CAS: 124351-85-5; ((Cycloheptylamino)Methylene)Diphosphonic Acid

该化合物是一种化学化合物,被归类为二磷酸,主要用于处理与骨头有关的疾病,特别是骨质疏松症,其结构有两种磷酸化合物,有助于其抑制骨骼再吸附的能力,从而提高骨密度;氨酸以其相对长的半衰期而闻名,允许与其他二磷酸相比,较少频繁地使用.该化合物显示出对骨骼组织中骨质疏松的矿物成分 ----水氧化物的亲近性,有利于其本地化.此外,还研究了其对矿物代谢的潜在影响及其在减少骨折风险方面的作用.与其他二磷酸一样,常见的副作用可能包括胃肠扰动和潜在的肾毒性,需要在治疗期间进行仔细监测.

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Tetraethyl (Cycloheptylamino)Methyl-1,1-Bisphosphonate 124351-81-1

合成工艺路线路线简述

    📜Tetraethyl (Cycloheptylamino)Methyl-1,1-Bisphosphonate置于盐酸体系中,化学反应 2.5H,以63.1%的收率获得英卡膦酸
    参考文献:新型骨吸收抑制剂的研究.I.氨基亚甲基双膦酸酯衍生物的合成和药理活性.
    标题:新型骨吸收抑制剂的研究.I.氨基亚甲基双膦酸酯衍生物的合成和药理活性.
    摘要:合成了一系列氨基亚甲基双膦酸酯衍生物,并使用甲状旁腺激素(pth)诱导的大鼠高钙血症模型(pih模型)评估了其抗吸收活性.在这些化合物中,最终选择了(环庚基氨基)亚甲基双(膦酸)(3J)进行进一步研究,在pih模型和固定化大鼠骨萎缩模型(da模型)中证明其效力是帕米膦酸盐的10倍.讨论了该系列双膦酸酯的结构-活性关系.
    Doi:10.1248/cpb.41.688

    海关参考信息

    专利信息


    专利号:EP-1566177-A1
    优先权日:2004-02-23
    标 题:The use of bisphosphonates for treating skin by stimulating of collagen synthesis
    发明人:KIM JIN; YOOK JONG IN; KIM NAM HEE; RYU JU KYOUNG
    权利人:TIGEN BIOTECH CO LTD
    摘要:The present invention relates to a novel use of bisphosphonate, and morenparticularly to a composition for increasing collagen synthesis comprisingnbisphosphonate as an active ingredient, as well as the use thereof. The inventivencomposition comprising the bisphosphonate promotes collagen synthesis, and thus, whennit is applied to the skin, it reduces wrinkles of the skin and makes the skin elastic. Fornthis reason, the inventive composition will be useful as cosmetics for the prevention ornimprovement of skin aging or a wound-healing agent. Furthermore, the inventivencomposition can remarkably increase the collagen synthesis of fibroblasts in vitro , andnthus, can be effectively used in the production of products containing collagen.

    专利号:US-2006287257-A1
    优先权日:2005-06-20
    标 题 :Pharmaceutical compositions to treat diseases caused by mycobacterium
    发明人:STOCKEL RICHARD F
    权利人:STOCKEL RICHARD F
    摘要:The invention teaches the synthesis of pharmaceutical composition and methods of synthesis to treat people and animals infected with a pathogenic mycobacterium. In particular the compositions of this invention are suitable for the treatment of tuberculosis, malaria, and other infections diseases caused by mycobacterium.

    专利号:US-2007155693-A1
    优先权日:2004-01-19
    标 题 :Inhibitor of cancer bone metastasis
    发明人:YAGITA AKIKUNI
    权利人:ORIENT CANCER THERAPY CO LTD
    摘要:The subject of the present invention is to provide means to fully achieve the inhibition of cancer bone metastasis, which was accomplished through the repeated selection of agents with aiming at obtaining more beneficial effects on the inhibition of cancer bone metastasis. The invention is achieved by combining an inhibition substance of the activation of osteoclast caused by the degradation of a signaling molecule, TRAF6, in the activation of osteoclast, a suppressive substance of the differentiation from osteoclast precursor cells to mature osteoclasts, and/or a bone resorption inhibitor and/or a Cox2 synthesis inhibitor. This combination was found to have an extremely high utility for the inhibition of cancer bone metastasis. Further, the invention is achieved by the inhibitor of cancer bone metastasis, wherein an IL-12 production inducer as an inhibition substance of the activation of osteoclast caused by the degradation of a signaling molecule, TRAF6, in the activation of osteoclast, a tyrosine kinase inhibitor as a suppressive substance of the differentiation from osteoclast precursor cells to mature osteoclasts, and/or a bisphosphonate as a bone resorption inhibitor and/or a Cox2 synthesis inhibitor for inhibiting the stimulation of RANKL/RANK receptor are combined.

    专利号:US-8183409-B2
    优先权日:2004-05-06
    标题:High yield and rapid synthesis methods for producing metallo-organic salts
    发明人:CHRISTGAU STEPHAN; ANDERSEN JENS E T
    权利人:CHRISTGAU STEPHAN; ANDERSEN JENS E T; OSTEOLOGIX AS
    摘要:A new method for preparing salts of metal cations and organic acids, especially divalent salts of alkaline earth metal ions from group II of the periodic system and carboxylic acids. The method comprising the use of a high temperature (about 90° or more) and, optionally. high pressure, in order to obtain a higher yield, purity and faster reaction speed than obtained with known synthesis methods. In particular, the present invention relates to the production of strontium salts of carboxylic acids. Novel strontium salts are also provided by the present method.

    专利号:US-2022118123-A1
    优先权日:2019-02-22
    标 题 :Combination of ar antagonists and targeted thorium conjugates
    发明人:HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY
    权利人:BAYER AG; BAYER AS
    摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.

    专利号:US-2009137678-A1
    优先权日:2005-07-06
    标 题:High yield synthesis methods for producing organic salts of strontium
    发明人:CHRISTGAU STEPHAN; ANDERSEN JENS E T
    权利人:CHRISTGAU STEPHAN; ANDERSEN JENS E T
    摘要:New organic salts of strontium and methods of synthesizing such salts with high purity, high yields and with short processing times, at neutral conditions and at low reaction temperature, such as a temperature at or below 50° C.

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    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Miszczyk P, Wieczorek D, Gałęzowska J, Dziuk B, Wietrzyk J, Chmielewska E. Reaction of 3-Amino-1,2,4-Triazole with Diethyl Phosphite and Triethyl Orthoformate: Acid-Base Properties and Antiosteoporotic Activities of the Products. Molecules. 2017 Feb 8;22(2):254. doi: 10.3390/molecules22020254.

    合成参考文献


    参考文献:10.5517/ccn62jf
    摘要:doi:10.5517/ccn62jf
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