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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (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 And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (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) DE68922577T2 (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 (61)

* Cited by examiner, † Cited by third party
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GB9008850D0 (en) * 1990-04-19 1990-06-13 Janssen Pharmaceutica Nv Novel 2,9-disubstituted-4h-pyridol(1,2-a)pyrimidin-4-ones
JPH07502268A (ja) * 1991-11-27 1995-03-09 ノボ　ノルディスク　アクティーゼルスカブ 化学化合物、それらの製法および使用
US5378714A (en) * 1991-11-27 1995-01-03 Novo Nordisk A/S Antipsychotic piperidine derivatives
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.
DK60593D0 (da) * 1993-05-26 1993-05-26 Novo Nordisk As Kemiske forbindelser, deres fremstilling og anvendelse
DK60793D0 (da) * 1993-05-26 1993-05-26 Novo Nordisk As Kemiske forbindelser, deres fremstilling og anvendelse
ES2236700T3 (es) * 1993-11-19 2005-07-16 Janssen Pharmaceutica N.V. 1,2-benzazoles microencapsulados.
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.
AU3900499A (en) * 1998-05-18 1999-12-06 Sepracor, Inc. (+)-hydroxyrisperidone compositions and methods
WO1999059589A1 (fr) * 1998-05-18 1999-11-25 Sepracor Inc. Compositions d'hydroxyrisperidone (-) et methodes associees
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
ES2546268T3 (es) 2004-09-09 2015-09-22 Janssen Pharmaceutica Nv Preparación de 9-hidroxi-3-(2-hidroxietil)-2-metil-4H-pirido[1,2-a]pirimidin-4-ona y sus cristales
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)
EP1940834A2 (fr) 2006-08-14 2008-07-09 Teva Pharmaceutical Industries Ltd. Formes cristallines de la 9-hydroxy-rispéridone (palipéridone)
EP2133351A3 (fr) * 2006-08-14 2010-01-13 Teva Pharmaceutical Industries Ltd. Forme cristalline de la 9-hydroxy-rispéridone (palipéridone)
US7820816B2 (en) 2006-08-23 2010-10-26 Teva Pharmaceutical Industries Ltd. Process for the synthesis of CMHTP and intermediates thereof
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
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
DK2154138T3 (en) * 2007-04-19 2015-11-02 Youxin Li Novel compounds for the treatment of psychotic disorders, methods of 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
US20090036470A1 (en) * 2007-07-27 2009-02-05 Jiri Bartl Paliperidone derivatives
WO2009045489A2 (fr) * 2007-10-03 2009-04-09 Teva Pharmaceutical Industries Ltd. Procédé de synthèse de cmhtp, un intermédiaire de la palipéridone
US8242269B2 (en) 2007-10-09 2012-08-14 Cipla Limited Processes for the preparation of paliperidone and pharmaceutically acceptable salts thereof and intermediates for use in the processes
US7977480B2 (en) 2007-12-10 2011-07-12 Synthon Bv Synthesis of paliperidone
AU2009227507A1 (en) * 2008-02-05 2009-09-24 Watson Pharma Private Limited An improved process for preparation of paliperidone
WO2009130710A2 (fr) * 2008-04-21 2009-10-29 Glenmark Generics Limited Procédé pour la fabrication d'intermédiaires de palipéridone
EP2303877B1 (fr) 2008-05-29 2017-02-15 Inke, S.A. Procédé de fabrication de la palipéridone et d'intermédiaires pour celui-ci
US8481729B2 (en) 2008-06-16 2013-07-09 Msn Laboratories Limited Processes for the preparation of paliperidone
WO2010003702A1 (fr) * 2008-07-11 2010-01-14 Synthon B.V. Synthèse de palipéridone
EP2318405A2 (fr) 2008-07-11 2011-05-11 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
SI2275423T1 (sl) 2009-07-13 2012-06-29 Krka D.D., Novo Mesto Postopek za sintezo paliperidona
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
WO2011074017A1 (fr) * 2009-12-17 2011-06-23 Alkem Laboratories Ltd. Nouveau procédé de préparation de palipéridone
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
CA2818025A1 (fr) 2010-11-15 2012-05-24 Agenebio, Inc. Derives de pyridazine, compositions et methodes de traitement d'une deficience cognitive
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
EP2919788A4 (fr) 2012-11-14 2016-05-25 Univ Johns Hopkins Méthodes et compositions pour le traitement de la schizophrénie
EP3083569B1 (fr) 2013-12-20 2022-01-26 Agenebio, Inc. Dérivés de benzodiazépine, compositions et procédés de traitement de la déficience cognitive
WO2016205739A1 (fr) 2015-06-19 2016-12-22 Belew Mekonnen Dérivés de benzodiazépine, compositions et méthodes de traitement de la déficience cognitive
BR112019012821A2 (pt) 2016-12-19 2019-11-26 Agenebio Inc derivados de benzodiazepina, composições e métodos para o tratamento do comprometimento cognitivo
US20180170941A1 (en) 2016-12-19 2018-06-21 Agenebio, Inc. Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment
WO2019162746A1 (fr) * 2018-02-21 2019-08-29 Zenvision Pharma Llp Nouveaux dérivés de palipéridone et leur procédé de préparation
CN112601749B (zh) 2018-06-19 2024-03-26 艾吉因生物股份有限公司 用于治疗认知损害的苯并二氮杂环庚三烯衍生物，组合物和方法
WO2024039886A1 (fr) 2022-08-19 2024-02-22 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
IL92208A0 (en) 1990-07-26
FI92201C (fi) 1994-10-10
CY2007025I2 (el) 2009-11-04
EP0368388A2 (fr) 1990-05-16
DK169923B1 (da) 1995-04-03
ZA898436B (en) 1991-07-31
NO894411D0 (no) 1989-11-06
FI92201B (fi) 1994-06-30
ES2075036T3 (es) 1995-10-01
NO173015C (no) 1993-10-13
CY1926A (en) 1989-10-30
CL43432B (es) 2005-06-03
CY2007025I1 (el) 2009-11-04
CA2000786C (fr) 1999-01-26
DE68922577D1 (de) 1995-06-14
DE122007000081I1 (de) 2008-02-28
AU614437B2 (en) 1991-08-29
DE122007000081I2 (de) 2010-01-28
HK131696A (en) 1996-07-26
NO2007017I2 (no) 2010-01-25
AU4443689A (en) 1990-05-10
DK551989D0 (da) 1989-11-06
KR0146053B1 (ko) 1998-08-17
FI895261A0 (fi) 1989-11-06
PT92206B (pt) 1995-07-06
KR910009700A (ko) 1991-06-28
EP0368388B1 (fr) 1995-05-10
JPH02191276A (ja) 1990-07-27
IE893564L (en) 1990-05-07
PT92206A (pt) 1990-05-31
NL300298I2 (nl) 2008-03-03
NO894411L (no) 1990-05-08
DE68922577T2 (de) 1995-09-28
JP2758045B2 (ja) 1998-05-25
NO2007017I1 (no) 2008-01-14
IE66370B1 (en) 1995-12-27
NO173015B (no) 1993-07-05
ATE122349T1 (de) 1995-05-15
LU91362I2 (fr) 2007-11-12
EP0368388A3 (fr) 1991-07-17
DK551989A (da) 1990-05-08
NL300298I1 (nl) 2007-12-03
NZ231062A (en) 1991-09-25

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