合成目标产物 Biib-021 主要起始原料 2-Chloromethyl-4-Methoxy-3,5-Dimethylpyridine Hydrochloride And 6-Chloroguanine
86604-75-3 + 10310-21-1 = 848695-25-0 反应条件:1.1 Reagents: Potassium Carbonate Solvents: Dimethyl Sulfoxide; 12 H,40 °C 标题:Targeted Protein Degradation Induced By Hemtacs Based On Hsp90 作者:Li,Zhenzhen; Ma,Siyue; Zhang,Ling; Zhang,Shuxin; Ma,Zhao; Et Al 参考文献:Journal Of Medicinal Chemistry 日期:2023 卷标:66(1) 页码:733-751]
10310-21-1 + 84006-10-0 = 848695-25-0 反应条件:1.1 Reagents: Potassium Carbonate,Sodium Iodide Solvents: Dimethylformamide; 6 H,40 °C 标题:Rationally Designed High-Affinity 2-Amino-6-Halopurine Heat Shock Protein 90 Inhibitors That Exhibit Potent Antitumor Activity 作者:Kasibhatla,Srinivas R.; Hong,Kevin; Biamonte,Marco A.; Busch,David J.; Karjian,Patricia L.; Et Al 参考文献:Journal Of Medicinal Chemistry 日期:2007 卷标:50(12) 页码:2767-2778]
86604-75-3 + 10310-21-1 = 848695-25-0 + 1665299-23-9 反应条件:1.1 Reagents: Potassium Carbonate Catalysts: Sodium Iodide Solvents: Dimethylformamide; 50 °C 标题:Process Development Of An N-Benzylated Chloropurine At The Kilogram Scale 作者:Shi,Xianglin; Chang,Hexi; Grohmann,Markus; Kiesman,William F.; Kwok,Daw-Iong Albert 参考文献:Organic Process Research & Development 日期:2015 卷标:19(3) 页码:437-443
专利号:US-2017283878-A1 优先权日:2015-12-11 标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING 权利人:ACADEMIA SINICA 摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.
专利号:US-2025206743-A1 优先权日:2022-03-25 标 题:Tyk2 inhibitor synthesis and intermediates thereof 发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG 权利人:TAKEDA PHARMACEUTICALS CO 摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.
专利号:US-10772971-B2 优先权日:2017-06-22 标 题:Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates 发明人:GURIJALA VENU REDDY; BOLLU SATYANARAYAN REDDY; LEBLANC JACQUES; LOWINGER TIMOTHY B; MCGILLICUDDY DENNIS; YIN MAO; YURKOVETSKIY ALEKSANDR V 权利人:MERSANA THERAPEUTICS INC; MERSANA THERPEUTICS INC 摘要:The disclosure provides methods of synthesis of polymeric scaffolds, e.g., those useful for conjugating with a protein based recognition-molecule (PBRM) to form PBRM-polymer-drug conjugates, and PBRM-polymer-drug conjugates thereof. The methods according to the disclosure allow for large-scale preparation of polymeric scaffolds having a high purity. In some embodiments, the methods according to the disclosure also allow for the preparation of scaffolds and conjugates thereof in better yield than previously used methods for preparing same. Also disclosed are methods of purifying polymeric scaffolds.
专利号:WO-2014018862-A1 优先权日:2012-07-27 标 题 :Pharmaceutical compositions comprising a heat shock protein inhibitor and a; purine de novo synthesis inhibitor for treating rheumatoid arthritis or cancer 发明人:FANG YE 权利人:CORNING INC; FANG YE 摘要:A pharmaceutical composition including an effective amount of the combination of: an heat shock protein (HSP) inhibitor, and a purine de novo biosynthesis inhibitor, or a pharmaceutically acceptable salt thereof. Also disclosed is a method of treating rheumatoid arthritis or cancer including administering an effective amount of the above mentioned pharmaceutical composition to a patient in need of such treatment, as defined herein.
专利号:CN-118922420-A 优先权日:2022-03-25 标题 :Synthesis of TYK2 inhibitors and their intermediates
专利号:US-11312722-B2 优先权日:2019-05-08 标 题:Hsp90 inhibitors and uses thereof 发明人:BROWN LAUREN ELAINE; HUANG DAVID S; COWEN LEAH E; WHITESELL LUKE; MARCYK PAUL 权利人:UNIV BOSTON; GOVERNING COUNCIL UNIV TORONTO 摘要:Herein is described the design and synthesis of resorcylate aminopyrazole compounds. These compounds show broad, potent and fungal-selective Hsp90 inhibitory activity. These compounds also find use in treating Hsp90 related diseases.
1: Xu L, Woodward C, Khan S, Prakash C. In Vitro Metabolism of 6-Chloro-9-(4-methoxy-3,5-dimethylpyridin-2-ylmethyl)-9H-purin-2-ylamine (BIIB021), an Inhibitor of HSP90, in Liver Microsomes and Hepatocytes of Rats, Dogs, and Humans and Recombinant Human Cytochrome P450 Isoforms. Drug Metab Dispos. 2012 Jan 4. [Epub ahead of print] Epub 2009 Aug 11.
合成参考文献
摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749