专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-8273403-B2 优先权日:2002-05-10 标题 :Generation of surface coating diversity 发明人:BARDEN MICHAEL C; KAMBOURIS PETER A 权利人:BARDEN MICHAEL C; KAMBOURIS PETER A; BIO LAYER PTY LTD 摘要:This invention relates to a surface discovery system and high-throughput combinatorial synthesis methods for generating large numbers of diverse surface coatings on solid substrates. The system is built upon a synthon which comprises at least three elements: a chemical backbone coating on the solid substrate that comprises a copolymer (B) of at least one passive constituent (P) and at least one active constituent (A); a spacer unit (S) separating the backbone from a functional group; and a functional group (F). The methods comprise the following steps: 1) selecting a plurality of synthons so that each synthon has at least two points of diversity selected from P, A, S and F; 2) applying copolymer B onto a substrate; and 3) attaching a combination of S and F to constituent A of copolymer B. Steps 2) and 3) are performed such that different synthons are generated on localized regions of the substrate.
专利号:US-6562844-B2 优先权日:1998-01-23 标 题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-9217012-B2 优先权日:2009-04-08 标题 :Inhibitors of protein tyrosine phosphatases 发明人:ZHANG ZHONG-YIN; ZHANG SHENG 权利人:ZHANG ZHONG-YIN; ZHANG SHENG; UNIV INDIANA RES & TECH CORP 摘要:Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.
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-7002020-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
[参考文献]: Masayuki Iwakubo, Et Al. Design And Synthesis Of Rho Kinase Inhibitors (Ii). Bioorg Med Chem. 2007 Jan 1;15(1):350-64.
合成参考文献
参考文献:10.1007/s11030-013-9450-1 摘要:Camarasa M, Barnils C, Puig de la Bellacasa R, Teixidó J, Borrell JI. A new and practical method for the synthesis of 6-aryl-5,6-dihydropyrido[2,3- $$d$$ d ]pyrimidine-4,7(3 $$H$$ H ,8 $$H$$ H )-diones. Mol Divers. 2013 May 26;17(3):525–36. doi: 10.1007/s11030-013-9450-1.