ATE251613T1 - Pyrimidinonderivate zur behandlung von atheroscleros - Google Patents
Pyrimidinonderivate zur behandlung von atherosclerosInfo
- Publication number
- ATE251613T1 ATE251613T1 AT99942894T AT99942894T ATE251613T1 AT E251613 T1 ATE251613 T1 AT E251613T1 AT 99942894 T AT99942894 T AT 99942894T AT 99942894 T AT99942894 T AT 99942894T AT E251613 T1 ATE251613 T1 AT E251613T1
- Authority
- AT
- Austria
- Prior art keywords
- group
- bond
- formula
- ring system
- conh
- Prior art date
Links
- 201000001320 Atherosclerosis Diseases 0.000 title abstract 2
- VTGOHKSTWXHQJK-UHFFFAOYSA-N pyrimidin-2-ol Chemical class OC1=NC=CC=N1 VTGOHKSTWXHQJK-UHFFFAOYSA-N 0.000 title 1
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 abstract 2
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 2
- 125000002950 monocyclic group Chemical group 0.000 abstract 2
- 125000003837 (C1-C20) alkyl group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- -1 CR15R16 Chemical group 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 abstract 1
- 150000008318 pyrimidones Chemical class 0.000 abstract 1
- 150000003839 salts Chemical group 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
- 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
- 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
-
- 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
- C07D401/14—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 three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9818375.9A GB9818375D0 (en) | 1998-08-21 | 1998-08-21 | Novel compounds |
| GBGB9902009.1A GB9902009D0 (en) | 1999-01-29 | 1999-01-29 | Novel compounds |
| PCT/EP1999/006093 WO2000010980A1 (en) | 1998-08-21 | 1999-08-18 | Pyrimidinone derivatives for the treatment of atherosclerosis |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE251613T1 true ATE251613T1 (de) | 2003-10-15 |
Family
ID=26314252
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT99942894T ATE251613T1 (de) | 1998-08-21 | 1999-08-18 | Pyrimidinonderivate zur behandlung von atheroscleros |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US6559155B1 (de) |
| EP (1) | EP1105377B1 (de) |
| JP (1) | JP2002523402A (de) |
| AT (1) | ATE251613T1 (de) |
| DE (1) | DE69911980T2 (de) |
| WO (1) | WO2000010980A1 (de) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR0009739A (pt) | 1999-04-13 | 2002-04-09 | Basf Ag | Composto, medicamento, preparação farmacêutica, e, usos de um elemento estrutural, de um composto e de uma preparação farmacêutica |
| GB9910079D0 (en) * | 1999-05-01 | 1999-06-30 | Smithkline Beecham Plc | Novel compounds |
| DE60042286D1 (de) * | 1999-05-01 | 2009-07-09 | Smithkline Beecham Plc | Pyrimidinon Verbindungen |
| GB9910378D0 (en) * | 1999-05-05 | 1999-06-30 | Smithkline Beecham Plc | Novel compounds |
| DE60139429D1 (de) * | 2000-02-16 | 2009-09-10 | Smithkline Beecham Plc | Pyrimidin-5-Onderivate als LDL-PLA2 Inhibitoren |
| GB0024808D0 (en) | 2000-10-10 | 2000-11-22 | Smithkline Beecham Plc | Novel compounds |
| FR2815345B1 (fr) * | 2000-10-12 | 2002-12-13 | Servier Lab | Nouveaux derives de cyclobutene-dione, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| GB0119793D0 (en) * | 2001-08-14 | 2001-10-03 | Smithkline Beecham Plc | Novel compounds |
| 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 |
| 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 |
