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

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)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2899091A1 (en) 2013-01-25 2014-07-31 Glaxosmithkline Intellectual Property Development Limited Compounds
CA2970537C (en) 2014-07-22 2023-02-21 Glaxosmithkline Intellectual Property Development Limited Tricyclic imidazo-pyrimidinone compounds for the mediation of lipoprotein-associated phospholipase a2
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, METHOD FOR THE PRODUCTION THEREOF, 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
WO2024027116A1 (en) * 2022-08-04 2024-02-08 4B Technologies (Beijing) Co., Limited Dihydroimidazo-pyrimidinone compounds as lp-pla2 inhibitors and use thereof

Family Cites Families (48)

* Cited by examiner, † Cited by third party
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
BR9510420A (pt) 1994-12-22 2004-04-20 Smithkline Beecham Plc Azetidin-2-onas substituìdas para o tratamento de aterosclerose
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
JP2002515728A (ja) 1995-09-29 2002-05-28 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー 新規用途
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
EP0915843A1 (en) 1996-04-26 1999-05-19 Smithkline Beecham Plc Azetidinone derivatives for the treatment of atheroscleroses
GB9608649D0 (en) 1996-04-26 1996-07-03 Smithkline Beecham Plc 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
GB9626616D0 (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
US6559155B1 (en) 1998-08-21 2003-05-06 Smithkline Beecham P.L.C. Pyrimidinone derivatives for the treatment of atherosclerosis
CA2371671A1 (en) 1999-05-01 2000-11-09 Smithkline Beecham Plc Pyrimidinone compounds
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
DK1263740T3 (da) 2000-02-16 2006-11-13 Smithkline Beecham Plc Pyrimidin-4-on-derivat som LDL-PLA2-inhibitor
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
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
GB0127143D0 (en) 2001-11-10 2002-01-02 Smithkline Beecham Novel compounds
GB0127140D0 (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
CA2530816A1 (en) 2003-07-02 2005-01-13 Bayer Healthcare Ag Amide-substituted 1,2,4-triazin-5(2h)-ones for the treatment of chronic inflammatory diseases
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
US20080090852A1 (en) 2006-10-13 2008-04-17 Colin Andrew Leach 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
US8338437B2 (en) 2007-02-28 2012-12-25 Methylgene Inc. Amines as small molecule inhibitors
US20080279846A1 (en) 2007-05-11 2008-11-13 Thomas Jefferson University Methods of treatment and prevention of neurodegenerative diseases and disorders
US9029383B2 (en) 2007-05-11 2015-05-12 The Trustees Of The University Of Pennsylvania Methods of treatment of skin ulcers
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
EP2619203A4 (en) * 2010-09-20 2014-04-16 Glaxo Group Ltd TRICYCLIC COMPOUNDS, PROCESS FOR THEIR PREPARATION AND APPLICATIONS THEREOF
EP2649050A4 (en) * 2010-12-06 2014-04-23 Glaxo Group Ltd LINKS
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
BR112014001665A2 (pt) * 2011-07-27 2017-02-14 Glaxo Group Ltd compostos de 2,3-di-hidroimidazo[1,2-c]pirimidin-5(1h)-ona utilizados como inibidores de lp-plaz
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
CA2899091A1 (en) 2013-01-25 2014-07-31 Glaxosmithkline Intellectual Property Development Limited Compounds

Also Published As

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

Similar Documents

Publication Publication Date Title
PE20151251A1 (es) Derivados [5,6] biciclicos de imidazo pirimidona con actividad sobre enzimas lp-pla2
PE20152033A1 (es) Heterociclos bicicliclos como inhibidores de fgfr
CO6390080A2 (es) Compuestos organicos
CL2010001486A1 (es) Compuestos derivados de [1,2,4]triazolo[1,5-a]piridina, inhibidores de jak; composicion farmaceutica; kit farmaceutico; su uso en el tratamiento de enfermedades tales como cancer, diabetes, enfermedad de alzheimer, enfermedad hepatica, trastornos del snc, entre otras.
CL2014001752A1 (es) Compuestos biciclicos sustituidos; composicion farmaceutica que los comprende; y uso en el tratamiento de enfermedades tales como cancer, alzheimer, sida, entre otras.
PE20141557A1 (es) Derivado de pirazoloquinolina
PE20120534A1 (es) PIRIMIDINAS FUSIONADAS COMO INHIBIDORES DE Akt
ECSP14007473A (es) COMPOSICIONES FARMACÉUTICAS DE 7-(6-(2-HIDROXIPROPAN-2-IL) PIRIDIN-3-IL)-1-( (TRANS)-4METOXICICLOHEXIL)-3, 4-DIHIDROPIRAZINO [2, 3-b] PIRAZIN-2 (1H)-ONA, UNA FORMA SÓLIDA DE LAS MISMAS Y MÉTODOS DE SU USO
CL2013000368A1 (es) Compuestos derivados de 6-cicloalquil-1,5-dihidro-pirazolo(3,4-d) pirimidin-4-ona, inhibidores de fosfodiesterasa 9a pde9a; composicion farmaceutica que comprende a uno de los compuestos; y uso de los compuestos y la composicion farmaceutica en la preparacion de un medicamento util en el tratamiento de enfermedades del snc.
CR20160076A (es) NUEVOS DERIVADOS DE TRIAZOLO[4,5-d]PIRIMIDINA
AR101261A1 (es) Compuesto de tetrahidropirrolo[1,2:3,4]imidazo[1,2-c]pirimidin-1(6h)-ona y composición farmacéutica que lo comprende
CL2008001374A1 (es) Compuestos derivados de pirazolo pirimidinas, inhibidores de pde9; composicion farmaceutica que comprende a dichos compuetos; utiles en el tratamiento de un trastorno neurodegenerativo y cognitivo tal como la enfermedad de alzheimer y esquizofrenia.
EA201170771A1 (ru) Органические соединения
EA201270498A1 (ru) 8-этил-6-(арил)пиридо[2,3-d]пиримидин-7(8h)-оны для лечения заболеваний цнс
BR112014028395A2 (pt) derivados 3,4-di-hidro-2h-pirido[1,2-a] pirazina-1,6-diona substituídos úteis para o tratamento de (inter alia) doença de alzheimer
BR112014001665A2 (pt) compostos de 2,3-di-hidroimidazo[1,2-c]pirimidin-5(1h)-ona utilizados como inibidores de lp-plaz
GT201400213A (es) Inhibidores de diacilglicerol aciltransferasa 2
DOP2013000130A (es) Compuestos de pirimidinona para uso en el tratamiento de las enfermedades o condiciones mediada por lp - pla2
PE20090944A1 (es) PIRIMIDINAS BICICLICAS FUSIONADAS COMO INHIBIDORES DE LA VIA Pi3K/AKT
PE20151748A1 (es) Inhibidores de bace1
EA201500654A1 (ru) Терапевтически активные производные пиразолопиримидина
PE20170683A1 (es) Triazolo[4,5-d]pirimidinas como agonistas del receptor canabinoide 2
HRP20182021T1 (hr) Derivati [1,2,4]triazolo[1,5-a]pirimidina kao inhibitori proteazoma protozoe za liječenje parazitskih bolesti poput lišmenijaze
BR112015007503A2 (pt) derivados de oxazolina terapeuticamente ativos
MA46690A (fr) Composés de [1,2,4]triazolo [1,5-a]pyrimidine en tant qu'inhibiteurs de pde2

Legal Events

Date Code Title Description
FD Application declared void or lapsed