AU7436691A - Creación de Inventos y Patentes con Inteligencia Artificial

AU7436691A – Novel 2,9-disubstituted-4H-pyrido(1,2-a)pyrimidin-4-ones
– Google Patents

AU7436691A – Novel 2,9-disubstituted-4H-pyrido(1,2-a)pyrimidin-4-ones
– Google Patents
Novel 2,9-disubstituted-4H-pyrido(1,2-a)pyrimidin-4-ones

Info

Publication number
AU7436691A

AU7436691A
AU74366/91A
AU7436691A
AU7436691A
AU 7436691 A
AU7436691 A
AU 7436691A
AU 74366/91 A
AU74366/91 A
AU 74366/91A
AU 7436691 A
AU7436691 A
AU 7436691A
AU 7436691 A
AU7436691 A
AU 7436691A
Authority
AU
Australia
Prior art keywords
4alkyl
compounds
methyl
hydroxyc1
furanyl
Prior art date
1990-04-19
Legal status (The legal status 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 status listed.)

Granted

Application number
AU74366/91A
Other versions

AU636969B2
(en

Inventor
Ludo Edmond Josephine Kennis
Albertus Hendricus Maria Theresia Van Heertum
Jan Vandenberk
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Janssen Pharmaceutica NV

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
1991-04-11
Publication date
1991-10-24

1991-04-11
Application filed by Janssen Pharmaceutica NV
filed
Critical
Janssen Pharmaceutica NV

1991-10-24
Publication of AU7436691A
publication
Critical
patent/AU7436691A/en

1993-05-13
Application granted
granted
Critical

1993-05-13
Publication of AU636969B2
publication
Critical
patent/AU636969B2/en

2011-04-11
Anticipated expiration
legal-status
Critical

Status
Expired
legal-status
Critical
Current

Links

Espacenet

Global Dossier

Discuss

-1
2,9-disubstituted-4H-pyrido(1,2-a)pyrimidin-4-ones
Chemical class

0.000
title
abstract
3

150000001875
compounds
Chemical class

0.000
abstract
4

125000004178
(C1-C4) alkyl group
Chemical group

0.000
abstract
3

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

Abstract

Compounds of formula pharmaceutically acceptable acid addition salts thereof, and stereochemically isomeric forms thereof, wherein Alk is C1-4alkanediyl, and D is wherein R<1> represents C1-4alkyl, hydroxyC1-4alkyl, carboxaldehyde, carboxyl, C1-10alkylcarbonyloxyC1-4alkyl; each R<2> represents hydrogen or C1-4alkyl; R<3> represents C1-4alkyl, hydroxyC1-4alkyl or methyl substituted with phenyl, 5-methyl-2-furanyl or 3-pyridinyl; and R<4> represents C1-3alkyl, phenyl, 5-methyl-2-furanyl or 3-pyridinyl, which compounds are potent antagonists of dopamine and are therapeutically useful in treating patients suffering from acute psychoses. Compositions containing these compounds as active ingredient and processes of preparing said compounds and compositions.

AU74366/91A
1990-04-19
1991-04-11
Novel 2,9-disubstituted-4h-pyrido(1,2-a)pyrimidin-4-ones

Expired

AU636969B2
(en)

Applications Claiming Priority (2)

Application Number
Priority Date
Filing Date
Title

GB9008850

1990-04-19

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

AU7436691A
true

AU7436691A
(en)

1991-10-24

AU636969B2

AU636969B2
(en)

1993-05-13

Family
ID=10674694
Family Applications (1)

Application Number
Title
Priority Date
Filing Date

AU74366/91A
Expired

AU636969B2
(en)

1990-04-19
1991-04-11
Novel 2,9-disubstituted-4h-pyrido(1,2-a)pyrimidin-4-ones

Country Status (26)

Country
Link

US
(1)

US5482943A
(en)

EP
(1)

EP0453042B1
(en)

JP
(1)

JP3216889B2
(en)

KR
(1)

KR100190297B1
(en)

CN
(1)

