PL357382A1 - Pochodne pirymidyn-4-onu jako inhibitory LDL-PLA 2 - Google Patents

Pochodne pirymidyn-4-onu jako inhibitory LDL-PLA 2

Info

Publication number: PL357382A1
Authority: PL; Poland
Prior art keywords: pla2; ldl; pyrimidine; derivatives; lppla2
Prior art date: 2000-02-16

Application number

PL01357382A

Other languages

English (en)

Other versions

PL209824B1 (pl

Inventor

Deirdre Mary Bernadette Hickey

Robert John Ife

Colin Andrew Leach

Ivan Leo Pinto

Stephen Allan Smith

Steven James Stanway

Original Assignee

Smithkline Beecham P.L.C.

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.)

2000-02-16

Filing date

2001-02-13

Publication date

2004-07-26

2000-02-16 Priority claimed from GB0003636A external-priority patent/GB0003636D0/en

2001-01-19 Priority claimed from GB0101437A external-priority patent/GB0101437D0/en

2001-02-13 Application filed by Smithkline Beecham P.L.C. filed Critical Smithkline Beecham P.L.C.

2004-07-26 Publication of PL357382A1 publication Critical patent/PL357382A1/pl

2011-10-31 Publication of PL209824B1 publication Critical patent/PL209824B1/pl

Links

DNCYBUMDUBHIJZ-UHFFFAOYSA-N 1h-pyrimidin-6-one Chemical class O=C1C=CN=CN1 DNCYBUMDUBHIJZ-UHFFFAOYSA-N 0.000 title 1
201000001320 Atherosclerosis Diseases 0.000 abstract 1
102000004190 Enzymes Human genes 0.000 abstract 1
108090000790 Enzymes Proteins 0.000 abstract 1
239000003112 inhibitor Substances 0.000 abstract 1
VTGOHKSTWXHQJK-UHFFFAOYSA-N pyrimidin-2-ol Chemical class OC1=NC=CC=N1 VTGOHKSTWXHQJK-UHFFFAOYSA-N 0.000 abstract 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/56—One oxygen atom and one sulfur atom
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
- 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/60—Three or more oxygen or sulfur atoms
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Veterinary Medicine (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Diabetes (AREA)
Cardiology (AREA)
Heart & Thoracic Surgery (AREA)
Biomedical Technology (AREA)
Neurosurgery (AREA)
Hematology (AREA)
Obesity (AREA)
Neurology (AREA)
Rheumatology (AREA)
Hospice & Palliative Care (AREA)
Dermatology (AREA)
Vascular Medicine (AREA)
Urology & Nephrology (AREA)
Psychiatry (AREA)
Emergency Medicine (AREA)
Endocrinology (AREA)
Pain & Pain Management (AREA)
Immunology (AREA)
Orthopedic Medicine & Surgery (AREA)
Physical Education & Sports Medicine (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

PL357382A 2000-02-16 2001-02-13 1-(N-2-(dietyloamino)etylo)-N-(4-(4-trifluorometylo-fenylo)benzylo)aminokarbonylometylo)-2-(4-fluorobenzylo)tio-5,6-trimetylenopirymidyn-4-on, jego zastosowania i zawierająca go farmaceutyczna kompozycja PL209824B1 (pl)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
GB0003636A GB0003636D0 (en)	2000-02-16	2000-02-16	Novel compounds
GB0101437A GB0101437D0 (en)	2001-01-19	2001-01-19	Novel Compounds
PCT/EP2001/001515 WO2001060805A1 (en)	2000-02-16	2001-02-13	Pyrimidine-4-one derivatives as ldl-pla2 inhibitors

Publications (2)

Publication Number	Publication Date
PL357382A1 true PL357382A1 (pl)	2004-07-26
PL209824B1 PL209824B1 (pl)	2011-10-31

Family

ID=26243663

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
PL357382A PL209824B1 (pl)	2000-02-16	2001-02-13	1-(N-2-(dietyloamino)etylo)-N-(4-(4-trifluorometylo-fenylo)benzylo)aminokarbonylometylo)-2-(4-fluorobenzylo)tio-5,6-trimetylenopirymidyn-4-on, jego zastosowania i zawierająca go farmaceutyczna kompozycja

Country Status (31)

Country	Link
US (10)	US20020103213A1 (pl)
EP (2)	EP1263740B1 (pl)
JP (1)	JP4095804B2 (pl)
KR (1)	KR100781425B1 (pl)
CN (1)	CN1179952C (pl)
AR (1)	AR030190A1 (pl)
AT (2)	ATE333446T1 (pl)
AU (2)	AU2001235466B2 (pl)
BG (1)	BG66014B1 (pl)
BR (1)	BRPI0108396B1 (pl)
CA (1)	CA2400554C (pl)
CO (1)	CO5271661A1 (pl)
CY (2)	CY1105649T1 (pl)
CZ (1)	CZ304450B6 (pl)
DE (2)	DE60139429D1 (pl)
DK (2)	DK1263740T3 (pl)
ES (2)	ES2330552T3 (pl)
GC (1)	GC0000221A (pl)
HU (1)	HU229479B1 (pl)
IL (2)	IL151236A (pl)
MX (1)	MXPA02008062A (pl)
MY (1)	MY135732A (pl)
NO (1)	NO324691B1 (pl)
NZ (1)	NZ520752A (pl)
PL (1)	PL209824B1 (pl)
PT (2)	PT1263740E (pl)
SI (2)	SI1686119T1 (pl)
SK (1)	SK287296B6 (pl)
TW (1)	TW550259B (pl)
UA (1)	UA73762C2 (pl)
WO (1)	WO2001060805A1 (pl)

