SG10201705984XA - Method of synthesizing thyroid hormone analogs and polymorphs thereof - Google Patents
Method of synthesizing thyroid hormone analogs and polymorphs thereofInfo
- Publication number
- SG10201705984XA SG10201705984XA SG10201705984XA SG10201705984XA SG10201705984XA SG 10201705984X A SG10201705984X A SG 10201705984XA SG 10201705984X A SG10201705984X A SG 10201705984XA SG 10201705984X A SG10201705984X A SG 10201705984XA SG 10201705984X A SG10201705984X A SG 10201705984XA
- Authority
- SG
- Singapore
- Prior art keywords
- polymorphs
- thyroid hormone
- hormone analogs
- synthesizing
- synthesizing thyroid
- Prior art date
Links
Classifications
-
- 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
-
- 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
- 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)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Endocrinology (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)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Medicinal Preparation (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 (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261702137P | 2012-09-17 | 2012-09-17 | |
| US201361790432P | 2013-03-15 | 2013-03-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG10201705984XA true SG10201705984XA (en) | 2017-08-30 |
Family
ID=50278769
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG10201705984XA SG10201705984XA (en) | 2012-09-17 | 2013-09-17 | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
| SG10202006058QA SG10202006058QA (en) | 2012-09-17 | 2013-09-17 | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
| SG11201501907YA SG11201501907YA (en) | 2012-09-17 | 2013-09-17 | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG10202006058QA SG10202006058QA (en) | 2012-09-17 | 2013-09-17 | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
| SG11201501907YA SG11201501907YA (en) | 2012-09-17 | 2013-09-17 | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
Country Status (23)
| Country | Link |
|---|---|
| US (8) | US9266861B2 (en) |
| EP (4) | EP3689853B1 (en) |
| JP (8) | JP6616688B2 (en) |
| KR (4) | KR102138750B1 (en) |
| CN (2) | CN108101851A (en) |
| AR (1) | AR092872A1 (en) |
| AU (1) | AU2013315017C1 (en) |
| BR (2) | BR122021024202B1 (en) |
| CA (3) | CA3111317C (en) |
| DK (3) | DK2895466T3 (en) |
| ES (2) | ES2795450T3 (en) |
| FI (1) | FI4406594T3 (en) |
| IL (7) | IL320269A (en) |
| IN (1) | IN2015DN03133A (en) |
| MX (2) | MX395148B (en) |
| MY (1) | MY170520A (en) |
| NZ (2) | NZ705827A (en) |
| PT (1) | PT4406594T (en) |
| RU (2) | RU2668960C2 (en) |
| SG (3) | SG10201705984XA (en) |
| TW (4) | TWI804870B (en) |
| WO (1) | WO2014043706A1 (en) |
| ZA (1) | ZA201501795B (en) |
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| CA3111317C (en) | 2012-09-17 | 2023-08-29 | F. Hoffmann-La Roche Ltd. | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
| AU2017346871B2 (en) | 2016-10-18 | 2023-08-03 | Madrigal Pharmaceuticals, Inc. | Methods of treating liver disorders or lipid disorders with a THR-beta agonist |
| CN109574995B (en) * | 2018-01-23 | 2020-07-24 | 深圳市塔吉瑞生物医药有限公司 | Substituted pyridazinone compounds |
| US11964964B2 (en) | 2018-06-12 | 2024-04-23 | 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 |
| TW202019914A (en) * | 2018-07-02 | 2020-06-01 | 美商瑪德瑞高製藥公司 | 2-(3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)-3,5-di Solid type of pendant-2,3,4,5-tetrahydro-1,2,4-triazine-6-nitrile |
| AU2019359141A1 (en) | 2018-10-12 | 2021-04-22 | InventisBio Co., Ltd. | Thyroid hormone receptor agonists |
| CN121081472A (en) | 2018-12-13 | 2025-12-09 | 拓臻股份有限公司 | THR beta receptor agonist compound and preparation method and application thereof |
| EP3927693A4 (en) * | 2019-02-21 | 2023-04-05 | Nanjing Ruijie Pharma Co., Ltd. | NOVEL COMPOUNDS AND THEIR USES AS THYROID HORMONE RECEPTOR AGONISTS |
| AU2020267576B2 (en) | 2019-05-08 | 2025-03-13 | Aligos Therapeutics, Inc. | Modulators of THR-β and methods of use thereof |
| WO2020228577A1 (en) * | 2019-05-10 | 2020-11-19 | 深圳微芯生物科技股份有限公司 | Pyridazinone derivative and use thereof |
| CN114174282A (en) * | 2019-05-29 | 2022-03-11 | 南京明德新药研发有限公司 | Pyridazinone derivatives as thyroxine receptor-beta agonists and uses thereof |
| WO2021043185A1 (en) * | 2019-09-04 | 2021-03-11 | Sunshine Lake Pharma Co., Ltd. | A compound as a thyroid hormone beta receptor agonist and use thereof |
| CA3154391A1 (en) | 2019-09-12 | 2021-03-18 | Terns Pharmaceuticals, Inc. | Thyroid hormone receptor beta agonist compounds |
| WO2021063367A1 (en) * | 2019-09-30 | 2021-04-08 | 苏州科睿思制药有限公司 | Resmetirom crystal form and preparation method therefor and use thereof |
| CN112707892A (en) * | 2019-10-24 | 2021-04-27 | 苏州泽璟生物制药股份有限公司 | Pyridazinone or pyridazine compound and derivative and pharmaceutical composition thereof |
