AU2021208027B2 - Substituted triazinones as thyroid hormone receptor agonists - Google Patents

Substituted triazinones as thyroid hormone receptor agonists

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Publication number
AU2021208027B2
AU2021208027B2 AU2021208027A AU2021208027A AU2021208027B2 AU 2021208027 B2 AU2021208027 B2 AU 2021208027B2 AU 2021208027 A AU2021208027 A AU 2021208027A AU 2021208027 A AU2021208027 A AU 2021208027A AU 2021208027 B2 AU2021208027 B2 AU 2021208027B2
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AU
Australia
Prior art keywords
dichloro
phenoxy
dioxo
triazin
difluoromethyl
Prior art date
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Active
Application number
AU2021208027A
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English (en)
Other versions
AU2021208027A1 (en
Inventor
Mingwei Zheng
Jingye Zhou
Jiuxiang Zhu
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Eccogene Inc United States
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Eccogene Inc United States
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Application filed by Eccogene Inc United States filed Critical Eccogene Inc United States
Publication of AU2021208027A1 publication Critical patent/AU2021208027A1/en
Assigned to ECCOGENE INC. reassignment ECCOGENE INC. Request for Assignment Assignors: ECCOGENE (SHANGHAI) CO., LTD.
Application granted granted Critical
Publication of AU2021208027B2 publication Critical patent/AU2021208027B2/en
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Classifications

    • 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
    • A61K31/53Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D253/00Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02Heterocyclic 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
    • C07D253/061,2,4-Triazines
    • C07D253/0651,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
    • C07D253/071,2,4-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
    • C07D253/075Two hetero atoms, in positions 3 and 5
    • 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
    • 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
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • 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
    • 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • 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
    • 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
    • C07D471/08Bridged systems

Landscapes

  • 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)
AU2021208027A 2020-01-13 2021-01-13 Substituted triazinones as thyroid hormone receptor agonists Active AU2021208027B2 (en)

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)

Publication Number Publication Date
AU2021208027A1 AU2021208027A1 (en) 2022-07-28
AU2021208027B2 true AU2021208027B2 (en) 2025-10-16

Family

ID=74418122

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2021208027A Active AU2021208027B2 (en) 2020-01-13 2021-01-13 Substituted triazinones as thyroid hormone receptor agonists

Country Status (10)

Country Link
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=)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1088819A2 (en) * 1999-09-30 2001-04-04 Pfizer Products Inc. 6-azauracil derivatives as thyroid receptor ligands
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
WO2020169069A1 (en) * 2019-02-21 2020-08-27 Nanjing Ruijie Pharma Co., Ltd. Novel compounds and their uses as thyroid hormone receptor agonists

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1088819A2 (en) * 1999-09-30 2001-04-04 Pfizer Products Inc. 6-azauracil derivatives as thyroid receptor ligands
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
WO2020169069A1 (en) * 2019-02-21 2020-08-27 Nanjing Ruijie Pharma Co., Ltd. Novel compounds and their uses as thyroid hormone receptor agonists

Also Published As

Publication number Publication date
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
CN115244037B (zh) 2024-10-25
US11780825B2 (en) 2023-10-10
CN115244037A (zh) 2022-10-25
MX2022008626A (es) 2022-08-22

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