CN104662006B - 作为parp抑制剂的喹唑酮衍生物 - Google Patents

作为parp抑制剂的喹唑酮衍生物 Download PDF

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Publication number
CN104662006B
CN104662006B CN201380050421.9A CN201380050421A CN104662006B CN 104662006 B CN104662006 B CN 104662006B CN 201380050421 A CN201380050421 A CN 201380050421A CN 104662006 B CN104662006 B CN 104662006B
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methyl
quinazolin
phenyl
ethyl
hydroxy
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CN104662006A (zh
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D.多施
H-P.布希施塔勒
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Merck Patent GmbH
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Merck Patent GmbH
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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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201380050421.9A 2012-09-26 2013-08-27 作为parp抑制剂的喹唑酮衍生物 Active CN104662006B (zh)

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
CN104662006A CN104662006A (zh) 2015-05-27
CN104662006B true CN104662006B (zh) 2017-10-24

Family

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Family Applications (1)

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CN201380050421.9A Active CN104662006B (zh) 2012-09-26 2013-08-27 作为parp抑制剂的喹唑酮衍生物

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)

Families Citing this family (17)

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SG10201610936RA (en) 2011-12-22 2017-02-27 Alios Biopharma Inc Substituted nucleosides, nucleotides and analogs thereof
EP2822656B1 (en) 2012-03-07 2016-10-19 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
WO2013174962A1 (en) 2012-05-25 2013-11-28 Janssen R&D Ireland Uracyl spirooxetane nucleosides
CN110684067A (zh) 2012-12-21 2020-01-14 艾丽奥斯生物制药有限公司 取代的核苷和核苷酸
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
WO2017156350A1 (en) 2016-03-09 2017-09-14 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
JP7369968B2 (ja) * 2017-12-27 2023-10-27 公益財団法人がん研究会 抗がん剤
ES2998084T3 (en) * 2017-12-27 2025-02-19 Japanese Found For Cancer Res Novel dihydroquinazolinone compound or pharmacologically acceptable salt, and cell growth inhibitor
US20220348549A1 (en) * 2019-08-28 2022-11-03 Hoffmann-La Roche Inc. 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

Citations (5)

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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
CN1143358A (zh) * 1994-03-09 1997-02-19 钮卡斯尔大学风险投资有限公司 苯甲酰胺类似物，用作parp(adp-核糖基转移酶，adrpt)dna修复酶抑制剂
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
WO2012028578A1 (de) * 2010-09-03 2012-03-08 Bayer Cropscience Ag Substituierte anellierte pyrimidinone und dihydropyrimidinone

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JP4471404B2 (ja) 1996-02-13 2010-06-02 アストラゼネカ ユーケイ リミテッド Ｖｅｇｆインヒビターとしてのキナゾリン誘導体
ATE211134T1 (de) 1996-03-05 2002-01-15 4-anilinochinazolin derivate
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Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0054132A1 (de) * 1980-12-12 1982-06-23 Dr. Karl Thomae GmbH Neue Pyrimidinone, ihre Herstellung und Arzneimittel mit einem Gehalt an diesen Stoffen
CN1143358A (zh) * 1994-03-09 1997-02-19 钮卡斯尔大学风险投资有限公司 苯甲酰胺类似物，用作parp(adp-核糖基转移酶，adrpt)dna修复酶抑制剂
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
WO2012028578A1 (de) * 2010-09-03 2012-03-08 Bayer Cropscience Ag Substituierte anellierte pyrimidinone und dihydropyrimidinone

Non-Patent Citations (3)

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Title
copper-catalyzed domino synthesis of quinazolinones via ullmann-type coupling and aerobic oxidative C-H amidation;wei xu et al.;《organic letters》;20110223;第13卷(第6期);1274-1277，尤其是第1276页表2 *
Modeling of poly(ADP-ribose) polymerase(PARP) Inhibitors. Docking of Ligands and quantitative structure-Activity relationship analysis;costantino, gabriele et al;《JOURNAL OF MEDICINAL CHEMISTRY》;20011013;第44卷(第23期);3786-3794，尤其是第3786页左栏，第3788页表1 *
synthesis of 5- and 7-fluoroquianzolin-4(1H)-ones;layeva, a.a.et al.;《Russian Chemical Bulletin》;20070930;第56卷(第9期);1821-1827,尤其是第1823页示意图4 *

Also Published As

Publication number Publication date
AR092670A1 (es) 2015-04-29
ES2654464T3 (es) 2018-02-13
US20150239850A1 (en) 2015-08-27
AU2013324681A1 (en) 2015-05-07
CA2886000A1 (en) 2014-04-03
JP6276769B2 (ja) 2018-02-07
KR102200628B1 (ko) 2021-01-08
KR20150063474A (ko) 2015-06-09
HK1210777A1 (en) 2016-05-06
CN104662006A (zh) 2015-05-27
CA2886000C (en) 2020-11-10
RU2015115576A (ru) 2016-11-20
AU2013324681B2 (en) 2017-08-10
IL237840A (en) 2017-05-29
WO2014048532A1 (en) 2014-04-03
BR112015006524A8 (pt) 2019-08-20
MX362855B (es) 2019-02-20
BR112015006524A2 (pt) 2017-07-04
US9388142B2 (en) 2016-07-12
JP2015535831A (ja) 2015-12-17
ZA201502838B (en) 2017-11-29
SG11201502120XA (en) 2015-04-29
RU2650107C2 (ru) 2018-04-09
MX2015003570A (es) 2015-06-22
EP2900643B1 (en) 2017-09-27
EP2900643A1 (en) 2015-08-05

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