CN101970424B - 具有检测点激酶1抑制活性的吲哚基吡啶酮衍生物 - Google Patents

具有检测点激酶1抑制活性的吲哚基吡啶酮衍生物 Download PDF

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Publication number
CN101970424B
CN101970424B CN200980103188XA CN200980103188A CN101970424B CN 101970424 B CN101970424 B CN 101970424B CN 200980103188X A CN200980103188X A CN 200980103188XA CN 200980103188 A CN200980103188 A CN 200980103188A CN 101970424 B CN101970424 B CN 101970424B
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oxo
carboxylic acid
title compound
dihydro
methyl
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Expired - Fee Related
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CN200980103188XA
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English (en)
Chinese (zh)
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CN101970424A (zh
Inventor
S·斯托克斯
N·福洛普
A·福曼纳
M·德赖斯代尔
S·贝德福特
P·韦伯
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Vernellis R&d Co ltd
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Vernellis R&d Co ltd
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Priority claimed from GBGB0801090.2A external-priority patent/GB0801090D0/en
Priority claimed from GBGB0818695.9A external-priority patent/GB0818695D0/en
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Publication of CN101970424A publication Critical patent/CN101970424A/zh
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    • 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
    • C07D401/14—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 three or more hetero 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Transplantation (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN200980103188XA 2008-01-22 2009-01-20 具有检测点激酶1抑制活性的吲哚基吡啶酮衍生物 Expired - Fee Related CN101970424B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB0801090.2 2008-01-22
GBGB0801090.2A GB0801090D0 (en) 2008-01-22 2008-01-22 New chemical compounds
GBGB0818695.9A GB0818695D0 (en) 2008-10-11 2008-10-11 New chemical compounds
GB0818695.9 2008-10-11
PCT/GB2009/000149 WO2009093012A1 (en) 2008-01-22 2009-01-20 Indolyl- pyridone derivatives having checkpoint kinase 1 inhibitory activity

Publications (2)

Publication Number Publication Date
CN101970424A CN101970424A (zh) 2011-02-09
CN101970424B true CN101970424B (zh) 2013-06-12

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CN200980103188XA Expired - Fee Related CN101970424B (zh) 2008-01-22 2009-01-20 具有检测点激酶1抑制活性的吲哚基吡啶酮衍生物

Country Status (17)

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US (5) US8916591B2 (enExample)
EP (1) EP2294065B1 (enExample)
JP (1) JP5386508B2 (enExample)
CN (1) CN101970424B (enExample)
AU (1) AU2009207478B2 (enExample)
BR (1) BRPI0906495B8 (enExample)
CA (1) CA2712959C (enExample)
DK (1) DK2294065T3 (enExample)
EA (1) EA021464B1 (enExample)
ES (1) ES2461799T3 (enExample)
IL (1) IL206808A (enExample)
MX (1) MX2010007525A (enExample)
NZ (1) NZ586756A (enExample)
PL (1) PL2294065T3 (enExample)
PT (1) PT2294065E (enExample)
WO (1) WO2009093012A1 (enExample)
ZA (1) ZA201005210B (enExample)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101970424B (zh) 2008-01-22 2013-06-12 弗奈利斯（R&D）有限公司 具有检测点激酶1抑制活性的吲哚基吡啶酮衍生物
GB0912499D0 (en) * 2009-07-18 2009-08-26 Vernalis R&D Ltd Indopyl-pyridone derivatives
JP6161537B2 (ja) 2010-04-07 2017-07-12 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト ピラゾール−４−イル−ヘテロシクリル−カルボキサミド化合物及び使用の方法
EP2463289A1 (en) * 2010-11-26 2012-06-13 Almirall, S.A. Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors
RU2638552C2 (ru) 2011-09-27 2017-12-14 Ф. Хоффманн-Ля Рош Аг Пиразол-4-ил-гетероциклил-карбоксамидные соединения и способы применения
GB201201566D0 (en) * 2012-01-30 2012-03-14 Vernalis R&D Ltd New chemical compounds
AU2014293013A1 (en) 2013-07-26 2016-03-17 Race Oncology Ltd. Combinatorial methods to improve the therapeutic benefit of bisantrene
TN2017000329A1 (en) * 2015-01-28 2019-01-16 Bayer Pharma AG 4h-pyrrolo[3,2-c]pyridin-4-one derivatives
MX2020005515A (es) * 2017-12-19 2020-09-03 Bristol Myers Squibb Co Compuestos de indol sustituidos con amida, utiles como inhibidores de receptores de tipo toll (tlr).
SG11202100158WA (en) * 2018-07-24 2021-02-25 Epizyme Inc Pyridin-2-one compounds useful as smarca2 antagonists
US10253606B1 (en) 2018-07-27 2019-04-09 Upwing Energy, LLC Artificial lift
US10370947B1 (en) * 2018-07-27 2019-08-06 Upwing Energy, LLC Artificial lift
US10787873B2 (en) 2018-07-27 2020-09-29 Upwing Energy, LLC Recirculation isolator for artificial lift and method of use
US10280721B1 (en) 2018-07-27 2019-05-07 Upwing Energy, LLC Artificial lift
EP3842425B1 (en) * 2018-08-24 2024-05-22 TransThera Sciences (Nanjing), Inc. Novel quinoline derivative inhibitor
US11686161B2 (en) 2018-12-28 2023-06-27 Upwing Energy, Inc. System and method of transferring power within a wellbore
CN112625027B (zh) * 2019-09-24 2022-09-09 药捷安康(南京)科技股份有限公司 杂环衍生物及其用途
WO2023250141A2 (en) * 2022-06-24 2023-12-28 Enalare Therapeutics Inc. Methods of treating neurological ventilatory insufficiency
CN115594634B (zh) * 2022-10-26 2024-10-01 浙江工业大学 一种连续化制备4-硝基吡唑的新工艺