| 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 (en) * | 2019-12-16 | 2021-06-24 | 江苏恒瑞医药股份有限公司 | Fused-ring derivative, and preparation method therefor and medical use thereof |
| WO2021129465A1 (en) * | 2019-12-26 | 2021-07-01 | 苏州科睿思制药有限公司 | Resmetirom crystal, preparation method for same, and uses thereof |
| US20230339911A1 (en) * | 2020-08-27 | 2023-10-26 | InventisBio Co., Ltd. | Pyridazinone compounds |
| EP4286377A4 (en) * | 2020-09-10 | 2024-10-09 | Crystal Pharmaceutical (Suzhou) Co., Ltd. | CRYSTAL FORM OF RESMETIROM, PRODUCTION PROCESS THEREOF AND USE THEREOF |
| WO2022086894A1 (en) | 2020-10-19 | 2022-04-28 | Teva Pharmaceuticals International Gmbh | Solid state forms of resmetirom |
| CN114437042A (en) * | 2020-11-03 | 2022-05-06 | 深圳微芯生物科技股份有限公司 | Crystal form of phthalazine compound and preparation method thereof |
| CN114437034A (en) * | 2020-11-06 | 2022-05-06 | 深圳微芯生物科技股份有限公司 | Pharmaceutical salt and crystal form of phthalazine compound and preparation method thereof |
| EP4284373A1 (en) * | 2021-02-01 | 2023-12-06 | Madrigal Pharmaceuticals, Inc. | Therapeutic combinations of rosuvastatin and resmetirom for the treatment of liver disorders or lipid disorders |
| CN114907327A (en) * | 2021-02-10 | 2022-08-16 | 杭州领业医药科技有限公司 | Crystal form of Resmetirom and preparation method and application thereof |
| CN115073429A (en) * | 2021-03-15 | 2022-09-20 | 昆药集团股份有限公司 | Salt form and crystal form of 1,2, 4-triazine-3, 5-diketone compound and preparation method thereof |
| MX2024003967A (en) | 2021-09-27 | 2024-06-03 | Madrigal Pharmaceuticals Inc | Resmetirom for reducing liver volume. |
| WO2024165571A2 (en) | 2023-02-06 | 2024-08-15 | E-Therapeutics Plc | Inhibitors of expression and/or function |
| KR20250166323A (en) | 2023-04-07 | 2025-11-27 | 테른스 파마슈티칼스, 인크. | A combination comprising a THR beta agonist and a GLP-1R agonist for use in the treatment of liver disorders or cardiometabolic diseases |
| CN116768802B (en) * | 2023-05-25 | 2025-11-21 | 杭州科巢生物科技有限公司 | Rasemet-teh Synthesis method of roxburgh |
| WO2024263714A1 (en) | 2023-06-22 | 2024-12-26 | Madrigal Pharmaceuticals, Inc. | BIOMARKERS FOR TREATING LIVER DISORDERS WITH THR-β AGONISTS AND RELATED USES |
| CN119613386A (en) * | 2023-09-14 | 2025-03-14 | 杭州科巢生物科技有限公司 | Ralset tilobal 1, 4-dioxane solvent compound and preparation method thereof |
| CN117263870A (en) * | 2023-09-21 | 2023-12-22 | 江西同和药业股份有限公司 | Preparation method of Resmetirom key intermediate III |
| WO2025083699A2 (en) | 2023-10-16 | 2025-04-24 | Cipla Limited | Resmetirom polymorphs and process thereof |
| WO2025125576A2 (en) | 2023-12-15 | 2025-06-19 | E-Therapeutics Plc | Inhibitors of expression and/or function |
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| US11964964B2 (en) | 2018-06-12 | 2024-04-23 | Xizang Haisco Pharmaceutical Co., Ltd. | Thyroid hormone receptor agonists and uses thereof |
| TW202019914A (en) | 2018-07-02 | 2020-06-01 | 美商瑪德瑞高製藥公司 | 2-(3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)-3,5-di Solid type of pendant-2,3,4,5-tetrahydro-1,2,4-triazine-6-nitrile |
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2013
- 2013-09-17 CA CA3111317A patent/CA3111317C/en active Active
- 2013-09-17 KR KR1020187034908A patent/KR102138750B1/en active Active
- 2013-09-17 MX MX2018014924A patent/MX395148B/en unknown
- 2013-09-17 KR KR1020217019940A patent/KR102363776B1/en active Active
- 2013-09-17 AU AU2013315017A patent/AU2013315017C1/en active Active
- 2013-09-17 KR KR1020157009807A patent/KR101966490B1/en active Active
- 2013-09-17 EP EP20157696.4A patent/EP3689853B1/en active Active
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- 2013-09-17 RU RU2015114327A patent/RU2668960C2/en active
- 2013-09-17 TW TW110117935A patent/TWI804870B/en active
- 2013-09-17 DK DK13837402.0T patent/DK2895466T3/en active
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- 2013-09-17 CN CN201810077707.0A patent/CN108101851A/en active Pending
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- 2013-09-17 WO PCT/US2013/060177 patent/WO2014043706A1/en not_active Ceased
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- 2013-09-17 EP EP24173563.8A patent/EP4406594B1/en active Active
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- 2013-09-17 MY MYPI2015000591A patent/MY170520A/en unknown
- 2013-09-17 CN CN201380059943.5A patent/CN105008335B/en active Active
- 2013-09-17 EP EP21209827.1A patent/EP4023641B1/en active Active
- 2013-09-17 SG SG11201501907YA patent/SG11201501907YA/en unknown
- 2013-09-17 PT PT241735638T patent/PT4406594T/en unknown
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- 2013-09-17 BR BR112015005891A patent/BR112015005891A2/en not_active Application Discontinuation
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2015
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2016
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