CAS: 62087-72-3; Human Ige Pentapeptide Hepp

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合成工艺路线路线简述

    📜N-Carbobenzoxy-O-Benzyl-L-Aspartyl-O-Benzyl-L-Seryl-L-Aspartyl-L-Prolyl-L-Arginine置于钯 氮,氢气体系中,用 乙酸铵 作为反应溶剂,15.0~25.0 °C,59.47 Mpa 条件下,反应 16.0H,反应生成 喷替吉肽
    参考文献:Pentapeptide Synthesis
    标题:Pentapeptide Synthesis
    摘要:本发明揭示了一种合成商业数量的五肽l-天冬氨酸-L-丝氨酸-L-天冬氨酸-L-脯氨酰-L-精氨酸及其盐或溶剂合物(例如盐酸盐或醋酸盐或水溶剂),这些化合物在制药组合物中用于治疗过敏症状,同时还揭示了在合成过程中产生的新型中间化合物.

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    专利信息


    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.

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    主要参考文献


    1: Mansmann HC Jr, Rosen J, Ziering R, Hampel F, Ratner P, Findlay S, Kniker W, Haddad Z, Daigle A. Pentigetide nasal solution: a multicenter study evaluating efficacy and safety in patients with seasonal allergic rhinitis. Ann Allergy. 1991 Oct;67(4):409-15. 66(5):393-8. 68(1):68. 37(4):133-5. Spanish. 91(2):446-50. doi: 10.1016/0003-2697(78)90530-4.
    374:153-65. doi: 10.1016/j.gene.2006.01.027. Epub 2006 Mar 20. 4(4):298-302. doi: 10.1248/cpb1953.4.298. 27(3):206-12.
    9: Cohen GA, O'Connor RD, Hamburger RN. Safety and efficacy of human IgE pentapeptide. Ann Allergy. 1984 Feb;52(2):83-6. 58(5):332-5. 77(18-19):587-8. Undetermined Language. 37(3):101-4. Spanish. 92(3):182-94. French.

    合成参考文献


    参考文献:10.1007/978-94-010-9060-5_366
    参考文献:10.1007/978-94-010-9060-5_151
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