1581304-53-1 = 920509-32-6 反应条件:1.1 Reagents: Potassium Acetate Solvents: Dimethylacetamide; Rt; 3 H,120 °C1.2 Reagents: Water 标题:Preparation Of Aryltriazinones As Modulators Of Thr-β And Methods Of Use Thereof 参考文献:World Intellectual Property Organization]
1581304-53-1 = 920509-32-6 反应条件:1.1 Reagents: Potassium Acetate Solvents: Dimethylacetamide; Rt -> 120 °C; 2 H,120 °C 标题:Method Of Synthesizing Thyroid Hormone Analogs And Polymorphs Thereof 参考文献:World Intellectual Property Organization]
920509-33-7 = 920509-32-6 反应条件:1.1 Reagents: Acetic Acid,Sodium Acetate; Rt; 1.5 H,Rt -> 120 °C; 120 °C -> 0 °C 标题:Preparation Of Pyridazinone Derivatives As Thyroid Hormone Receptor Agonists For Treating Metabolic Disorders And Other Diseases 参考文献:World Intellectual Property Organization]
920509-33-7 = 920509-32-6 反应条件:1.1 Reagents: Sodium Acetate Solvents: Acetic Acid; Rt; 1.5 H,120 °C; 120 °C -> 0 °C1.2 Reagents: Water; 30 Min,0 °C 标题:Discovery Of 2-[3,5-Dichloro-4-(5-Isopropyl-6-Oxo-1,6-Dihydropyridazin-3-Yloxy)Phenyl]-3,5-Dioxo-2,3,4,5-Tetrahydro[1,2,4]Triazine-6-Carbonitrile (Mgl-3196),A Highly Selective Thyroid Hormone Receptor β Agonist In Clinical Trials For The Treatment Of Dyslipidemia 作者:Kelly,Martha J.; Pietranico-Cole,Sherrie; Larigan,J. Douglas; Haynes,Nancy-Ellen; Reynolds,Charles H.; Et Al 参考文献:Journal Of Medicinal Chemistry 日期:2014 卷标:57(10) 页码:3912-3923]
= 920509-32-6 [标题:Reaction Conditions 标题:Process For The Preparation Of 6-(4-Nitro-Phenoxy)-2H-Pyridazin-3-One And 6-(4-Amino-Phenoxy)-2H-Pyridazin-3-One Derivatives As Intermediates Of Thyroid Hormone Analogues 参考文献:World Intellectual Property Organization
3,5-Dichloro-4-((6-Chloropyridazin-3-yl)Oxy)Aniline置于盐酸,水,Potassium Acetate,溶剂黄146,Lithium Chloride,Potassium Hydroxide,Sodium Nitrite体系中,用 四氢呋喃,N,N-二甲基乙酰胺,水 作为反应溶剂,化学反应 14.01H,反应生成 2-(3,5-二氯-4-((5-异丙基-6-氧代-1,6-二氢哒嗪-3-基)氧基)苯基)-3,5-二氧基-2,3,4,5-四氢-1,2,4-三嗪-6-碳腈 参考文献: Method Of Synthesizing Thyroid Hormone Analogs And Polymorphs Thereof[fr] Procédé De Synthèse D'Analogues De L'Hormone Thyroïdienne Et De Ses Polymorphes 标题: Method Of Synthesizing Thyroid Hormone Analogs And Polymorphs Thereof[fr] Procédé De Synthèse D'Analogues De L'Hormone Thyroïdienne Et De Ses Polymorphes
专利号:WO-2024084491-A1 优先权日:2022-10-21 标题:Process for synthesis of res metirom and its intermediates thereof 发明人:MEHTA NILESH VIPINCHANDRA 权利人:MEHTA NILESH VIPINCHANDRA 摘要:The present invention discloses a process for synthesis of Res metirom and its intermediates thereof. More particularly, the invention discloses process for synthesis of a key intermediate, 6-(4-amino, 2,6-dichlorophenoxy)4- isopropylpyridazin-3(2H)-one, of Res metirom via novel intermediate compounds of formula A. Wherein, R is selected from methyl, ethyl and propyl.
