专利号:US-10047122-B2 优先权日:2013-03-14 标 题 :Peptide and peptide mimetic binding antagonists of polo-like kinase 1 polo box domain and methods of use 发明人:QIAN WENJIAN; PARK JUNG EUN; LAI CHRISTOPHER C; KELLEY JAMES A; LEE KYUNG S; BURKE JR TERRENCE R 权利人:THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES 摘要:The invention provides novel compounds that may serve as anticancer therapeutics. The compounds of the invention bind to polo-like kinases through the polo-box domain. In certain embodiments, the compounds of the invention are POM-protected peptide derivatives. The use of cationic bis-alkyl his residues in combination with a mono POM-protected phophoryl group results in a peptide possessing an overall neutral charge. The peptide derivatives of the invention have achieved both good efficacy and an enhanced bioavailability. The invention also provides methods of use, compositions, and kits thereof. Further, the invention provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.
专利号:US-8536318-B2 优先权日:2008-05-29 标题 :Chemical RNA synthesis method 发明人:DEBART FRANCOISE; VASSEUR JEAN-JACQUES; LAVERGNE THOMAS 权利人:DEBART FRANCOISE; VASSEUR JEAN-JACQUES; LAVERGNE THOMAS; CENTRE NAT RECH SCIENT; UNIV MONTPELLIER 2 摘要:The invention relates to a method for the chemical synthesis of RNA, comprising the following steps: a) bonding to a solid support of a monomer having formula (II) in which—X 1 is a dimethoxytrityl group,—X 6 is H or an OAc group or OX 3 , in which X 3 is a group having formula (A), in which X is O or S, R′ is H or CH 3 and R is selected from a linear or branched alkyl group at C 1 to C 4 and a R 1 —O—R 2 group in which R 1 is an alkyl group at C 1 to C 2 and R 2 is a CH 3 group or CH 2 CH 2 —O—CH 3 or aryl; b) assembly with the monomer having formula (II) bound to the support thereof obtained in step (a) of at least one monomer having formula (III) in which X 1 , Bp, X 3 are as defined for formula (II) and X 5 is a hydrogen phosphonate monoester or phosphoramidite group, preferably a 2-cyanoethyl-N,N-diisopropylphosphoramidite group, which is used to obtain a protected single-strand RNA bound to a support.
专利号:US-9963472-B2 优先权日:2013-11-04 标 题 :Stable pantetheine derivatives for the treatment of pantothenate kinase associated neurodegeneration (PKAN) and methods for the synthesis of such compounds 发明人:JENKO BRANKO; KOSEC GREGOR; PETKOVIC HRVOJE; PODGORSEK BERKE AJDA; PAHOR JERCA; CUSAK ALEN; SIBON ODA CORNELIA MARIA; SRINIVASAN BALAJI 权利人:ACIES BIO D O O; UNIV GRONINGEN; ACADEMISCH ZIEKENHUIS GRONINGEN 摘要:The invention relates to (S)-acyl-4′-phosphopantetheine derivatives, methods of their synthesis, and related medical uses of such compounds. Preferred medical uses relate to the treatment of neurodegenerative diseases, such as PKAN.
专利号:US-9907796-B2 优先权日:2012-10-04 标题:Methods of treating tumoral diseases, or bacterial or viral infections 发明人:DEOKAR RHUSHIKESH CHANDRABHAN; DUGAR SUNDEEP; MAHAJAN DINESH; WERNER MILTON HENRY 权利人:DEOKAR RHUSHIKESH CHANDRABHAN; DUGAR SUNDEEP; MAHAJAN DINESH; WERNER MILTON HENRY; INHIBIKASE THERAPEUTICS INC 摘要:Novel compounds and their synthesis are described. Methods for using these compounds in the prevention or treatment of cancer, a bacterial infection or a viral infection in a subject are also described.
专利号:US-2018118767-A1 优先权日:2013-11-04 标题 :Stable pantetheine derivatives for the treatment of pantothenate kinase associated neurodegeneration (pkan) and methods for the synthesis of such compounds
专利号:EP-3066106-A1 优先权日:2013-11-04 标题 :Stable pantetheine derivatives for the treatment of pantothenate kinase associated neurodegeneration (pkan) and methods for the synthesis of such compounds
摘要:Yorimitsu, H., Science of Synthesis Knowledge Updates, (2010) 3, 11. 摘要:Chemla, F.; Pérez-Luna, A., Science of Synthesis, (2020) , 299. 摘要:Fogel, M. S.; Shellnutt, Z. S.; Koide, K., Science of Synthesis: Dearomatizations, (2026) .