专利号:US-9439423-B2 优先权日:2007-10-29 标 题 :Antiparasitic agent for fish and method of controlling proliferation of fish parasites 发明人:KAWANO FUMI; HIRAZAWA NORITAKA 权利人:KAWANO FUMI; HIRAZAWA NORITAKA; NIPPON SUISAN KAISHA LTD 摘要:An antiparasitic agent for fish includes an inhibitor of folate synthesis and/or an inhibitor of folate activation as the active substance(s). A combination preparation composed of an inhibitor of folate synthesis and an inhibitor of folate activation is disclosed. Sulfonamide is disclosed as suitable for the inhibitor of folate synthesis. A dihydrofolate reductase inhibitor, a folate antagonist are disclosed as suitable inhibitors of folate activation. The antiparasitic agent is able to exterminate fish parasites via oral administration. It is effective against fish parasites belonging to the ciliate group.
专利号:US-9265777-B2 优先权日:2009-04-27 标题 :Antiparasitic agent for fish and method of controlling proliferation of fish parasites 发明人:KAWANO FUMI; HIRAZAWA NORITAKA 权利人:KAWANO FUMI; HIRAZAWA NORITAKA; NIPPON SUISAN KAISHA LTD 摘要:A method of controlling proliferation of fish parasites comprising the administration of 1 to 50 mg/kg fish body weight/day of an inhibitor of folate synthesis and/or an inhibitor of folate activation to fish continuously for 1 to 2 weeks. Using a combination preparation composed of an inhibitor of folate synthesis and an inhibitor of folate activation is preferable, and a sulfonamide is preferable for the inhibitor of folate synthesis. A dihydrofolate reductase inhibitor, a folate antagonist, etc., can be used as the inhibitor of folate activation. The antiparasitic agent is able to exterminate fish parasites via oral administration. It is particularly effective against parasites belonging to the ciliate group among fish parasites.
专利号:WO-2023192384-A1 优先权日:2022-03-29 标题 :Tetrazine-derived linkers for single guide rnas 发明人:WATTS JONATHAN K; ZAMORE PHILLIP D; ARIF AMENA; CHEN ZEXIANG; DEVI GITALI; SONTHEIMER ERIK J 权利人:UNIV MASSACHUSETTS 摘要:CRISPR-Cas genome editing technology has applications in biomedical research and therapeutics that has led to an increased demand for guide RNAs. Synthesis of chemically modified single-guide RNAs (sgRNAs) >100 nt remains a bottleneck. A tetrazine ligation method is disclosed herein for the preparation of sgRNAs that overcomes this synthesis challenge. For example, a tetrazine moiety on a 3'-end of crRNA and a norbornene moiety on a 5'-end of tracrRNA permits ligation between crRNA and tracrRNA to form an sgRNA under mild conditions. Tetrazine-ligated sgRNAs allow efficient genome editing as demonstrated by reporter models and endogenous loci in human cells. A structural modification of the linker moiety permits achievement of high efficiency editing.
专利号:US-2003138490-A1 优先权日:2001-09-08 标 题 :Synthesis and uses of polymer gel nanoparticle networks 发明人:HU ZHIBING; LU XIHUA; GAO JUN; PONDER BILL C; JOHN JOHN ST; MORO DANIEL G 摘要:Disclosed is a new class of nanostructured polymeric materials comprising polymer gel nanoparticles that are covalently bonded through functional groups on the surfaces of neighboring particles. These nanoparticles may be prepared as suspensions in an aqueous or, non-aqueous environment. These gels have two unique and different structural networks; the primary network comprises crosslinked polymer chains in each individual particle, while the secondary network is a system of crosslinked nanoparticles. Particular polymer gel nanoparticle network compositions disclosed herein may function as carriers for controlled delivery of pharmaceuticals or other chemical agents, gel sensors and other commercial applications.
专利号:US-2008051323-A1 优先权日:2004-08-21 标 题 :Chloroquine drug compositions and methods for their synthesis 发明人:KOSAK KENNETH M 权利人:KOSAK KENNETH M 摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. n The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.
专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
1: Wang Z, Li X, Zhang F, Gao Y, Cheng J, Fu F. Regulating the Growth Rate of Gold Nanobipyramids via a HCl-NADH-Ascorbic Acid System toward a Dual-Channel Multicolor Colorimetric Immunoassay for Simultaneously Screening and Detecting Multiple Sulfonamides. Anal Chem. 2023 Jul 11;95(27):10438-10447. doi: 10.1021/acs.analchem.3c01928. Epub 2023 Jun 29. 258:124449. doi: 10.1016/j.talanta.2023.124449. Epub 2023 Mar 11. 122:227-235. doi: 10.1016/j.jes.2022.02.007. Epub 2022 Feb 17. 40(4):333-342. Chinese. doi: 10.3724/SP.J.1123.2021.08010.
合成参考文献
摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664 摘要:A. V. Willi and W. Meier, Helv. Chim. Acta 39, 54 (1956). 摘要:Yang TS. Teratogenic effects of sulfadimethoxypyrimidines and sulfadimethylpyrimidines in chick embryos. Taiwan Yi Xue Hui Za Zhi. 1973 Aug;72(8):450–7. 摘要:Oelssner W, Funk KF. [Experimental studies of some new halogenated sulfapyrimidines]. Arzneimittelforschung. 1966 Sep;16(9):1134–40.