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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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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    • 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 Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (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 (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) DE122007000081I2 (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)

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WO1993010742A2 (en) * 1991-11-27 1993-06-10 Novo Nordisk A/S Chemical compounds, their preparation and use
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
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.
US6326362B1 (en) 1998-05-18 2001-12-04 Sepracor Inc. (-)-phosphonorisperidone and (-)-sulforisperidone compositions and methods
US6500833B1 (en) 1998-05-18 2002-12-31 Sepracor Inc. (+)-Hydroxyrisperidone compositions and methods
WO2000010572A1 (en) * 1998-08-18 2000-03-02 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
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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
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
DE07811307T1 (de) 2006-08-14 2008-07-31 Teva Pharmaceutical Industries Ltd. Amorphe und Kristlline Formen von 9-Hydroxyrisperidon (Paliperidon)
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)
US7820816B2 (en) 2006-08-23 2010-10-26 Teva Pharmaceutical Industries Ltd. Process for the synthesis of CMHTP and intermediates thereof
EP1924583A2 (en) * 2006-08-23 2008-05-28 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
KR101244185B1 (ko) * 2007-04-19 2013-03-25 유씬 리 정신 장애 치료용 신규 화합물, 그의 제조 방법 및 용도
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
CA2700803A1 (en) * 2007-10-09 2009-04-16 Rajendra Narayanrao Kankan Processes for the preparation of paliperidone and pharmaceutically acceptable salts thereof and intermediates for use in the processes
AR069621A1 (es) 2007-12-10 2010-02-03 Synthon Bv Sintesis de paliperidona
BRPI0905938A2 (pt) * 2008-02-05 2018-05-29 Watson Pharma Private Ltd processo para preparação de 3-(2 cloroetil)- 2- metil hidróxi- 4h-pirido [l, 2-a] pirimidina-4- ona, de 3- (2-cloroetil)-6,7,8,9- tetraidro 9- hidróxil-2-metil-4h-pirido[1,2-a]pirimidina-4-ona, de 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-il)-1-piperidinil]etil]-6,7,8,9-tetaidro-9-hidróxi-2-metil-4h-pirido[1,2-a]pirimidina-4-ona bruta, e processo para a purificação da paliperidona
EP2285804A4 (en) * 2008-04-21 2011-09-14 Glenmark Generics Ltd METHOD FOR MANUFACTURING 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
EP2318405A2 (en) * 2008-07-11 2011-05-11 Synthon B.V. Paliperidone ketone
EP2321311B1 (en) * 2008-07-11 2012-09-19 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
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Also Published As

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

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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