CAS: 180064-38-4; (1-Hydroxy-2-(Imidazo[1,2-A]Pyridin-3-yl)Ethane-1,1-Diyl)Diphosphonic Acid

该化合物是一种主要用于治疗骨质疏松症和其他与骨头有关的失调的合成双光磷化合物,其作用是抑制骨质疏松的中枢骨吸附,从而增进骨密度和强度.细诺诺米酸的化学结构特征是磷磷原子与碳和氧结合的化学结构,这是二光磷酸的特点,有助于其生物活动.它一般是口服的,具有有利的药理动因特征,允许在骨骼组织中有效吸收和分布.已知氨基诺酸的半衰期相对较长,可支持其治疗效果.此外,它具有低毒性和安全性,适合有骨折危险的病人长期使用.与其他双光磷酸一样,潜在副作用可能包括胃肠扰动,在罕见的情况下,还有卵巢的骨质疏松.

结构式图片

上下游产品

咪唑并[1,2-A]吡啶-3-乙酸 2-(Imidazo[1,2-A]Pyridin-3-yl)Acetic Acid 17745-04-9
咪唑并[1,2-A]吡啶-3-乙酸乙酯 Ethyl 2-(Imidazo[1,2-A]Pyridin-3-yl)Acetate 101820-69-3

合成工艺路线路线简述

    (2-Oxo-3H-Imidazo<1,2-A>Pyridin-3-yl)Essigsaeure置于氯化亚砜,磷酸,Lindlar'S Catalyst,Potassium Formate,Potassium Carbonate,三氯氧磷,三氯化磷体系中,用 氯苯,异丙醇 用作溶剂,化学反应 29.0H,反应生成米诺膦酸
    参考文献:从2-氯咪唑[1,2-A ]吡啶类制备实用且可扩展的米诺膦酸和唑吡坦
    标题:从2-氯咪唑[1,2-A ]吡啶类制备实用且可扩展的米诺膦酸和唑吡坦
    摘要:开发了米诺膦酸和唑吡坦的实用且可扩展的方法,分别以较短的反应序列从2-氨基吡啶和马来酸酐中提取.新程序避免了在所有合成步骤中进行纯化的柱色谱法.该进展的关键方面涉及2-氯咪唑[1,2-A ]吡啶的还原加氢脱氯和suzuki偶联反应,并且还探讨了它们在两种药物合成中的应用.
    Doi:10.1016/j.Tet.2019.01.015

    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-8017776-B2
    优先权日:2003-07-15
    标题 :Methods for synthesis of acyloxyalkyl compounds
    发明人:BHAT LAXMINARAYAN; GALLOP MARK A
    权利人:XENOPORT INC
    摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

    专利号:US-8431714-B2
    优先权日:2007-04-16
    标题:Synthesis of drug conjugates via reaction with epoxide-containing linkers
    发明人:MCKENNA CHARLES E; KASHEMIROV BORIS A; BALA JOY LYNN F
    权利人:MCKENNA CHARLES E; KASHEMIROV BORIS A; BALA JOY LYNN F; UNIV SOUTHERN CALIFORNIA
    摘要:The present invention relates to drug derivatives and linkers. The invention specifically relates to compounds and methods of phosphonates and linkers, that are useful as carriers for imaging agents and useful in the treatment of various bone diseases.

    专利号:WO-2008058722-A1
    优先权日:2006-11-16
    标 题:Reagent and use thereof for the production of bisphosphonates
    发明人:LERSTRUP KNUD; PREIKSCHAT HERBERT FRITZ; FISCHER ERIK
    权利人:SANDOZ AS; LERSTRUP KNUD; PREIKSCHAT HERBERT FRITZ; FISCHER ERIK
    摘要:A new liquid reagent is disclosed in form of an ionic liquid containing phosphorous acid and a tertiary amine. The reagent can be used as a replacement of phosphorous acid, where the new reagent as a liquid reagent can be handled using usual equipment for handling liquids and the dosing of the reagent can therefore be controlled more precisely in industrial plants compared to phosphorous acid, which is a solid at ambient temperature. The new liquid reagent is particular suitable for the synthesis of bisphosphonates.

    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-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.
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    主要参考文献


    1: Tanaka M, Mori H, Kawabata K, Mashiba T. Minodronic acid ameliorates vertebral bone strength by increasing bone mineral density in 9-month treatment of ovariectomized cynomolgus monkeys. Bone. 2016 Jul;88:157-64. doi: 10.1016/j.bone.2016.05.001. Epub 2016 May 4. doi: 10.3109/09513590.2015.1112783. Epub 2015 Nov 20. doi: 10.1016/j.clinthera.2015.01.015. Epub 2015 Mar 5. doi: 10.1007/s00774-015-0658-2. Epub 2015 Apr 3. doi: 10.1016/j.bone.2014.04.003. Epub 2014 Apr 13. doi: 10.1007/s00223-014-9876-1. Epub 2014 Jun 6. doi: 10.1016/j.jpba.2015.05.038. Epub 2015 Jun 18. doi: 10.1016/j.bone.2013.02.013. Epub 2013 Feb 26. doi: 10.1007/s00223-015-0017-2. Epub 2015 Jun 6.

    合成参考文献


    参考文献:10.1186/1749-799x-6-34
    摘要:Wang Y, Huang P, Tang P, Chan K, Li G. Alendronate (ALN) combined with Osteoprotegerin (OPG) significantly improves mechanical properties of long bone than the single use of ALN or OPG in the ovariectomized rats. Journal of Orthopaedic Surgery and Research. 2011 Jul 13;6(1):34. doi: 10.1186/1749-799x-6-34.
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