PE20151251A1 - Derivados [5,6] biciclicos de imidazo pirimidona con actividad sobre enzimas lp-pla2 - Google Patents
Derivados [5,6] biciclicos de imidazo pirimidona con actividad sobre enzimas lp-pla2Info
- Publication number
- PE20151251A1 PE20151251A1 PE2015001537A PE2015001537A PE20151251A1 PE 20151251 A1 PE20151251 A1 PE 20151251A1 PE 2015001537 A PE2015001537 A PE 2015001537A PE 2015001537 A PE2015001537 A PE 2015001537A PE 20151251 A1 PE20151251 A1 PE 20151251A1
- Authority
- PE
- Peru
- Prior art keywords
- activity
- oxy
- bicyclic
- derivatives
- pyrimidone
- Prior art date
Links
- BOUNFBOFBGBYBT-UHFFFAOYSA-N purin-8-one Chemical compound C1=NC=NC2=NC(=O)N=C21 BOUNFBOFBGBYBT-UHFFFAOYSA-N 0.000 title abstract 2
- 102000004190 Enzymes Human genes 0.000 title 1
- 108090000790 Enzymes Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- SLRMQYXOBQWXCR-UHFFFAOYSA-N 2154-56-5 Chemical class [CH2]C1=CC=CC=C1 SLRMQYXOBQWXCR-UHFFFAOYSA-N 0.000 abstract 2
- WZKSXHQDXQKIQJ-UHFFFAOYSA-N F[C](F)F Chemical class F[C](F)F WZKSXHQDXQKIQJ-UHFFFAOYSA-N 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 102000004895 Lipoproteins Human genes 0.000 abstract 1
- 108090001030 Lipoproteins Proteins 0.000 abstract 1
- 102100037611 Lysophospholipase Human genes 0.000 abstract 1
- 108010058864 Phospholipases A2 Proteins 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
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)
- Epidemiology (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013070976 | 2013-01-25 | ||
| CN2013001556 | 2013-12-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20151251A1 true PE20151251A1 (es) | 2015-09-10 |
Family
ID=50002724
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2015001537A PE20151251A1 (es) | 2013-01-25 | 2014-01-23 | Derivados [5,6] biciclicos de imidazo pirimidona con actividad sobre enzimas lp-pla2 |
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 (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6306053B2 (ja) | 2013-01-25 | 2018-04-04 | 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 | ２，３−ジヒドロイミダゾール［１，２−ｃ］ピリミジン−５（１Ｈ）−オンに基づくリポタンパク質関連ホスホリパーゼＡ２（Ｌｐ−ＰＬＡ２）阻害剤 |
| KR20170034889A (ko) | 2014-07-22 | 2017-03-29 | 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 | 화합물 |
| 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 |
| 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 |
| EP4056571A4 (en) | 2019-11-09 | 2024-01-24 | Shanghai Simr Biotechnology Co., Ltd. | Tricyclic dihydroimidazopyrimidone derivative, preparation method therefor, pharmaceutical composition and use thereof |
| 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 |
| JP2025527291A (ja) * | 2022-08-04 | 2025-08-20 | ４ビー テクノロジーズ （ベイジン） カンパニー リミテッド | Ｌｐ－ＰＬＡ２阻害剤としてのジヒドロイミダゾピリミジノン化合物およびその使用 |
| WO2025015951A1 (zh) | 2023-07-17 | 2025-01-23 | 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 |
| 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 |
Family Cites Families (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| SK80397A3 (en) | 1994-12-22 | 1998-01-14 | Smithkline Beecham Plc | Substituted azetidin-2-ones, preparation method thereof, farmaceutical compositions and their use |
| 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. |
| AU708032B2 (en) | 1995-07-01 | 1999-07-29 | 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 |
| EP0869943A1 (en) | 1995-12-08 | 1998-10-14 | Smithkline Beecham Plc | Monocyclic beta-lactame derivatives for treatment of atherosclerosis |
| WO1997021676A1 (en) | 1995-12-08 | 1997-06-19 | Smithkline Beecham Plc | Azetidinone compounds for the treatment of atherosclerosis |
| NZ332476A (en) | 1996-04-26 | 2000-06-23 | Smithkline Beecham Plc | substituted 4-(carboxybenzylsulphinyl)-2-oxo-azetidine derivatives |
| 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 |
| 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 |
| BR0010220A (pt) | 1999-05-01 | 2002-05-14 | Smithkline Beecham Plc | Compostos de pirimidinona |
| 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 |
| SI1686119T1 (sl) | 2000-02-16 | 2009-12-31 | Smithkline Beecham Plc | Derivati pirimidin-5-ona kot inhibitorji ldl-pla2 |
