CN112638904A - 2-(3,5-二氯-4-((5-异丙基-6-氧代-1,6-二氢哒嗪-3-基)氧基)苯基)-3,5-二氧代-2,3,4,5-四氢-1,2,4-三嗪-6-腈的固体形式 - Google Patents

2-(3,5-二氯-4-((5-异丙基-6-氧代-1,6-二氢哒嗪-3-基)氧基)苯基)-3,5-二氧代-2,3,4,5-四氢-1,2,4-三嗪-6-腈的固体形式 Download PDF

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CN112638904A
CN112638904A CN201980056826.0A CN201980056826A CN112638904A CN 112638904 A CN112638904 A CN 112638904A CN 201980056826 A CN201980056826 A CN 201980056826A CN 112638904 A CN112638904 A CN 112638904A
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diffraction pattern
crystalline form
ray powder
powder diffraction
crystalline
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Chinese (zh)
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M·米尔赫拉比
M·乔纳斯
P·K·巴楚
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Synta Phamaceuticals Corp
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Synta Phamaceuticals Corp
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    • 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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline 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)
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  • Medicinal Chemistry (AREA)
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  • 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)
CN201980056826.0A 2018-07-02 2019-07-02 2-(3,5-二氯-4-((5-异丙基-6-氧代-1,6-二氢哒嗪-3-基)氧基)苯基)-3,5-二氧代-2,3,4,5-四氢-1,2,4-三嗪-6-腈的固体形式 Pending CN112638904A (zh)

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

Publications (1)

Publication Number Publication Date
CN112638904A true CN112638904A (zh) 2021-04-09

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CN201980056826.0A Pending CN112638904A (zh) 2018-07-02 2019-07-02 2-(3,5-二氯-4-((5-异丙基-6-氧代-1,6-二氢哒嗪-3-基)氧基)苯基)-3,5-二氧代-2,3,4,5-四氢-1,2,4-三嗪-6-腈的固体形式

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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)

Cited By (3)

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CN114787153A (zh) * 2019-12-26 2022-07-22 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
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

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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
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
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

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CN101228135A (zh) * 2005-07-21 2008-07-23 霍夫曼-拉罗奇有限公司 作为甲状腺激素受体激动剂的哒嗪酮衍生物
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CN105008335A (zh) * 2012-09-17 2015-10-28 马德里加尔制药公司 合成甲状腺激素类似物及其多形体的方法
WO2018075650A1 (en) * 2016-10-18 2018-04-26 Madrigal Pharmaceuticals, Inc. Methods of treating liver disorders or lipid disorders with a thr-beta agonist

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MARTHA J. KELLY等: "Discovery of 2‑[3,5-Dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β Agonist in Clinical Trials for the Treatment of Dyslipidemia" *
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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114787153A (zh) * 2019-12-26 2022-07-22 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
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

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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
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
AU2019298236A1 (en) 2021-01-21
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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