专利号:US-10266565-B2 优先权日:2011-04-12 标 题 :Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG-EUN 权利人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG EUN; THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES 摘要:Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.
专利号:WO-2005103035-A1 优先权日:2004-04-23 标题:Modified fischer indole synthesis of eletriptan 发明人:ASHCROFT CHRISTOPHER PAUL 权利人:PFIZER LTD; ASHCROFT CHRISTOPHER PAUL; PFIZER 摘要:The present invention relates to a new process for the preparation of eletriptan (I), or its enantiomer comprising a modified Fischer indole synthesis, namely the reaction of a compound of formula (II), wherein R1 is a suitable hydrazine protecting group, with a compound of formula (III) wherein R2 is an aldehyde group (-CHO) or the functional equivalent thereof.
专利号:US-4567265-A 优先权日:1984-01-16 标题:Cyclopropanoid cyanoesters and method of making same 发明人:BABLER JAMES H 权利人:UNIV LOYOLA CHICAGO 摘要:Cyclopropanoid cyanoesters of the formula: where R' is -CH3 or -CH2CH3, and A is (a) -H, or (b) A, B represents an aliphatic group joined to a carbon atom on the cyclopropanoid ring, thereby forming a spiro group, A, B being selected from structures having the formula: (i) -(CH2)n-, wherein n=3, 4, or 5, and (ii) -(CH2)2-Y-(CH2)2-, wherein Y is NCH3, O, or S); and, when A is -H, B is selected from the group consisting of: +TR (CH3)2CHCH2. are disclosed. These compositions are useful in the synthesis of pyrethroids. A process for synthesis of cyclopropanoid cyanoesters by reacting 2-nitropropane with cyanoesters of the general formula: is also disclosed and claimed.
专利号:US-7067622-B2 优先权日:2001-06-25 标题 :Method of the solid phase synthesis of pyrrole-imidazole polyamide 发明人:SUGIYAMA HIROSHI; IIDA HIROKAZU; SAITO ISAO; SAITO TAKASHI 权利人:JAPAN SCIENCE & TECH AGENCY 摘要:It is intended to provide a method of producing a pyrrole-imidazole polyamide whereby a longer pyrrole-imidazole polyamide can be conveniently synthesized and a peptide (protein) can be easily transferred. According to this method, a pyrrole-imidazole polyamide having a carboxylate group which can be excised from a solid phase carrier at its end, makes it possible to directly transfer various functional groups and can exactly distinguish DNA sequences can be efficiently produced. A method of synthesizing a pyrrole-imidazole polyamide characterized by performing automatic synthesis by the solid phase Fmoc method with the used of a peptide synthesizer; a pyrrole-imidazole polyamide having a carboxyl group at its end obtained by this method; a pyrrole-imidazole polyamide having a DNA alkylation agent transferred into the carboxyl group at the end of the above-described pyrrole-imidazole polyamide; and a sequence-specific DNA alkylation method characterized by using the above compound.
专利号:US-5783577-A 优先权日:1995-09-15 标题 :Synthesis of quinazolinone libraries and derivatives thereof 发明人:HOUGHTEN RICHARD A; OSTRESH JOHN M 权利人:TREGA BIOSCIENCES INC 摘要:The present invention provides synthetic combinatorial libraries of organic compounds based on the quinazolinone ring.
专利号:US-5175302-A 优先权日:1987-07-13 标 题 :Nucleophilic fluoroalkylation of aldehydes 发明人:STAHLY G PATRICK 权利人:ETHYL CORP 摘要:Aryl difluoromethyl sulfone adds to aldehydes under phase transfer conditions to give novel substituted alcohols of the general formula n n RCH(OH)CF.sub.2 SO.sub.2 Ar (I) n n wherein R is an aryl, cycloaliphatic, sec- or tert-aliphatic, or heterocyclic group and Ar is an aryl group. The substituted alcohols of formula I are of particular utility as intermediates in the synthesis of a variety of useful end products. For example, the products of formula I may be utilized in desulfonylation reactions, oxidation reactions and fluorination reactions.
[参考文献]: Yu Luo, Et Al. Design And Synthesis Of Novel Benzimidazole Derivatives As Inhibitors Of Hepatitis B Virus. Bioorg Med Chem. 2010 Jul 15;18(14):5048-55.
合成参考文献
参考文献:10.1107/s1600536811009214 摘要:Liu L, Li J, Shao Y. (E)-3-(1-Methyl-1H-pyrrol-2-yl)-1-phenylprop-2-en-1-one. Acta Crystallogr E Struct Rep Online. 2011 Mar 15;67(4):o894. doi: 10.1107/s1600536811009214.