BG94282A - 2,9-дизаместени-4н-пиридо/1,2,-а/пиримидин-4-они - Google Patents

2,9-дизаместени-4н-пиридо/1,2,-а/пиримидин-4-они

Info

Publication number
BG94282A
BG94282A BG094282A BG9428291A BG94282A BG 94282 A BG94282 A BG 94282A BG 094282 A BG094282 A BG 094282A BG 9428291 A BG9428291 A BG 9428291A BG 94282 A BG94282 A BG 94282A
Authority
BG
Bulgaria
Prior art keywords
4alkyl
methyl
hydroxyc1
furanyl
pyridinyl
Prior art date
Application number
BG094282A
Other languages
English (en)
Other versions
BG60394B1 (bg
Inventor
Ludo Edmond Kennis
Jan Vandenberk
Albertus Hendricus M.T. Heertum
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 BG94282A publication Critical patent/BG94282A/bg
Publication of BG60394B1 publication Critical patent/BG60394B1/bg

Links

Classifications

    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychiatry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurosurgery (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Electrochromic Elements, Electrophoresis, Or Variable Reflection Or Absorption Elements (AREA)

Abstract

Съединенията са силно действащи антагонисти на допамина и могат да се използват при лечението на пациенти, страдащи от остри психози. Те са с обща формула в която аlк е с1-4алкандиил, d е бицикличен хетероцикъл с формула в която r1 е с1-4алкил, хидроксис1-4алкил, карбоксалдехид, карбоксил, с1-10алкилкарбонилоксис1-4алкил; r2 водород или с1-4алкил; r3 е с1-4алкил, хидроксис1-4алкил или метил, заместен с фенил, 5-метил-2-фуранил или 3-пиридинил; r4 е с1-3алкил, фенил, 5-метил-2-фуранил или 3-пиридинил. Изобретението се отнася и до техните фармацевтично приемливи, присъединителни с киселина соли, до техните стереохимично изомерни форми, до методи за получаване на съединенията, както и на състави, които ги съдържат. 8 претенции
BG94282A 1990-04-19 1991-04-18 2,9-дизаместени-4н-пиридо/1,2,-а/пиримидин-4-они BG60394B1 (bg)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB909008850A GB9008850D0 (en) 1990-04-19 1990-04-19 Novel 2,9-disubstituted-4h-pyridol(1,2-a)pyrimidin-4-ones

Publications (2)

Publication Number Publication Date
BG94282A true BG94282A (bg) 1993-12-24
BG60394B1 BG60394B1 (bg) 1995-02-28

Family

ID=10674694

Family Applications (2)

Application Number Title Priority Date Filing Date
BG94282A BG60394B1 (bg) 1990-04-19 1991-04-18 2,9-дизаместени-4н-пиридо/1,2,-а/пиримидин-4-они
BG095241A BG95241A (bg) 1990-04-19 1991-09-30 Метод за получаване на 2,9-дизаместени-4н-пиридо/1.2-а/ пиримидин-4-они

Family Applications After (1)

Application Number Title Priority Date Filing Date
BG095241A BG95241A (bg) 1990-04-19 1991-09-30 Метод за получаване на 2,9-дизаместени-4н-пиридо/1.2-а/ пиримидин-4-они

Country Status (26)

