专利号:US-5990341-A 优先权日:1993-11-08 标 题 :Diastereoselective synthesis hydroxyethylene dipeptide isosteres 发明人:LIOTTA DENNIS C; LAGU BHARAT RAMKRISHNA 权利人:UNIV EMORY 摘要:A process for the synthesis of hydroxyethylene dipeptide isosteres from α-N,N-di(protected)amino(alkyl or substituted alkyl) methyl ketones that can be efficiently carried out on an industrial scale. The process proceeds with excellent diastereoselectivity and chemical efficiency, and can be used to prepare a wide variety of hydroxyethylene dipeptide isosteres for a variety of uses, including as HIV-1 protease inhibitors and renin inhibitors.
专利号:US-11560357-B2 优先权日:2018-09-22 标题 :Methods of producing pyrazole compounds 发明人:GUPTA RAMESH CHANDRA; SINGARAVEL MOHAN; CHHIPA LAXMIKANT; KASUNDRA ASHOK 权利人:TORRENT PHARMACEUTICALS LTD 摘要:The present invention is directed to methods of producing substituted pyrazole based compounds through novel intermediates and unique processes for preparing such intermediates which enables synthesis of final product through commercially viable route of synthesis. The present invention is also directed to novel methods of producing substituted pyrazole based thyroid like compounds, and solid forms of 3-{4-[(7-hydroxy-6-methyl-indan-4-yl)methyl]-3,5-dimethyl-1H-pyrazol-1-yl}-propanoic acid, its pharmaceutical compositions, and methods of preparation thereof.
专利号:US-2003144441-A1 优先权日:2001-11-13 标题 :Controlled copolymerization of methyl acrylate with olefins under mild conditions 发明人:SEN AYUSMAN; ELYASHIV-BARAD SHARON; LIU SHENGSHENG 摘要:A copper-mediated process for the synthesis of random copolymers of methyl acrylate with non-polarolefins, ranging from ethene to 1-octene, norbornene and norbornene derivatives, and capable of synthesizing copolymers having greater than 5% incorporation of the olefin, as well as copolymers synthesized using the process are described. The process displays many of the characteristics of a living polymerization process: the polydispersities of the copolymers obtained are less than about 1.7, preferably from about 1.1 to about 1.4, and it is possible to synthesize novel block terpolymers of methyl acrylate with olefins by the sequential addition of the latter monomers.
专利号:US-8653238-B2 优先权日:2006-02-27 标题:Compositions and methods for transport of molecules with enhanced release properties across biological barriers 发明人:WENDER PAUL A; GOUN ELENA A; JONES LISA R 权利人:WENDER PAUL A; GOUN ELENA A; JONES LISA R; UNIV LELAND STANFORD JUNIOR 摘要:Conjugates of a cargo molecule with a transporter molecule are disclosed, where the cargo molecule and the transporter molecule are linked covalently by a releasable linker. The cargo of the conjugate can be a biologically active agent or a reporter molecule. The transporter modulates the transport of the cargo across a biological barrier (e.g., a cell membrane) compared to the transport of the unconjugated cargo. Releasable linkers suitable for rapid and facile conjugation to various types of cargo and transporters are also disclosed, along with methods for using the linkers in the synthesis of conjugates.
专利号:US-11512097-B2 优先权日:2019-11-25 标题 :Heterocyclic compounds as Delta-5 desaturase inhibitors and methods of use 发明人:ALLEN JENNIFER R; BELTRANI MICHELA; BOURBEAU MATTHEW P; DAMYANOVA TEODORA P; LINGARD IAIN; MINATTI ANA E; VINCETTI PAOLO 权利人:AMGEN INC 摘要:The present disclosure provides compounds useful for the inhibition of Delta-5 Desaturase (“D5Dâ€?). The compounds have a general Formula I n nwherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a metabolic or cardiovascular disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:WO-2008148560-A1 优先权日:2007-06-07 标题 :New hybrid compounds of nucleobases and organic redox molecules and their use 发明人:ASAFTEI SIMONA CARMEN 权利人:UNIV OSNABRUECK; ASAFTEI SIMONA CARMEN 摘要:The present invention relates to new compounds as well as methods for the synthesis of the same, said compounds comprise a redox active group, e.g. a 4,4-bipyridine (viologen), a 1,2-di(4-pyridyl)ethane, a 2,7-diazapyrene or 2,9-diazaperylene group and a N-heterocyclic nucleobase (HB), also referred to as base.
摘要:Amatore, M.; Aubert, C.; Malacria, M.; Petit, M., Science of Synthesis Knowledge Updates, (2012) 3, 57. 摘要:Kawęcki, R., Science of Synthesis Knowledge Updates, (2018) 4, 256. 摘要:Shu, X.-Z.; Pang, X., Science of Synthesis: Special Topics, (2022) 1, 436.