NO173015C - Analogifremgangsmaate til fremstilling av pyrido(1,2-a)pyrimidin-3-piperidinyl-1,2-benzisoksazoler - Google Patents

Analogifremgangsmaate til fremstilling av pyrido(1,2-a)pyrimidin-3-piperidinyl-1,2-benzisoksazoler

Info

Publication number
NO173015C
NO173015C NO894411A NO894411A NO173015C NO 173015 C NO173015 C NO 173015C NO 894411 A NO894411 A NO 894411A NO 894411 A NO894411 A NO 894411A NO 173015 C NO173015 C NO 173015C
Authority
NO
Norway
Prior art keywords
piperidinyl
benzisoxazols
pyrido
pyrimidin
preparation
Prior art date
Application number
NO894411A
Other languages
English (en)
Norwegian (no)
Other versions
NO894411L (no
NO894411D0 (no
NO173015B (no
Inventor
Cornelus Gerardus Mari Janssen
Alfonsus Guilielmus Knaeps
Ludo Edmond Josephine Kennis
Jan Vandenberk
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 NO894411D0 publication Critical patent/NO894411D0/no
Publication of NO894411L publication Critical patent/NO894411L/no
Publication of NO173015B publication Critical patent/NO173015B/no
Publication of NO173015C publication Critical patent/NO173015C/no

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
NO894411A 1988-11-07 1989-11-06 Analogifremgangsmaate til fremstilling av pyrido(1,2-a)pyrimidin-3-piperidinyl-1,2-benzisoksazoler NO173015C (no)

Applications Claiming Priority (1)

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

Publications (4)

Publication Number Publication Date
NO894411D0 NO894411D0 (no) 1989-11-06
NO894411L NO894411L (no) 1990-05-08
NO173015B NO173015B (no) 1993-07-05
NO173015C true NO173015C (no) 1993-10-13

Family

ID=23020416

Family Applications (2)

Application Number Title Priority Date Filing Date
NO894411A NO173015C (no) 1988-11-07 1989-11-06 Analogifremgangsmaate til fremstilling av pyrido(1,2-a)pyrimidin-3-piperidinyl-1,2-benzisoksazoler
NO2007017C NO2007017I2 (no) 1988-11-07 2007-12-21 3-[2-[4-(6-fluor-1,2-benzoksazol-3-yl)-1-piperidinyl]etyl]-6,7,8,9-tetrahydro-9-hydroksy-2-metyl-4H-pyridol]1,2-a]pyrimidin-4-on(palperidone)

Family Applications After (1)

Application Number Title Priority Date Filing Date
NO2007017C NO2007017I2 (no) 1988-11-07 2007-12-21 3-[2-[4-(6-fluor-1,2-benzoksazol-3-yl)-1-piperidinyl]etyl]-6,7,8,9-tetrahydro-9-hydroksy-2-metyl-4H-pyridol]1,2-a]pyrimidin-4-on(palperidone)

