AU2020345899B2 - MTA-cooperative PRMT5 inhibitors - Google Patents

MTA-cooperative PRMT5 inhibitors

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Publication number
AU2020345899B2
AU2020345899B2 AU2020345899A AU2020345899A AU2020345899B2 AU 2020345899 B2 AU2020345899 B2 AU 2020345899B2 AU 2020345899 A AU2020345899 A AU 2020345899A AU 2020345899 A AU2020345899 A AU 2020345899A AU 2020345899 B2 AU2020345899 B2 AU 2020345899B2
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AU
Australia
Prior art keywords
mmol
bromo
heteroaryl
alkyl
aryl
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Active
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AU2020345899A
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English (en)
Other versions
AU2020345899A1 (en
Inventor
Thomas P. Bobinski
Aaron Craig BURNS
Anthony IVETAC
John Michael Ketcham
Jon KUEHLER
Svitlana KULYK
John David Lawson
Matthew Arnold Marx
Christopher Ronald Smith
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.)
Mirati Therapeutics Inc
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Mirati Therapeutics Inc
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Publication of AU2020345899A1 publication Critical patent/AU2020345899A1/en
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    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/30—Phthalazines
    • C07D237/32—Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D417/10—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 carbon chain containing aromatic rings
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    • 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
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    • C07D471/12—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 three hetero rings
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    • C12N9/10—Transferases (2.)
    • C12N9/1003—Transferases (2.) transferring one-carbon groups (2.1)
    • C12N9/1007—Methyltransferases (general) (2.1.1.)

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
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  • Engineering & Computer Science (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Biomedical Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
AU2020345899A 2019-09-12 2020-09-11 MTA-cooperative PRMT5 inhibitors Active AU2020345899B2 (en)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US201962899575P 2019-09-12 2019-09-12
US62/899,575 2019-09-12
US201962942833P 2019-12-03 2019-12-03
US62/942,833 2019-12-03
US202062961371P 2020-01-15 2020-01-15
US62/961,371 2020-01-15
US202062994927P 2020-03-26 2020-03-26
US62/994,927 2020-03-26
US202063060261P 2020-08-03 2020-08-03
US63/060,261 2020-08-03
PCT/US2020/050457 WO2021050915A1 (en) 2019-09-12 2020-09-11 Mta-cooperative prmt5 inhibitors

Publications (2)

Publication Number Publication Date
AU2020345899A1 AU2020345899A1 (en) 2022-03-03
AU2020345899B2 true AU2020345899B2 (en) 2026-03-12

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AU2020345899A Active AU2020345899B2 (en) 2019-09-12 2020-09-11 MTA-cooperative PRMT5 inhibitors

