JP7574223B2 - THR-βの調節物質およびその使用方法 - Google Patents
THR-βの調節物質およびその使用方法 Download PDFInfo
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- JP7574223B2 JP7574223B2 JP2021566558A JP2021566558A JP7574223B2 JP 7574223 B2 JP7574223 B2 JP 7574223B2 JP 2021566558 A JP2021566558 A JP 2021566558A JP 2021566558 A JP2021566558 A JP 2021566558A JP 7574223 B2 JP7574223 B2 JP 7574223B2
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- 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
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- 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
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- 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
- A61P3/04—Anorexiants; Antiobesity agents
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- 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
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- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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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
- C07D403/10—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 carbon chain containing aromatic rings
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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
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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
- C07D403/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Peptides Or Proteins (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Crystals, And After-Treatments Of Crystals (AREA)
- Optical Modulation, Optical Deflection, Nonlinear Optics, Optical Demodulation, Optical Logic Elements (AREA)
- Magnetic Resonance Imaging Apparatus (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024180616A JP7844578B2 (ja) | 2019-05-08 | 2024-10-16 | THR-βの調節物質およびその使用方法 |
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962845252P | 2019-05-08 | 2019-05-08 | |
| US62/845,252 | 2019-05-08 | ||
| US201962944052P | 2019-12-05 | 2019-12-05 | |
| US62/944,052 | 2019-12-05 | ||
| US202063005661P | 2020-04-06 | 2020-04-06 | |
| US63/005,661 | 2020-04-06 | ||
| PCT/US2020/031904 WO2020227549A1 (en) | 2019-05-08 | 2020-05-07 | MODULATORS OF THR-β AND METHODS OF USE THEREOF |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024180616A Division JP7844578B2 (ja) | 2019-05-08 | 2024-10-16 | THR-βの調節物質およびその使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022532706A JP2022532706A (ja) | 2022-07-19 |
| JP2022532706A5 JP2022532706A5 (https=) | 2023-05-12 |
| JP7574223B2 true JP7574223B2 (ja) | 2024-10-28 |
Family
ID=70919081
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021566558A Active JP7574223B2 (ja) | 2019-05-08 | 2020-05-07 | THR-βの調節物質およびその使用方法 |
| JP2024180616A Active JP7844578B2 (ja) | 2019-05-08 | 2024-10-16 | THR-βの調節物質およびその使用方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024180616A Active JP7844578B2 (ja) | 2019-05-08 | 2024-10-16 | THR-βの調節物質およびその使用方法 |
Country Status (32)
| Country | Link |
|---|---|
| US (3) | US11091467B2 (https=) |
| EP (2) | EP3965884B1 (https=) |
