专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-5877296-A 优先权日:1994-06-03 标题:Process for preparing conjugates of methyltrithio antitumor agents 发明人:HAMANN PHILIP ROSS; HINMAN LOIS; HOLLANDER IRWIN 权利人:AMERICAN CYANAMID CO 摘要:This invention describes carrier-drug conjugates prepared from disulfide analogs of the calicheamicin family of potent antitumor antibiotics and their derivatives, as well as similar analogs from related antitumor antibiotics such as the esperamicins. The carrier can be an antibody, growth factor, or steroid which targets an undesired population of cells, such as those of a tumor. Whole protein carriers as well as their antigen-recognizing fragments and their chemically or genetically manipulated counterparts are useful for the targeting portion of the conjugates. This invention includes compounds required for the synthesis of these conjugates, appropriate pharmaceutical compositions of the carrier-drug conjugates, and their method of use.
专利号:US-5739116-A 优先权日:1994-06-03 标题:Enediyne derivatives useful for the synthesis of conjugates of methyltrithio antitumor agents
专利号:CN-101357137-A 优先权日:2007-03-26 标题 :Use of a vitreoscilla filiformis lipopolysaccharide fraction as an agent for stimulating the synthesis of anti-microbial skin peptides
专利号:EP-0766662-A1 优先权日:1994-04-22 标 题 :Asymmetric synthesis of (r)- and (s)-arylethanolamines from iminoketones
专利号:WO-9529146-A1 优先权日:1994-04-22 标 题:Asymmetric synthesis of (r)- and (s)-arylethanolamines from iminoketones