CN103827118B - 双环嘧啶酮化合物 - Google Patents

双环嘧啶酮化合物 Download PDF

Info

Publication number
CN103827118B
CN103827118B CN201280045746.3A CN201280045746A CN103827118B CN 103827118 B CN103827118 B CN 103827118B CN 201280045746 A CN201280045746 A CN 201280045746A CN 103827118 B CN103827118 B CN 103827118B
Authority
CN
China
Prior art keywords
esi
pyrimido
retention time
chloro
methyl
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.)
Expired - Fee Related
Application number
CN201280045746.3A
Other languages
English (en)
Chinese (zh)
Other versions
CN103827118A (zh
Inventor
万泽红
龙凯
张晓敏
余海华
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Glaxo Group Ltd
Original Assignee
Glaxo Group Ltd
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
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Priority to CN201280045746.3A priority Critical patent/CN103827118B/zh
Publication of CN103827118A publication Critical patent/CN103827118A/zh
Application granted granted Critical
Publication of CN103827118B publication Critical patent/CN103827118B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • 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
    • 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
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (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)
CN201280045746.3A 2011-07-27 2012-07-25 双环嘧啶酮化合物 Expired - Fee Related CN103827118B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201280045746.3A CN103827118B (zh) 2011-07-27 2012-07-25 双环嘧啶酮化合物

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CNPCT/CN2011/077702 2011-07-27
CN2011077702 2011-07-27
CN201280045746.3A CN103827118B (zh) 2011-07-27 2012-07-25 双环嘧啶酮化合物
PCT/EP2012/064598 WO2013014185A1 (en) 2011-07-27 2012-07-25 Bicyclic pyrimidone compounds

Publications (2)

Publication Number Publication Date
CN103827118A CN103827118A (zh) 2014-05-28
CN103827118B true CN103827118B (zh) 2016-03-09

Family

ID=46579034

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201280045746.3A Expired - Fee Related CN103827118B (zh) 2011-07-27 2012-07-25 双环嘧啶酮化合物

Country Status (13)

Country Link
US (2) US9273054B2 (enExample)
EP (1) EP2736908A1 (enExample)
JP (1) JP2014521625A (enExample)
KR (1) KR20140059204A (enExample)
CN (1) CN103827118B (enExample)
AR (1) AR087309A1 (enExample)
AU (1) AU2012288865B2 (enExample)
BR (1) BR112014001634A2 (enExample)
CA (1) CA2843102A1 (enExample)
RU (1) RU2014107486A (enExample)
TW (1) TW201321382A (enExample)
UY (1) UY34216A (enExample)
WO (1) WO2013014185A1 (enExample)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9273054B2 (en) * 2011-07-27 2016-03-01 Glaxo Group Limited Substituted pyrimido[1,6-a]pyrimidines as Lp-PLA2 inhibitors
US20160029630A1 (en) 2012-11-27 2016-02-04 Basf Se Substituted 2-[phenoxy-phenyl]-1-[1,2,4]triazol-1-yl-ethanol compounds and their use as fungicides
US20150313229A1 (en) 2012-11-27 2015-11-05 Basf Se Substituted [1,2,4] Triazole Compounds
EP2925730A1 (en) 2012-11-27 2015-10-07 Basf Se Substituted 2-[phenoxy-phenyl]-1-[1,2,4]triazol-1-yl-ethanol compounds and their use as fungicides
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
CA2899124A1 (en) 2013-01-25 2014-07-31 Glaxosmithkline Intellectual Property Development Limited Compounds
US9630896B2 (en) 2013-11-22 2017-04-25 Tansna Therapeutics, Inc. 2,5-dialkyl-4-H/halo/ether-phenol compounds
EP3172211B1 (en) 2014-07-22 2019-07-03 GlaxoSmithKline Intellectual Property Development Limited Tricyclic imidazo-pyrimidinone derivatives for the treatment of diseases 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
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
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
CN106188063A (zh) * 2015-05-08 2016-12-07 中国科学院上海药物研究所 用作Lp-PLA2抑制剂的双环类化合物、其制备方法及医药用途
US20190092789A1 (en) * 2015-09-04 2019-03-28 Lysosomal Therapeutics Inc. Heterobicyclic pyrimidinone compounds and their use in the treatment of medical disorders
GB201522179D0 (en) * 2015-12-16 2016-01-27 Autifony Therapeutics Ltd Novel compounds
CN111868055B (zh) 2018-02-16 2024-03-08 勃林格殷格翰国际有限公司 Trpc6的抑制剂
CN108947782B (zh) * 2018-08-15 2021-08-24 上海罕道医药科技有限公司 一种溴氟多取代苯甲醛衍生物和制备方法
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
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
CN113666930B (zh) * 2020-05-13 2022-10-25 上海纽思克生物科技有限公司 桥环嘧啶酮类化合物、其制备方法、其组合物和用途
JP7595964B2 (ja) * 2020-05-13 2024-12-09 上海紐思克生物科技有限公司 架橋環状ピリミジノン類化合物、その製造方法、その組成物及び使用
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
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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1123028A (zh) * 1993-05-12 1996-05-22 纳幕尔杜邦公司 杀真菌的稠合双环嘧啶酮类化合物
WO2000010980A1 (en) * 1998-08-21 2000-03-02 Smithkline Beecham Plc Pyrimidinone derivatives for the treatment of atherosclerosis
CN101184758A (zh) * 2005-03-25 2008-05-21 葛兰素集团有限公司 新的化合物

