RU2650107C2 - Производные хиназолинона в качестве ингибиторов parp - Google Patents

Производные хиназолинона в качестве ингибиторов parp Download PDF

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Publication number
RU2650107C2
RU2650107C2 RU2015115576A RU2015115576A RU2650107C2 RU 2650107 C2 RU2650107 C2 RU 2650107C2 RU 2015115576 A RU2015115576 A RU 2015115576A RU 2015115576 A RU2015115576 A RU 2015115576A RU 2650107 C2 RU2650107 C2 RU 2650107C2
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Prior art keywords
quinazolin
phenyl
methylethyl
fluoro
hydroxy
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RU2015115576A
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English (en)
Russian (ru)
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RU2015115576A (ru
Inventor
Дитер Дорш
Ханс-Петер Бухшталлер
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Мерк Патент Гмбх
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • 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
    • C07D401/10—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 carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • 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
    • C07D405/10—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 carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
RU2015115576A 2012-09-26 2013-08-27 Производные хиназолинона в качестве ингибиторов parp RU2650107C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12006707.9 2012-09-26
EP12006707 2012-09-26
PCT/EP2013/002577 WO2014048532A1 (en) 2012-09-26 2013-08-27 Quinazolinone derivatives as parp inhibitors

Publications (2)

Publication Number Publication Date
RU2015115576A RU2015115576A (ru) 2016-11-20
RU2650107C2 true RU2650107C2 (ru) 2018-04-09

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
RU2015115576A RU2650107C2 (ru) 2012-09-26 2013-08-27 Производные хиназолинона в качестве ингибиторов parp

Country Status (16)

Country Link
US (1) US9388142B2 (cg-RX-API-DMAC7.html)
EP (1) EP2900643B1 (cg-RX-API-DMAC7.html)
JP (1) JP6276769B2 (cg-RX-API-DMAC7.html)
KR (1) KR102200628B1 (cg-RX-API-DMAC7.html)
CN (1) CN104662006B (cg-RX-API-DMAC7.html)
AR (1) AR092670A1 (cg-RX-API-DMAC7.html)
AU (1) AU2013324681B2 (cg-RX-API-DMAC7.html)
BR (1) BR112015006524A8 (cg-RX-API-DMAC7.html)
CA (1) CA2886000C (cg-RX-API-DMAC7.html)
ES (1) ES2654464T3 (cg-RX-API-DMAC7.html)
IL (1) IL237840A (cg-RX-API-DMAC7.html)
MX (1) MX362855B (cg-RX-API-DMAC7.html)
RU (1) RU2650107C2 (cg-RX-API-DMAC7.html)
SG (1) SG11201502120XA (cg-RX-API-DMAC7.html)
WO (1) WO2014048532A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA201502838B (cg-RX-API-DMAC7.html)

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PL2794627T3 (pl) 2011-12-22 2019-04-30 Alios Biopharma Inc Podstawione nukleozydy, nukleotydy i ich analogi
CA2865511A1 (en) 2012-03-07 2013-09-12 Institute Of Cancer Research: Royal Cancer Hospital (The) 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use
US9441007B2 (en) 2012-03-21 2016-09-13 Alios Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
USRE48171E1 (en) 2012-03-21 2020-08-25 Janssen Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
EA027929B1 (ru) 2012-05-25 2017-09-29 Янссен Сайенсиз Айрлэнд Юси Нуклеозиды на основе урацила и спирооксетана
EA201590943A1 (ru) 2012-12-21 2016-01-29 Алиос Биофарма, Инк. Замещенные нуклеозиды, нуклеотиды и их аналоги
US9611223B2 (en) 2013-09-11 2017-04-04 Institute Of Cancer Research: Royal Cancer Hospital (The) 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use
CA2964113A1 (en) 2014-10-14 2016-04-21 La Jolla Institute Of Allergy & Immunology Inhibitors of low molecular weight protein tyrosine phosphatase and uses thereof
US10722484B2 (en) 2016-03-09 2020-07-28 K-Gen, Inc. Methods of cancer treatment
CN107286169B (zh) * 2016-04-05 2020-11-24 北京四环制药有限公司 端锚聚合酶抑制剂
CN106432103A (zh) * 2016-09-14 2017-02-22 信阳师范学院 一种喹唑酮类化合物及其制备方法
US11066420B2 (en) 2017-05-01 2021-07-20 Sanford Burnham Prebys Medical Discovery Institute Inhibitors of low molecular weight protein tyrosine phosphatase (LMPTP) and uses thereof
US20210060016A1 (en) * 2017-12-27 2021-03-04 Japanese Foundation For Cancer Research Anticancer agent
WO2019131798A1 (ja) * 2017-12-27 2019-07-04 国立研究開発法人理化学研究所 新規ジヒドロキナゾリノン系化合物又はその薬理学的に許容される塩、及び細胞増殖阻害剤
EP4021895A1 (en) * 2019-08-28 2022-07-06 F. Hoffmann-La Roche AG Novel quinazoline compounds for the treatment and prophylaxis of hepatitis b virus disease
WO2025111705A1 (en) * 2023-11-30 2025-06-05 Waverley Pharma Inc. Quinazolinone derivatives as poly (adp ribose) polymerase 1 (parp-1) inhibitors
WO2025221809A1 (en) * 2024-04-16 2025-10-23 Eluciderm Inc. 2-aryl-quinazolin-4(3h)-one inhibitors for the treatment of diseases

