IL314360B2 - Method for the synthesis of thyroid hormone analogs and their polymorphs - Google Patents
Method for the synthesis of thyroid hormone analogs and their polymorphsInfo
- Publication number
- IL314360B2 IL314360B2 IL314360A IL31436024A IL314360B2 IL 314360 B2 IL314360 B2 IL 314360B2 IL 314360 A IL314360 A IL 314360A IL 31436024 A IL31436024 A IL 31436024A IL 314360 B2 IL314360 B2 IL 314360B2
- Authority
- IL
- Israel
- Prior art keywords
- compound
- use according
- pharmaceutical composition
- subject
- administered
- Prior art date
Links
Classifications
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
-
- 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
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings 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
- C07D237/14—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings 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
- C07D237/14—Oxygen atoms
- C07D237/16—Two oxygen atoms
-
- 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
-
- 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
-
- 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
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicinal Preparation (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261702137P | 2012-09-17 | 2012-09-17 | |
| US201361790432P | 2013-03-15 | 2013-03-15 | |
| PCT/US2013/060177 WO2014043706A1 (en) | 2012-09-17 | 2013-09-17 | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| IL314360A IL314360A (en) | 2024-09-01 |
| IL314360B1 IL314360B1 (en) | 2025-05-01 |
| IL314360B2 true IL314360B2 (en) | 2025-09-01 |
Family
ID=50278769
Family Applications (7)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL314360A IL314360B2 (en) | 2012-09-17 | 2013-09-17 | Method for the synthesis of thyroid hormone analogs and their polymorphs |
| IL288133A IL288133B2 (en) | 2012-09-17 | 2013-09-17 | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
| IL320269A IL320269A (en) | 2012-09-17 | 2013-09-17 | Method for the synthesis of thyroid hormone analogs and their polymorphs |
| IL237628A IL237628B (en) | 2012-09-17 | 2015-03-09 | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
| IL259610A IL259610B (en) | 2012-09-17 | 2018-05-27 | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
| IL265030A IL265030B (en) | 2012-09-17 | 2019-02-25 | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
| IL275393A IL275393B (en) | 2012-09-17 | 2020-06-15 | A method for synthesizing thyroid hormone analogs and their polymorphs |
Family Applications After (6)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL288133A IL288133B2 (en) | 2012-09-17 | 2013-09-17 | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
| IL320269A IL320269A (en) | 2012-09-17 | 2013-09-17 | Method for the synthesis of thyroid hormone analogs and their polymorphs |
| IL237628A IL237628B (en) | 2012-09-17 | 2015-03-09 | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
| IL259610A IL259610B (en) | 2012-09-17 | 2018-05-27 | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
