CAS: 153259-65-5; Cilomilast

该化合物是一种选择性磷化物酶-4(PDE4)抑制剂,主要针对其在呼吸道疾病,特别是慢性阻塞性肺病和哮喘中的潜在治疗用途进行调查,作为小有机分子,硅酸酯功能抑制环氧亚丁胺单磷酸酯破裂,导致细胞内丙氧磷酸酯浓度增加;这一机制促进抗炎效应和支气管化,有利于管理气道炎;硅酸盐的特点是水中中溶性及其渗透生物膜的能力,这对于其药用活动至关重要;该化合物经历了各种临床试验,以评估其功效和安全情况,尽管临床实践尚未广泛采用,其化学结构包括有助于其生物活动的特定功能组,以及PDE4对其他磷化亚胺亚酸盐的选择性.总的来说,硅酸盐是一种旨在调节呼吸道炎道的药物,尽管其临床用途与其他现有疗法相比可能受到限制.

结构式图片

上下游产品

CAS号152630-47-2 1-[3-(CYCLOPENT...

合成工艺路线路线简述

  • 合成目标产物 Cilomilast 主要起始原料 1-Cyclohexene-1-Carboxylic Acid, 4-Cyano-4-[3-(Cyclopentyloxy)-4-Methoxyphenyl]-, Methyl Ester
  • (文献来源)合成步骤主要原料 1-Cyclohexene-1-Carboxylic Acid, 4-Cyano-4-[3-(Cyclopentyloxy)-4-Methoxyphenyl]-, Methyl Ester

海关参考信息

专利信息


专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:US-7919505-B2
优先权日:2006-07-11
标题 :Xinafoate salt of a substituted 5-oxazol-2-yl-quinoline compound
发明人:TING PAULINE C; LEE JOE F; FENG KUNG-I; REEDER MICHAEL R; TRZASKA SCOTT T; ZHU MAN; MAO CHEN; FILIPOV DIMITAR L; ZARKADAS DIMITRIOS N
权利人:SCHERING CORP
摘要:The present invention relates to the compound of the formula n nTo methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to polymorphs and processes of synthesis of the polymorphic forms.

专利号:US-2011003780-A1
优先权日:2007-07-10
标题:Hydrogen chloride salt of a substituted 5-oxazol-2-yl-quinoline compound and a process for the production thereof
发明人:ZHU MAN
权利人:SCHERING CORP
摘要:The present invention relates to the compound of the Formula I: n n n n n n n n n n and to methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to a particular crystalline form and processes of synthesis of the crystalline form. n IM=105109

专利号:EP-1473034-A1
优先权日:2003-03-17
标 题 :Use of an inhibitor of the phosphodiesterase-4-enzyme (PDE4) alone or in combination with relaxin and derivatives thereof for the manufacture of a medicament to promote decidualization of endometrial cells and to increase fertility
发明人:IVELL PROF DR RICHARD; BARTSCH DR OLAF
权利人:LAGOW GMBH
摘要:This invention relates to the use of an inhibitor of the phosphodiesterase-4nenzyme (PDE4) for the preparation of a pharmaceuticalncomposition for promoting the decidualization of endometrialncells. n The pharmaceutical composition may further comprise a compoundnwhich increases the synthesis of cAMP, such as relaxin or annagonist of the action of relaxin receptors such as relaxin receptorsnLGR7 and/or LGR8.

专利号:US-8598153-B2
优先权日:2006-09-22
标题 :Method of treatment using fatty acid synthesis inhibitors
发明人:SINGH SHEO B; TOTA MICHAEL R; WANG JUN
权利人:SINGH SHEO B; TOTA MICHAEL R; WANG JUN; MERCK SHARP & DOHME
摘要:The present invention relates to natural products that possess fatty acid synthesis inhibitor activity and can be used to treat and prevent diseases such as obesity, cancer, diabetes, fungal infections, Mycobacterium tuberculosis infections, malarial infections and other apicomplexan protozoal diseases.

专利号:US-9982006-B2
优先权日:2014-08-21
标题:2′-chloro aminopyrimidinone and pyrimidine dione nucleosides
发明人:CLARKE MICHAEL O'NEIL HANRAHAN; MACKMAN RICHARD L; SIEGEL DUSTIN
权利人:GILEAD SCIENCES INC
摘要:Provided herein are formulations, methods and substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds.
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主要参考文献


1: Munisso MC, Kang JH, Tsurufuji M, Yamaoka T. Cilomilast enhances osteoblast differentiation of mesenchymal stem cells and bone formation induced by bone morphogenetic protein 2. Biochimie. 2012 Jun 15. [Epub ahead of print] Epub 2011 Feb 20. Epub 2009 Feb 20. Epub 2008 Jun 9. doi: 10.2165/0003495-200868002-00002. Review. doi: 10.2165/0003495-200868002-00001. PMID: 17178338

合成参考文献


参考文献:10.1186/1465-9921-5-4
摘要:Clayton RA, Dick CA, Mackenzie A, Nagasawa M, Galbraith D, Hastings SF, MacKenzie SJ. The effect of selective phosphodiesterase inhibitors, alone and in combination, on a murine model of allergic asthma. Respiratory Research. 2004 May 05;5(1):4. doi: 10.1186/1465-9921-5-4.
参考文献:10.1371/journal.pone.0020000
摘要:Trian T, Burgess JK, Niimi K, Moir LM, Ge Q, Berger P, Liggett SB, Black JL, Oliver BG. β2-Agonist Induced cAMP Is Decreased in Asthmatic Airway Smooth Muscle Due to Increased PDE4D. PLoS ONE. 2011 May 17;6(5):e20000. doi: 10.1371/journal.pone.0020000.
参考文献:10.1038/sj.bjp.0705927
摘要:Jacob C, Szilagyi C, Allen JM, Bertrand C, Lagente V. Role of PDE4 in superoxide anion generation through p44/42MAPK regulation: a cAMP and a PKA‐independent mechanism. British J Pharmacology. 2004 Sep;143(2):257–68. doi: 10.1038/sj.bjp.0705927.
参考文献:10.1177/0091270004266488
摘要:Murdoch RD, Zussman B, Schofield JP, Webber DM. Lack of pharmacokinetic interactions between cilomilast and theophylline or smoking in healthy volunteers. J Clin Pharmacol. 2004 Sep;44(9):1046–53. doi: 10.1177/0091270004266488.
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