JP6374959B2 - Ｄｎａ−ｐｋ阻害剤 - Google Patents
Ｄｎａ−ｐｋ阻害剤 Download PDFInfo
- 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
- Authority
- JP
- Japan
- Prior art keywords
- compound
- alkyl
- mmol
- cancer
- pharmaceutically acceptable
- 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
Links
- 0 Cc1cnc(*)cc1 Chemical compound Cc1cnc(*)cc1 0.000 description 20
- AKPUZJOEQGBKPY-HSHIGALWSA-N C/C=N\C=C(\C)/C=C Chemical compound C/C=N\C=C(\C)/C=C AKPUZJOEQGBKPY-HSHIGALWSA-N 0.000 description 1
- HPZXEWQLFFUHHD-UHFFFAOYSA-N CC(COc1ccccc1Br)=C Chemical compound CC(COc1ccccc1Br)=C HPZXEWQLFFUHHD-UHFFFAOYSA-N 0.000 description 1
- SGYAHQJEQHTWHR-VOTSOKGWSA-N CC1(C)c2cccc(/C=C/[N+]([O-])=O)c2OC1 Chemical compound CC1(C)c2cccc(/C=C/[N+]([O-])=O)c2OC1 SGYAHQJEQHTWHR-VOTSOKGWSA-N 0.000 description 1
- HNCLOAJZDAMBQR-UHFFFAOYSA-N CC1(C)c2cccc(C=O)c2OC1 Chemical compound CC1(C)c2cccc(C=O)c2OC1 HNCLOAJZDAMBQR-UHFFFAOYSA-N 0.000 description 1
- FHRIFPIEZKZPBE-UHFFFAOYSA-N CC1(C)c2cccc(CCN)c2OC1 Chemical compound CC1(C)c2cccc(CCN)c2OC1 FHRIFPIEZKZPBE-UHFFFAOYSA-N 0.000 description 1
- SNOPQSLWDMEXLN-UHFFFAOYSA-N CC1(C)c2cccc(CCNc3cc(-c4ccc(N5CCN(C)CC5)nc4)ncn3)c2OC1 Chemical compound CC1(C)c2cccc(CCNc3cc(-c4ccc(N5CCN(C)CC5)nc4)ncn3)c2OC1 SNOPQSLWDMEXLN-UHFFFAOYSA-N 0.000 description 1
- MNUVJIPQYZJXAV-UHFFFAOYSA-N CC1(C)c2cccc(CCNc3cc(Cl)ncn3)c2OC1 Chemical compound CC1(C)c2cccc(CCNc3cc(Cl)ncn3)c2OC1 MNUVJIPQYZJXAV-UHFFFAOYSA-N 0.000 description 1
- BEIGEFOVGRASOO-UHFFFAOYSA-N CC1(C)c2ccccc2OC1 Chemical compound CC1(C)c2ccccc2OC1 BEIGEFOVGRASOO-UHFFFAOYSA-N 0.000 description 1
- XOGDXTACOCVNOT-UHFFFAOYSA-N CC1(C23C)C=NC2=CC(C)=CC=C3N=C1 Chemical compound CC1(C23C)C=NC2=CC(C)=CC=C3N=C1 XOGDXTACOCVNOT-UHFFFAOYSA-N 0.000 description 1
- MVTHDBVIVSNEHZ-UHFFFAOYSA-N Cc(cc1N=C)ccc1SC Chemical compound Cc(cc1N=C)ccc1SC MVTHDBVIVSNEHZ-UHFFFAOYSA-N 0.000 description 1
- XJPZKYIHCLDXST-UHFFFAOYSA-N Clc1cc(Cl)ncn1 Chemical compound Clc1cc(Cl)ncn1 XJPZKYIHCLDXST-UHFFFAOYSA-N 0.000 description 1
- VADKRMSMGWJZCF-UHFFFAOYSA-N Oc1ccccc1Br Chemical compound Oc1ccccc1Br VADKRMSMGWJZCF-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/14—Heterocyclic 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
-
- 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
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D403/14—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 three or more hetero rings
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic 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
- C07D471/02—Heterocyclic 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
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (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)
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 (esLanguage) | 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 (esLanguage) |
| JP (1) | JP6374959B2 (esLanguage) |
| CN (1) | CN105636958B (esLanguage) |
| AU (1) | AU2014337208B2 (esLanguage) |
| BR (1) | BR112016008423B1 (esLanguage) |
| CA (1) | CA2927392C (esLanguage) |
| DK (1) | DK3057959T3 (esLanguage) |
| ES (1) | ES2671354T3 (esLanguage) |
| HR (1) | HRP20180804T1 (esLanguage) |
| HU (1) | HUE037516T2 (esLanguage) |
| LT (1) | LT3057959T (esLanguage) |
