专利号:US-5877278-A 优先权日:1992-09-24 标题:Synthesis of N-substituted oligomers 发明人:ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA 权利人:CHIRON CORP 摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.
专利号:US-2004028702-A1 优先权日:2002-07-26 标 题:Muramic acid derivative compounds 发明人:MALETIC MILANA M; LEEMAN AARON H; SANTORELLI GINA M; WADDELL SHERMAN T 摘要:The present invention pertains to the combinatorial synthesis of antibacterial agents that inhibit the Mur-pathway enzymes involved in bacterial cell wall assembly. The method uses p-alkoxybenzylidene as the linker for the attachment of a derivatized muramic acid to the polymeric resin support. This intermediate becomes the starting point for the combinatorial synthesis, which in conjunction with split-pooling techniques allows rapid synthesis of diverse analogues for high-throughput screening (HTS). The invention is further directed to the libraries of these finished compounds that vary at the peptide, N-acyl and anomeric UDP positions.
专利号:CN-115515998-A 优先权日:2020-05-06 标题 :Synthesis of Polyurethanes by Chain Growth Copolymerization
专利号:EP-0789577-A1 优先权日:1995-06-07 标 题:Synthesis of n-substituted oligomers
专利号:JP-2006182780-A 优先权日:1995-06-07 标 题 :Synthesis of N-substituted oligomers
专利号:EP-0789577-B1 优先权日:1995-06-07 标 题:Synthesis of n-substituted oligomers
摘要:Braverman, S.; Cherkinsky, M.; Birsa, M. L., Science of Synthesis, (2005) 18, 101. 摘要:Braverman, S.; Cherkinsky, M.; Birsa, M. L., Science of Synthesis, (2005) 18, 147. 摘要:Gilchrist, T. L., Science of Synthesis, (2005) 18, 1052. 摘要:Shcherbakova, I., Science of Synthesis, (2007) 31, 810.