WO2012123963A3 - A process for preparation of iloperidone and amorphous co- precipitate of iloperidone with pharmaceutically acceptable excipient - Google Patents

A process for preparation of iloperidone and amorphous co- precipitate of iloperidone with pharmaceutically acceptable excipient Download PDF

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Publication number
WO2012123963A3
WO2012123963A3 PCT/IN2012/000126 IN2012000126W WO2012123963A3 WO 2012123963 A3 WO2012123963 A3 WO 2012123963A3 IN 2012000126 W IN2012000126 W IN 2012000126W WO 2012123963 A3 WO2012123963 A3 WO 2012123963A3
Authority
WO
WIPO (PCT)
Prior art keywords
iloperidone
precipitate
preparation
pharmaceutically acceptable
amorphous
Prior art date
Application number
PCT/IN2012/000126
Other languages
French (fr)
Other versions
WO2012123963A2 (en
Inventor
Vijayavitthal Thippannachar Mathad
Pavankumar Vrajlal Solanki
Bhushan Sudhakar Pandit
Sekhar Babu UPPELLI
Original Assignee
Megafine Pharma (P) 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 Megafine Pharma (P) Ltd. filed Critical Megafine Pharma (P) Ltd.
Publication of WO2012123963A2 publication Critical patent/WO2012123963A2/en
Publication of WO2012123963A3 publication Critical patent/WO2012123963A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

A process for preparation of iloperidone wherein l-(4-(3-chloro- propoxy)-3-methoxyphenyl)ethanone is reacted with 6-fluo- ro-3-piperidin-4-yl-l,2 benzisoxazole hydrochloride in a biphasic solvent system in presence of an inorganic base and a phase transfer catalyst. Further, process for preparation of an amorphous co-precipitate of iloperidone or its acid addition salt along with pharmaceutically acceptable excipient is proposed. Further, the present invention also relates to a co-precipitate of amorphous form of iloperidone along with pharmaceutically acceptable excipients.
PCT/IN2012/000126 2011-02-24 2012-02-23 A process for preparation of iloperidone and amorphous co- precipitate of iloperidone with pharmaceutically acceptable excipient WO2012123963A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN511MU2011 2011-02-24
IN511/MUM/2011 2011-02-24

Publications (2)

Publication Number Publication Date
WO2012123963A2 WO2012123963A2 (en) 2012-09-20
WO2012123963A3 true WO2012123963A3 (en) 2013-01-10

Family

ID=46640712

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2012/000126 WO2012123963A2 (en) 2011-02-24 2012-02-23 A process for preparation of iloperidone and amorphous co- precipitate of iloperidone with pharmaceutically acceptable excipient

Country Status (1)

Country Link
WO (1) WO2012123963A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103130785A (en) * 2012-12-20 2013-06-05 安徽悦康凯悦制药有限公司 Preparation method of iloperidone
CN103880828A (en) * 2012-12-24 2014-06-25 凌沛学 Oxide of benzisoxazole compound

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0542136A1 (en) * 1991-11-05 1993-05-19 Hoechst-Roussel Pharmaceuticals Incorporated Heteroarylpiperidines, pyrrolidines and piperazines and their use as antipsychotics and analgetics
WO2003037337A1 (en) * 2001-10-30 2003-05-08 Novartis Ag Depot formulations of iloperidone and a star polymer
WO2008027993A2 (en) * 2006-08-31 2008-03-06 Eurand, Inc. Drug delivery systems comprising solid solutions of weakly basic drugs
CN101768154A (en) * 2009-09-19 2010-07-07 浙江华海药业股份有限公司 New preparation method of iloperidone
EP2479176A1 (en) * 2009-09-19 2012-07-25 Zhejiang Huahai Pharmaceutical Co., Ltd. Method for preparation of iloperidone and crystallization method thereof

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69021645T2 (en) 1989-05-19 1996-02-22 Hoechst-Roussel Pharmaceuticals Inc., Somerville, N.J. N- (aryloxyalkyl) heteroarylpiperidines and heteroarylpiperazines, processes for their preparation and their use as medicaments.
US5776963A (en) 1989-05-19 1998-07-07 Hoechst Marion Roussel, Inc. 3-(heteroaryl)-1- (2,3-dihydro-1h-isoindol-2-yl)alkyl!pyrrolidines and 3-(heteroaryl)-1- (2,3-dihydro-1h-indol-1-yl)alkyl!pyrrolidines and related compounds and their therapeutic untility

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5364866A (en) * 1989-05-19 1994-11-15 Hoechst-Roussel Pharmaceuticals, Inc. Heteroarylpiperidines, pyrrolidines and piperazines and their use as antipsychotics and analetics
EP0542136A1 (en) * 1991-11-05 1993-05-19 Hoechst-Roussel Pharmaceuticals Incorporated Heteroarylpiperidines, pyrrolidines and piperazines and their use as antipsychotics and analgetics
WO2003037337A1 (en) * 2001-10-30 2003-05-08 Novartis Ag Depot formulations of iloperidone and a star polymer
WO2008027993A2 (en) * 2006-08-31 2008-03-06 Eurand, Inc. Drug delivery systems comprising solid solutions of weakly basic drugs
CN101768154A (en) * 2009-09-19 2010-07-07 浙江华海药业股份有限公司 New preparation method of iloperidone
EP2479176A1 (en) * 2009-09-19 2012-07-25 Zhejiang Huahai Pharmaceutical Co., Ltd. Method for preparation of iloperidone and crystallization method thereof

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
DATABASE CAPLUS [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; XP002682935, retrieved from STN Database accession no. 2010:418618 *
DATABASE WPI Week 201061, Derwent World Patents Index; AN 2010-K01796, XP002683008 *

Also Published As

Publication number Publication date
WO2012123963A2 (en) 2012-09-20

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