Family Cites Families (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9421816D0 (en) 1994-10-29 1994-12-14 Smithkline Beecham Plc Novel compounds
WO1996019451A1 (en) 1994-12-22 1996-06-27 Smithkline Beecham Plc Substituted azetidin-2-ones for treatment of atherosclerosis
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.
HUP9901153A3 (en) 1995-07-01 1999-11-29 Smithkline Beecham Plc Azetidinone derivatives for the treatment of atherosclerosis, their production and pharmaceutical compositions containing them
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
EP0865429A1 (en) 1995-12-08 1998-09-23 Smithkline Beecham Plc Azetidinone compounds for the treatment of atherosclerosis
CZ341098A3 (cs) 1996-04-26 1999-03-17 Smithkline Beecham Plc Azetidinonové deriváty pro ošetřování aterosklerózy
GB9608649D0 (en) 1996-04-26 1996-07-03 Smithkline Beecham Plc Novel compounds
GB9626536D0 (en) 1996-12-20 1997-02-05 Symphar Sa Novel compounds
GB9626615D0 (en) 1996-12-20 1997-02-05 Symphar Sa Novel compounds
GB9626616D0 (en) 1996-12-20 1997-02-05 Symphar Sa Novel compounds
WO1999024420A1 (en) 1997-11-06 1999-05-20 Smithkline Beecham Plc Pyrimidinone compounds and pharmaceutical compositions containing them
DE60042286D1 (de) 1999-05-01 2009-07-09 Smithkline Beecham Plc Pyrimidinon Verbindungen
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
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
GB0024807D0 (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
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
EP1644353A1 (de) 2003-07-02 2006-04-12 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
WO2008048867A2 (en) 2006-10-13 2008-04-24 Glaxo Group Limited Bicyclic heteroaromatic compounds
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
US8962633B2 (en) 2007-05-11 2015-02-24 Thomas Jefferson University Methods of treatment and prevention of metabolic bone diseases and disorders
US9029383B2 (en) 2007-05-11 2015-05-12 The Trustees Of The University Of Pennsylvania Methods of treatment of skin ulcers
US20080279846A1 (en) 2007-05-11 2008-11-13 Thomas Jefferson University Methods of treatment and prevention of neurodegenerative diseases and disorders
US8022057B2 (en) * 2007-11-12 2011-09-20 Takeda Pharmaceutical Company Limited MAPK/ERK kinase inhibitors
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
US9273054B2 (en) * 2011-07-27 2016-03-01 Glaxo Group Limited Substituted pyrimido[1,6-a]pyrimidines as Lp-PLA2 inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1123028A (zh) * 1993-05-12 1996-05-22 纳幕尔杜邦公司 杀真菌的稠合双环嘧啶酮类化合物
WO2000010980A1 (en) * 1998-08-21 2000-03-02 Smithkline Beecham Plc Pyrimidinone derivatives for the treatment of atherosclerosis
CN101184758A (zh) * 2005-03-25 2008-05-21 葛兰素集团有限公司 新的化合物

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
"Preparation of imidazo[1,2-c]pyrimidinones from a chloropyrimidine and an electron poor ω-allylic amine";Frances Heaney,et al.;《Journal of the Chemical Society, Perkin Transaction 1》;19980101(第15期);第2255-2257页 *

Also Published As

Publication number Publication date
TW201321382A (zh) 2013-06-01
CA2843102A1 (en) 2013-01-31
AR087309A1 (es) 2014-03-12
BR112014001634A2 (pt) 2017-02-14
US9273054B2 (en) 2016-03-01
EP2736908A1 (en) 2014-06-04
US20130030012A1 (en) 2013-01-31
CN103827118A (zh) 2014-05-28
US20140179716A1 (en) 2014-06-26
UY34216A (es) 2013-02-28
WO2013014185A1 (en) 2013-01-31
RU2014107486A (ru) 2015-09-10
AU2012288865B2 (en) 2015-10-01
KR20140059204A (ko) 2014-05-15
JP2014521625A (ja) 2014-08-28
AU2012288865A1 (en) 2014-02-13

Similar Documents

Publication Publication Date Title
CN103827118A (zh) 双环嘧啶酮化合物
CN103827116B (zh) 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
CN105008368B (zh) 基于2,3‑二氢咪唑并[1,2‑c]嘧啶‑5(1H)‑酮的脂蛋白相关磷脂酶A2(Lp‑PLA2)抑制剂
CN106536521B (zh) 化合物
CN104968665A (zh) 作为lp-pla2抑制剂的双环嘧啶酮化合物
WO2012037782A1 (en) Tricyclic compounds, preparation methods, and their uses
CN104478812A (zh) 用于治疗由Lp-PLA2介导的疾病或病症的嘧啶酮化合物
IL292668A (en) A tricyclic derivative of dihydroimidazopyrimidone, its preparation method, pharmaceutical preparation and its use
JP2021521128A (ja) 二環式カルボキサミドおよびその使用方法
US9051325B2 (en) Bicyclic [5,6] imidazo pyrimodone compounds for use in the treatment of diseases or conditions mediated by Lp-PLA2

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20160309

Termination date: 20160725