JP7655863B2 - Ｄｎａポリメラーゼシータ阻害剤としてのチアジアゾリル誘導体 - Google Patents
Ｄｎａポリメラーゼシータ阻害剤としてのチアジアゾリル誘導体 Download PDFInfo
- Publication number
- JP7655863B2 JP7655863B2 JP2021570943A JP2021570943A JP7655863B2 JP 7655863 B2 JP7655863 B2 JP 7655863B2 JP 2021570943 A JP2021570943 A JP 2021570943A JP 2021570943 A JP2021570943 A JP 2021570943A JP 7655863 B2 JP7655863 B2 JP 7655863B2
- Authority
- JP
- Japan
- Prior art keywords
- thiadiazol
- mixture
- oxy
- cancer
- chlorobenzyl
- 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.)
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Classifications
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 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
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962855495P | 2019-05-31 | 2019-05-31 | |
| US62/855,495 | 2019-05-31 | ||
| US202062990239P | 2020-03-16 | 2020-03-16 | |
| US62/990,239 | 2020-03-16 | ||
| PCT/US2020/035165 WO2020243459A1 (en) | 2019-05-31 | 2020-05-29 | Thiadiazolyl derivatives as dna polymerase theta inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022535227A JP2022535227A (ja) | 2022-08-05 |
| JP2022535227A5 JP2022535227A5 (https=) | 2023-06-06 |
| JP7655863B2 true JP7655863B2 (ja) | 2025-04-02 |
Family
ID=72179163
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021570943A Active JP7655863B2 (ja) | 2019-05-31 | 2020-05-29 | Ｄｎａポリメラーゼシータ阻害剤としてのチアジアゾリル誘導体 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US12509454B2 (https=) |
| EP (1) | EP3976608B1 (https=) |
| JP (1) | JP7655863B2 (https=) |
| CN (1) | CN114127062A (https=) |
| AU (1) | AU2020282768B2 (https=) |
| BR (1) | BR112021024101A2 (https=) |
| CA (1) | CA3141134A1 (https=) |
| ES (1) | ES2968796T3 (https=) |
| TW (1) | TW202110834A (https=) |
| WO (1) | WO2020243459A1 (https=) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW202237595A (zh) * | 2020-12-02 | 2022-10-01 | 美商愛德亞生物科學公司 | 作為DNA聚合酶θ抑制劑之經取代噻二唑基衍生物 |
| TW202315618A (zh) * | 2021-06-11 | 2023-04-16 | 美商愛德亞生物科學公司 | 作為DNA聚合酶θ抑制劑之O-聯結噻二唑基化合物 |
| MX2024003795A (es) * | 2021-09-29 | 2024-06-03 | Repare Therapeutics Inc | Compuestos de n-(5-sustituido-[(1,3,4-tiadiazolil) o (tiazolil)])(sustituido)carboxamida y uso de estos para inhibir la polimerasa theta humana. |
| WO2023060573A1 (en) * | 2021-10-15 | 2023-04-20 | Beijing Danatlas Pharmaceutical Co., Ltd. | Novel thiadiazolyl derivatives of dna polymerase theta inhibitors |
| WO2023067515A1 (en) * | 2021-10-22 | 2023-04-27 | Ideaya Biosciences, Inc. | Thiadiazolyl compounds as dna polymerase theta inhibitors |
| EP4455129A4 (en) * | 2021-12-30 | 2025-05-07 | Shanghai Apeiron Therapeutics Company Limited | Dna polymerase theta inhibitor and use thereof |
| CN118510778A (zh) * | 2022-01-12 | 2024-08-16 | 百济神州有限公司 | 作为DNA聚合酶θ抑制剂的噻唑并吡啶基酰胺衍生物 |
| US20250122221A1 (en) | 2022-01-13 | 2025-04-17 | Nanjing Zaiming Pharmaceutical Co., Ltd. | Six-membered cyclothiazole compound and use thereof |
| TW202332442A (zh) | 2022-01-31 | 2023-08-16 | 瑞士商瑞森製藥公司 | ＰＯＬθ抑制劑 |
| CN118871430A (zh) * | 2022-03-10 | 2024-10-29 | 西藏海思科制药有限公司 | DNA聚合酶 θ 抑制剂及其用途 |
| WO2023202623A1 (zh) * | 2022-04-20 | 2023-10-26 | 南京再明医药有限公司 | Polq抑制剂化合物及其应用 |
