CN103635472B - 丝氨酸/苏氨酸激酶抑制剂 - Google Patents

丝氨酸/苏氨酸激酶抑制剂 Download PDF

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Publication number
CN103635472B
CN103635472B CN201280020897.3A CN201280020897A CN103635472B CN 103635472 B CN103635472 B CN 103635472B CN 201280020897 A CN201280020897 A CN 201280020897A CN 103635472 B CN103635472 B CN 103635472B
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Prior art keywords
alkyl
phenyl
optionally substituted
pyrimidine
hydroxy
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Chinese (zh)
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CN103635472A (zh
Inventor
J.F.布雷克
陈慧芬
M.J.希凯利
J.德米斯
R.加雷
J.J.高蒂诺
R.J.考斯
G.R.科拉科夫斯基
A.L.马洛
P.J.莫尔
L.任
J.施瓦兹
C.S.希德姆
A.A.托马斯
E.华莱士
S.M.温格洛夫斯基
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Genentech Inc
Array Biopharma Inc
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Genentech Inc
Array Biopharma Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • 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
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • 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
    • C07D491/052Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201280020897.3A 2011-02-28 2012-02-28 丝氨酸/苏氨酸激酶抑制剂 Active CN103635472B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161447587P 2011-02-28 2011-02-28
US61/447,587 2011-02-28
PCT/US2012/027009 WO2012118850A1 (en) 2011-02-28 2012-02-28 Serine/threonine kinase inhibitors

Publications (2)

Publication Number Publication Date
CN103635472A CN103635472A (zh) 2014-03-12
CN103635472B true CN103635472B (zh) 2018-01-12

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Country Link
US (1) US9133187B2 (https=)
EP (1) EP2681215B1 (https=)
JP (1) JP6085866B2 (https=)
KR (1) KR101961500B1 (https=)
CN (1) CN103635472B (https=)
BR (1) BR112013021896A2 (https=)
CA (1) CA2828478C (https=)
ES (1) ES2543050T3 (https=)
MX (1) MX339873B (https=)
RU (1) RU2013143839A (https=)
WO (1) WO2012118850A1 (https=)

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CN111170929A (zh) * 2019-12-12 2020-05-19 北京达因高科儿童药物研究院有限公司 一种由末端烯烃制备β-氨基醇的方法
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CN115040522B (zh) * 2022-06-30 2024-02-06 牡丹江医学院 一种用于治疗肺癌的药物及其制备方法
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Also Published As

Publication number Publication date
JP2014506930A (ja) 2014-03-20
CA2828478C (en) 2019-12-31
BR112013021896A2 (pt) 2016-11-08
WO2012118850A1 (en) 2012-09-07
EP2681215B1 (en) 2015-04-22
CN103635472A (zh) 2014-03-12
KR20140014190A (ko) 2014-02-05
EP2681215A1 (en) 2014-01-08
RU2013143839A (ru) 2015-04-10
ES2543050T3 (es) 2015-08-14
MX2013009877A (es) 2014-02-11
US20130338140A1 (en) 2013-12-19
CA2828478A1 (en) 2012-09-07
JP6085866B2 (ja) 2017-03-01
US9133187B2 (en) 2015-09-15
KR101961500B1 (ko) 2019-03-22
MX339873B (es) 2016-06-15

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