AU2020345899B2 - MTA-cooperative PRMT5 inhibitors - Google Patents

MTA-cooperative PRMT5 inhibitors

Info

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
Authority
AU
Australia
Prior art keywords
mmol
bromo
heteroaryl
alkyl
aryl
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
AU2020345899A
Other languages
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
Original Assignee
Mirati Therapeutics Inc
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.)
Filing date
Publication date
Application filed by Mirati Therapeutics Inc filed Critical Mirati Therapeutics Inc
Publication of AU2020345899A1 publication Critical patent/AU2020345899A1/en
Application granted granted Critical
Publication of AU2020345899B2 publication Critical patent/AU2020345899B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

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
    • A61K31/50—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
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—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
    • C07D403/10—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 carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • C07D405/02—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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • C07D405/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—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
    • C07D413/10—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 linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D417/04—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
    • 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
    • C07D417/10—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
    • 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
    • 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
    • C07D471/12—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
    • C07D471/14—Ortho-condensed systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—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
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/1003—Transferases (2.) transferring one-carbon groups (2.1)
    • C12N9/1007—Methyltransferases (general) (2.1.1.)

Landscapes

  • 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)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Genetics & Genomics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • 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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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

Family

ID=72659905

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2020345899A Active AU2020345899B2 (en) 2019-09-12 2020-09-11 MTA-cooperative PRMT5 inhibitors

Country Status (17)

Country Link
US (3) US11479551B2 (enExample)
EP (1) EP4028388A1 (enExample)
JP (1) JP7789662B2 (enExample)
KR (1) KR20220083691A (enExample)
CN (2) CN114728912A (enExample)
AU (1) AU2020345899B2 (enExample)
BR (1) BR112022004248A2 (enExample)
CA (1) CA3150515A1 (enExample)
CL (1) CL2022000603A1 (enExample)
CO (1) CO2022004513A2 (enExample)
IL (2) IL290341B2 (enExample)
MX (1) MX2022002938A (enExample)
NO (1) NO20220309A1 (enExample)
PH (1) PH12022550399A1 (enExample)
SA (1) SA522431915B1 (enExample)
TW (1) TW202122387A (enExample)
WO (1) WO2021050915A1 (enExample)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024008176A1 (zh) 2022-07-07 2024-01-11 西藏海思科制药有限公司 一种可抑制prmt5·mta的杂环化合物及其用途
IL290341B2 (en) * 2019-09-12 2024-11-01 Mirati Therapeutics Inc Mta-cooperative prmt5 inhibitors
US20240208912A1 (en) * 2021-03-11 2024-06-27 Mirati Therapeutics, Inc. MTA-Cooperative PRMT5 Inhibitors
EP4319753A1 (en) 2021-04-08 2024-02-14 Mirati Therapeutics, Inc. Combination therapies using prmt5 inhibitors for the treatment of cancer
WO2022216648A1 (en) 2021-04-08 2022-10-13 Mirati Therapeutics, Inc. Combination therapies using prmt5 inhibitors for the treatment of cancer
EP4347569A4 (en) * 2021-06-02 2025-03-26 Ideaya Biosciences, Inc. Combination therapy comprising a mat2a inhibitor and a type ii prmt inhibitor
MX2024004171A (es) 2021-10-06 2024-04-23 Mirati Therapeutics Inc Tratamientos conjuntos que usan inhibidores de la proteina arginina n-metil transferasa 5 (prmt5) para el tratamiento de cancer.
EP4412997A1 (en) 2021-10-06 2024-08-14 Mirati Therapeutics, Inc. Methods for separation of enantiomers
KR20240157631A (ko) 2021-11-05 2024-11-01 미라티 테라퓨틱스, 인크. Prmt5 저해제로서 2-아미노 이미다졸 유도체
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
WO2023125540A1 (zh) * 2021-12-27 2023-07-06 南京明德新药研发有限公司 吡唑-1(2h)-酞嗪酮类化合物及其应用
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
JP2025509404A (ja) * 2022-03-15 2025-04-11 ベイジーン スイッツァランド ゲーエムベーハー Ｐｒｍｔ５のｍｔａ協働阻害剤としての４－（アミノメチル）－６－（１－メチル－１ｈ－ピラゾール－４－イル）イソキノリン－１（２ｈ）－オン誘導体
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
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
WO2024027703A1 (zh) * 2022-08-02 2024-02-08 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
AU2023327684A1 (en) 2022-08-15 2025-03-20 Astrazeneca Ab Mta-cooperative prmt5 inhibitors for use in the treatment of cancer
IL319193A (en) 2022-09-01 2025-04-01 Mirati Therapeutics Inc Combination therapies using PRMT5 inhibitors and BCL-2 family inhibitors for cancer treatment
AU2023366908A1 (en) * 2022-10-25 2025-05-08 Tango Therapeutics, Inc. Crystalline forms, pharmaceutical compositions and methods of use thereof
CN120265615A (zh) * 2022-11-29 2025-07-04 正大天晴药业集团股份有限公司 含有二氢酞嗪的化合物
CN120693329A (zh) 2023-02-13 2025-09-23 米拉蒂治疗公司 2-(4-(4-(氨基甲基)-1-氧代-1,2-二氢酞嗪-6-基)-1-甲基-1h-吡唑-5-基)-4-氯-6-环丙氧基-3-氟苄腈的晶形
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
KR20250143848A (ko) 2023-02-13 2025-10-02 미라티 테라퓨틱스, 인크. 2-(4-(4-(아미노메틸)-1-옥소-1,2-디히드로프탈라진-6-일)-1-메틸-1h-피라졸-5-일)-4-클로로-6-시클로프로폭시-3-플루오로벤조니트릴의결정질 형태
KR102818470B1 (ko) * 2023-02-23 2025-06-10 한양대학교 산학협력단 신규한 아미노락톤 유도체 및 이의 신규한 제조방법
CR20250446A (es) 2023-04-21 2025-12-02 Gilead Sciences Inc Inhibidores de prmt5 y usos de los mismos
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
CN121646468A (zh) 2023-08-08 2026-03-10 米拉蒂治疗公司 用于治疗恶性周围神经鞘瘤的方法和组合物
TW202521525A (zh) 2023-08-09 2025-06-01 大陸商江蘇恆瑞醫藥股份有限公司 雜芳基化合物、其製備方法及其在醫藥上的應用
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
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
WO2025064750A1 (en) 2023-09-20 2025-03-27 Ideaya Biosciences, Inc. Combination therapy with a parg inhibitor
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
WO2025113499A1 (zh) * 2023-11-28 2025-06-05 正大天晴药业集团股份有限公司 含有杂环二氢酞嗪的化合物
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
US20250304556A1 (en) 2024-04-02 2025-10-02 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
WO2025217015A1 (en) 2024-04-08 2025-10-16 Mirati Therapeutics, Inc. Combination therapies using prmt5 inhibitors and kras g12d inhibitors for the treatment of cancer
US20250312344A1 (en) 2024-04-08 2025-10-09 Mirati Therapeutics, Inc. Combination therapies using prmt5 inhibitors and immune checkpoint inhibitors for the treatment of cancer
WO2026082013A1 (zh) * 2024-10-14 2026-04-23 西藏海思科制药有限公司 一种酞嗪酮类prmt5抑制剂及其中间体的制备方法