| CA3257870A1 (en) * | 2022-06-01 | 2023-12-07 | Ideaya Biosciences, Inc. | THIADIAZOLYL DERIVATIVES USED AS DNA POLYMERASE THETA INHIBITORS AND THEIR USES |
| WO2023241322A1 (en) * | 2022-06-16 | 2023-12-21 | Danatlas Pharmaceuticals Co., Ltd. | Heterocyclic derivatives, compositions and uses thereof |
| AU2023352129A1 (en) * | 2022-09-29 | 2025-05-01 | Repare Therapeutics Inc. | N-(5-substituted-[(1,3,4-thiadiazolyl) or (1,3-thiazolyl)](substituted)carboxamide compounds, pharmaceutical compositions, and methods of preparing the amide compounds and of their use |
| AU2023356904A1 (en) * | 2022-10-03 | 2025-05-22 | Recombination Therapeutics, Llc | Pyrrolidine and imidazolidine based dna polymerase theta inhibitors and use thereof |
| CN117946138A (zh) * | 2022-10-28 | 2024-04-30 | 杭州圣域生物医药科技有限公司 | 并环含氮化合物、其中间体、制备方法和应用 |
| CN120077028A (zh) * | 2022-11-10 | 2025-05-30 | 北京丹擎医药科技有限公司 | 噻二唑衍生物及其组合物和应用 |
| WO2024099336A1 (en) * | 2022-11-10 | 2024-05-16 | Danatlas Pharmaceuticals Co., Ltd. | Thiadiazolyl derivatives, compositions and uses thereof |
| JP2025541823A (ja) * | 2022-12-09 | 2025-12-23 | グラクソスミスクライン、インテレクチュアル、プロパティー、（ナンバー４）、リミテッド | Ｄｎａポリメラーゼシータ阻害剤としてのチアジアゾリル誘導体およびその使用 |
| WO2024149349A1 (zh) * | 2023-01-14 | 2024-07-18 | 西藏海思科制药有限公司 | 靶向Polθ的化合物及其用途 |
| KR20250153866A (ko) | 2023-03-10 | 2025-10-27 | 브레이크포인트 테라퓨틱스 게엠베하 | Dna 중합효소 세타 억제제 |
| WO2024211836A2 (en) | 2023-04-05 | 2024-10-10 | Moma Therapeutics, Inc. | Semi-saturated bicyclic derivatives and related uses |
| WO2024213082A1 (en) * | 2023-04-13 | 2024-10-17 | Danatlas Pharmaceuticals Co., Ltd. | Thiadiazolone derivatives, compositions and uses thereof |
| CN121729418A (zh) * | 2023-05-05 | 2026-03-24 | 北京丹擎医药科技有限公司 | 环状衍生物及其组合物和应用 |
| CN121712768A (zh) * | 2023-05-30 | 2026-03-20 | 宁波新湾科技发展有限公司 | 噻唑基或噻二唑基酰胺衍生物及其用途 |
| CN121399118A (zh) * | 2023-06-02 | 2026-01-23 | 成都微芯药业有限公司 | Polθ抑制剂及其制备方法和用途 |
| WO2025011617A1 (zh) * | 2023-07-12 | 2025-01-16 | 杭州圣域生物医药科技有限公司 | 并环杂芳环类化合物、其中间体、制备方法和应用 |
| WO2025011603A1 (zh) * | 2023-07-12 | 2025-01-16 | 南京再明医药有限公司 | 一种化合物用于预防或治疗53BP1/Shieldin复合物缺陷的癌症的用途 |
| AU2024295853A1 (en) * | 2023-07-12 | 2026-02-12 | Simcere Zaiming Pharmaceutical Co., Ltd. | Salt of thiazolopyrazine compound or crystal thereof and use thereof |
| CN121772924A (zh) * | 2023-07-12 | 2026-03-31 | 先声再明医药股份有限公司 | Polq抑制剂化合物和抗癌治疗剂或者放射疗法的组合 |
| CN121773109A (zh) * | 2023-07-27 | 2026-03-31 | 北京丹擎医药科技有限公司 | PolQ降解剂及其组合物和应用 |
| WO2025036490A1 (zh) * | 2023-08-17 | 2025-02-20 | 海思科医药集团股份有限公司 | 一种DNA聚合酶θ抑制剂及其用途 |
| KR20260040065A (ko) * | 2023-09-01 | 2026-03-23 | 항저우 신알엑스 테라퓨틱스 바이오메디컬 테크놀로지 컴퍼니 리미티드 | 바이아릴 고리계 화합물, 이의 중간체, 제조 방법 및 용도 |
| CN117229260B (zh) * | 2023-11-13 | 2024-02-27 | 中国药科大学 | DNA聚合酶θ与聚ADP核糖聚合酶1双靶点抑制剂及其制备方法和医药用途 |
| WO2025110780A1 (en) * | 2023-11-24 | 2025-05-30 | Daewoong Pharmaceutical Co., Ltd. | Novel heterocyclic compounds and pharmaceutical composition comprising the same as dna polymerase theta inhibitors for the prevention or treatment of cancer |
| WO2025119195A1 (en) * | 2023-12-08 | 2025-06-12 | Danatlas Pharmaceuticals Co., Ltd. | Combination of polq inhibitor and anti-cancer therapeutic agent |
