DK1686119T3 - Pyrimidin-5-on-derivater som LDL-PLA2 inhibitorer - Google Patents

Pyrimidin-5-on-derivater som LDL-PLA2 inhibitorer

Info

Publication number
DK1686119T3
DK1686119T3 DK06075890T DK06075890T DK1686119T3 DK 1686119 T3 DK1686119 T3 DK 1686119T3 DK 06075890 T DK06075890 T DK 06075890T DK 06075890 T DK06075890 T DK 06075890T DK 1686119 T3 DK1686119 T3 DK 1686119T3
Authority
DK
Denmark
Prior art keywords
ldl
pyrimidin
derivatives
pla2 inhibitors
inhibitors
Prior art date
Application number
DK06075890T
Other languages
Danish (da)
English (en)
Inventor
Deidre Mary 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
Application granted granted Critical
Publication of DK1686119T3 publication Critical patent/DK1686119T3/da

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    • 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

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (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)
DK06075890T 2000-02-16 2001-02-13 Pyrimidin-5-on-derivater som LDL-PLA2 inhibitorer DK1686119T3 (da)

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
DK1686119T3 true DK1686119T3 (da) 2009-11-09

Family

ID=26243663

Family Applications (2)

Application Number Title Priority Date Filing Date
DK06075890T DK1686119T3 (da) 2000-02-16 2001-02-13 Pyrimidin-5-on-derivater som LDL-PLA2 inhibitorer
DK01907522T DK1263740T3 (da) 2000-02-16 2001-02-13 Pyrimidin-4-on-derivat som LDL-PLA2-inhibitor

Family Applications After (1)

Application Number Title Priority Date Filing Date
DK01907522T DK1263740T3 (da) 2000-02-16 2001-02-13 Pyrimidin-4-on-derivat som LDL-PLA2-inhibitor

Country Status (32)

Country Link
US (10) US20020103213A1 (ja)
EP (2) EP1686119B1 (ja)
JP (1) JP4095804B2 (ja)
KR (1) KR100781425B1 (ja)
CN (1) CN1179952C (ja)
AR (1) AR030190A1 (ja)
AT (2) ATE333446T1 (ja)
AU (2) AU3546601A (ja)
BG (1) BG66014B1 (ja)
BR (1) BRPI0108396B1 (ja)
CA (1) CA2400554C (ja)
CO (1) CO5271661A1 (ja)
CY (2) CY1105649T1 (ja)
CZ (1) CZ304450B6 (ja)
DE (2) DE60139429D1 (ja)
DK (2) DK1686119T3 (ja)
ES (2) ES2330552T3 (ja)
GC (1) GC0000221A (ja)
HK (1) HK1053466A1 (ja)
HU (1) HU229479B1 (ja)
IL (2) IL151236A (ja)
MX (1) MXPA02008062A (ja)
MY (1) MY135732A (ja)
NO (1) NO324691B1 (ja)
NZ (1) NZ520752A (ja)
PL (1) PL209824B1 (ja)
PT (2) PT1686119E (ja)
SI (2) SI1263740T1 (ja)
SK (1) SK287296B6 (ja)
TW (1) TW550259B (ja)
UA (1) UA73762C2 (ja)
WO (1) WO2001060805A1 (ja)