| BRPI0721697A2 (pt) | 2007-05-11 | 2014-08-05 | Univ Jefferson | " métodos para tratar e/ou prevenir uma doença ou distúrbio neurodegenerativo em um indivíduo, para tratar e/ou prevenir um indivíduo com ou em risco de demência vascular, para tratar e/ou prevenir uma doença ou distúrbio associado com uma barreira hematoencefálica anormal em um indivíduo, para diminuir o acúmulo beta amilóide no cérebro de um indivíduo, para tratar e/ou prevenir mal de alzheimer em um indivíduo e para prevenir ou reduzir o risco de desenvolver mal de alzhheimer, e, uso de um agente que inibe a expressão e/ou atividade da proteína lp-pla2." |
| US9029383B2 (en) | 2007-05-11 | 2015-05-12 | The Trustees Of The University Of Pennsylvania | Methods of treatment of skin ulcers |
| CA2759187A1 (en) * | 2009-04-03 | 2010-10-07 | Medisyn Technologies, Inc. | Compositions for treatment of alzheimer's disease |
| US8637536B2 (en) * | 2010-12-06 | 2014-01-28 | Glaxo Group Limited | Pyrimidinone compounds for use in the treatment of diseases or conditions mediated by Lp-PLA2 |
| WO2012075917A1 (en) * | 2010-12-06 | 2012-06-14 | Glaxo Group Limited | Compounds |
| EP2651403B1 (de) | 2010-12-17 | 2020-12-02 | Glaxo Group Limited | Verwendung von lp-pla2-inhibitoren zur behandlung und vorbeugung von augenerkrankungen |
| US9273054B2 (en) * | 2011-07-27 | 2016-03-01 | Glaxo Group Limited | Substituted pyrimido[1,6-a]pyrimidines as Lp-PLA2 inhibitors |
| EP2739627A4 (de) | 2011-07-27 | 2015-01-21 | Glaxo Group Ltd | 2,3-dihydroimidazo-[1,2-c-] pyrimidin-5 (1h)-on-verbindungen als lp-pla²- inhibitoren |
| CA2899124A1 (en) | 2013-01-25 | 2014-07-31 | 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 |
| WO2014114694A1 (en) | 2013-01-25 | 2014-07-31 | Glaxosmithkline Intellectual Property Development Limited | 2,3-dihydroimidazol[1,2-c]pyrimidin-5(1h)-one based lipoprotein-associated phospholipase a2 (lp-pla2) inhibitors |
| 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 |
| CN114805389B (zh) | 2019-11-09 | 2023-08-29 | 上海赛默罗生物科技有限公司 | 三环二氢咪唑并嘧啶酮衍生物、其制备方法、药物组合物和用途 |
| 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 |
| WO2024196698A2 (en) * | 2023-03-17 | 2024-09-26 | Curadh Mtr | Compounds and constructs useful for targeting fibroblast activation protein |
| JP2026516205A (ja) | 2023-04-18 | 2026-05-20 | サイニューロ セラピューティクス インコーポレイテッド | Lp-pla2阻害剤と第2の薬剤の併用治療 |
| CN118221687B (zh) | 2023-07-17 | 2024-12-31 | 上海枢境生物科技有限公司 | 双环[5,6]咪唑嘧啶酮类衍生物、其制备方法和应用 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4145546A (en) | 1975-10-02 | 1979-03-20 | Smith Kline & French Laboratories Limited | 4-Pyrimidone compounds |
| US4154834A (en) | 1975-12-29 | 1979-05-15 | Smith Kline & French Laboratories Limited | Substituted isocytosines having histamine H2 -antagonist activity |
| WO1999024420A1 (en) * | 1997-11-06 | 1999-05-20 | Smithkline Beecham Plc | Pyrimidinone compounds and pharmaceutical compositions containing them |
-
1999
- 1999-08-18 DE DE69911980T patent/DE69911980T2/de not_active Expired - Fee Related
- 1999-08-18 AT AT99942894T patent/ATE251613T1/de not_active IP Right Cessation
- 1999-08-18 US US09/763,492 patent/US6559155B1/en not_active Expired - Fee Related
- 1999-08-18 JP JP2000566254A patent/JP2002523402A/ja active Pending
- 1999-08-18 EP EP99942894A patent/EP1105377B1/de not_active Expired - Lifetime
- 1999-08-18 WO PCT/EP1999/006093 patent/WO2000010980A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| JP2002523402A (ja) | 2002-07-30 |
| DE69911980D1 (de) | 2003-11-13 |
| US6559155B1 (en) | 2003-05-06 |
| WO2000010980A1 (en) | 2000-03-02 |
| EP1105377A1 (de) | 2001-06-13 |
| EP1105377B1 (de) | 2003-10-08 |
| DE69911980T2 (de) | 2004-09-09 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |