JP2021530456A - ２−（３，５−ジクロロ−４−（（５−イソプロピル−６−オキソ−１，６−ジヒドロピリダジン−３−イル）オキシ）フェニル）−３，５−ジオキソ−２，３，４，５−テトラヒドロ−１，２，４−トリアジン−６−カルボニトリルの固体形態 - Google Patents

２−（３，５−ジクロロ−４−（（５−イソプロピル−６−オキソ−１，６−ジヒドロピリダジン−３−イル）オキシ）フェニル）−３，５−ジオキソ−２，３，４，５−テトラヒドロ−１，２，４−トリアジン−６−カルボニトリルの固体形態 Download PDF

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JP2021530456A
JP2021530456A JP2020572517A JP2020572517A JP2021530456A JP 2021530456 A JP2021530456 A JP 2021530456A JP 2020572517 A JP2020572517 A JP 2020572517A JP 2020572517 A JP2020572517 A JP 2020572517A JP 2021530456 A JP2021530456 A JP 2021530456A
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diffraction pattern
powder diffraction
morphic form
ray powder
ray
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Japanese (ja)
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JPWO2020010068A5 (enExample
Inventor
ミアメラビ，マフムード
ジョナス，マルコ
バッチュ，パバン・カーティク
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Madrigal Pharmaceuticals Inc
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Madrigal Pharmaceuticals Inc
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Publication of JPWO2020010068A5 publication Critical patent/JPWO2020010068A5/ja
Priority to JP2024076310A priority Critical patent/JP2024105460A/ja
Pending legal-status Critical Current

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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)
  • 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)
JP2020572517A 2018-07-02 2019-07-02 ２−（３，５−ジクロロ−４−（（５−イソプロピル−６−オキソ−１，６−ジヒドロピリダジン−３−イル）オキシ）フェニル）−３，５−ジオキソ−２，３，４，５−テトラヒドロ−１，２，４−トリアジン−６−カルボニトリルの固体形態 Pending JP2021530456A (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2024076310A JP2024105460A (ja) 2018-07-02 2024-05-09 ２－（３，５－ジクロロ－４－（（５－イソプロピル－６－オキソ－１，６－ジヒドロピリダジン－３－イル）オキシ）フェニル）－３，５－ジオキソ－２，３，４，５－テトラヒドロ－１，２，４－トリアジン－６－カルボニトリルの固体形態

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
JP2024076310A Division JP2024105460A (ja) 2018-07-02 2024-05-09 ２－（３，５－ジクロロ－４－（（５－イソプロピル－６－オキソ－１，６－ジヒドロピリダジン－３－イル）オキシ）フェニル）－３，５－ジオキソ－２，３，４，５－テトラヒドロ－１，２，４－トリアジン－６－カルボニトリルの固体形態

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JP2021530456A true JP2021530456A (ja) 2021-11-11
JPWO2020010068A5 JPWO2020010068A5 (enExample) 2022-07-08

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JP2020572517A Pending JP2021530456A (ja) 2018-07-02 2019-07-02 ２−（３，５−ジクロロ−４−（（５−イソプロピル−６−オキソ−１，６−ジヒドロピリダジン−３−イル）オキシ）フェニル）−３，５−ジオキソ−２，３，４，５−テトラヒドロ−１，２，４−トリアジン−６−カルボニトリルの固体形態
JP2024076310A Pending JP2024105460A (ja) 2018-07-02 2024-05-09 ２－（３，５－ジクロロ－４－（（５－イソプロピル－６－オキソ－１，６－ジヒドロピリダジン－３－イル）オキシ）フェニル）－３，５－ジオキソ－２，３，４，５－テトラヒドロ－１，２，４－トリアジン－６－カルボニトリルの固体形態

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JP2024076310A Pending JP2024105460A (ja) 2018-07-02 2024-05-09 ２－（３，５－ジクロロ－４－（（５－イソプロピル－６－オキソ－１，６－ジヒドロピリダジン－３－イル）オキシ）フェニル）－３，５－ジオキソ－２，３，４，５－テトラヒドロ－１，２，４－トリアジン－６－カルボニトリルの固体形態

