TWI755628B - 用以合成甲狀腺激素類似物及其多形體之方法 - Google Patents
用以合成甲狀腺激素類似物及其多形體之方法 Download PDFInfo
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- TWI755628B TWI755628B TW108132827A TW108132827A TWI755628B TW I755628 B TWI755628 B TW I755628B TW 108132827 A TW108132827 A TW 108132827A TW 108132827 A TW108132827 A TW 108132827A TW I755628 B TWI755628 B TW I755628B
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- 0 Cc1cc(N2C(*)=CC2*)cc(Cl)c1OC(C=C1)=NNC1=O Chemical compound Cc1cc(N2C(*)=CC2*)cc(Cl)c1OC(C=C1)=NNC1=O 0.000 description 4
- OWOFTQVKAQEQCR-UHFFFAOYSA-N CC(C)C1=CC(Oc(c(Cl)cc([N]2(C)C3=C2CCC3)c2)c2Cl)=NNC1=O Chemical compound CC(C)C1=CC(Oc(c(Cl)cc([N]2(C)C3=C2CCC3)c2)c2Cl)=NNC1=O OWOFTQVKAQEQCR-UHFFFAOYSA-N 0.000 description 1
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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
- A61K31/495—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
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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
- 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
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- 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
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- 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
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- 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 (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261702137P | 2012-09-17 | 2012-09-17 | |
| US61/702,137 | 2012-09-17 | ||
| US201361790432P | 2013-03-15 | 2013-03-15 | |
| US61/790,432 | 2013-03-15 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW201946917A TW201946917A (zh) | 2019-12-16 |
| TWI755628B true TWI755628B (zh) | 2022-02-21 |
Family
ID=50278769
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW108132827A TWI755628B (zh) | 2012-09-17 | 2013-09-17 | 用以合成甲狀腺激素類似物及其多形體之方法 |
| TW110117935A TWI804870B (zh) | 2012-09-17 | 2013-09-17 | 用以合成甲狀腺激素類似物及其多形體之方法 |
| TW107137798A TWI681957B (zh) | 2012-09-17 | 2013-09-17 | 用以合成甲狀腺激素類似物及其多形體之方法 |
| TW102133687A TWI652260B (zh) | 2012-09-17 | 2013-09-17 | 用以合成甲狀腺激素類似物及其多形體之方法 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW110117935A TWI804870B (zh) | 2012-09-17 | 2013-09-17 | 用以合成甲狀腺激素類似物及其多形體之方法 |
| TW107137798A TWI681957B (zh) | 2012-09-17 | 2013-09-17 | 用以合成甲狀腺激素類似物及其多形體之方法 |
| TW102133687A TWI652260B (zh) | 2012-09-17 | 2013-09-17 | 用以合成甲狀腺激素類似物及其多形體之方法 |
Country Status (23)
| Country | Link |
|---|---|
| US (8) | US9266861B2 (enExample) |
| EP (4) | EP2895466B1 (enExample) |
| JP (8) | JP6616688B2 (enExample) |
| KR (4) | KR101966490B1 (enExample) |
| CN (2) | CN105008335B (enExample) |
| AR (1) | AR092872A1 (enExample) |
| AU (1) | AU2013315017C1 (enExample) |
| BR (2) | BR112015005891A2 (enExample) |
| CA (3) | CA3111317C (enExample) |
| DK (3) | DK3689853T3 (enExample) |
| ES (2) | ES2907926T3 (enExample) |
| FI (1) | FI4406594T3 (enExample) |
| IL (7) | IL314360B2 (enExample) |
| IN (1) | IN2015DN03133A (enExample) |
| MX (2) | MX364661B (enExample) |
| MY (1) | MY170520A (enExample) |
| NZ (2) | NZ705827A (enExample) |
| PT (1) | PT4406594T (enExample) |
| RU (2) | RU2018128393A (enExample) |
| SG (3) | SG11201501907YA (enExample) |
| TW (4) | TWI755628B (enExample) |
| WO (1) | WO2014043706A1 (enExample) |
| ZA (1) | ZA201501795B (enExample) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2907926T3 (es) | 2012-09-17 | 2022-04-27 | Madrigal Pharmaceuticals Inc | Procedimiento para sintetizar análogos de hormonas tiroideas y polimorfos de los mismos |
| IL266054B2 (en) * | 2016-10-18 | 2023-10-01 | Madrigal Pharmaceuticals Inc | Methods for treating liver disorders or lipid disorders using a THR-BETA agonist |
