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-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-2023017323-A1 优先权日:2021-08-12 标题 :Method of the effective synthesis of active choline chloride ingredient using heterogeneous nanocatalysts based on copper and molybdenum 发明人:SOLTANI SOBH ZAHRA 权利人:HAFEZ VARESH 摘要:In this invention, the active substance of choline chloride is produced using copper and molybdenum based heterogeneous nanocatalysts which is a food supplement for livestock, poultry and aquatic animals and increases productivity. Choline chloride synthesis consists of two steps. The first step is the production of trimethylamine from ammonium chloride and paraformaldehyde, and the second step is the reaction between trimethylamine and chloroethanol, which will produce choline chloride. In the claimed invention, the production method is designed to produce high purity choline chloride from cheap raw materials in the shortest possible time. Choline chloride is an essential compound in the diet of birds and mammals and is required for the proper function of cells. Choline chloride in poultry diets is popular as vitamin B4.
专利号:US-2005080260-A1 优先权日:2003-04-22 标 题 :Preparation of prodrugs for selective drug delivery 发明人:MILLS RANDELL L; WU GUO-ZHANG 摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.
专利号:US-10975048-B2 优先权日:2015-12-14 标题 :Composition of 1,3,4-selenadiazole containing compounds with pharmacological activity 发明人:RUAN BENFANG HELEN; RUAN JENNIFER JIN 权利人:HANGZHOU JENNIFER BIOTECH CO LTD 摘要:The invention belongs to the field of biomedical research involving the 1,3,4-selenyldiazo derivatives that have cell protective activity. Because there are not so many heterocyclic selenium compounds, we synthesized a new type of selenium analog of BPTES. As the isoacceptor of BPTES, the compounds have antitumor activity, anti-oxidation and cell protection function. Currently many drugs contain the thiodiazo motif, so synthesis of selenyldiazo functional group could further optimize these drugs and are important in new drug development and application.
专利号:WO-2024189472-A1 优先权日:2023-03-14 标题 :Improved synthetic methods of making substituted pyrimidine intermediates for synthesis of orexin receptor modulators 发明人:MATCHA KIRAN; DEPRE DOMINIQUE; HUYGAERTS ANDY 权利人:JANSSEN PHARMACEUTICA NV 摘要:Processes for preparing (4,6-dimethylpyrimidin-2-yl)glycine (Formula 1) are described, which are useful for commercial manufacturing. Said compound is useful for the manufacture of an orexin receptor modulator which may be useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by orexin activity, such as insomnia and depression.
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