AU2019298236A1 - Solid forms of 2-(3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile - Google Patents

Solid forms of 2-(3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile Download PDF

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Publication number
AU2019298236A1
AU2019298236A1 AU2019298236A AU2019298236A AU2019298236A1 AU 2019298236 A1 AU2019298236 A1 AU 2019298236A1 AU 2019298236 A AU2019298236 A AU 2019298236A AU 2019298236 A AU2019298236 A AU 2019298236A AU 2019298236 A1 AU2019298236 A1 AU 2019298236A1
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diffraction pattern
ray powder
powder diffraction
morphic form
crystalline salt
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Abandoned
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AU2019298236A
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English (en)
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Pavan Karthik BATCHU
Marco Jonas
Mahmoud Mirmehrabi
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Madrigal Pharmaceuticals Inc
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Madrigal Pharmaceuticals Inc
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Publication of AU2019298236A1 publication Critical patent/AU2019298236A1/en
Priority to AU2025200189A priority Critical patent/AU2025200189A1/en
Abandoned legal-status Critical Current

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    • 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
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • 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
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Inorganic Chemistry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2019298236A 2018-07-02 2019-07-02 Solid forms of 2-(3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile Abandoned AU2019298236A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2025200189A AU2025200189A1 (en) 2018-07-02 2025-01-10 Solid forms of 2-(3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862692914P 2018-07-02 2018-07-02
US62/692,914 2018-07-02
PCT/US2019/040276 WO2020010068A1 (en) 2018-07-02 2019-07-02 Solid forms of 2-(3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2025200189A Division AU2025200189A1 (en) 2018-07-02 2025-01-10 Solid forms of 2-(3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile

Publications (1)

Publication Number Publication Date
AU2019298236A1 true AU2019298236A1 (en) 2021-01-21

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AU2019298236A Abandoned AU2019298236A1 (en) 2018-07-02 2019-07-02 Solid forms of 2-(3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
AU2025200189A Pending AU2025200189A1 (en) 2018-07-02 2025-01-10 Solid forms of 2-(3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile

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AU2025200189A Pending AU2025200189A1 (en) 2018-07-02 2025-01-10 Solid forms of 2-(3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile

Country Status (12)

