CAS: 7421-40-1; Carbenoxolone Disodium,(3β,20β)-3-(3-Carboxy-1-Oxopropoxy)-11-Oxoolean-12-En-29-Oicaciddisodium

该化合物是一种以其抗炎和溃疡-健康特性而闻名的甘油酸合成衍生物.作为二钠盐,它提供了水溶液中的强化溶性,便利了其在药理学和研究应用中的使用.化合物抑制了11β-羟丁基激素脱氢酶,调节了有助于其治疗效果的凝固质类物质活动.其主要优势包括高纯度,持续的生物利用率和在标准储存条件下的稳定性.卡比诺酮二钠被广泛用于涉及气态肌肉保护,肾上腺类代谢和炎症相关途径的研究.其精密的机制和可靠的性能使得它成为临床前科和临床研究的宝贵工具.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

合成工艺路线路线简述

    丁二酸酐,甘草次酸 在 4-二甲氨基吡啶,Sodium Ethanolate体系中,用 甲苯,乙醇作为反应溶剂,以125.1 G的收率获得carbenoxolone Disodium
    参考文献:一种甘珀酸钠的制备方法
    标题:一种甘珀酸钠的制备方法
    摘要:本发明公开了一种甘珀酸钠的制备方法,涉及化工合成技术领域.包括如下步骤:(1)以甘草次酸和丁二酸酐为原料,4‑二甲氨基吡啶为催化剂,甲苯为溶剂反应生成甘珀酸;(2)将甘珀酸用醇钠调碱得到甘珀酸钠.本发明的制备方法反应时间短,成本低,毒性小,有良好的产率和产物转化率,且原料利用率高,操作简单,后处理简单,绿色环保,得到的产品纯度高,含量高.

    海关参考信息

    专利信息


    专利号:EP-1886695-A1
    优先权日:2006-06-27
    标 题:Pharmaceutical combination of an aldosterone synthase inhibitor and a glucocorticoid receptor antagonist or a cortisol synthesis inhibitor or a corticotropin releasing factor antagonist
    发明人:SCHUMACHER CHRISTOPH
    权利人:SPEEDEL EXPERIMENTA AG
    摘要:The invention relates to a pharmaceutical combination comprising (a) an aldosterone synthase inhibitor or a pharmaceutically acceptable salt thereof, and (b) a glucocorticoid receptor antagonist or a cortisol synthesis inhibitor or a cortisol re-synthesis inhibitor or a corticotrophin-releasing hormone receptor antagonist or combinations thereof or in each case a pharmaceutically acceptable salt thereof. Said composition is useful for the manufacture of a medicament, in particular for the manufacture of a medicament for the prevention of, delay of progression of treatment of a disease or condition characterized by the metabolic syndrome.

    专利号:WO-9709067-A1
    优先权日:1995-09-05
    标 题 :Combination of 5-lipoxygenase and leukotriene synthesis inhibitors with glucocorticosteroids
    发明人:BURCHARDT ELMAR-REINHOLD; MUELLER-PEDDINGHAUS REINER
    权利人:BAYER AG; BURCHARDT ELMAR REINHOLD; MUELLER PEDDINGHAUS REINER
    摘要:The combination is disclosed of 5-lipoxygenase inhibitors as direct action lipoxygenase inhibitors (LOI) or of leukotriene synthesis inhibitors (LSI) with glucocorticosteroids (GCS). This combination is suitable for treating and preventing various acute and chronic inflammatory processes, in particular of the respiratory tract, and may therefore be used as a medicament, in particular for treating asthma.

    专利号:US-10947273-B2
    优先权日:2015-10-09
    标 题 :Peptides of use in the preventive and curative treatment of alopecia
    发明人:HOCQUAUX MICHEL; ALMEIDA ÉPOUSE SCALVINO STÉPHANIE; LATI ELIAN; BAKALA JOANNA
    权利人:INST EUROPEEN DE BIOLOGIE CELLULAIRE; CENTRE DE RECH BIOLOGIQUES ET DEXPERIMENTATIONS CUTANEES; CENTRE NAT RECH SCIENT; INST EUROPEAN DE BIOLOGIC CELLULAIRE
    摘要:The object of the present invention relates to a novel family of peptide conjugates of formula (I):n nA-X 1 -X 2 -Pro-Ala-X—B  (I)n wherein:n A represents a hydrogen atom, a C 6 to C 20 acyl group or a cholesterol residue; X 1 represents a covalent bond, an alanine or a proline; X 2 represents an arginine, a lysine, or an alanine; X represents a lysine, an alanine, or a phenylalanine; and B represents a hydroxyl or an amine; n or one of its preferentially pharmaceutically, dermatologically or cosmetically acceptable salts,n nas well as their synthesis processes and their uses for reducing hair loss and stimulating hair growth.

