CAS: 34973-08-5; Gonadorelin Acetate

该化合物是一种合成的脱脂性激素(GnRH)模拟物,与内生激素相同,具有氨基酸序列,与内生激素相同,在垂体干燥腺上活动,刺激润滑荷尔蒙(LH)和刺激激素(FSH)的释放,使其在生殖内分泌学的研究和临床应用中具有价值.乙酸盐形式增强稳定性和溶性,确保实验室和治疗环境中的可靠性能.其高纯度和精确的生物活动使得对低血压-皮下心血管-角轴轴调节进行有控制的研究.Gonadorelin 乙酸盐在生育治疗,诊断测试和荷尔蒙反馈机制研究中广泛使用.

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欧盟法规

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合成工艺路线路线简述

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    专利信息


    专利号:WO-2023030277-A1
    优先权日:2021-08-30
    标 题:Method for fully liquid-phase synthesis of grnh nonapeptide amide analog
    发明人:SUN PENGCHENG; PAN JING; WU JUNYONG; TANG YONGBO; Du Yixiong; GUO LIN
    权利人:HUNAN MICRO PEPTIDE BIOMEDICAL CO LTD
    摘要:Provided is a method for fully liquid-phase synthesis of a GRnH nonapeptide amide analog, which belongs to the technical field of medicine synthesis. The method comprises respectively synthesizing a 'Trp-Ser-Tyr' fragment, an 'R-Leu' fragment, a 'Pyr-His' fragment and 'Arg-Pro-Hunan T', wherein, R = D-Ala (alarelin), D-Leu (leuprorelin), D-Trp (deslorelin) and D-His (histrelin), and obtaining the GRnH nonapeptide amide analog with high yield and high purity by means of a '3 +2 +2 +2' fragment condensation method. The synthesis method is environmentally friendly, mild, and free of any highly toxic and poisonable reagents. The cost is greatly reduced and the synthesis method is very suitable for large-scale production.

    专利号:US-12383499-B2
    优先权日:2018-01-01
    标题:Scale up synthesis of silicasome nanocarriers
    发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
    权利人:UNIV CALIFORNIA
    摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

    专利号:US-11858901-B2
    优先权日:2019-10-30
    标 题:3-((R)-2-(amino-2-phenylethyl)-1-(2-fluoro-6 trifluoromethyl benzyl)-5-iodo-6-methyl-1H-pyrimidine-2,4-dione or a salt thereof, process for its preparation, and its use in the synthesis of elagolix
    发明人:BALLETTE ROBERTO; JIMÉNEZ ALONSO OSCAR; GARCÃ?A GARCÃ?A ELENA; DOBARRO RODRÃ?GUEZ ALICIA
    权利人:MOEHS IBERICA SL
    摘要:A new intermediate is useful in the synthesis of elagolix. A process for obtaining the intermediate includes reacting a precursor with iodine monochloride in the presence of an organic solvent. A process for preparing elagolix makes use of the intermediate. The intermediate can be 3-((R)-2-(amino-2-phenylethyl)-1-(2-fluoro-6-trifluoromethylbenzyl)-5-iodo-6-methyl-1H-pyrimidine-2,4-dione or a salt thereof, such as a hydrochloride.

    专利号:US-2022233673-A1
    优先权日:2019-06-04
    标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
    发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
    权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
    摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

    专利号:US-11649285-B2
    优先权日:2016-08-03
    标题 :Identification of VSIG3/VISTA as a novel immune checkpoint and use thereof for immunotherapy
    发明人:KALABOKIS VASSILIOS; WANG JINGHUA; WU GUOPING; BAZAN JOSE FERNANDO; VALLEY CHRISTOPHER CARLIN
    权利人:BIO TECHNE CORP
    摘要:The ligand for VISTA is identified (VSIG3) as well as the use of this ligand and receptor interaction in the identification or synthesis of a VSIG3 agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG3 and/or VISTA and/or the VSIG3/VISTA interaction. These antagonists may be used to suppress VSIG3/VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VSIG3/VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.

    专利号:US-12383520-B2
    优先权日:2019-05-16
    标 题 :Compound and composition for use in the treatment of premenstrual syndrome and/or premenstrual dysphoric disorder
    发明人:DANHIER PHILIPPE; AZZAM PASCALE
    权利人:SYNAPHARM IND SYNTHESIS
    摘要:This invention pertains to a compound and a composition for use in the treatment of premenstrual syndrome and/or premenstrual dysphoric disorder.
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    主要参考文献


    1: Li CX, Tang ST, Zhang Q. Changes in Bone Mineral Density and Metabolic Parameters after Pulsatile Gonadorelin Treatment in Young Men with Hypogonadotropic Hypogonadism. Int J Endocrinol. 2015;2015:324524. doi: 10.1155/2015/324524. Epub 2015 Aug 31.
    2: Akın O, Yavuz ST, Hacıhamdioğlu B, Sarı E, Gürsel O, Yeşilkaya E. Anaphylaxis to gonadorelin acetate in a girl with central precocious puberty. J Pediatr Endocrinol Metab. 2015 Nov 1;28(11-12):1387-9. doi: 10.1515/jpem-2015-0183. doi: 10.1016/j.theriogenology.2015.04.002. Epub 2015 Apr 14. doi: 10.1016/j.theriogenology.2015.03.004. Epub 2015 Mar 14. doi: 10.1002/oby.21010. Epub 2015 Feb 3. doi: 10.15653/TPG-140315. Epub 2014 Nov 17. German. Review. Chinese. doi: 10.1158/1940-6207.CAPR-13-0345. Epub 2014 Jan 15.
    9: Shanehsazzadeh S, Lahooti A, Sadeghi HR, Jalilian AR. Estimation of human effective absorbed dose of 67Ga-cDTPA-gonadorelin based on biodistribution rat data. Nucl Med Commun. 2011 Jan;32(1):37-43. doi: 10.1097/MNM.0b013e328340b916. doi: 10.1016/j.theriogenology.2009.02.016. Epub 2009 Apr 24. Epub 2007 Oct 30. Epub 2007 Mar 14. Dutch. No:25-7. Review. French. Chinese.

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    摘要:Drugs in Japan, -(404), 1990
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