CN115244037B - 作为甲状腺激素受体激动剂的被取代的三嗪酮类 - Google Patents

作为甲状腺激素受体激动剂的被取代的三嗪酮类 Download PDF

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CN115244037B
CN115244037B CN202180019696.0A CN202180019696A CN115244037B CN 115244037 B CN115244037 B CN 115244037B CN 202180019696 A CN202180019696 A CN 202180019696A CN 115244037 B CN115244037 B CN 115244037B
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CN115244037A (zh
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周敬业
朱久香
郑明伟
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Chengyi Biological Usa Co
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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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
    • C07D253/06—1,2,4-Triazines
    • C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
    • C07D253/07—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members with hetero atoms, or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D253/075—Two hetero atoms, in positions 3 and 5
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D403/12—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
    • 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
    • C07D405/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D471/08—Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
CN202180019696.0A 2020-01-13 2021-01-13 作为甲状腺激素受体激动剂的被取代的三嗪酮类 Active CN115244037B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CNPCT/CN2020/071741 2020-01-13
CN2020071741 2020-01-13
CNPCT/CN2020/107757 2020-08-07
CN2020107757 2020-08-07
PCT/CN2021/071381 WO2021143706A1 (en) 2020-01-13 2021-01-13 Substituted triazinones as thyroid hormone receptor agonists

Publications (2)

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CN115244037A CN115244037A (zh) 2022-10-25
CN115244037B true CN115244037B (zh) 2024-10-25

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US (3) US11780825B2 (https=)
EP (1) EP4090652A1 (https=)
JP (1) JP7728265B2 (https=)
KR (1) KR20220128383A (https=)
CN (1) CN115244037B (https=)
AU (1) AU2021208027B2 (https=)
IL (1) IL294494A (https=)
MX (1) MX2022008626A (https=)
WO (1) WO2021143706A1 (https=)
ZA (1) ZA202207541B (https=)

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GEP20247637B (en) 2019-05-08 2024-06-25 Aligos Therapeutics Inc Modulators of thr-b and methods of use thereof
EP4090652A1 (en) 2020-01-13 2022-11-23 Eccogene (Shanghai) Co., Ltd. Substituted triazinones as thyroid hormone receptor agonists
JP7813730B2 (ja) 2020-06-17 2026-02-13 オートバーン セラピューティクス，インク． 甲状腺様作用剤
WO2021257851A1 (en) 2020-06-17 2021-12-23 Autobahn Therapeutics, Inc. Thyromimetics
EP4240730A1 (en) 2020-11-06 2023-09-13 Aligos Therapeutics, Inc. 2-pyridones as thyroid hormone receptor modulators
CN114685450A (zh) * 2020-12-30 2022-07-01 昆药集团股份有限公司 2-吡啶酮类衍生物及其制备方法和在医药上的应用
CN117624069A (zh) * 2022-08-19 2024-03-01 凯思凯迪（上海）医药科技有限公司 一种多环类甲状腺激素β受体激动剂及其用途
CN118146123A (zh) * 2024-02-04 2024-06-07 河北鼎泰制药有限公司 一种盐酸安罗替尼中间体的合成方法
WO2026067791A1 (en) * 2024-09-30 2026-04-02 Ascletis Pharma (China) Co., Limited 2-phenyl-1,2,4-triazine-3,5(2h,4h)-dione derivatives as thr-beta agonist or modulators for the treatment of obesity

Citations (1)

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JP2012106996A (ja) * 2010-10-19 2012-06-07 Mitsubishi Tanabe Pharma Corp 新規甲状腺ホルモンβ受容体作動薬

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US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
EP1088819B1 (en) * 1999-09-30 2005-06-15 Pfizer Products Inc. 6-azauracil derivatives as thyroid receptor ligands
DK1262177T3 (da) 2001-05-31 2006-11-20 Pfizer Prod Inc Medicinsk brug af thyromimetiske forbindelser til behandling af hårtab og kompositioner
PL1919878T3 (pl) 2005-07-21 2011-03-31 Hoffmann La Roche Pochodne pirydazynonu jako agoniści receptora hormonu tarczycy
US8076334B2 (en) 2007-09-20 2011-12-13 Hoffmann-La Roche Inc. Prodrugs of thyroid hormone analogs
TWI534144B (zh) 2009-04-20 2016-05-21 田邊三菱製藥股份有限公司 甲狀腺荷爾蒙β受體作動藥
CN109574995B (zh) 2018-01-23 2020-07-24 深圳市塔吉瑞生物医药有限公司 取代的哒嗪酮化合物
CN111801324B (zh) 2018-06-12 2021-10-22 四川海思科制药有限公司 甲状腺激素受体激动剂及其用途
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EP4090652A1 (en) 2020-01-13 2022-11-23 Eccogene (Shanghai) Co., Ltd. Substituted triazinones as thyroid hormone receptor agonists
JP7813730B2 (ja) * 2020-06-17 2026-02-13 オートバーン セラピューティクス，インク． 甲状腺様作用剤

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JP2023510835A (ja) 2023-03-15
EP4090652A1 (en) 2022-11-23
CA3164404A1 (en) 2021-07-22
US12291518B2 (en) 2025-05-06
JP7728265B2 (ja) 2025-08-22
US20240190846A1 (en) 2024-06-13
US20250320197A1 (en) 2025-10-16
AU2021208027A1 (en) 2022-07-28
ZA202207541B (en) 2024-12-18
US20210230146A1 (en) 2021-07-29
IL294494A (en) 2022-09-01
KR20220128383A (ko) 2022-09-20
WO2021143706A1 (en) 2021-07-22
AU2021208027B2 (en) 2025-10-16
US11780825B2 (en) 2023-10-10
CN115244037A (zh) 2022-10-25
MX2022008626A (es) 2022-08-22

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