JP6374959B2 - Dna−pk阻害剤 - Google Patents

Dna−pk阻害剤 Download PDF

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Publication number
JP6374959B2
JP6374959B2 JP2016523925A JP2016523925A JP6374959B2 JP 6374959 B2 JP6374959 B2 JP 6374959B2 JP 2016523925 A JP2016523925 A JP 2016523925A JP 2016523925 A JP2016523925 A JP 2016523925A JP 6374959 B2 JP6374959 B2 JP 6374959B2
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Prior art keywords
compound
alkyl
mmol
cancer
pharmaceutically acceptable
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Japanese (ja)
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JP2016533366A5 (enExample
JP2016533366A (ja
Inventor
ポール エス. チャリフソン,
ポール エス. チャリフソン,
ケビン マイケル コットレル,
ケビン マイケル コットレル,
ホンボ デン,
ホンボ デン,
ジョン ピー. ダフィー,
ジョン ピー. ダフィー,
ファイ ガオ,
ファイ ガオ,
サイモン ジルー,
サイモン ジルー,
ジェレミー グリーン,
ジェレミー グリーン,
カトリーナ リー ジャクソン,
カトリーナ リー ジャクソン,
ジョセフ エム. ケネディー,
ジョセフ エム. ケネディー,
デイビッド ジェイ. ラウファー,
デイビッド ジェイ. ラウファー,
マーク ウィレム レデボーア,
マーク ウィレム レデボーア,
パン リー,
パン リー,
ジョン パトリック マクスウェル,
ジョン パトリック マクスウェル,
マーク エー. モリス,
マーク エー. モリス,
アルバート チャールズ ピアース,
アルバート チャールズ ピアース,
ネイサン ディー. ワール,
ネイサン ディー. ワール,
ジンワン シュー,
ジンワン シュー,
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Priority claimed from US14/056,560 external-priority patent/US9376448B2/en
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of JP2016533366A publication Critical patent/JP2016533366A/ja
Publication of JP2016533366A5 publication Critical patent/JP2016533366A5/ja
Application granted granted Critical
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04Ortho-condensed systems

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2016523925A 2013-10-17 2014-10-17 Dna−pk阻害剤 Active JP6374959B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US14/056,560 US9376448B2 (en) 2012-04-24 2013-10-17 DNA-PK inhibitors
US14/056,560 2013-10-17
PCT/US2014/061033 WO2015058031A1 (en) 2013-10-17 2014-10-17 Dna-pk inhibitors

Publications (3)

Publication Number Publication Date
JP2016533366A JP2016533366A (ja) 2016-10-27
JP2016533366A5 JP2016533366A5 (enExample) 2017-11-24
JP6374959B2 true JP6374959B2 (ja) 2018-08-15

Family

ID=51932571

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016523925A Active JP6374959B2 (ja) 2013-10-17 2014-10-17 Dna−pk阻害剤

Country Status (17)

Country Link
EP (1) EP3057959B1 (enExample)
JP (1) JP6374959B2 (enExample)
CN (1) CN105636958B (enExample)
AU (1) AU2014337208B2 (enExample)
BR (1) BR112016008423B1 (enExample)
CA (1) CA2927392C (enExample)
DK (1) DK3057959T3 (enExample)
ES (1) ES2671354T3 (enExample)
HR (1) HRP20180804T1 (enExample)
HU (1) HUE037516T2 (enExample)
LT (1) LT3057959T (enExample)
PL (1) PL3057959T3 (enExample)
PT (1) PT3057959T (enExample)
RS (1) RS57306B1 (enExample)
SI (1) SI3057959T1 (enExample)
TR (1) TR201807411T4 (enExample)
WO (1) WO2015058031A1 (enExample)

