DK1686119T3 - Pyrimidin-5-on-derivater som LDL-PLA2 inhibitorer - Google Patents
Pyrimidin-5-on-derivater som LDL-PLA2 inhibitorerInfo
- 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
Links
- BDTRIDKONHOQQN-UHFFFAOYSA-N 4h-pyrimidin-5-one Chemical class O=C1CN=CN=C1 BDTRIDKONHOQQN-UHFFFAOYSA-N 0.000 title 1
- 101001097889 Homo sapiens Platelet-activating factor acetylhydrolase Proteins 0.000 title 1
- 102100037518 Platelet-activating factor acetylhydrolase Human genes 0.000 title 1
- 239000003358 phospholipase A2 inhibitor Substances 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
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- 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
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- 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)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (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)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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 |
|---|---|---|---|
| DK01907522T DK1263740T3 (da) | 2000-02-16 | 2001-02-13 | Pyrimidin-4-on-derivat som LDL-PLA2-inhibitor |
| DK06075890T DK1686119T3 (da) | 2000-02-16 | 2001-02-13 | Pyrimidin-5-on-derivater som LDL-PLA2 inhibitorer |
Family Applications Before (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 (31)
| Country | Link |
|---|---|
| US (10) | US20020103213A1 (da) |
| EP (2) | EP1686119B1 (da) |
| JP (1) | JP4095804B2 (da) |
| KR (1) | KR100781425B1 (da) |
| CN (1) | CN1179952C (da) |
| AR (1) | AR030190A1 (da) |
| AT (2) | ATE437862T1 (da) |
| AU (2) | AU3546601A (da) |
| BG (1) | BG66014B1 (da) |
| BR (1) | BRPI0108396B1 (da) |
| CA (1) | CA2400554C (da) |
| CO (1) | CO5271661A1 (da) |
| CY (2) | CY1105649T1 (da) |
| CZ (1) | CZ304450B6 (da) |
| DE (2) | DE60121550T2 (da) |
| DK (2) | DK1263740T3 (da) |
| ES (2) | ES2330552T3 (da) |
| GC (1) | GC0000221A (da) |
| HU (1) | HU229479B1 (da) |
| IL (2) | IL151236A (da) |
| MX (1) | MXPA02008062A (da) |
| MY (1) | MY135732A (da) |
| NO (1) | NO324691B1 (da) |
| NZ (1) | NZ520752A (da) |
| PL (1) | PL209824B1 (da) |
| PT (2) | PT1686119E (da) |
| SI (2) | SI1263740T1 (da) |
| SK (1) | SK287296B6 (da) |
| TW (1) | TW550259B (da) |
| UA (1) | UA73762C2 (da) |
| WO (1) | WO2001060805A1 (da) |
Families Citing this family (62)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE437862T1 (de) | 2000-02-16 | 2009-08-15 | Smithkline Beecham Plc | Pyrimidin-5-onderivate als ldl-pla2 inhibitoren |
| GB0024807D0 (en) | 2000-10-10 | 2000-11-22 | Smithkline Beecham Plc | Novel compounds |
| CA2422717A1 (en) * | 2000-10-20 | 2002-04-25 | Biovitrum Ab | 2-, 3-, 4-, or 5-substituted-n1-(benzensulfonyl)indoles and their use in therapy |
| GB0119793D0 (en) * | 2001-08-14 | 2001-10-03 | Smithkline Beecham Plc | Novel compounds |
| GB0119795D0 (en) * | 2001-08-14 | 2001-10-03 | Smithkline Beecham Plc | Novel process |
| GB0127143D0 (en) * | 2001-11-10 | 2002-01-02 | Smithkline Beecham | Novel compounds |
| GB0127139D0 (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 (en) * | 2001-12-28 | 2003-07-17 | Takeda Chemical Industries, Ltd. | Biaryl compound and use thereof |
| 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 | 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 |
| CA2543249C (en) | 2003-11-05 | 2012-08-07 | 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 |
| WO2005113797A2 (en) | 2004-04-16 | 2005-12-01 | 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 |
| 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 |
| US7705005B2 (en) * | 2006-10-13 | 2010-04-27 | Glaxo Group Limited | Bicyclic heteroaromatic compounds |
| MX2009012197A (es) | 2007-05-11 | 2010-01-15 | Univ Pennsylvania | Metodos para tratamiento de ulceras en la piel. |
| CN101986785A (zh) | 2007-05-11 | 2011-03-16 | 托马斯杰弗逊大学 | 治疗和预防神经退行性疾病和紊乱的方法 |
| US8962633B2 (en) | 2007-05-11 | 2015-02-24 | Thomas Jefferson University | Methods of treatment and prevention of metabolic bone diseases and disorders |
| 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. |
| CA2805409A1 (en) | 2010-06-18 | 2011-12-22 | Whitehead Institute For Biomedical Research | Pla2g16 as a target for antiviral compounds |
| JP5886310B2 (ja) | 2010-12-06 | 2016-03-16 | グラクソ グループ リミテッドGlaxo Group Limited | Lp−PLA2により媒介される疾患または状態の処置における使用のためのピリミジノン化合物 |
