CA2927392C - Dna-pk inhibitors - Google Patents

Dna-pk inhibitors Download PDF

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Publication number
CA2927392C
CA2927392C CA2927392A CA2927392A CA2927392C CA 2927392 C CA2927392 C CA 2927392C CA 2927392 A CA2927392 A CA 2927392A CA 2927392 A CA2927392 A CA 2927392A CA 2927392 C CA2927392 C CA 2927392C
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Canada
Prior art keywords
compound
date
mhz
nmr
date received
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CA2927392A
Other languages
English (en)
French (fr)
Other versions
CA2927392A1 (en
Inventor
Paul S. Charifson
Kevin Michael Cottrell
Hongbo Deng
John P. Duffy
Huai Gao
Simon Giroux
Jeremy Green
Katrina Lee Jackson
Joseph M. Kennedy
David J. Lauffer
Mark Willem Ledeboer
Pan Li
John Patrick Maxwell
Mark A. Morris
Albert Charles Pierce
Nathan D. Waal
Jinwang Xu
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.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from US14/056,560 external-priority patent/US9376448B2/en
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of CA2927392A1 publication Critical patent/CA2927392A1/en
Application granted granted Critical
Publication of CA2927392C publication Critical patent/CA2927392C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA2927392A 2013-10-17 2014-10-17 Dna-pk inhibitors Active CA2927392C (en)

Applications Claiming Priority (3)

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

Publications (2)

Publication Number Publication Date
CA2927392A1 CA2927392A1 (en) 2015-04-23
CA2927392C true CA2927392C (en) 2021-11-09

Family

ID=51932571

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2927392A Active CA2927392C (en) 2013-10-17 2014-10-17 Dna-pk inhibitors

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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CN104364239B (zh) 2012-06-13 2017-08-25 霍夫曼-拉罗奇有限公司 二氮杂螺环烷烃和氮杂螺环烷烃
MX368615B (es) 2012-09-25 2019-10-09 Hoffmann La Roche Derivados bicíclicos como inhibidores de la autotaxina (atx) que son inhibidores de la producción de ácido lisofosfatídico (lpa) y el uso de los mismos.
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
DK3074400T3 (en) 2013-11-26 2018-01-15 Hoffmann La Roche Octahydro-cyclobuta [1,2-c; 3,4-c '] dipyrrole derivatives as autotaxin inhibitors
EA032357B1 (ru) 2014-03-26 2019-05-31 Ф. Хоффманн-Ля Рош Аг Конденсированные [1,4]диазепиновые соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa)
CA2937616A1 (en) 2014-03-26 2015-10-01 F. Hoffmann-La Roche Ag Bicyclic 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
CA2992889A1 (en) 2015-09-04 2017-03-09 F. Hoffmann-La Roche Ag Phenoxymethyl derivatives
JP6876685B2 (ja) 2015-09-24 2021-05-26 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Atx阻害剤としての二環式化合物
WO2017050732A1 (en) 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
BR112017026682A2 (pt) 2015-09-24 2018-08-14 Hoffmann La Roche novos compostos bicíclicos como inibidores de dupla ação de atx/ca
AU2016328436B2 (en) 2015-09-24 2020-05-14 F. Hoffmann-La Roche Ag New bicyclic compounds as dual ATX/CA inhibitors
CR20180323A (es) 2015-11-20 2018-08-06 Idorsia Pharmaceuticals Ltd Derivados de indol n-sustituídos como moduladores de los receptores de pge2
EP3518931A4 (en) 2016-09-27 2020-05-13 Vertex Pharmaceuticals Incorporated METHOD FOR TREATING CANCER WITH A COMBINATION OF DNA-DAMAGING SUBSTANCES AND DNA-PK INHIBITORS
JP7090099B2 (ja) 2017-03-16 2022-06-23 エフ.ホフマン-ラ ロシュ アーゲー Atxインヒビターとしての新規二環式化合物
RU2019132254A (ru) 2017-03-16 2021-04-16 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca
US11839613B2 (en) * 2017-05-18 2023-12-12 Idorsia Pharmaceuticals Ltd Pyrimidine derivatives as PGE2 receptor modulators
PE20191814A1 (es) * 2017-05-18 2019-12-27 Idorsia Pharmaceuticals Ltd Derivados de pirimidina como moduladores del receptor de pge2
TWI768043B (zh) 2017-05-18 2022-06-21 瑞士商愛杜西亞製藥有限公司 N-取代吲哚衍生物
KR102612140B1 (ko) * 2017-05-18 2023-12-08 이도르시아 파마슈티컬스 리미티드 피리미딘 유도체
TW201900179A (zh) 2017-05-18 2019-01-01 瑞士商愛杜西亞製藥有限公司 作為pge2受體調節劑之苯并呋喃及苯并噻吩衍生物
WO2019100062A1 (en) 2017-11-20 2019-05-23 Ichan School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
WO2019136320A1 (en) 2018-01-05 2019-07-11 Icahn School Of Medicine At Mount Sinai Method of increasing proliferation of pancreatic beta cells, treatment method, and composition
JP7466448B2 (ja) 2018-01-17 2024-04-12 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 Dna-pk阻害剤
BR112020013626A2 (pt) 2018-01-17 2020-12-01 Vertex Pharmaceuticals Incorporated compostos de quinoxalinona, composições, métodos e kits para aumentar a eficiência de edição de genoma
CN112135613A (zh) 2018-03-20 2020-12-25 西奈山伊坎医学院 激酶抑制剂化合物和组合物及使用方法
JP2022515650A (ja) * 2018-12-31 2022-02-21 アイカーン スクール オブ メディシン アット マウント サイナイ キナーゼ阻害剤化合物及び組成物ならびに使用方法
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
CN113121574B (zh) * 2019-12-31 2023-02-17 成都百裕制药股份有限公司 嘌呤衍生物及其在医药上的用途
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ras相關疾病或病症之組合療法
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic ras inhibitors
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
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ras抑制劑
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
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
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WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

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US8084457B2 (en) * 2003-09-15 2011-12-27 Lead Discovery Center Gmbh Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases
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MX371331B (es) * 2012-04-24 2020-01-27 Vertex Pharma Inhibidores de la proteina cinasa dependiente de acido desoxirribonucleico(adn-pk).

Also Published As

Publication number Publication date
HUE037516T2 (hu) 2018-09-28
BR112016008423A2 (enExample) 2017-08-01
ES2671354T3 (es) 2018-06-06
EP3057959A1 (en) 2016-08-24
BR112016008423B1 (pt) 2022-02-22
WO2015058031A1 (en) 2015-04-23
DK3057959T3 (en) 2018-06-06
TR201807411T4 (tr) 2018-06-21
LT3057959T (lt) 2018-06-11
SI3057959T1 (en) 2018-07-31
JP6374959B2 (ja) 2018-08-15
CA2927392A1 (en) 2015-04-23
CN105636958B (zh) 2018-01-05
AU2014337208B2 (en) 2018-05-24
JP2016533366A (ja) 2016-10-27
HRP20180804T1 (hr) 2018-08-10
EP3057959B1 (en) 2018-02-28
PT3057959T (pt) 2018-06-04
CN105636958A (zh) 2016-06-01
PL3057959T3 (pl) 2018-08-31
RS57306B1 (sr) 2018-08-31

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Effective date: 20191017