ES2075036T3 - 3-piperidinil-1,2-benzoisoxazoles. - Google Patents

3-piperidinil-1,2-benzoisoxazoles.

Info

Publication number
ES2075036T3
ES2075036T3 ES89202724T ES89202724T ES2075036T3 ES 2075036 T3 ES2075036 T3 ES 2075036T3 ES 89202724 T ES89202724 T ES 89202724T ES 89202724 T ES89202724 T ES 89202724T ES 2075036 T3 ES2075036 T3 ES 2075036T3
Authority
ES
Spain
Prior art keywords
alkyl
piperidinyl
pharmaceutical compositions
compounds
benzoisoxazoles
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
ES89202724T
Other languages
English (en)
Inventor
Cornelus Gerardus Mari Janssen
Alfonsus Guilielmus Knaeps
Ludo Edmond Josephine 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
Application granted granted Critical
Publication of ES2075036T3 publication Critical patent/ES2075036T3/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
    • 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 And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

NUEVOS 3-PIPERIDINIL-1,2-BENCISOOXAZOLES DE FORMULA EN DONDE ALK ES C1-4 ALCANODIIL; R1 ES HIDROGENO, C1-4 ALQUILO O ION HALOGENO; R2 ES C1-4 ALQUILO; R3 ES HIDROXILO O R4-C(=O)O-; Y R4 ES C1-19 ALQUILO; LAS SALES FARMACEUTICAMENTE ACEPTABLES DE ADICION ACIDA Y ESTEREOISOMEROS DE ELLOS, CUYOS COMPUESTOS SON AGENTES ANTIPSICOTICOS; COMPOSICIONES FARMACEUTICAS CONTENIENDO TALES COMPUESTOS COMO UN INGREDIENTE ACTIVO Y METODOS DE PREPARAR DICHOS COMPUESTOS Y COMPOSICIONES FARMACEUTICAS.
ES89202724T 1988-11-07 1989-10-30 3-piperidinil-1,2-benzoisoxazoles. Expired - Lifetime ES2075036T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US26785788A 1988-11-07 1988-11-07

Publications (1)

Publication Number Publication Date
ES2075036T3 true ES2075036T3 (es) 1995-10-01

Family

ID=23020416

Family Applications (1)

Application Number Title Priority Date Filing Date
ES89202724T Expired - Lifetime ES2075036T3 (es) 1988-11-07 1989-10-30 3-piperidinil-1,2-benzoisoxazoles.

Country Status (21)

Country Link
EP (1) EP0368388B1 (es)
JP (1) JP2758045B2 (es)
KR (1) KR0146053B1 (es)
AT (1) ATE122349T1 (es)
AU (1) AU614437B2 (es)
CA (1) CA2000786C (es)
CL (1) CL43432B (es)
CY (2) CY1926A (es)
DE (2) DE68922577T2 (es)
DK (1) DK169923B1 (es)
ES (1) ES2075036T3 (es)
FI (1) FI92201C (es)
HK (1) HK131696A (es)
IE (1) IE66370B1 (es)
IL (1) IL92208A0 (es)
LU (1) LU91362I2 (es)
NL (1) NL300298I2 (es)
NO (2) NO173015C (es)
NZ (1) NZ231062A (es)
PT (1) PT92206B (es)
ZA (1) ZA898436B (es)

