CN106795179B - 一类激酶抑制剂 - Google Patents

一类激酶抑制剂 Download PDF

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Publication number
CN106795179B
CN106795179B CN201580027559.6A CN201580027559A CN106795179B CN 106795179 B CN106795179 B CN 106795179B CN 201580027559 A CN201580027559 A CN 201580027559A CN 106795179 B CN106795179 B CN 106795179B
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base
amino
pyrimidine
pyridine
cyclopenta
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CN106795179A (zh
Inventor
王为波
赵兴东
李同双
田强
张华杰
谭浩瀚
王宪龙
刘启洪
李志福
张卫鹏
陈志方
姜立花
刘研新
令狐莉
林敏�
孙婧
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AOHONG PHARMACEUTICAL Co Ltd JINZHOU
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Shanghai Fochon Pharmaceutical Co Ltd
Fochon Pharmaceuticals Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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 two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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 two hetero rings
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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 two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic 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 two hetero rings
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201580027559.6A 2014-05-28 2015-05-27 一类激酶抑制剂 Active CN106795179B (zh)

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CN201910743940.2A CN110372720B (zh) 2014-05-28 2015-05-27 一类激酶抑制剂

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462003626P 2014-05-28 2014-05-28
US62/003626 2014-05-28
PCT/CN2015/079910 WO2015180642A1 (en) 2014-05-28 2015-05-27 Certain protein kinase inhibitors

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EP (1) EP3149008B8 (enExample)
JP (1) JP2017516855A (enExample)
KR (1) KR101864589B1 (enExample)
CN (2) CN106795179B (enExample)
AU (1) AU2015266492B2 (enExample)
BR (1) BR112016027679B1 (enExample)
CA (1) CA2950330C (enExample)
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CN106188060A (zh) * 2015-04-29 2016-12-07 厦门大学 嘧啶并吡咯类化合物、其制备方法、药用组合物及其应用
CN105130992B (zh) * 2015-07-16 2018-02-09 苏州大学 具有激酶抑制活性的含氮杂环化合物、制备方法和用途
CN113549069A (zh) * 2015-12-27 2021-10-26 重庆复创医药研究有限公司 一类激酶抑制剂
WO2017161253A1 (en) 2016-03-18 2017-09-21 Tufts Medical Center Compositions and methods for treating and preventing metabolic disorders
CN109153686B (zh) * 2016-05-07 2021-04-30 上海复尚慧创医药研究有限公司 一类蛋白激酶抑制剂
WO2018005860A1 (en) 2016-07-01 2018-01-04 G1 Therapeutics, Inc. Pyrimidine-based antiproliferative agents
JP6905069B2 (ja) * 2016-11-11 2021-07-21 上海海雁醫藥科技有限公司 ピリジルアミノ置換へテロ三環式化合物並びにその製造方法及び医薬用途
CN107312006B (zh) * 2017-06-28 2019-11-15 郑州大学第一附属医院 吡咯并嘧啶类衍生物及其应用
JP7569688B2 (ja) 2017-12-22 2024-10-18 ハイバーセル,インコーポレイテッド ホスファチジルイノシトールリン酸キナーゼ阻害剤としてのアミノピリジン誘導体
US11174252B2 (en) 2018-02-15 2021-11-16 Nuvation Bio Inc. Heterocyclic compounds as kinase inhibitors
WO2019168874A1 (en) 2018-02-27 2019-09-06 The Research Foundation For The State University Of New York Difluoromethoxylation and trifluoromethoxylation compositions and methods for synthesizing same
EP3786161A4 (en) 2018-04-24 2021-05-05 Shanghai Haiyan Pharmaceutical Technology Co., Ltd CDK4 / 6 INHIBITOR, PHARMACEUTICALLY ACCEPTABLE SALT, POLYMORPHIC OF THEM AND ASSOCIATED USE
TW202112767A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物
CN112094272A (zh) * 2019-06-18 2020-12-18 北京睿熙生物科技有限公司 Cdk激酶抑制剂
EP4652997A2 (en) 2020-05-19 2025-11-26 Pharmacosmos Holding A/s Cyclin-dependent kinase inhibiting compounds for the treatment of medical disorders
AR124154A1 (es) 2020-11-27 2023-02-22 Rhizen Pharmaceuticals Ag Inhibidores de cdk
WO2022149057A1 (en) 2021-01-05 2022-07-14 Rhizen Pharmaceuticals Ag Cdk inhibitors
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors
CA3249870A1 (en) * 2022-01-25 2023-08-03 Kinnate Biopharma Inc. CDK4/6 KINASE INHIBITORS
CN116836177A (zh) * 2022-09-28 2023-10-03 锦州奥鸿药业有限责任公司 一种蛋白激酶抑制剂的枸橼酸盐、其晶型、制备方法和用途

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WO2005121107A1 (en) * 2004-06-09 2005-12-22 F. Hoffmann-La Roche Ag Pyrazolo pyrimidines
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WO2005121107A1 (en) * 2004-06-09 2005-12-22 F. Hoffmann-La Roche Ag Pyrazolo pyrimidines
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WO2011101409A1 (en) * 2010-02-19 2011-08-25 Novartis Ag Pyrrolopyrimidine compounds as inhibitors of cdk4/6
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WO2015180642A1 (en) 2015-12-03
CA2950330A1 (en) 2015-12-03
KR101864589B1 (ko) 2018-07-04
CN106795179A (zh) 2017-05-31
BR112016027679B1 (pt) 2022-10-25
BR112016027679A2 (enExample) 2017-08-15
RU2016151315A (ru) 2018-07-02
US20170267696A1 (en) 2017-09-21
CN110372720A (zh) 2019-10-25
US10087195B2 (en) 2018-10-02
JP2017516855A (ja) 2017-06-22
EP3149008A4 (en) 2018-01-17
DK3149008T3 (en) 2019-04-01
MX2016015565A (es) 2017-07-04
MX381487B (es) 2025-03-12
AU2015266492B2 (en) 2017-11-02
RU2671494C2 (ru) 2018-11-01
CA2950330C (en) 2019-04-30
EP3149008B8 (en) 2019-03-06
RU2016151315A3 (enExample) 2018-07-02
EP3149008B1 (en) 2018-12-12
KR20170023872A (ko) 2017-03-06
CN110372720B (zh) 2021-03-05
EP3149008A1 (en) 2017-04-05
ES2715462T3 (es) 2019-06-04
AU2015266492A1 (en) 2017-01-19

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