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
-
- 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
-
- 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
- A61K31/53—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)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (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 |
---|---|---|---|
SG11201501907YA SG11201501907YA (en) | 2012-09-17 | 2013-09-17 | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
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 |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
SG11201501907YA SG11201501907YA (en) | 2012-09-17 | 2013-09-17 | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
Family Applications After (1)
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 |
Country Status (21)
Country | Link |
---|---|
US (8) | US9266861B2 (en:Method) |
EP (4) | EP3689853B1 (en:Method) |
JP (7) | JP6616688B2 (en:Method) |
KR (4) | KR102138750B1 (en:Method) |
CN (2) | CN105008335B (en:Method) |
AR (1) | AR092872A1 (en:Method) |
AU (1) | AU2013315017C1 (en:Method) |
BR (2) | BR112015005891A2 (en:Method) |
CA (3) | CA3090070C (en:Method) |
DK (2) | DK3689853T3 (en:Method) |
ES (2) | ES2795450T3 (en:Method) |
IL (7) | IL288133B2 (en:Method) |
IN (1) | IN2015DN03133A (en:Method) |
MX (2) | MX395148B (en:Method) |
MY (1) | MY170520A (en:Method) |
NZ (2) | NZ739645A (en:Method) |
RU (2) | RU2018128393A (en:Method) |
SG (3) | SG11201501907YA (en:Method) |
TW (4) | TWI755628B (en:Method) |
WO (1) | WO2014043706A1 (en:Method) |
ZA (1) | ZA201501795B (en:Method) |
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BR112015005891A2 (pt) * | 2012-09-17 | 2017-08-08 | F Hoffmann La Roche Ltd | método de sintetizar análogos do hormônio da tireoide e polimorfos destes |
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. |
JP7156722B2 (ja) * | 2018-01-23 | 2022-10-19 | 深▲チェン▼市塔吉瑞生物医薬有限公司 | 置換ピリダジノン化合物 |
EP3807267B1 (en) * | 2018-06-12 | 2025-03-19 | Xizang Haisco Pharmaceutical Co., Ltd. | Thyroid hormone receptor agonists and uses thereof |
WO2019242766A1 (zh) * | 2018-06-22 | 2019-12-26 | 成都海创药业有限公司 | 氘代mgl-3196化合物及其用途 |
AR115666A1 (es) * | 2018-07-02 | 2021-02-10 | Madrigal Pharmaceuticals Inc | Formas sólidas de 2-(3,5-dicloro-4-((5-isopropil-6-oxo-1,6-dihidropiridazin-3-il)oxi)fenil)-3,5-dioxo-2,3,4,5-tetrahidro-1,2,4-triazin-6-carbonitrilo |
WO2020073974A1 (en) * | 2018-10-12 | 2020-04-16 | Inventisbio Shanghai Ltd. | Thyroid hormone receptor agonists |
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 |
EP3927693A4 (en) | 2019-02-21 | 2023-04-05 | Nanjing Ruijie Pharma Co., Ltd. | NOVEL COMPOUNDS AND THEIR USES AS THYROID HORMONE RECEPTOR AGONISTS |
LT3965884T (lt) | 2019-05-08 | 2025-04-10 | Aligos Therapeutics, Inc. | Thr-beta moduliatoriai su diokso-1,2,4-triazilo galine grupe |
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 |
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 |
AU2020346057A1 (en) | 2019-09-12 | 2022-04-21 | 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 |
CN113454069B (zh) * | 2019-11-26 | 2025-03-14 | 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 |
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 |
US20230339911A1 (en) * | 2020-08-27 | 2023-10-26 | InventisBio Co., Ltd. | Pyridazinone compounds |
US20230416234A1 (en) * | 2020-09-10 | 2023-12-28 | Crystal Pharmaceutical (Suzhou) Co., Ltd. | Crystal form of resmetirom, preparation method therefor, and use thereof |
CA3195789A1 (en) | 2020-10-19 | 2022-04-28 | 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 |
CN116847847A (zh) | 2021-02-01 | 2023-10-03 | 马德里加尔制药公司 | 用于治疗肝紊乱或血脂紊乱的瑞舒伐他汀和resmetirom的治疗组合 |
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 |
