EA201171448A1 - Производные изохинолин-1(2h)-она в качестве ингибиторов parp-1 - Google Patents

Производные изохинолин-1(2h)-она в качестве ингибиторов parp-1

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Publication number
EA201171448A1
EA201171448A1 EA201171448A EA201171448A EA201171448A1 EA 201171448 A1 EA201171448 A1 EA 201171448A1 EA 201171448 A EA201171448 A EA 201171448A EA 201171448 A EA201171448 A EA 201171448A EA 201171448 A1 EA201171448 A1 EA 201171448A1
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Prior art keywords
compounds
parp
methods
diseases
adp
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EA201171448A
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EA023112B1 (ru
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Джанлука Мариано Энрико Папео
Джей Аарон Бертран
Джованни Черви
Барбара Форте
Розита Лупи
Алессия Монтаньоли
Алессандра Сколаро
Фабио Дзуккотто
Паоло Орсини
Элена Постери
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НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л.
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Application filed by НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. filed Critical НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л.
Publication of EA201171448A1 publication Critical patent/EA201171448A1/ru
Publication of EA023112B1 publication Critical patent/EA023112B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • C07D217/24—Oxygen atoms
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/18—Ring systems of four or more rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
    • Y10T436/00—Chemistry: analytical and immunological testing
    • Y10T436/14—Heterocyclic carbon compound [i.e., O, S, N, Se, Te, as only ring hetero atom]
    • Y10T436/145555—Hetero-N

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Изобретение относится к замещенным производным изохинолин-1(2Н)-она, которые избирательно ингибируют активность поли(АДФ-рибоза)полимеразы PARP-1 относительно поли(АДФ-рибоза)полимеразы PARP-2. В связи с этим соединения согласно настоящему изобретению являются пригодными в лечении заболеваний, таких как рак, сердечно-сосудистые заболевания, повреждение центральной нервной системы и различные формы воспаления. Настоящее изобретение также относится к способам получения указанных соединений, фармацевтическим композициям, содержащим указанные соединения, и способам лечения заболеваний с использованием фармацевтических композиций, содержащих указанные соединения. Скрининг-метод для идентификации соединений, способных связываться с некоторыми белками PARP, а также зонды, используемые в таких методах, являются предметами изобретения.
EA201171448A 2009-05-21 2010-05-19 Производные изохинолин-1(2h)-она в качестве ингибиторов parp-1, способы их получения, фармацевтическая композиция на их основе и применение EA023112B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09160869 2009-05-21
PCT/EP2010/056921 WO2010133647A1 (en) 2009-05-21 2010-05-19 Isoquinolin-1 (2h) -one derivatives as parp-1 inhibitors

Publications (2)

Publication Number Publication Date
EA201171448A1 true EA201171448A1 (ru) 2012-06-29
EA023112B1 EA023112B1 (ru) 2016-04-29

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ID=42372343

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EA201171448A EA023112B1 (ru) 2009-05-21 2010-05-19 Производные изохинолин-1(2h)-она в качестве ингибиторов parp-1, способы их получения, фармацевтическая композиция на их основе и применение

Country Status (16)

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US (2) US8592416B2 (ru)
EP (1) EP2432765B1 (ru)
JP (1) JP5731486B2 (ru)
CN (1) CN102438986B (ru)
AR (1) AR076688A1 (ru)
AU (1) AU2010251112B2 (ru)
BR (1) BRPI1011046B1 (ru)
CA (1) CA2762226C (ru)
CL (1) CL2011002925A1 (ru)
DK (1) DK2432765T3 (ru)
EA (1) EA023112B1 (ru)
ES (1) ES2568936T3 (ru)
HK (1) HK1166076A1 (ru)
MX (1) MX2011012187A (ru)
TW (1) TWI499418B (ru)
WO (1) WO2010133647A1 (ru)

