专利号:US-2003180804-A1 优先权日:2001-10-29 标题:Solid phase synthesis of chemical libraries 发明人:PRYOR KENT E; LEWIS RONALD D; BROWN JASON W 权利人:CORVAS INT INC 摘要:The present invention provides compounds and compound libraries that are useful as protease modulators. The compounds and compound libraries are preferably made using the methods of the present invention which utilize peptide synthesis and combinatorial chemistry methods on a solid phase.
专利号:US-7244753-B2 优先权日:2002-07-29 标 题:Cyclooxygenase-2 selective inhibitors, compositions and methods of use 发明人:GARVEY DAVID S; KHANAPURE SUBHASH P; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D 权利人:NITROMED INC 摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
专利号:US-6441189-B1 优先权日:2000-03-31 标 题 :Process for the preparation of matrix metalloproteinase inhibitors 发明人:BAILEY ANNE E; HILL DAVID R; HSIAO CHI-NUNG W; KURUKULASURIYA RAVI; WITTENBERGER STEVE; MCDERMOTT TODD; MCLAUGHLIN MAUREEN A 权利人:ABBOTT LAB 摘要:The instant invention provides a process for the synthesis of matrix metalloproteinase inhibitors.
专利号:US-5684195-A 优先权日:1994-07-14 标 题:Method of preparing sulfmonamides from sulfones 发明人:HUANG HORNG-CHIH; HARRING SCOTT R 权利人:SEARLE & CO 摘要:A one-pot synthesis of sulfonamides from sulfones has been developed. Conversion of sulfones to the corresponding sulfinic acid salts is followed by oxidative-amination to give the sulfonamides.
专利号:US-4794108-A 优先权日:1984-04-24 标题:1-carboxymethoxy acetidinones and their production 发明人:KISHIMOTO SHOJI; SENDAI MICHIYUKI; OCHIAI MICHIHIKO 权利人:TAKEDA CHEMICAL INDUSTRIES LTD 摘要:A 2-azetidinone derivative having a group of the formula wherein R1 and R2 are the same or different and each represents a hydrogen atom, alkyl, aryl or arylalkyl which may have a substituent at the 1-position and an amino group, at the 3-position, which may be acylated or protected, its salt or ester, and methods of producing the same, (1) a method comprising subjecting a 2-azetidinone derivative having a group of the formula wherein the symbols are as defined above at the 1-position and an amino group at the 3-position, its salt or ester to an acylation or protective-group introduction reaction, and (2) a method comprising reacting a 2-azetidinone derivative having a hydroxy group at the 1-position and an amino group, at the 3-position, which may be acylated or protected, or its salt with a compound of the formula wherein W is a halogen atom; other symbols are as defined above, its salt or ester. The above objective compounds are utilizable as excellent antimicrobial agents or as valuable intermediates for the synthesis of the same.
专利号:US-7371852-B2 优先权日:2003-01-22 标 题 :Alkyl-linked nucleotide compositions 发明人:HARDEMAN KLASS P; HALL STEVEN E; WARE ROY W; HINKLEY LINDSAY A; JENKS MATTHEW G 权利人:SERENEX INC 摘要:Alkyl-linked nucleotide non-homogeneous solid supports and nucleotide affinity media comprising an alkyl-linked nucleotide are provided. The linker is generally a hydrophobic linker that can be a 3, 4, 5, 6, 7, 8, 9, 10, or a longer carbon chain. Also included in the invention are methods for synthesis of an alkyl-linked nucleotide, nucleotide affinity media and methods of use thereof for affinity chromatography and screening methods.
[参考文献]: Jiuxiang Zhu, Et Al. Using Cyclooxygenase-2 Inhibitors As Molecular Platforms To Develop A New Class Of Apoptosis-Inducing Agents. J Natl Cancer Inst. 2002 Dec 4;94(23):1745-57.
合成参考文献
摘要:Schatz, J.; Seler, M., Science of Synthesis Knowledge Updates, (2011) 2, 372.