CA2000786A1 - 3-piperidinyl-1,2-benzisoxazoles - Google Patents

3-piperidinyl-1,2-benzisoxazoles

Info

Publication number
CA2000786A1
CA2000786A1 CA2000786A CA2000786A CA2000786A1 CA 2000786 A1 CA2000786 A1 CA 2000786A1 CA 2000786 A CA2000786 A CA 2000786A CA 2000786 A CA2000786 A CA 2000786A CA 2000786 A1 CA2000786 A1 CA 2000786A1
Authority
CA
Canada
Prior art keywords
benzisoxazoles
piperidinyl
saidcompounds
warm
preparing
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.)
Granted
Application number
CA2000786A
Other languages
English (en)
Other versions
CA2000786C (fr
Inventor
Cornelus G. M. Janssen
Alfonsus G. Knaeps
Ludo E. J. Kennis
Jan Vandenberk
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
Publication of CA2000786A1 publication Critical patent/CA2000786A1/fr
Application granted granted Critical
Publication of CA2000786C publication Critical patent/CA2000786C/fr
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
    • A61P25/00—Drugs for disorders of the nervous 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • 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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CA002000786A 1988-11-07 1989-10-16 3-piperidinyl-1,2-benzisoxazoles Expired - Lifetime CA2000786C (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US26785788A 1988-11-07 1988-11-07
US267,857 1988-11-07

Publications (2)

Publication Number Publication Date
CA2000786A1 true CA2000786A1 (fr) 1990-05-07
CA2000786C CA2000786C (fr) 1999-01-26

Family

ID=23020416

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002000786A Expired - Lifetime CA2000786C (fr) 1988-11-07 1989-10-16 3-piperidinyl-1,2-benzisoxazoles

Country Status (21)

Country Link
EP (1) EP0368388B1 (fr)
JP (1) JP2758045B2 (fr)
KR (1) KR0146053B1 (fr)
AT (1) ATE122349T1 (fr)
AU (1) AU614437B2 (fr)
CA (1) CA2000786C (fr)
CL (1) CL43432B (fr)
CY (2) CY1926A (fr)
DE (2) DE122007000081I2 (fr)
DK (1) DK169923B1 (fr)
ES (1) ES2075036T3 (fr)
FI (1) FI92201C (fr)
HK (1) HK131696A (fr)
IE (1) IE66370B1 (fr)
IL (1) IL92208A0 (fr)
LU (1) LU91362I2 (fr)
NL (1) NL300298I2 (fr)
NO (2) NO173015C (fr)
NZ (1) NZ231062A (fr)
PT (1) PT92206B (fr)
ZA (1) ZA898436B (fr)