CN116768802A (zh) * | 2023-05-25 | 2023-09-19 | 杭州科巢生物科技有限公司 | 一种瑞司美替罗的合成方法 |
US20240423992A1 (en) | 2023-06-22 | 2024-12-26 | Madrigal Pharmaceuticals, Inc. | Biomarkers for treating liver disorders with thr-b 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 |
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BR112015005891A2 (pt) * | 2012-09-17 | 2017-08-08 | F Hoffmann La Roche Ltd | método de sintetizar análogos do hormônio da tireoide e polimorfos destes |
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EP3807267B1 (en) | 2018-06-12 | 2025-03-19 | Xizang Haisco Pharmaceutical Co., Ltd. | Thyroid hormone receptor agonists and uses thereof |
AR115666A1 (es) | 2018-07-02 | 2021-02-10 | Madrigal Pharmaceuticals Inc | Formas sólidas de 2-(3,5-dicloro-4-((5-isopropil-6-oxo-1,6-dihidropiridazin-3-il)oxi)fenil)-3,5-dioxo-2,3,4,5-tetrahidro-1,2,4-triazin-6-carbonitrilo |
WO2020073974A1 (en) | 2018-10-12 | 2020-04-16 | Inventisbio Shanghai Ltd. | Thyroid hormone receptor agonists |
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 |
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2013
- 2013-09-17 BR BR112015005891A patent/BR112015005891A2/pt not_active Application Discontinuation
- 2013-09-17 IN IN3133DEN2015 patent/IN2015DN03133A/en unknown
- 2013-09-17 CA CA3090070A patent/CA3090070C/en active Active
- 2013-09-17 CN CN201380059943.5A patent/CN105008335B/zh active Active
- 2013-09-17 DK DK20157696.4T patent/DK3689853T3/da active
- 2013-09-17 RU RU2018128393A patent/RU2018128393A/ru unknown
- 2013-09-17 CA CA3111317A patent/CA3111317C/en active Active
- 2013-09-17 MX MX2018014924A patent/MX395148B/es unknown
- 2013-09-17 JP JP2015532148A patent/JP6616688B2/ja active Active
- 2013-09-17 NZ NZ73964513A patent/NZ739645A/en unknown
- 2013-09-17 KR KR1020187034908A patent/KR102138750B1/ko active Active
- 2013-09-17 EP EP20157696.4A patent/EP3689853B1/en active Active
- 2013-09-17 ES ES13837402T patent/ES2795450T3/es active Active
- 2013-09-17 TW TW108132827A patent/TWI755628B/zh active
- 2013-09-17 IL IL288133A patent/IL288133B2/en unknown
- 2013-09-17 TW TW110117935A patent/TWI804870B/zh active
- 2013-09-17 SG SG11201501907YA patent/SG11201501907YA/en unknown
- 2013-09-17 KR KR1020157009807A patent/KR101966490B1/ko active Active
- 2013-09-17 TW TW107137798A patent/TWI681957B/zh active
- 2013-09-17 IL IL320269A patent/IL320269A/en unknown
- 2013-09-17 CA CA2884481A patent/CA2884481C/en active Active
- 2013-09-17 MY MYPI2015000591A patent/MY170520A/en unknown
- 2013-09-17 KR KR1020207005528A patent/KR20200023528A/ko not_active Ceased
- 2013-09-17 AR ARP130103332A patent/AR092872A1/es active IP Right Grant
- 2013-09-17 SG SG10201705984XA patent/SG10201705984XA/en unknown
- 2013-09-17 RU RU2015114327A patent/RU2668960C2/ru active
- 2013-09-17 EP EP24173563.8A patent/EP4406594B1/en active Active
- 2013-09-17 EP EP21209827.1A patent/EP4023641B1/en active Active
- 2013-09-17 DK DK13837402.0T patent/DK2895466T3/da active
- 2013-09-17 WO PCT/US2013/060177 patent/WO2014043706A1/en active Application Filing
- 2013-09-17 TW TW102133687A patent/TWI652260B/zh active
- 2013-09-17 MX MX2015003418A patent/MX364661B/es active IP Right Grant
- 2013-09-17 BR BR122021024202-0A patent/BR122021024202B1/pt active IP Right Grant
- 2013-09-17 ES ES20157696T patent/ES2907926T3/es active Active
- 2013-09-17 AU AU2013315017A patent/AU2013315017C1/en active Active
- 2013-09-17 SG SG10202006058QA patent/SG10202006058QA/en unknown
- 2013-09-17 EP EP13837402.0A patent/EP2895466B1/en active Active
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2015
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2016
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