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US (3) US20210122740A1 (enExample)
EP (2) EP4552643A3 (enExample)
JP (2) JP2021530456A (enExample)
KR (2) KR20250167140A (enExample)
CN (1) CN112638904A (enExample)
AR (1) AR115666A1 (enExample)
AU (2) AU2019298236A1 (enExample)
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Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR092872A1 (es) 2012-09-17 2015-05-06 Madrigal Pharmaceuticals Inc Metodo para sintetizar analogos de la hormona tiroidea y polimorfos de los mismos
CN110167557A (zh) 2016-10-18 2019-08-23 马德里加尔制药公司 用thr-beta兴奋剂治疗肝脏疾病或脂质疾病的方法
US12338206B2 (en) 2019-02-21 2025-06-24 Nanjing Ruijie Pharma Co., Ltd. Compounds and their uses as thyroid hormone receptor agonists
SI3965884T1 (sl) 2019-05-08 2025-05-30 Aligos Therapeutics, Inc. Modulatorji thr-beta z glavno skupino dioxo-1,2,4-triazil
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
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
CA3192243A1 (en) 2020-09-10 2022-03-17 Crystal Pharmaceutical (Suzhou) Co., Ltd. Crystal form of resmetirom, preparation method therefor, and use thereof
US20230364099A1 (en) 2020-10-19 2023-11-16 Teva Pharmaceuticals International Gmbh Solid state forms of resmetirom
JP2024506848A (ja) * 2021-02-01 2024-02-15 マドリガル ファーマシューティカルズ インコーポレイテッド 肝障害又は脂質障害の治療のためのロスバスタチンとレスメチロムの治療的組み合わせ
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
IL312637A (en) * 2021-11-11 2024-07-01 Terns Pharmaceuticals Inc Treatment of liver disorders with a thr-β agonist
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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015535817A (ja) * 2012-09-17 2015-12-17 マドリガル・ファーマシューティカルズ・インコーポレーテッドＭａｄｒｉｇａｌ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． 甲状腺ホルモンアナログ及びその多形体の合成方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SK9742002A3 (en) * 2000-01-07 2003-02-04 Transform Pharmaceuticals Inc High-throughput formation, identification, and analysis of diverse solid-forms
RU2379295C2 (ru) * 2005-07-21 2010-01-20 Ф.Хоффманн-Ля Рош Аг Производные пиридазинона в качестве агонистов рецептора тиреоидного гормона
CN110167557A (zh) * 2016-10-18 2019-08-23 马德里加尔制药公司 用thr-beta兴奋剂治疗肝脏疾病或脂质疾病的方法

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015535817A (ja) * 2012-09-17 2015-12-17 マドリガル・ファーマシューティカルズ・インコーポレーテッドＭａｄｒｉｇａｌ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． 甲状腺ホルモンアナログ及びその多形体の合成方法

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
BERGE，S. M., ET AL., JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 66, no. 1, JPN5004004439, 1977, US, pages 1 - 19, ISSN: 0005231967 *
PATRIC STAHLY: "医薬品の塩選択、結晶多形のスクリーニングの重要性について", 薬剤学, vol. 66(6), JPN7023002657, 2006, pages 435 - 439, ISSN: 0005231966 *
高田則幸: "創薬段階における原薬Formスクリーニングと選択", PHARM STAGE, vol. 6, no. 10, JPN6009053755, 15 January 2007 (2007-01-15), pages 20 - 25, ISSN: 0005231968 *

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AU2019298236A1 (en) 2021-01-21
KR102890565B1 (ko) 2025-11-24
US20210122740A1 (en) 2021-04-29
WO2020010068A1 (en) 2020-01-09
CN112638904A (zh) 2021-04-09
CA3104860A1 (en) 2020-01-09
AR115666A1 (es) 2021-02-10
MX2024013198A (es) 2024-12-06
IL321116A (en) 2025-07-01
MX2021000107A (es) 2021-05-27
EP3818057A1 (en) 2021-05-12
EP4552643A3 (en) 2025-07-02
MX2023009701A (es) 2023-08-29
US20250368626A1 (en) 2025-12-04
IL279700A (en) 2021-03-01
KR20250167140A (ko) 2025-11-28
US20250074898A1 (en) 2025-03-06
TW202019914A (zh) 2020-06-01
AU2025200189A1 (en) 2025-01-30
JP2024105460A (ja) 2024-08-06
EP4552643A2 (en) 2025-05-14
KR20210027454A (ko) 2021-03-10

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