AU2014209949B2 - 2,3-dihydroimidazol(1,2-c)pyrimidin-5(1h)-one based lipoprotein-associated phospholipase a2 (Lp-PLA2) inhibitors - Google Patents
2,3-dihydroimidazol(1,2-c)pyrimidin-5(1h)-one based lipoprotein-associated phospholipase a2 (Lp-PLA2) inhibitors Download PDFInfo
- Publication number
- AU2014209949B2 AU2014209949B2 AU2014209949A AU2014209949A AU2014209949B2 AU 2014209949 B2 AU2014209949 B2 AU 2014209949B2 AU 2014209949 A AU2014209949 A AU 2014209949A AU 2014209949 A AU2014209949 A AU 2014209949A AU 2014209949 B2 AU2014209949 B2 AU 2014209949B2
- Authority
- AU
- Australia
- Prior art keywords
- pyrimidin
- oxy
- dihydroimidazo
- esi
- mmol
- Prior art date
- Legal status (The legal status 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 status listed.)
- Ceased
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Epidemiology (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013070976 | 2013-01-25 | ||
| CNPCT/CN2013/070976 | 2013-01-25 | ||
| CNPCT/CN2013/001556 | 2013-12-12 | ||
| CN2013001556 | 2013-12-12 | ||
| PCT/EP2014/051286 WO2014114694A1 (en) | 2013-01-25 | 2014-01-23 | 2,3-dihydroimidazol[1,2-c]pyrimidin-5(1h)-one based lipoprotein-associated phospholipase a2 (lp-pla2) inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2014209949A1 AU2014209949A1 (en) | 2015-07-30 |
| AU2014209949B2 true AU2014209949B2 (en) | 2016-09-08 |
Family
ID=50002724
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2014209949A Ceased AU2014209949B2 (en) | 2013-01-25 | 2014-01-23 | 2,3-dihydroimidazol(1,2-c)pyrimidin-5(1h)-one based lipoprotein-associated phospholipase a2 (Lp-PLA2) inhibitors |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US9708330B2 (enExample) |
| EP (1) | EP2948452B1 (enExample) |
| JP (1) | JP6306053B2 (enExample) |
| KR (1) | KR20150108897A (enExample) |
| CN (1) | CN105008368B (enExample) |
| AU (1) | AU2014209949B2 (enExample) |
| BR (1) | BR112015017759B1 (enExample) |
| CA (1) | CA2899091A1 (enExample) |
| CL (1) | CL2015002060A1 (enExample) |
| CR (1) | CR20150390A (enExample) |
| EA (1) | EA025885B1 (enExample) |
| ES (1) | ES2642762T3 (enExample) |
| HK (1) | HK1216425A1 (enExample) |
| IL (1) | IL240046A0 (enExample) |
| MA (1) | MA38284B1 (enExample) |
| MX (1) | MX2015009633A (enExample) |
| PE (1) | PE20151251A1 (enExample) |
| PH (1) | PH12015501586A1 (enExample) |
| SG (1) | SG11201505520WA (enExample) |
| TW (1) | TW201443054A (enExample) |
| UY (1) | UY35276A (enExample) |
| WO (1) | WO2014114694A1 (enExample) |
| ZA (1) | ZA201505025B (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201443054A (zh) | 2013-01-25 | 2014-11-16 | Glaxosmithkline Ip Dev Ltd | 化合物 |
| 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 |
| JP6625604B2 (ja) * | 2014-07-22 | 2019-12-25 | 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 | 化合物 |
| CN104892459A (zh) * | 2015-06-16 | 2015-09-09 | 苏州明锐医药科技有限公司 | 利奥西呱中间体及其制备方法 |
| CN112574221B (zh) * | 2019-09-30 | 2022-03-04 | 上海纽思克生物科技有限公司 | 四环嘧啶酮类化合物、其制备方法、其组合物和用途 |
| IL292668A (en) * | 2019-11-09 | 2022-07-01 | Shanghai Simr Biotechnology Co Ltd | A tricyclic derivative of dihydroimidazopyrimidone, its preparation method, pharmaceutical preparation and its use |
| CN111533699B (zh) * | 2020-05-27 | 2023-12-01 | 龙曦宁（上海）医药科技有限公司 | 一种2-（三氟甲基）嘧啶-5-醇的合成方法 |
| CN113861220B (zh) * | 2020-06-30 | 2023-06-16 | 上海纽思克生物科技有限公司 | 三环嘧啶酮类化合物、其制备方法、其组合物和用途 |
| CN113912622B (zh) * | 2020-07-10 | 2023-12-01 | 上海纽思克生物科技有限公司 | 三环嘧啶酮类化合物、其制备方法、其组合物和用途 |
| 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 |
| CN114057740B (zh) * | 2021-12-15 | 2024-04-02 | 上海赛默罗生物科技有限公司 | 螺环嘧啶酮衍生物、其制备方法、药物组合物和用途 |
| EP4565587A1 (en) * | 2022-08-04 | 2025-06-11 | 4B Technologies (Beijing) Co., Limited | Dihydroimidazo-pyrimidinone compounds as lp-pla2 inhibitors and use thereof |