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GB0119793D0 (en) *	2001-08-14	2001-10-03	Smithkline Beecham Plc	Novel compounds
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US8962633B2 (en)	2007-05-11	2015-02-24	Thomas Jefferson University	Methods of treatment and prevention of metabolic bone diseases and disorders
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KR101861883B1 (ko) *	2010-12-06	2018-05-28	글락소 그룹 리미티드	Lp-PLA₂에 의해 매개되는 질환 또는 상태의 치료에 사용하기 위한 피리미디논 화합물
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BR112015017397A2 (pt)	2013-01-25	2017-07-11	Glaxosmithkline Ip Dev Ltd	compostos pirimidona bicíclica como inibidores de lp-pla2
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- 2001-02-13 WO PCT/EP2001/001515 patent/WO2001060805A1/en not_active Ceased
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Also Published As

Publication number	Publication date
SK287296B6 (sk)	2010-06-07
HK1053466A1 (en)	2003-10-24
CN1179952C (zh)	2004-12-15
KR20030011772A (ko)	2003-02-11
US7652019B2 (en)	2010-01-26
AR030190A1 (es)	2003-08-13
ATE333446T1 (de)	2006-08-15
JP4095804B2 (ja)	2008-06-04
US6649619B1 (en)	2003-11-18
JP2003523335A (ja)	2003-08-05
BG66014B1 (bg)	2010-10-29
BR0108396A (pt)	2003-03-11
IL181957A0 (en)	2009-02-11
SI1686119T1 (sl)	2009-12-31
US9266841B2 (en)	2016-02-23
US20090118313A1 (en)	2009-05-07
PT1263740E (pt)	2006-11-30
SK11772002A3 (sk)	2003-02-04
AU3546601A (en)	2001-08-27
MXPA02008062A (es)	2002-11-29
EP1263740B1 (en)	2006-07-19
EP1686119B1 (en)	2009-07-29
PT1686119E (pt)	2009-10-06
CY1109484T1 (el)	2014-08-13
EP1263740A1 (en)	2002-12-11
KR100781425B1 (ko)	2007-12-03
DE60121550T2 (de)	2007-06-21
US8871775B2 (en)	2014-10-28
HUP0204410A2 (en)	2003-05-28
US20090170877A1 (en)	2009-07-02
HU229479B1 (en)	2014-01-28
US20100144765A1 (en)	2010-06-10
NZ520752A (en)	2004-03-26
CA2400554C (en)	2009-04-07
US20120172378A1 (en)	2012-07-05
ATE437862T1 (de)	2009-08-15
US20040097525A1 (en)	2004-05-20
CY1105649T1 (el)	2010-12-22
CN1418199A (zh)	2003-05-14
NO20023828D0 (no)	2002-08-13
ES2267714T3 (es)	2007-03-16
TW550259B (en)	2003-09-01
MY135732A (en)	2008-06-30
NO324691B1 (no)	2007-12-03
US20070123549A1 (en)	2007-05-31
AU2001235466B2 (en)	2004-04-22
US20020103213A1 (en)	2002-08-01
CZ20022768A3 (cs)	2003-05-14
GC0000221A (en)	2006-03-29
NO20023828L (no)	2002-09-30
BG107034A (bg)	2003-04-30
US20150045375A1 (en)	2015-02-12
PL209824B1 (pl)	2011-10-31
UA73762C2 (uk)	2005-09-15
SI1263740T1 (sl)	2006-12-31
EP1686119A1 (en)	2006-08-02
HUP0204410A3 (en)	2003-07-28
US7153861B2 (en)	2006-12-26
IL151236A (en)	2009-02-11
ES2330552T3 (es)	2009-12-11
US7470694B2 (en)	2008-12-30
DE60121550D1 (de)	2006-08-31
DK1263740T3 (da)	2006-11-13
US7638520B2 (en)	2009-12-29
WO2001060805A1 (en)	2001-08-23
DK1686119T3 (da)	2009-11-09
CZ304450B6 (cs)	2014-05-14
US20070155762A1 (en)	2007-07-05
CO5271661A1 (es)	2003-04-30
BRPI0108396B1 (pt)	2015-05-19
CA2400554A1 (en)	2001-08-23
DE60139429D1 (de)	2009-09-10

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