TW202315618A - 作為DNA聚合酶θ抑制劑之O-聯結噻二唑基化合物 - Google Patents

作為DNA聚合酶θ抑制劑之O-聯結噻二唑基化合物 Download PDF

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TW202315618A
TW202315618A TW111121145A TW111121145A TW202315618A TW 202315618 A TW202315618 A TW 202315618A TW 111121145 A TW111121145 A TW 111121145A TW 111121145 A TW111121145 A TW 111121145A TW 202315618 A TW202315618 A TW 202315618A
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Taiwan
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pharmaceutically acceptable
alkyl
acceptable salt
group
independently selected
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TW111121145A
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Chinese (zh)
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波爾 A 班撒提
費洛茲 阿里 賈玻里
丹尼爾 李 賽佛羅斯
王晨博
凱文 J 達菲
布萊恩 G 羅霍恩
尼可拉斯 大衛 亞當斯
亞諾斯 柏提安斯基
麥可 G 達西
泰瑞絲 J 凱索
約翰 J 麥卡緹
庫斯伯特 馬太爾
山塔尼拉 亞歷山大 布它果
辛朗 譚
Original Assignee
美商愛德亞生物科學公司
英商葛蘭素史密斯克藍智慧財產權有限公司
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Publication of TW202315618A publication Critical patent/TW202315618A/zh

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW111121145A 2021-06-11 2022-06-08 作為DNA聚合酶θ抑制劑之O-聯結噻二唑基化合物 TW202315618A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US202163209555P 2021-06-11 2021-06-11
US63/209,555 2021-06-11
US202263319826P 2022-03-15 2022-03-15
US63/319,826 2022-03-15

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TW202315618A true TW202315618A (zh) 2023-04-16

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TW111121145A TW202315618A (zh) 2021-06-11 2022-06-08 作為DNA聚合酶θ抑制劑之O-聯結噻二唑基化合物

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Country Link
US (1) US20240287080A1 (https=)
EP (1) EP4352055A1 (https=)
JP (1) JP2024522373A (https=)
KR (1) KR20240044412A (https=)
AU (1) AU2022289762B2 (https=)
BR (1) BR112023025245A2 (https=)
CA (1) CA3222078A1 (https=)
CL (1) CL2023003671A1 (https=)
CO (1) CO2023017082A2 (https=)
IL (1) IL308912A (https=)
MX (1) MX2023014665A (https=)
TW (1) TW202315618A (https=)
WO (1) WO2022259204A1 (https=)

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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

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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
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
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
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
TW202502745A (zh) * 2023-02-28 2025-01-16 美商賽堤爾醫療公司 4,5-稠和雙環吡咯啶及4,5-稠和雙環吡咯啶-酮化合物
US12215102B2 (en) * 2023-02-28 2025-02-04 Reglagene, Inc. Compositions and methods for making and using small molecules for tubulin-targeted therapy in the treatment of cancers and related conditions
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
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
EP4727540A2 (en) * 2023-06-16 2026-04-22 Quantx Biosciences US, Inc. Fused bicyclic heterocyclic or hetero aryl amide compounds
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
WO2025016391A1 (zh) * 2023-07-18 2025-01-23 南京再明医药有限公司 噻唑并吡嗪类化合物及其应用
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
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
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
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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AU2020282768B2 (en) * 2019-05-31 2023-09-14 Ideaya Biosciences, Inc. Thiadiazolyl derivatives as DNA Polymerase Theta inhibitors
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

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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

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CA3222078A1 (en) 2022-12-15
KR20240044412A (ko) 2024-04-04
AU2022289762A1 (en) 2023-12-14
US20240287080A1 (en) 2024-08-29
CL2023003671A1 (es) 2024-07-12
WO2022259204A1 (en) 2022-12-15
CO2023017082A2 (es) 2024-04-18
EP4352055A1 (en) 2024-04-17
IL308912A (en) 2024-01-01
JP2024522373A (ja) 2024-06-18
BR112023025245A2 (pt) 2024-02-20
AU2022289762B2 (en) 2025-12-04
MX2023014665A (es) 2024-04-29

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