CN114585622B - 作为nsd2抑制剂和抗癌剂的哌啶基-甲基-嘌呤胺 - Google Patents

作为nsd2抑制剂和抗癌剂的哌啶基-甲基-嘌呤胺 Download PDF

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Publication number
CN114585622B
CN114585622B CN202080069611.5A CN202080069611A CN114585622B CN 114585622 B CN114585622 B CN 114585622B CN 202080069611 A CN202080069611 A CN 202080069611A CN 114585622 B CN114585622 B CN 114585622B
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compound
pharmaceutically acceptable
alkyl
mixture
acceptable salt
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Chinese (zh)
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CN114585622A (zh
Inventor
邓海兵
刘金镖
欧阳孔德
王策
肖启桃
寻国良
曾海强
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Novartis AG
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Novartis AG
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    • 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
    • A61K31/52Purines, e.g. adenine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN202080069611.5A 2019-08-14 2020-08-12 作为nsd2抑制剂和抗癌剂的哌啶基-甲基-嘌呤胺 Active CN114585622B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/CN2019/100542 WO2021026803A1 (en) 2019-08-14 2019-08-14 Piperidinyl-methyl-purineamines as nsd2 inhibitors and anti-cancer agents
CNPCT/CN2019/100542 2019-08-14
PCT/IB2020/057602 WO2021028854A1 (en) 2019-08-14 2020-08-12 Piperidinyl-methyl-purineamines as nsd2 inhibitors and anti-cancer agents

Publications (2)

Publication Number Publication Date
CN114585622A CN114585622A (zh) 2022-06-03
CN114585622B true CN114585622B (zh) 2024-08-09

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CN202080069611.5A Active CN114585622B (zh) 2019-08-14 2020-08-12 作为nsd2抑制剂和抗癌剂的哌啶基-甲基-嘌呤胺

Country Status (20)

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US (3) US11420970B1 (enExample)
EP (2) EP4559915A1 (enExample)
JP (2) JP7638960B2 (enExample)
KR (1) KR102946008B1 (enExample)
CN (1) CN114585622B (enExample)
AU (1) AU2020328919A1 (enExample)
BR (1) BR112022002520A2 (enExample)
CO (1) CO2022002804A2 (enExample)
DK (1) DK4013755T3 (enExample)
EC (1) ECSP22019360A (enExample)
ES (1) ES3023540T3 (enExample)
FI (1) FI4013755T3 (enExample)
IL (2) IL289754B2 (enExample)
MX (1) MX2022001784A (enExample)
MY (1) MY209614A (enExample)
PH (1) PH12022550343A1 (enExample)
PL (1) PL4013755T3 (enExample)
PT (1) PT4013755T (enExample)
WO (2) WO2021026803A1 (enExample)
ZA (1) ZA202200519B (enExample)

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WO2021026803A1 (en) * 2019-08-14 2021-02-18 Novartis Ag Piperidinyl-methyl-purineamines as nsd2 inhibitors and anti-cancer agents
ES2987269T3 (es) * 2019-09-20 2024-11-14 Novartis Ag Inhibidores de MLL1 y agentes anticancerígenos
KR20240158230A (ko) * 2022-01-05 2024-11-04 케이36 테라퓨틱스, 인크. 중수소-풍부 피페리디닐-메틸-퓨린 아민 및 관련 화합물 및 질환 및 병태 치료에 있어서 이것들의 용도
IL314895A (en) * 2022-02-16 2024-10-01 Duke Street Bio Ltd Pharmaceutical compound
IL316882A (en) * 2022-05-18 2025-01-01 K36 Therapeutics Inc Piperidinyl-methyl-purine amine D-tartaric acid salts, crystalline forms, and their use in the treatment of diseases and medical conditions
WO2023225150A1 (en) * 2022-05-18 2023-11-23 K36 Therapeutics, Inc. Piperidinyl-methyl-purine amine fumaric acid salts, crystalline forms, and their use in treating medical diseases and conditions
WO2023225144A1 (en) * 2022-05-18 2023-11-23 K36 Therapeutics, Inc. Piperidinyl-methyl-purine amine salts, crystalline forms, and their use in treating medical diseases and conditions
US20250326752A1 (en) * 2022-05-18 2025-10-23 K36 Therapeutics, Inc. Piperidinyl-methyl-purine amine salts, crystalline forms, and their use in treating medical diseases and conditions
WO2023230026A1 (en) * 2022-05-23 2023-11-30 K36 Therapeutics, Inc. Piperidinyl-methylpurine benzenes and related compounds and their use in treating diseases and conditions
WO2023230038A1 (en) * 2022-05-23 2023-11-30 K36 Therapeutics, Inc. Piperidinyl-methylpurine pyrimidines and related compounds and their use in treating diseases and conditions
WO2024073282A2 (en) * 2022-09-26 2024-04-04 Board Of Regents, The University Of Texas System Heterocycles as modulators of nsd activity
WO2024073283A1 (en) * 2022-09-26 2024-04-04 Board Of Regents, The University Of Texas System Heterocycles as modulators of nsd activity
WO2024129670A1 (en) * 2022-12-12 2024-06-20 K36 Therapeutics, Inc. Pharmaceutical compositions containing a piperidinyl-methyl-purine amine and their use in treating diseases and conditions
US20250171445A1 (en) * 2023-11-17 2025-05-29 K36 Therapeutics, Inc. Deuterium-enriched piperidinyl-methyl-purine amine salts, crystalline forms, and their use in treating medical diseases and conditions
CN117720550A (zh) * 2023-12-14 2024-03-19 深圳市华先医药科技有限公司 (s)-3-甲基-4-氧代-2-氧杂-8-氮杂螺[4.5]癸烷-8-甲酸叔丁酯合成方法
CN117843641B (zh) * 2023-12-28 2025-04-25 和径医药科技(上海)有限公司 Nsd3抑制剂及其制备方法和应用
WO2025147514A1 (en) * 2024-01-02 2025-07-10 K36 Therapeutics, Inc. Piperidinyl-methyl-purineamine nsd2 inhibitor therapeutic methods and compositions for treating cancer
CN118459395A (zh) * 2024-05-10 2024-08-09 南通大学 一种5-(叔丁氧羰基氨基)哌啶-3-羧酸甲酯的合成方法

