HK1053466A1 - Pyrimidine-4-one derivative as ldl-pla2 inhibitor - Google Patents

Pyrimidine-4-one derivative as ldl-pla2 inhibitor

Info

Publication number
HK1053466A1
HK1053466A1 HK03104052A HK03104052A HK1053466A1 HK 1053466 A1 HK1053466 A1 HK 1053466A1 HK 03104052 A HK03104052 A HK 03104052A HK 03104052 A HK03104052 A HK 03104052A HK 1053466 A1 HK1053466 A1 HK 1053466A1
Authority
HK
Hong Kong
Prior art keywords
ldl
pyrimidine
derivative
pla2 inhibitor
pla2
Prior art date
Application number
HK03104052A
Other languages
English (en)
Inventor
Deirdre Mary B Hickey
Robert John Ife
Colin Andrew Leach
Ivan Leo Pinto
Stephen Allan Smith
Steven James Stanway
Original Assignee
Smithkline Beecham Plc
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
Priority claimed from GB0003636A external-priority patent/GB0003636D0/en
Priority claimed from GB0101437A external-priority patent/GB0101437D0/en
Application filed by Smithkline Beecham Plc filed Critical Smithkline Beecham Plc
Publication of HK1053466A1 publication Critical patent/HK1053466A1/xx

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/56One oxygen atom and one sulfur atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/60Three or more oxygen or sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/95Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic 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
    • C07D495/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (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)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (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)
HK03104052A 2000-02-16 2003-06-09 Pyrimidine-4-one derivative as ldl-pla2 inhibitor HK1053466A1 (en)

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 (1)

Publication Number Publication Date
HK1053466A1 true HK1053466A1 (en) 2003-10-24

Family

ID=26243663

Family Applications (1)

Application Number Title Priority Date Filing Date
HK03104052A HK1053466A1 (en) 2000-02-16 2003-06-09 Pyrimidine-4-one derivative as ldl-pla2 inhibitor

Country Status (32)

Country Link
US (10) US20020103213A1 (sl)
EP (2) EP1686119B1 (sl)
JP (1) JP4095804B2 (sl)
KR (1) KR100781425B1 (sl)
CN (1) CN1179952C (sl)
AR (1) AR030190A1 (sl)
AT (2) ATE333446T1 (sl)
AU (2) AU2001235466B2 (sl)
BG (1) BG66014B1 (sl)
BR (1) BRPI0108396B1 (sl)
CA (1) CA2400554C (sl)
CO (1) CO5271661A1 (sl)
CY (2) CY1105649T1 (sl)
CZ (1) CZ304450B6 (sl)
DE (2) DE60121550T2 (sl)
DK (2) DK1686119T3 (sl)
ES (2) ES2267714T3 (sl)
GC (1) GC0000221A (sl)
HK (1) HK1053466A1 (sl)
HU (1) HU229479B1 (sl)
IL (2) IL151236A (sl)
MX (1) MXPA02008062A (sl)
MY (1) MY135732A (sl)
NO (1) NO324691B1 (sl)
NZ (1) NZ520752A (sl)
PL (1) PL209824B1 (sl)
PT (2) PT1263740E (sl)
SI (2) SI1686119T1 (sl)
SK (1) SK287296B6 (sl)
TW (1) TW550259B (sl)
UA (1) UA73762C2 (sl)
WO (1) WO2001060805A1 (sl)

Families Citing this family (61)

