JP6543252B2 - ＡＴＲキナーゼ阻害剤として有用な２−アミノ−６−フルオロ−Ｎ−［５−フルオロ−ピリジン−３−イル］ピラゾロ［１，５−ａ］ピリミジン−３−カルボキサミド化合物、その調製、その異なる固体形態および放射性標識された誘導体 - Google Patents

ＡＴＲキナーゼ阻害剤として有用な２−アミノ−６−フルオロ−Ｎ−［５−フルオロ−ピリジン−３−イル］ピラゾロ［１，５−ａ］ピリミジン−３−カルボキサミド化合物、その調製、その異なる固体形態および放射性標識された誘導体 Download PDF

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JP6543252B2
JP6543252B2 JP2016536576A JP2016536576A JP6543252B2 JP 6543252 B2 JP6543252 B2 JP 6543252B2 JP 2016536576 A JP2016536576 A JP 2016536576A JP 2016536576 A JP2016536576 A JP 2016536576A JP 6543252 B2 JP6543252 B2 JP 6543252B2
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formula
composition
solid form
pharmaceutically acceptable
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JP2016539155A5 (enExample
JP2016539155A (ja
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ジーン−ダミアン シャリエ，
ジーン−ダミアン シャリエ，
クリストファー ジョン デイビス，
クリストファー ジョン デイビス，
ダミアン フレイス，
ダミアン フレイス，
イ ハリディ， ゴルカ エチェバリア
イ ハリディ， ゴルカ エチェバリア
サイモン ペグ，
サイモン ペグ，
フランソワーズ ピラード，
フランソワーズ ピラード，
ジョアン ピンダー，
ジョアン ピンダー，
ジョン スタッドリー，
ジョン スタッドリー，
カール ズウィカー，
カール ズウィカー，
タパン サングビ，
タパン サングビ，
マイケル ウォールドー，
マイケル ウォールドー，
アレス メデック，
アレス メデック，
デイビッド マシュー シャウ，
デイビッド マシュー シャウ，
マニンダー パネサル，
マニンダー パネサル，
ユエガン ジャン，
ユエガン ジャン，
ナジハ アレム，
ナジハ アレム，
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • 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
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/63—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by introduction of halogen; by substitution of halogen atoms by other halogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Epidemiology (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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Physics & Mathematics (AREA)
  • Condensed Matter Physics & Semiconductors (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2016536576A 2013-12-06 2014-12-05 ＡＴＲキナーゼ阻害剤として有用な２−アミノ−６−フルオロ−Ｎ−［５−フルオロ−ピリジン−３−イル］ピラゾロ［１，５−ａ］ピリミジン−３−カルボキサミド化合物、その調製、その異なる固体形態および放射性標識された誘導体 Active JP6543252B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201361912636P 2013-12-06 2013-12-06
US61/912,636 2013-12-06
US201462008220P 2014-06-05 2014-06-05
US62/008,220 2014-06-05
US201462058819P 2014-10-02 2014-10-02
US62/058,819 2014-10-02
PCT/US2014/068713 WO2015085132A1 (en) 2013-12-06 2014-12-05 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof

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JP2016539155A JP2016539155A (ja) 2016-12-15
JP2016539155A5 JP2016539155A5 (enExample) 2017-05-18
JP6543252B2 true JP6543252B2 (ja) 2019-07-10

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WO (1) WO2015085132A1 (enExample)
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BR112015012454B1 (pt) 2012-12-07 2022-07-05 Vertex Pharmaceuticals Incorporated Compostos inibidores de atr quinase, seu uso e composição farmacêutica compreendendo os mesmos
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