| CN116925023B (zh) * | 2023-07-18 | 2025-11-21 | 江苏桐孚高新材料有限公司 | 2-全氟烷基-4h-吡喃-4-酮衍生物的改进合成方法 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012037782A1 (en) * | 2010-09-20 | 2012-03-29 | Glaxo Group Limited | Tricyclic compounds, preparation methods, and their uses |
Family Cites Families (47)
| Publication number | Priority date | Publication date | Assignee | Title |
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| WO1993018035A1 (en) | 1992-03-04 | 1993-09-16 | Abbott Laboratories | Angiotensin ii receptor antagonists |
| GB9421816D0 (en) | 1994-10-29 | 1994-12-14 | Smithkline Beecham Plc | Novel compounds |
| AR002012A1 (es) | 1994-12-22 | 1998-01-07 | Smithkline Beecham Plc | Un compuesto, una composicion farmaceutica que lo comprende, su uso, metodo de tratamiento terapeutico, metodo para la preparacion del compuesto. |
| 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. |
| CZ422197A3 (cs) | 1995-07-01 | 1998-06-17 | Smithkline Beecham Plc | Azetidinonové deriváty, způsob jejich přípravy, meziprodukty tohoto postupu, farmaceutický prostředek obsahující tyto sloučeniny a použití těchto sloučenin jako léčiv |
| EP0859834A2 (en) | 1995-09-29 | 1998-08-26 | 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 |
| WO1997021675A1 (en) | 1995-12-08 | 1997-06-19 | Smithkline Beecham Plc | Monocyclic beta-lactame derivatives for treatment of atherosclerosis |
| 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. |
| GB9626536D0 (en) | 1996-12-20 | 1997-02-05 | Symphar Sa | 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 |
| DE69816471T2 (de) | 1997-11-06 | 2004-05-27 | Smithkline Beecham P.L.C., Brentford | Pyrimidinon verbindungen und diese enthaltende pharmazeutische zusammenstellungen |
| EP1105377B1 (en) | 1998-08-21 | 2003-10-08 | SmithKline Beecham plc | Pyrimidinone derivatives for the treatment of atherosclerosis |
| ES2233361T3 (es) | 1999-05-01 | 2005-06-16 | Smithkline Beecham Plc | Compuestos de piridinona. |
| 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 |
| JP3757703B2 (ja) | 1999-09-22 | 2006-03-22 | 凸版印刷株式会社 | 再封可能な開口維持部材付パウチ |
| ES2330552T3 (es) | 2000-02-16 | 2009-12-11 | Smithkline Beecham Plc | Derivados de pirimidin-5-ona como inhibidores de ldl-pla2. |
| 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 |
| 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 |
| GB0127141D0 (en) | 2001-11-10 | 2002-01-02 | Smithkline Beecham Plc | Novel compounds |
| GB0127140D0 (en) | 2001-11-10 | 2002-01-02 | Smithkline Beecham | Novel compounds |
| GB0127139D0 (en) | 2001-11-10 | 2002-01-02 | Smithkline Beecham | Novel compounds |
| 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 |
| WO2005003118A1 (de) | 2003-07-02 | 2005-01-13 | Bayer Healthcare Ag | Amid-substituierte 1,2,4-triazin-5 (2h)-one zur behandlung von chronisch inflammatorischen krankheiten |
| DE102004061009A1 (de) | 2004-12-18 | 2006-06-22 | Bayer Healthcare Ag | Substituierte 1,2,4-Triazin-5(2H)-one |
| DE102004061008A1 (de) | 2004-12-18 | 2006-06-22 | Bayer Healthcare Ag | 3-Arylalkyl- und 3-Heteroarylalkyl-substituierte 1,2,4-Triazin-5(2H)-one |
| EP2083625A4 (en) * | 2006-10-13 | 2011-10-19 | Glaxo Group Ltd | BICYCLIC HETOROAROMATIC COMPOUNDS |
| 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 |
| WO2008104077A1 (en) | 2007-02-28 | 2008-09-04 | Methylgene Inc. | Small molecule inhibitors of protein arginine methyltransferases (prmts) |
| BRPI0810336A2 (pt) | 2007-05-11 | 2019-03-19 | The Trustees Of The University Of Pennsylvania | "método para tratar e/ou prevenir úlceras de pele em um indivíduo" |
| US20080279846A1 (en) | 2007-05-11 | 2008-11-13 | Thomas Jefferson University | Methods of treatment and prevention of neurodegenerative diseases and disorders |
| US8962633B2 (en) | 2007-05-11 | 2015-02-24 | Thomas Jefferson University | Methods of treatment and prevention of metabolic bone diseases and disorders |
| JP2011088847A (ja) * | 2009-10-21 | 2011-05-06 | Takeda Chem Ind Ltd | 三環性化合物およびその用途 |