CN1027506C
(en)

AT
(1)

ATE186301T1
(en)

AU
(1)

AU636969B2
(en)

BG
(1)

BG60394B1
(en)

CA
(1)

CA2040086C
(en)

CZ
(1)

CZ281135B6
(en)

DE
(1)

DE69131759T2
(en)

DK
(1)

DK0453042T3
(en)

ES
(1)

ES2140381T3
(en)

FI
(1)

FI96206C
(en)

GB
(1)

GB9008850D0
(en)

GR
(1)

GR3032122T3
(en)

HU
(1)

HUT57763A
(en)

IE
(1)

IE911301A1
(en)

IL
(1)

IL97892A
(en)

NO
(1)

NO176840C
(en)

NZ
(1)

NZ237713A
(en)

PL
(2)

PL169740B1
(en)

PT
(1)

PT97395B
(en)

RU
(1)

RU2037495C1
(en)

SK
(1)

SK279005B6
(en)

ZA
(1)

ZA912913B
(en)

Cited By (1)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

AU687940B2
(en)

1993-11-23
1998-03-05
Janssen Pharmaceutica N.V.
Novel 9-hydroxy-pyrido(1,2-a)pyrimidin-4-one ether derivatives

Families Citing this family (19)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

ES2050069B1
(en)

1992-07-10
1994-12-16
Vita Invest Sa

PROCEDURE FOR OBTAINING 3- (2- (4- (6-FLUORO-1,2-BENZISOXAZOL-3-IL) PIPERIDINO) ETIL) -2-METHYL-6,7,8,9-TETRAHIDRO-4H-PIRIDO (1,2-A) PIRIMIDIN-4-ONA.

DK0672043T3
(en)

1992-07-13
2001-08-27
Janssen Pharmaceutica Nv

New 4- (3-benzofuranyl) -piperidinyl and 4- (3-benzothienyl) -piperidinyl derivatives and pharmaceutical compositions containing them

ES2085234B1
(en)

1994-02-24
1997-01-16
Vita Invest Sa

ACTIVE AGENT ON THE CENTRAL NERVOUS SYSTEM, PROCEDURE FOR ITS PREPARATION AND PHARMACEUTICAL COMPOSITIONS THAT CONTAIN IT.

JP3274579B2
(en)

1995-01-12
2002-04-15
住友製薬株式会社

Agent for treating psychiatric symptoms associated with cerebrovascular disorders

ES2141671B1
(en)

1997-12-26
2001-01-01
Vita Invest Sa

ACTIVE PYRIMIDINIC COMPOUND ON THE CENTRAL NERVOUS SYSTEM, PROCEDURE FOR THE PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING IT.

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
(en)

2002-03-05
2005-03-16
Ferrer Internacional,S.A

PROCEDURE FOR OBTAINING THE 3- (2- (4- (6-FLUORO-BENZO (D) ISOXAZOL-3-IL) PIPERIDIN-1-IL) -ETIL) -2-METHYL-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
(en)

2002-09-18
2004-03-24
주식회사 대웅
2-(2-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-3-yl)acetaldehyde and preparation process of the same

EP1560814A1
(en)

2002-11-13
2005-08-10
Synthon B.V.
Process for making risperidone and intermediates therefor

EP1615923A1
(en)

2003-04-22
2006-01-18
Synthon B.V.
Risperidone monohydrochloride

HU0401379A3
(en)

2004-07-08
2006-04-28
Richter Gedeon Vegyeszet
Process for the preparation of risperidon

HU0402163A2
(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
Fast Dissociting Dopamine 2 Receptor Antagonists

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
EP
EP91200897A
patent/EP0453042B1/en
not_active
Expired – Lifetime

