专利号:US-6525061-B1 优先权日:1999-11-16 标题 :Methods for the solid phase synthesis of 2-amino-4(H)-quinazolinone derivatives 发明人:GOPALSAMY ARIAMALA; YANG HUI Y 权利人:WYETH CORP 摘要:The present invention relates to solid phase synthesis of substituted 2-amino-4(H)-quinazolinone compounds of formula (I):having pharmacological activity, to processes for their preparation, to a combinatorial library and solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, and to pharmaceutical compositions thereof.
专利号:US-2012189547-A1 优先权日:2009-10-08 标 题 :[18f] labelled analogues of flumazenil as in vivo imaging agents 发明人:WOODCRAFT JOHN; JONES CLARE L; GAETA ALESSANDRA; TRIGG WILLIAM JOHN; JONES PAUL ALEXANDER; PLANT STUART 权利人:WOODCRAFT JOHN; JONES CLARE L; GAETA ALESSANDRA; TRIGG WILLIAM JOHN; JONES PAUL ALEXANDER; PLANT STUART 摘要:The present invention provides radiofluorinated compounds useful for in vivo imaging GABA A receptors. Also provided by the present invention is a method of synthesis for the radiofluorinated compounds of the invention, in particular an automated method of synthesis. A further aspect of the invention is a cassette suitable for carrying out the automated method of synthesis of the invention.
专利号:US-6274383-B1 优先权日:1997-12-15 标题:Methods for synthesizing libraries of dihydro-quinazolinones 发明人:GAO YUN 权利人:SEPRACOR INC 摘要:Synthetic methods for solution and solid-phase synthesis of combinatorial libraries of dihydro-quinazolinones, including synthesis of 2,3-dihydro-3-alkoxy-4(1H)-quinazolinones or 2,3-dihydro-3-hydroxy-4(1H)-quinazolinones via the Lewis-acid catalyzed reaction of an appropriate 2-aminobenzamide with an aldehyde at ambient temperature performed on a solid support or in solution.
专利号:US-8946410-B2 优先权日:2009-10-08 标 题 :Automated radiosynthesis 发明人:WOODCRAFT JOHN; JONES L CLARE; GAETA ALESSANDRA; TRIGG JOHN WILLIAM; JONES ALEXANDER PAUL; PLANT STUART; JACKSON ALEXANDER 权利人:WOODCRAFT JOHN; JONES L CLARE; GAETA ALESSANDRA; TRIGG JOHN WILLIAM; JONES ALEXANDER PAUL; PLANT STUART; JACKSON ALEXANDER; GE HEALTHCARE LTD 摘要:The present invention provides a method to obtain radiofluorinated compounds useful for in vivo imaging GABA A receptors. The method of the invention is high-yielding and may conveniently be carried out on an automated synthesizer such as Fastlabâ„¢. A further aspect of the invention is a cassette suitable for carrying out the automated method of synthesis of the invention. Novel precursor compounds useful in the method of the invention are also provided, as are a number of novel compounds obtained by the method of the invention.