专利号:US-12351573-B2 优先权日:2019-05-09 标 题:Compounds for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; CHENG KAI FAN 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.
专利号:US-2023159450-A1 优先权日:2020-05-08 标 题 :Dimers for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; ALTITI AHMAD 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.
专利号:US-5811515-A 优先权日:1995-06-12 标 题 :Synthesis of conformationally restricted amino acids, peptides, and peptidomimetics by catalytic ring closing metathesis 发明人:GRUBBS ROBERT H; MILLER SCOTT J; BLACKWELL HELEN E 权利人:CALIFORNIA INST OF TECHN 摘要:A method for synthesizing conformationally restricted amino acids, peptides, and peptidomimetics by ring closing metathesis. The method includes the steps of synthesizing a peptide precursor containing first and second unsaturated C--C bonds and contacting the peptide precursor with a RCM catalyst to yield a conformationally restricted peptide. Suitable peptide precursors may contain two or more unsaturated C--C bonds. These bonds may be olefinic bonds and may be contained in first and second alkenyl groups which may be allyl groups. The RCM catalyst may be a Ruthenium or Osmium carbene complex catalyst and more specifically, a Ruthenium or Osmium carbene complex catalyst that includes a Ruthenium or Osmium metal center that is in a +2 oxidation state, has an electron count of 16, and is pentacoordinated. The method may be carried out using solid-phase-peptide-synthesis techniques. In this embodiment, the precursor, which is anchored to a solid support, is contacted with a RCM catalyst and the product is then cleaved from the solid support to yield a conformationally restricted peptide.
专利号:US-12122759-B2 优先权日:2017-11-07 标 题:Method for the synthesis of cyclic depsipeptides 发明人:HEIMBACH DIRK; OMURA SATOSHI; SUNAZUKA TOSHIAKI; HIROSE TOMOYASU; NOGUCHI YOSHIHIKO; Köbberling Johannes; WU ZHIJIE; FU SHUIBIAO; WU WEI; QIU JINFENG; HE LIU; WEI XUDONG 权利人:ELANCO ANIMAL HEALTH GMBH; THE KITASATO INST 摘要:The present invention relates to a method for the synthesis of cyclic depsipeptides, in particular emodepside, from the open form.
专利号:US-7691635-B2 优先权日:2004-03-26 标题 :Labeling reagents, methods for the synthesis of such reagents and methods for the detection of biological molecules 发明人:LAAYOUN ALI; BERNAL-MENDEZ ELOY 权利人:BIOMERIEUX SA 摘要:The present invention relates to a temperature-stable labeling reagent of formula (0): n nin which:n R 1 represents H or an alkyl, aryl or substituted aryl group, R 2 represents a detectable marker or at least two detectable markers interlinked by at least one multimeric structure, L is a linker arm comprising a linear chain of at least two covalent bonds and n is an integer equal to 0 or 1, R 3 and R 4 represent, independently of one another: H, NO 2 , Cl, Br, F, I, R 2 -(L) n -Y—X—, OR, SR, NR 2 , R, NHCOR, CONHR, COOR, —CO—NH—(CH 2 ) 3 —(O—CH 2 —CH 2 ) 3 —CH 2 —NH—R 2 , —CO—NH—(CH 2 ) 3 —(O—CH 2 —CH 2 ) 4 —CH 2 —NH—R 2 with R=alkyl or aryl, A is a linker arm comprising at least one covalent double bond enabling the conjugation of the diazo function with the aromatic ring and u is an integer between 0 and 2, preferably 0 or 1, —Y—X— represents —CONH—, —NHCO—, —CH 2 O—, —CH 2 S—, —Z— represents —NH—, —NHCO—, —CONH— or —O—, m is an integer between 1 and 10, preferably between 1 and 3, and p is an integer between 1 and 10, preferably between 1 and 3. n The present invention also describes a method for the synthesis of said labels and also applications for the labeling of biological molecules, in particular of nucleic acids, with a labeling reagent bearing the diazomethyl function. n The invention is particularly suitable for use in the field of diagnostics.
专利号:WO-9726002-A1 优先权日:1996-01-17 标 题:Synthesis of conformationally restricted amino acids, peptides and peptidomimetics by catalytic ring closing metathesis 发明人:GRUBBS ROBERT H; MILLER J SCOTT; BLACKWELL HELEN E 权利人:CALIFORNIA INST OF TECHN 摘要:A method for synthesizing conformationally restricted amino acids, peptides, and peptidomimetics by ring closing metathesis. The method includes the steps of synthesizing a peptide precursor containing first and second unsaturated C-C bonds and contacting the peptide precursor with an RCM catalyst to yield a conformationally restricted peptide. Suitable peptide precursors may contain two or more unsaturated C-C bonds. These bonds may be olefinic bonds and may be contained in first and second alkenyl groups which may be allyl groups. The RCM catalyst may be a Ruthenium or Osmium carbene complex catalyst and more specifically, a Ruthenium or Osmium carbene complex catalyst that includes a Ruthenium or Osmium metal center that is in a +2 oxidation state, has an electron count of 16, and is pentacoordinated. The method may be carried out using solid-phase-peptide-synthesis techniques. In this embodiment, the precursor, which is anchored to a solid support, is contacted with an RCM catalyst and the product is then cleaved from the solid support to yield a conformationally restricted peptide.