CN116547274B - Magl抑制剂 - Google Patents

Magl抑制剂

Info

Publication number
CN116547274B
CN116547274B CN202180073621.0A CN202180073621A CN116547274B CN 116547274 B CN116547274 B CN 116547274B CN 202180073621 A CN202180073621 A CN 202180073621A CN 116547274 B CN116547274 B CN 116547274B
Authority
CN
China
Prior art keywords
azaspiro
octane
hexafluoropropan
ester
carboxylic acid
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
CN202180073621.0A
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English (en)
Chinese (zh)
Other versions
CN116547274A (zh
Inventor
约翰·J·M·维纳
谢丽尔·A·格莱斯
丹尼尔·J·布扎德
贾斯汀·S·奇萨
奥利维亚·D·韦伯
A·艾伦
N·拉法埃莱
J·V·穆迪
迈克尔·B·沙格哈飞
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.)
H Lundbeck AS
Original Assignee
H Lundbeck AS
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Priority to CN202512011225.8A priority Critical patent/CN121824488A/zh
Publication of CN116547274A publication Critical patent/CN116547274A/zh
Application granted granted Critical
Publication of CN116547274B publication Critical patent/CN116547274B/zh
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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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
    • 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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/20Spiro-condensed ring systems
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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 chain containing hetero atoms as chain links
    • 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
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN202180073621.0A 2020-11-13 2021-11-12 Magl抑制剂 Active CN116547274B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202512011225.8A CN121824488A (zh) 2020-11-13 2021-11-12 Magl抑制剂

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063113662P 2020-11-13 2020-11-13
US63/113,662 2020-11-13
PCT/EP2021/081522 WO2022101412A1 (en) 2020-11-13 2021-11-12 A magl inhibitor

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN202512011225.8A Division CN121824488A (zh) 2020-11-13 2021-11-12 Magl抑制剂

Publications (2)

Publication Number Publication Date
CN116547274A CN116547274A (zh) 2023-08-04
CN116547274B true CN116547274B (zh) 2026-02-13

Family

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Family Applications (2)

Application Number Title Priority Date Filing Date
CN202180073621.0A Active CN116547274B (zh) 2020-11-13 2021-11-12 Magl抑制剂
CN202512011225.8A Pending CN121824488A (zh) 2020-11-13 2021-11-12 Magl抑制剂

Family Applications After (1)

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Country Status (33)

Country Link
US (2) US11434222B2 (https=)
EP (2) EP4244208B1 (https=)
JP (1) JP2023549051A (https=)
KR (1) KR20230107225A (https=)
CN (2) CN116547274B (https=)
AR (1) AR124057A1 (https=)
AU (1) AU2021379081A1 (https=)
CA (1) CA3196119A1 (https=)
CL (1) CL2023001339A1 (https=)
CO (1) CO2023004649A2 (https=)
CR (1) CR20230203A (https=)
DK (1) DK4244208T3 (https=)
DO (1) DOP2023000086A (https=)
ES (1) ES3025484T3 (https=)
FI (1) FI4244208T3 (https=)
GE (2) GEP20257794B (https=)
HR (1) HRP20250644T1 (https=)
HU (1) HUE071543T2 (https=)
IL (1) IL301818B1 (https=)
JO (1) JOP20230091A1 (https=)
LT (1) LT4244208T (https=)
MA (1) MA62148B1 (https=)
MX (1) MX2023005576A (https=)
PL (1) PL4244208T3 (https=)
PT (1) PT4244208T (https=)
RS (1) RS66839B1 (https=)
SA (1) SA523440403B1 (https=)
SI (1) SI4244208T1 (https=)
TW (1) TWI904281B (https=)
UA (1) UA130186C2 (https=)
UY (1) UY39516A (https=)
WO (1) WO2022101412A1 (https=)
ZA (1) ZA202304134B (https=)

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JOP20190107A1 (ar) 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
CA3242372A1 (en) 2021-12-29 2023-07-06 Psy Therapeutics, Inc. Inhibiting monoacylglycerol lipase (magl)
KR20250005229A (ko) * 2022-05-04 2025-01-09 하. 룬드벡 아크티에셀스카브 모노아실글리세롤 리파제 억제제로서 1,1,1,3,3,3-헥사플루오로프로판-2-일 (s)-1-(피리다진-3-일카르바모일)-6 아자스피로[2.5]옥탄-6-카르복실레이트의 결정질 형태

Citations (2)

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CN110198944A (zh) * 2017-01-23 2019-09-03 辉瑞大药厂 作为单酰基甘油脂肪酶抑制剂的杂环螺环化合物

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JOP20190105A1 (ar) 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
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KR20250005229A (ko) * 2022-05-04 2025-01-09 하. 룬드벡 아크티에셀스카브 모노아실글리세롤 리파제 억제제로서 1,1,1,3,3,3-헥사플루오로프로판-2-일 (s)-1-(피리다진-3-일카르바모일)-6 아자스피로[2.5]옥탄-6-카르복실레이트의 결정질 형태

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CN104520290A (zh) * 2012-03-02 2015-04-15 基因科技股份有限公司 酰氨基螺环酰胺和磺酰胺衍生物
CN110198944A (zh) * 2017-01-23 2019-09-03 辉瑞大药厂 作为单酰基甘油脂肪酶抑制剂的杂环螺环化合物

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IL301818A (en) 2023-06-01
US20220153721A1 (en) 2022-05-19
SI4244208T1 (sl) 2025-07-31
EP4244208A1 (en) 2023-09-20
IL301818B1 (en) 2026-02-01
CA3196119A1 (en) 2022-05-19
ES3025484T3 (en) 2025-06-09
PT4244208T (pt) 2025-05-22
GEP20257794B (en) 2025-09-10
TWI904281B (zh) 2025-11-11
CR20230203A (es) 2023-06-14
MX2023005576A (es) 2023-05-29
HUE071543T2 (hu) 2025-09-28
EP4244208B1 (en) 2025-04-02
DK4244208T3 (da) 2025-05-26
PL4244208T3 (pl) 2025-06-30
TW202229255A (zh) 2022-08-01
WO2022101412A1 (en) 2022-05-19
KR20230107225A (ko) 2023-07-14
EP4574150A2 (en) 2025-06-25
AR124057A1 (es) 2023-02-08
DOP2023000086A (es) 2023-06-30
FI4244208T3 (fi) 2025-06-10
RS66839B1 (sr) 2025-06-30
AU2021379081A1 (en) 2023-05-18
ZA202304134B (en) 2024-08-28
JP2023549051A (ja) 2023-11-22
SA523440403B1 (ar) 2024-10-10
JOP20230091A1 (ar) 2023-05-01
UY39516A (es) 2022-05-31
CN116547274A (zh) 2023-08-04
EP4574150A3 (en) 2025-08-20
LT4244208T (lt) 2025-06-10
US20240018120A1 (en) 2024-01-18
US11434222B2 (en) 2022-09-06
MA62148B1 (fr) 2025-05-30
UA130186C2 (uk) 2025-12-10
CL2023001339A1 (es) 2023-10-20
HRP20250644T1 (hr) 2025-07-18
CN121824488A (zh) 2026-04-10
GEAP202516246A (en) 2025-04-10
CO2023004649A2 (es) 2023-05-08

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