    专利号:US-4381301-A
    优先权日:1980-05-07
    标题 :Substituted tricyclic thieno compounds, their synthesis, their use, their compositions and their medicaments
    发明人:RAINER GEORG
    权利人:BYK GULDEN LOMBERG CHEM FAB
    摘要:Substituted thienobenzodiazepinones of the general formula I (I) [wherein R1 denotes a hydrogen atom (-H) or an alkyl radical with 1 to 4 carbon atoms; R2 represents a halogen atom (halo) or has one of the meanings of R1; R3 denotes a halogen atom (halo) or the group -N(R4)R5; R4 denotes an alkyl radical with 1 to 4 carbon atoms or an alkenyl radical with 3 to 5 carbon atoms; R5 has one of the meanings of R4 or represents the group -(CH2)m-N(R6)R7; or R4 and R5, together with the nitrogen atom to which both are bonded, denote a morpholino group, a pyrrolidino group, a piperidino group, a hexahydroazepin-1-yl group, a piperazin-1-yl group (which is optionally substituted in the 4-position by a methyl, ethyl or benzyl group), a 2,4-dimethylpiperazin-1-yl group, or a hexahydro-1H-1,4-diazepin-1-yl group (which is substituted in the 4-position by a methyl or ethyl group); R6 denotes an alkyl group with 1 to 4 carbon atoms; R7 denotes an alkyl group with 1 to 4 carbon atoms; A denotes a straight-chain or branched alkylene group with 1 to 5 carbon atoms; and m denotes 2 or 3] and their acid-addition salts are new compounds. They either have a protective action on the stomach and intestine and are suitable for treating illnesses based on disorders of the stomach or intestine, or they are intermediates for preparing products having protective action. Processes for the preparation of the new pharmacologically-active compounds and of the intermediate products are presented.

    专利号:WO-2009025888-A2
    优先权日:2007-05-10
    标 题:Regulated synthesis of antigen and/or regulated attentuation to enhance vaccine immunogenics and/or safety

    专利号:WO-0026406-A1
    优先权日:1998-11-04
    标题:METHOD FOR INDEXING AND DETERMINING THE RELATIVE CONCENTRATION OF EXPRESSED MESSENGER RNAs
    发明人:HASEL KARL W; HILBUSH BRIAN S
    权利人:DIGITAL GENE TECH INC
    摘要:An improved method for the simultaneous sequence-specific identification of mRNAs in a mRNA population allows the visualization of nearly every mRNA expressed by a tissue as a distinct band on a gel whose intensity corresponds roughly to the concentration of the mRNA. In general, the method comprises the formation of cDNA using anchor primers to fix a 3'-endpoint, producing cloned inserts from the cDNA in a vector containing a bacteriophage-specific promoter for subsequent RNA synthesis, generating linearized fragments of the cloned inserts, preparing cRNA, transcribing cDNA from the cRNA and performing two sequence specific PCR amplifications of the cDNA. In preferred embodiments, the method comprises comparing the length and at least part of the nucleotide sequence of the PCR products to expected values determined from a database of nucleotide sequences. The method can identify changes in expression of mRNA associated with the administration of drugs or with physiological or pathological conditions. Also provided are vectors and primers useful for the practice of the improved method.
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    主要参考文献


    1: Wattanakorn N, Asavapichayont P, Nunthanid J, Limmatvapirat S, Sungthongjeen S, Chantasart D, Sriamornsak P. Pectin-based bioadhesive delivery of carbenoxolone sodium for aphthous ulcers in oral cavity. AAPS PharmSciTech. 2010 Jun;11(2):743-51. doi: 10.1208/s12249-010-9424-x. Epub 2010 May 5.
    2: Zhou JJ, Jiang YX, Jin SJ, Tao LJ, Liu LJ. [Studies on analgesic effects and sites of oxymatrine-carbenoxolone sodium complex]. Zhongguo Zhong Yao Za Zhi. 2008 Apr;33(7):822-4. Chinese. doi: 10.1016/j.ejphar.2009.09.065. Epub 2009 Oct 8. doi: 10.1107/S2052520614026419. Epub 2015 Jan 20. Chinese. doi: 10.1016/j.ejphar.2016.09.035. Epub 2016 Sep 28. doi: 10.1016/j.bbrc.2015.11.034. Epub 2015 Nov 11. doi: 10.1016/j.abb.2014.06.027. Epub 2014 Jul 1.
    13: Luo L, Deng J, Wang DX, He J, Deng W. Regulation of epithelial sodium channel expression by oestradiol and progestogen in alveolar epithelial cells. Respir Physiol Neurobiol. 2015 Sep 15;216:52-62. doi: 10.1016/j.resp.2015.06.001. Epub 2015 Jun 4. doi: 10.1016/j.neulet.2015.06.037. Epub 2015 Jun 30. doi: 10.1016/j.neulet.2014.01.042. Epub 2014 Jan 31.

    合成参考文献


    摘要:Symposium on Carbenoxolone Sodium, Robson, J.M., and F.M. Sullivan, eds., London, Butterworth, 1968, -(6), 1968
    摘要:Oyo Yakuri. Pharmacometrics., 11(263), 1976
    摘要:Canadian Medical Association Journal., 117(1155), 1977 []
    摘要:S13 | EUCOSMETICS | Combined Inventory of Ingredients Employed in Cosmetic Products (2000) and Revised Inventory (2006) | DOI:10.5281/zenodo.2624118
    摘要:International Journal of Toxicology 26(Suppl. 2):79-112, 2007
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