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
AU672182B2 (en) * 1991-11-27 1996-09-26 Novo Nordisk A/S Piperidine derivatives and their use in treating psychosis
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.
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
ES2236700T3 (es) 1993-11-19 2005-07-16 Janssen Pharmaceutica N.V. 1,2-benzazoles microencapsulados.
SI0730594T1 (en) * 1993-11-23 1999-12-31 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.
US6500833B1 (en) 1998-05-18 2002-12-31 Sepracor Inc. (+)-Hydroxyrisperidone compositions and methods
WO1999059589A1 (fr) * 1998-05-18 1999-11-25 Sepracor Inc. Compositions d'hydroxyrisperidone (-) et methodes associees
WO2000010572A1 (fr) * 1998-08-18 2000-03-02 Sepracor Inc. Utilisation de l'hydroxyrisperidone pour la fabrication d'un medicament destine au traitement et a la prevention des psychoses, des vomissements et des syndromes de sevrage a l'alcool et a la 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
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
CN101014601B (zh) * 2004-09-09 2011-09-14 詹森药业有限公司 制备9-羟基-3-(2-羟基乙基)-2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮及其晶体
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 (fr) * 2006-08-14 2010-01-13 Teva Pharmaceutical Industries Ltd. Forme cristalline 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)
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
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
KR101244185B1 (ko) * 2007-04-19 2013-03-25 유씬 리 정신 장애 치료용 신규 화합물, 그의 제조 방법 및 용도
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
EP2235009B1 (fr) * 2007-12-10 2013-10-30 Synthon B.V. Synthèse de palipéridone
US20100311969A1 (en) * 2008-02-05 2010-12-09 Watson Pharma Private Limited Process For Preparation of Paliperidone
US20110087024A1 (en) * 2008-04-21 2011-04-14 Glenmark House process for the preparation of paliperidone intermediates
US8309717B2 (en) 2008-05-29 2012-11-13 Inke, S.A. Process to prepare paliperidone and intermediates thereof
EP2300467A4 (fr) * 2008-06-16 2012-04-25 Msn Lab Ltd Nouveaux procédés améliorés de préparation de la palipéridone
WO2010003703A2 (fr) * 2008-07-11 2010-01-14 Synthon B.V. Palipéridone cétone
EP2321311B1 (fr) * 2008-07-11 2012-09-19 Synthon B.V. Synthèse de palipéridone
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
JP5916746B2 (ja) 2010-11-15 2016-05-11 エージンバイオ, インコーポレイテッド 認知障害を処置するためのピリダジン誘導体、組成物、および方法
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
US10154988B2 (en) 2012-11-14 2018-12-18 The Johns Hopkins University Methods and compositions for treating schizophrenia
CN106068256B (zh) 2013-12-20 2020-10-23 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*衍生物、组合物和方法
EP3310785A4 (fr) 2015-06-19 2018-12-26 Agenebio, Inc. 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
CA3104478A1 (fr) 2018-06-19 2019-12-26 Agenebio, Inc. Derives de benzodiazepine, compositions, et methodes de traitement de deficience cognitive
WO2024039886A1 (fr) 2022-08-19 2024-02-22 Agenebio, Inc. Dérivés de benzoazépine, compositions et méthodes de traitement de déficience cognitive
CN116003404A (zh) * 2022-12-14 2023-04-25 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

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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
AU4443689A (en) 1990-05-10
ATE122349T1 (de) 1995-05-15
CY2007025I1 (el) 2009-11-04
ZA898436B (en) 1991-07-31
CL43432B (es) 2005-06-03
DK551989A (da) 1990-05-08
JP2758045B2 (ja) 1998-05-25
NL300298I2 (nl) 2008-03-03
NO894411L (no) 1990-05-08
IL92208A0 (en) 1990-07-26
DE68922577T2 (de) 1995-09-28
PT92206B (pt) 1995-07-06
DE122007000081I1 (de) 2008-02-28
KR910009700A (ko) 1991-06-28
ES2075036T3 (es) 1995-10-01
CY2007025I2 (el) 2009-11-04
NO2007017I1 (no) 2008-01-14
EP0368388B1 (fr) 1995-05-10
NL300298I1 (nl) 2007-12-03
IE66370B1 (en) 1995-12-27
DK169923B1 (da) 1995-04-03
KR0146053B1 (ko) 1998-08-17
EP0368388A3 (fr) 1991-07-17
DK551989D0 (da) 1989-11-06
JPH02191276A (ja) 1990-07-27
LU91362I2 (fr) 2007-11-12
NO2007017I2 (no) 2010-01-25
NO894411D0 (no) 1989-11-06
EP0368388A2 (fr) 1990-05-16
HK131696A (en) 1996-07-26
CA2000786C (fr) 1999-01-26
FI92201C (fi) 1994-10-10
CY1926A (en) 1989-10-30
FI92201B (fi) 1994-06-30
IE893564L (en) 1990-05-07
AU614437B2 (en) 1991-08-29
DE122007000081I2 (de) 2010-01-28
NZ231062A (en) 1991-09-25
PT92206A (pt) 1990-05-31
NO173015B (no) 1993-07-05
CA2000786A1 (fr) 1990-05-07
FI895261A0 (fi) 1989-11-06
DE68922577D1 (de) 1995-06-14

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