Families Citing this family (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4095804B2 (ja) 2000-02-16 2008-06-04 スミスクライン ビーチャム ピー エル シー Ldl−pla2阻害剤としてのピリミジン−4−オン誘導体
GB0024807D0 (en) * 2000-10-10 2000-11-22 Smithkline Beecham Plc Novel compounds
IL154685A0 (en) * 2000-10-20 2003-09-17 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
GB0127140D0 (en) * 2001-11-10 2002-01-02 Smithkline Beecham Novel compounds
GB0127143D0 (en) * 2001-11-10 2002-01-02 Smithkline Beecham Novel compounds
GB0127141D0 (en) * 2001-11-10 2002-01-02 Smithkline Beecham Plc Novel compounds
GB0127139D0 (en) * 2001-11-10 2002-01-02 Smithkline Beecham 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
GB0208279D0 (en) * 2002-04-10 2002-05-22 Glaxo Group Ltd Novel compounds
GB0208280D0 (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 日立オムロンターミナルソリューションズ株式会社 紙葉類搬送装置
GB0320522D0 (en) * 2003-09-02 2003-10-01 Glaxo Group Ltd Formulation
WO2005049573A1 (en) 2003-11-05 2005-06-02 F. Hoffmann-La Roche Ag 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
US7741020B2 (en) 2004-04-16 2010-06-22 Glaxo Group Limited Methods for detecting Lp-PLA2 activity and inhibition of Lp-PLA2 activity
AU2005244104B2 (en) 2004-05-08 2012-03-15 Novartis International Pharmaceutical Ltd. 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
US20080090851A1 (en) * 2006-10-13 2008-04-17 Colin Andrew Leach Bicyclic Heteroaromatic Compounds
US20080090852A1 (en) * 2006-10-13 2008-04-17 Colin Andrew Leach Bicyclic Heteroaromatic Compounds
EA200971050A1 (ru) 2007-05-11 2010-06-30 Томас Джефферсон Юниверсити Способы лечения и предупреждения нейродегенеративных заболеваний и нарушений
US8962633B2 (en) 2007-05-11 2015-02-24 Thomas Jefferson University Methods of treatment and prevention of metabolic bone diseases and disorders
EP2155225B1 (en) * 2007-05-11 2015-07-08 The Trustees of the University of Pennsylvania Methods of treatment of skin ulcers
US8637524B2 (en) 2009-07-28 2014-01-28 Auspex Pharmaceuticals, Inc Pyrimidinone inhibitors of lipoprotein-associated phospholipase A2
AR081399A1 (es) 2010-05-17 2012-08-29 Glaxo Group Ltd Proceso para preparar un compuesto de pirimidinona, compuestos intermediarios en dicho proceso y procesos para repararlos.
JP6053675B2 (ja) 2010-06-18 2016-12-27 ホワイトヘッド・インスティチュート・フォア・バイオメディカル・リサーチ 抗ウイルス化合物のためのターゲットとしてのpla2g16
US20130252963A1 (en) 2010-12-06 2013-09-26 Yun Jin Pyrimidinone compounds for use in the treatment of disease or conditions mediated by lp-pla2
EP2649050A4 (en) * 2010-12-06 2014-04-23 Glaxo Group Ltd LINKS
CN104478812A (zh) * 2010-12-06 2015-04-01 葛兰素集团有限公司 用于治疗由Lp-PLA2介导的疾病或病症的嘧啶酮化合物
US20130267544A1 (en) 2010-12-17 2013-10-10 Peter Adamson Use of LP-PLA2 Inhibitors in the Treatment and Prevention of Eye Diseases
CN102643269B (zh) * 2011-02-21 2014-07-23 天津药物研究院 一类含吡唑结构的磷脂酶a2抑制剂及用途
WO2012122707A1 (zh) * 2011-03-16 2012-09-20 中国科学院上海药物研究所 季铵盐类化合物、其制备方法、药物组合物及用途
WO2012129792A1 (zh) * 2011-03-30 2012-10-04 中国科学院上海药物研究所 嘧啶酮类化合物、其制备方法及药物组合物和用途
US20140171431A1 (en) * 2011-06-27 2014-06-19 Jianhua Shen Azole heterocyclic compound, preparation method, pharmaceutical composition and use
AU2012288865B2 (en) 2011-07-27 2015-10-01 Glaxo Group Limited Bicyclic pyrimidone compounds
CN103827116B (zh) * 2011-07-27 2016-08-31 葛兰素集团有限公司 用作LP-PLA2抑制剂的2,3-二氢咪唑并[1,2-c]嘧啶-5(1H)-酮化合物
EP2739627A4 (en) 2011-07-27 2015-01-21 Glaxo Group Ltd 2,3-DIHYDROIMIDAZO [1,2-C] PYRIMIDIN-5 (1H) -ONE COMPOUNDS AND USE AS INHIBITORS OF LP-PLA2
BR112015017759B1 (pt) 2013-01-25 2022-05-24 Glaxosmithkline Intellectual Property Development Limited Compostos inibidores de fosfolipase a2 associada à lipoproteína (lp-pla2) à base de 2,3-dihidroimidazol[1,2-c]pirimidin5(1h)-ona, e composição farmacêutica compreendendo tais compostos