| IL265030A IL265030B (en) | 2012-09-17 | 2019-02-25 | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
| IL275393A IL275393B (en) | 2012-09-17 | 2020-06-15 | A method for synthesizing thyroid hormone analogs and their polymorphs |
Country Status (32)
Families Citing this family (49)
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| ES2795450T3 (es) * | 2012-09-17 | 2020-11-23 | Madrigal Pharmaceuticals Inc | Procedimiento para sintetizar análogos de hormonas tiroideas y polimorfos de los mismos |
| MX394463B (es) * | 2016-10-18 | 2025-03-19 | Madrigal Pharmaceuticals Inc | Métodos para tratar trastornos del hígado o trastornos lipídicos con un agonista de thr-beta. |
| 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 |
| ES3029158T3 (en) | 2018-06-12 | 2025-06-23 | Xizang Haisco Pharmaceutical Co Ltd | Thyroid hormone receptor agonists and uses thereof |
| US20210292304A1 (en) * | 2018-06-22 | 2021-09-23 | Hinova Pharmaceuticals Inc. | Deuterated mgl-3196 compound and use thereof |
| TW202615431A (zh) * | 2018-07-02 | 2026-04-16 | 美商瑪德瑞高製藥公司 | ２－（３，５－二氯－４－（（５－異丙基－６－側氧基－１，６－二氫噠嗪－３－基）氧）苯基）－３，５－二側氧基－２，３，４，５－四氫－１，２，４－三嗪－６－腈之固體型式 |
| CN119552152A (zh) * | 2018-10-12 | 2025-03-04 | 益方生物科技(上海)股份有限公司 | 甲状腺激素受体激动剂 |
| EP4775207A2 (en) | 2018-12-05 | 2026-07-15 | Viking Therapeutics, Inc. | Compositions for the treatment of fibrosis |
| CN121081472A (zh) | 2018-12-13 | 2025-12-09 | 拓臻股份有限公司 | 一种THRβ受体激动剂化合物及其制备方法和用途 |
| CN119431265A (zh) | 2019-02-21 | 2025-02-14 | 南京瑞捷医药科技有限公司 | 一种作为甲状腺激素受体激动剂的化合物 |
| WO2020227549A1 (en) * | 2019-05-08 | 2020-11-12 | Aligos Therapeutics, Inc. | MODULATORS OF THR-β AND METHODS OF USE THEREOF |
| WO2020228577A1 (zh) * | 2019-05-10 | 2020-11-19 | 深圳微芯生物科技股份有限公司 | 一种哒嗪酮衍生物及其应用 |
| WO2020239076A1 (zh) * | 2019-05-29 | 2020-12-03 | 南京明德新药研发有限公司 | 作为甲状腺素受体-β激动剂的哒嗪酮类衍生物及其应用 |
| CA3154488A1 (en) | 2019-08-23 | 2021-03-04 | Terns Pharmaceuticals, Inc. | Thyroid hormone receptor beta agonist compounds |
| CN112442013B (zh) * | 2019-09-04 | 2022-07-26 | 广东东阳光药业有限公司 | 一种作为甲状腺激素β受体激动剂的化合物及其用途 |
| CA3154391A1 (en) | 2019-09-12 | 2021-03-18 | Terns Pharmaceuticals, Inc. | Thyroid hormone receptor beta agonist compounds |
| 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 |
| CN112707892A (zh) * | 2019-10-24 | 2021-04-27 | 苏州泽璟生物制药股份有限公司 | 哒嗪酮或哒嗪类化合物及其衍生物和药物组合物 |
| CA3158379A1 (en) * | 2019-11-26 | 2021-06-03 | Hejun Lv | 1,2,4-triazine-3,5-dione compound, preparation method therefor, and application thereof |
| WO2021121210A1 (zh) * | 2019-12-16 | 2021-06-24 | 江苏恒瑞医药股份有限公司 | 并环类衍生物、其制备方法及其在医药上的应用 |
| 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 |
| WO2022041026A1 (en) * | 2020-08-27 | 2022-03-03 | InventisBio Co., Ltd. | Pyridazinone compounds |
| KR20230066408A (ko) * | 2020-09-10 | 2023-05-15 | 크리스탈 파마슈티컬 (쑤저우) 씨오., 엘티디. | 레스메티롬의 결정형, 이의 제조 방법 및 이의 용도 |
| US12616701B2 (en) | 2020-10-19 | 2026-05-05 | Assia Chemical Industries Ltd | Solid state forms of Resmetirom |
| CN114437042A (zh) * | 2020-11-03 | 2022-05-06 | 深圳微芯生物科技股份有限公司 | 酞嗪类化合物的晶型及其制备方法 |
| CN114437034A (zh) * | 2020-11-06 | 2022-05-06 | 深圳微芯生物科技股份有限公司 | 一种酞嗪类化合物的可药用盐、晶型及其制备方法 |
