NO2007017I2 - 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) - Google Patents

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)

Info

Publication number
NO2007017I2
NO2007017I2 NO2007017C NO2007017C NO2007017I2 NO 2007017 I2 NO2007017 I2 NO 2007017I2 NO 2007017 C NO2007017 C NO 2007017C NO 2007017 C NO2007017 C NO 2007017C NO 2007017 I2 NO2007017 I2 NO 2007017I2
Authority
NO
Norway
Prior art keywords
piperidinyl
hydroxy
palperidone
pyridol
benzoxazol
Prior art date
Application number
NO2007017C
Other languages
English (en)
Other versions
NO2007017I1 (no
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 NO2007017I1 publication Critical patent/NO2007017I1/no
Publication of NO2007017I2 publication Critical patent/NO2007017I2/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

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)
NO2007017C 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) NO2007017I2 (no)

Applications Claiming Priority (1)

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

Publications (2)

Publication Number Publication Date
NO2007017I1 NO2007017I1 (no) 2008-01-14
NO2007017I2 true NO2007017I2 (no) 2010-01-25

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 Before (1)

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

Country Status (21)

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

Families Citing this family (61)

* 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
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
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
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
ES2137486T3 (es) * 1993-11-23 1999-12-16 Janssen Pharmaceutica Nv Derivados de 9-hidroxi-pirido(1,2-a)pirimidin-4-ona-eter.
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
EP1791839B1 (en) 2004-09-09 2015-06-10 Janssen Pharmaceutica NV Preparation of 9-hydroxy-3-(2-hydroxyethyl)-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one and crystalls thereof
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
EP2133351A3 (en) * 2006-08-14 2010-01-13 Teva Pharmaceutical Industries Ltd. Crystal form of 9-hydroxy-risperidone (paliperidone)
EP2133352A3 (en) * 2006-08-14 2010-01-13 Teva Pharmaceutical Industries Ltd. Crystal form of 9-hydroxy-risperidone (paliperidone)
US20080177067A1 (en) * 2006-08-14 2008-07-24 Ben-Zion Dolitzky Crystal forms of 9-hydroxy-risperidone (paliperidone)
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 (en) * 2007-01-08 2008-07-24 Actavis Group Ptc Ehf An improved process for preparation of 9-hydroxy-3-(2-chloroethyl)- 2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one hydrochloride
JP5315336B2 (ja) * 2007-04-19 2013-10-16 又欣 李 精神疾患治療用の新規化合物とその調剤及び使用
WO2009010988A1 (en) * 2007-07-19 2009-01-22 Natco Pharma Limited An improved, industrially viable process for the preparation of high purity paliperidone
WO2009015828A1 (en) * 2007-07-27 2009-02-05 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
NZ584370A (en) * 2007-10-09 2011-04-29 Cipla Ltd 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
US20100311969A1 (en) * 2008-02-05 2010-12-09 Watson Pharma Private Limited 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
EP2321311B1 (en) * 2008-07-11 2012-09-19 Synthon B.V. Synthesis of paliperidone
WO2010003703A2 (en) * 2008-07-11 2010-01-14 Synthon B.V. 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
EP3034079B1 (en) 2010-11-15 2018-01-10 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
US20140206667A1 (en) 2012-11-14 2014-07-24 Michela Gallagher Methods and compositions for treating schizophrenia
EP3083569B1 (en) 2013-12-20 2022-01-26 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
US20180170941A1 (en) 2016-12-19 2018-06-21 Agenebio, Inc. Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment
US11505555B2 (en) 2016-12-19 2022-11-22 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
US11414425B2 (en) 2018-06-19 2022-08-16 Agenebio, Inc. Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment
WO2024039886A1 (en) 2022-08-19 2024-02-22 Agenebio, Inc. Benzazepine derivatives, compositions, and methods for treating cognitive impairment
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
CA2000786A1 (en) 1990-05-07
CY2007025I1 (el) 2009-11-04
IE66370B1 (en) 1995-12-27
NZ231062A (en) 1991-09-25
IL92208A0 (en) 1990-07-26
NO894411L (no) 1990-05-08
CY1926A (en) 1989-10-30
DK551989D0 (da) 1989-11-06
CA2000786C (en) 1999-01-26
NO894411D0 (no) 1989-11-06
FI895261A0 (fi) 1989-11-06
FI92201C (fi) 1994-10-10
EP0368388A3 (en) 1991-07-17
KR0146053B1 (ko) 1998-08-17
JPH02191276A (ja) 1990-07-27
ZA898436B (en) 1991-07-31
EP0368388B1 (en) 1995-05-10
FI92201B (fi) 1994-06-30
LU91362I2 (fr) 2007-11-12
KR910009700A (ko) 1991-06-28
ES2075036T3 (es) 1995-10-01
DK169923B1 (da) 1995-04-03
DE122007000081I2 (de) 2010-01-28
NL300298I2 (nl) 2008-03-03
NO173015B (no) 1993-07-05
EP0368388A2 (en) 1990-05-16
NO173015C (no) 1993-10-13
JP2758045B2 (ja) 1998-05-25
DE122007000081I1 (de) 2008-02-28
PT92206B (pt) 1995-07-06
HK131696A (en) 1996-07-26
AU4443689A (en) 1990-05-10
PT92206A (pt) 1990-05-31
DE68922577T2 (de) 1995-09-28
NO2007017I1 (no) 2008-01-14
NL300298I1 (nl) 2007-12-03
DE68922577D1 (de) 1995-06-14
AU614437B2 (en) 1991-08-29
DK551989A (da) 1990-05-08
ATE122349T1 (de) 1995-05-15
CY2007025I2 (el) 2009-11-04
CL43432B (es) 2005-06-03
IE893564L (en) 1990-05-07

Similar Documents

Publication Publication Date Title
NO2007017I2 (no) 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)
FI900085A0 (fi) Menetelmä terapeuttisesti käyttökelpoisten N-(pyrimidin- ja kondensoitu pyrimidin-4-oni)etyyli-piperidiini- ja piperatsiinijohdannaisten valmistamiseksi
EP0206415A3 (en) (4-piperidinylmethyl and -hetero)purines
EP0151824A3 (en) N-(4-piperidinyl) bicyclic condesed 2-imidazolamine derivatives
NO176051C (no) Analogifremgangsmåte for fremstilling av terapeutisk aktive 3-piperazinylbenzazol-derivater
JPS6425776A (en) Piperidine derivative
NO176608C (no) Analogifremgangsmåte for fremstilling av terapeutisk aktive 3-piperidinylindazol-derivater