| JP (2) | JP7574223B2 (https=) |
| KR (1) | KR20220017917A (https=) |
| CN (1) | CN114096531B (https=) |
| AU (1) | AU2020267576B2 (https=) |
| BR (1) | BR112021021718A2 (https=) |
| CA (1) | CA3139101A1 (https=) |
| CL (1) | CL2021002883A1 (https=) |
| CO (1) | CO2021015698A2 (https=) |
| DK (1) | DK3965884T3 (https=) |
| ES (1) | ES3020290T3 (https=) |
| FI (1) | FI3965884T3 (https=) |
| GE (2) | GEP20247637B (https=) |
| HR (1) | HRP20250384T1 (https=) |
| HU (1) | HUE070650T2 (https=) |
| IL (1) | IL287720A (https=) |
| LT (1) | LT3965884T (https=) |
| MA (1) | MA55890B1 (https=) |
| MD (1) | MD3965884T2 (https=) |
| MX (1) | MX2021013472A (https=) |
| MY (1) | MY210357A (https=) |
| PE (1) | PE20220255A1 (https=) |
| PH (1) | PH12021552782A1 (https=) |
| PL (1) | PL3965884T3 (https=) |
| PT (1) | PT3965884T (https=) |
| RS (1) | RS66686B1 (https=) |
| SG (1) | SG11202111552YA (https=) |
| SI (1) | SI3965884T1 (https=) |
| TW (1) | TWI855068B (https=) |
| WO (1) | WO2020227549A1 (https=) |
| ZA (1) | ZA202409114B (https=) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN111320609A (zh) | 2018-12-13 | 2020-06-23 | 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 |
| KR20220017917A (ko) * | 2019-05-08 | 2022-02-14 | 알리고스 테라퓨틱스 인코포레이티드 | Thr-베타의 조절제 및 이의 사용 방법 |
| AU2020336272A1 (en) * | 2019-08-23 | 2022-04-14 | Terns Pharmaceuticals, Inc. | Thyroid hormone receptor beta agonist compounds |
| WO2021050945A1 (en) | 2019-09-12 | 2021-03-18 | Terns, Inc. | Thyroid hormone receptor beta agonist compounds |
| WO2021104288A1 (zh) * | 2019-11-26 | 2021-06-03 | 昆药集团股份有限公司 | 1,2,4-三嗪-3,5-二酮类化合物及其制备方法和应用 |
| 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 |
| CN113278013B (zh) * | 2020-02-20 | 2022-09-23 | 昆药集团股份有限公司 | 2,6-二取代的1,2,4-三嗪-3,5-二酮化合物及其制备方法和应用 |
| US20230257367A1 (en) * | 2020-06-02 | 2023-08-17 | Chengdu Kanghong Pharmaceutical Co., Ltd. | Novel thyroid hormone beta receptor agonist |
| WO2021257851A1 (en) | 2020-06-17 | 2021-12-23 | Autobahn Therapeutics, Inc. | Thyromimetics |
| US12590072B2 (en) | 2020-06-17 | 2026-03-31 | Autobahn Therapeutics, Inc. | Thyromimetics |
| WO2022053028A1 (zh) * | 2020-09-10 | 2022-03-17 | 南京明德新药研发有限公司 | 1,2,4-三嗪-3,5(2h,4h)-二酮类化合物及其应用 |
| WO2022052822A1 (zh) * | 2020-09-10 | 2022-03-17 | 苏州科睿思制药有限公司 | Resmetirom的晶型及其制备方法和用途 |
| CA3192169A1 (en) * | 2020-09-17 | 2022-03-24 | Sunshine Lake Pharma Co., Ltd. | A compound as a thyroid hormone beta receptor agonist and use thereof |
| AU2021373043A1 (en) * | 2020-11-06 | 2023-06-15 | Aligos Therapeutics, Inc. | Oxindoles and methods of use thereof |
| JP2023551782A (ja) * | 2020-11-06 | 2023-12-13 | アリゴス セラピューティクス,インコーポレーテッド | 甲状腺受容体アゴニストとしてのピリダジノン誘導体、及びその使用 |
| CN114591300A (zh) * | 2020-12-04 | 2022-06-07 | 南京圣和药业股份有限公司 | 作为THRβ激动剂的杂环化合物及其应用 |
| CN112645936B (zh) * | 2020-12-17 | 2022-03-01 | 山东第一医科大学(山东省医学科学院) | 取代的哒嗪酮类化合物及其用途 |
| CN114685450A (zh) * | 2020-12-30 | 2022-07-01 | 昆药集团股份有限公司 | 2-吡啶酮类衍生物及其制备方法和在医药上的应用 |
| 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 |
| PE20240097A1 (es) * | 2021-03-03 | 2024-01-18 | Terns Pharmaceuticals Inc | Compuestos agonistas beta del receptor de la hormona tiroidea |
