专利号:US-2009099267-A1 优先权日:2005-05-27 标题 :Polymers, compositions and methods of making the same 发明人:KUMAR RAJESH; KUMAR JAYANT; PARMAR VIRINDER SINGH; WATTERSON ARTHUR C 权利人:UNIV MASSACHUSETTS 摘要:Polymers having a main chain having both aromatic units and aliphatic units (with repeating heteroatoms) and a side chain macromonomer are described. Methods of making these polymers using enzymatic synthesis and the applications of these polymers are also described.
专利号:US-6020341-A 优先权日:1994-12-01 标题 :Enediyne quinone imines and methods of preparation and use thereof 发明人:DANISHEFSKY SAMUEL J; SHAIR MATTHEW D; YOON TAEYOUNG; CHOU TING-CHAO; MOSNY KAROLINE K 权利人:SLOAN KETTERING INST CANCER 摘要:A quinone imine enediyne possessing cytotoxic activity towards cancer cells having general structure (I) wherein R 1 , R 2 and R 3 are independently the same or different and are H, Br, Cl, F, NH 2 , CO 2 H, OH, linear or branched alkyl, etc.; wherein R 4 is H, OH or linear or branched alkoxy, linear or branched alkoxycarbonyl, etc.; wherein R 5 is H, Br, Cl, F, Oâ•?, OH or S--SR, or linear or branched alkyl, etc.; wherein R 6 is H, Br, Cl, F, CO 2 H, OH or S--SR', or linear or branched alkyl, etc.; wherein R 7 is H, OH or S--SR', or linear or branched alkyl, linear or branched alkoxycarbonyl, linear or branched alkoxy or linear or branched hydroxyalkyl; and wherein R, R' and R' are independently the same or different and are linear or branched alkyl, linear or branched acyl or linear or branched alkoxyalkyl. Also provided are conjugates of the compound with cleavable peptides, enzymes, carbohydrates and monoclonal antibodies immunoreactive with cancer cells, as well as compositions comprising the analogues and conjugates, and methods of synthesis and treatment of tumos.
专利号:EP-1957644-B1 优先权日:2005-12-01 标 题 :Enzymatic encoding methods for efficient synthesis of large libraries
专利号:EA-002100-B1 优先权日:1996-12-23 标题:CYCLOALCYL COMPOUNDS, LACTAMS, LACTONES AND RELATED COMPOUNDS CONTAINING THEIR PHARMACEUTICAL COMPOSITIONS AND METHODS OF INHIBITING THE SURVIVAL AND / OR SYNTHESIS OF β-AMYLOUS PEPTIDE SOFTWARE AGREED SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE AND SOFTWORK
专利号:US-5753458-A 优先权日:1994-06-10 标 题:Acylation method for penicillins and cephalosporins 发明人:CLAUSEN KIM; NIELSEN ANNETTE; PETERSEN NIELS; NIKOLOV ALEXANDER 权利人:GIST BROCADES BV 摘要:PCT No. PCT/EP95/02277 Sec. 371 Date Jan. 7, 1996 Sec. 102(e) Date Jan. 7, 1996 PCT Filed Jun. 12, 1995 PCT Pub. No. WO95/34675 PCT Pub. Date Dec. 21, 1995A method for providing a semisynthetic beta -lactam antibiotic by enzyme catalyzed acylation of the parent beta -lactam with an activated derivative of the side chain acid wherein a modulator, which consists of one or more compounds different from the reactants and the reaction product and which suppresses the hydrolysis of the activated derivative of the side chain acid and the desired product more than it suppresses the synthesis of the desired product, is added to the reaction mixture, at the beginning of the reaction process, in a concentration from about 0.2 to 100x103 mu m.\\!
专利号:US-9878999-B2 优先权日:2011-03-24 标题 :Proteasome chymotrypsin-like inhibition using PI-1833 analogs 发明人:LAWRENCE HARSHANI R; SEBTI SAID M; OZCAN SEVIL 权利人:H LEE MOFFITT CANCER CT & RES 摘要:Focused library synthesis and medicinal chemistry on an oxadiazole-isopropylamide core proteasome inhibitor provided the lead compound that strongly inhibits CT-L activity. Structure activity relationship studies indicate the amide moiety and two phenyl rings are sensitive toward synthetic modifications. Only para-substitution in the A-ring was important to maintain potent CT-L inhibitory activity. Hydrophobic residues in the A-ring's para-position and meta-pyridyl group at the B-ring significantly improved inhibition. The meta-pyridyl moiety improved cell permeability. The length of the aliphatic chain at the para position of the A-ring is critical with propyl yielding the most potent inhibitor, whereas shorter (i.e. ethyl, methyl or hydrogen) or longer (i.e. butyl, propyl and hexyl) chains demonstrating progressively less potency. Introduction of a stereogenic center next to the ether moiety (i.e. substitution of one of the hydrogens by methyl) demonstrated chiral discrimination in proteasome CT-L activity inhibition (the S-enantiomer was 35-40 fold more potent than the R-enantiomer).
[参考文献]: Choolakadavil Khalid Najeeb, Et Al. Highly Efficient Individual Dispersion Of Single-Walled Carbon Nanotubes Using Biocompatible Dispersant. Colloids Surf B Biointerfaces. 2013 Feb 1:102:95-101. [参考文献]: M Benezra, Et Al. A Synthetic Heparin-Mimicking Polyanionic Compound Binds To The Ldl Receptor-Related Protein And Inhibits Vascular Smooth Muscle Cell Proliferation. J Cell Biochem. 2001;81(1):114-27. [参考文献]: Yun-Loung Lin, Et Al. Design, Synthesis, And Evaluation Of Postulated Transient Intermediate And Substrate Analogues As Inhibitors Of 4-Hydroxyphenylpyruvate Dioxygenase. Bioorg Med Chem Lett. 2002 Jul 8;12(13):1709-13.
合成参考文献
参考文献:10.1007/bf01577691 摘要:Chang LT, McGrory EL, Elander RP. Penicillin production by glucose-derepressed mutants ofPenicillium chrysogenum. Journal of Industrial Microbiology & Biotechnology. 1990 Nov;6(3):165–9. doi: 10.1007/bf01577691.