* Cited by examiner, ā€  Cited by third party
Publication number Priority date Publication date Assignee Title
ATE333446T1 (de) * 2000-02-16 2006-08-15 Smithkline Beecham Plc Pyrimidin-4-onderivat als ldl-pla2 inhibitor
GB0024807D0 (en) 2000-10-10 2000-11-22 Smithkline Beecham Plc Novel compounds
AU9619301A (en) * 2000-10-20 2002-04-29 Biovitrum Ab 2-, 3-, 4-, or 5-substituted-n1-(benzensulfonyl)indoles and their use in therapy
GB0119795D0 (en) * 2001-08-14 2001-10-03 Smithkline Beecham Plc Novel process
GB0119793D0 (en) * 2001-08-14 2001-10-03 Smithkline Beecham Plc Novel compounds
GB0127139D0 (en) * 2001-11-10 2002-01-02 Smithkline Beecham Novel compounds
GB0127143D0 (en) * 2001-11-10 2002-01-02 Smithkline Beecham Novel compounds
GB0127140D0 (en) * 2001-11-10 2002-01-02 Smithkline Beecham Novel compounds
GB0127141D0 (en) * 2001-11-10 2002-01-02 Smithkline Beecham Plc Novel compounds
WO2003057671A1 (fr) * 2001-12-28 2003-07-17 Takeda Chemical Industries, Ltd. Compose biaryle et son utilisation
US6939863B2 (en) 2002-01-04 2005-09-06 Wei-Jan Chen Prevention of atherosclerosis and restenosis
GB0208280D0 (en) * 2002-04-10 2002-05-22 Glaxo Group Ltd Novel compounds
GB0208279D0 (en) * 2002-04-10 2002-05-22 Glaxo Group Ltd Novel compounds
US20050227974A9 (en) * 2002-08-01 2005-10-13 Euro-Celtique S.A. Aminoalkyl-substituted aryl compounds and their use as sodium channel blockers
JP4366122B2 (ja) * 2003-06-24 2009-11-18 ę—„ē«‹ć‚Ŗćƒ ćƒ­ćƒ³ć‚æćƒ¼ćƒŸćƒŠćƒ«ć‚½ćƒŖćƒ„ćƒ¼ć‚·ćƒ§ćƒ³ć‚ŗę Ŗ式会ē¤¾ ē“™č‘‰é”žę¬é€č£…ē½®
GB0320522D0 (en) * 2003-09-02 2003-10-01 Glaxo Group Ltd Formulation
NZ546444A (en) 2003-11-05 2009-09-25 Hoffmann La Roche Phenyl derivatives as PPAR agonists
US20150017671A1 (en) 2004-04-16 2015-01-15 Yaping Shou Methods for detecting lp-pla2 activity and inhibition of lp-pla2 activity
JP4812751B2 (ja) 2004-04-16 2011-11-09 ć‚°ćƒ©ć‚Æć‚½ ć‚°ćƒ«ćƒ¼ćƒ— ćƒŖ惟惆惃惉 ļ¼¬ļ½āˆ’ļ¼°ļ¼¬ļ¼”ļ¼’ę“»ę€§ćŠć‚ˆć³ļ¼¬ļ½āˆ’ļ¼°ļ¼¬ļ¼”ļ¼’ę“»ę€§é˜»å®³ć‚’ę¤œå‡ŗć™ć‚‹ę–¹ę³•
CA2563607C (en) 2004-05-08 2014-04-08 Neurogen Corporation 4,5-disubstituted-2-aryl pyrimidines
DE102004061005A1 (de) * 2004-12-18 2006-06-22 Bayer Healthcare Ag 3-Cycloalkyl-1,2,4-triazin-5(2H)-one
US7705005B2 (en) * 2006-10-13 2010-04-27 Glaxo Group Limited Bicyclic heteroaromatic compounds
US20080090852A1 (en) * 2006-10-13 2008-04-17 Colin Andrew Leach Bicyclic Heteroaromatic Compounds
US20080090851A1 (en) * 2006-10-13 2008-04-17 Colin Andrew Leach Bicyclic Heteroaromatic Compounds
EA018101B1 (ru) * 2007-05-11 2013-05-30 Š”Š·Šµ Š¢Ń€Š°ŃŃ‚ŠøŠ· ŠžŃ„ Š”Š·Šµ Š®Š½ŠøŠ²ŠµŃ€ŃŠøтŠø ŠžŃ„ ŠŸŠµŠ½ŃŠøŠ»ŃŒŠ²Š°Š½Šøя Š”ŠæŠ¾ŃŠ¾Š±Ń‹ Š»ŠµŃ‡ŠµŠ½Šøя ŠŗŠ¾Š¶Š½Ń‹Ń… яŠ·Š²
