FI112483B - Menetelmä terapeuttisesti käyttökelpoisten 3-[2-[4-(6-fluori-1,2-bentsisoksatsol-3-yyli) -1-piperidinyyli]etyyli]-2-alkyyli-pyrimidin-4-onijohdannaisten valmistamiseksi - Google Patents

Menetelmä terapeuttisesti käyttökelpoisten 3-[2-[4-(6-fluori-1,2-bentsisoksatsol-3-yyli) -1-piperidinyyli]etyyli]-2-alkyyli-pyrimidin-4-onijohdannaisten valmistamiseksi

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Publication number
FI112483B
FI112483B FI962155A FI962155A FI112483B FI 112483 B FI112483 B FI 112483B FI 962155 A FI962155 A FI 962155A FI 962155 A FI962155 A FI 962155A FI 112483 B FI112483 B FI 112483B
Authority
FI
Finland
Prior art keywords
pct
novel compounds
date
benzioxazol
alkylpyrimidin
Prior art date
Application number
FI962155A
Other languages
English (en)
Finnish (fi)
Swedish (sv)
Other versions
FI962155A (fi
FI962155A0 (fi
Inventor
Jan Vandenberk
Ludo Edmond Josephine Kennis
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of FI962155A publication Critical patent/FI962155A/fi
Publication of FI962155A0 publication Critical patent/FI962155A0/fi
Application granted granted Critical
Publication of FI112483B publication Critical patent/FI112483B/fi

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/26Psychostimulants, e.g. nicotine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
FI962155A 1993-11-23 1996-05-22 Menetelmä terapeuttisesti käyttökelpoisten 3-[2-[4-(6-fluori-1,2-bentsisoksatsol-3-yyli) -1-piperidinyyli]etyyli]-2-alkyyli-pyrimidin-4-onijohdannaisten valmistamiseksi FI112483B (fi)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP93203270 1993-11-23
PCT/EP1994/003804 WO1995014691A1 (en) 1993-11-23 1994-11-16 NOVEL 9-HYDROXY-PYRIDO[1,2-a]PYRIMIDIN-4-ONE ETHER DERIVATIVES

Publications (3)

Publication Number Publication Date
FI962155A FI962155A (fi) 1996-05-22
FI962155A0 FI962155A0 (fi) 1996-05-22
FI112483B true FI112483B (fi) 2003-12-15

Family

ID=8214180

Family Applications (1)

Application Number Title Priority Date Filing Date
FI962155A FI112483B (fi) 1993-11-23 1996-05-22 Menetelmä terapeuttisesti käyttökelpoisten 3-[2-[4-(6-fluori-1,2-bentsisoksatsol-3-yyli) -1-piperidinyyli]etyyli]-2-alkyyli-pyrimidin-4-onijohdannaisten valmistamiseksi

Country Status (14)