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CN108853110A (zh) * 2018-08-24 2018-11-23 江苏理工学院 一种化合物a8作为组蛋白甲基转移酶nsd3活性抑制剂及其应用
CN109223794A (zh) * 2018-08-24 2019-01-18 江苏理工学院 一种化合物c6作为组蛋白甲基转移酶nsd3活性抑制剂及其应用

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US7332486B2 (en) * 2002-08-08 2008-02-19 Memory Pharmaceuticals Corp. Phosphodiesterase 4 inhibitors
KR101111085B1 (ko) * 2002-09-27 2012-04-12 다이닛본 스미토모 세이야꾸 가부시끼가이샤 신규 아데닌 화합물 및 그 용도
JP2004137157A (ja) * 2002-10-16 2004-05-13 Sumitomo Pharmaceut Co Ltd 新規アデニン誘導体を有効成分として含有する医薬
JP2007269629A (ja) 2004-06-21 2007-10-18 Astellas Pharma Inc キナゾリン誘導体
AR065784A1 (es) 2007-03-20 2009-07-01 Dainippon Sumitomo Pharma Co Derivados de 8-oxo adenina,medicamentos que los contienen y usos como agentes terapeuticos para enfermedades alergicas, antivirales o antibacterianas.
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WO2021026803A1 (en) * 2019-08-14 2021-02-18 Novartis Ag Piperidinyl-methyl-purineamines as nsd2 inhibitors and anti-cancer agents
KR20240158230A (ko) 2022-01-05 2024-11-04 케이36 테라퓨틱스, 인크. 중수소-풍부 피페리디닐-메틸-퓨린 아민 및 관련 화합물 및 질환 및 병태 치료에 있어서 이것들의 용도
WO2023225150A1 (en) 2022-05-18 2023-11-23 K36 Therapeutics, Inc. Piperidinyl-methyl-purine amine fumaric acid salts, crystalline forms, and their use in treating medical diseases and conditions
IL316882A (en) 2022-05-18 2025-01-01 K36 Therapeutics Inc Piperidinyl-methyl-purine amine D-tartaric acid salts, crystalline forms, and their use in the treatment of diseases and medical conditions
WO2023225144A1 (en) 2022-05-18 2023-11-23 K36 Therapeutics, Inc. Piperidinyl-methyl-purine amine salts, crystalline forms, and their use in treating medical diseases and conditions
US20250326752A1 (en) 2022-05-18 2025-10-23 K36 Therapeutics, Inc. Piperidinyl-methyl-purine amine salts, crystalline forms, and their use in treating medical diseases and conditions

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CN108853110A (zh) * 2018-08-24 2018-11-23 江苏理工学院 一种化合物a8作为组蛋白甲基转移酶nsd3活性抑制剂及其应用
CN109223794A (zh) * 2018-08-24 2019-01-18 江苏理工学院 一种化合物c6作为组蛋白甲基转移酶nsd3活性抑制剂及其应用

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JP2025081505A (ja) 2025-05-27
CN114585622A (zh) 2022-06-03
IL289754B2 (en) 2025-09-01
CA3144542A1 (en) 2021-02-18
MX2022001784A (es) 2022-04-18
EP4013755B1 (en) 2025-01-08
EP4559915A1 (en) 2025-05-28
KR102946008B1 (ko) 2026-04-01
WO2021028854A1 (en) 2021-02-18
JP7638960B2 (ja) 2025-03-04
MY209614A (en) 2025-07-24
ZA202200519B (en) 2024-08-28
PL4013755T3 (pl) 2025-05-12
US11420970B1 (en) 2022-08-23
DK4013755T3 (da) 2025-03-31
PT4013755T (pt) 2025-05-02
ES3023540T3 (en) 2025-06-02
US20230002388A1 (en) 2023-01-05
IL289754B1 (en) 2025-05-01
IL320143A (en) 2025-06-01
IL289754A (en) 2022-03-01
CO2022002804A2 (es) 2022-04-08
EP4013755A1 (en) 2022-06-22
BR112022002520A2 (pt) 2022-05-10
PH12022550343A1 (en) 2023-03-13
ECSP22019360A (es) 2022-04-29
US12312353B2 (en) 2025-05-27
US20250276971A1 (en) 2025-09-04
JP2022544946A (ja) 2022-10-24
FI4013755T3 (fi) 2025-04-02
WO2021026803A1 (en) 2021-02-18
KR20220047330A (ko) 2022-04-15
AU2020328919A1 (en) 2022-02-17

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