US8962633B2 (en) 2007-05-11 2015-02-24 Thomas Jefferson University Methods of treatment and prevention of metabolic bone diseases and disorders
KR101690390B1 (ko) 2007-05-11 2016-12-27 ķ† ė§ˆģŠ¤ ģ œķ¼ģŠØ ģœ ė‹ˆė²„ģ‹œķ‹° ģ‹ ź²½ė³€ģ„± ģ§ˆķ™˜ ė° ģž„ģ• ģ˜ ģ¹˜ė£Œ ė° ģ˜ˆė°© ė°©ė²•
US8637524B2 (en) 2009-07-28 2014-01-28 Auspex Pharmaceuticals, Inc Pyrimidinone inhibitors of lipoprotein-associated phospholipase A2
TW201209043A (en) * 2010-05-17 2012-03-01 Glaxo Group Ltd Novel processes
AU2011268127B2 (en) 2010-06-18 2016-01-14 Whitehead Institute For Biomedical Research PLA2G16 as a target for antiviral compounds
AU2011340690C1 (en) 2010-12-06 2016-03-10 Glaxo Group Limited Pyrimidinone compounds for use in the treatment of diseases or conditions mediated by Lp - PLA2
JP2013544854A (ja) * 2010-12-06 2013-12-19 ć‚°ćƒ©ć‚Æć‚½ ć‚°ćƒ«ćƒ¼ćƒ— ćƒŖ惟惆惃惉 化合ē‰©
CN104478812A (zh) * 2010-12-06 2015-04-01 č‘›å…°ē“ é›†å›¢ęœ‰é™å…¬åø ē”ØäŗŽę²»ē–—ē”±Lp-PLA2介åƼēš„ē–¾ē—…ęˆ–ē—…ē—‡ēš„嘧啶酮化合ē‰©
EP2651403B1 (en) 2010-12-17 2020-12-02 Glaxo Group Limited Use of lp-pla2 inhibitors in the treatment and prevention of eye diseases
CN102643269B (zh) * 2011-02-21 2014-07-23 å¤©ę“„čÆē‰©ē ”ē©¶é™¢ äø€ē±»å«å”唑ē»“ęž„ēš„ē£·č„‚é…¶a2ęŠ‘åˆ¶å‰‚åŠē”Ø途
WO2012122707A1 (zh) * 2011-03-16 2012-09-20 äø­å›½ē§‘学院äøŠęµ·čÆē‰©ē ”ē©¶ę‰€ 季铵ē›ē±»åŒ–合ē‰©ć€å…¶åˆ¶å¤‡ę–¹ę³•ć€čÆē‰©ē»„合ē‰©åŠē”Ø途
WO2012129792A1 (zh) * 2011-03-30 2012-10-04 äø­å›½ē§‘学院äøŠęµ·čÆē‰©ē ”ē©¶ę‰€ 嘧啶酮ē±»åŒ–合ē‰©ć€å…¶åˆ¶å¤‡ę–¹ę³•åŠčÆē‰©ē»„合ē‰©å’Œē”Ø途
US20140171431A1 (en) * 2011-06-27 2014-06-19 Jianhua Shen Azole heterocyclic compound, preparation method, pharmaceutical composition and use
WO2013014185A1 (en) 2011-07-27 2013-01-31 Glaxo Group Limited Bicyclic pyrimidone compounds
CN103827116B (zh) * 2011-07-27 2016-08-31 č‘›å…°ē“ é›†å›¢ęœ‰é™å…¬åø ē”Ø作LP-PLA2ęŠ‘åˆ¶å‰‚ēš„2,3-äŗŒę°¢å’Ŗ唑并[1,2-c]嘧啶-5(1H)-酮化合ē‰©
US8975400B2 (en) 2011-07-27 2015-03-10 Glaxo Group Limited 2,3-dihydroimidazo[1, 2-c] pyrimidin-5(1 H)-one compounds use as LP-PLA2 inhibitors
EP2948452B1 (en) 2013-01-25 2017-08-09 GlaxoSmithKline Intellectual Property Development Limited 2,3-dihydroimidazol[1,2-c]pyrimidin-5(1h)-one based lipoprotein-associated phospholipase a2 (lp-pla2) inhibitors
KR20150108896A (ko) 2013-01-25 2015-09-30 źø€ė½ģ†ŒģŠ¤ėÆøģŠ¤ķ“ė¼ģø ģøķ„øė ‰ģø„ģ–¼ ķ”„ė”œķ¼ķ‹° ė””ė²Øė”œķ”„ėؼķŠø ė¦¬ėÆøķ‹°ė“œ Lp-pla2ģ˜ ģ–µģ œģ œė”œģ„œģ˜ ė¹„ģ‹œķ“ė¦­ ķ”¼ė¦¬ėÆøėˆ ķ™”ķ•©ė¬¼
CN105008365B (zh) 2013-01-25 2017-03-15 č‘›å…°ē“ å²åƆę–Æå…‹čŽ±ēŸ„čƆäŗ§ęƒå‘å±•ęœ‰é™å…¬åø 化合ē‰©
