JP6212045B2 - Ａｔｒキナーゼの阻害剤として有用な化合物を作製するためのプロセス - Google Patents

Ａｔｒキナーゼの阻害剤として有用な化合物を作製するためのプロセス Download PDF

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JP6212045B2
JP6212045B2 JP2014533441A JP2014533441A JP6212045B2 JP 6212045 B2 JP6212045 B2 JP 6212045B2 JP 2014533441 A JP2014533441 A JP 2014533441A JP 2014533441 A JP2014533441 A JP 2014533441A JP 6212045 B2 JP6212045 B2 JP 6212045B2
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formula
item
conditions
solvent
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JP2014532054A (ja
JP2014532054A5 (enExample
Inventor
ジャン−ダミアン シャリエ，
ジャン−ダミアン シャリエ，
ジョン スタッドレー，
ジョン スタッドレー，
フランソワ イヴォンヌ テオドラ マリー ピラール，
フランソワ イヴォンヌ テオドラ マリー ピラール，
スティーブン ジョン デュラント，
スティーブン ジョン デュラント，
ベンジャミン ジョセフ リトラー，
ベンジャミン ジョセフ リトラー，
ロバート マイケル ユース，
ロバート マイケル ユース，
デイビッド アンドリュー シーセル，
デイビッド アンドリュー シーセル，
ポール アンジェル，
ポール アンジェル，
アルマンド ウルビーナ，
アルマンド ウルビーナ，
イー シー，
イー シー，
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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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • 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
    • C07C251/00—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
    • C07C251/32—Oximes
    • C07C251/34—Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • C07C251/48—Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with the carbon atom of at least one of the oxyimino groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C269/06—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D309/14—Nitrogen atoms not forming part of a nitro radical
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
JP2014533441A 2011-09-30 2012-09-28 Ａｔｒキナーゼの阻害剤として有用な化合物を作製するためのプロセス Expired - Fee Related JP6212045B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161541865P 2011-09-30 2011-09-30
US61/541,865 2011-09-30
PCT/US2012/058127 WO2013049726A2 (en) 2011-09-30 2012-09-28 Processes for making compounds useful as inhibitors of atr kinase

Related Child Applications (2)

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JP2016221714A Division JP6317800B2 (ja) 2011-09-30 2016-11-14 Ａｔｒキナーゼの阻害剤として有用な化合物を作製するためのプロセス
JP2017148280A Division JP2017226676A (ja) 2011-09-30 2017-07-31 Ａｔｒキナーゼの阻害剤として有用な化合物を作製するためのプロセス

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JP2014532054A JP2014532054A (ja) 2014-12-04
JP2014532054A5 JP2014532054A5 (enExample) 2015-11-12
JP6212045B2 true JP6212045B2 (ja) 2017-10-11

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JP2014533441A Expired - Fee Related JP6212045B2 (ja) 2011-09-30 2012-09-28 Ａｔｒキナーゼの阻害剤として有用な化合物を作製するためのプロセス
JP2016221714A Expired - Fee Related JP6317800B2 (ja) 2011-09-30 2016-11-14 Ａｔｒキナーゼの阻害剤として有用な化合物を作製するためのプロセス
JP2017148280A Withdrawn JP2017226676A (ja) 2011-09-30 2017-07-31 Ａｔｒキナーゼの阻害剤として有用な化合物を作製するためのプロセス
JP2019099224A Pending JP2019172684A (ja) 2011-09-30 2019-05-28 Ａｔｒキナーゼの阻害剤として有用な化合物を作製するためのプロセス

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JP2016221714A Expired - Fee Related JP6317800B2 (ja) 2011-09-30 2016-11-14 Ａｔｒキナーゼの阻害剤として有用な化合物を作製するためのプロセス
JP2017148280A Withdrawn JP2017226676A (ja) 2011-09-30 2017-07-31 Ａｔｒキナーゼの阻害剤として有用な化合物を作製するためのプロセス
JP2019099224A Pending JP2019172684A (ja) 2011-09-30 2019-05-28 Ａｔｒキナーゼの阻害剤として有用な化合物を作製するためのプロセス

Country Status (23)

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US (4) US9035053B2 (enExample)
EP (4) EP2751097A2 (enExample)
JP (4) JP6212045B2 (enExample)
KR (2) KR102184246B1 (enExample)
CN (2) CN103987709B (enExample)
AR (1) AR088092A1 (enExample)
AU (3) AU2012315615A1 (enExample)
BR (1) BR112014007721B1 (enExample)
CA (2) CA2850566C (enExample)
ES (1) ES2751741T3 (enExample)
HR (1) HRP20191641T1 (enExample)
HU (1) HUE046429T2 (enExample)
IL (3) IL231771A0 (enExample)
IN (1) IN2014KN00929A (enExample)
MX (1) MX353461B (enExample)
PL (1) PL2940017T3 (enExample)
PT (1) PT2940017T (enExample)
RS (1) RS59337B1 (enExample)
RU (2) RU2677292C2 (enExample)
SG (2) SG10201606774UA (enExample)
TW (3) TWI625324B (enExample)
WO (1) WO2013049726A2 (enExample)
ZA (1) ZA201402625B (enExample)

Cited By (1)

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JP2017061519A (ja) * 2011-09-30 2017-03-30 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ａｔｒキナーゼの阻害剤として有用な化合物を作製するためのプロセス

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US9630956B2 (en) 2010-05-12 2017-04-25 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
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CN102947272A (zh) 2010-05-12 2013-02-27 沃泰克斯药物股份有限公司 用作atr激酶抑制剂的2-氨基吡啶衍生物
JP2013526538A (ja) 2010-05-12 2013-06-24 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｔｒキナーゼ阻害剤として有用な化合物
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CA2932757C (en) 2013-12-06 2023-10-31 Vertex Pharmaceuticals Incorporated 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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JP6918829B2 (ja) 2016-01-11 2021-08-11 メリマック ファーマシューティカルズ インコーポレーティッド 血管拡張性失調症及びＲａｄ３関連タンパク質（ＡＴＲ）の阻害
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