| CA3210814A1 (en) * | 2021-03-04 | 2022-09-09 | Xiaokun SHEN | Aromatic compound, preparation method therefor, and application thereof |
| 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 |
| CN117279911B (zh) * | 2021-05-21 | 2025-07-08 | 深圳微芯生物科技股份有限公司 | 一种杂环化合物及其应用 |
| WO2023023474A1 (en) * | 2021-08-16 | 2023-02-23 | Senya Pharmaceuticals, Inc. | Tr-beta modulators, pharmaceutical compositions, and therapeutic applications |
| US20250243491A1 (en) | 2021-09-01 | 2025-07-31 | Aligos Therapeutics, Inc. | Pnpla3-targeting short interfering rna (sirna) molecules and uses thereof |
| CN118234862A (zh) | 2021-09-08 | 2024-06-21 | 阿利戈斯治疗公司 | 经修饰的短干扰核酸分子(siNA)及其用途 |
| TWI910297B (zh) * | 2021-12-24 | 2026-01-01 | 大陸商廣東東陽光藥業股份有限公司 | 一種作為甲狀腺激素β受體激動劑的化合物及其用途 |
| CN116354934A (zh) * | 2021-12-28 | 2023-06-30 | 中国科学院上海药物研究所 | 一类喹啉类化合物及其制备方法、药物组合物和用途 |
| CN115650928B (zh) * | 2022-12-28 | 2023-03-31 | 凯思凯旭(上海)医药科技有限公司 | 一种多环类甲状腺激素β受体激动剂及其用途 |
| WO2024182446A2 (en) | 2023-02-28 | 2024-09-06 | Aligos Therapeutics, Inc. | Pnpla3-targeting short interfering rna (sirna) molecules and uses thereof |
| US20240352464A1 (en) | 2023-03-07 | 2024-10-24 | Aligos Therapeutics, Inc. | Modified Short Interfering Nucleic Acid (siNA) Molecules and Uses Thereof |
| EP4568664B1 (en) | 2023-04-07 | 2026-04-01 | Terns Pharmaceuticals, Inc. | Combination comprising a thr-beta agonist and a glp-1r agonist for use in treating obesity |
| CN121358734A (zh) * | 2023-06-19 | 2026-01-16 | 西威埃医药技术(上海)有限公司 | THR-β受体激动剂、其制备方法和其使用方法 |
| 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 |
| CN117327057B (zh) * | 2023-08-30 | 2026-03-03 | 南京雷正医药科技有限公司 | 一类作为甲状腺激素受体激动剂的三嗪二酮类化合物及其合成、用途 |
| US20250206725A1 (en) * | 2023-12-21 | 2025-06-26 | Aligos Therapeutics, Inc. | Modulators of thr-beta and methods of use thereof |
| WO2025230749A1 (en) | 2024-05-03 | 2025-11-06 | Aligos Therapeutics, Inc. | Methods of preparing 6-amino-2-[3,5-dichloro-4-[(5-isopropyl-6-oxo-1 h-pyridazin-3-yl)oxy]phenyl]-4h- 1, 2, 4-tri-azine-3, 5-dione |
| WO2025252147A1 (zh) * | 2024-06-07 | 2025-12-11 | 珠海联邦制药股份有限公司 | 一种甲状腺激素β受体激动剂的化合物及其应用 |
| WO2026050911A1 (zh) * | 2024-09-04 | 2026-03-12 | 西威埃医药技术(上海)有限公司 | 一种TR-β选择性激动剂的晶型、制备方法和应用 |
| WO2026067791A1 (en) | 2024-09-30 | 2026-04-02 | Ascletis Pharma (China) Co., Limited | 2-phenyl-1,2,4-triazine-3,5(2h,4h)-dione derivatives as thr-beta agonist or modulators for the treatment of obesity |
| US20260102403A1 (en) * | 2024-10-11 | 2026-04-16 | Aligos Therapeutics, Inc. | Oral formulations of thr-beta agonist |
| CN120923503A (zh) * | 2025-10-10 | 2025-11-11 | 吉斯凯(苏州)制药有限公司 | 具有杂环结构的化合物、THRβ受体激动剂及用途 |
Citations (4)
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| JP2009501759A (ja) | 2005-07-21 | 2009-01-22 | エフ.ホフマン−ラ ロシュ アーゲー | 甲状腺ホルモン受容体アゴニストとしてのピリダジノン誘導体 |
| WO2010122980A1 (ja) | 2009-04-20 | 2010-10-28 | 田辺三菱製薬株式会社 | 新規甲状腺ホルモンβ受容体作動薬 |
| JP2010539209A (ja) | 2007-09-20 | 2010-12-16 | エフ.ホフマン−ラ ロシュ アーゲー | 甲状腺ホルモンアナログのプロドラッグ |
| 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 |
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