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TWI499418B (zh) 2009-05-21 2015-09-11 Nerviano Medical Sciences Srl 異喹啉－１（２ｈ）－酮衍生物
FR2956816B1 (fr) * 2010-03-01 2012-05-18 Univ Joseph Fourier Utilisation de quinolones pour la preparation de medicaments, nouvelles quinolones et leur procede de synthese
EP2736896B1 (en) 2011-07-26 2016-12-14 Nerviano Medical Sciences S.r.l. 3-oxo-2,3-dihydro-1h-indazole-4-carboxamide derivatives as parp-1 inhibitors
EA027800B1 (ru) * 2011-11-25 2017-09-29 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Производные 3-фенилизохинолин-1(2h)-она в качестве ингибиторов parp-1
ES2611504T3 (es) 2012-03-07 2017-05-09 Institute Of Cancer Research: Royal Cancer Hospital (The) Compuestos de isoquinolin-1-ona 3-aril-5-sustituida y sus usos terapéuticos
RU2654216C2 (ru) 2012-08-08 2018-05-17 Мерк Патент Гмбх Производные (аза-)изохинолинона
US9388142B2 (en) 2012-09-26 2016-07-12 Merck Patent Gmbh Quinazolinone derivatives as PARP inhibitors
WO2014055311A1 (en) * 2012-10-01 2014-04-10 Merck Sharp & Dohme Corp. Substituted isoquinolines as crth2 receptor modulators
US10385018B2 (en) 2012-10-26 2019-08-20 Nerviano Medical Sciences S.R.L. 4-carboxamido-isoindolinone derivatives as selective PARP-1 inhibitors
CN105722835B (zh) * 2013-09-11 2018-07-31 癌症研究协会:皇家癌症医院 3-芳基-5-取代的-异喹啉-1-酮化合物及它们的疗法应用
US11261466B2 (en) 2015-03-02 2022-03-01 Sinai Health System Homologous recombination factors
WO2017174879A1 (en) 2016-04-06 2017-10-12 University Of Oulu Compounds for use in the treatment of cancer
CN106083716B (zh) * 2016-06-07 2018-10-30 温州医科大学仁济学院 一种3-芳基异喹啉化合物的制备方法
US9891509B2 (en) 2016-06-17 2018-02-13 Mimono LLC Projector holder
US10899733B2 (en) 2017-08-23 2021-01-26 Oregon Health & Science University Inhibitors of PARPs that catalyze mono-ADP-ribosylation
CN113549044B (zh) * 2021-07-23 2024-01-23 中国药科大学 8-氮杂环取代色酮类衍生物及其制备方法与制药用途
WO2023242302A1 (en) 2022-06-15 2023-12-21 Astrazeneca Ab Combination therapy for treating cancer

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JPS59116269A (ja) * 1982-12-24 1984-07-05 Nisshin Flour Milling Co Ltd イソカルボスチリル誘導体
JPS60237070A (ja) * 1984-05-08 1985-11-25 Nisshin Flour Milling Co Ltd 光学活性イソカルボスチリル誘導体の製法
DE69019774T2 (de) 1989-03-28 1995-11-09 Nisshin Flour Milling Co Isochinolin-Derivate zur Behandlung des Glaukoms oder der okulären Hypertonie.
JP3141051B2 (ja) 1992-10-09 2001-03-05 日清製粉株式会社 抗動脈硬化剤
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US6664269B2 (en) * 2001-05-08 2003-12-16 Maybridge Plc Isoquinolinone derivatives
ATE552252T1 (de) * 2002-10-01 2012-04-15 Mitsubishi Tanabe Pharma Corp Isochinolinverbindungen und deren medizinische verwendung
JP4567460B2 (ja) * 2002-11-22 2010-10-20 田辺三菱製薬株式会社 イソキノリン化合物及びその医薬用途
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TWI499418B (zh) 2009-05-21 2015-09-11 Nerviano Medical Sciences Srl 異喹啉－１（２ｈ）－酮衍生物

Also Published As

Publication number Publication date
ES2568936T3 (es) 2016-05-05
MX2011012187A (es) 2012-01-27
AU2010251112A2 (en) 2012-02-02
EP2432765B1 (en) 2016-03-02
DK2432765T3 (en) 2016-04-25
JP5731486B2 (ja) 2015-06-10
TW201043232A (en) 2010-12-16
JP2012527428A (ja) 2012-11-08
CA2762226A1 (en) 2010-11-25
CN102438986A (zh) 2012-05-02
US20120157454A1 (en) 2012-06-21
AU2010251112B2 (en) 2015-11-12
US20140045846A1 (en) 2014-02-13
EA023112B1 (ru) 2016-04-29
CN102438986B (zh) 2015-07-01
US8993594B2 (en) 2015-03-31
US8592416B2 (en) 2013-11-26
BRPI1011046B1 (pt) 2020-02-27
CA2762226C (en) 2017-12-05
CL2011002925A1 (es) 2012-04-13
HK1166076A1 (en) 2012-10-19
AU2010251112A1 (en) 2012-01-19
EP2432765A1 (en) 2012-03-28
TWI499418B (zh) 2015-09-11
BRPI1011046A2 (pt) 2016-03-15
WO2010133647A1 (en) 2010-11-25
AR076688A1 (es) 2011-06-29

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