ATE186301T1 - An den positionen 2 und 9 substituierte 4h-pyrido-(1,2-a)pyrimidin-4-one - Google Patents

An den positionen 2 und 9 substituierte 4h-pyrido-(1,2-a)pyrimidin-4-one

Info

Publication number: ATE186301T1
Authority: AT; Austria
Prior art keywords: 4alkyl; compounds; methyl; substituted; hydroxyc1
Prior art date: 1990-04-19

Application number

AT91200897T

Other languages

English (en)

Inventor

Ludo Edmond Josephine Kennis

Jan Vandenberk

Heertum Albertus Hendricus Van

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.)

1990-04-19

Filing date

1991-04-16

Publication date

1999-11-15

1991-04-16 Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv

1999-11-15 Application granted granted Critical

1999-11-15 Publication of ATE186301T1 publication Critical patent/ATE186301T1/de

Links

NYJWYCAHJRGKMI-UHFFFAOYSA-N pyrido[1,2-a]pyrimidin-4-one Chemical group C1=CC=CN2C(=O)C=CN=C21 NYJWYCAHJRGKMI-UHFFFAOYSA-N 0.000 title 1
150000001875 compounds Chemical class 0.000 abstract 4
125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 3
-1 5-methyl-2-furanyl Chemical group 0.000 abstract 2
KPCZJLGGXRGYIE-UHFFFAOYSA-N [C]1=CC=CN=C1 Chemical group [C]1=CC=CN=C1 KPCZJLGGXRGYIE-UHFFFAOYSA-N 0.000 abstract 2
VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 abstract 2
239000000203 mixture Substances 0.000 abstract 2
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
MBVFRSJFKMJRHA-UHFFFAOYSA-N 4-fluoro-1-benzofuran-7-carbaldehyde Chemical compound FC1=CC=C(C=O)C2=C1C=CO2 MBVFRSJFKMJRHA-UHFFFAOYSA-N 0.000 abstract 1
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
208000028017 Psychotic disease Diseases 0.000 abstract 1
239000002253 acid Substances 0.000 abstract 1
239000004480 active ingredient Substances 0.000 abstract 1
230000001154 acute effect Effects 0.000 abstract 1
239000005557 antagonist Substances 0.000 abstract 1
125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
229960003638 dopamine Drugs 0.000 abstract 1
229910052739 hydrogen Inorganic materials 0.000 abstract 1
239000001257 hydrogen Substances 0.000 abstract 1
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
230000003389 potentiating effect Effects 0.000 abstract 1
150000003839 salts Chemical class 0.000 abstract 1

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

AT91200897T 1990-04-19 1991-04-16 An den positionen 2 und 9 substituierte 4h-pyrido-(1,2-a)pyrimidin-4-one ATE186301T1 (de)

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 (1)

Publication Number	Publication Date
ATE186301T1 true ATE186301T1 (de)	1999-11-15

Family

ID=10674694

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
AT91200897T ATE186301T1 (de)	1990-04-19	1991-04-16	An den positionen 2 und 9 substituierte 4h-pyrido-(1,2-a)pyrimidin-4-one

Country Status (26)

Country	Link
US (1)	US5482943A (de)
EP (1)	EP0453042B1 (de)
JP (1)	JP3216889B2 (de)
KR (1)	KR100190297B1 (de)
CN (1)	CN1027506C (de)
AT (1)	ATE186301T1 (de)
AU (1)	AU636969B2 (de)
BG (1)	BG60394B1 (de)
CA (1)	CA2040086C (de)
CZ (1)	CZ281135B6 (de)
DE (1)	DE69131759T2 (de)
DK (1)	DK0453042T3 (de)
ES (1)	ES2140381T3 (de)
FI (1)	FI96206C (de)
GB (1)	GB9008850D0 (de)
GR (1)	GR3032122T3 (de)
HU (1)	HUT57763A (de)
IE (1)	IE911301A1 (de)
IL (1)	IL97892A (de)
NO (1)	NO176840C (de)
NZ (1)	NZ237713A (de)
PL (2)	PL169740B1 (de)
PT (1)	PT97395B (de)
RU (1)	RU2037495C1 (de)
SK (1)	SK279005B6 (de)
ZA (1)	ZA912913B (de)