1991-04-16
DK
DK91200897T
patent/DK0453042T3/en
active

1991-04-16
DE
DE69131759T
patent/DE69131759T2/en
not_active
Expired – Lifetime

1991-04-16
AT
AT91200897T
patent/ATE186301T1/en
not_active
IP Right Cessation

1991-04-16
ES
ES91200897T
patent/ES2140381T3/en
not_active
Expired – Lifetime

1991-04-16
JP
JP10968691A
patent/JP3216889B2/en
not_active
Expired – Lifetime

1991-04-17
IL
IL9789291A
patent/IL97892A/en
not_active
IP Right Cessation

1991-04-17
KR
KR1019910006108A
patent/KR100190297B1/en
not_active
IP Right Cessation

1991-04-18
RU
SU914895183A
patent/RU2037495C1/en
active

1991-04-18
BG
BG94282A
patent/BG60394B1/en
unknown

1991-04-18
IE
IE130191A
patent/IE911301A1/en
not_active
IP Right Cessation

1991-04-18
NO
NO911525A
patent/NO176840C/en
not_active
IP Right Cessation

1991-04-18
PT
PT97395A
patent/PT97395B/en
not_active
IP Right Cessation

1991-04-18
FI
FI911885A
patent/FI96206C/en
active

1991-04-18
PL
PL91289935A
patent/PL169740B1/en
unknown

1991-04-18
ZA
ZA912913A
patent/ZA912913B/en
unknown

1991-04-18
PL
PL91312561A
patent/PL169744B1/en
unknown

1991-04-18
CZ
CS911099A
patent/CZ281135B6/en
not_active
IP Right Cessation

1991-04-18
SK
SK1099-91A
patent/SK279005B6/en
not_active
IP Right Cessation

1991-04-19
CN
CN91102516A
patent/CN1027506C/en
not_active
Expired – Lifetime

1991-04-19
HU
HU911301A
patent/HUT57763A/en
unknown

1999

1999-12-14
GR
GR990403201T
patent/GR3032122T3/en
unknown

Cited By (1)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

AU687940B2
(en)

1993-11-23
1998-03-05
Janssen Pharmaceutica N.V.
Novel 9-hydroxy-pyrido(1,2-a)pyrimidin-4-one ether derivatives

Also Published As

Publication number
Publication date

JP3216889B2
(en)

2001-10-09

NO911525D0
(en)

1991-04-18

PL169740B1
(en)

1996-08-30

RU2037495C1
(en)

1995-06-19

EP0453042B1
(en)

1999-11-03

GR3032122T3
(en)

2000-04-27

CS9101099A2
(en)

1991-11-12

PT97395A
(en)

1992-01-31

HU911301D0
(en)

1991-10-28

CZ281135B6
(en)

1996-06-12

NZ237713A
(en)

1992-09-25

ES2140381T3
(en)

2000-03-01

AU636969B2
(en)

1993-05-13

CN1027506C
(en)

1995-01-25

ZA912913B
(en)

1992-12-30

DE69131759T2
(en)

2000-06-21

IL97892A
(en)

1995-03-30

FI911885A
(en)

1991-10-20

ATE186301T1
(en)

1999-11-15

FI96206B
(en)

1996-02-15

DE69131759D1
(en)

1999-12-09

KR910018380A
(en)

1991-11-30

CA2040086A1
(en)

1991-10-20

GB9008850D0
(en)

1990-06-13

HUT57763A
(en)

1991-12-30

JPH04234882A
(en)

1992-08-24

NO176840B
(en)

1995-02-27

PT97395B
(en)

1998-08-31

CA2040086C
(en)

2003-12-30

DK0453042T3
(en)

2000-04-25

EP0453042A1
(en)

1991-10-23

IE911301A1
(en)

1991-10-23

BG60394B1
(en)

1995-02-28

FI96206C
(en)

1996-05-27

NO176840C
(en)

1995-06-07

IL97892A0
(en)

1992-06-21

KR100190297B1
(en)

1999-06-01

PL169744B1
(en)

1996-08-30

PL289935A1
(en)

1992-04-06

SK279005B6
(en)

1998-05-06

NO911525L
(en)

1991-10-21

US5482943A
(en)

1996-01-09

FI911885A0
(en)

1991-04-18

CN1055929A
(en)

1991-11-06

Información de contacto