专利号:US-2009318476-A1 优先权日:2006-08-09 标 题 :Azacycloalkane Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase 发明人:RAMTOHUL YEEMAM K 权利人:MERCK FROSST CANADA LTD 摘要:Azacycloalkane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis. Formula (I).
专利号:US-2008032288-A1 优先权日:2004-03-26 标题:Labeling Reagents, Methods for the Synthesis of Such Reagents and Methods for the Detection of Biological Molecules
专利号:US-5576427-A 优先权日:1993-03-30 标 题 :Acyclic nucleoside analogs and oligonucleotide sequences containing them 发明人:COOK PHILIP D; DELECKI DANIEL J; GUINOSSO CHARLES 权利人:STERLING WINTHROP INC 摘要:Compounds of formula I; I wherein R1 is hydrogen, or a blocking group that is compatible with oligonucleotide synthesis; R2 is hydrogen, nitro, lower alkyl amino, diloweralkyl amino or methyl; R3 is hydrogen or -P(R4)OR5; R4 is chlorine, 4-nitroimidazole, imidazole, tetrazole, triazole or di(lower-alkyl)amino-; R5 is methyl, 2-cyanoethyl or 2,2,2-trichloroethyl; n is from 0 to 2 X is oxygen, sulfur, or -NR6; R6 is hydrogen or lower alkyl; Q is chosen from the group consisting of and R7 is lower-alkyl or loweralkyloxy methylene; and R8 is hydrogen, benzoyl, anisoyl, or lower-alkyl carbonyl and its pharmaceutically acceptable addition salts are nucleotide analogs. Modified oligonucleotides containing the nucleoside analogs of formula I are stable to nuclease degradation and are useful in inhibiting gene expression, in sequencing, and in mutagenesis.
[参考文献]: E A Véliz, Et Al. 6-Bromopurine Nucleosides As Reagents For Nucleoside Analogue Synthesis. J Org Chem. 2001 Dec 14;66(25):8592-8. [参考文献]: Eva Galante, Et Al. Chelator-Accelerated One-Pot 'Click' Labeling Of Small Molecule Tracers With 2-[1F]Fluoroethyl Azide. Molecules. 2013 May 10;18(5):5335-47.