| PL (1) | PL3057959T3 (esLanguage) |
| PT (1) | PT3057959T (esLanguage) |
| RS (1) | RS57306B1 (esLanguage) |
| SI (1) | SI3057959T1 (esLanguage) |
| TR (1) | TR201807411T4 (esLanguage) |
| WO (1) | WO2015058031A1 (esLanguage) |
Families Citing this family (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112014030473A2 (pt) | 2012-06-13 | 2017-06-27 | Hoffmann La Roche | novo diazaespirocicloalcano e azaespirocicloalcano |
| SI2900669T1 (sl) | 2012-09-25 | 2019-12-31 | F. Hoffmann-La Roche Ag | Derivati heksahidropirolo(3,4-C)pirola in sorodne spojine kot zaviralci avtotaksina (ATX) in kot zaviralci tvorbe lizofosfatidne kisline (LPA) za zdravljenje npr. bolezni ledvic |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| JP6496730B2 (ja) | 2013-11-26 | 2019-04-03 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 新規なオクタヒドロ−シクロブタ［１，２−ｃ；３，４−ｃ’］ジピロール−２−イル |
| MX373236B (es) | 2014-03-26 | 2020-05-08 | Hoffmann La Roche | Compuestos condensados de [1,4]diazepina como inhibidores de producción de la autotaxina (atx) y ácido lisofosfatidico (lpa). |
| MX370659B (es) | 2014-03-26 | 2019-12-19 | Hoffmann La Roche | Compuestos bicíclicos como inhibidores de producción de autotaxina (atx) y ácido lisofosfatídico (lpa). |
| MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
| MX387736B (es) | 2015-09-04 | 2025-03-18 | Hoffmann La Roche | Derivados de fenoximetilo. |
| PE20180461A1 (es) | 2015-09-24 | 2018-03-06 | Hoffmann La Roche | Nuevos compuestos biciclicos como inhibidores de la atx |
| KR20180054635A (ko) | 2015-09-24 | 2018-05-24 | 에프. 호프만-라 로슈 아게 | 오토탁신(atx) 억제제로서 이환형 화합물 |
| CA2984585A1 (en) | 2015-09-24 | 2017-03-30 | F. Hoffmann-La Roche Ag | New bicyclic compounds as dual atx/ca inhibitors |
| KR20180054634A (ko) | 2015-09-24 | 2018-05-24 | 에프. 호프만-라 로슈 아게 | 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서 신규한 이환형 화합물 |
| CR20180323A (es) | 2015-11-20 | 2018-08-06 | Idorsia Pharmaceuticals Ltd | Derivados de indol n-sustituídos como moduladores de los receptores de pge2 |
| RU2758669C2 (ru) | 2016-09-27 | 2021-11-01 | Вертекс Фармасьютикалз Инкорпорейтед | Способ лечения рака с применением сочетания днк-поражающих агентов и ингибиторов днк-пк |
| WO2018167113A1 (en) | 2017-03-16 | 2018-09-20 | F. Hoffmann-La Roche Ag | New bicyclic compounds as atx inhibitors |
| CN110392679B (zh) | 2017-03-16 | 2023-04-07 | 豪夫迈·罗氏有限公司 | 可用作双重atx/ca抑制剂的杂环化合物 |
| KR102632028B1 (ko) * | 2017-05-18 | 2024-01-31 | 이도르시아 파마슈티컬스 리미티드 | Pge2 수용체 조절제로서의 페닐 유도체 |
| 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 |
| PE20191811A1 (es) * | 2017-05-18 | 2019-12-26 | Idorsia Pharmaceuticals Ltd | Derivados de pirimidina como moduladores del receptor de pge2 |
| WO2018210987A1 (en) | 2017-05-18 | 2018-11-22 | Idorsia Pharmaceuticals Ltd | Benzofurane and benzothiophene derivatives as pge2 receptor modulators |
| EP3625223B1 (en) * | 2017-05-18 | 2021-08-11 | Idorsia Pharmaceuticals Ltd | Pyrimidine derivatives |
| US11547712B2 (en) | 2017-11-20 | 2023-01-10 | Icahn 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 |
| MA51623A (fr) | 2018-01-17 | 2021-04-14 | Vertex Pharma | Composés de quinoxalinone, compositions, procédés et kits pour augmenter l'efficacité d'édition du génome |
