TWI815061B - 作為δ-５去飽和酶抑制劑的雜環化合物以及使用方法 - Google Patents

作為δ-５去飽和酶抑制劑的雜環化合物以及使用方法 Download PDF

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Publication number
TWI815061B
TWI815061B TW109141315A TW109141315A TWI815061B TW I815061 B TWI815061 B TW I815061B TW 109141315 A TW109141315 A TW 109141315A TW 109141315 A TW109141315 A TW 109141315A TW I815061 B TWI815061 B TW I815061B
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Prior art keywords
methyl
trifluoromethyl
pyrimidin
compound
tautomer
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TW109141315A
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Chinese (zh)
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TW202132317A (zh
Inventor
馬修 保羅 鮑比優
珍妮佛 瑞貝卡 艾蓮
安娜 艾蓮娜 米那提
保羅 溫西蒂
米歇拉 貝爾特拉尼
特奧多拉 達米亞諾娃
伊安 霖嘉德
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美商安進公司
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Child & Adolescent Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (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)
TW109141315A 2019-11-25 2020-11-25 作為δ-５去飽和酶抑制劑的雜環化合物以及使用方法 TWI815061B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962939821P 2019-11-25 2019-11-25
US62/939,821 2019-11-25

Publications (2)

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TW202132317A TW202132317A (zh) 2021-09-01
TWI815061B true TWI815061B (zh) 2023-09-11

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TW109141315A TWI815061B (zh) 2019-11-25 2020-11-25 作為δ-５去飽和酶抑制劑的雜環化合物以及使用方法
TW112142068A TWI867822B (zh) 2019-11-25 2020-11-25 作為δ-5去飽和酶抑制劑的雜環化合物以及使用方法

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US (3) US11512097B2 (enExample)
EP (1) EP4065223A1 (enExample)
JP (2) JP7254246B2 (enExample)
KR (2) KR20230154292A (enExample)
CN (2) CN114728167B (enExample)
AR (1) AR120556A1 (enExample)
AU (1) AU2020392087B2 (enExample)
BR (1) BR112022010054A2 (enExample)
CA (1) CA3162281A1 (enExample)
CL (2) CL2022001357A1 (enExample)
CO (1) CO2022008690A2 (enExample)
CR (1) CR20220308A (enExample)
IL (1) IL293191B2 (enExample)
JO (1) JOP20220125A1 (enExample)
MX (1) MX2022006281A (enExample)
PE (1) PE20231097A1 (enExample)
PH (1) PH12022551282A1 (enExample)
SA (1) SA522432710B1 (enExample)
TW (2) TWI815061B (enExample)
UY (1) UY38971A (enExample)
WO (1) WO2021108408A1 (enExample)

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US11220510B2 (en) * 2018-04-09 2022-01-11 Incyte Corporation Pyrrole tricyclic compounds as A2A / A2B inhibitors
PH12022551282A1 (en) * 2019-11-25 2023-11-29 Amgen Inc Heterocyclic compounds as delta-5 desaturase inhibitors and methods of use
CN115557903A (zh) * 2022-09-27 2023-01-03 山东潍坊润丰化工股份有限公司 一种特草定的制备方法
TW202434254A (zh) 2022-11-23 2024-09-01 美商安進公司 選擇用於fads1調節劑治療的患者之方法

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CR20220308A (es) 2022-08-04
US11512097B2 (en) 2022-11-29
AU2020392087B2 (en) 2025-10-23
US20210221824A1 (en) 2021-07-22
PH12022551282A1 (en) 2023-11-29
TW202132317A (zh) 2021-09-01
BR112022010054A2 (pt) 2022-08-16
CN114728167B (zh) 2024-03-19
CL2022001357A1 (es) 2023-03-10
TW202409042A (zh) 2024-03-01
IL293191B1 (en) 2025-05-01
US12448396B2 (en) 2025-10-21
WO2021108408A1 (en) 2021-06-03
IL293191A (en) 2022-07-01
TWI867822B (zh) 2024-12-21
CL2023002486A1 (es) 2024-01-12
CN114728167A (zh) 2022-07-08
KR102598203B1 (ko) 2023-11-03
JP7698676B2 (ja) 2025-06-25
MX2022006281A (es) 2022-06-08
JP7254246B2 (ja) 2023-04-07
US20210188874A1 (en) 2021-06-24
CN118161500A (zh) 2024-06-11
JP2023078418A (ja) 2023-06-06
CO2022008690A2 (es) 2022-06-30
US20230159560A1 (en) 2023-05-25
IL293191B2 (en) 2025-09-01
AU2020392087A1 (en) 2022-06-09
UY38971A (es) 2021-06-30
KR20220106159A (ko) 2022-07-28
JP2022549739A (ja) 2022-11-28
SA522432710B1 (ar) 2025-05-29
KR20230154292A (ko) 2023-11-07
AR120556A1 (es) 2022-02-23
CA3162281A1 (en) 2021-06-03
EP4065223A1 (en) 2022-10-05
JOP20220125A1 (ar) 2023-01-30
PE20231097A1 (es) 2023-07-18

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