AU2020328919B2 - Piperidinyl-methyl-purineamines as NSD2 inhibitors and anti-cancer agents - Google Patents

Piperidinyl-methyl-purineamines as NSD2 inhibitors and anti-cancer agents

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Publication number
AU2020328919B2
AU2020328919B2 AU2020328919A AU2020328919A AU2020328919B2 AU 2020328919 B2 AU2020328919 B2 AU 2020328919B2 AU 2020328919 A AU2020328919 A AU 2020328919A AU 2020328919 A AU2020328919 A AU 2020328919A AU 2020328919 B2 AU2020328919 B2 AU 2020328919B2
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AU
Australia
Prior art keywords
amino
methyl
pyridin
piperidin
purin
Prior art date
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Active
Application number
AU2020328919A
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English (en)
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AU2020328919A1 (en
Inventor
Haibing DENG
Jinbiao Liu
Counde Oyang
Ce Wang
Qitao XIAO
Guoliang Xun
Haiqiang ZENG
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.)
Novartis AG
Original Assignee
Novartis AG
Priority date (The priority date 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 date listed.)
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Publication date
Application filed by Novartis AG filed Critical Novartis AG
Publication of AU2020328919A1 publication Critical patent/AU2020328919A1/en
Application granted granted Critical
Publication of AU2020328919B2 publication Critical patent/AU2020328919B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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
    • A61K31/52—Purines, e.g. adenine
    • 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
    • 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
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (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)
AU2020328919A 2019-08-14 2020-08-12 Piperidinyl-methyl-purineamines as NSD2 inhibitors and anti-cancer agents Active AU2020328919B2 (en)

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
AUPCT/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
AU2020328919A1 AU2020328919A1 (en) 2022-02-17
AU2020328919B2 true AU2020328919B2 (en) 2026-05-28

Family

ID=72145436

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2020328919A Active AU2020328919B2 (en) 2019-08-14 2020-08-12 Piperidinyl-methyl-purineamines as NSD2 inhibitors and anti-cancer agents

Country Status (20)

Country Link
US (3) US11420970B1 (enExample)
EP (2) EP4013755B1 (enExample)
JP (2) JP7638960B2 (enExample)
KR (1) KR102946008B1 (enExample)
CN (1) CN114585622B (enExample)
AU (1) AU2020328919B2 (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) IL320143A (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)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021026803A1 (en) * 2019-08-14 2021-02-18 Novartis Ag Piperidinyl-methyl-purineamines as nsd2 inhibitors and anti-cancer agents
CN114981270B (zh) * 2019-09-20 2024-10-18 诺华公司 Mll1抑制剂和抗癌剂
JP2025504379A (ja) * 2022-01-05 2025-02-12 ケイ３６・セラピューティクス・インコーポレイテッド 重水素濃縮ピペリジニル－メチル－プリンアミン及び関連化合物、ならびに疾患及び状態の治療におけるそれらの使用
JP2025508714A (ja) * 2022-02-16 2025-04-10 デューク ストリート バイオ リミテッド 医薬化合物
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
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
JP2025517349A (ja) * 2022-05-18 2025-06-05 ケイ３６・セラピューティクス・インコーポレイテッド ピペリジニル－メチル－プリンアミンｄ－酒石酸塩、結晶形態、ならびに医学的疾患及び状態の治療におけるそれらの使用
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
US20250361235A1 (en) * 2022-05-23 2025-11-27 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
CN119894513A (zh) * 2022-09-26 2025-04-25 德州大学系统董事会 作为nsd活性调节剂的杂环
WO2024073283A1 (en) * 2022-09-26 2024-04-04 Board Of Regents, The University Of Texas System Heterocycles as modulators of nsd activity
CN120641105A (zh) * 2022-12-12 2025-09-12 K36治疗股份有限公司 含有哌啶基甲基嘌呤胺的药物组合物及其在治疗疾病和疾患中的用途
US20250011329A1 (en) * 2023-06-21 2025-01-09 K36 Therapeutics, Inc. Substituted piperidinyl-methylpurine pyridines and related compounds and their use in treating diseases and conditions
AU2024381513A1 (en) * 2023-11-17 2026-06-04 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
IL330390A (en) * 2024-01-02 2026-08-01 K36 Therapeutics Inc Methods and medicinal compounds inhibiting NSD2 for the treatment of cancers from the piperidinyl-methyl-purinamine family
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

