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 Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (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)

Families Citing this family (61)

* Cited by examiner, † Cited by third party
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US5378714A (en) * 1991-11-27 1995-01-03 Novo Nordisk A/S Antipsychotic piperidine derivatives
AU672182B2 (en) * 1991-11-27 1996-09-26 Novo Nordisk A/S Piperidine derivatives and their use in treating psychosis
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
NZ276088A (en) 1993-11-19 1999-07-29 Janssen Pharmaceutica Nv [(1,2-benzisoxazol-3-yl)-1-piperidinyl-alkyl-6,7,8,9-tetrahydro-4h- pyrido[1,2-a]-pyrimidin-4-one derivatives (ie risperidone)
DE69420579T2 (de) * 1993-11-23 2000-04-27 Janssen Pharmaceutica Nv 9-HYDROXY-PYRIDO [1,2-a] PYRIMIDIN-4-ON-ETHER-DERIVATE
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.
US6500833B1 (en) 1998-05-18 2002-12-31 Sepracor Inc. (+)-Hydroxyrisperidone compositions and methods
US6326362B1 (en) 1998-05-18 2001-12-04 Sepracor Inc. (-)-phosphonorisperidone and (-)-sulforisperidone 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
CN100390146C (zh) 2002-11-13 2008-05-28 斯索恩有限公司 制备利培酮的方法和用于该方法的中间体
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
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
US20080177067A1 (en) * 2006-08-14 2008-07-24 Ben-Zion Dolitzky Crystal forms of 9-hydroxy-risperidone (paliperidone)
EP2133352A3 (en) * 2006-08-14 2010-01-13 Teva Pharmaceutical Industries Ltd. Crystal form of 9-hydroxy-risperidone (paliperidone)
EP2133351A3 (en) * 2006-08-14 2010-01-13 Teva Pharmaceutical Industries Ltd. Crystal form of 9-hydroxy-risperidone (paliperidone)
KR20090079189A (ko) * 2006-08-23 2009-07-21 테바 파마슈티컬 인더스트리즈 리미티드 Ｃｍｈｔｐ 및 이의 중간체의 합성 방법
US7820816B2 (en) 2006-08-23 2010-10-26 Teva Pharmaceutical Industries Ltd. Process for the synthesis of CMHTP and intermediates thereof
US8071767B2 (en) 2007-01-08 2011-12-06 Actavis Group Ptc Ehf Process for preparation of 9-hydroxy-3-(2-chloroethyl)-2-methyl-4H-pyrido[1,2-A]pyrimidin-4-one hydrochloride
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
EP2178872A1 (en) * 2007-07-27 2010-04-28 Synthon B.V. 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
EP2235009B1 (en) * 2007-12-10 2013-10-30 Synthon B.V. Synthesis of paliperidone
WO2009116071A2 (en) * 2008-02-05 2009-09-24 Watson Pharma Private Limited An improved process for preparation of paliperidone
EP2285804A4 (en) * 2008-04-21 2011-09-14 Glenmark Generics Ltd METHOD FOR MANUFACTURING PALIPERIDONE INTERMEDIATES
US8309717B2 (en) 2008-05-29 2012-11-13 Inke, S.A. Process to prepare paliperidone and intermediates thereof
US8481729B2 (en) 2008-06-16 2013-07-09 Msn Laboratories Limited Processes for the preparation of paliperidone
WO2010003702A1 (en) * 2008-07-11 2010-01-14 Synthon B.V. Synthesis of paliperidone
US7932385B2 (en) 2008-07-11 2011-04-26 Synthon Bv Paliperidone ketone
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
EP2275423B9 (en) 2009-07-13 2012-08-15 KRKA, d.d., Novo mesto Process for the synthesis of paliperidone
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
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 (en) * 2010-09-14 2012-03-22 Megafine Pharma (P) Ltd. An improved process for the preparation of highly pure paliperidone
CN103313712B (zh) 2010-11-15 2016-10-26 艾吉因生物股份有限公司 用于治疗认知障碍的哒嗪衍生物、组合物和方法
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
JP6440625B2 (ja) 2012-11-14 2018-12-19 ザ・ジョンズ・ホプキンス・ユニバーシティー 精神分裂病を処置するための方法および組成物
JP6883988B2 (ja) 2013-12-20 2021-06-09 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
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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
EA202190076A1 (ru) 2018-06-19 2021-09-22 Эйджинбайо, Инк. Производные бензодиазепина, композиции и способы лечения когнитивных нарушений
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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
HK131696A (en) 1996-07-26
CA2000786C (en) 1999-01-26
CL43432B (es) 2005-06-03
CY2007025I1 (el) 2009-11-04
NO894411L (no) 1990-05-08
FI895261A0 (fi) 1989-11-06
NO2007017I1 (no) 2008-01-14
IE66370B1 (en) 1995-12-27
ATE122349T1 (de) 1995-05-15
KR910009700A (ko) 1991-06-28
EP0368388A3 (en) 1991-07-17
EP0368388B1 (en) 1995-05-10
DE122007000081I1 (de) 2008-02-28
CA2000786A1 (en) 1990-05-07
IE893564L (en) 1990-05-07
DK551989A (da) 1990-05-08
PT92206B (pt) 1995-07-06
FI92201C (fi) 1994-10-10
DE68922577D1 (de) 1995-06-14
PT92206A (pt) 1990-05-31
CY1926A (en) 1989-10-30
ZA898436B (en) 1991-07-31
NO173015B (no) 1993-07-05
FI92201B (fi) 1994-06-30
NO173015C (no) 1993-10-13
DE68922577T2 (de) 1995-09-28
DE122007000081I2 (de) 2010-01-28
DK169923B1 (da) 1995-04-03
JPH02191276A (ja) 1990-07-27
NO2007017I2 (no) 2010-01-25
NZ231062A (en) 1991-09-25
KR0146053B1 (ko) 1998-08-17
AU4443689A (en) 1990-05-10
NL300298I1 (nl) 2007-12-03
IL92208A0 (en) 1990-07-26
EP0368388A2 (en) 1990-05-16
AU614437B2 (en) 1991-08-29
CY2007025I2 (el) 2009-11-04
DK551989D0 (da) 1989-11-06
NL300298I2 (nl) 2008-03-03
JP2758045B2 (ja) 1998-05-25
NO894411D0 (no) 1989-11-06
LU91362I2 (fr) 2007-11-12

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