专利号:US-5446158-A 优先权日:1989-01-11 标题:Process for synthesis of FK-506 and tricarbonyl intermediates 发明人:JONES TODD K; MILLS SANDER G; ASKIN DAVID; REAMER ROBERT A; DESMOND RICHARD; TSCHAEN DAVID M; VOLANTE RALPH P; SHINKAI ICHIRO 权利人:MERCK & CO INC 摘要:A process is described for the total synthesis of the macrolide immunosuppressant, FK-506, and important tricarbonyl process intermediates thereof. The tricarbonyl intermediates can be produced by the mild oxidation of 2,3-dihydroxy carboxylate compounds containing olefin moieties.
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-2018147294-A1 优先权日:2013-06-06 标 题:Antibody-drug conjugates, compositions and methods of use 发明人:JACKSON DAVID Y; HA EDWARD; PROBST GARY D 权利人:JACKSON DAVID Y; HA EDWARD; PROBST GARY D 摘要:Antibody-cytotoxin antibody-drug conjugates and related compounds, such as linker-cytotoxin conjugates and the linkers used to make them, tubulysin analogs, and intermediates in their synthesis; compositions; and methods, including methods of treating cancers.
专利号:EP-0378318-A1 优先权日:1989-01-11 标 题 :Process for synthesis of FK-506 and tricarbonyl intermediates
专利号:CA-2007490-A1 优先权日:1989-01-11 标 题:Process for synthesis of fk-506 and tricarbonyl intermediates
专利号:US-7199105-B2 优先权日:2002-08-15 标 题:Lincomycin derivatives possessing antibacterial activity 发明人:LEWIS JASON G; PATEL DINESH V; ANANDAN SAMPATH KUMAR; GORDEEV MIKHAIL F 权利人:VICURON PHARM INC 摘要:Novel lincomycin derivatives are disclosed. These lincomycin derivatives exhibit antibacterial activity. As the compounds of the subject invention exhibit potent activities against bacteria, including gram positive organisms, they are useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed.