FI4013755T3 - Piperidinyylimetyylipuriiniamiineja nsd2:n estäjinä ja syöpälääkkeinä - Google Patents
Piperidinyylimetyylipuriiniamiineja nsd2:n estäjinä ja syöpälääkkeinä Download PDFInfo
- Publication number
- FI4013755T3 FI4013755T3 FIEP20757967.3T FI20757967T FI4013755T3 FI 4013755 T3 FI4013755 T3 FI 4013755T3 FI 20757967 T FI20757967 T FI 20757967T FI 4013755 T3 FI4013755 T3 FI 4013755T3
- Authority
- FI
- Finland
- Prior art keywords
- alkyl
- alkoxy
- hydrogen
- alkylene
- pharmaceutically acceptable
- Prior art date
Links
- 102100029234 Histone-lysine N-methyltransferase NSD2 Human genes 0.000 title 1
- 101000634048 Homo sapiens Histone-lysine N-methyltransferase NSD2 Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- -1 (i) — hydrogen Chemical class 0.000 claims 25
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 22
- 150000001875 compounds Chemical class 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 22
- 239000001257 hydrogen Substances 0.000 claims 22
- 229910052736 halogen Inorganic materials 0.000 claims 19
- 150000003839 salts Chemical class 0.000 claims 19
- 150000002367 halogens Chemical class 0.000 claims 18
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 17
- 239000000203 mixture Substances 0.000 claims 17
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 15
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 14
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 5
- 229960000643 adenine Drugs 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 1
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 claims 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- 125000001359 1,2,3-triazol-4-yl group Chemical group [H]N1N=NC([*])=C1[H] 0.000 claims 1
- 125000004778 2,2-difluoroethyl group Chemical group [H]C([H])(*)C([H])(F)F 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 229930024421 Adenine Natural products 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000004212 difluorophenyl group Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000004284 isoxazol-3-yl group Chemical group [H]C1=C([H])C(*)=NO1 0.000 claims 1
- 125000004287 oxazol-2-yl group Chemical group [H]C1=C([H])N=C(*)O1 0.000 claims 1
- 125000000369 oxido group Chemical group [*]=O 0.000 claims 1
- HDOWRFHMPULYOA-UHFFFAOYSA-N piperidin-4-ol Chemical compound OC1CCNCC1 HDOWRFHMPULYOA-UHFFFAOYSA-N 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- 125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 1
- 229920001935 styrene-ethylene-butadiene-styrene Polymers 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 125000004495 thiazol-4-yl group Chemical group S1C=NC(=C1)* 0.000 claims 1
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)
Applications Claiming Priority (2)
| 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 |
| PCT/IB2020/057602 WO2021028854A1 (en) | 2019-08-14 | 2020-08-12 | Piperidinyl-methyl-purineamines as nsd2 inhibitors and anti-cancer agents |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| FI4013755T3 true FI4013755T3 (fi) | 2025-04-02 |
Family
ID=72145436
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FIEP20757967.3T FI4013755T3 (fi) | 2019-08-14 | 2020-08-12 | Piperidinyylimetyylipuriiniamiineja nsd2:n estäjinä ja syöpälääkkeinä |
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)
| 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 |
Family Cites Families (17)
| 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 |
| CN109223794B (zh) * | 2018-08-24 | 2020-07-28 | 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 |
| CN108853110B (zh) * | 2018-08-24 | 2020-07-28 | 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 |
| 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 |
-
2019
- 2019-08-14 WO PCT/CN2019/100542 patent/WO2021026803A1/en not_active Ceased
-
2020
- 2020-08-12 PL PL20757967.3T patent/PL4013755T3/pl unknown
- 2020-08-12 KR KR1020227008255A patent/KR102946008B1/ko active Active
- 2020-08-12 AU AU2020328919A patent/AU2020328919B2/en active Active
- 2020-08-12 JP JP2022509034A patent/JP7638960B2/ja active Active
- 2020-08-12 WO PCT/IB2020/057602 patent/WO2021028854A1/en not_active Ceased
- 2020-08-12 ES ES20757967T patent/ES3023540T3/es active Active
- 2020-08-12 EP EP20757967.3A patent/EP4013755B1/en active Active
- 2020-08-12 PT PT207579673T patent/PT4013755T/pt unknown
- 2020-08-12 PH PH1/2022/550343A patent/PH12022550343A1/en unknown
- 2020-08-12 CN CN202080069611.5A patent/CN114585622B/zh active Active
- 2020-08-12 IL IL320143A patent/IL320143A/en unknown
- 2020-08-12 IL IL289754A patent/IL289754B2/en unknown
- 2020-08-12 MY MYPI2022000244A patent/MY209614A/en unknown
- 2020-08-12 FI FIEP20757967.3T patent/FI4013755T3/fi active
- 2020-08-12 DK DK20757967.3T patent/DK4013755T3/da active
- 2020-08-12 MX MX2022001784A patent/MX2022001784A/es unknown
- 2020-08-12 BR BR112022002520A patent/BR112022002520A2/pt unknown
- 2020-08-12 EP EP25150251.4A patent/EP4559915A1/en active Pending
-
2021
- 2021-05-21 US US17/327,226 patent/US11420970B1/en active Active
-
2022
- 2022-01-11 ZA ZA2022/00519A patent/ZA202200519B/en unknown
- 2022-03-10 CO CONC2022/0002804A patent/CO2022002804A2/es unknown
- 2022-03-14 EC ECSENADI202219360A patent/ECSP22019360A/es unknown
- 2022-05-09 US US17/739,855 patent/US12312353B2/en active Active
-
2025
- 2025-02-19 JP JP2025024756A patent/JP2025081505A/ja active Pending
- 2025-05-20 US US19/213,478 patent/US20250276971A1/en active Pending
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