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DK169923B1 - 3-[[4-(1,2-benzisoxazol-3-yl)-1-piperidinyl]alkyl]-6,7,8,9-tetrahydro-2-alkyl-4H-pyrido[1,2-a]pyrimidin-4-on-forbindelser, fremgangsmåde til fremstilling deraf og antipsykotiske præparater indeholdende disse - Google Patents

3-[[4-(1,2-benzisoxazol-3-yl)-1-piperidinyl]alkyl]-6,7,8,9-tetrahydro-2-alkyl-4H-pyrido[1,2-a]pyrimidin-4-on-forbindelser, fremgangsmåde til fremstilling deraf og antipsykotiske præparater indeholdende disse Download PDF

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Publication number
DK169923B1
DK169923B1 DK551989A DK551989A DK169923B1 DK 169923 B1 DK169923 B1 DK 169923B1 DK 551989 A DK551989 A DK 551989A DK 551989 A DK551989 A DK 551989A DK 169923 B1 DK169923 B1 DK 169923B1
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Denmark
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formula
compounds
alkyl
alk
parts
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DK551989A
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Danish (da)
English (en)
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DK551989D0 (da
DK551989A (da
Inventor
Cornelus Gerardus Mari Janssen
Alfonsus Guilielmus Knaeps
Ludo Edmond Josephine Kennis
Jan Vandenberk
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Janssen Pharmaceutica Nv
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Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of DK551989D0 publication Critical patent/DK551989D0/da
Publication of DK551989A publication Critical patent/DK551989A/da
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Publication of DK169923B1 publication Critical patent/DK169923B1/da

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    • 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

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  • 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)
DK551989A 1988-11-07 1989-11-06 3-[[4-(1,2-benzisoxazol-3-yl)-1-piperidinyl]alkyl]-6,7,8,9-tetrahydro-2-alkyl-4H-pyrido[1,2-a]pyrimidin-4-on-forbindelser, fremgangsmåde til fremstilling deraf og antipsykotiske præparater indeholdende disse DK169923B1 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US26785788A 1988-11-07 1988-11-07
US26785788 1988-11-07

Publications (3)

Publication Number Publication Date
DK551989D0 DK551989D0 (da) 1989-11-06
DK551989A DK551989A (da) 1990-05-08
DK169923B1 true DK169923B1 (da) 1995-04-03

Family

ID=23020416

Family Applications (1)

Application Number Title Priority Date Filing Date
DK551989A DK169923B1 (da) 1988-11-07 1989-11-06 3-[[4-(1,2-benzisoxazol-3-yl)-1-piperidinyl]alkyl]-6,7,8,9-tetrahydro-2-alkyl-4H-pyrido[1,2-a]pyrimidin-4-on-forbindelser, fremgangsmåde til fremstilling deraf og antipsykotiske præparater indeholdende disse

Country Status (21)