| 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 |
| 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 | 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 |
| EP2725024A4 (en) | 2011-06-27 | 2014-12-03 | Shanghai Inst Materia Medica | HETEROCYCLIC AZOL COMPOUND, METHOD OF MANUFACTURING THEREOF, PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| JP2014521625A (ja) | 2011-07-27 | 2014-08-28 | グラクソ グループ リミテッド | 二環式ピリミドン化合物 |
| 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 |
| 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 |
| AU2014210259B2 (en) | 2013-01-25 | 2016-11-03 | Glaxosmithkline Intellectual Property Development Limited | Compounds |
| ES2642762T3 (es) | 2013-01-25 | 2017-11-20 | Glaxosmithkline Intellectual Property Development Limited | Inhibidores de fosfolipasa A2 asociada a lipoproteínas (LP-PLA2) basados en 2,3-dihidroimidazol[1,2-c]pirimidin-5(1H)-ona |
| EP2948456A4 (en) | 2013-01-25 | 2016-09-14 | Glaxosmithkline Ip Dev Ltd | BICYCLIC PYRIMIDONE COMPOUNDS AS LP-PLA2 INHIBITORS |
| 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 |
| KR102431436B1 (ko) | 2014-08-29 | 2022-08-10 | 테스 파마 에스.알.엘. | α-아미노-β-카복시뮤콘산 세미알데히드 데카복실라제의 억제제 |
| 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 |
| KR20180011843A (ko) * | 2015-06-11 | 2018-02-02 | 바실리어 파마슈티카 인터내셔널 리미티드 | 유출-펌프 억제제 및 이의 치료적 용도 |
| BR112018012112A2 (pt) | 2015-12-16 | 2018-12-04 | Bristol-Myers Squibb Company | heteroaril-hidroxipirimidinonas como agonistas do receptor apj |
| US10878307B2 (en) * | 2016-12-23 | 2020-12-29 | Microsoft Technology Licensing, Llc | EQ-digital conversation assistant |
| EP3687980B1 (en) * | 2017-09-26 | 2022-01-19 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Radiolabeled darapladib, analogs thereof 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 |
| MX2022005615A (es) | 2019-11-09 | 2022-07-27 | Shanghai Simr Biotechnology Co Ltd | Derivado triciclico de dihidroimidazopirimidona, metodo de preparacion del mismo, composicion farmaceutica 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 |
| CN119191998A (zh) * | 2024-11-29 | 2024-12-27 | 浙江省质量科学研究院 | 一种双羟乙基氨基丙基羟乙基十六胺的合成方法 |
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| WO1995000649A1 (en) | 1993-06-25 | 1995-01-05 | Smithkline Beecham Plc | Lipoprotein associated phospholipase a2, inhibitors thereof and use of the same in diagnosis and therapy |
| EP0673426B1 (en) * | 1993-10-06 | 2001-06-06 | Icos Corporation | Platelet-activating factor acetylhydrolase |
| GB9421816D0 (en) | 1994-10-29 | 1994-12-14 | Smithkline Beecham Plc | Novel compounds |
| NZ298416A (en) | 1994-12-22 | 1999-03-29 | Smithkline Beecham Plc | Substituted azetidin-2-one derivatives and medicaments thereof |
| 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. |
| IL122650A0 (en) | 1995-07-01 | 1998-08-16 | Smithkline Beecham Plc | Azetidinone derivatives for the treatment of atherosclerosis |
| WO1997012963A2 (en) | 1995-09-29 | 1997-04-10 | Smithkline Beecham Plc | A paf-acetylhydrolase and use in therapy |
| JP2000505063A (ja) | 1995-12-08 | 2000-04-25 | 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アゼチジノン化合物 |
| 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 |
| AU2698697A (en) | 1996-04-26 | 1997-11-19 | Smithkline Beecham Plc | Azetidinone derivatives for the treatment of atherosclerosis |
| 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 |
| JP2001522844A (ja) | 1997-11-06 | 2001-11-20 | 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 | ピリミジノン化合物およびそれを含有する医薬組成物 |
| ATE251613T1 (de) * | 1998-08-21 | 2003-10-15 | Smithkline Beecham Plc | Pyrimidinonderivate zur behandlung von atheroscleros |
| PT1175408E (pt) * | 1999-05-01 | 2005-04-29 | Smithkline Beecham Plc | Derivados sulfonamida |
| GB9910079D0 (en) | 1999-05-01 | 1999-06-30 | Smithkline Beecham Plc | Novel compounds |
| GB9910378D0 (en) | 1999-05-05 | 1999-06-30 | Smithkline Beecham Plc | Novel compounds |
| ATE437862T1 (de) | 2000-02-16 | 2009-08-15 | Smithkline Beecham Plc | Pyrimidin-5-onderivate als ldl-pla2 inhibitoren |
| 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 |
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2001
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