AU2022289762B2 - O-linked thiadiazolyl compounds as dna polymerase theta inhibitors - Google Patents

O-linked thiadiazolyl compounds as dna polymerase theta inhibitors

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Publication number
AU2022289762B2
AU2022289762B2 AU2022289762A AU2022289762A AU2022289762B2 AU 2022289762 B2 AU2022289762 B2 AU 2022289762B2 AU 2022289762 A AU2022289762 A AU 2022289762A AU 2022289762 A AU2022289762 A AU 2022289762A AU 2022289762 B2 AU2022289762 B2 AU 2022289762B2
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Australia
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independently selected
alkyl
cpd structure
nov
pharmaceutically acceptable
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AU2022289762A
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English (en)
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AU2022289762A1 (en
Inventor
Nicholas David ADAMS
Paul A. Barsanti
Janos Botyanszki
Alexander BUITRAGO SANTANILLA
Michael G. Darcy
Kevin J. Duffy
Firoz Ali JAIPURI
Terence J. Kiesow
Brian G. LAWHORN
Cuthbert Martyr
John J. MCATEE
Daniel Lee Severance
Xinrong Tian
Chenbo WANG
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
GlaxoSmithKline Intellectual Property No 4 Ltd
Ideaya Biosciences Inc
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GlaxoSmithKline Intellectual Property No 4 Ltd
Ideaya Biosciences Inc
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Publication of AU2022289762A1 publication Critical patent/AU2022289762A1/en
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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
    • A61K31/437—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • 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
    • C07D498/04—Ortho-condensed systems

Landscapes

  • 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)
AU2022289762A 2021-06-11 2022-06-09 O-linked thiadiazolyl compounds as dna polymerase theta inhibitors Active AU2022289762B2 (en)

Applications Claiming Priority (5)

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
PCT/IB2022/055384 WO2022259204A1 (en) 2021-06-11 2022-06-09 O-linked thiadiazolyl compounds as dna polymerase theta inhibitors

Publications (2)

Publication Number Publication Date
AU2022289762A1 AU2022289762A1 (en) 2023-12-14
AU2022289762B2 true AU2022289762B2 (en) 2025-12-04

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ID=82358548

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2022289762A Active AU2022289762B2 (en) 2021-06-11 2022-06-09 O-linked thiadiazolyl compounds as dna polymerase theta inhibitors

Country Status (13)

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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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
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
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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EP3034500A1 (en) * 2014-12-17 2016-06-22 Genkyotex Sa Amido thiazole derivatives as NADPH oxidase inhibitors
WO2020243459A1 (en) * 2019-05-31 2020-12-03 Ideaya Biosciences, Inc. Thiadiazolyl derivatives as dna polymerase theta inhibitors
WO2022118210A1 (en) * 2020-12-02 2022-06-09 Ideaya Biosciences, Inc. Substituted thiadiazolyl derivatives as dna polymerase theta inhibitors

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Also Published As

Publication number Publication date
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
TW202315618A (zh) 2023-04-16
EP4352055A1 (en) 2024-04-17
IL308912A (en) 2024-01-01
JP2024522373A (ja) 2024-06-18
BR112023025245A2 (pt) 2024-02-20
MX2023014665A (es) 2024-04-29

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