Families Citing this family (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9008850D0 (en) * 1990-04-19 1990-06-13 Janssen Pharmaceutica Nv Novel 2,9-disubstituted-4h-pyridol(1,2-a)pyrimidin-4-ones
US5378714A (en) * 1991-11-27 1995-01-03 Novo Nordisk A/S Antipsychotic piperidine derivatives
NZ245260A (en) * 1991-11-27 1995-06-27 Novo Nordisk As Piperidine derivatives, preparation and pharmaceutical compositions thereof
ES2050069B1 (es) * 1992-07-10 1994-12-16 Vita Invest Sa Procedimiento para la obtencion de 3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-il)piperidino)etil)-2-metil-6,7,8,9-tetrahidro-4h-pirido(1,2-a) pirimidin-4-ona.
DK60793D0 (da) * 1993-05-26 1993-05-26 Novo Nordisk As Kemiske forbindelser, deres fremstilling og anvendelse
DK60593D0 (da) * 1993-05-26 1993-05-26 Novo Nordisk As Kemiske forbindelser, deres fremstilling og anvendelse
ATE288270T1 (de) * 1993-11-19 2005-02-15 Janssen Pharmaceutica Nv Mikroverkapselte 1,2-benzazole
AU687940B2 (en) * 1993-11-23 1998-03-05 Janssen Pharmaceutica N.V. Novel 9-hydroxy-pyrido(1,2-a)pyrimidin-4-one ether derivatives
ES2085234B1 (es) * 1994-02-24 1997-01-16 Vita Invest Sa Agente activo sobre el sistema nervioso central, procedimiento para su preparacion y composiciones farmaceuticas que lo contienen.
TW487572B (en) * 1996-05-20 2002-05-21 Janssen Pharmaceutica Nv Aqueous suspensions of 9-hydroxyrisperidone fatty acid esters
US6028083A (en) * 1997-07-25 2000-02-22 Hoechst Marion Roussel, Inc. Esters of (+)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl) ethyl]-4-piperidinemethanol
UA72189C2 (uk) * 1997-11-17 2005-02-15 Янссен Фармацевтика Н.В. Фармацевтична композиція, що містить водну суспензію субмікронних ефірів 9-гідроксирисперидон жирних кислот
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.
WO1999059589A1 (fr) * 1998-05-18 1999-11-25 Sepracor Inc. Compositions d'hydroxyrisperidone (-) et methodes associees
AU3900499A (en) 1998-05-18 1999-12-06 Sepracor, Inc. (+)-hydroxyrisperidone compositions and methods
US6342488B1 (en) 1998-08-18 2002-01-29 Sepracor, Inc. Phosphonorisperidone and sulforisperidone compositions and methods
ES2197801B1 (es) * 2002-03-05 2005-03-16 Ferrer Internacional,S.A Procedimiento de obtencion de la 3-(2-(4-(6-fluoro-benzo(d)isoxazol-3-il) piperidin-1-il)-etil)-2-metil-6,7,8,9-tetrahidro-4h-pirido-(1,2-a ) pirimidin-4-ona.
KR20040025224A (ko) * 2002-09-18 2004-03-24 주식회사 대웅 2-(2-메틸-4-옥소-6,7,8,9-테트라하이드로-4Ｈ-피리도[1,2-ａ]피리미딘-3-일)아세트알데히드 및 그 제조방법
EP1560814A1 (fr) 2002-11-13 2005-08-10 Synthon B.V. Procede de fabrication de la risperidone et des intermediaires associes
WO2006027370A1 (fr) * 2004-09-09 2006-03-16 Janssen Pharmaceutica N.V. Preparation de 9-hydroxy-3-(2-hydroxyethyl)-2-methyl-4h-pyrido`1,2-a!pyrimidin-4-one et leurs cristaux
US20070197591A1 (en) 2005-12-12 2007-08-23 Sandra Boom Use of paliperidone for the treatment of a mental disorder in a psychiatric patient with reduced hepatic function
EP2133352A3 (fr) * 2006-08-14 2010-01-13 Teva Pharmaceutical Industries Ltd. Forme cristalline de la 9-hydroxy-rispéridone (palipéridone)
JP2009524685A (ja) * 2006-08-14 2009-07-02 テバ ファーマシューティカル インダストリーズ リミティド ９−ヒドロキシ−リスペリドン（パリペリドン）の結晶型
EP2133351A3 (fr) * 2006-08-14 2010-01-13 Teva Pharmaceutical Industries Ltd. Forme cristalline de la 9-hydroxy-rispéridone (palipéridone)
JP2009524574A (ja) * 2006-08-23 2009-07-02 テバ ファーマシューティカル インダストリーズ リミティド Ｃｍｈｔｐ及びその中間体の合成方法
US7820816B2 (en) 2006-08-23 2010-10-26 Teva Pharmaceutical Industries Ltd. Process for the synthesis of CMHTP and intermediates thereof
WO2008087557A2 (fr) * 2007-01-08 2008-07-24 Actavis Group Ptc Ehf Procédé amélioré de préparation de chlorhydrate de 9-hydroxy-3-(2-chloroéthyl)- 2-méthyl-4h-pyrido[1,2-a]pyrimidin-4-one
US8314110B2 (en) * 2007-04-19 2012-11-20 Youxin Li Compounds for treating mental disorders, and preparation and uses thereof
WO2009010988A1 (fr) * 2007-07-19 2009-01-22 Natco Pharma Limited Procédé amélioré, industriellement viable pour la préparation de palipéridone de haute pureté
WO2009015828A1 (fr) * 2007-07-27 2009-02-05 Synthon B.V. Dérivés de palipéridone
WO2009045489A2 (fr) * 2007-10-03 2009-04-09 Teva Pharmaceutical Industries Ltd. Procédé de synthèse de cmhtp, un intermédiaire de la palipéridone
JP2010540676A (ja) * 2007-10-09 2010-12-24 シプラ・リミテッド パリペリドン及びその医薬として許容し得る塩の製造方法、並びに該方法に使用する中間体
WO2009074333A1 (fr) * 2007-12-10 2009-06-18 Synthon B.V. Synthèse de palipéridone
EP2249649A4 (fr) * 2008-02-05 2012-09-26 Watson Pharma Private Ltd Procédé amélioré pour la préparation de palipéridone
EP2285804A4 (fr) * 2008-04-21 2011-09-14 Glenmark Generics Ltd Procédé pour la fabrication d'intermédiaires de palipéridone
US8309717B2 (en) 2008-05-29 2012-11-13 Inke, S.A. Process to prepare paliperidone and intermediates thereof
WO2010004578A2 (fr) * 2008-06-16 2010-01-14 Msn Laboratories Limited Nouveaux procédés améliorés de préparation de la palipéridone
WO2010003702A1 (fr) * 2008-07-11 2010-01-14 Synthon B.V. Synthèse de palipéridone
WO2010003703A2 (fr) * 2008-07-11 2010-01-14 Synthon B.V. Palipéridone cétone
SI22856A (sl) * 2008-07-31 2010-02-26 Krka, Tovarna Zdravil, D.D., Novo Mesto Proces za pripravo paliperidona
EP2161019A1 (fr) 2008-09-05 2010-03-10 KRKA, D.D., Novo Mesto Composition pharmaceutique multi-particules à libération prolongée comportant de la palipéridone
EP2199293A1 (fr) 2008-12-22 2010-06-23 Chemo Ibérica, S.A. Procédé à étape unique pour la préparation de palipéridone en son sel d'oxalate
EP2202234A1 (fr) 2008-12-24 2010-06-30 Laboratorios Lesvi, S.L. Purification de la palipéridone
EP2275423B9 (fr) 2009-07-13 2012-08-15 KRKA, d.d., Novo mesto Procédé de synthèse de palipéridone
WO2011018246A2 (fr) 2009-08-13 2011-02-17 Synthon B.V. Composition de palipéridone à libération contrôlée
EP2343296A1 (fr) 2009-12-01 2011-07-13 Chemo Ibérica, S.A. Procédé pour la purification de la palipéridone
US20120259116A1 (en) * 2009-12-17 2012-10-11 Rajiv Kumar Novel Process for the Preparation of Paliperidone
US8088594B2 (en) * 2010-03-16 2012-01-03 Saladax Biomedical Inc. Risperidone immunoassay
WO2012035554A1 (fr) * 2010-09-14 2012-03-22 Megafine Pharma (P) Ltd. Procédé amélioré de préparation de palipéridone très pure
AU2011328993B2 (en) 2010-11-15 2017-03-02 Agenebio, Inc. Pyridazine derivatives, compositions and methods for treating cognitive impairment
CN102153552B (zh) * 2011-03-01 2012-08-22 吉林大学 两种帕潘立酮药物共晶及其制备方法
CN102206210B (zh) * 2011-04-01 2014-07-02 常州市第四制药厂有限公司 一种6-氟-3-(4-哌啶基)-1，2-苯并异噁唑盐酸盐的生产方法
US10154988B2 (en) 2012-11-14 2018-12-18 The Johns Hopkins University Methods and compositions for treating schizophrenia
EP4032889B1 (fr) 2013-12-20 2026-05-06 Agenebio, Inc. Dérivés de benzodiazépine, compositions et méthodes de traitement de déficience cognitive
EP3310785B1 (fr) 2015-06-19 2024-11-20 Agenebio, Inc. Dérivés de benzodiazépine, compositions et méthodes de traitement de la déficience cognitive
US20180170941A1 (en) 2016-12-19 2018-06-21 Agenebio, Inc. Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment
US11377445B2 (en) 2018-02-21 2022-07-05 Zenvision Pharma Llp Derivatives of paliperidone and process for the preparation thereof
AU2019288382B2 (en) 2018-06-19 2024-07-25 Agenebio, Inc. Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment
EP4572852A1 (fr) 2022-08-19 2025-06-25 Agenebio, Inc. Dérivés de benzoazépine, compositions et méthodes de traitement de déficience cognitive
CN116003404B (zh) * 2022-12-14 2024-10-01 杭州同舟生物技术有限公司 一种利培酮人工半抗原、人工抗原及其制备方法和应用