AU2014210259B2 (en) 2013-01-25 2016-11-03 Glaxosmithkline Intellectual Property Development Limited Compounds
JP2016505053A (ja) 2013-01-25 2016-02-18 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited Lp‐PLA2の阻害剤としての二環式ピリミドン化合物
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
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
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
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 中国科学院上海药物研究所 用作Lp-PLA2抑制剂的嘧啶酮类化合物及其药物组合物
CN104840963B (zh) * 2015-05-26 2018-02-16 河北东康生物科技有限公司 含脂蛋白相关性磷脂酶a2抑制剂的药物组合物及应用
CN107709314A (zh) * 2015-06-11 2018-02-16 巴斯利尔药物国际股份公司 外排泵抑制剂及其治疗性用途
PE20181487A1 (es) * 2015-12-16 2018-09-18 Bristol Myers Squibb Co Heteroarilhidroxipirimidinonas como agonistas del receptor de apelina (apj)
US10878307B2 (en) * 2016-12-23 2020-12-29 Microsoft Technology Licensing, Llc EQ-digital conversation assistant
WO2019063634A1 (en) * 2017-09-26 2019-04-04 INSERM (Institut National de la Santé et de la Recherche Médicale) DARAPLADIB RADIOMARQUÉ, ITS ANALOGUES AND THEIR USE AS IMAGING COMPOUNDS
CN110746445B (zh) * 2019-10-16 2021-03-16 深圳海关食品检验检疫技术中心 一种头孢哌酮氘代内标物的制备方法
PE20230092A1 (es) 2019-11-09 2023-01-16 Shanghai Simr Biotechnology Co Ltd Derivado triciclico de dihidroimidazopirimidona, metodo de preparacion del mismo, composicion farmaceuticas y uso del mismo
CN115304620A (zh) 2021-05-07 2022-11-08 上海赛默罗生物科技有限公司 嘧啶酮衍生物、其制备方法、药物组合物和用途
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, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69423436T2 (de) 1993-06-25 2000-09-07 Smithkline Beecham P.L.C., Brentford An lipoprotein gebundene phospholipase a2, inhibitoren davon und deren verwendung für diagnose und therapie
ATE201905T1 (de) * 1993-10-06 2001-06-15 Icos Corp Acethylhydrolase des plättchen aktivierenden faktors
GB9421816D0 (en) 1994-10-29 1994-12-14 Smithkline Beecham Plc Novel compounds
BR9510420A (pt) 1994-12-22 2004-04-20 Smithkline Beecham Plc Azetidin-2-onas substituìdas para o tratamento de aterosclerose
CH690264A5 (fr) 1995-06-30 2000-06-30 Symphar Sa Dérivés aminophosphonates substitués, leur procédé de préparation et leur utilisation pour la préparation de compositions pharmaceutiques.
TR199701762T1 (xx) 1995-07-01 1998-05-21 Smithkline Beecham P.L.C. Damar t�kanmas� tedavisi i�in azetidinon t�revleri.
AU7216996A (en) 1995-09-29 1997-04-28 Smithkline Beecham Plc A paf-acetylhydrolase and use in therapy
WO1997021676A1 (en) 1995-12-08 1997-06-19 Smithkline Beecham Plc Azetidinone compounds for the treatment of atherosclerosis
JP2000502079A (ja) 1995-12-08 2000-02-22 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー アテローム性動脈硬化症の治療のための単環β―ラクタム誘導体
GB9608649D0 (en) 1996-04-26 1996-07-03 Smithkline Beecham Plc Novel compounds
TR199802160T2 (xx) 1996-04-26 1999-04-21 Smithkline Beecham Plc Ateroskleroz tedavisi i�in azetidinon t�revleri.
GB9626615D0 (en) 1996-12-20 1997-02-05 Symphar Sa Novel compounds
GB9626616D0 (en) 1996-12-20 1997-02-05 Symphar Sa Novel compounds
GB9626536D0 (en) 1996-12-20 1997-02-05 Symphar Sa Novel compounds
CA2309177A1 (en) * 1997-11-06 1999-05-20 Stephen Allan Smith 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
CN1286822C (zh) * 1999-05-01 2006-11-29 史密丝克莱恩比彻姆有限公司 嘧啶酮化合物
GB9910378D0 (en) 1999-05-05 1999-06-30 Smithkline Beecham Plc Novel compounds
JP4095804B2 (ja) * 2000-02-16 2008-06-04 スミスクライン ビーチャム ピー エル シー Ldl−pla2阻害剤としてのピリミジン−4−オン誘導体
GB0024807D0 (en) * 2000-10-10 2000-11-22 Smithkline Beecham Plc Novel compounds
GB0024808D0 (en) * 2000-10-10 2000-11-22 Smithkline Beecham Plc Novel compounds

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