US20140283157A1 (en) 2013-03-15 2014-09-18 Diadexus, Inc. Lipoprotein-associated phospholipase a2 antibody compositions and methods of use
WO2015087239A1 (en) 2013-12-11 2015-06-18 Ranbaxy Laboratories Limited Processes for the preparation of darapladib and its intermediates
WO2015092687A2 (en) 2013-12-17 2015-06-25 Ranbaxy Laboratories Limited Process for the purification of darapladib
WO2015114479A1 (en) 2014-01-28 2015-08-06 Ranbaxy Laboratories Limited Crystalline forms of darapladib oxalate, adipate, succinate, phosphate, sulphate, fumaratetartrate, nitrate and borate
WO2016012916A1 (en) 2014-07-22 2016-01-28 Glaxosmithkline Intellectual Property Development Limited 1,2,3,5-tetrahydroimidazo[1,2-c]pyrimidine derivatives useful in the treatment of diseases and disorders mediated by lp-pla2
WO2016012917A1 (en) 2014-07-22 2016-01-28 Glaxosmithkline Intellectual Property Development Limited 1,2,3,5-tetrahydroimidazo[1,2-c]pyrimidine derivatives useful in the treatment of diseases and disorders mediated by lp-pla2
CA2959208C (en) 2014-08-29 2023-09-19 Tes Pharma S.R.L. Pyrimidine derivatives and their use as inhibitors of alpha-amino-beta-carboxymuconate-epsilon-semialdehyde decarboxylase
CN105777653A (zh) 2014-12-26 2016-07-20 äø­å›½ē§‘学院äøŠęµ·čÆē‰©ē ”ē©¶ę‰€ ē”Ø作Lp-PLA2ęŠ‘åˆ¶å‰‚ēš„嘧啶酮ē±»åŒ–合ē‰©åŠå…¶čÆē‰©ē»„合ē‰©
CN104840963B (zh) * 2015-05-26 2018-02-16 ę²³åŒ—äøœåŗ·ē”Ÿē‰©ē§‘ęŠ€ęœ‰é™å…¬åø å«č„‚č›‹ē™½ē›øå…³ę€§ē£·č„‚é…¶a2ęŠ‘åˆ¶å‰‚ēš„čÆē‰©ē»„合ē‰©åŠåŗ”ē”Ø
CN107709314A (zh) * 2015-06-11 2018-02-16 å·“ę–Æ利尔čÆē‰©å›½é™…č‚”份公åø å¤–ęŽ’ę³µęŠ‘åˆ¶å‰‚åŠå…¶ę²»ē–—ꀧē”Ø途
EP3390400B1 (en) 2015-12-16 2021-01-20 Bristol-Myers Squibb Company Heteroarylhydroxypyrimidinones as agonists of the apj receptor
US10878307B2 (en) * 2016-12-23 2020-12-29 Microsoft Technology Licensing, Llc EQ-digital conversation assistant
ES2907130T3 (es) * 2017-09-26 2022-04-22 Inst Nat Sante Rech Med Darapladib radiomarcado, anĆ”logos del mismo y su uso como compuestos para la obtenciĆ³n de imĆ”genes
CN110746445B (zh) * 2019-10-16 2021-03-16 ę·±åœ³ęµ·å…³é£Ÿå“ę£€éŖŒę£€ē–«ęŠ€ęœÆäø­åæƒ äø€ē§å¤“å­¢å“Œé…®ę°˜ä»£å†…ę ‡ē‰©ēš„åˆ¶å¤‡ę–¹ę³•
WO2021089032A1 (zh) 2019-11-09 2021-05-14 äøŠęµ·čµ›é»˜ē½—ē”Ÿē‰©ē§‘ęŠ€ęœ‰é™å…¬åø äø‰ēŽÆäŗŒę°¢å’Ŗå”‘å¹¶å˜§å•¶é…®č”ē”Ÿē‰©ć€å…¶åˆ¶å¤‡ę–¹ę³•ć€čÆē‰©ē»„合ē‰©å’Œē”Ø途
CN115304620A (zh) 2021-05-07 2022-11-08 äøŠęµ·čµ›é»˜ē½—ē”Ÿē‰©ē§‘ęŠ€ęœ‰é™å…¬åø å˜§å•¶é…®č”ē”Ÿē‰©ć€å…¶åˆ¶å¤‡ę–¹ę³•ć€čÆē‰©ē»„合ē‰©å’Œē”Ø途
EP4257133A1 (en) 2022-04-05 2023-10-11 Institut Pasteur Oxo-azaheterocyclic derivatives for use in the treatment of malaria