Country Link
US (3) US20210122740A1 (enExample)
EP (2) EP3818057A1 (enExample)
JP (2) JP2021530456A (enExample)
KR (2) KR20250167140A (enExample)
CN (1) CN112638904A (enExample)
AR (1) AR115666A1 (enExample)
AU (2) AU2019298236A1 (enExample)
CA (1) CA3104860A1 (enExample)
IL (2) IL321116A (enExample)
MX (3) MX2021000107A (enExample)
TW (1) TW202019914A (enExample)
WO (1) WO2020010068A1 (enExample)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL314360B2 (en) 2012-09-17 2025-09-01 F Hoffmann La Roche Ltd Method for the synthesis of thyroid hormone analogs and their polymorphs
KR20190109387A (ko) 2016-10-18 2019-09-25 마드리갈 파마슈티칼스, 인크. Thr-베타 아고니스트로 간 질환 또는 지질 질환을 치료하는 방법
CN113474335B (zh) * 2019-02-21 2024-12-03 南京瑞捷医药科技有限公司 化合物及其作为甲状腺激素受体激动剂的用途
KR20220017917A (ko) 2019-05-08 2022-02-14 알리고스 테라퓨틱스 인코포레이티드 Thr-베타의 조절제 및 이의 사용 방법
WO2021063367A1 (zh) * 2019-09-30 2021-04-08 苏州科睿思制药有限公司 一种Resmetirom晶型及其制备方法和用途
WO2021129465A1 (zh) 2019-12-26 2021-07-01 苏州科睿思制药有限公司 一种Resmetirom晶型及其制备方法和用途
EP4286377A4 (en) * 2020-09-10 2024-10-09 Crystal Pharmaceutical (Suzhou) Co., Ltd. CRYSTALLINE FORM OF RESMETIROM, ITS PREPARATION METHOD AND ITS USE
CA3195789A1 (en) 2020-10-19 2022-04-28 Teva Pharmaceuticals International Gmbh Solid state forms of resmetirom
TW202245775A (zh) * 2021-02-01 2022-12-01 美商瑪德瑞高製藥公司 用於治療肝病症或脂質病症之瑞舒伐他汀(Rosuvastatin)和瑞司美替隆(Resmetirom)的治療組合
CN114907327A (zh) * 2021-02-10 2022-08-16 杭州领业医药科技有限公司 Resmetirom的晶型及其制备方法和用途
US20240218009A1 (en) * 2021-04-21 2024-07-04 Merck Sharp & Dohme Llc Novel forms of cyclic dinucleotide compounds
CN118871113A (zh) * 2021-11-11 2024-10-29 拓臻制药公司 使用THR-β激动剂的肝脏病症的治疗
US20240423992A1 (en) 2023-06-22 2024-12-26 Madrigal Pharmaceuticals, Inc. Biomarkers for treating liver disorders with thr-b agonists and related uses
WO2025011259A1 (zh) * 2023-07-07 2025-01-16 苏州科睿思制药有限公司 瑞司美替罗的晶型及其制备方法和用途
CN119613386A (zh) * 2023-09-14 2025-03-14 杭州科巢生物科技有限公司 一种瑞司美替罗1,4-二氧六环溶剂化合物及其制备方法
WO2025083699A2 (en) 2023-10-16 2025-04-24 Cipla Limited Resmetirom polymorphs and process thereof
US12377104B1 (en) 2024-02-06 2025-08-05 Madrigal Pharmaceuticals, Inc. Methods for treating a fatty liver disease
WO2025171032A1 (en) 2024-02-06 2025-08-14 Madrigal Pharmaceuticals, Inc. Methods for treating a fatty liver disease
WO2025172958A1 (en) * 2024-02-16 2025-08-21 Metrochem Api Pvt Ltd Solid state forms of resmetirom
WO2025231587A1 (zh) * 2024-05-06 2025-11-13 杭州科巢生物科技有限公司 一种瑞司美替罗无水晶型ch及其制备方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2930501A (en) * 2000-01-07 2001-07-24 Transform Pharmaceuticals, Inc. High-throughput formation, identification, and analysis of diverse solid-forms
JP5000649B2 (ja) * 2005-07-21 2012-08-15 エフ.ホフマン−ラ ロシュ アーゲー 甲状腺ホルモン受容体アゴニストとしてのピリダジノン誘導体
IL314360B2 (en) * 2012-09-17 2025-09-01 F Hoffmann La Roche Ltd Method for the synthesis of thyroid hormone analogs and their polymorphs
KR20190109387A (ko) * 2016-10-18 2019-09-25 마드리갈 파마슈티칼스, 인크. Thr-베타 아고니스트로 간 질환 또는 지질 질환을 치료하는 방법

Also Published As

Publication number Publication date
MX2024013198A (es) 2024-12-06
US20250074898A1 (en) 2025-03-06
AR115666A1 (es) 2021-02-10
KR20210027454A (ko) 2021-03-10
KR20250167140A (ko) 2025-11-28
US20250368626A1 (en) 2025-12-04
CN112638904A (zh) 2021-04-09
US20210122740A1 (en) 2021-04-29
IL321116A (en) 2025-07-01
AU2025200189A1 (en) 2025-01-30
KR102890565B1 (ko) 2025-11-24
JP2021530456A (ja) 2021-11-11
CA3104860A1 (en) 2020-01-09
EP4552643A2 (en) 2025-05-14
EP3818057A1 (en) 2021-05-12
EP4552643A3 (en) 2025-07-02
TW202019914A (zh) 2020-06-01
JP2024105460A (ja) 2024-08-06
MX2023009701A (es) 2023-08-29
IL279700A (en) 2021-03-01
MX2021000107A (es) 2021-05-27
WO2020010068A1 (en) 2020-01-09

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