CAS: 51781-21-6; Carteolol Hydrochloride

该化合物是一种主要用于治疗青光眼和眼部高血压的非选择性乙醇-肾抗争物;作为乙型阻塞剂的一员,它通过减少水性幽默生产,减少内腔压力;该物质在水中溶解,并展示出其基本性质.其分子公式反映了一种复杂的结构,其中包括一种芬诺单体,有助于其药理活动.碳酸盐的特点是能够穿透玉米,使其对局部眼科治疗有效.此外,它可能具有内在的同源体外活动,与其他乙型阻塞体相比,这种活动可导致较少的副作用.该化合物通常作为眼滴溶液施用,其功效通常在临床环境中评估,以管理高水平的内心压力.正如任何药物,潜在副作用和反作用一样,在使用该物质时必须遵循医学指导.

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CAS号51781-06-7 卡替洛尔

合成工艺路线路线简述

    5-(2,3-环氧丙氧基)-3,4-二氢喹诺酮,叔丁胺置于盐酸体系中,用 乙醇,丙酮,水 作为反应溶剂,化学反应 8.17H,以84.7%的收率获得产物盐酸卡替洛尔
    参考文献:稳定的盐酸卡替洛尔及其制法和眼用药物组 合物
    标题:稳定的盐酸卡替洛尔及其制法和眼用药物组 合物
    摘要:本发明涉及稳定的盐酸卡替洛尔及其制法和眼用药物组合物.具体的,本发明涉及一种制备盐酸卡替洛尔的方法,其包括如下步骤:制备3‑氨基‑2‑环己烯酮,制备四氢‑2,5(1H,6H)‑喹啉二酮,制备5‑羟基‑3,4‑二氢‑2(1H)‑喹诺酮,制备5‑(2,3‑环氧丙氧基)‑3,4‑二氢‑2(1H)‑喹诺酮,制备盐酸卡替洛尔.进一步的,本发明还提供了一种照本发明方法制备得到的盐酸卡替洛尔原料药,以本发明制得的盐酸卡替洛尔为原料药制备得到的眼用药物组合物,以及本发明制得的盐酸卡替洛尔在制备用于治疗或预防青光眼或高眼压症的药物中的用途.本发明方法具有优异的药学特征例如所制得的原料药和制剂具有优异的稳定性.

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    专利信息


    专利号:US-4535079-A
    优先权日:1982-10-20
    标题:Alkanolaminoxy derivatives of 3,4-dihydro-2H-1,4-benzothiazin-3-one, their production process, and their pharmaceutical use
    发明人:FRAVOLINI ARNALDO
    权利人:MEDIOLANUM FARMACEUTICI SRL
    摘要:Object of the invention is a class of new organic compounds derived from 1,4-benzothiazine through substitution of an hydrogen atom in position 6, 7 or 8 by an oxypropanolammine radical monosubstituted in N and furthermore a series of new phenyl derivatives of 1,4-benzothiazine, obtained as intermediate in the synthesis of oxypropanolammine derivatives, and process for obtained the new compounds in form suitable for the preparation of pharmaceutical compositions having antihypertensive, vasodilating and antiarrhythmic activity.

    专利号:US-7531164-B2
    优先权日:2005-10-21
    标 题 :Preventing bacterial or viral infectivity and composition containing infection preventing additive
    发明人:DAAKA YEHIA; STAMLER JONATHAN S
    权利人:UNIV DUKE
    摘要:A nitric oxide synthesis inhibitor or nitric oxide scavenger is administered to prevent development of infection, to prevent development of a cancer where overstimulation of a receptor contributes to the cancer development, and to prevent loss of beta agonist responsivity and as a treatment in combination with a receptor blocker. Compositions include nitric oxide synthesis inhibitor or nitric oxide scavenger containing spermicidal compositions, nasal steroid compositions, urinary tract infection prophylaxis compositions, compositions for prophylaxis of EGFR associated cancer and human blood component(s) composition for transfusion.

    专利号:US-2014315720-A1
    优先权日:2012-10-24
    标 题 :Polysaccharide ester microspheres and methods and articles relating thereto
    发明人:FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY
    权利人:CELANESE ACETATE LLC
    摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.

    专利号:US-2012232031-A1
    优先权日:2009-10-19
    标 题:Injectable formulations for intra-articular or peri-articular administration
    发明人:HUTCHINSON JOHN HOWARD; PRASIT PETPIBOON PEPPI; DEARMOND ISABELLE MARGUERITE
    权利人:HUTCHINSON JOHN HOWARD; PRASIT PETPIBOON PEPPI; DEARMOND ISABELLE MARGUERITE; PANMIRA PHARMACEUTICALS LLC
    摘要:Described herein are injectable formulations for intra-articular or peri-articular administration, wherein the formulation is administered to treat joint pain. An injectable formulation for intra-articular or peri-articular administration disclosed herein comprises a therapeutically-effective amount of a leukotriene synthesis inhibitor compound formulated for intra-articular or peri-articular administration.
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    主要参考文献


    1: Yao Q, Yu X, Zheng T, Liu H, Yang Y, Yi P. Spectroscopic studies on the interaction of carteolol hydrochloride and urea-induced bovine serum albumin. Spectrochim Acta A Mol Biomol Spectrosc. 2013 Sep;113:447-51. doi: 10.1016/j.saa.2013.04.129. Epub 2013 May 16. Japanese. Japanese. Japanese. doi: 10.2174/1874364101004010060.
    6: Nakamoto K, Yasuda N. Effect of carteolol hydrochloride on 24-hour variation of intraocular pressure in normal-tension glaucoma. Jpn J Ophthalmol. 2010 Mar;54(2):140-3. doi: 10.1007/s10384-009-0780-6. Epub 2010 Apr 18. German. German. Japanese.

    合成参考文献


    摘要:Oyo Yakuri. Pharmacometrics., 11(165), 1976
    摘要:Iyakuhin Kenkyu. Study of Medical Supplies., 12(668), 1981
    摘要:Arzneimittel-Forschung. Drug Research., 33(290), 1983 []
    参考文献:10.1007/bf02994749
    摘要:Sohn YT, Oh JH. Characterization of physicochemical properties of ferulic acid. Archives of Pharmacal Research. 2003 Dec;26(12):1002–8. doi: 10.1007/bf02994749.
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