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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China
Prior art keywords
alkyl
phenyl
optionally substituted
pyrimidine
hydroxy
Prior art date
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English (en)
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
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Genentech Inc
Array Biopharma Inc
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Genentech Inc
Array Biopharma Inc
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Publication of CN103635472A publication Critical patent/CN103635472A/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
    • 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
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • 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
    • 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
    • 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
    • C07D491/02—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 two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (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

Family

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CN201280020897.3A Active CN103635472B (zh) 2011-02-28 2012-02-28 丝氨酸/苏氨酸激酶抑制剂

Country Status (11)

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

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MX375902B (es) 2013-12-30 2025-03-07 Genentech Inc Inhibidores de serina/treonina cinasa.
KR102379517B1 (ko) * 2013-12-30 2022-03-25 제넨테크, 인크. 세린/트레오닌 키나아제 억제제
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JP6986565B2 (ja) 2017-09-29 2021-12-22 田辺三菱製薬株式会社 光学活性ピロリジン化合物及びその製造方法
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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
KR20250091232A (ko) * 2022-10-25 2025-06-20 투오지에 바이오텍 (상하이) 컴퍼니 리미티드 피페리디노피리미딘계 유도체, 이의 제조 방법 및 이의 의학적 응용
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TW202535869A (zh) * 2023-10-23 2025-09-16 大陸商上海拓界生物醫藥科技有限公司 一種含有噻唑基的哌啶并嘧啶類衍生物、其製備方法及其醫藥上的應用
WO2025223512A1 (zh) * 2024-04-24 2025-10-30 江苏恒瑞医药股份有限公司 一种二氢吡啶并嘧啶衍生物的可药用盐、结晶形式及用途
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Also Published As

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

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