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
- 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)
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) |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20161774T1 (hr) | 2012-06-13 | 2017-02-24 | F. Hoffmann - La Roche Ag | Novi diazaspirocikloalkan i azaspirocikloalkan |
| BR112015004111A2 (pt) | 2012-09-25 | 2017-07-04 | Hoffmann La Roche | novos derivados bicíclicos |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| KR20160087900A (ko) | 2013-11-26 | 2016-07-22 | 에프. 호프만-라 로슈 아게 | 신규한 옥타하이드로-사이클로부타[1,2-c；3,4-c'']다이피롤-2-일 |
| SI3122750T1 (sl) | 2014-03-26 | 2019-12-31 | F. Hoffmann-La Roche Ag | Biciklične spojine kot zaviralci proizvodnje avtotaksina (ATX) in lizofosfatidne kisline (LPA) |
| KR20160128428A (ko) | 2014-03-26 | 2016-11-07 | 에프. 호프만-라 로슈 아게 | 오토탁신(atx) 및 리소포스파티드산(lpa) 생성 억제제로서의 축합형 [1,4]다이아제핀 화합물 |
| MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
| JP6886967B2 (ja) | 2015-09-04 | 2021-06-16 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | フェノキシメチル誘導体 |
| RU2018112230A (ru) | 2015-09-24 | 2019-10-30 | Ф. Хоффманн-Ля Рош Аг | Бициклические соединения в качестве ингибиторов atx |
| CN107635995B (zh) | 2015-09-24 | 2022-08-19 | 豪夫迈·罗氏有限公司 | 作为atx抑制剂的二环化合物 |
| JP6877413B2 (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 | 二重ａｔｘ／ｃａ阻害剤としての新規な二環式化合物 |
| AU2016328365B2 (en) | 2015-09-24 | 2020-04-23 | 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 |
| EP3596059B1 (en) | 2017-03-16 | 2024-04-24 | F. Hoffmann-La Roche AG | Heterocyclic compounds useful as dual atx/ca inhibitors |
| WO2018167113A1 (en) | 2017-03-16 | 2018-09-20 | F. Hoffmann-La Roche Ag | New bicyclic compounds as atx inhibitors |
| EP3625223B1 (en) | 2017-05-18 | 2021-08-11 | Idorsia Pharmaceuticals Ltd | Pyrimidine derivatives |
| JP7093791B2 (ja) | 2017-05-18 | 2022-06-30 | イドーシア ファーマシューティカルズ リミテッド | Ｐｇｅ２レセプター調節剤としてのベンゾフラン及びベンゾチオフェン誘導体 |
| MX388257B (es) * | 2017-05-18 | 2025-03-19 | Idorsia Pharmaceuticals Ltd | Derivados de pirimidina como moduladores del receptor de pge2. |
| US20200069686A1 (en) | 2017-05-18 | 2020-03-05 | Idorsia Pharmaceuticals Ltd | N-substituted indole derivatives |
| AR111941A1 (es) | 2017-05-18 | 2019-09-04 | Idorsia Pharmaceuticals Ltd | Derivados de pirimidina como moduladores del receptor de pge2 |
| US11547712B2 (en) | 2017-11-20 | 2023-01-10 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| CN111819193A (zh) | 2018-01-05 | 2020-10-23 | 西奈山伊坎医学院 | 增加胰腺β细胞增殖的方法、治疗方法以及组合物 |
| ES2940786T3 (es) | 2018-01-17 | 2023-05-11 | Vertex Pharma | Compuestos de quinoxalinona, composiciones, métodos y kits para aumentar la eficiencia de edición del genoma |
| EA202091709A1 (ru) | 2018-01-17 | 2020-11-10 | Вертекс Фармасьютикалз Инкорпорейтед | Ингибиторы днк-пк |
| AU2019240065A1 (en) | 2018-03-20 | 2020-09-24 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| CA3124353A1 (en) * | 2018-12-31 | 2020-07-09 | 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 |
| WO2021136463A1 (zh) * | 2019-12-31 | 2021-07-08 | 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 |
| 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 |
| 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 |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2001288432A1 (en) * | 2000-09-01 | 2002-03-22 | 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 |
| EP1901747A2 (en) * | 2005-05-25 | 2008-03-26 | Ingenium Pharmaceuticals AG | Pyrimidine-based cdk inhibitors for treating pain |
| CN103739595A (zh) * | 2006-10-02 | 2014-04-23 | Irm责任有限公司 | 作为蛋白激酶抑制剂的化合物和组合物 |
| SG183192A1 (en) * | 2010-03-10 | 2012-09-27 | Ingenium Pharmaceuticals Gmbh | Inhibitors of protein kinases |
| IN2014KN02601A (enExample) * | 2012-04-24 | 2015-05-08 | Vertex Pharma |
-
2014
- 2014-10-17 WO PCT/US2014/061033 patent/WO2015058031A1/en not_active Ceased
- 2014-10-17 JP JP2016523925A patent/JP6374959B2/ja active Active
- 2014-10-17 SI SI201430733T patent/SI3057959T1/en unknown
- 2014-10-17 AU AU2014337208A patent/AU2014337208B2/en active Active
- 2014-10-17 EP EP14800181.1A patent/EP3057959B1/en active Active
- 2014-10-17 HU HUE14800181A patent/HUE037516T2/hu unknown
- 2014-10-17 CA CA2927392A patent/CA2927392C/en active Active
- 2014-10-17 HR HRP20180804TT patent/HRP20180804T1/hr unknown
- 2014-10-17 DK DK14800181.1T patent/DK3057959T3/en active
- 2014-10-17 BR BR112016008423-3A patent/BR112016008423B1/pt active IP Right Grant
- 2014-10-17 CN CN201480057118.6A patent/CN105636958B/zh active Active
- 2014-10-17 TR TR2018/07411T patent/TR201807411T4/tr unknown
- 2014-10-17 PL PL14800181T patent/PL3057959T3/pl unknown
- 2014-10-17 ES ES14800181.1T patent/ES2671354T3/es active Active
- 2014-10-17 PT PT148001811T patent/PT3057959T/pt unknown
- 2014-10-17 LT LTEP14800181.1T patent/LT3057959T/lt unknown
- 2014-10-17 RS RS20180605A patent/RS57306B1/sr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP3057959B1 (en) | 2018-02-28 |
| CA2927392C (en) | 2021-11-09 |
| HUE037516T2 (hu) | 2018-09-28 |
| BR112016008423A2 (enExample) | 2017-08-01 |
| PL3057959T3 (pl) | 2018-08-31 |
| TR201807411T4 (tr) | 2018-06-21 |
| CA2927392A1 (en) | 2015-04-23 |
| LT3057959T (lt) | 2018-06-11 |
| BR112016008423B1 (pt) | 2022-02-22 |
| SI3057959T1 (en) | 2018-07-31 |
| PT3057959T (pt) | 2018-06-04 |
| HRP20180804T1 (hr) | 2018-08-10 |
| DK3057959T3 (en) | 2018-06-06 |
| RS57306B1 (sr) | 2018-08-31 |
| CN105636958A (zh) | 2016-06-01 |
| EP3057959A1 (en) | 2016-08-24 |
| ES2671354T3 (es) | 2018-06-06 |
| CN105636958B (zh) | 2018-01-05 |
| AU2014337208B2 (en) | 2018-05-24 |
| WO2015058031A1 (en) | 2015-04-23 |
| JP2016533366A (ja) | 2016-10-27 |
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