 publication Critical patent/WO2016125190A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/096—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants

Landscapes

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

Abstract

Crystalline forms of vortioxetine hydrobromide, designated as form-M1, form-M2, form-M3, and form-M4are disclosed herein.The present disclosure also provides apharmaceutical premix of crystalline form-M2 of vortioxetine hydrobromide and pharmaceutically acceptable excipients and a process for the preparation thereof, as well as a pharmaceutical premix of amorphous vortioxetine hydrobromide and pharmaceutical acceptable excipients and a process for the preparation thereof. In some embodiments, the generation of a premix that includes amorphous vortioxetine hydrobromide and β-cyclodextrin was found to be particularly stable and advantageous.
PCT/IN2016/050041 2015-02-04 2016-02-04 Novel crystalline forms of vortioxetine, premixes, and processes for the preparation thereof Ceased WO2016125190A2 (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
IN551CH2015 2015-02-04
IN551/CHE/2015 2015-02-04
IN2301/CHE/2015 2015-05-05
IN2301CH2015 2015-05-05
IN5243CH2015 2015-09-30
IN5243/CHE/2015 2015-09-30

Publications (2)

Publication Number Publication Date
WO2016125190A2 WO2016125190A2 (en) 2016-08-11
WO2016125190A3 true WO2016125190A3 (en) 2016-09-29

Family

ID=55802406

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2016/050041 Ceased WO2016125190A2 (en) 2015-02-04 2016-02-04 Novel crystalline forms of vortioxetine, premixes, and processes for the preparation thereof

Country Status (1)

Country Link
WO (1) WO2016125190A2 (en)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ2015633A3 (en) * 2015-09-16 2017-03-29 Zentiva, K.S. The amorphous form of vortioxetine hydrobromide stabilized with cyclodextrin
WO2017125504A1 (en) * 2016-01-20 2017-07-27 Amneal Pharmaceuticals Company Gmbh Polymorphic forms of vortioxetine hydrobromide tert-butanolate
US20190224192A1 (en) * 2016-08-29 2019-07-25 Cipla Limited Stable Pharmaceutical Composition of Vortioxetine Hydrobromide
US10519121B2 (en) 2016-12-30 2019-12-31 Apicore Us Llc Process and novel polymorphic form of vortioxetine and its pharmaceutically acceptable salts
US10836730B2 (en) * 2017-02-23 2020-11-17 Unichem Laboratories Ltd. Process for preparation and purification of vortioxetine hydrobromide
CN110372635B (en) * 2018-04-12 2021-06-04 浙江京新药业股份有限公司 Preparation method of vortioxetine hydrobromide alpha crystal form
CN111330018B (en) * 2018-12-18 2023-07-21 浙江京新药业股份有限公司 Vortioxetine-cyclodextrin inclusion compound, preparation method and pharmaceutical composition thereof
CN115160258B (en) * 2022-06-24 2023-11-17 辰欣药业股份有限公司 Preparation method of vortioxetine hydrobromide gamma crystal form

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007144005A1 (en) * 2006-06-16 2007-12-21 H. Lundbeck A/S 1- [2- (2, 4-dimethylphenylsulfanyl) -phenyl] piperazine as a compound with combined serotonin reuptake, 5-ht3 and 5-ht1a activity for the treatment of cognitive impairment
WO2014044721A1 (en) * 2012-09-19 2014-03-27 Sandoz Ag Novel crystalline form of vortioxetine hydrobromide
WO2014177491A1 (en) * 2013-04-29 2014-11-06 Lek Pharmaceuticals D.D. New solid form of 1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine hydrobromide
WO2015044963A1 (en) * 2013-09-30 2015-04-02 Cadila Healthcare Limited An amorphous vortioxetine and salts thereof
WO2016062860A1 (en) * 2014-10-24 2016-04-28 H E X A L Aktiengesellschaft Amorphous vortioxetine hydrobromide

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA81749C2 (en) 2001-10-04 2008-02-11 Х. Луннбек А/С Derivated of phenylpiperazine as serotonin reuptake inhibitorS
TW201033181A (en) 2009-02-17 2010-09-16 Lundbeck & Co As H Purification of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine
CA2759456C (en) 2009-04-24 2017-10-31 H. Lundbeck A/S Liquid formulations of salts of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine
EA029060B1 (en) 2014-01-31 2018-02-28 Эгиш Дьёдьсердьяр Зрт. Process for the preparation of vortioxetine salts

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007144005A1 (en) * 2006-06-16 2007-12-21 H. Lundbeck A/S 1- [2- (2, 4-dimethylphenylsulfanyl) -phenyl] piperazine as a compound with combined serotonin reuptake, 5-ht3 and 5-ht1a activity for the treatment of cognitive impairment
WO2014044721A1 (en) * 2012-09-19 2014-03-27 Sandoz Ag Novel crystalline form of vortioxetine hydrobromide
WO2014177491A1 (en) * 2013-04-29 2014-11-06 Lek Pharmaceuticals D.D. New solid form of 1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine hydrobromide
WO2015044963A1 (en) * 2013-09-30 2015-04-02 Cadila Healthcare Limited An amorphous vortioxetine and salts thereof
WO2016062860A1 (en) * 2014-10-24 2016-04-28 H E X A L Aktiengesellschaft Amorphous vortioxetine hydrobromide

Also Published As

Publication number Publication date
WO2016125190A2 (en) 2016-08-11

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