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4342870A (en) * 1980-03-28 1982-08-03 Janssen Pharmaceutica N.V. Novel 3-(1-piperidinylalkyl)-4H-pyrido[1,2-a]pyrimidin-4-one derivatives
US4804663A (en) * 1985-03-27 1989-02-14 Janssen Pharmaceutica N.V. 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles

Also Published As

Publication number Publication date
DK169923B1 (da) 1995-04-03
IE893564L (en) 1990-05-07
LU91362I2 (fr) 2007-11-12
HK131696A (en) 1996-07-26
NO173015B (no) 1993-07-05
JP2758045B2 (ja) 1998-05-25
AU614437B2 (en) 1991-08-29
IE66370B1 (en) 1995-12-27
PT92206B (pt) 1995-07-06
ATE122349T1 (de) 1995-05-15
FI895261A0 (fi) 1989-11-06
JPH02191276A (ja) 1990-07-27
NL300298I2 (nl) 2008-03-03
KR0146053B1 (ko) 1998-08-17
NL300298I1 (nl) 2007-12-03
CA2000786C (fr) 1999-01-26
IL92208A0 (en) 1990-07-26
FI92201B (fi) 1994-06-30
NZ231062A (en) 1991-09-25
NO2007017I2 (no) 2010-01-25
NO894411L (no) 1990-05-08
ZA898436B (en) 1991-07-31
CY2007025I2 (el) 2009-11-04
KR910009700A (ko) 1991-06-28
NO173015C (no) 1993-10-13
EP0368388A3 (fr) 1991-07-17
DK551989A (da) 1990-05-08
NO894411D0 (no) 1989-11-06
ES2075036T3 (es) 1995-10-01
DK551989D0 (da) 1989-11-06
AU4443689A (en) 1990-05-10
EP0368388B1 (fr) 1995-05-10
EP0368388A2 (fr) 1990-05-16
DE68922577D1 (de) 1995-06-14
CY1926A (en) 1989-10-30
NO2007017I1 (no) 2008-01-14
CL43432B (es) 2005-06-03
PT92206A (pt) 1990-05-31
FI92201C (fi) 1994-10-10
DE122007000081I2 (de) 2010-01-28
CY2007025I1 (el) 2009-11-04
DE122007000081I1 (de) 2008-02-28
DE68922577T2 (de) 1995-09-28

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