CAS: 40391-99-9; (3-Amino-1-Hydroxypropane-1,1-Diyl)Bis(Phosphonic Acid)

该化合物是一种第二代双磷化合物,因其在抑制骨质激素中介质的骨吸附方面的效力而得到广泛承认,其主要用途包括治疗与恶性肿瘤,Pacet病和骨质疏松有关的超热性贫血.分子在骨骼组织中对氢氧亚丙酸晶体的高度亲和性确保采取有针对性的行动,减少系统性副作用.氨酸与早期的二磷酸相比,表现出较高的稳定性和生物利用率,允许较少的剂量.其机制涉及通过抑制等温带途径干扰骨质疏松动功能,导致骨质疏松.该化合物通常通过静脉注射进行,以确保最佳治疗效果,同时尽量减少肠道刺激.其有据可查的临床状况使得它成为管理与骨质有关的疾病的一个可靠选择.

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CAS号107-95-9 β-丙氨酸 | CAS号63132-39-8 奥帕膦酸钠

合成工艺路线路线简述

    📜β-丙氨酸置于磷酸,三氯化磷,水体系中,化学反应 4.5H,以72%的收率获得产物帕米膦酸
    参考文献:使用离子液体添加剂高效合成帕米膦酸
    标题:使用离子液体添加剂高效合成帕米膦酸
    摘要:开发了一种高效的合成帕米膦酸的方法,该方法包括在0.3或0.6当量的[bmim] [pf 6]存在下,在75oc下使β-丙氨酸与3当量的三氯化磷和2当量的亚磷酸反应.作为添加剂.
    DOI:10.2174/1570180812666151022221805

    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: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-2012177593-A1
    优先权日:2009-07-20
    标 题 :Synthesis of dendrimer conjugates
    发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
    权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
    摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

    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-12391691-B2
    优先权日:2018-11-16
    标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
    发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
    权利人:AMGEN INC
    摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

    专利号:US-2025206736-A1
    优先权日:2019-11-14
    标题 :Synthesis of kras g12c inhibitor compound
    发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
    权利人:AMGEN INC
    摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Fauzi MSA, Sabri MSA, Halim AAA, Abidin SAIZ. Combinatorial effects of hydroxyapatite and Tualang honey on medication-related osteonecrosis of the jaw (MRONJ): An in vitro study. J Stomatol Oral Maxillofac Surg. 2024 Jul
    30:101999. doi: 10.1016/j.jormas.2024.101999. Epub ahead of print. 26(11):8767-8774. doi: 10.1039/d3cp05846h. 14(4):473-478. doi: 10.1021/acsmedchemlett.3c00022.
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    合成参考文献


    参考文献:10.1016/j.joms.2009.08.027
    摘要:Oizumi T, Funayama H, Yamaguchi K, Yokoyama M, Takahashi H, Yamamoto M, Kuroishi T, Kumamoto H, Sasaki K, Kawamura H, Sugawara S, Endo Y. Inhibition of Necrotic Actions of Nitrogen-Containing Bisphosphonates (NBPs) and Their Elimination From Bone by Etidronate (a Non-NBP): A Proposal for Possible Utilization of Etidronate as a Substitution Drug for NBPs. Journal of Oral and Maxillofacial Surgery. 2010 May;68(5):1043–54. doi: 10.1016/j.joms.2009.08.027.
    参考文献:10.1111/j.1476-5381.2011.01592.x
    摘要:Kuiper J, Forster C, Sun C, Peel S, Glogauer M. Zoledronate and pamidronate depress neutrophil functions and survival in mice. British J Pharmacology. 2011 Dec 16;165(2):532–9. doi: 10.1111/j.1476-5381.2011.01592.x.
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    参考文献:10.2217/imt.11.71
    摘要:Goyne H, Stone PJ, Cannon MJ. Combinatorial strategies for alleviation of tumor-associated immune suppression and therapeutic vaccination against ovarian cancer. Immunotherapy. 2011 Jul;3(7):805–7.
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