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WO1995024379A1 (en) * 1994-03-09 1995-09-14 Newcastle University Ventures Limited Benzamide analogs, useful as parp (adp-ribosyltransferase, adprt) dna repair enzyme inhibitors
WO1998033802A1 (en) * 1997-02-01 1998-08-06 Newcastle University Ventures Limited Quinazolinone compounds
WO2004014873A1 (ja) * 2002-08-09 2004-02-19 Kyorin Pharmaceutical Co., Ltd. 4-置換キナゾリン-8-カルボン酸アミド誘導体とその薬理上許容される付加塩
RU2007137266A (ru) * 2005-03-09 2009-04-20 Мерк энд Ко., Инк. (US) Хиназолиноновые антагонисты кальциевых каналов т-типа
WO2012028578A1 (de) * 2010-09-03 2012-03-08 Bayer Cropscience Ag Substituierte anellierte pyrimidinone und dihydropyrimidinone

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EP0054132A1 (de) * 1980-12-12 1982-06-23 Dr. Karl Thomae GmbH Neue Pyrimidinone, ihre Herstellung und Arzneimittel mit einem Gehalt an diesen Stoffen
SU1056900A3 (ru) * 1980-12-12 1983-11-23 Др.Карл Томэ Гмбх (Фирма) Способ получени пиримидинонов или их кислотно-аддитивных солей
WO1995024379A1 (en) * 1994-03-09 1995-09-14 Newcastle University Ventures Limited Benzamide analogs, useful as parp (adp-ribosyltransferase, adprt) dna repair enzyme inhibitors
WO1998033802A1 (en) * 1997-02-01 1998-08-06 Newcastle University Ventures Limited Quinazolinone compounds
WO2004014873A1 (ja) * 2002-08-09 2004-02-19 Kyorin Pharmaceutical Co., Ltd. 4-置換キナゾリン-8-カルボン酸アミド誘導体とその薬理上許容される付加塩
RU2007137266A (ru) * 2005-03-09 2009-04-20 Мерк энд Ко., Инк. (US) Хиназолиноновые антагонисты кальциевых каналов т-типа
WO2012028578A1 (de) * 2010-09-03 2012-03-08 Bayer Cropscience Ag Substituierte anellierte pyrimidinone und dihydropyrimidinone

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Gabriele Constantino et al. Modeling of Poly(ADP-ribose)polymerase (PARP) Inhibitors Docking of Ligands and Quatitative Structure -Activity Relationship Analysis, J. Med. Chem., 2011, 44, 3786-3794. *
Gabriele Constantino et al. Modeling of Poly(ADP-ribose)polymerase (PARP) Inhibitors Docking of Ligands and Quatitative Structure -Activity Relationship Analysis, J. Med. Chem., 2011, 44, 3786-3794. Layeva A.A. et al. Synthesis of 5-and 7-fluoroquinazolin-4(1H)-ones, Russian Chemical Bulletin, 2007, Kluwer Academic Publishers-Plenum Publishers, Ne - ISSN 1573-9171 Vol:56, Nr:9, Page(s): 1821 - 1827. *
Layeva A.A. et al. Synthesis of 5-and 7-fluoroquinazolin-4(1H)-ones, Russian Chemical Bulletin, 2007, Kluwer Academic Publishers-Plenum Publishers, Ne - ISSN 1573-9171 Vol:56, Nr:9, Page(s): 1821 - 1827. *
Wei Xu et al. Copper-Catalyzed Domino Synthesis of Quinazolinones via Ullmann-Type Coupling and Aerobic Oxidative C−H Amidation ORGANIC LETTERS, 14(23), 6012-6015 Vol:13, Nr:6, Page(s): 1274-1277. *

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Publication number Publication date
AU2013324681A1 (en) 2015-05-07
ES2654464T3 (es) 2018-02-13
RU2015115576A (ru) 2016-11-20
MX2015003570A (es) 2015-06-22
KR102200628B1 (ko) 2021-01-08
CA2886000C (en) 2020-11-10
HK1210777A1 (en) 2016-05-06
US9388142B2 (en) 2016-07-12
CN104662006A (zh) 2015-05-27
JP2015535831A (ja) 2015-12-17
JP6276769B2 (ja) 2018-02-07
EP2900643A1 (en) 2015-08-05
CA2886000A1 (en) 2014-04-03
BR112015006524A8 (pt) 2019-08-20
AU2013324681B2 (en) 2017-08-10
US20150239850A1 (en) 2015-08-27
ZA201502838B (en) 2017-11-29
SG11201502120XA (en) 2015-04-29
WO2014048532A1 (en) 2014-04-03
CN104662006B (zh) 2017-10-24
AR092670A1 (es) 2015-04-29
EP2900643B1 (en) 2017-09-27
BR112015006524A2 (pt) 2017-07-04
KR20150063474A (ko) 2015-06-09
IL237840A (en) 2017-05-29
MX362855B (es) 2019-02-20

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