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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-pla2

Info

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
Application number
PE2015001537A
Other languages
English (en)
Inventor
Yingxia Sang
Zehong Wan
Qing Zhang
Original Assignee
Glaxosmithkline Ip Dev 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=50002724&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20151251(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Glaxosmithkline Ip Dev Ltd filed Critical Glaxosmithkline Ip Dev Ltd
Publication of PE20151251A1 publication Critical patent/PE20151251A1/es

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)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE [5,6] BICICLICOS DE IMIDAZO PIRIMIDONA DE FORMULA (I) DONDE R1, R2, R3, R4, R5 Y A SON TAL COMO SE DEFINEN EN LA DESCRIPCION. SON COMPUESTOS PREFERIDOS: (R)-7-((3,5-DIFLUORO-4-((2-(TRIFLUOROMETIL)PIRIDIN-4-IL)OXI)BENCIL)OXI)-2-METIL-2,3-DIHIDROIMIDAZO[1,2-c]PIRIMIDIN-5(1H)-ONA; 7-((3,5-DIFLUORO-4-((2-(TRIFLUOROMETIL)PIRIDIN-4-IL)OXI)BENCIL)OXI)-2,2-DIMETIL-2,3-DIHIDROIMIDAZO[1,2-c]PIRIMIDIN-5(1H)-ONA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS INHIBEN LA ACTIVIDAD DE LA FOSFOLIPASA A2 ASOCIADA A LAS LIPOPROTEINAS (LP-PLA2) SIENDO UTILES EN EL TRATAMIENTO DE ATEROSCLEROSIS, ENFERMEDAD DE ALZHEIMER
PE2015001537A 2013-01-25 2014-01-23 Derivados [5,6] biciclicos de imidazo pirimidona con actividad sobre enzimas lp-pla2 PE20151251A1 (es)

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 (es)
EP (1) EP2948452B1 (es)
JP (1) JP6306053B2 (es)
KR (1) KR20150108897A (es)
CN (1) CN105008368B (es)
AU (1) AU2014209949B2 (es)
BR (1) BR112015017759B1 (es)
CA (1) CA2899091A1 (es)
CL (1) CL2015002060A1 (es)
CR (1) CR20150390A (es)
EA (1) EA025885B1 (es)
ES (1) ES2642762T3 (es)
HK (1) HK1216425A1 (es)
IL (1) IL240046A0 (es)
MA (1) MA38284B1 (es)
MX (1) MX2015009633A (es)
PE (1) PE20151251A1 (es)
PH (1) PH12015501586A1 (es)
SG (1) SG11201505520WA (es)
TW (1) TW201443054A (es)
UY (1) UY35276A (es)
WO (1) WO2014114694A1 (es)
ZA (1) ZA201505025B (es)

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AU2014209949B2 (en) 2013-01-25 2016-09-08 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
US9783546B2 (en) 2014-07-22 2017-10-10 Glaxosmithkline Intellectual Property Development Limited Compounds
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
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
BR112022008786A2 (pt) * 2019-11-09 2022-07-26 Shanghai Simr Biotechnology Co Ltd Composto, composição, uso do composto ou da composição, e, método para tratar ou prevenir uma complicação diabética, doença relacionada à neuroinflamação ou aterosclerose
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
US20250154153A1 (en) * 2022-08-04 2025-05-15 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

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Also Published As

Publication number Publication date
US9708330B2 (en) 2017-07-18
JP6306053B2 (ja) 2018-04-04
MA38284B1 (fr) 2018-05-31
ES2642762T3 (es) 2017-11-20
MA38284A1 (fr) 2017-12-29
HK1216425A1 (zh) 2016-11-11
PH12015501586A1 (en) 2015-10-05
SG11201505520WA (en) 2015-08-28
CN105008368B (zh) 2017-02-01
IL240046A0 (en) 2015-08-31
CA2899091A1 (en) 2014-07-31
AU2014209949B2 (en) 2016-09-08
WO2014114694A1 (en) 2014-07-31
TW201443054A (zh) 2014-11-16
MX2015009633A (es) 2015-11-30
CN105008368A (zh) 2015-10-28
KR20150108897A (ko) 2015-09-30
EP2948452B1 (en) 2017-08-09
US20150361082A1 (en) 2015-12-17
JP2016505058A (ja) 2016-02-18
UY35276A (es) 2014-08-29
BR112015017759B1 (pt) 2022-05-24
CL2015002060A1 (es) 2015-11-27
EA201591379A1 (ru) 2016-01-29
BR112015017759A2 (pt) 2017-07-11
ZA201505025B (en) 2017-08-30
CR20150390A (es) 2015-10-19
EP2948452A1 (en) 2015-12-02
EA025885B1 (ru) 2017-02-28
AU2014209949A1 (en) 2015-07-30

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