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

Landscapes

  • 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 2012-09-26
EP12006707.9 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 (enExample)
EP (1) EP2900643B1 (enExample)
JP (1) JP6276769B2 (enExample)
KR (1) KR102200628B1 (enExample)
CN (1) CN104662006B (enExample)
AR (1) AR092670A1 (enExample)
AU (1) AU2013324681B2 (enExample)
BR (1) BR112015006524A8 (enExample)
CA (1) CA2886000C (enExample)
ES (1) ES2654464T3 (enExample)
IL (1) IL237840A (enExample)
MX (1) MX362855B (enExample)
RU (1) RU2650107C2 (enExample)
SG (1) SG11201502120XA (enExample)
WO (1) WO2014048532A1 (enExample)
ZA (1) ZA201502838B (enExample)

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KR102072041B1 (ko) 2011-12-22 2020-01-31 앨리오스 바이오파마 인크. 치환된 뉴클레오사이드, 뉴클레오타이드 및 그의 유사체
RU2696572C2 (ru) 2012-03-07 2019-08-05 Инститьют Оф Кансер Ресёрч: Ройял Кансер Хоспитал (Зе) 3-арил-5-замещенные соединения изохинолин-1-она и их терапевтическое применение
USRE48171E1 (en) 2012-03-21 2020-08-25 Janssen Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
US9441007B2 (en) 2012-03-21 2016-09-13 Alios Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
PT2861611T (pt) 2012-05-25 2016-10-11 Janssen Sciences Ireland Uc Nucleósidos de espirooxetano de uracilo
US9243022B2 (en) 2012-12-21 2016-01-26 Alios Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
CA2922469A1 (en) 2013-09-11 2015-03-19 Institute Of Cancer Research: Royal Cancer Hospital (The) 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use
JP6899323B2 (ja) 2014-10-14 2021-07-07 ラ ホーヤ インスティテュート オブ アレルギー アンド イミュノロジー 低分子量タンパク質チロシンホスファターゼの阻害剤、及びその使用
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
WO2019131794A1 (ja) * 2017-12-27 2019-07-04 公益財団法人がん研究会 抗がん剤
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
US20220348549A1 (en) * 2019-08-28 2022-11-03 Hoffmann-La Roche Inc. Quinazoline compounds for the treatment and prophylaxis of hepatitis b virus disease
KR102969020B1 (ko) * 2020-10-29 2026-05-22 한국화학연구원 퀴나졸린-4(3h)-온 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 grk5 활성 관련 질환의 예방 또는 치료용 약학 조성물
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
CN121226265B (zh) * 2025-09-29 2026-05-26 亳州学院 一种含喹唑啉酮片段的酰腙类化合物及其制备方法与应用

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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
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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BR0111230A (pt) 2000-05-31 2003-06-10 Astrazeneca Ab Composto, e, uso e processo para a preparação do mesmo
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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
KR102200628B1 (ko) 2021-01-08
AU2013324681B2 (en) 2017-08-10
AU2013324681A1 (en) 2015-05-07
JP2015535831A (ja) 2015-12-17
MX362855B (es) 2019-02-20
ZA201502838B (en) 2017-11-29
JP6276769B2 (ja) 2018-02-07
EP2900643B1 (en) 2017-09-27
ES2654464T3 (es) 2018-02-13
EP2900643A1 (en) 2015-08-05
US20150239850A1 (en) 2015-08-27
MX2015003570A (es) 2015-06-22
WO2014048532A1 (en) 2014-04-03
BR112015006524A2 (pt) 2017-07-04
US9388142B2 (en) 2016-07-12
CA2886000A1 (en) 2014-04-03
KR20150063474A (ko) 2015-06-09
SG11201502120XA (en) 2015-04-29
IL237840A (en) 2017-05-29
AR092670A1 (es) 2015-04-29
CN104662006B (zh) 2017-10-24
CA2886000C (en) 2020-11-10
CN104662006A (zh) 2015-05-27
RU2015115576A (ru) 2016-11-20
HK1210777A1 (en) 2016-05-06
BR112015006524A8 (pt) 2019-08-20

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