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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
US5378714A (en) * 1991-11-27 1995-01-03 Novo Nordisk A/S Antipsychotic piperidine derivatives
WO1993010742A2 (en) * 1991-11-27 1993-06-10 Novo Nordisk A/S Chemical compounds, their preparation and use
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
CN1074923C (zh) * 1993-11-19 2001-11-21 詹森药业有限公司 微囊密封的3-哌啶基取代的1,2-苯并异唑类和1,2-苯并异噻唑类
US5688799A (en) * 1993-11-23 1997-11-18 Janssen Pharmaceutica N.V. 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 (en) * 1998-05-18 1999-11-25 Sepracor Inc. (-)-hydroxyrisperidone compositions and methods
AU5489299A (en) * 1998-08-18 2000-03-14 Sepracor, Inc. Use of hydroxyrisperidone for the manufacture of a medicament for the treatment and prevention of psychoses, emesis and symptoms of withdrawal from alcohol and nicotine
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 (en) 2002-11-13 2005-08-10 Synthon B.V. Process for making risperidone and intermediates therefor
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 (en) * 2006-08-14 2010-01-13 Teva Pharmaceutical Industries Ltd. Crystal form of 9-hydroxy-risperidone (paliperidone)
WO2008021342A2 (en) * 2006-08-14 2008-02-21 Teva Pharmaceutical Industries Ltd. Amorphous and crystalline forms of 9-hydroxy-risperidone ( paliperidone )
EP2133351A3 (en) * 2006-08-14 2010-01-13 Teva Pharmaceutical Industries Ltd. Crystal form 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
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
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
US8314110B2 (en) * 2007-04-19 2012-11-20 Youxin Li Compounds for treating mental disorders, and preparation and uses thereof
WO2009010988A1 (en) * 2007-07-19 2009-01-22 Natco Pharma Limited An improved, industrially viable process for the preparation of high purity paliperidone
US20090036470A1 (en) * 2007-07-27 2009-02-05 Jiri Bartl Paliperidone derivatives
WO2009045489A2 (en) * 2007-10-03 2009-04-09 Teva Pharmaceutical Industries Ltd. Process for the synthesis of cmhtp, a paliperidone intermediate
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
ES2436658T3 (es) * 2007-12-10 2014-01-03 Synthon B.V. Síntesis de paliperidona
EP2249649A4 (en) * 2008-02-05 2012-09-26 Watson Pharma Private Ltd IMPROVED METHOD FOR THE MANUFACTURE OF PALIPERIDONE
WO2009130710A2 (en) * 2008-04-21 2009-10-29 Glenmark Generics Limited A process for the preparation of paliperidone intermediates
ES2625323T3 (es) 2008-05-29 2017-07-19 Inke, S.A. Proceso para preparar paliperidona e intermedios de la misma
WO2010004578A2 (en) * 2008-06-16 2010-01-14 Msn Laboratories Limited Novel and improved processes for the preparation of paliperidone
WO2010003703A2 (en) * 2008-07-11 2010-01-14 Synthon B.V. Paliperidone ketone
WO2010003702A1 (en) * 2008-07-11 2010-01-14 Synthon B.V. Synthesis of paliperidone
SI22856A (sl) * 2008-07-31 2010-02-26 Krka, Tovarna Zdravil, D.D., Novo Mesto Proces za pripravo paliperidona
EP2161019A1 (en) 2008-09-05 2010-03-10 KRKA, D.D., Novo Mesto Prolonged release multiparticulate pharmaceutical composition comprising paliperidone
EP2199293A1 (en) 2008-12-22 2010-06-23 Chemo Ibérica, S.A. One-step process for preparing paliperidone and its oxalate salt
EP2202234A1 (en) 2008-12-24 2010-06-30 Laboratorios Lesvi, S.L. Purification of paliperidone
ATE544766T1 (de) 2009-07-13 2012-02-15 Krka Verfahren zur synthese von paliperidon
WO2011018246A2 (en) 2009-08-13 2011-02-17 Synthon B.V. Controlled release paliperidone composition
EP2343296A1 (en) 2009-12-01 2011-07-13 Chemo Ibérica, S.A. A process for the purification of paliperidone
WO2011074017A1 (en) * 2009-12-17 2011-06-23 Alkem Laboratories Ltd. A novel process for the preparation of paliperidone
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
EP2640391B1 (en) 2010-11-15 2015-11-11 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
CA2891122C (en) 2012-11-14 2021-07-20 The Johns Hopkins University Methods and compositions for treating schizophrenia
WO2015095783A1 (en) 2013-12-20 2015-06-25 Agenebio, Inc. Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment
JP6987384B2 (ja) 2015-06-19 2021-12-22 エージンバイオ， インコーポレイテッド ベンゾジアゼピン誘導体、組成物、および認知障害を処置するための方法
US11505555B2 (en) 2016-12-19 2022-11-22 Agenebio, Inc. Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment
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
BR112020026062B1 (pt) 2018-06-19 2023-04-04 Agenebio, Inc Compostos derivados de benzodiazepina ou um sal farmaceuticamente aceitavel, isômero ou combinação dos mesmos, composição farmacêutica compreendendo os mesmos e usos dos mesmos para o tratamento de comprometimento cognitivo, câncer cerebral e psicose da doença de parkinson
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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
ATE122349T1 (de) 1995-05-15
EP0368388B1 (en) 1995-05-10
ZA898436B (en) 1991-07-31
AU4443689A (en) 1990-05-10
CY1926A (en) 1989-10-30
FI92201B (fi) 1994-06-30
JP2758045B2 (ja) 1998-05-25
CA2000786C (en) 1999-01-26
NO2007017I2 (no) 2010-01-25
JPH02191276A (ja) 1990-07-27
DE68922577T2 (de) 1995-09-28
PT92206A (pt) 1990-05-31
DE68922577D1 (de) 1995-06-14
KR0146053B1 (ko) 1998-08-17
NO173015B (no) 1993-07-05
EP0368388A3 (en) 1991-07-17
NO173015C (no) 1993-10-13
DK551989A (da) 1990-05-08
FI895261A0 (fi) 1989-11-06
LU91362I2 (fr) 2007-11-12
DK551989D0 (da) 1989-11-06
IE893564L (en) 1990-05-07
FI92201C (fi) 1994-10-10
KR910009700A (ko) 1991-06-28
NO894411D0 (no) 1989-11-06
AU614437B2 (en) 1991-08-29
EP0368388A2 (en) 1990-05-16
PT92206B (pt) 1995-07-06
IL92208A0 (en) 1990-07-26
IE66370B1 (en) 1995-12-27
CY2007025I2 (el) 2009-11-04
HK131696A (en) 1996-07-26
NL300298I1 (nl) 2007-12-03
DE122007000081I1 (de) 2008-02-28
NL300298I2 (nl) 2008-03-03
CL43432B (es) 2005-06-03
CY2007025I1 (el) 2009-11-04
NO2007017I1 (no) 2008-01-14
NO894411L (no) 1990-05-08
NZ231062A (en) 1991-09-25
DK169923B1 (da) 1995-04-03
CA2000786A1 (en) 1990-05-07
DE122007000081I2 (de) 2010-01-28

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