专利号:US-10973847-B2 优先权日:2017-06-30 标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof 发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.
专利号:US-2024368164-A1 优先权日:2021-04-28 标 题 :Purine nucleosides, their intermediates, and methods of preparation thereof 发明人:RAVI RAMA SURESH; JACOBSON KENNETH A; POE RUSSELL BIRCH 权利人:ASTROCYLE PHARMACEUTICALS INC; US HEALTH 摘要:The present invention provides purine nucleoside analog compounds and methods of use thereof for treatment of certain injuries, disorders and conditions, for example brain injuries such as stroke or traumatic brain injuries. The present invention further provides methods of synthesizing such compounds, and intermediates useful in the synthesis of such compounds.
专利号:US-11485721-B2 优先权日:2017-11-21 标 题:Method for the metal-free preparation of a biaryl by a photosplicing reaction and their uses 发明人:KLOSS FLORIAN; NEUWIRTH TONI; HAENSCH VEIT; HERTWECK CHRISTIAN 权利人:LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST HKI; LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST 摘要:The present invention relates to a method for the metal-free preparation of a biaryl compound by a photosplicing reaction and its use in the preparation of chemical compounds, preferably of active ingredients e.g. in the fields of pharmaceuticals and agrochemicals. In particular, it refers to a method for the regiocontrolled preparation of a biaryl compound of formula (I): Ar—Ar′ by photochemically reacting a precursor compound of formula (II): Ar—L—Ar′ to form a biaryl compound of general formula: Ar—L—Ar′(II)→Ar—Ar′ (I) wherein Ar and Ar′, independently of each other, represent an unsubstituted or substituted C6-C20 aryl group or a heteroaryl group with 5-20 ring atoms selected from carbon, nitrogen, oxygen and sulfur, and L represents a group —X—Y—Z— as defined herein. The biaryl compounds are generally suitable as intermediates or key building blocks in a very broad spectrum of organic chemical syntheses and their respective utilities. Their use within the field of synthesis of active ingredients is an aspect of the invention, and their use in the preparation of pharmaceutically active ingredients is particularly preferred.
专利号:EP-3645600-A1 优先权日:2017-06-30 标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
专利号:US-2025049968-A1 优先权日:2022-04-21 标 题 :Therapeutic and imaging agents for targeting myocardial tissue 发明人:EEDA VENKATESWARARAO; AWASTHI VIBHUDUTTA 权利人:UNIV OKLAHOMA 摘要:Analogs and derivatives of omecamtiv mecarbil (OM), including an 18F-labeled analog, and methods of synthesis thereof. Cardiac myosin targeting vectors comprising a lipid anchoring/solubilizing moiety conjugated to a head made of OM or the OM analog or derivative. Liposomes comprising a cardiac-treating cargo molecule and the cardiac myosin targeting vector. Methods of treating a cardiac condition or disease in a subject by administering to the subject the cardiac-treating cargo molecule and the cardiac myosin targeting vector. Methods of synthesizing an 18F-labeled analog of OM.
专利号:CN-107973784-B 优先权日:2017-11-16 标题 :Synthesis method of fimasartan
1: Kim CK, Yang XL, Kim YJ, Choi IY, Jeong HG, Park HK, Kim D, Kim TJ, Jang H, Ko SB, Yoon BW. Effect of Long-Term Treatment with Fimasartan on Transient Focal Ischemia in Rat Brain. Biomed Res Int. 2015;2015:295925. doi: 10.1155/2015/295925. Epub 2015 Sep 13. 2: Ghim JL, Paik SH, Hasanuzzaman M, Chi YH, Choi HK, Kim DH, Shin JG. Absolute bioavailability and pharmacokinetics of the angiotensin II receptor antagonist fimasartan in healthy subjects. J Clin Pharmacol. 2015 Aug 13. doi: 10.1002/jcph.618. [Epub ahead of print] doi: 10.2147/DDDT.S82098. eCollection 2015. 4: Lee JY, Choi YJ, Oh SJ, Chi YH, Paik SH, Lee KH, Jung JK, Ryu CS, Kim KB, Kim DH, Yoon YR, Kim SK. Characterization of fimasartan metabolites in human liver microsomes and human plasma. Xenobiotica. 2015 Jun
合成参考文献
参考文献:10.1097/fjc.0b013e31822b9092 摘要:Shin KH, Kim TE, Kim SE, Lee MG, Song IS, Yoon SH, Cho JY, Jang IJ, Shin SG, Yu KS. The effect of the newly developed angiotensin receptor II antagonist fimasartan on the pharmacokinetics of atorvastatin in relation to OATP1B1 in healthy male volunteers. J Cardiovasc Pharmacol. 2011 Nov;58(5):492–9. doi: 10.1097/fjc.0b013e31822b9092.