Country Link
US (1) US5482943A (bg)
EP (1) EP0453042B1 (bg)
JP (1) JP3216889B2 (bg)
KR (1) KR100190297B1 (bg)
CN (1) CN1027506C (bg)
AT (1) ATE186301T1 (bg)
AU (1) AU636969B2 (bg)
BG (2) BG60394B1 (bg)
CA (1) CA2040086C (bg)
CZ (1) CZ281135B6 (bg)
DE (1) DE69131759T2 (bg)
DK (1) DK0453042T3 (bg)
ES (1) ES2140381T3 (bg)
FI (1) FI96206C (bg)
GB (1) GB9008850D0 (bg)
GR (1) GR3032122T3 (bg)
HU (1) HUT57763A (bg)
IE (1) IE911301A1 (bg)
IL (1) IL97892A (bg)
NO (1) NO176840C (bg)
NZ (1) NZ237713A (bg)
PL (2) PL169744B1 (bg)
PT (1) PT97395B (bg)
RU (1) RU2037495C1 (bg)
SK (1) SK279005B6 (bg)
ZA (1) ZA912913B (bg)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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.
PT672043E (pt) 1992-07-13 2001-11-30 Janssen Pharmaceutica Nv Novos derivados de 4-(3-benzofuranil)piperidinilo e 4-(3-benzotienil)piperidinilo e composicoes farmaceuticas que os contem
US5688799A (en) * 1993-11-23 1997-11-18 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.
JP3274579B2 (ja) * 1995-01-12 2002-04-15 住友製薬株式会社 脳血管障害に伴う精神症候治療剤
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.
HU227118B1 (en) * 2001-11-13 2010-07-28 Egis Gyogyszergyar Nyilvanosan Process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzizoxazol-3-yl)-1-piperidinyl]-ethyl}-6,7,8,9-tetrahydro-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one
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.
WO2004009591A1 (en) * 2002-07-22 2004-01-29 Aurobindo Pharma Ltd. A process for the preparation of antipsychotic risperidone
WO2004020439A2 (en) * 2002-08-30 2004-03-11 Sunil Sadanand Nadkarni Improved process for preparation of risperidone
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
WO2004094415A1 (en) * 2003-04-22 2004-11-04 Synthon B.V. Risperidone monohydrochloride
HUP0401379A3 (en) * 2004-07-08 2006-04-28 Richter Gedeon Vegyeszet Process for the preparation of risperidon
HUP0402163A2 (en) * 2004-10-25 2006-05-29 Richter Gedeon Vegyeszet Process for the preparation of risperidone
EP1690540A1 (en) * 2005-02-15 2006-08-16 Neuro3D Composition comprising ocaperidone
EP1695973A1 (en) * 2005-02-24 2006-08-30 Neuro3D Ocaperidone salt and pharmaceutical compositions containing the same
JO2769B1 (en) * 2005-10-26 2014-03-15 جانسين فارماسوتيكا ان. في Rapid decomposition of physiologically antagonistic agents of the 2-dopamine receptor
WO2009077551A1 (en) * 2007-12-18 2009-06-25 Janssen Pharmaceutica Nv Process for preparing risperidone
WO2023135528A1 (en) 2022-01-11 2023-07-20 Suven Life Sciences Limited Heteroalicyclic derivatives and their use in the treatment of cns disorders

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4485107A (en) * 1982-11-01 1984-11-27 Janssen Pharmaceutica N.V. [[Bis(aryl)methylene]-1-piperidinyl]alkyl-pyrimidinones
US4804663A (en) * 1985-03-27 1989-02-14 Janssen Pharmaceutica N.V. 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
NZ223654A (en) * 1987-03-09 1990-03-27 Janssen Pharmaceutica Nv 1-alkyl-substituted-benzimidazole-4-piperidinamines and pharmaceutical compositions
US4777252A (en) * 1987-08-13 1988-10-11 E. R. Squibb & Sons, Inc. 2-oxo-1-[[(substituted sulfonyl)amino]-carbonyl]azetidines
CA2000786C (en) * 1988-11-07 1999-01-26 Cornelus G. M. Janssen 3-piperidinyl-1,2-benzisoxazoles
GB8900382D0 (en) * 1989-01-09 1989-03-08 Janssen Pharmaceutica Nv 2-aminopyrimidinone derivatives

Also Published As

Publication number Publication date
HUT57763A (en) 1991-12-30
PL289935A1 (en) 1992-04-06
SK279005B6 (sk) 1998-05-06
AU636969B2 (en) 1993-05-13
KR910018380A (ko) 1991-11-30
CN1027506C (zh) 1995-01-25
BG95241A (bg) 1993-12-24
PL169744B1 (pl) 1996-08-30
NO176840C (no) 1995-06-07
JP3216889B2 (ja) 2001-10-09
GR3032122T3 (en) 2000-04-27
CA2040086A1 (en) 1991-10-20
DE69131759D1 (de) 1999-12-09
CS9101099A2 (en) 1991-11-12
FI96206B (fi) 1996-02-15
CA2040086C (en) 2003-12-30
NZ237713A (en) 1992-09-25
IE911301A1 (en) 1991-10-23
NO176840B (no) 1995-02-27
HU911301D0 (en) 1991-10-28
AU7436691A (en) 1991-10-24
IL97892A0 (en) 1992-06-21
BG60394B1 (bg) 1995-02-28
PT97395B (pt) 1998-08-31
PT97395A (pt) 1992-01-31
CN1055929A (zh) 1991-11-06
FI96206C (fi) 1996-05-27
CZ281135B6 (cs) 1996-06-12
JPH04234882A (ja) 1992-08-24
ATE186301T1 (de) 1999-11-15
PL169740B1 (pl) 1996-08-30
EP0453042B1 (en) 1999-11-03
KR100190297B1 (ko) 1999-06-01
NO911525D0 (no) 1991-04-18
FI911885A0 (fi) 1991-04-18
EP0453042A1 (en) 1991-10-23
US5482943A (en) 1996-01-09
ES2140381T3 (es) 2000-03-01
GB9008850D0 (en) 1990-06-13
DK0453042T3 (da) 2000-04-25
RU2037495C1 (ru) 1995-06-19
IL97892A (en) 1995-03-30
ZA912913B (en) 1992-12-30
DE69131759T2 (de) 2000-06-21
FI911885A (fi) 1991-10-20
NO911525L (no) 1991-10-21

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