专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-2024132430-A1 优先权日:2021-08-05 标 题 :Chemicals and use of hypohalites in mechanism-based selective dual radical organic synthesis 发明人:PALOMINO EDUARDO 权利人:WALKER CANCER RES INSTITUTE INC 摘要:The synthesis of pattern-specific compounds using hypohalites, such as hypochlorous acid, sodium hypochlorite, and potassium hypoiodite, as dual-radical generators is provided. The synthesis can be implemented by a cyclization reaction, a dehydrogenation reaction, a hydroxylation reaction, a decarboxylation reaction, or any combination of the above four. The reactions are typically carried out in water, in a nonpolar solvent such as ethyl acetate, or a mixture of both. Hypochlorous acid is made by adding a weak acid such as acetic acid to sodium hypochlorite.
专利号:US-2004053355-A1 优先权日:2000-05-26 标题:Modular approach to on-line synthesis, drug discovery and biochemical transformations using immobilized enzyme reactors 发明人:WAINER IRVING; MARKOGLOU NEKTARIA 摘要:A coupled system using extremely different enzymes with incompatible cofactors and reaction conditions has been constructed using standard liquid chromatographic formats and open tubular formats. One of the significant aspects of the present invention lies in the development of the liquid chromatographic on-line enzyme cascade. This has been illustrated by the biosynthetic pathway involving dopamine beta-hydroxylase and phenylethanolamine N-methyltransferase which encompass the synthesis of the key neurotransmitters, norepinephrine and epinephrine. The results demonstrate for the first time the immobilization of dopamine beta-hydroxylase and phenylethanolamine N-methyltransferase. The IMERs are active and can be used in a liquid chromatographic format for qualitative and quantitative determinations. The IMER-HPLC system can be used to carry out standard Michaelis-Menten enzyme kinetic studies and to quantitatively determine enzyme kinetic constants, identify specific enzyme inhibitors, provide information regarding the mode of inhibition and the inhibitor constants (K i ). A second significant aspect of the present invention lies in the ability of the immobilized enzyme reactors to be used independently or as a combination, thus providing a unique opportunity to explore the interrelationships between these enzymes, to investigate the source of diseases and to design new drug entities for identified clinical syndromes.
专利号:WO-2025128098-A1 优先权日:2023-12-13 标 题 :Solid oral dosage forms, kits, and methods of using the same 发明人:LI YING; LANGER ROBERT; TRAVERSO CARLO 权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC 摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).
专利号:US-2024052097-A1 优先权日:2021-02-08 标题 :Synthesis of peg-based thiol-norbornene hydrogels with tunable hydroylitic degradation properties 发明人:LIN CHIEN-CHI; LIN FANG-YI 权利人:UNIV INDIANA TRUSTEES 摘要:Methods for synthesizing a hydrogel having tunable hydrolylic degradation kinetics according to certain embodiments include synthesizing a norborene-functionalized polyethylene glycol macromer having an ester linkage between a polyethylene glycol domain of the macromer and a norbornene domain of the macromer and having a carboxyl group on the norbornene; and reacting a quantity of such macromers with a quantity of dithiol molecules by an ultraviolet-initiated photo-gelation reaction to yield a hydrogel. Such macromers and such hydrogels form additional aspects of the disclosure, as do a wide variety of methods for tuning and for using such hydrogels.
专利号:US-3903077-A 优先权日:1973-04-05 标题:Direct synthesis of dopamine amino acid amides 发明人:JONES PETER HADLEY; OURS CARROLL WAYNE; ROTEMAN ROBERT 权利人:ABBOTT LAB 摘要:An improved process for synthesizing amino acid amides of dopamine comprising reacting an active ester of an appropriate Ncarbobenzyloxy amino acid directly with a dopamine salt. The amino acid amides of dopamine are useful as renal vasodilators and antihypertensive agents.
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