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-2004127467-A1 优先权日:2002-04-17 标 题:Synthesis of pancratistatin prodrugs 发明人:PETTIT GEORGE R; ORR BRIAN; DUCKI SYLVIE 摘要:A new and efficient synthesis of the (+)-pancratistatin phosphate prodrug 2 a has been accomplished. Selective protection (tetraacetate 4 ) of (+)-pancratistatin ( 1 a ) was followed by phosphorylation (to 5 ) with dibenzyl chlorophosphite (prepared in situ from dibenzyl phosphite). Cleavage of the acetate (with sodium methoxide) and benzyl (by hydrogenolysis) protecting groups followed by concomitant reaction with two equivalents of sodium methoxide afforded good yield of disodium (+)-pancratistatin phosphate ( 2 a ). Further increases in yields of the prodrug ( 2 a ) were realized by avoiding heat in the final purification steps. Fourteen ( 2 b - o ) additional metal and ammonium derived phosphate prodrugs were also synthesized.
专利号:US-8268936-B2 优先权日:2005-01-04 标题:Synthesis of hybrid block copolymers and uses thereof 发明人:BREITENKAMP KURT; SILL KEVIN N 权利人:BREITENKAMP KURT; SILL KEVIN N; INTEZYNE TECHNOLOGIES INC 摘要:The present invention relates to the field of polymer chemistry and more particularly to multiblock copolymers and methods of preparing the same.
专利号:US-2012196989-A1 优先权日:2005-02-11 标题:Synthesis of homopolymers and block copolymers 发明人:BREITENKAMP KURT; SILL KEVIN N 权利人:BREITENKAMP KURT; SILL KEVIN N; INTEZYNE TECHNOLOGIES INC 摘要:The present invention relates to the field of polymer chemistry and more particularly to homopolymers and block copolymers and methods of preparing the same.
专利号:US-7320993-B1 优先权日:1997-12-17 标题 :Aryl-substituted pyridylalkane, alkene, and alkine carboxamides useful as cytostatic useful as cytostatic and immuosuppressive agents 发明人:BIEDERMANN ELFI; HASMANN MAX; LOESER ROLAND; RATTEL BENNO; REITER FRIEDEMANN; SCHEIN BARBARA; SEIBEL KLAUS; VOGT KLAUS; WOSIKOWSKI KATJA; SCHEMAINDA ISABEL 权利人:ASTELLAS DEUTSCHLAND GMBH 摘要:The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.
专利号:US-2006172914-A1 优先权日:2005-01-04 标题:Synthesis of hybrid block copolymers and uses thereof
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合成参考文献
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