专利号:US-2004014168-A1 优先权日:1998-06-11 标题:Reagents and methods for library synthesis and screening 发明人:SCHREIBER STUART L; BLACKWELL HELEN E; PEREZ FERNANDEZ LUCY; TALLARICO JOHN A 权利人:HUGHES HOWARD MED INST 摘要:The invention provides novel solid supports for the synthesis of compound libraries. The solid supports have the physical capacity to deliver at least 50 nmol of compound and are functionalized with a silicon-containing linker. In one embodiment of the invention the solid support comprises a bead having a diameter of between approximately 400 and 600 μm functionalized with a silicon-containing linker. According to certain embodiments of the invention the bead is a polystyrene bead. According to certain embodiments of the invention the linker is a diisopropylalkyl-substituted silyl ether. The invention further provides grafted polymeric supports such as lanterns functionalized with a silicon-containing linker. n The invention provides methods for screening in which compounds are synthesized on solid supports in a quantity so that a single solid support such as a bead provides a stock solution sufficient to perform hundreds or thousands of biological or chemical assays. The methods include decoding the sequence of chemical reactions used to synthesize the compound by identifying tags incorporated into the compound during synthesis.
专利号:US-6906046-B2 优先权日:2000-12-22 标题 :Pharmaceutical uses and synthesis of benzobicyclooctanes 发明人:JACKSON RANDY W; DARWISH IHAB; BAUGHMAN TED A; HOWBERT J JEFFRY 权利人:CELLTECH R & D INC 摘要:Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
专利号:US-6147159-A 优先权日:1998-09-30 标 题 :Compositions for organic synthesis on solid phase and methods of using the same 发明人:HU YONGHAN; LABADIE JEFFREY W; PORCO JR JOHN ANTHONY; TROST BARRY MARTIN 权利人:ARGONAUT TECHNOLOGIES 摘要:A modified solid support for use in solid phase synthesis which comprises: a solid support having a linker group extending therefrom having the general formula: wherein R1 and R2 are each independently selected from the group consisting of alkyl, cycloalkyl, aryl, alkoxy, aryloxy, fluorine, chlorine, iodine and bromine.
专利号:US-2004053999-A1 优先权日:1997-09-17 标题 :Novel compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; DAHL TERRENCE C; HITCHCOCK MICHAEL J M; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; MILLS ROGER G; WILLIAMS MATTHEW A 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
专利号:US-7186709-B2 优先权日:2002-08-27 标 题:Dihydropyrancarboxamides and uses thereof 发明人:SCHREIBER STUART L; STAVENGER ROBERT A; MITCHISON TIMOTHY J; MALIGA ZOLTAN 权利人:HARVARD COLLEGE 摘要:The present invention provides novel dihydropyrancarboxamide compounds of formula (I): n nand collections of these compounds, and provides methods for the synthesis of these compounds; wherein R 1 –R 6 are as defined herein. Additionally, the present invention provides pharmaceutical compositions and methods for treating disorders such as proliferative diseases, and cancer, to name a few.
专利号:US-6225341-B1 优先权日:1995-02-27 标 题:Compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; WILLIAMS MATTHEW A 权利人:GILEAD SCIENCES INC 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
[参考文献]: Tianlin Wang, Et Al. Modified Field Amplification Sample Injection For Micellar Electrokinetic Chromatography Of Neutral Compounds With Amino-Substituted Cyclodextrin As Carrier And 1-Adamantanecarboxylate As Displacer. J Chromatogr A. 2003 Sep 26;1013(1-2):19-27.
合成参考文献
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