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
EP1326611B1 (en) * 2000-10-12 2007-06-13 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
IL290341B2 (en) * 2019-09-12 2024-11-01 Mirati Therapeutics Inc Mta-cooperative prmt5 inhibitors

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

Also Published As

Publication number Publication date
CN114728912A (zh) 2022-07-08
JP2022548255A (ja) 2022-11-17
AU2020345899A1 (en) 2022-03-03
WO2021050915A1 (en) 2021-03-18
IL313281A (en) 2024-08-01
KR20220083691A (ko) 2022-06-20
BR112022004248A2 (pt) 2022-05-31
JP7789662B2 (ja) 2025-12-22
SA522431915B1 (ar) 2025-06-12
US11479551B2 (en) 2022-10-25
US20210078994A1 (en) 2021-03-18
CL2022000603A1 (es) 2023-01-27
MX2022002938A (es) 2022-05-26
IL290341B2 (en) 2024-11-01
US20210079003A1 (en) 2021-03-18
CN120208880A (zh) 2025-06-27
US20230054883A1 (en) 2023-02-23
CA3150515A1 (en) 2021-03-18
US11492351B2 (en) 2022-11-08
IL290341A (en) 2022-04-01
CO2022004513A2 (es) 2022-06-21
IL290341B1 (en) 2024-07-01
PH12022550399A1 (en) 2023-03-13
IL313281B1 (en) 2026-03-01
NO20220309A1 (en) 2022-03-11
EP4028388A1 (en) 2022-07-20
TW202122387A (zh) 2021-06-16

Similar Documents

Publication Publication Date Title
AU2020345899B2 (en) MTA-cooperative PRMT5 inhibitors
US20240208912A1 (en) MTA-Cooperative PRMT5 Inhibitors
AU2022263410B2 (en) Carboxy-benzimidazole glp-1r modulating compounds
AU2021266351B2 (en) PRC2 inhibitors
JP5144532B2 (ja) ｃ−Ｍｅｔ阻害剤及び用法
WO2023278564A1 (en) Aminopyridine-based mta-cooperative prmt5 inhibitors
BRPI0707945A2 (pt) derivados de 3-deazapurina como modulares de tlr7
BR112016028845B1 (pt) Composto, composição farmacêutica e uso de um composto
WO2023081367A2 (en) 2-amino imidazole derivatives
EP3959214A1 (en) Naphthyridine derivatives as prc2 inhibitors
JP5937201B2 (ja) ２−アミノ−３−（イミダゾール−２−イル）ピリジン−４−オン誘導体及びｖｅｇｆ受容体キナーゼ阻害剤としてのその使用
EA048673B1 (ru) Mta-кооперативные ингибиторы prmt5
HK40110743A (zh) 腺苷受体拮抗剂
HK40077182B (en) Prc2 inhibitors
CN118974035A (zh) 作为prmt5抑制剂的2-氨基咪唑衍生物