| AU2019209290B2 (en) | 2018-01-17 | 2024-03-07 | Vertex Pharmaceuticals Incorporated | DNA-PK inhibitors |
| 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 |
| CN113543783A (zh) * | 2018-12-31 | 2021-10-22 | 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | 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 |
| 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 |
| WO2026015790A1 (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 |
| 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 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7179912B2 (en) * | 2000-09-01 | 2007-02-20 | Icos Corporation | Materials and methods to potentiate cancer treatment |
| EP1678147B1 (en) * | 2003-09-15 | 2012-08-08 | Lead Discovery Center GmbH | Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases |
| WO2006125616A2 (en) * | 2005-05-25 | 2006-11-30 | Ingenium Pharmaceuticals Ag | Pyrimidine-based cdk inhibitors for treating pain |
| AU2007305016B2 (en) * | 2006-10-02 | 2011-11-03 | Novartis Ag | Compounds and compositions as protein kinase inhibitors |
| SG183192A1 (en) * | 2010-03-10 | 2012-09-27 | Ingenium Pharmaceuticals Gmbh | Inhibitors of protein kinases |
| SI2841428T1 (sl) * | 2012-04-24 | 2018-12-31 | Vertex Pharmaceuticals Incorporated | Inhibitorji DNA-PK |
-
2014
- 2014-10-17 ES ES14800181.1T patent/ES2671354T3/es active Active
- 2014-10-17 DK DK14800181.1T patent/DK3057959T3/en active
- 2014-10-17 WO PCT/US2014/061033 patent/WO2015058031A1/en not_active Ceased
- 2014-10-17 AU AU2014337208A patent/AU2014337208B2/en active Active
- 2014-10-17 BR BR112016008423-3A patent/BR112016008423B1/pt active IP Right Grant
- 2014-10-17 CA CA2927392A patent/CA2927392C/en active Active
- 2014-10-17 HU HUE14800181A patent/HUE037516T2/hu unknown
- 2014-10-17 TR TR2018/07411T patent/TR201807411T4/tr unknown
- 2014-10-17 JP JP2016523925A patent/JP6374959B2/ja active Active
- 2014-10-17 EP EP14800181.1A patent/EP3057959B1/en active Active
- 2014-10-17 SI SI201430733T patent/SI3057959T1/en unknown
- 2014-10-17 PT PT148001811T patent/PT3057959T/pt unknown
- 2014-10-17 RS RS20180605A patent/RS57306B1/sr unknown
- 2014-10-17 PL PL14800181T patent/PL3057959T3/pl unknown
- 2014-10-17 HR HRP20180804TT patent/HRP20180804T1/hr unknown
- 2014-10-17 CN CN201480057118.6A patent/CN105636958B/zh active Active
- 2014-10-17 LT LTEP14800181.1T patent/LT3057959T/lt unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PL3057959T3 (pl) | 2018-08-31 |
| PT3057959T (pt) | 2018-06-04 |
| LT3057959T (lt) | 2018-06-11 |
| RS57306B1 (sr) | 2018-08-31 |
| AU2014337208B2 (en) | 2018-05-24 |
| EP3057959B1 (en) | 2018-02-28 |
| CA2927392A1 (en) | 2015-04-23 |
| CN105636958A (zh) | 2016-06-01 |
| BR112016008423B1 (pt) | 2022-02-22 |
| TR201807411T4 (tr) | 2018-06-21 |
| BR112016008423A2 (esLanguage) | 2017-08-01 |
| CA2927392C (en) | 2021-11-09 |
| WO2015058031A1 (en) | 2015-04-23 |
| EP3057959A1 (en) | 2016-08-24 |
| SI3057959T1 (en) | 2018-07-31 |
| ES2671354T3 (es) | 2018-06-06 |
| CN105636958B (zh) | 2018-01-05 |
| HRP20180804T1 (hr) | 2018-08-10 |
| JP2016533366A (ja) | 2016-10-27 |
| DK3057959T3 (en) | 2018-06-06 |
| HUE037516T2 (hu) | 2018-09-28 |
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