CN114127062A - 作为DNA聚合酶Theta抑制剂的噻二唑基衍生物 - Google Patents

作为DNA聚合酶Theta抑制剂的噻二唑基衍生物 Download PDF

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Publication number
CN114127062A
CN114127062A CN202080050232.1A CN202080050232A CN114127062A CN 114127062 A CN114127062 A CN 114127062A CN 202080050232 A CN202080050232 A CN 202080050232A CN 114127062 A CN114127062 A CN 114127062A
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compound
pharmaceutically acceptable
acceptable salt
alkyl
hydrogen
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Chinese (zh)
Inventor
P.A.巴桑蒂
H.P.贝克
M.弗卢里
J.E.诺克斯
E.D.麦克斯帕登
B.T.琼斯
L.P.马丁内斯
Z.裴
C.王
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Idia Bioscience Co ltd
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Idia Bioscience Co ltd
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    • 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
    • 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
    • C07D417/14—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

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  • 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)
CN202080050232.1A 2019-05-31 2020-05-29 作为DNA聚合酶Theta抑制剂的噻二唑基衍生物 Pending CN114127062A (zh)

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 (1)

Publication Number Publication Date
CN114127062A true CN114127062A (zh) 2022-03-01

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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=)

Cited By (13)

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Publication number Priority date Publication date Assignee Title
WO2023169547A1 (zh) * 2022-03-10 2023-09-14 四川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
CN117229260A (zh) * 2023-11-13 2023-12-15 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
WO2024099337A1 (en) * 2022-11-10 2024-05-16 Danatlas Pharmaceuticals Co., Ltd. Thiadiazolyl derivatives, compositions, and uses thereof
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
CN118515661A (zh) * 2024-07-22 2024-08-20 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
WO2024230578A1 (en) * 2023-05-05 2024-11-14 Danatlas Pharmaceuticals Co., Ltd. Cyclic derivatives, compositions and uses thereof
WO2024245415A1 (zh) * 2023-06-02 2024-12-05 成都微芯药业有限公司 Polθ抑制剂及其制备方法和用途
WO2025011618A1 (zh) * 2023-07-12 2025-01-16 南京再明医药有限公司 噻唑并吡嗪类化合物的盐或其结晶及其应用
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
WO2025021198A1 (en) * 2023-07-27 2025-01-30 Danatlas Pharmaceuticals Co., Ltd. PolQ DEGRADERS, COMPOSITIONS AND USES THEREOF
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
WO2025045248A1 (zh) * 2023-09-01 2025-03-06 杭州圣域生物医药科技有限公司 联芳环类化合物、其中间体、制备方法和应用

Families Citing this family (29)

* Cited by examiner, † Cited by third party
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
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
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
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
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
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
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
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

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Cited By (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023169547A1 (zh) * 2022-03-10 2023-09-14 四川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
WO2024099337A1 (en) * 2022-11-10 2024-05-16 Danatlas Pharmaceuticals Co., Ltd. Thiadiazolyl derivatives, compositions, and uses thereof
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
WO2024230578A1 (en) * 2023-05-05 2024-11-14 Danatlas Pharmaceuticals Co., Ltd. Cyclic derivatives, compositions and uses thereof
WO2024245415A1 (zh) * 2023-06-02 2024-12-05 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
WO2025011618A1 (zh) * 2023-07-12 2025-01-16 南京再明医药有限公司 噻唑并吡嗪类化合物的盐或其结晶及其应用
WO2025021198A1 (en) * 2023-07-27 2025-01-30 Danatlas Pharmaceuticals Co., Ltd. PolQ DEGRADERS, COMPOSITIONS AND USES THEREOF
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
WO2025045248A1 (zh) * 2023-09-01 2025-03-06 杭州圣域生物医药科技有限公司 联芳环类化合物、其中间体、制备方法和应用
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
CN117229260A (zh) * 2023-11-13 2023-12-15 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
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
CN118515661A (zh) * 2024-07-22 2024-08-20 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

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US20260049074A1 (en) 2026-02-19
WO2020243459A1 (en) 2020-12-03
CA3141134A1 (en) 2020-12-03
US20230078112A1 (en) 2023-03-16
JP7655863B2 (ja) 2025-04-02
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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