专利号:US-10029014-B2 优先权日:2013-09-10 标题:Synthesis of novel asymmetric bow-tie PAMAM dendrimer-based conjugates for tumor-targeting drug delivery 发明人:OJIMA IWAO; WANG TAO; TENG YU-HAN 权利人:UNIV NEW YORK STATE RES FOUND 摘要:The present disclosure relates to a dendrimer-based conjugate of the formula V m -D-C-D′-(T-F) n , which is useful for tumor targeting drug delivery. The use of asymmetric dendrimers allow for specific targeting as well as synthetic reproducibility.
专利号:US-2023399688-A1 优先权日:2015-08-20 标 题 :Compositions and multiplexed systems for coupled cell-free transcription-translation and protein synthesis and methods for using them 发明人:CULLER STEPHANIE; CHEN IHSIUNG BRANDON; PHARKYA PRITI; VAN DIEN STEVE; BARTON NELSON 权利人:GENOMATICA INC 摘要:In alternative embodiments, provided herein are transcription/translation (TX-TL) systems and methods of using them for use as rapid prototyping platforms for the synthesis, modification and identification of natural products (NPs), and natural product analogs (NPAs) and secondary metabolites, from biosynthetic gene cluster pipelines. In alternative embodiments, exemplary TX-TL systems as provided herein are used for the combinatorial biosynthesis of natural products (NPs), natural product analogs (NPAs) and secondary metabolites. In alternative embodiments, exemplary TX-TL systems as provided herein are used for the rapid prototyping of complex biosynthetic pathways as a way to rapidly assess combinatorial and biosynthetic designs before moving to cellular hosts. In alternative embodiments, these exemplary TX-TL systems are multiplexed for high-throughput (HT) automation and for prototyping engineered platforms for the synthesis or modification of natural products (NPs), and natural product analogs (NPAs) and secondary metabolites analogs.
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-2007060499-A1 优先权日:2005-09-15 标 题 :Chloroquine combination drugs 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. 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-2006040879-A1 优先权日:2004-08-21 标 题:Chloroquine coupled nucleic acids and methods for their synthesis 发明人:KOSAK KENNETH M 权利人:KOSAK KENNETH M 摘要:This invention discloses compositions and methods for preparing chloroquine-coupled nucleic acid compositions. 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 nucleic acid needs to be released, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to a nucleic acid 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 nucleic acids for therapeutic or other medical uses. The invention also discloses nucleic acid carrier compositions that are coupled to targeting molecules for targeting the delivery of nucleic acids to their site of action.
专利号:US-2005153913-A1 优先权日:2001-04-10 标 题 :Nucleic acid carrier compositions and methods for their synthesis 发明人:KOSAK KENNETH M 摘要:This invention discloses compositions and methods for preparing pharmaceutical nucleic acid carriers. The compositions comprise a carrier substance coupled to a nucleic acid intercalator whereby the intercalator is coupled by intercalation to the nucleic acid. The compositions can also include a biocleavable linkage for carrying and releasing nucleic acids for therapeutic or other medical uses. The invention also discloses nucleic acid carrier compositions that are coupled to targeting molecules for targeting the delivery of nucleic acids to their site of action.
1: Ueberschaar N, Meyer F, Dahse HM, Hertweck C. Bipiperidine conjugates as soluble sugar surrogates in DNA-intercalating antiproliferative polyketides. Chem Commun (Camb). 2016 Apr 7;52(27):4894-7. doi: 10.1039/c6cc00890a. Epub 2016 Mar 14. doi: 10.1021/ja4080024. Epub 2013 Nov 6. doi: 10.1002/rcm.6663. 5: Xu Z, Jakobi K, Welzel K, Hertweck C. Biosynthesis of the antitumor agent chartreusin involves the oxidative rearrangement of an anthracyclic polyketide. Chem Biol. 2005 May;12(5):579-88. Review. 11: Asai G, Yamamoto N, Toi M, Shin E, Nishiyama K, Sekine T, Nomura Y, Takashima S, Kimura M, Tominaga T. Pharmacokinetic and pharmacodynamic study of IST-622, a novel synthetic derivative of chartreusin, by oral administration in a phase II study of patients with breast cancer. Cancer Chemother Pharmacol. 2002 Jun;49(6):468-72. Epub 2002 Apr 9. Review. Japanese.
合成参考文献
参考文献:10.1385/1-59259-057-8:149 摘要:Shen LL. DNA-unwinding test using eukaryotic DNA topoisomerase I. Methods Mol Biol. 2001;95():149–60. doi: 10.1385/1-59259-057-8:149.