专利号:US-9453037-B2 优先权日:2011-07-28 标 题 :Methylphenidate-prodrugs, processes of making and using the same 发明人:GUENTHER SVEN; CHI GUOCHEN; BERA BINDU; MICKLE TRAVIS; BERA SANJIB 权利人:KEMPHARM INC; KEMPHARM INC 摘要:The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.
专利号:WO-2024054881-A1 优先权日:2022-09-07 标题:Ligand-enabled scalable c-h hydroxylation of benzoic and phenylacetic acids at room temperature 发明人:YU JIN-QUAN; LI ZHEN; PARK HAN 权利人:SCRIPPS RESEARCH INST 摘要:The application discloses industry scalable methods of using bifunctional bidentate pyridone-carboxylic acid ligands, such as 2-methyl-2-(6-oxo-1,6-dihydropyridin-2-yl)propanoic acid, that enable room-temperature Pd-catalyzed C-H hydroxylation of a broad range of benzoic and phenylacetic acids with an industry-compatible oxidant, aqueous hydrogen peroxide, at room temperature. Further disclosed are methods of derivatization of the resulting hydroxylation products, synthesis of polyfluorinated natural products coumestan or pterocarpene from phenol building blocks, and hydroxylation of ibuprofen using this methodology,
专利号:US-7101684-B2 优先权日:1995-07-06 标 题:Modified modular polyketide synthase 发明人:KHOSLA CHAITAN; PIEPER REMBERT; LUO GUANGLIN; CANE DAVID 权利人:UNIV BROWN RES FOUND 摘要:Modular polyketide synthases modified so as not to incorporate natural starter units can be used for clean synthesis of novel polyketides.
专利号:US-6080555-A 优先权日:1995-07-06 标题 :Synthesis of polyketides from diketides
专利号:US-7947480-B2 优先权日:2000-01-12 标 题 :Everninomicin biosynthetic genes 发明人:HOSTED THOMAS J; WANG TIM X; HORAN ANN C 权利人:SCHERING CORP 摘要:This invention is directed to nucleic acids which encode the proteins that direct the synthesis of the orthosomycin everninomicin and to use of the nucleic acids and proteins to produce compounds exhibiting antibiotic activity based on the everninomycin structure. The DNA sequence for the gene clusters responsible for encoding everninomicin biosynthetic genes, which provide the machinery for producing everninomicin, are provided. Thus, this invention provides the nucleic acid sequences needed to synthesize novel everninomicin-related compounds based on everninomicin, arising from modifications of the DNA sequence designed to change glycosyl and modified orsellinic acid groups contained in everninomicin. A Micromonospora site-specific integrase gene is also provided, which can be incorporated in a vector for integration into any actinomycete, and, particularly into Monospora . Thus, the invention further provides methods for introducing heterologous genes into an actinomycete chromosome using this particular vector.
专利号:US-6927286-B1 优先权日:1999-01-06 标 题 :Bleomycin gene cluster components and their uses 发明人:SHEN BEN; DU LIANGCHENG; SANCHEZ CESAR; CHEN MEI; EDWARDS DANIEL J 权利人:UNIV CALIFORNIA 摘要:This invention provides detailed sequence analysis and characterization of the gene cluster responsible for the synthesis of bleomycin in Streptomyces verticillus . The bleomycin gene cluster provides the first hybrid polyketide synthase/nonribosomal peptide synthetase pathway and elucidation of the various modules and enzymatic domains characterizing the pathway provides convenient synthetic routes for bleomycins, bleomycin analogs, and various other polyketides.
摘要:Hitomi, Y.; Arakawa, K., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 297. 摘要:D. Peltier, C. R. Acad. Sci., Ser. C 241, 1467 (1955). 摘要:M. V. Park, Nature (London) 197, 283 (1963). 摘要:L. G. Bray, J. F. J. Dippy, S. R. C. Hughes and L. W. Laxton, J. Chem. Soc. 1957, 2405. 参考文献:10.1006/bbrc.2002.2017 摘要:Light RJ. Yeast Hydroxy Fatty Acids and Fungal Polyketides: Lessons Learned from the Konrad Bloch Laboratory. Biochemical and Biophysical Research Communications. 2002 Apr;292(5):1213–9. doi: 10.1006/bbrc.2002.2017.