Family Cites Families (22)

* Cited by examiner, ā€  Cited by third party
Publication number Priority date Publication date Assignee Title
EP0974663A1 (en) 1993-06-25 2000-01-26 Smithkline Beecham Plc Lipoprotein associated phospholipase A2, inhibitors thereof and use of same in diagnosis and therapy
DK0673426T3 (da) * 1993-10-06 2001-08-27 Icos Corp Blodpladeaktiveringsfaktor-acetylhydrolase
GB9421816D0 (en) 1994-10-29 1994-12-14 Smithkline Beecham Plc Novel compounds
DZ1958A1 (fr) 1994-12-22 2002-02-17 Smithkline Beecham Plc ComposƩs inhibiteurs de l'enzyme l-lpa compositionpharmaceutiques les composant et procƩdƩs pour leur prƩparation.
CH690264A5 (fr) 1995-06-30 2000-06-30 Symphar Sa DƩrivƩs aminophosphonates substituƩs, leur procƩdƩ de prƩparation et leur utilisation pour la prƩparation de compositions pharmaceutiques.
CZ422197A3 (cs) 1995-07-01 1998-06-17 Smithkline Beecham Plc AzetidinonovĆ© derivĆ”ty, zpÅÆsob jejich pÅ™Ć­pravy, meziprodukty tohoto postupu, farmaceutickĆ½ prostředek obsahujĆ­cĆ­ tyto sloučeniny a použitĆ­ těchto sloučenin jako lĆ©Äiv
CA2233300A1 (en) 1995-09-29 1997-04-10 Christopher Donald Southan A paf-acetylhydrolase and use in therapy
EP0865429A1 (en) 1995-12-08 1998-09-23 Smithkline Beecham Plc Azetidinone compounds for the treatment of atherosclerosis
WO1997021675A1 (en) 1995-12-08 1997-06-19 Smithkline Beecham Plc Monocyclic beta-lactame derivatives for treatment of atherosclerosis
PL329530A1 (en) 1996-04-26 1999-03-29 Smithkline Beecham Plc Derivatives of azetidinone for use in treatment of arterial atheromatosis
GB9608649D0 (en) 1996-04-26 1996-07-03 Smithkline Beecham Plc Novel compounds
GB9626616D0 (en) 1996-12-20 1997-02-05 Symphar Sa Novel compounds
GB9626615D0 (en) 1996-12-20 1997-02-05 Symphar Sa Novel compounds
GB9626536D0 (en) 1996-12-20 1997-02-05 Symphar Sa Novel compounds
US6417192B1 (en) * 1997-11-06 2002-07-09 Smithkline Beecham P.L.C. Pyrimidinone compounds and pharmaceutical compositions containing them
US6559155B1 (en) 1998-08-21 2003-05-06 Smithkline Beecham P.L.C. Pyrimidinone derivatives for the treatment of atherosclerosis
GB9910079D0 (en) 1999-05-01 1999-06-30 Smithkline Beecham Plc Novel compounds
US6953803B1 (en) * 1999-05-01 2005-10-11 Smithkline Beecham P.L.C. Pyrimidine compounds
GB9910378D0 (en) 1999-05-05 1999-06-30 Smithkline Beecham Plc Novel compounds
ATE333446T1 (de) * 2000-02-16 2006-08-15 Smithkline Beecham Plc Pyrimidin-4-onderivat als ldl-pla2 inhibitor
GB0024808D0 (en) * 2000-10-10 2000-11-22 Smithkline Beecham Plc Novel compounds
GB0024807D0 (en) * 2000-10-10 2000-11-22 Smithkline Beecham Plc Novel compounds