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HRP20191937T1 (hr) 2012-09-25 2020-01-10 F. Hoffmann - La Roche Ag Derivati heksahidropirolo [3,4-c]pirola i srodni spojevi kao inhibitori autotaksina (atx) i kao inhibitori proizvodnje lizofosfatidne kiseline (lpa) za liječenje npr. bubrežnih bolesti
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
RS56776B1 (sr) 2013-11-26 2018-04-30 Hoffmann La Roche Derivati oktahidro-ciklobuta [1,2-c;3,4-c']dipirola kao inhibitori autotaksina
UA118582C2 (uk) 2014-03-26 2019-02-11 Ф. Хоффманн-Ля Рош Аг Біциклічні сполуки як інгібітори продукції аутотаксину (atx) і лізофосфатидилової кислоти (lpa)
CA2935612A1 (en) 2014-03-26 2015-10-01 F. Hoffmann-La Roche Ag Condensed [1,4]diazepine compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
CR20180058A (es) 2015-09-04 2018-02-26 Hoffmann La Roche Nuevos derivados de fenoximetilo
BR112017026682A2 (pt) 2015-09-24 2018-08-14 Hoffmann La Roche novos compostos bicíclicos como inibidores de dupla ação de atx/ca
EP3353176B1 (en) 2015-09-24 2022-01-19 F. Hoffmann-La Roche AG Bicyclic compounds as atx inhibitors
PE20180552A1 (es) 2015-09-24 2018-04-02 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores duales de atx/ca
EP3353180B1 (en) 2015-09-24 2022-03-16 F. Hoffmann-La Roche AG Bicyclic compounds as atx inhibitors
CR20180323A (es) 2015-11-20 2018-08-06 Idorsia Pharmaceuticals Ltd Derivados de indol n-sustituídos como moduladores de los receptores de pge2
MX394860B (es) * 2016-09-27 2025-03-24 Vertex Pharma Metodo para tratar cancer usando una combinacion de agentes que dañan adn e inhibidores de proteina cinasa dependiente de adn (adn-pk).
BR112019019017A2 (pt) 2017-03-16 2020-04-14 Hoffmann La Roche compostos heterocíclicos de utilidade como inibidores duplos de atx/ca
EP3596060B1 (en) 2017-03-16 2023-09-20 F. Hoffmann-La Roche AG New bicyclic compounds as atx inhibitors
ES2893452T3 (es) * 2017-05-18 2022-02-09 Idorsia Pharmaceuticals Ltd Derivados de pirimidina como moduladores del receptor de PGE2
EP3625223B1 (en) * 2017-05-18 2021-08-11 Idorsia Pharmaceuticals Ltd Pyrimidine derivatives
DK3625224T3 (da) 2017-05-18 2021-11-08 Idorsia Pharmaceuticals Ltd N-substituerede indolderivater
ES2887041T3 (es) * 2017-05-18 2021-12-21 Idorsia Pharmaceuticals Ltd Derivados de pirimidina como moduladores del receptor de PGE2
AR111807A1 (es) 2017-05-18 2019-08-21 Idorsia Pharmaceuticals Ltd Derivados de benzofurano y benzotiofeno como moduladores del receptor pge2
EP3717475B1 (en) 2017-11-20 2023-06-07 Icahn School of Medicine at Mount Sinai Kinase inhibitor compounds and compositions and methods of use
AU2019205944A1 (en) 2018-01-05 2020-07-09 Icahn School Of Medicine At Mount Sinai Method of increasing proliferation of pancreatic beta cells, treatment method, and composition
WO2019143675A1 (en) 2018-01-17 2019-07-25 Vertex Pharmaceuticals Incorporated Dna-pk inhibitors
JP7483612B2 (ja) 2018-01-17 2024-05-15 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 ゲノム編集効率を増加するためのキノキサリノン化合物、組成物、方法、およびキット
AU2019240065A1 (en) 2018-03-20 2020-09-24 Icahn School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
AU2019418800A1 (en) * 2018-12-31 2021-07-01 Icahn School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
CN112300126A (zh) * 2019-07-31 2021-02-02 山东轩竹医药科技有限公司 杂环类dna-pk抑制剂
CN112574211B (zh) * 2019-09-29 2022-06-14 山东轩竹医药科技有限公司 杂环类激酶抑制剂
CN112574179B (zh) * 2019-09-29 2022-05-10 山东轩竹医药科技有限公司 Dna-pk抑制剂
EP4086258A4 (en) * 2019-12-31 2023-11-29 Chengdu Baiyu Pharmaceutical Co., Ltd. Purine derivative and medical use thereof
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
TW202530228A (zh) 2023-10-12 2025-08-01 美商銳新醫藥公司 Ras抑制劑
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025217307A1 (en) 2024-04-09 2025-10-16 Revolution Medicines, Inc. Methods for predicting response to a ras(on) inhibitor and combination therapies
WO2025229177A1 (en) 2024-05-02 2025-11-06 Idorsia Pharmaceuticals Ltd Crystalline forms of an n-substituted indole derivative
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors

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AU2001288432A1 (en) * 2000-09-01 2002-03-22 Icos Corporation Materials and methods to potentiate cancer treatment
WO2005026129A1 (en) * 2003-09-15 2005-03-24 Gpc Biotech Ag Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases
US20090221581A1 (en) * 2005-05-25 2009-09-03 Philipp Wabnitz Methods of treating pain
MX2009003456A (es) * 2006-10-02 2009-04-14 Irm Llc Compuestos y composiciones como inhibidores de proteina cinasa.
US8518948B2 (en) * 2010-03-10 2013-08-27 Ingenium Pharmaceuticals Gmbh Inhibitors of protein kinases
SI3459942T1 (sl) * 2012-04-24 2021-05-31 Vertex Pharmaceuticals Incorporated Inhibitorji DNA-PK

Also Published As

Publication number Publication date
PL3057959T3 (pl) 2018-08-31
AU2014337208B2 (en) 2018-05-24
RS57306B1 (sr) 2018-08-31
JP2016533366A (ja) 2016-10-27
CA2927392A1 (en) 2015-04-23
EP3057959B1 (en) 2018-02-28
CA2927392C (en) 2021-11-09
CN105636958A (zh) 2016-06-01
WO2015058031A1 (en) 2015-04-23
TR201807411T4 (tr) 2018-06-21
BR112016008423B1 (pt) 2022-02-22
BR112016008423A2 (enExample) 2017-08-01
LT3057959T (lt) 2018-06-11
DK3057959T3 (en) 2018-06-06
ES2671354T3 (es) 2018-06-06
PT3057959T (pt) 2018-06-04
HUE037516T2 (hu) 2018-09-28
HRP20180804T1 (hr) 2018-08-10
CN105636958B (zh) 2018-01-05
SI3057959T1 (en) 2018-07-31
EP3057959A1 (en) 2016-08-24

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