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.
NZ254113A (en)	1992-07-13	1995-08-28	Janssen Pharmaceutica Nv	Fused piperidine derivatives and medicaments
EP0730594B1 (de) *	1993-11-23	1999-09-08	Janssen Pharmaceutica N.V.	9-HYDROXY-PYRIDO [1,2-a] PYRIMIDIN-4-ON-ETHER-DERIVATE
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 (de)	2002-11-13	2005-08-10	Synthon B.V.	Verfahren zur herstellung von risperidon und zwischenprodukte
WO2004094414A1 (en) *	2003-04-22	2004-11-04	Synthon B.V.	Water soluble salts of risperidone
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 (de) *	2005-02-15	2006-08-16	Neuro3D	Zusammensetzung enthaltend Ocaperidon
EP1695973A1 (de) *	2005-02-24	2006-08-30	Neuro3D	Ocaperidonsalz und dieser enthaltende pharmazeutische Zubereitung
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

1990
- 1990-04-19 GB GB909008850A patent/GB9008850D0/en active Pending
1991
- 1991-03-28 US US07/676,681 patent/US5482943A/en not_active Expired - Lifetime
- 1991-04-05 NZ NZ237713A patent/NZ237713A/en unknown
- 1991-04-09 CA CA002040086A patent/CA2040086C/en not_active Expired - Lifetime
- 1991-04-11 AU AU74366/91A patent/AU636969B2/en not_active Expired
- 1991-04-16 ES ES91200897T patent/ES2140381T3/es not_active Expired - Lifetime
- 1991-04-16 AT AT91200897T patent/ATE186301T1/de not_active IP Right Cessation
- 1991-04-16 EP EP91200897A patent/EP0453042B1/de not_active Expired - Lifetime
- 1991-04-16 JP JP10968691A patent/JP3216889B2/ja not_active Expired - Lifetime
- 1991-04-16 DE DE69131759T patent/DE69131759T2/de not_active Expired - Lifetime
- 1991-04-16 DK DK91200897T patent/DK0453042T3/da active
- 1991-04-17 KR KR1019910006108A patent/KR100190297B1/ko not_active IP Right Cessation
- 1991-04-17 IL IL9789291A patent/IL97892A/en not_active IP Right Cessation
- 1991-04-18 NO NO911525A patent/NO176840C/no not_active IP Right Cessation
- 1991-04-18 PT PT97395A patent/PT97395B/pt not_active IP Right Cessation
- 1991-04-18 FI FI911885A patent/FI96206C/fi active
- 1991-04-18 PL PL91289935A patent/PL169740B1/pl unknown
- 1991-04-18 RU SU914895183A patent/RU2037495C1/ru active
- 1991-04-18 IE IE130191A patent/IE911301A1/en not_active IP Right Cessation
- 1991-04-18 ZA ZA912913A patent/ZA912913B/xx unknown
- 1991-04-18 CZ CS911099A patent/CZ281135B6/cs not_active IP Right Cessation
- 1991-04-18 BG BG94282A patent/BG60394B1/bg unknown
- 1991-04-18 SK SK1099-91A patent/SK279005B6/sk not_active IP Right Cessation
- 1991-04-18 PL PL91312561A patent/PL169744B1/pl unknown
- 1991-04-19 CN CN91102516A patent/CN1027506C/zh not_active Expired - Lifetime
- 1991-04-19 HU HU911301A patent/HUT57763A/hu unknown
1999
- 1999-12-14 GR GR990403201T patent/GR3032122T3/el unknown

Also Published As

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

Legal Events

Date	Code	Title	Description
2000-05-15	UEP	Publication of translation of european patent specification
2011-07-15	EELA	Cancelled due to lapse of time

Publication	Publication Date	Title
ATE186301T1 (de)	1999-11-15	An den positionen 2 und 9 substituierte 4h-pyrido-(1,2-a)pyrimidin-4-one
DK0482208T3 (da)	2000-09-18	Pyridazinonderivat
NO882036L (no)	1988-11-14	Fremgangsmaate for fremstilling av terapeutisk aktive heterocykliske ketoner.
FI900085A0 (fi)	1990-01-08	Menetelmä terapeuttisesti käyttökelpoisten N-(pyrimidin- ja kondensoitu pyrimidin-4-oni)etyyli-piperidiini- ja piperatsiinijohdannaisten valmistamiseksi
PH25504A (en)	1991-07-24	Novel substituted n-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides pharmaceutical composition containing said compound, method of use thereof
NO873125D0 (no)	1987-07-27	Fremgangsmaate for fremstilling av antibakterielle forbindelser.
NO302821B1 (no)	1998-04-27	Aminobenzosyrederivat, preparat omfattende derivatet og anvendelse av derivatet
NO176608C (no)	1995-05-03	Analogifremgangsmåte for fremstilling av terapeutisk aktive 3-piperidinylindazol-derivater
DE3884878T2 (de)	1994-02-17	Uricosuretische Zusammensetzung.