| WO2025165092A1 (en) * | 2024-01-30 | 2025-08-07 | Daewoong Pharmaceutical Co., Ltd. | Novel heterocyclic compounds and pharmaceutical composition comprising the same as dna polymerase theta inhibitors for the prevention or treatment of cancer |
| WO2025165094A1 (en) * | 2024-01-30 | 2025-08-07 | Daewoong Pharmaceutical Co., Ltd. | Novel heterocyclic compounds and pharmaceutical composition comprising the same as dna polymerase theta inhibitors for the prevention or treatment of cancer |
| CN120829441A (zh) * | 2024-04-24 | 2025-10-24 | 杭州圣域生物医药科技有限公司 | 一种并环含氮化合物及其中间体的制备方法 |
| CN120829442A (zh) * | 2024-04-24 | 2025-10-24 | 杭州圣域生物医药科技有限公司 | 一种并环含氮化合物及其中间体的制备方法 |
| WO2025223483A1 (zh) * | 2024-04-24 | 2025-10-30 | 杭州圣域生物医药科技有限公司 | 并环含氮化合物、其晶型及其制备方法和用途 |
| CN118515661B (zh) * | 2024-07-22 | 2024-11-15 | 中国药科大学 | 一种靶向降解Polθ的化合物及其制备方法和用途 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010513444A (ja) | 2006-12-21 | 2010-04-30 | アストラゼネカ アクチボラグ | 新規化合物 |
| JP2017537948A (ja) | 2014-12-17 | 2017-12-21 | ジャンキョテックス スイス エスアーＧｅｎｋｙｏｔｅｘ Ｓｕｉｓｓｅ Ｓａ | Ｎａｄｐｈオキシダーゼ阻害剤としてのアミドチアジアゾール誘導体 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0721095D0 (en) * | 2007-10-26 | 2007-12-05 | Piramed Ltd | Pharmaceutical compounds |
| EP3778600A1 (en) * | 2014-03-20 | 2021-02-17 | The Johns Hopkins University | Compounds which inhibit rna polymerase, compositions including such compounds, and their use |
| USRE50319E1 (en) | 2017-10-16 | 2025-03-04 | Dana-Farber Cancer Institute, Inc. | Compounds and methods for treating cancer |
-
2020
- 2020-05-29 AU AU2020282768A patent/AU2020282768B2/en active Active
- 2020-05-29 WO PCT/US2020/035165 patent/WO2020243459A1/en not_active Ceased
- 2020-05-29 CA CA3141134A patent/CA3141134A1/en active Pending
- 2020-05-29 CN CN202080050232.1A patent/CN114127062A/zh active Pending
- 2020-05-29 TW TW109118207A patent/TW202110834A/zh unknown
- 2020-05-29 BR BR112021024101A patent/BR112021024101A2/pt unknown
- 2020-05-29 US US17/615,123 patent/US12509454B2/en active Active
- 2020-05-29 JP JP2021570943A patent/JP7655863B2/ja active Active
- 2020-05-29 ES ES20760608T patent/ES2968796T3/es active Active
- 2020-05-29 EP EP20760608.8A patent/EP3976608B1/en active Active
-
2025
- 2025-10-28 US US19/370,959 patent/US20260049074A1/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010513444A (ja) | 2006-12-21 | 2010-04-30 | アストラゼネカ アクチボラグ | 新規化合物 |
| JP2017537948A (ja) | 2014-12-17 | 2017-12-21 | ジャンキョテックス スイス エスアーＧｅｎｋｙｏｔｅｘ Ｓｕｉｓｓｅ Ｓａ | Ｎａｄｐｈオキシダーゼ阻害剤としてのアミドチアジアゾール誘導体 |
Also Published As
| Publication number | Publication date |
|---|---|
| US20260049074A1 (en) | 2026-02-19 |
| WO2020243459A1 (en) | 2020-12-03 |
| CN114127062A (zh) | 2022-03-01 |
| CA3141134A1 (en) | 2020-12-03 |
| US20230078112A1 (en) | 2023-03-16 |
| AU2020282768A1 (en) | 2021-12-23 |
| EP3976608A1 (en) | 2022-04-06 |
| BR112021024101A2 (pt) | 2022-02-08 |
| AU2020282768B2 (en) | 2023-09-14 |
| JP2022535227A (ja) | 2022-08-05 |
| EP3976608B1 (en) | 2023-11-08 |
| ES2968796T3 (es) | 2024-05-14 |
| TW202110834A (zh) | 2021-03-16 |
| EP3976608C0 (en) | 2023-11-08 |
| US12509454B2 (en) | 2025-12-30 |
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