ES2137486T3 - Derivados de 9-hidroxi-pirido(1,2-a)pirimidin-4-ona-eter. - Google Patents

Derivados de 9-hidroxi-pirido(1,2-a)pirimidin-4-ona-eter.

Info

Publication number
ES2137486T3
ES2137486T3 ES95901389T ES95901389T ES2137486T3 ES 2137486 T3 ES2137486 T3 ES 2137486T3 ES 95901389 T ES95901389 T ES 95901389T ES 95901389 T ES95901389 T ES 95901389T ES 2137486 T3 ES2137486 T3 ES 2137486T3
Authority
ES
Spain
Prior art keywords
sub
alkyl
pirido
pirimidin
eter
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.)
Expired - Lifetime
Application number
ES95901389T
Other languages
English (en)
Inventor
Jan Vandenberk
Ludo Edmond Josephine Kennis
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.)
Janssen Pharmaceutica NV
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
Application granted granted Critical
Publication of ES2137486T3 publication Critical patent/ES2137486T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

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
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • 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
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs 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)

Abstract

ESTA INVENCION SE REFIERE A LOS NUEVOS COMPUESTOS CON LA FORMULA (I), LAS SALES DE ADICION DE ACIDOS DE LOS MISMOS FARMACEUTICAMENTE ACEPTABLES Y LAS FORMAS ISOMERICAS ESTEREOQUIMICAS DE LOS MISMOS, DONDE ALQ REPRESENTA C{SUB,1-4}ALCANIEDILO; D ES UN HETEROCICLO BICICLICO DE LA FORMULA (A) O (B) DONDE CADA R{SUP,1} ES INDEPENDIENTEMENTE C{SUB,2-6} ALQUENILO; C{SUB,2-6}ALQUINILO; C{SUB,36}CICLOALQUILO, SUSTITUIBLE OPTATIVAMENTE POR C{SUB,1-4}ALQUILO; C{SUB,1-19}ALQUILO, SUSTITUIBLE OPTATIVAMENTE POR C{SUB,36}CICLOALQUILO, HALO, C{SUB,1-6} ALQUILOXI O CIANO; Y CADA R{SUP,2} ES INDEPENDIENTEMENTE HIDROGENO O C{1-4}ALQUILO. SE DESCRIBEN COMPUESTOS NUEVOS; COMPOSICIONES; PROCESOS PARA PREPARAR LOS COMPUESTOS NUEVOS E INTERMEDIOS.
ES95901389T 1993-11-23 1994-11-16 Derivados de 9-hidroxi-pirido(1,2-a)pirimidin-4-ona-eter. Expired - Lifetime ES2137486T3 (es)

Applications Claiming Priority (3)

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
EP95901389A EP0730594B1 (en) 1993-11-23 1994-11-16 9-HYDROXY-PYRIDO [1,2-a]PYRIMIDIN-4-ONE ETHER DERIVATIVES

Publications (1)

Publication Number Publication Date
ES2137486T3 true ES2137486T3 (es) 1999-12-16

Family

ID=8214180

Family Applications (1)

Application Number Title Priority Date Filing Date
ES95901389T Expired - Lifetime ES2137486T3 (es) 1993-11-23 1994-11-16 Derivados de 9-hidroxi-pirido(1,2-a)pirimidin-4-ona-eter.

Country Status (14)

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

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
EP1791839B1 (en) * 2004-09-09 2015-06-10 Janssen Pharmaceutica NV Preparation of 9-hydroxy-3-(2-hydroxyethyl)-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one and crystalls thereof
HUP0402163A2 (en) * 2004-10-25 2006-05-29 Richter Gedeon Vegyeszet Process for the preparation of risperidone
WO2008021342A2 (en) * 2006-08-14 2008-02-21 Teva Pharmaceutical Industries Ltd. Amorphous and crystalline forms of 9-hydroxy-risperidone ( paliperidone )
WO2008021345A2 (en) 2006-08-14 2008-02-21 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
CN101600716A (zh) * 2007-01-08 2009-12-09 阿特维斯集团公司 用于制备9-羟基-3-(2-氯乙基)-2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮盐酸盐的改进方法
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
EP2178872A1 (en) * 2007-07-27 2010-04-28 Synthon B.V. Paliperidone derivatives
WO2009056990A2 (en) * 2007-08-21 2009-05-07 Actavis Group Ptc Ehf Paliperidone polymorphs
PT2079446E (pt) * 2007-08-21 2011-12-23 Teva Pharma Formulação de libertação sustida de paliperidona
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)
WO2009074333A1 (en) * 2007-12-10 2009-06-18 Synthon B.V. Synthesis of paliperidone
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
US20100311969A1 (en) * 2008-02-05 2010-12-09 Watson Pharma Private Limited Process For Preparation of Paliperidone
US20090247553A1 (en) * 2008-03-27 2009-10-01 Actavis Group Ptc Ehf Highly Pure Paliperidone or a Pharmaceutically Acceptable Salt Thereof Substantially Free of Keto Impurity
ES2625323T3 (es) * 2008-05-29 2017-07-19 Inke, S.A. Proceso para preparar paliperidona e intermedios de la misma
EP2300467A4 (en) 2008-06-16 2012-04-25 Msn Lab Ltd NEW AND IMPROVED METHODS FOR THE MANUFACTURE OF PALIPERIDONE
EP2321311B1 (en) * 2008-07-11 2012-09-19 Synthon B.V. Synthesis of paliperidone
WO2010003703A2 (en) * 2008-07-11 2010-01-14 Synthon B.V. Paliperidone ketone
WO2010064134A2 (en) * 2008-12-05 2010-06-10 Cadila Pharmaceuticals Ltd. Process of synthesis of paliperidone
EP2202234A1 (en) 2008-12-24 2010-06-30 Laboratorios Lesvi, S.L. Purification of paliperidone
US20120100188A1 (en) 2009-05-28 2012-04-26 Actavis Group Ptc Ehf Solid state forms of paliperidone salts and process for the preparation thereof
WO2011030224A2 (en) 2009-09-10 2011-03-17 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 (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4485107A (en) * 1982-11-01 1984-11-27 Janssen Pharmaceutica N.V. [[Bis(aryl)methylene]-1-piperidinyl]alkyl-pyrimidinones
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
CA2175372A1 (en) 1995-06-01
WO1995014691A1 (en) 1995-06-01
GR3031500T3 (en) 2000-01-31
JP3553951B2 (ja) 2004-08-11
DE69420579T2 (de) 2000-04-27
AU1065495A (en) 1995-06-13
FI962155L (fi) 1996-05-22
ATE184281T1 (de) 1999-09-15
JPH09505574A (ja) 1997-06-03
FI112483B (fi) 2003-12-15
AU687940B2 (en) 1998-03-05
SI0730594T1 (en) 1999-12-31
EP0730594B1 (en) 1999-09-08
EP0730594A1 (en) 1996-09-11
DK0730594T3 (da) 2000-03-27
RU2126406C1 (ru) 1999-02-20
FI962155A0 (fi) 1996-05-22
US5688799A (en) 1997-11-18
DE69420579D1 (de) 1999-10-14
CA2175372C (en) 2006-02-21

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