| EP2649050A4 (en) * | 2010-12-06 | 2014-04-23 | Glaxo Group Ltd | LINKS |
| EP2651403B1 (en) | 2010-12-17 | 2020-12-02 | Glaxo Group Limited | Use of lp-pla2 inhibitors in the treatment and prevention of eye diseases |
| JP2014521611A (ja) * | 2011-07-27 | 2014-08-28 | グラクソ グループ リミテッド | Ｌｐ−ＰＬＡ２阻害剤としての２，３−ジヒドロイミダゾ［１，２−ｃ］ピリミジン−５（１Ｈ）−オン化合物の使用 |
| 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 |
| TW201443054A (zh) | 2013-01-25 | 2014-11-16 | Glaxosmithkline Ip Dev Ltd | 化合物 |
-
2014
- 2014-01-23 TW TW103102388A patent/TW201443054A/zh unknown
- 2014-01-23 AU AU2014209949A patent/AU2014209949B2/en not_active Ceased
- 2014-01-23 ES ES14701355.1T patent/ES2642762T3/es active Active
- 2014-01-23 UY UY0001035276A patent/UY35276A/es not_active Application Discontinuation
- 2014-01-23 US US14/761,636 patent/US9708330B2/en not_active Expired - Fee Related
- 2014-01-23 HK HK16104389.3A patent/HK1216425A1/zh unknown
- 2014-01-23 EP EP14701355.1A patent/EP2948452B1/en active Active
- 2014-01-23 BR BR112015017759-0A patent/BR112015017759B1/pt not_active IP Right Cessation
- 2014-01-23 JP JP2015554138A patent/JP6306053B2/ja not_active Expired - Fee Related
- 2014-01-23 KR KR1020157022396A patent/KR20150108897A/ko not_active Ceased
- 2014-01-23 EA EA201591379A patent/EA025885B1/ru not_active IP Right Cessation
- 2014-01-23 WO PCT/EP2014/051286 patent/WO2014114694A1/en not_active Ceased
- 2014-01-23 CN CN201480013675.8A patent/CN105008368B/zh not_active Expired - Fee Related
- 2014-01-23 SG SG11201505520WA patent/SG11201505520WA/en unknown
- 2014-01-23 MA MA38284A patent/MA38284B1/fr unknown
- 2014-01-23 MX MX2015009633A patent/MX2015009633A/es unknown
- 2014-01-23 PE PE2015001537A patent/PE20151251A1/es not_active Application Discontinuation
- 2014-01-23 CA CA2899091A patent/CA2899091A1/en not_active Abandoned
-
2015
- 2015-07-13 ZA ZA2015/05025A patent/ZA201505025B/en unknown
- 2015-07-20 IL IL240046A patent/IL240046A0/en unknown
- 2015-07-20 PH PH12015501586A patent/PH12015501586A1/en unknown
- 2015-07-23 CL CL2015002060A patent/CL2015002060A1/es unknown
- 2015-07-24 CR CR20150390A patent/CR20150390A/es unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012037782A1 (en) * | 2010-09-20 | 2012-03-29 | Glaxo Group Limited | Tricyclic compounds, preparation methods, and their uses |
Also Published As
| Publication number | Publication date |
|---|---|
| EP2948452A1 (en) | 2015-12-02 |
| PH12015501586A1 (en) | 2015-10-05 |
| CN105008368B (zh) | 2017-02-01 |
| EP2948452B1 (en) | 2017-08-09 |
| US9708330B2 (en) | 2017-07-18 |
| JP2016505058A (ja) | 2016-02-18 |
| US20150361082A1 (en) | 2015-12-17 |
| HK1216425A1 (zh) | 2016-11-11 |
| KR20150108897A (ko) | 2015-09-30 |
| CN105008368A (zh) | 2015-10-28 |
| TW201443054A (zh) | 2014-11-16 |
| JP6306053B2 (ja) | 2018-04-04 |
| ES2642762T3 (es) | 2017-11-20 |
| UY35276A (es) | 2014-08-29 |
| MX2015009633A (es) | 2015-11-30 |
| CA2899091A1 (en) | 2014-07-31 |
| EA201591379A1 (ru) | 2016-01-29 |
| BR112015017759B1 (pt) | 2022-05-24 |
| SG11201505520WA (en) | 2015-08-28 |
| IL240046A0 (en) | 2015-08-31 |
| CL2015002060A1 (es) | 2015-11-27 |
| MA38284A1 (fr) | 2017-12-29 |
| PE20151251A1 (es) | 2015-09-10 |
| CR20150390A (es) | 2015-10-19 |
| MA38284B1 (fr) | 2018-05-31 |
| EA025885B1 (ru) | 2017-02-28 |
| ZA201505025B (en) | 2017-08-30 |
| AU2014209949A1 (en) | 2015-07-30 |
| WO2014114694A1 (en) | 2014-07-31 |
| BR112015017759A2 (pt) | 2017-07-11 |
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| AU2012289492B2 (en) | 2,3-dihydroimidazo[1,2-c] pyrimidin-5(1H)-one compounds use as Lp-PLA2 inhibitors | |
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| CN104968665A (zh) | 作为lp-pla2抑制剂的双环嘧啶酮化合物 | |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) | ||
| MK14 | Patent ceased section 143(a) (annual fees not paid) or expired |