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-2020354404-A1 优先权日:2019-05-09 标 题 :Peptidomimetic agents, synthesis and uses thereof 发明人:AL-ABED YOUSEF 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
专利号:US-9034576-B2 优先权日:2009-09-24 标题 :Systems and methods for measuring translation of target proteins in cells 发明人:SMILANSKY ZEEV; COOPERMAN BARRY S; GOODMAN YALE E 权利人:SMILANSKY ZEEV; COOPERMAN BARRY S; GOODMAN YALE E; ANIMA CELL METROLOGY INC 摘要:The present invention relates to systems and methods for measuring the rate of translation of a target protein in cells, which are based on the detection of translation of one or more predetermined codon pairs during synthesis of the target protein. The detection is provided by a FRET signal emitted from labeled tRNA molecules which are juxtaposed during synthesis of the protein.
专利号:US-5212287-A 优先权日:1988-12-21 标题:Pentapeptide synthesis 发明人:TOLLE JOHN C; GIFFORD WENYING Z; FUNK KENNETH W 权利人:IMMUNETECH PHARMACEUTICALS INC 摘要:A method of synthesizing commercial quantities of the pentapeptide L-aspartyl-L-seryl-L-aspartyl-L-prolyl-L-arginine, and salts or solvates thereof, e.g., the hydrochloride or acetate salt or water solvate, compounds useful in pharmaceutical compositions for the treatment of allergic conditions, is disclosed, as are novel intermediate compounds produced in the course of the synthesis.
专利号:US-5252464-A 优先权日:1989-03-14 标题:Process for producing pentapeptides and intermediates for use in the synthesis 发明人:ANDERSEN ANDERS J 权利人:CARLSBERG BIOTECHNOLOGY LTD 摘要:Pentapeptides having the formula H-Asp-Ser-C-Pro-Arg-OH, where Asp, Ser, Pro and Arg may have L- or D-configuration, and C denotes Asp or Asn in L or D configuration, are synthesized by reacting in an aqueous medium Y 2 -Pro-OH, wherein Y 2 is a protective group, with Arg-Ro, wherein Ro is OH or is as defined below for R 1 below, to form Y 2 -Pro-Arg-Ro, which is deprotected, if necessary under conversion to Pro-Arg-R 1 , wherein R 1 is an enzymatically cleavable α- carboxy substituting group selected form esters, amides, anilides, hydrazides or L-amino acid esters, and thereafter reacting Y 3 -C(Z 3 )-OH with Pro-Arg-R 1 to form Y 3 -C(Z 3 )-Pro-Arg-R 1 which is deprotected to C-Pro-Arg-R 1 , and then reacting Y 4 -Ser-OH with C-Pro-Arg-R 1 to form Y 4 -Ser-C-Pro-Arg-R 1 , which is deprotected to Ser-C-Pro-Arg-R 1 , and reacting Y 5 -Asp(Z 5 )-OH with Ser-C-Pro-Arg-R 1 to form Y 5 -Asp(Z 5 )-Ser-C-Pro-Arg-R 1 , which is deprotected to the intermediate Asp-Ser-C-Pro-Arg-R 1 , and finally removing the group R 1 with an enzyme, preferably trypsin to form Asp-Ser-C-Pro-Arg, or removing R.sub. 1 from Y 5 -Asp(Z 5 )-Ser-C-Pro-Arg-R 1 before deprotection to Asp-Ser-C-Pro-Arg-OH. n The groups Y 2 , Y 3 , Y 4 , Y 5 , Z 3 and Z 5 are protective groups which apart from Y 2 are removable by catalytic hydrogenation. The employed synthesis strategy based on the combination hydrogenation/enzyme, both proceeding under mild conditions, leads to the peptides, in particular HEPP, in good yield without risk of formation of β-aspartyl peptides and cleavage of Asp-Pro bonds.