| 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 |
| 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 |
| 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 |
| JP2010506852A (ja) | 2006-10-13 | 2010-03-04 | グラクソ グループ リミテッド | 二環式ヘテロ芳香族化合物 |
| 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 |
| US8338437B2 (en) | 2007-02-28 | 2012-12-25 | Methylgene Inc. | Amines as small molecule inhibitors |
| US8962633B2 (en) | 2007-05-11 | 2015-02-24 | Thomas Jefferson University | Methods of treatment and prevention of metabolic bone diseases and disorders |
| MX2009012197A (es) | 2007-05-11 | 2010-01-15 | Univ Pennsylvania | Metodos para tratamiento de ulceras en la piel. |
| US20080279846A1 (en) | 2007-05-11 | 2008-11-13 | Thomas Jefferson University | Methods of treatment and prevention of neurodegenerative 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 |
| JP2013537203A (ja) * | 2010-09-20 | 2013-09-30 | グラクソ グループ リミテッド | 三環式化合物、製造方法、およびそれらの使用 |
| JP2013544854A (ja) * | 2010-12-06 | 2013-12-19 | グラクソ グループ リミテッド | 化合物 |
| JP2013545792A (ja) | 2010-12-17 | 2013-12-26 | グラクソ グループ リミテッド | 眼疾患の処置および防止方法 |
| 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 |
| CA2842965A1 (en) * | 2011-07-27 | 2013-01-31 | Glaxo Group Limited | 2,3-dihydroimidazo[1,2-c] pyrimidin-5(1h)-one compounds use as lp-pla2 inhibitors |
| JP6306053B2 (ja) | 2013-01-25 | 2018-04-04 | 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 | ２，３−ジヒドロイミダゾール［１，２−ｃ］ピリミジン−５（１Ｈ）−オンに基づくリポタンパク質関連ホスホリパーゼＡ２（Ｌｐ−ＰＬＡ２）阻害剤 |
-
2014
- 2014-01-23 JP JP2015554138A patent/JP6306053B2/ja not_active Expired - Fee Related
- 2014-01-23 HK HK16104389.3A patent/HK1216425A1/zh unknown
- 2014-01-23 TW TW103102388A patent/TW201443054A/zh unknown
- 2014-01-23 EA EA201591379A patent/EA025885B1/ru not_active IP Right Cessation
- 2014-01-23 ES ES14701355.1T patent/ES2642762T3/es active Active
- 2014-01-23 MA MA38284A patent/MA38284B1/fr unknown
- 2014-01-23 SG SG11201505520WA patent/SG11201505520WA/en unknown
- 2014-01-23 KR KR1020157022396A patent/KR20150108897A/ko not_active Ceased
- 2014-01-23 WO PCT/EP2014/051286 patent/WO2014114694A1/en not_active Ceased
- 2014-01-23 CA CA2899091A patent/CA2899091A1/en not_active Abandoned
- 2014-01-23 EP EP14701355.1A patent/EP2948452B1/en active Active
- 2014-01-23 MX MX2015009633A patent/MX2015009633A/es unknown
- 2014-01-23 PE PE2015001537A patent/PE20151251A1/es not_active Application Discontinuation
- 2014-01-23 BR BR112015017759-0A patent/BR112015017759B1/pt not_active IP Right Cessation
- 2014-01-23 AU AU2014209949A patent/AU2014209949B2/en not_active Ceased
- 2014-01-23 CN CN201480013675.8A patent/CN105008368B/zh not_active Expired - Fee Related
- 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
-
2015
- 2015-07-13 ZA ZA2015/05025A patent/ZA201505025B/en unknown
- 2015-07-20 PH PH12015501586A patent/PH12015501586A1/en unknown
- 2015-07-20 IL IL240046A patent/IL240046A0/en unknown
- 2015-07-23 CL CL2015002060A patent/CL2015002060A1/es unknown
- 2015-07-24 CR CR20150390A patent/CR20150390A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| UY35276A (es) | 2014-08-29 |
| CL2015002060A1 (es) | 2015-11-27 |
| SG11201505520WA (en) | 2015-08-28 |
| AU2014209949B2 (en) | 2016-09-08 |
| CA2899091A1 (en) | 2014-07-31 |
| MA38284B1 (fr) | 2018-05-31 |
| US9708330B2 (en) | 2017-07-18 |
| EP2948452A1 (en) | 2015-12-02 |
| MX2015009633A (es) | 2015-11-30 |
| TW201443054A (zh) | 2014-11-16 |
| JP2016505058A (ja) | 2016-02-18 |
| BR112015017759A2 (pt) | 2017-07-11 |
| IL240046A0 (en) | 2015-08-31 |
| PH12015501586A1 (en) | 2015-10-05 |
| CN105008368A (zh) | 2015-10-28 |
| HK1216425A1 (zh) | 2016-11-11 |
| EA025885B1 (ru) | 2017-02-28 |
| EA201591379A1 (ru) | 2016-01-29 |
| EP2948452B1 (en) | 2017-08-09 |
| ZA201505025B (en) | 2017-08-30 |
| CN105008368B (zh) | 2017-02-01 |
| WO2014114694A1 (en) | 2014-07-31 |
| ES2642762T3 (es) | 2017-11-20 |
| MA38284A1 (fr) | 2017-12-29 |
| CR20150390A (es) | 2015-10-19 |
| BR112015017759B1 (pt) | 2022-05-24 |
| US20150361082A1 (en) | 2015-12-17 |
| KR20150108897A (ko) | 2015-09-30 |
| JP6306053B2 (ja) | 2018-04-04 |
| AU2014209949A1 (en) | 2015-07-30 |
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