CN109311908B - 作为Akt抑制剂的二氢吡唑氮杂卓类化合物 - Google Patents

作为Akt抑制剂的二氢吡唑氮杂卓类化合物 Download PDF

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Publication number
CN109311908B
CN109311908B CN201780037686.3A CN201780037686A CN109311908B CN 109311908 B CN109311908 B CN 109311908B CN 201780037686 A CN201780037686 A CN 201780037686A CN 109311908 B CN109311908 B CN 109311908B
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lcms
esi
thiophene
acid
δppm
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CN109311908A (zh
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卢伦
张志博
李刚
胡利红
丁照中
陈曙辉
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Harbin Zhenbao Pharmaceutical Co ltd
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Harbin Zhenbao Pharmaceutical Co ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems
    • 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
    • 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
    • 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
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14—Ortho-condensed systems
    • C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CN201780037686.3A 2016-06-16 2017-06-13 作为Akt抑制剂的二氢吡唑氮杂卓类化合物 Active CN109311908B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201610428049 2016-06-16
CN2016104280496 2016-06-16
CN2016106740210 2016-08-15
CN201610674021 2016-08-15
PCT/CN2017/088030 WO2017215588A1 (zh) 2016-06-16 2017-06-13 作为Akt抑制剂的二氢吡唑氮杂卓类化合物

Publications (2)

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CN109311908A CN109311908A (zh) 2019-02-05
CN109311908B true CN109311908B (zh) 2021-05-07

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CN201780037686.3A Active CN109311908B (zh) 2016-06-16 2017-06-13 作为Akt抑制剂的二氢吡唑氮杂卓类化合物

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Country Link
US (1) US10654868B2 (enExample)
EP (1) EP3473628B1 (enExample)
JP (1) JP6900406B2 (enExample)
KR (1) KR102351270B1 (enExample)
CN (1) CN109311908B (enExample)
WO (1) WO2017215588A1 (enExample)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019114741A1 (zh) * 2017-12-13 2019-06-20 南京明德新药研发股份有限公司 作为Akt抑制剂的盐型及其晶型
WO2022121788A1 (zh) * 2020-12-07 2022-06-16 南京正大天晴制药有限公司 一种吡唑并氮杂卓类akt抑制剂

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1639151A (zh) * 2002-03-12 2005-07-13 霍夫曼-拉罗奇有限公司 新的氮杂环庚烷衍生物
CN101094833A (zh) * 2004-07-12 2007-12-26 伊邓药品公司 四肽类似物
WO2008065054A1 (en) * 2006-11-28 2008-06-05 Nerviano Medical Sciences S.R.L. Tricyclic indoles and (4,5-dihydro) indoles
WO2008098104A1 (en) * 2007-02-07 2008-08-14 Smithkline Beecham Corporation Inhibitors of akt activity
EP2002836A1 (en) * 2007-05-31 2008-12-17 Nerviano Medical Sciences S.r.l. Cyclocondensed azaindoles active as kinase inhibitors
WO2009089305A1 (en) * 2008-01-07 2009-07-16 Synta Pharmaceuticals Corp. Compounds for inflammation and immune-related uses
CN103298461A (zh) * 2010-11-17 2013-09-11 霍夫曼-拉罗奇有限公司 治疗肿瘤的方法

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009158371A1 (en) 2008-06-26 2009-12-30 Smithklike Beecham Corporation Inhibitors of akt activity

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1639151A (zh) * 2002-03-12 2005-07-13 霍夫曼-拉罗奇有限公司 新的氮杂环庚烷衍生物
CN101094833A (zh) * 2004-07-12 2007-12-26 伊邓药品公司 四肽类似物
WO2008065054A1 (en) * 2006-11-28 2008-06-05 Nerviano Medical Sciences S.R.L. Tricyclic indoles and (4,5-dihydro) indoles
WO2008098104A1 (en) * 2007-02-07 2008-08-14 Smithkline Beecham Corporation Inhibitors of akt activity
EP2002836A1 (en) * 2007-05-31 2008-12-17 Nerviano Medical Sciences S.r.l. Cyclocondensed azaindoles active as kinase inhibitors
WO2009089305A1 (en) * 2008-01-07 2009-07-16 Synta Pharmaceuticals Corp. Compounds for inflammation and immune-related uses
CN103298461A (zh) * 2010-11-17 2013-09-11 霍夫曼-拉罗奇有限公司 治疗肿瘤的方法

Also Published As

Publication number Publication date
US10654868B2 (en) 2020-05-19
CN109311908A (zh) 2019-02-05
KR20190017996A (ko) 2019-02-20
JP6900406B2 (ja) 2021-07-07
JP2019518052A (ja) 2019-06-27
KR102351270B1 (ko) 2022-01-14
WO2017215588A1 (zh) 2017-12-21
EP3473628A4 (en) 2019-05-01
US20190233434A1 (en) 2019-08-01
EP3473628B1 (en) 2019-12-11
EP3473628A1 (en) 2019-04-24

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Address after: Room 218, No. 9 Commercial Office Building, Gaoxin Road, Nanjing High-tech Development Zone, Jiangsu Province

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