Also Published As

Publication number Publication date
SK11772002A3 (sk) 2003-02-04
SI1263740T1 (sl) 2006-12-31
DK1686119T3 (da) 2009-11-09
ES2330552T3 (es) 2009-12-11
US6649619B1 (en) 2003-11-18
ATE437862T1 (de) 2009-08-15
CA2400554A1 (en) 2001-08-23
US9266841B2 (en) 2016-02-23
US8871775B2 (en) 2014-10-28
CY1109484T1 (el) 2014-08-13
GC0000221A (en) 2006-03-29
AU2001235466B2 (en) 2004-04-22
AU3546601A (en) 2001-08-27
NO324691B1 (no) 2007-12-03
US20120172378A1 (en) 2012-07-05
US20100144765A1 (en) 2010-06-10
CZ20022768A3 (cs) 2003-05-14
JP4095804B2 (ja) 2008-06-04
BRPI0108396B1 (pt) 2015-05-19
AR030190A1 (es) 2003-08-13
US20070155762A1 (en) 2007-07-05
EP1263740B1 (en) 2006-07-19
KR20030011772A (ko) 2003-02-11
DE60121550T2 (de) 2007-06-21
MXPA02008062A (es) 2002-11-29
EP1686119B1 (en) 2009-07-29
DE60139429D1 (de) 2009-09-10
HUP0204410A3 (en) 2003-07-28
SK287296B6 (sk) 2010-06-07
NZ520752A (en) 2004-03-26
ATE333446T1 (de) 2006-08-15
CZ304450B6 (cs) 2014-05-14
US7638520B2 (en) 2009-12-29
BG107034A (bg) 2003-04-30
CN1179952C (zh) 2004-12-15
PT1263740E (pt) 2006-11-30
EP1686119A1 (en) 2006-08-02
CN1418199A (zh) 2003-05-14
IL181957A0 (en) 2009-02-11
SI1686119T1 (sl) 2009-12-31
WO2001060805A1 (en) 2001-08-23
CA2400554C (en) 2009-04-07
TW550259B (en) 2003-09-01
BR0108396A (pt) 2003-03-11
EP1263740A1 (en) 2002-12-11
HU229479B1 (en) 2014-01-28
MY135732A (en) 2008-06-30
US7470694B2 (en) 2008-12-30
PT1686119E (pt) 2009-10-06
JP2003523335A (ja) 2003-08-05
IL151236A (en) 2009-02-11
US20090118313A1 (en) 2009-05-07
BG66014B1 (bg) 2010-10-29
HUP0204410A2 (en) 2003-05-28
PL209824B1 (pl) 2011-10-31
CO5271661A1 (es) 2003-04-30
DE60121550D1 (de) 2006-08-31
PL357382A1 (en) 2004-07-26
US20090170877A1 (en) 2009-07-02
KR100781425B1 (ko) 2007-12-03
ES2267714T3 (es) 2007-03-16
NO20023828L (no) 2002-09-30
US7153861B2 (en) 2006-12-26
US20150045375A1 (en) 2015-02-12
US7652019B2 (en) 2010-01-26
US20070123549A1 (en) 2007-05-31
UA73762C2 (uk) 2005-09-15
DK1263740T3 (da) 2006-11-13
NO20023828D0 (no) 2002-08-13
CY1105649T1 (el) 2010-12-22
US20040097525A1 (en) 2004-05-20
US20020103213A1 (en) 2002-08-01

