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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DK551989A (da
DK551989D0 (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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    • 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

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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
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
KR100354270B1 (ko) * 1993-11-19 2003-02-11 알커메스 컨트롤드 테라포이틱스 인코퍼레이티드 Ii 마이크로캡슐화된3-피페리디닐-치환된1,2-벤즈이속사졸및1,2-벤즈이소티아졸
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
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AU5489299A (en) 1998-08-18 2000-03-14 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
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
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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
DK2154138T3 (en) * 2007-04-19 2015-11-02 Youxin Li Novel compounds for the treatment of psychotic disorders, methods of 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
KR20100091959A (ko) * 2007-10-09 2010-08-19 시플라 리미티드 팔리페리돈 및 그의 약학적으로 허용가능한 염의 제조방법 및 상기 제조방법에 사용되는 중간체
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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
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
US20100010218A1 (en) * 2008-07-11 2010-01-14 Jiri Bartl 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
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Also Published As

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

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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