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

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US5378714A (en) * 1991-11-27 1995-01-03 Novo Nordisk A/S Antipsychotic piperidine derivatives
NZ245260A (en) * 1991-11-27 1995-06-27 Novo Nordisk As Piperidine derivatives, preparation and pharmaceutical compositions thereof
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
DK0729357T3 (da) * 1993-11-19 2005-06-06 Janssen Pharmaceutica Nv Mikroindkapslede 1,2-benzazoler
JP3553951B2 (ja) * 1993-11-23 2004-08-11 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 新規な９−ヒドロキシ−ピリド［１，２−ａ］ピリミジン−４−オンエーテル誘導体
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.
WO1999059589A1 (en) * 1998-05-18 1999-11-25 Sepracor Inc. (-)-hydroxyrisperidone compositions and methods
AU3900499A (en) 1998-05-18 1999-12-06 Sepracor, Inc. (+)-hydroxyrisperidone 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
AU2003288017A1 (en) 2002-11-13 2004-06-03 Synthon B.V. Process for making risperidone and intermediates therefor
WO2006027370A1 (en) * 2004-09-09 2006-03-16 Janssen Pharmaceutica N.V. PREPARATION OF 9-HYDROXY-3- (2-HYDROXYETHYL) -2-METHYL-4H-PYRID0[1, 2-a] PYRIMIDIN-4-ONE AND CRYSTALS 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
EP2133352A3 (en) * 2006-08-14 2010-01-13 Teva Pharmaceutical Industries Ltd. Crystal form of 9-hydroxy-risperidone (paliperidone)
JP2009524685A (ja) * 2006-08-14 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 ９−ヒドロキシ−リスペリドン（パリペリドン）の結晶型
EP2133351A3 (en) * 2006-08-14 2010-01-13 Teva Pharmaceutical Industries Ltd. Crystal form 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
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
EP2154138B1 (en) * 2007-04-19 2015-08-19 Youxin Li Novel compounds for treatment of psychotic disorders, preparation methods 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
WO2009047499A2 (en) * 2007-10-09 2009-04-16 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
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
EP2303877B1 (en) 2008-05-29 2017-02-15 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
EP2318405A2 (en) 2008-07-11 2011-05-11 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
SI2275423T1 (sl) 2009-07-13 2012-06-29 Krka D.D., Novo Mesto Postopek za sintezo paliperidona
WO2011018246A2 (en) 2009-08-13 2011-02-17 Synthon B.V. Controlled release paliperidone composition
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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
NO3034079T3 (pt) 2010-11-15 2018-06-09
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
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Also Published As

Publication number Publication date
IL92208A0 (en) 1990-07-26
NL300298I2 (nl) 2008-03-03
ZA898436B (en) 1991-07-31
NO173015B (no) 1993-07-05
CY2007025I1 (el) 2009-11-04
ATE122349T1 (de) 1995-05-15
JPH02191276A (ja) 1990-07-27
ES2075036T3 (es) 1995-10-01
LU91362I2 (fr) 2007-11-12
CA2000786A1 (en) 1990-05-07
NO173015C (no) 1993-10-13
NO2007017I2 (no) 2010-01-25
NO2007017I1 (no) 2008-01-14
NL300298I1 (nl) 2007-12-03
NO894411D0 (no) 1989-11-06
IE893564L (en) 1990-05-07
FI92201B (fi) 1994-06-30
DE122007000081I2 (de) 2010-01-28
EP0368388A2 (en) 1990-05-16
AU614437B2 (en) 1991-08-29
EP0368388A3 (en) 1991-07-17
PT92206B (pt) 1995-07-06
AU4443689A (en) 1990-05-10
CY1926A (en) 1989-10-30
HK131696A (en) 1996-07-26
FI895261A0 (fi) 1989-11-06
EP0368388B1 (en) 1995-05-10
KR910009700A (ko) 1991-06-28
CL43432B (es) 2005-06-03
JP2758045B2 (ja) 1998-05-25
DK551989D0 (da) 1989-11-06
DE68922577D1 (de) 1995-06-14
PT92206A (pt) 1990-05-31
NZ231062A (en) 1991-09-25
FI92201C (fi) 1994-10-10
CY2007025I2 (el) 2009-11-04
DE122007000081I1 (de) 2008-02-28
IE66370B1 (en) 1995-12-27
DK551989A (da) 1990-05-08
DE68922577T2 (de) 1995-09-28
CA2000786C (en) 1999-01-26
KR0146053B1 (ko) 1998-08-17
NO894411L (no) 1990-05-08

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Legal Events

Date Code Title Description
B1 Patent granted (law 1993)
CTFF Application for supplementary protection certificate (spc) filed

Spc suppl protection certif: CA 2007 00071

Filing date: 20071219

Expiry date: 20141106

CTFG Supplementary protection certificate (spc) issued

Free format text: PRODUCT NAME: PALIPERIDON ((PLUS MINUS)-3-{2-[4-(6-FLUOR-1,2-BENZISOXAZOL-3-YL)PIPERIDINO]ETHYL}-6,7,8,9-TETRAHYDRO-9-HYDROXY-2-METHYL-4H-PYRIDO[1,2-A]PYRIMIDIN-4-ON)

Spc suppl protection certif: CA 2007 00071

Filing date: 20071219

PUP Patent expired