Citations (2)

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

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4331944B2 (ja) * 2001-04-17 2009-09-16 大日本住友製薬株式会社 新規アデニン誘導体
US7332486B2 (en) * 2002-08-08 2008-02-19 Memory Pharmaceuticals Corp. Phosphodiesterase 4 inhibitors
CA2497765A1 (en) * 2002-09-27 2004-04-08 Sumitomo Pharmaceuticals Co., Ltd. 8-hydroxy substituted adenine compounds and uses thereof
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
TW200902018A (en) * 2007-03-20 2009-01-16 Dainippon Sumitomo Pharma Co Novel adenine compound
BR112012009329A2 (pt) * 2009-10-22 2016-06-07 Gilead Sciences Inc derivados de purina ou deazapurina úteis para o tratamento de infecções virais (inter alia)
GB201204985D0 (en) 2012-03-21 2012-05-02 Genentech Inc Compounds
WO2019196918A1 (zh) 2018-04-13 2019-10-17 罗欣药业(上海)有限公司 五元杂环并嘧啶类化合物、药物组合物及用途
WO2021026803A1 (en) * 2019-08-14 2021-02-18 Novartis Ag Piperidinyl-methyl-purineamines as nsd2 inhibitors and anti-cancer agents
JP2025504379A (ja) 2022-01-05 2025-02-12 ケイ３６・セラピューティクス・インコーポレイテッド 重水素濃縮ピペリジニル－メチル－プリンアミン及び関連化合物、ならびに疾患及び状態の治療におけるそれらの使用
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
JP2025517349A (ja) 2022-05-18 2025-06-05 ケイ３６・セラピューティクス・インコーポレイテッド ピペリジニル－メチル－プリンアミンｄ－酒石酸塩、結晶形態、ならびに医学的疾患及び状態の治療におけるそれらの使用
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
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

Patent Citations (2)

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

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DOMINIC TISI, ELISABETTA CHIARPARIN, EMILIANO TAMANINI, PUJA PATHURI, JOSEPH E. COYLE, ADAM HOLD, FINN P. HOLDING, NADER AMIN, AGN: "Structure of the Epigenetic Oncogene MMSET and Inhibition by N -Alkyl Sinefungin Derivatives", ACS CHEMICAL BIOLOGY, AMERICAN CHEMICAL SOCIETY, vol. 11, no. 11, 18 November 2016 (2016-11-18), pages 3093 - 3105, XP055650361, ISSN: 1554-8929, DOI: 10.1021/acschembio.6b00308 *

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ECSP22019360A (es) 2022-04-29
EP4013755B1 (en) 2025-01-08
IL289754B1 (en) 2025-05-01
JP7638960B2 (ja) 2025-03-04
KR102946008B1 (ko) 2026-04-01
US11420970B1 (en) 2022-08-23
EP4013755A1 (en) 2022-06-22
PH12022550343A1 (en) 2023-03-13
BR112022002520A2 (pt) 2022-05-10
WO2021028854A1 (en) 2021-02-18
CN114585622B (zh) 2024-08-09
US20250276971A1 (en) 2025-09-04
MY209614A (en) 2025-07-24
ES3023540T3 (en) 2025-06-02
IL320143A (en) 2025-06-01
WO2021026803A1 (en) 2021-02-18
FI4013755T3 (fi) 2025-04-02
JP2025081505A (ja) 2025-05-27
IL289754A (en) 2022-03-01
IL289754B2 (en) 2025-09-01
CO2022002804A2 (es) 2022-04-08
MX2022001784A (es) 2022-04-18
CN114585622A (zh) 2022-06-03
US20230002388A1 (en) 2023-01-05
KR20220047330A (ko) 2022-04-15
ZA202200519B (en) 2024-08-28
US12312353B2 (en) 2025-05-27
AU2020328919A1 (en) 2022-02-17
PT4013755T (pt) 2025-05-02
EP4559915A1 (en) 2025-05-28
DK4013755T3 (da) 2025-03-31
JP2022544946A (ja) 2022-10-24
PL4013755T3 (pl) 2025-05-12
CA3144542A1 (en) 2021-02-18