CAS: 66376-36-1; (4-Amino-1-Hydroxybutane-1,1-Diyl)Diphosphonic Acid

该化合物是主要用于治疗骨质疏松症和其他与骨头有关的紊乱的双磷化合物,抑制骨质疏松的中位吸附,从而增加骨质密度,降低骨折风险; 肾上腺酸的特点是其能够与骨头中的氢氧亚丙酸结合,这提高了其治疗效果; 该化合物通常以口头方式施用,以其生物利用率相对较低而闻名,需要具体的剂量说明,例如将其用在空腹部和全杯水中,在一段时间后保持直立,以尽量减少胃肠刺激; 肾上腺酸一般都得到很好的调制,但潜在的副作用可能包括胃肠道不适,肌肉骨骼疼痛,在稀有的情况下,还有卵巢的骨质固痛; 其化学结构包括磷酸组,这对于其生物活动至关重要,并且被归类为合成有机化合物.

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4-amino-n-butyric acid tetramethyl (4-phthalimido-1-hydroxybutylidene)bisphosphonate 4-phthalimidobutyryl chloride 2-pyrrolidinon sodium alendronate

合成工艺路线路线简述

    Sodium Alendronate置于盐酸,乙醇,水体系中,化学反应 2.0H,反应生成 阿仑膦酸
    参考文献: Antiresorptive Mutual Salt Of Raloxifene And Bisphosphonic Acid[fr] Sels Antiresorbants De Raloxifene Et D'Acide Biphosphonique
    标题: Antiresorptive Mutual Salt Of Raloxifene And Bisphosphonic Acid[fr] Sels Antiresorbants De Raloxifene Et D'Acide Biphosphonique
    摘要:来自拉洛西芬和双磷酸盐的相互盐表现出两种成分之间意想不到的协同效应,以增强骨密度(bmd),控制血钙密度并降低血清胆固醇水平.

    海关参考信息

    专利信息


    专利号:US-9353057-B2
    优先权日:2003-12-30
    标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
    发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
    权利人:XENOPORT INC
    摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

    专利号:WO-2025078505-A1
    优先权日:2023-10-13
    标 题 :One pot gmp scalable production method for the synthesis of dextran-guanidine-bisphosphonate conjugate
    发明人:HOLMBERG ANDERS R
    权利人:DEXTECH MEDICAL AB
    摘要:The disclosure relates to a large scale GMP synthesis of a modified dextran conjugate, and more particularly to a dextran-guanidine-bisphosphonate conjugate wherein the bisphosphonate is an alendronate group. The disclosure relates to a large scale GMP synthesis that produces high purity, pharmaceutical grade dextran-guanidine-bisphosphonate conjugate. The present disclosure further concerns the use of said dextran-guanidine-bisphosphonate conjugate in medicines treating tumors.

    专利号:US-12146136-B2
    优先权日:2020-03-26
    标题:Synthesis of modified oligonucleotides with increased stability
    发明人:KHVOROVA ANASTASIA; ROUX LOÃ?C MAURICE RENÉ JEAN; YAMADA KEN
    权利人:UNIV MASSACHUSETTS
    摘要:This disclosure relates to the synthesis of novel modified oligonucleotides. The synthesis of novel phosphoramidites are also provided.

    专利号:US-8178712-B2
    优先权日:2006-06-23
    标 题:Process for the synthesis of Ibandronate sodium
    发明人:RAO DHARAMARAJ RAMCHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI GANPATI
    权利人:RAO DHARAMARAJ RAMCHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI GANPATI; CIPLA LTD
    摘要:The present invention relates to an improved process for the synthesis of Ibandronate sodium of formula (I). The present invention also provides novel processes for the synthesis of 3-[N-(methylpentyl)amino]propionic acid (III).

    专利号:US-2024009660-A1
    优先权日:2022-07-05
    标题 :Methods for synthesis of hierarchically ordered crystalline microporous materials with long-range mesoporous order
    发明人:PARSAPUR RAJESH KUMAR; HODGKINS ROBERT PETER; KOSEOGLU OMER REFA; HUANG KUO-WEI; SEDJERARI ANISSA BENDJERIOU
    权利人:SAUDI ARABIAN OIL CO; UNIV KING ABDULLAH SCI & TECH
    摘要:Methods for synthesis of hierarchically ordered zeolites and zeolite-type materials are provided. Synthesized hierarchically ordered zeolites and zeolite-type materials formed according to the methods herein possess a high-degree of well-defined long-range mesoporous ordering. The methods include base-mediated reassembly, by dissolution of the parent material to the level of oligomeric structural building units of the parent material, and minimizing or avoiding amorphization/structural collapse. The dissolution and self-assembly is comprehensively controlled to produce hierarchically ordered zeolites and zeolite-type materials according to the methods herein.

    专利号:US-2024010662-A1
    优先权日:2022-07-05
    标题 :Methods for synthesis of hierarchically ordered crystalline microporous materials with long-range mesoporous order
    发明人:PARSAPUR RAJESH KUMAR; HODGKINS ROBERT P; KOSEOGLU OMER REFA; HUANG KUO-WEI; SEDJERARI ANISSA BENDJERIOU
    权利人:SAUDI ARABIAN OIL CO; UNIV KING ABDULLAH SCI & TECH
    摘要:Methods for synthesis of hierarchically ordered zeolites and zeolite-type materials are provided. Synthesized hierarchically ordered zeolites and zeolite-type materials formed according to the methods herein possess a high-degree of well-defined long-range mesoporous ordering. The methods include base-mediated reassembly, by dissolution of the parent material to the level of oligomeric structural building units of the parent material, and minimizing or avoiding amorphization/structural collapse. The dissolution and self-assembly is comprehensively controlled to produce hierarchically ordered zeolites and zeolite-type materials according to the methods herein.
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    主要参考文献


    1: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Available from http://www.ncbi.nlm.nih.gov/books/NBK501621/ doi: 10.2147/CLEP.S154914. eCollection 2018.
    3: Nsubuga A, Sgarzi M, Zarschler K, Kubeil M, Hübner R, Steudtner R, Graham B, Joshi T, Stephan H. Facile preparation of multifunctionalisable 'stealth' upconverting nanoparticles for biomedical applications. Dalton Trans. 2018 Jul 14;47(26):8595-8604. doi: 10.1039/c8dt00241j. Epub 2018 Apr 25. doi: 10.1016/j.coph.2018.03.010. Epub 2018 Apr 4. Review. doi: 10.1017/S0022215118000324. Epub 2018 Feb 28. Review. doi: 10.2106/JBJS.CC.16.00006. doi: 10.1039/c7nr07035g. doi: 10.2147/DDDT.S138286. eCollection 2017.
    9: Xie H, Chen G, Young RN. Design, Synthesis, and Pharmacokinetics of a Bone-Targeting Dual-Action Prodrug for the Treatment of Osteoporosis. J Med Chem. 2017 Aug 24;60(16):7012-7028. doi: 10.1021/acs.jmedchem.6b00951. Epub 2017 Aug 10. doi: 10.1016/j.addr.2017.07.003. Epub 2017 Jul 8. Review. doi: 10.1016/j.injury.2017.03.025. Epub 2017 Apr 4. pii: bcr2017219692. doi: 10.1136/bcr-2017-219692. doi: 10.11138/ccmbm/2016.13.3.209. Epub 2017 Feb 10.

    合成参考文献


    摘要:Virtanen SS, Väänänen HK, Härkönen PL, Lakkakorpi PT. Alendronate inhibits invasion of PC-3 prostate cancer cells by affecting the mevalonate pathway. Cancer Res. 2002 May 01;62(9):2708–14.
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