| CN111646979B (zh) * | 2018-01-23 | 2021-08-31 | 深圳市塔吉瑞生物医药有限公司 | 取代的哒嗪酮化合物 |
| EP3807267B1 (en) * | 2018-06-12 | 2025-03-19 | 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 (zh) * | 2018-07-02 | 2020-06-01 | 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 |
| US12391677B2 (en) | 2018-10-12 | 2025-08-19 | InventisBio Co., Ltd. | Thyroid hormone receptor agonists |
| 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 |
| WO2020169069A1 (en) | 2019-02-21 | 2020-08-27 | Nanjing Ruijie Pharma Co., Ltd. | Novel compounds and their uses as thyroid hormone receptor agonists |
| KR20220017917A (ko) * | 2019-05-08 | 2022-02-14 | 알리고스 테라퓨틱스 인코포레이티드 | Thr-베타의 조절제 및 이의 사용 방법 |
| TW202108556A (zh) * | 2019-05-10 | 2021-03-01 | 大陸商深圳微芯生物科技股份有限公司 | 一種噠嗪酮衍生物及其應用 |
| 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 |
| 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 |
| EP4028008A4 (en) | 2019-09-12 | 2023-09-13 | 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 |
| TWI763147B (zh) | 2019-11-26 | 2022-05-01 | 大陸商昆藥集團股份有限公司 | 1，2，4-三嗪-3，5-二酮類化合物及其製備方法和應用 |
| TW202128668A (zh) * | 2019-12-16 | 2021-08-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 并環類衍生物、其製備方法及其在醫藥上的應用 |
| 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 |
| EP4204419A1 (en) | 2020-10-19 | 2023-07-05 | Teva Pharmaceuticals International GmbH | 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 |
| EP4408428A1 (en) | 2021-09-27 | 2024-08-07 | 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 (ko) | 2023-04-07 | 2025-11-27 | 테른스 파마슈티칼스, 인크. | 간 장애 또는 심장대사 질환의 치료에 사용하기 위한 thr베타 효현제 및 glp-1r 효현제를 포함하는 조합 |
| 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 |
| WO2024263714A1 (en) | 2023-06-22 | 2024-12-26 | Madrigal Pharmaceuticals, Inc. | BIOMARKERS FOR TREATING LIVER DISORDERS WITH THR-β AGONISTS AND RELATED USES |
| 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 |
| CN117263870A (zh) * | 2023-09-21 | 2023-12-22 | 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 |
| 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 |
| WO2025133348A1 (en) | 2023-12-22 | 2025-06-26 | E-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 |
| WO2025171032A1 (en) | 2024-02-06 | 2025-08-14 | Madrigal Pharmaceuticals, Inc. | Methods for treating a fatty liver disease |
| US12377104B1 (en) | 2024-02-06 | 2025-08-05 | Madrigal Pharmaceuticals, Inc. | Methods for treating a fatty liver disease |
| WO2025191457A1 (en) * | 2024-03-13 | 2025-09-18 | Morepen Laboratories Limited | Process for the preparation of pyridazinone derivative |
| 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 |
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| TW200745052A (en) * | 2005-07-21 | 2007-12-16 | Hoffmann La Roche | Thyroid hormone receptor agonists |
| CN101801960A (zh) * | 2007-09-20 | 2010-08-11 | 霍夫曼-拉罗奇有限公司 | 甲状腺激素类似物的前药 |
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| IL266054B2 (en) | 2016-10-18 | 2023-10-01 | Madrigal Pharmaceuticals Inc | Methods for treating liver disorders or lipid disorders using a THR-BETA agonist |
| EP3807267B1 (en) | 2018-06-12 | 2025-03-19 | Xizang Haisco Pharmaceutical Co., Ltd. | Thyroid hormone receptor agonists and uses thereof |
| TW202019914A (zh) | 2018-07-02 | 2020-06-01 | 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 |
| US12391677B2 (en) | 2018-10-12 | 2025-08-19 | InventisBio Co., Ltd. | Thyroid hormone receptor agonists |
| 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 |
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| TW200745052A (en) * | 2005-07-21 | 2007-12-16 | Hoffmann La Roche | Thyroid hormone receptor agonists |
| CN101801960A (zh) * | 2007-09-20 | 2010-08-11 | 霍夫曼-拉罗奇有限公司 | 甲状腺激素类似物的前药 |
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