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

Info

Publication number
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
Authority
CN
China
Prior art keywords
diffraction pattern
crystalline form
ray powder
powder diffraction
crystalline
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN201980056826.0A
Other languages
English (en)
Chinese (zh)
Inventor
M·米尔赫拉比
M·乔纳斯
P·K·巴楚
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Synta Phamaceuticals Corp
Original Assignee
Synta Phamaceuticals Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Synta Phamaceuticals Corp filed Critical Synta Phamaceuticals Corp
Publication of CN112638904A publication Critical patent/CN112638904A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • 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

Landscapes

  • 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)
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

Family

ID=67441642

Family Applications (1)

Application Number Title Priority Date Filing Date
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

Country Status (12)

Country Link
US (3) US20210122740A1 (https=)
EP (2) EP3818057A1 (https=)
JP (2) JP2021530456A (https=)
KR (2) KR102890565B1 (https=)
CN (1) CN112638904A (https=)
AR (1) AR115666A1 (https=)
AU (2) AU2019298236A1 (https=)
CA (1) CA3104860A1 (https=)
IL (2) IL321116A (https=)
MX (3) MX2021000107A (https=)
TW (1) TW202019914A (https=)
WO (1) WO2020010068A1 (https=)

Cited By (4)

* 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
WO2026067708A1 (zh) * 2024-09-30 2026-04-02 齐鲁制药有限公司 瑞司美替罗晶型及其制备方法和用途

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LT4406594T (lt) 2012-09-17 2025-12-29 Madrigal Pharmaceuticals, Inc. Skydliaukės hormono analogai
IL266054B2 (en) 2016-10-18 2023-10-01 Madrigal Pharmaceuticals Inc Methods for treating liver disorders or lipid disorders using a THR-BETA agonist
US12338206B2 (en) 2019-02-21 2025-06-24 Nanjing Ruijie Pharma Co., Ltd. Compounds and their uses as thyroid hormone receptor agonists
GEP20247637B (en) 2019-05-08 2024-06-25 Aligos Therapeutics Inc Modulators of thr-b and methods of use thereof
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
US12595254B2 (en) 2020-09-10 2026-04-07 Crystal Pharmaceutical (Suzhou) Co., Ltd. Crystal form of Resmetirom, preparation method therefor, and use thereof
WO2022086894A1 (en) 2020-10-19 2022-04-28 Teva Pharmaceuticals International Gmbh Solid state forms of resmetirom
KR20230142523A (ko) * 2021-02-01 2023-10-11 마드리갈 파마슈티칼스, 인크. 간 장애 또는 지질 장애의 치료를 위한 로수바스타틴 및 레스메티롬의 치료용 조합
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
WO2022225827A1 (en) * 2021-04-21 2022-10-27 Merck Sharp & Dohme Llc Novel forms of cyclic dinucleotide compounds
JP2024544538A (ja) * 2021-11-11 2024-12-03 ターンズ・ファーマシューティカルズ・インコーポレイテッド ＴＨＲ－βアゴニストによる肝障害の治療
WO2024263714A1 (en) 2023-06-22 2024-12-26 Madrigal Pharmaceuticals, Inc. BIOMARKERS FOR TREATING LIVER DISORDERS WITH THR-β 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
WO2026074443A1 (en) 2024-10-01 2026-04-09 Assia Chemical Industries Ltd. Solid state forms of resmetirom

Citations (3)

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

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001051919A2 (en) * 2000-01-07 2001-07-19 Transform Pharmaceuticals, Inc. High-throughput formation, identification, and analysis of diverse solid-forms

Patent Citations (3)

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

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
ABU T. M. SERAJUDDIN等: "Solid Dispersion of Poorly Water-Soluble Drugs: Early Promises,Subsequent Problems, and Recent Breakthroughs" *
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" *
MINO R. CAIRA等: "Crystalline Polymorphism of Organic Compounds" *
ROLF HILFIKER等: "Relevance of Solid-state Properties for Pharmaceutical Products" *

Cited By (4)

* 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
WO2026067708A1 (zh) * 2024-09-30 2026-04-02 齐鲁制药有限公司 瑞司美替罗晶型及其制备方法和用途

Also Published As

Publication number Publication date
US20250074898A1 (en) 2025-03-06
AU2025200189A1 (en) 2025-01-30
IL279700A (en) 2021-03-01
TW202019914A (zh) 2020-06-01
JP2024105460A (ja) 2024-08-06
WO2020010068A1 (en) 2020-01-09
MX2021000107A (es) 2021-05-27
JP2021530456A (ja) 2021-11-11
EP3818057A1 (en) 2021-05-12
EP4552643A3 (en) 2025-07-02
MX2023009701A (es) 2023-08-29
US20250368626A1 (en) 2025-12-04
AU2019298236A1 (en) 2021-01-21
KR102890565B1 (ko) 2025-11-24
IL321116A (en) 2025-07-01
CA3104860A1 (en) 2020-01-09
US20210122740A1 (en) 2021-04-29
KR20250167140A (ko) 2025-11-28
KR20210027454A (ko) 2021-03-10
AR115666A1 (es) 2021-02-10
EP4552643A2 (en) 2025-05-14
MX2024013198A (es) 2024-12-06

Similar Documents

Publication Publication Date Title
CN112638904A (zh) 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
EP3453703A1 (en) Crystalline form e of tafamidis methylglucamine salt, and preparation method and application thereof
US20250388550A1 (en) Salts of an antioxidant and crystalline forms thereof
JP2021512910A (ja) ノボビオシン類似体とプロリンとの共結晶形態
CN111918859B (zh) 稠合三环γ-氨基酸衍生物的盐的晶型及制备和应用
US8946474B2 (en) Polymorphic form of a calcimimetic compound
US11136332B2 (en) Morphic forms of marizomib and uses thereof
AU2025200217A1 (en) Systems and methods for preparing tailored radioactive isotope solutions
EP4444720A1 (en) Rabeximod compounds
EP3941588A1 (en) Co-crystal forms of selinexor
US9056814B2 (en) Polymorphic form of a calcimimetic compound
JP7813100B2 (ja) ４－フェニルチアゾール誘導体の結晶形およびその調製方法
HK40119275A (zh) 新生霉素类似物与脯氨酸的共晶体形式
CN112384221A (zh) 异喹啉酮的多晶态和非晶态形式及其使用方法

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20210409

WD01 Invention patent application deemed withdrawn after publication