| WO2022165227A1 (en) | 2021-02-01 | 2022-08-04 | Madrigal Pharmaceuticals, Inc. | Therapeutic combinations of rosuvastatin and resmetirom for the treatment of liver disorders or lipid disorders |
| 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 |
| CN115073429A (zh) * | 2021-03-15 | 2022-09-20 | 昆药集团股份有限公司 | 一种1，2，4-三嗪-3，5-二酮类化合物的盐型、晶型及其制备方法 |
| TW202337470A (zh) | 2021-09-27 | 2023-10-01 | 美商瑪德瑞高製藥公司 | 用於縮減肝臟體積之瑞美替隆 |
| WO2024165571A2 (en) | 2023-02-06 | 2024-08-15 | E-Therapeutics Plc | Inhibitors of expression and/or function |
| PE20252787A1 (es) | 2023-04-07 | 2025-12-22 | Terns Pharmaceuticals Inc | Combinacion que comprende un agonista de thr-beta y un agonista de glp-1r para su uso en el tratamiento de un trastorno hepatico o una enfermedad cardiometabolica |
| CN116768802B (zh) * | 2023-05-25 | 2025-11-21 | 杭州科巢生物科技有限公司 | 一种瑞司美替罗的合成方法 |
| JP2026521649A (ja) | 2023-06-22 | 2026-06-30 | 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 | ＴＨＲ－βアゴニストを用いて肝障害を治療するためのバイオマーカーおよび関連する使用 |
| 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 |
| CN117263870B (zh) * | 2023-09-21 | 2026-02-06 | 江西同和药业股份有限公司 | 一种Resmetirom关键中间体III的制备方法 |
| EP4762048A2 (en) | 2023-10-16 | 2026-06-24 | Cipla Limited | Resmetirom polymorphs and process for their preparation |
| WO2025125576A2 (en) | 2023-12-15 | 2025-06-19 | E-Therapeutics Plc | Inhibitors of expression and/or function |
| EP4686757A1 (en) | 2024-07-31 | 2026-02-04 | e-therapeutics PLC | Inhibitors of expression and/or function |
| AU2024408289A1 (en) | 2023-12-22 | 2026-08-06 | Tangram Therapeutics Plc | Inhibitors of expression and/or function |
| WO2025164161A1 (ja) * | 2024-01-29 | 2025-08-07 | シオノギファーマ株式会社 | カンナビジオールの溶媒和物及びカンナビジオールの精製方法 |
| US12377104B1 (en) | 2024-02-06 | 2025-08-05 | Madrigal Pharmaceuticals, Inc. | Methods for treating a fatty liver disease |
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| CN119019375A (zh) * | 2024-08-14 | 2024-11-26 | 奥锐特药业(天津)有限公司 | 一种瑞司美替罗新晶型及其制备方法 |
| 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 |
| WO2026074443A1 (en) | 2024-10-01 | 2026-04-09 | Assia Chemical Industries Ltd. | Solid state forms of resmetirom |
| CN119306670A (zh) * | 2024-10-12 | 2025-01-14 | 北京海美桐医药科技有限公司 | 瑞司美替罗中间体、其合成方法和瑞司美替罗的合成方法 |
| WO2026107045A1 (en) | 2024-11-12 | 2026-05-21 | Madrigal Pharmaceuticals, Inc. | Resmetirom for use in treating cardiomyopathy and/or related heart failure and portal hypertension |
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| TW202615431A (zh) | 2018-07-02 | 2026-04-16 | 美商瑪德瑞高製藥公司 | ２－（３，５－二氯－４－（（５－異丙基－６－側氧基－１，６－二氫噠嗪－３－基）氧）苯基）－３，５－二側氧基－２，３，４，５－四氫－１，２，４－三嗪－６－腈之固體型式 |
| CN119552152A (zh) | 2018-10-12 | 2025-03-04 | 益方生物科技(上海)股份有限公司 | 甲状腺激素受体激动剂 |
| CN121081472A (zh) | 2018-12-13 | 2025-12-09 | 拓臻股份有限公司 | 一种THRβ受体激动剂化合物及其制备方法和用途 |
-
2013
- 2013-09-17 ES ES13837402T patent/ES2795450T3/es active Active
- 2013-09-17 IL IL314360A patent/IL314360B2/en unknown
- 2013-09-17 DK DK20157696.4T patent/DK3689853T3/da active
- 2013-09-17 SI SI201332113T patent/SI4406594T1/sl unknown
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