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002079192A1 (en) * 2001-03-28 2002-10-10 Bristol-Myers Squibb Company Novel tyrosine kinase inhibitors
WO2006134318A1 (en) * 2005-06-11 2006-12-21 Vernalis R & D Limited Pyrazole-substituted benzimidazole derivatives for use in the treatment of cancer and autoimmune disorders

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR0213562A (pt) 2001-10-26 2004-08-31 Aventis Pharma Inc Benzimidazóis e análogos e seu uso como inibidores de cinases de proteìna
US20050256157A1 (en) * 2002-08-23 2005-11-17 Chiron Corporation Combination therapy with CHK1 inhibitors
AU2004251175A1 (en) 2003-06-05 2005-01-06 Merck & Co., Inc. Substituted indoles and a process for preparing substituted indoles
TWI372050B (en) * 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
AU2006324144A1 (en) * 2005-01-28 2007-08-02 Merck Sharp & Dohme Corp. Inhibitors of checkpoint kinases
EP2046330A2 (en) * 2006-07-14 2009-04-15 Astex Therapeutics Limited Pharmaceutical combinations
WO2008025526A1 (en) * 2006-08-31 2008-03-06 F. Hoffmann-La Roche Ag Indole derivatives, their manufacture and use as pharmaceutical agents
CN101970424B (zh) 2008-01-22 2013-06-12 弗奈利斯（R&D）有限公司 具有检测点激酶1抑制活性的吲哚基吡啶酮衍生物
EA201101619A1 (ru) * 2009-05-15 2012-05-30 Новартис Аг Производные 5-пиридин-3-ил-1,3-дигидроиндол-2-она и их применение в качестве модуляторов альдостеронсинтазы и/или cyp11b1

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002079192A1 (en) * 2001-03-28 2002-10-10 Bristol-Myers Squibb Company Novel tyrosine kinase inhibitors
WO2006134318A1 (en) * 2005-06-11 2006-12-21 Vernalis R & D Limited Pyrazole-substituted benzimidazole derivatives for use in the treatment of cancer and autoimmune disorders

Also Published As

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DK2294065T3 (da) 2014-04-28
ZA201005210B (en) 2011-03-30
US10696652B2 (en) 2020-06-30
ES2461799T3 (es) 2014-05-21
AU2009207478A1 (en) 2009-07-30
JP5386508B2 (ja) 2014-01-15
US20170298043A1 (en) 2017-10-19
CA2712959A1 (en) 2009-07-30
IL206808A (en) 2015-08-31
BRPI0906495B1 (pt) 2020-11-10
WO2009093012A1 (en) 2009-07-30
EP2294065A1 (en) 2011-03-16
US8916591B2 (en) 2014-12-23
EA021464B1 (ru) 2015-06-30
JP2011510055A (ja) 2011-03-31
PL2294065T3 (pl) 2014-11-28
AU2009207478B2 (en) 2013-11-21
NZ586756A (en) 2012-04-27
BRPI0906495A2 (pt) 2015-07-14
US20110021498A1 (en) 2011-01-27
US20200361905A1 (en) 2020-11-19
US20150099736A1 (en) 2015-04-09
PT2294065E (pt) 2014-05-15
MX2010007525A (es) 2010-08-18
CN101970424A (zh) 2011-02-09
US20180244652A1 (en) 2018-08-30
CA2712959C (en) 2015-06-23
IL206808A0 (en) 2010-12-30
BRPI0906495A8 (pt) 2015-10-06
EA201001197A1 (ru) 2011-04-29
US9604975B2 (en) 2017-03-28
BRPI0906495B8 (pt) 2021-05-25
EP2294065B1 (en) 2014-03-19

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