Similar Documents

Publication Publication Date Title
HK1053466A1 (en) Pyrimidine-4-one derivative as ldl-pla2 inhibitor
EE200300227A (et) P38 kinaasiga seotud haigusseisundite ravimeetodid ja kinaasi inhibiitoritena kasulikud pĆ¼rrolotriasiiniĆ¼hendid
IL150641A0 (en) Nicotinamide benzofused-heterocyclyl derivatives useful as selective inhibitors of pde4 isozymes
YU83302A (sh) Jedinjenja pirolo (2,3-d) pirimidina kao imunosupresivni agensi
AU6116701A (en) Beta-carboline derivatives useful as inhibitors of phosphodiesterase
AU2001285163A1 (en) Quinoline inhibitors of cgmp phosphodiesterase
SI1070056T1 (sl) Ftalazinonski PDE III/IV inhibitorji
AU2001228309A1 (en) N-substituted 2-cyanopyroles and -pyrrolines which are inhibitors of the enzyme dpp-iv
HK1076598A1 (en) Substituted quinazoline derivatives as inhibitors of aurora kinases
MY136037A (en) Biphenyl pyrimidone lp-pla2 inhibitors
HK1078850A1 (en) Novel alkoxypyridine-derivatives
IL140244A0 (en) Heterocyclic compounds as inhibitors of rotamase enzymes
AU2002226911A1 (en) Indol derivative and their use as inhibitors of p38 kinase
WO2004030620A3 (en) Novel tyrosine kinase inhibitors
WO2002085906A3 (en) Phthalazinones derivatives useful as pde4/7 inhibitors
MXPA04004372A (es) Derivados heterociclicos de glicinamida y su uso medico.
AU1782301A (en) 3,4-dihydro-(1h)quinazolin-2-one compounds as csbp/p39 kinase inhibitors
ATE374189T1 (de) Phthalazinon-derivate als pde 4 hemmer
MXPA02011558A (es) Inhibidores de mmp-2/mp-9 novedosos.
IL169334A0 (en) Phthalazine derivatives as phosphodiesterase 4 inhibitors
SI1289985T1 (sl) beta-karbolinski derivati, koristni kot inhibitorji fosfodiesteraze
SI1178967T1 (sl) Kinolinski derivati kot inhibitorji MEK encimov

Legal Events

Date Code Title Description
PC Patent ceased (i.e. patent has lapsed due to the failure to pay the renewal fee)

Effective date: 20170213