Country Link
US (1) US5688799A (de)
EP (1) EP0730594B1 (de)
JP (1) JP3553951B2 (de)
AT (1) ATE184281T1 (de)
AU (1) AU687940B2 (de)
CA (1) CA2175372C (de)
DE (1) DE69420579T2 (de)
DK (1) DK0730594T3 (de)
ES (1) ES2137486T3 (de)
FI (1) FI112483B (de)
GR (1) GR3031500T3 (de)
RU (1) RU2126406C1 (de)
SI (1) SI0730594T1 (de)
WO (1) WO1995014691A1 (de)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2141671B1 (es) * 1997-12-26 2001-01-01 Vita Invest Sa Compuesto pirimidinico activo sobre el sistema nervioso central, procedimiento para su preparacion y composiciones farmaceuticas que lo contienen.
WO2004009591A1 (en) * 2002-07-22 2004-01-29 Aurobindo Pharma Ltd. A process for the preparation of antipsychotic risperidone
AU2003256006A1 (en) * 2002-08-30 2004-03-19 Sunil Sadanand Nadkarni Improved process for preparation of risperidone
HUP0401379A3 (en) * 2004-07-08 2006-04-28 Richter Gedeon Vegyeszet Process for the preparation of risperidon
US7723518B2 (en) * 2004-09-09 2010-05-25 Janssen Pharmaceutica N.V. Preparation of 9-hydroxy-3-(2-hydroxyethyl)-2-methyl-4H-pyrido[1,2-A]pyrimidin-4-one
HUP0402163A2 (en) * 2004-10-25 2006-05-29 Richter Gedeon Vegyeszet Process for the preparation of risperidone
EP1940834A2 (de) * 2006-08-14 2008-07-09 Teva Pharmaceutical Industries Ltd. Amorphe und kristalline formen von 9-hydroxy-risperidon (paliperidon)
US7915412B2 (en) * 2006-08-14 2011-03-29 Teva Pharmaceutical Industries, Ltd. Process for the synthesis of 9-hydroxy risperidone (paliperidone)
US7820816B2 (en) * 2006-08-23 2010-10-26 Teva Pharmaceutical Industries Ltd. Process for the synthesis of CMHTP and intermediates thereof
WO2008087557A2 (en) * 2007-01-08 2008-07-24 Actavis Group Ptc Ehf An improved process for preparation of 9-hydroxy-3-(2-chloroethyl)- 2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one hydrochloride
US20080171876A1 (en) * 2007-05-10 2008-07-17 Santiago Ini Pure paliperidone and processes for preparing thereof
WO2009010988A1 (en) * 2007-07-19 2009-01-22 Natco Pharma Limited An improved, industrially viable process for the preparation of high purity paliperidone
WO2009015828A1 (en) * 2007-07-27 2009-02-05 Synthon B.V. Paliperidone derivatives
ATE530170T1 (de) * 2007-08-21 2011-11-15 Teva Pharma Paliperidonformulierung mit verzögerter freisetzung
US20090061005A1 (en) * 2007-08-21 2009-03-05 Actavis Group Ptc Ehf Paliperidone Polymorphs
WO2009044413A2 (en) * 2007-10-05 2009-04-09 Matrix Laboratories Limited Improved process for preparing paliperidone, novel polymorphic forms of the same and process thereof
US20090270620A1 (en) * 2007-11-27 2009-10-29 Santiago Ini Processes for preparing crystal forms of 9-hydroxy-risperidone (paliperidone)
CL2008003667A1 (es) * 2007-12-10 2010-06-04 Synthon Bv Proceso de preparacion de etil-6,7,8,9-tetrahidro-9-hidroxi-2-metil-4h-pirido[1,2-a]piridin-4-ona; y uno de los intermediarios considerados en el proceso descrito; util en la preparacion de paliperidona.
TWI385157B (zh) * 2008-01-16 2013-02-11 Scinopharm Taiwan Ltd 用於製備帕潘立酮(paliperidone)之新穎中間體
NZ586930A (en) * 2008-02-05 2012-06-29 Watson Pharma Private Ltd An improved process for preparation of paliperidone
EP2280967A2 (de) * 2008-03-27 2011-02-09 Actavis Group PTC EHF Hochreines paliperidon oder ein pharmazeutisch unbedenkliches salz davon, welches im wesentlichen frei von keto-verunreinigungen ist
ES2625323T3 (es) 2008-05-29 2017-07-19 Inke, S.A. Proceso para preparar paliperidona e intermedios de la misma
US8481729B2 (en) 2008-06-16 2013-07-09 Msn Laboratories Limited Processes for the preparation of paliperidone
US7932385B2 (en) * 2008-07-11 2011-04-26 Synthon Bv Paliperidone ketone
US20100010218A1 (en) * 2008-07-11 2010-01-14 Jiri Bartl Synthesis of paliperidone
WO2010064134A2 (en) * 2008-12-05 2010-06-10 Cadila Pharmaceuticals Ltd. Process of synthesis of paliperidone
EP2202234A1 (de) 2008-12-24 2010-06-30 Laboratorios Lesvi, S.L. Reinigung von Paliperidon
WO2010136895A1 (en) 2009-05-28 2010-12-02 Actavis Group Ptc Ehf Solid state forms of paliperidone salts and process for the preparation thereof
US20120164188A1 (en) 2009-09-10 2012-06-28 Actavis Group Ptc Ehf Paliperidone or a pharmaceutically acceptable salt thereof substantially free of impurities
WO2011073997A2 (en) * 2009-12-14 2011-06-23 Cadila Healthcare Limited Process for preparing paliperidone and pharmaceutically acceptable salts thereof
US8088594B2 (en) * 2010-03-16 2012-01-03 Saladax Biomedical Inc. Risperidone immunoassay
WO2012035554A1 (en) 2010-09-14 2012-03-22 Megafine Pharma (P) Ltd. An improved process for the preparation of highly pure paliperidone
CN103387575A (zh) * 2013-07-22 2013-11-13 江苏万特制药有限公司 帕潘立酮的制备方法及其关键中间体
KR101867988B1 (ko) * 2016-11-02 2018-06-15 주식회사 엔지켐생명과학 팔리페리돈 중간체 및 이를 이용한 팔리페리돈의 제조방법
CN115260190A (zh) * 2022-08-30 2022-11-01 南开大学 一种帕利哌酮前药、制剂及其制备方法和应用

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4804663A (en) * 1985-03-27 1989-02-14 Janssen Pharmaceutica N.V. 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
CA2000786C (en) * 1988-11-07 1999-01-26 Cornelus G. M. Janssen 3-piperidinyl-1,2-benzisoxazoles
US5158952A (en) * 1988-11-07 1992-10-27 Janssen Pharmaceutica N.V. 3-[2-[4-(6-fluoro-1,2-benzisoxozol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9 tetrahydro-9-hydroxy-2-methyl-4H-pyrido [1,2-a]pyrimidin-4-one, compositions and method of use
GB9008850D0 (en) * 1990-04-19 1990-06-13 Janssen Pharmaceutica Nv Novel 2,9-disubstituted-4h-pyridol(1,2-a)pyrimidin-4-ones

Also Published As

Publication number Publication date
RU2126406C1 (ru) 1999-02-20
WO1995014691A1 (en) 1995-06-01
AU687940B2 (en) 1998-03-05
EP0730594A1 (de) 1996-09-11
CA2175372A1 (en) 1995-06-01
AU1065495A (en) 1995-06-13
DK0730594T3 (da) 2000-03-27
DE69420579D1 (de) 1999-10-14
JPH09505574A (ja) 1997-06-03
GR3031500T3 (en) 2000-01-31
DE69420579T2 (de) 2000-04-27
EP0730594B1 (de) 1999-09-08
US5688799A (en) 1997-11-18
FI962155A (fi) 1996-05-22
CA2175372C (en) 2006-02-21
SI0730594T1 (en) 1999-12-31
FI962155A0 (fi) 1996-05-22
ES2137486T3 (es) 1999-12-16
JP3553951B2 (ja) 2004-08-11
ATE184281T1 (de) 1999-09-15

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