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US (3) US11492351B2 (https=)
EP (1) EP4028388A1 (https=)
JP (1) JP7789662B2 (https=)
KR (1) KR20220083691A (https=)
CN (2) CN114728912A (https=)
AU (1) AU2020345899B2 (https=)
BR (1) BR112022004248A2 (https=)
CA (1) CA3150515A1 (https=)
CL (1) CL2022000603A1 (https=)
CO (1) CO2022004513A2 (https=)
IL (2) IL290341B2 (https=)
MX (1) MX2022002938A (https=)
NO (1) NO20220309A1 (https=)
PH (1) PH12022550399A1 (https=)
SA (1) SA522431915B1 (https=)
TW (1) TW202122387A (https=)
WO (1) WO2021050915A1 (https=)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202122387A (zh) * 2019-09-12 2021-06-16 美商米瑞替療法公司 Mta協同性之prmt5抑制劑
US20240208912A1 (en) * 2021-03-11 2024-06-27 Mirati Therapeutics, Inc. MTA-Cooperative PRMT5 Inhibitors
IL307393A (en) * 2021-04-08 2023-12-01 Mirati Therapeutics Inc Combination therapies used in PRMT5 inhibitors to treat cancer
IL307392A (en) * 2021-04-08 2023-12-01 Mirati Therapeutics Inc Combination therapies with PRMT5 inhibitors for cancer treatment
EP4347569A4 (en) * 2021-06-02 2025-03-26 Ideaya Biosciences, Inc. Combination therapy comprising a mat2a inhibitor and a type ii prmt inhibitor
EP4412607A1 (en) 2021-10-06 2024-08-14 Mirati Therapeutics, Inc. Combination therapies using prmt5 inhibitors for the treatment of cancer
IL311707A (en) 2021-10-06 2024-05-01 Mirati Therapeutics Inc Methods for the separation of enantiomers
US20260109709A1 (en) 2021-11-05 2026-04-23 Mirati Therapeutics, Inc. 2-amino imidazole derivatives as prmt5 inhibitors
WO2023098439A1 (zh) * 2021-11-30 2023-06-08 上海和誉生物医药科技有限公司 一种吡唑衍生物，其制备方法和在药学上的应用
EP4458812A1 (en) * 2021-12-27 2024-11-06 Medshine Discovery Inc. Pyrazole-1(2h)-phthalazinone compound and application thereof
CN114315735B (zh) * 2021-12-29 2023-08-01 广州中医药大学(广州中医药研究院) 一种鲁米诺酯化衍生物及其制备方法与应用
CN116903611A (zh) * 2022-01-26 2023-10-20 上海优理惠生医药有限公司 一种酞嗪酮类化合物、其制备方法、包含其药物组合物及其应用
EP4493555A4 (en) * 2022-03-15 2026-03-25 Beone Medicines I Gmbh 4-(AMINOMETHYL)-6-(1-METHYL-1H-PYRAZOL-4-YL)ISOQUINOLIN-1(2H)-ONE DERIVATIVES USED AS PRMT5 INHIBITORS COOPERATE WITH MTA
WO2023202626A1 (zh) * 2022-04-22 2023-10-26 北京望实智慧科技有限公司 稠和哒嗪酮化合物作为prmt5抑制剂
CN117843634A (zh) * 2022-05-24 2024-04-09 上海美悦生物科技发展有限公司 Sik抑制剂及其组合物、制备方法和用途
CN116178347B (zh) * 2022-06-29 2025-07-04 苏州浦合医药科技有限公司 Prmt5-mta抑制剂
EP4574816A4 (en) 2022-07-07 2026-01-14 Xizang Haisco Pharmaceutical Co Ltd HETEROCYCLIC COMPOUND CAPABLE OF INHIBITING PRMT5 - MTA AND ITS USE
CN117430596A (zh) * 2022-07-13 2024-01-23 上海海和药物研究开发股份有限公司 二并环类mat2a抑制剂及其用途
CN119301101A (zh) * 2022-07-29 2025-01-10 四川科伦博泰生物医药股份有限公司 甲基吡唑化合物、包含其的药物组合物及其制备方法和用途
CN119585261A (zh) * 2022-08-02 2025-03-07 上海艾力斯医药科技股份有限公司 一种prmt5抑制剂、其制备方法及应用
CN119730853A (zh) 2022-08-15 2025-03-28 阿斯利康(瑞典)有限公司 用于治疗癌症的mta协同prmt5抑制剂
CN119836290A (zh) 2022-09-01 2025-04-15 米拉蒂治疗公司 使用prmt5抑制剂和bcl-2家族抑制剂治疗癌症的组合疗法
WO2024091551A1 (en) * 2022-10-25 2024-05-02 Tango Therapeutics, Inc. Crystalline forms, pharmaceutical compositions and methods of use thereof
EP4628483A1 (en) * 2022-11-29 2025-10-08 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Dihydrophthalazine-containing compound
WO2024173215A1 (en) 2023-02-13 2024-08-22 Mirati Therapeutics, Inc. Crystalline forms of 2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin-6-yl)-1-methyl-1h- pyrazol-5-yl)-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile
US20240270719A1 (en) 2023-02-13 2024-08-15 Mirati Therapeutics, Inc. Crystalline forms of 2-(4-(4-(aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl)-1-methyl-1h-pyrazol-5-yl)-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile
WO2024170488A1 (en) 2023-02-13 2024-08-22 Astrazeneca Ab Prmt5 inhibitor for use in cancer therapy
EP4665722A1 (en) 2023-02-13 2025-12-24 Mirati Therapeutics, Inc. Crystalline forms of 2-(4-(4-(aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl)-1-methyl-1h-pyrazol-5-yl)-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile
KR102818470B1 (ko) * 2023-02-23 2025-06-10 한양대학교 산학협력단 신규한 아미노락톤 유도체 및 이의 신규한 제조방법
WO2024220917A1 (en) 2023-04-21 2024-10-24 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
CN121752566A (zh) * 2023-06-16 2026-03-27 中山优理生物医药有限公司 一种氨基吡啶类化合物、其制备方法、包含其药物组合物及其应用
WO2025016323A1 (zh) 2023-07-14 2025-01-23 江苏亚虹医药科技股份有限公司 蛋白质精氨酸酶甲基转移酶-5抑制剂及其医药用途
AU2024320474A1 (en) 2023-08-08 2026-03-26 Mirati Therapeutics, Inc. Methods and compositions for treating malignant peripheral nerve sheath tumors
AU2024319888A1 (en) * 2023-08-09 2026-02-26 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Heteroaryl compound, preparation method therefor, and use thereof in medicine
WO2025059579A1 (en) 2023-09-15 2025-03-20 Ideaya Biosciences, Inc. Methods of treating mat2a related diseases
WO2025064286A1 (en) * 2023-09-19 2025-03-27 Mirati Therapeutics, Inc. Stable 4-(aminomethyl)-6-(phenylpyrazolyl)phthalazinone compositions and processes for preparation thereof
AU2024344078A1 (en) 2023-09-20 2026-04-02 Ideaya Biosciences, Inc. Combination therapy with a parg inhibitor
WO2025061102A1 (zh) * 2023-09-20 2025-03-27 西藏海思科制药有限公司 一种含氰基的杂环化合物及其用途
WO2025072544A1 (en) 2023-09-27 2025-04-03 Ideaya Biosciences, Inc. Sulfonamino indazole compounds as inhibitors of parg
WO2025068985A1 (en) * 2023-09-28 2025-04-03 Beigene Switzerland Gmbh 1-(1-oxo-1,2-dihydrophthalazin-6-yl)cycloalkyl-1-carboxamide derivatives as mta-cooperative inhibitors of prmt5
TW202532064A (zh) * 2023-11-28 2025-08-16 大陸商正大天晴藥業集團股份有限公司 含有雜環二氫酞嗪的化合物
WO2025180390A1 (zh) * 2024-02-27 2025-09-04 烨辉医药科技(上海)有限公司 具有四环并环结构的mta协同性prmt5抑制剂化合物
WO2025212574A1 (en) 2024-04-02 2025-10-09 Mirati Therapeutics, Inc. Processes for preparation of prmt5 inhibitors and intermediates for making the same
WO2025217008A1 (en) 2024-04-08 2025-10-16 Mirati Therapeutics, Inc. Combination therapies using prmt5 inhibitors and sos1 inhibitors for the treatment of cancer
US20250312343A1 (en) 2024-04-08 2025-10-09 Mirati Therapeutics, Inc. Combination therapies using prmt5 inhibitors and kras g12d inhibitors for the treatment of cancer
WO2025217007A1 (en) 2024-04-08 2025-10-16 Mirati Therapeutics, Inc. Combination therapies using prmt5 inhibitors and immune checkpoint inhibitors for the treatment of cancer

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002006285A1 (en) * 2000-07-17 2002-01-24 Merck Sharp & Dohme Limited Imidazolophthalazine derivatives as ligands for gabaa receptors

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6919351B2 (en) * 2000-10-12 2005-07-19 Merck & Co., Inc. Aza-and polyaza-naphthalenyl-carboxamides useful as HIV integrase inhibitors
US20030073692A1 (en) 2001-08-07 2003-04-17 Pharmacia & Upjohn S.P.A. Amino-phthalazinone derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions containing them
GB201604027D0 (en) 2016-03-09 2016-04-20 Ctxt Pty Ltd Compounds
TW202122387A (zh) * 2019-09-12 2021-06-16 美商米瑞替療法公司 Mta協同性之prmt5抑制劑

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002006285A1 (en) * 2000-07-17 2002-01-24 Merck Sharp & Dohme Limited Imidazolophthalazine derivatives as ligands for gabaa receptors

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