TWI786777B - Sarm1之抑制劑 - Google Patents

Sarm1之抑制劑 Download PDF

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Publication number
TWI786777B
TWI786777B TW110130799A TW110130799A TWI786777B TW I786777 B TWI786777 B TW I786777B TW 110130799 A TW110130799 A TW 110130799A TW 110130799 A TW110130799 A TW 110130799A TW I786777 B TWI786777 B TW I786777B
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TW
Taiwan
Prior art keywords
compound
pharmaceutically acceptable
acceptable salt
chiral
mmol
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TW110130799A
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English (en)
Chinese (zh)
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TW202214597A (zh
Inventor
陶德 波薩納克
拉杰什 德芙拉吉
羅伯特 歐文 修斯
安德鲁 布雷利
派克 理查 安德魯 傑瑞斯
雪莉 安妮 帕勒特
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美商達薩瑪治療公司
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW110130799A 2020-08-24 2021-08-20 Sarm1之抑制劑 TWI786777B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US202063069408P 2020-08-24 2020-08-24
US63/069,408 2020-08-24
US202163142398P 2021-01-27 2021-01-27
US63/142,398 2021-01-27

Publications (2)

Publication Number Publication Date
TW202214597A TW202214597A (zh) 2022-04-16
TWI786777B true TWI786777B (zh) 2022-12-11

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TW110130799A TWI786777B (zh) 2020-08-24 2021-08-20 Sarm1之抑制劑
TW111144632A TW202334117A (zh) 2020-08-24 2021-08-20 Sarm1之抑制劑

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Country Status (18)

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US (2) US12043613B2 (enExample)
EP (1) EP4200293A1 (enExample)
JP (2) JP7349046B2 (enExample)
KR (1) KR20230057396A (enExample)
AU (2) AU2021333558C1 (enExample)
BR (1) BR112023002575A2 (enExample)
CA (1) CA3189181A1 (enExample)
CL (1) CL2023000525A1 (enExample)
CO (1) CO2023001975A2 (enExample)
CR (1) CR20230113A (enExample)
DO (1) DOP2023000038A (enExample)
EC (1) ECSP23012981A (enExample)
IL (1) IL300586A (enExample)
MX (1) MX2023002256A (enExample)
PE (1) PE20230737A1 (enExample)
TW (2) TWI786777B (enExample)
WO (1) WO2022046606A1 (enExample)
ZA (1) ZA202301801B (enExample)

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WO2022060812A1 (en) 2020-09-16 2022-03-24 Nura Bio, Inc. Substituted pyridine derivatives as sarm1 inhibitors
CA3226869A1 (en) 2021-07-28 2023-02-02 Rao Kolluri Substituted pyridine derivatives as sarm1 inhibitors
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WO2024125624A1 (en) * 2022-12-15 2024-06-20 Sironax Ltd. Sarm1 modulators, preparations, and uses thereof
EP4655069A1 (en) 2023-01-24 2025-12-03 Disarm Therapeutics, Inc. Pyridazines as sarm1 inhibitors
WO2024222835A1 (en) * 2023-04-27 2024-10-31 Sironax Ltd. Sarm1 modulators, preparations, and uses thereof
CN119219603A (zh) * 2023-06-28 2024-12-31 科辉智药(深圳)新药研究中心有限公司 Sarm1酶活性抑制剂及其用途
WO2025049184A1 (en) 2023-08-25 2025-03-06 Eli Lilly And Company (s)-3-((6-fluoropyridin-3-yl)methyl)-1-(5-(pyridin-4-yl)-4h-1,2,4-triazol-3-yl)piperidin-2-one benzenesulfonate
WO2025045746A1 (en) * 2023-08-25 2025-03-06 F. Hoffmann-La Roche Ag Pyrazole derivatives as sarm1 inhibitors useful for the treatment of neurodegenerative disorders
WO2025076088A1 (en) * 2023-10-05 2025-04-10 Genentech, Inc. Lactams for use as sarm1 inhibitors
WO2025076017A1 (en) * 2023-10-05 2025-04-10 Genentech, Inc. Carbamates for use as sarm1 inhibitors
WO2025157895A1 (en) 2024-01-25 2025-07-31 UCB Biopharma SRL Pyrrolidinone derivatives

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US7585881B2 (en) 2004-02-18 2009-09-08 Astrazeneca Ab Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
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Publication number Publication date
JP2023535236A (ja) 2023-08-16
AU2021333558C1 (en) 2024-06-20
TW202214597A (zh) 2022-04-16
MX2023002256A (es) 2023-03-17
US20220056013A1 (en) 2022-02-24
JP7756130B2 (ja) 2025-10-17
WO2022046606A1 (en) 2022-03-03
CO2023001975A2 (es) 2023-03-07
US12043613B2 (en) 2024-07-23
DOP2023000038A (es) 2023-03-15
AU2024203373A1 (en) 2024-06-13
BR112023002575A2 (pt) 2023-03-07
TW202530197A (zh) 2025-08-01
PE20230737A1 (es) 2023-05-03
CR20230113A (es) 2023-04-14
AU2021333558B2 (en) 2024-02-22
CA3189181A1 (en) 2022-03-03
AU2021333558A1 (en) 2023-03-02
ZA202301801B (en) 2024-09-25
JP7349046B2 (ja) 2023-09-21
ECSP23012981A (es) 2023-03-31
KR20230057396A (ko) 2023-04-28
IL300586A (en) 2023-04-01
EP4200293A1 (en) 2023-06-28
JP2024016014A (ja) 2024-02-06
TW202334117A (zh) 2023-09-01
US20240376083A1 (en) 2024-11-14
CL2023000525A1 (es) 2023-09-15

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