CAS: 220810-26-4; Histrelin Acetate

该化合物是主要用于医疗领域的合成化学化合物,被归类为激素剂,具体而言,是一种GnRH(激素激素)模拟剂.Vantas用于治疗对激素敏感的病症,如前列腺癌,禁止生产某些激素,促进肿瘤生长.合成天然GNRH,导致润滑激素和泡泡激素分泌减少,从而降低雄性睾酮水平.Vantas通常通过亚切植入进行,长期持续释放活性成分.其药性肿瘤和药性动力学旨在确保对激素相关疾病进行有效管理,同时尽量减少副作用.与任何药物一样,必须监测病人可能与其他药物发生不良反应和相互作用的情况.

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    专利信息


    专利号:US-8633204-B2
    优先权日:2006-09-15
    标 题 :4-methylpyridopyrimidinone compounds
    发明人:CHENG HENGMIAO; BHUMRALKAR DILIP; DRESS KLAUS RUPRECHT; HOFFMAN JACQUI ELIZABETH; JOHNSON MARY CATHERINE; KANIA ROBERT STEVEN; LE PHUONG THI QUY; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; PLEWE MICHAEL BRUNO; TRAN KHANH TUAN
    权利人:CHENG HENGMIAO; BHUMRALKAR DILIP; DRESS KLAUS RUPRECHT; HOFFMAN JACQUI ELIZABETH; JOHNSON MARY CATHERINE; KANIA ROBERT STEVEN; LE PHUONG THI QUY; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; PLEWE MICHAEL BRUNO; TRAN KHANH TUAN; PFIZER
    摘要:The present invention is directed to novel 4-methylpyridopyrimidinone compounds of Formula (I), n nand to salts thereof, their synthesis, and their use as inhibitors of phosphoinositide 3-kinase alpha (PI3-Kα).

    专利号:US-11319320-B2
    优先权日:2017-11-06
    标题:PIM kinase inhibitor compositions, methods, and uses thereof
    发明人:BURK MARK J; CHEN BRANDON; LI JINGYI; BACHAN SHAWN
    权利人:SNAP BIO INC
    摘要:This application relates to compounds of formulae (I) and (II) and compositions thereof useful as inhibitors of PIM kinases. Also provided are methods of synthesis and methods of use of PIM inhibitors in treating individuals suffering from cancerous malignancies.

    专利号:US-8080556-B2
    优先权日:2008-08-13
    标 题 :2-amino pyrimidine compounds as potent HSP-90 inhibitors
    发明人:KUNG PEI-PEI; MENG JERRY JIALUN
    权利人:KUNG PEI-PEI; MENG JERRY JIALUN; PFIZER
    摘要:The present invention is directed to compounds of formula (I), n nor pharmaceutically acceptable salts thereof, their synthesis, and their use as HSP-90 inhibitors.

    专利号:FR-2956816-A1
    优先权日:2010-03-01
    标 题 :USE OF QUINOLONES FOR THE PREPARATION OF MEDICAMENTS, NEW QUINOLONES AND THEIR METHOD OF SYNTHESIS

    专利号:EP-2118111-B1
    优先权日:2007-02-06
    标题 :2-amin0-5, 7-dihydr0-6h- pyrrolo [3, 4-d] pyrimidine derivatives as hsp-90 inhibitors for treating cancer
    发明人:BENNETT MICHAEL JOHN; ZEHNDER LUKE RAYMOND; NINKOVIC SACHA; KUNG PEI-PEI; MENG JERRY JIALUN; HUANG BUWEN
    权利人:PFIZER
    摘要:The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, their synthesis, and their use as HSP-90 inhibitors.

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    主要参考文献


    1: Lewis KA, Goldyn AK, West KW, Eugster EA. A single histrelin implant is effective for 2 years for treatment of central precocious puberty. J Pediatr. 2013 Oct;163(4):1214-6. doi: 10.1016/j.jpeds.2013.05.033. Epub 2013 Jul 1. doi: 10.1016/j.jpeds.2013.01.021. Epub 2013 Feb 26. doi: 10.1016/j.jpeds.2012.08.038. Epub 2012 Oct 3. doi: 10.1111/j.1464-410X.2011.10370.x. Epub 2011 Aug 18. doi: 10.1210/jc.2009-2078. Epub 2010 Mar 25. doi: 10.2165/11204800-000000000-00000. Review. doi: 10.1097/SMJ.0b013e3181c376a6. doi: 10.1155/2009/812517. Epub 2009 Feb 26.
    10: Lewis KA, Eugster EA. Experience with the once-yearly histrelin (GnRHa) subcutaneous implant in the treatment of central precocious puberty. Drug Des Devel Ther. 2009 Sep 21;3:1-5.

    合成参考文献


    参考文献:10.1016/j.drudis.2016.02.015
    摘要:Chen M, Suzuki A, Thakkar S, Yu K, Hu C, Tong W. DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. Drug Discov Today. 2016 Apr;21(4):648–53. doi: 10.1016/j.drudis.2016.02.015.
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