CN103502241B - 作为激酶抑制剂的取代的嘧啶基-吡咯类活性剂 - Google Patents

作为激酶抑制剂的取代的嘧啶基-吡咯类活性剂 Download PDF

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Publication number
CN103502241B
CN103502241B CN201280018834.4A CN201280018834A CN103502241B CN 103502241 B CN103502241 B CN 103502241B CN 201280018834 A CN201280018834 A CN 201280018834A CN 103502241 B CN103502241 B CN 103502241B
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China
Prior art keywords
formula
compound
pyrrole
chloro
aminopyrimidin
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Expired - Fee Related
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CN201280018834.4A
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English (en)
Chinese (zh)
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CN103502241A (zh
Inventor
M·G·布拉斯卡
T·班迪拉
J·A·伯特兰德
P·戈奇
D·米利兹
M·内希
A·潘泽利
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Nerviano Medical Sciences SRL
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Nerviano Medical Sciences SRL
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201280018834.4A 2011-04-19 2012-04-05 作为激酶抑制剂的取代的嘧啶基-吡咯类活性剂 Expired - Fee Related CN103502241B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11162960.6 2011-04-19
EP11162960 2011-04-19
PCT/EP2012/056266 WO2012143248A1 (en) 2011-04-19 2012-04-05 Substituted pyrimidinyl-pyrroles active as kinase inhibitors

Publications (2)

Publication Number Publication Date
CN103502241A CN103502241A (zh) 2014-01-08
CN103502241B true CN103502241B (zh) 2016-03-23

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CN201280018834.4A Expired - Fee Related CN103502241B (zh) 2011-04-19 2012-04-05 作为激酶抑制剂的取代的嘧啶基-吡咯类活性剂

Country Status (8)

Country Link
US (1) US9283224B2 (https=)
EP (1) EP2699564B1 (https=)
JP (1) JP5970537B2 (https=)
CN (1) CN103502241B (https=)
BR (1) BR112013026137B1 (https=)
ES (1) ES2616458T3 (https=)
RU (1) RU2621732C2 (https=)
WO (1) WO2012143248A1 (https=)

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CN108697708A (zh) 2015-10-26 2018-10-23 洛克索肿瘤学股份有限公司 Trk抑制剂抗性癌症中的点突变以及与此相关的方法
RS65988B1 (sr) 2016-04-04 2024-10-31 Loxo Oncology Inc Postupak lečenja pedijatrijskih karcinoma
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
ES2987474T3 (es) 2016-04-04 2024-11-15 Loxo Oncology Inc Formulaciones líquidas de (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-IL)-pirazolo[1,5-A]pirimidin-3-IL)-3-hidroxipirrolidina-1-carboxamida
ES2836222T3 (es) 2016-05-18 2021-06-24 Loxo Oncology Inc Preparación de (S)-N-(5-((R)-2-(2,5-difluorofenil)pirrolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida
TWI752098B (zh) 2016-10-10 2022-01-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
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WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
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GB201706806D0 (en) * 2017-04-28 2017-06-14 Sentinel Oncology Ltd Pharmaceutical compounds
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
TWI812649B (zh) 2017-10-10 2023-08-21 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
CN107970438B (zh) * 2017-11-28 2021-08-13 镇江市中西医结合医院（镇江市第二人民医院） 一种神经再生凝胶及其制备方法和应用
CN111615514B (zh) 2018-01-18 2022-10-11 奥瑞生物药品公司 作为ret激酶抑制剂的取代的吡唑并[4,3-c]吡啶化合物
WO2019143991A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. SUBSTITUTED PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS AS RET KINASE INHIBITORS
EP3740491A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
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US20240285621A1 (en) * 2020-09-23 2024-08-29 Nerviano Medical Sciences S.R.L. Pyrazolyl-pyrimidine derivatives as kinase inhibitors
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CN101421250A (zh) * 2006-01-30 2009-04-29 埃克塞里艾克西斯公司 作为jak-2调节剂的4-芳基-2-氨基-嘧啶或4-芳基-2-氨基烷基-嘧啶及包含它们的药物组合物
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Also Published As

Publication number Publication date
US9283224B2 (en) 2016-03-15
ES2616458T3 (es) 2017-06-13
EP2699564B1 (en) 2016-12-14
JP2014516360A (ja) 2014-07-10
BR112013026137A2 (pt) 2017-10-24
RU2621732C2 (ru) 2017-06-07
US20140155421A1 (en) 2014-06-05
CN103502241A (zh) 2014-01-08
HK1187905A1 (zh) 2014-04-17
RU2013151174A (ru) 2015-05-27
JP5970537B2 (ja) 2016-08-17
WO2012143248A1 (en) 2012-10-26
BR112013026137A8 (pt) 2018-01-30
BR112013026137B1 (pt) 2020-12-01
EP2699564A1 (en) 2014-02-26

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