CN101395155A - PI3Kα的吡啶并嘧啶酮抑制剂 - Google Patents

PI3Kα的吡啶并嘧啶酮抑制剂 Download PDF

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Publication number
CN101395155A
CN101395155A CNA2006800370996A CN200680037099A CN101395155A CN 101395155 A CN101395155 A CN 101395155A CN A2006800370996 A CNA2006800370996 A CN A2006800370996A CN 200680037099 A CN200680037099 A CN 200680037099A CN 101395155 A CN101395155 A CN 101395155A
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China
Prior art keywords
pyrimidin
ethyl
methyl
optionally substituted
ethylamino
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Pending
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Chinese (zh)
Inventor
T·-G·拜克
C·A·布尔
K·拉拉
马星熏
M·麦克
J·M·努斯
王龙成
王勇
杨敬诚
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Exelixis Inc
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Exelixis Inc
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Publication of CN101395155A publication Critical patent/CN101395155A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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
    • A61K31/495—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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Dispersion Chemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CNA2006800370996A 2005-10-07 2006-10-09 PI3Kα的吡啶并嘧啶酮抑制剂 Pending CN101395155A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US72457105P 2005-10-07 2005-10-07
US60/724,571 2005-10-07
US74371906P 2006-03-23 2006-03-23
US60/743,719 2006-03-23
PCT/US2006/039734 WO2007044813A1 (en) 2005-10-07 2006-10-09 PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN2012102106887A Division CN102746298A (zh) 2005-10-07 2006-10-09 PI3Kα的吡啶并嘧啶酮抑制剂

Publications (1)

Publication Number Publication Date
CN101395155A true CN101395155A (zh) 2009-03-25

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CNA2006800370996A Pending CN101395155A (zh) 2005-10-07 2006-10-09 PI3Kα的吡啶并嘧啶酮抑制剂

Country Status (19)

Country Link
US (2) US8044062B2 (https=)
EP (2) EP2322523B1 (https=)
JP (1) JP5461012B2 (https=)
KR (3) KR20140105621A (https=)
CN (1) CN101395155A (https=)
AU (1) AU2006302078B2 (https=)
BR (1) BRPI0617159B8 (https=)
CA (1) CA2623770C (https=)
DK (1) DK1940839T3 (https=)
EA (1) EA016945B1 (https=)
ES (1) ES2432046T3 (https=)
GE (1) GEP20115304B (https=)
HR (1) HRP20130902T1 (https=)
IL (1) IL190292A (https=)
NO (1) NO343136B1 (https=)
NZ (2) NZ594628A (https=)
PL (1) PL1940839T3 (https=)
RS (1) RS52953B (https=)
WO (1) WO2007044813A1 (https=)

Cited By (5)

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CN103402999A (zh) * 2010-11-24 2013-11-20 埃克塞里艾克西斯公司 作为PI3K/mTOR抑制剂的苯并氧氮杂卓及其使用和生产方法
CN103596951A (zh) * 2011-04-08 2014-02-19 阿弗拉克西斯控股股份有限公司 用于治疗神经系统障碍和癌症的8-乙基-6-(芳基)吡啶并[2,3-d]嘧啶-7(8h)-酮
CN103635183A (zh) * 2011-04-29 2014-03-12 埃克塞利希斯股份有限公司 使用pi3k/mtor的吡啶并嘧啶抑制剂来治疗淋巴瘤的方法
CN114394966A (zh) * 2016-08-15 2022-04-26 辉瑞公司 吡啶并嘧啶酮cdk2/4/6抑制剂
WO2024012543A1 (zh) * 2022-07-14 2024-01-18 浙江同源康医药股份有限公司 用作cdk4激酶抑制剂的化合物及其应用

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