专利号:US-2018297925-A1 优先权日:2015-10-12 标题 :Methods for total synthesis of resolvin e1 发明人:JAGTAP PRAKASH 权利人:SALZMAN LOVELACE INVEST LTD 摘要:Methods for total chemical synthesis of Resolvin E1 (RvE1) include Wittig reaction of two compounds having hydroxyl protecting group in the presence of a strong base, removal of the hydroxyl-protecting groups with a deprotecting reagent to produce a compound having an ester group, and hydrolysis of the ester group to obtain RvE1
专利号:US-2005239767-A1 优先权日:2003-10-28 标题 :Intermolecular SNAr of the heterocycle-activated nitro and fluoro groups-application in the synthesis of polyazamacrocyclic ligands 发明人:CHAN MICHAEL K; FEKNER TOMASZ 权利人:CHAN MICHAEL K; FEKNER TOMASZ 摘要:A new class of tetracylic benzimidazole compounds and derivatives thereof. Additionally provided is a synthetic route for the generation of these and related compounds via Intramolecular Aromatic Nucleophilic Substitution (S N Ar) of the Benzimidazole-Activated Nitro Groups. Additionally, a facile route for the generation of novel phenol species as thermal decomposition of compounds the S N Ar product, which occurs at high temperature resulting in cleavage of the ether linkage and formation of a vinyl group and phenol is provided. Also provided are methods of using the compounds described herein in the treatment HIV.
专利号:US-9968612-B2 优先权日:2012-09-17 标题:Method of synthesizing thyroid hormone analogs and polymorphs thereof 发明人:TAUB REBECCA; REYNOLDS CHARLES H 权利人:MADRIGAL PHARMACEUTICALS INC 摘要:The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TRβ mutation.
专利号:EA-031768-B1 优先权日:2009-12-18 标题:METHODS OF SYNTHESIS OF INTERMEDIATE COMPOUNDS FOR THE APPLICATION IN THE SYNTHESIS OF DEOXIC ACID
专利号:US-11905244-B2 优先权日:2017-09-26 标题 :Chemical modulators of store-operated calcium channels and their therapeutic applications 发明人:ZHOU YUBIN; HE LIAN 权利人:TEXAS A & M UNIV SYS 摘要:Methods of identification of inhibitors of calcium release-activated calcium (CRAC) channel and small molecule inhibitors of CRAC channel, including methods of their synthesis and pharmaceutical use, are disclosed.
1: Ratziu V, Scanlan TS, Bruinstroop E. Thyroid hormone receptor-β analogs for the treatment of Metabolic Dysfunction-Associated Steatohepatitis (MASH). J Hepatol. 2024 Oct 18:S0168-8278(24)02639-4. doi: 10.1016/j.jhep.2024.10.018. Epub ahead of print. 8(10):e70025. doi: 10.1002/jgh3.70025. 8: Dixon ED, Claudel T, Nardo AD, Riva A, Fuchs C, Mlitz V, Busslinger G, Schnarnagl H, Stojakovic T, Senéca J, Hinteregger H, Grabner GF, Kratky D, Verkade H, Zimmermann R, Haemmerle G, Trauner M. Inhibition of ATGL alleviates MASH via impaired PPARα signalling that favours hydrophilic bile acid composition in mice. J Hepatol. 2024 Sep
合成参考文献
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025). 参考文献:10.1016/j.cgh.2021.07.039 摘要:Younossi ZM, Stepanova M, Taub RA, Barbone JM, Harrison SA. Hepatic Fat Reduction Due to Resmetirom in Patients With Nonalcoholic Steatohepatitis Is Associated With Improvement of Quality of Life. Clin Gastroenterol Hepatol. 2022 Jun;20(6):1354–1361.e7. doi: 10.1016/j.cgh.2021.07.039.