CAS: 73218-79-8; 2,6-Dichloro-N1-(4,5-Dihydro-1H-Imidazol-2-yl)Benzene-1,4-Diamine Hydrochloride

该化合物是一种选择性的甲型二型肾上腺活性剂,主要用于眼科治疗,以减少在青光眼或激光外科等条件下的内压(IOP),其机制包括减少水幽默生产,同时增加肺外流.该化合物显示出行动迅速开始,对短期IOP有效控制.对甲型二型受体的高度选择性将系统性副作用降至最低程度,而相对于非选择性的刺激剂而言.亚丙烯二型盐在溶液中稳定且符合标准的眼科配方,确保可靠的架子生命和易于管理.临床研究支持其作为辅助疗法的效力,特别是在除初级治疗外需要更多IOP管理的病人中.

结构式图片

欧盟法规

C&L通报

上下游产品

p-amin°Clonidine 4-nitro-2,6-dichloroaniline N-(2,6-dichloro-4-nitrophenyl)formamide (2,6-dichloro-4-nitrophenyl)carbonimidic dichloride(trans beta-carbethoxyacrylamido)-4-clonidine

合成工艺路线路线简述

  • 合成目标产物 Apraclonidine Hydrochloride 主要起始原料 Apraclonidine
  • (文献来源)合成步骤主要原料 Apraclonidine
阿可乐定置于盐酸体系中,用 乙醇,水 作为反应溶剂,化学反应 0.5H,以84%的收率获得产物盐酸安普乐定
参考文献:盐酸阿普乐定制备方法的改进
标题:盐酸阿普乐定制备方法的改进
摘要:青光眼是损害视神经并可能导致视力丧失的眼部疾病的总称.视神经损伤的主要原因是眼压(iop),除了...
DOI:10.1080/00304948.2016.1206429

海关参考信息

专利信息


专利号:US-9662347-B2
优先权日:2010-05-11
标题 :Method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of age-albumin in cells of the mononuclear phagocyte system
发明人:LEE BONG HEE; BYUN KYUNG HEE
权利人:LEE BONG HEE; BYUN KYUNG HEE; GACHON UNIV OF INDUSTRY-ACADEMIC COOP FOUND
摘要:The present invention relates to a method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of AGE-albumin in cells of the mononuclear phagocyte system, to an AGE-albumin synthesis inhibitor, and to a pharmaceutical composition comprising the AGE-albumin synthesis inhibitor for preventing or treating degenerative disease and autoimmune disease. The AGE-albumin of the present invention is synthesized and secreted in human microglia or human macrophages in an Alzheimer's model, stroke model, Parkinson's disease model and rheumatoid arthritis model. The AGE-albumin synthesis and secretion are caused by oxidative stress. The expression of RAGE increases in first-order human neurons or cartilage cells to which AGE-albumin is administered, whereupon a MAPK signaling pathway is activated and the expression of Bax increases to induce an increase in calcium in mitochondria, thus finally inducing cell death. Therefore, the AGE-albumin synthesis inhibitor of the present invention can be valuably used in the diagnosis or treatment of degenerative diseases or autoimmune diseases such as Alzheimer's disease, strokes, Parkinson's disease, amyotrophic lateral sclerosis, rheumatoid arthritis, diabetic retinopathy, AIDS, aging, pulmonary fibrosis, spinal cord injuries, etc.

专利号:US-9757463-B2
优先权日:2012-06-15
标题 :Linear polyester and semi-linear glycidol polymer systems: formulation and synthesis of novel monomers and macromolecular structures
发明人:HARTH EVA M; BEEZER DAIN B; LI GUANGZHAO; SPEARS BENJAMIN R; STEVENS DAVID M
权利人:UNIV VANDERBILT
摘要:Disclosed herein are glycidol-based polymers, nanoparticles, and methods related thereto useful for drug delivery. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

专利号:US-9371387-B2
优先权日:2011-11-10
标题 :Composition for prevention or treatment of ischemic cardiac disease, comprising inhibitor against age-albumin synthesis or release of mononuclear phagocyte system cells as active ingredient
发明人:LEE BONG HEE; BYUN KYUNG HEE
权利人:UNIV GACHON IND ACAD COOP FOUND
摘要:Disclosed is a pharmaceutical composition for the prevention or treatment of ischemic heart diseases, comprising as an active ingredient an inhibitor which acts to restrain mononuclear phagocyte system cells from synthesizing or releasing AGE-albumin, which induces the apoptosis of cardiomyocytes upon the onset of the ischemic heart disease. Also, a method is provided for screening an inhibitor against the AGE-albumin synthesis or release of mononuclear phagocyte system cells. Inhibitory or suppressive of AGE-albumin-induced cell death, the pharmaceutical composition comprising as an active ingredient an inhibitor against the AGE-albumin synthesis or release of mononuclear phagocyte system cells can be applied to the prevention or treatment of a wide spectrum of ischemic heart diseases including myocardial infarction.

专利号:US-9745419-B2
优先权日:2014-01-24
标 题 :Aqueous polyglycidol synthesis with ultra-low branching
发明人:HARTH EVA M; SPEARS BENJAMIN R
权利人:UNIV VANDERBILT
摘要:Disclosed herein are glycidol-based polymers, nanoparticles, and methods related thereto useful for a variety of applications, including, but not limited to, drug delivery. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

专利号:US-2016206743-A1
优先权日:2012-06-15
标题 :Linear Polyester and Semi-Linear Glycidol Polymer Systems: Formulation and Synthesis of Novel Monomers and Macromolecular Structures

专利号:US-2014005278-A1
优先权日:2012-06-15
标题 :Linear polyester and semi-linear glycidol polymer systems: formulation and synthesis of novel monomers and macromolecular structures
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主要参考文献


1: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Apraclonidine. 2021 Sep 20. 11(1):9. 21(5):347-51. doi: 10.1007/s10286-011-0118-6. Epub 2011 Mar 8.
376:129-132. doi: 10.1016/j.jns.2017.03.025. Epub 2017 Mar 16. 30(1):12-7. doi: 10.1097/WNO.0b013e3181b1b41f. 112(12):2238; author reply 2244. doi: 10.1016/j.ophtha.2005.09.021. 209(1):A7-13. German. 20(4):practneurol-2020-002497. doi: 10.1136/practneurol-2020-002497. Epub 2020 Mar 17.
419:117190. doi: 10.1016/j.jns.2020.117190. Epub 2020 Oct 14. 20(10):3133-3146. doi: 10.1111/jocd.14361. Epub 2021 Aug 11.

合成参考文献


参考文献:10.1007/bf00917987
摘要:Yüksel N, Güler C, Caglar Y, Elibol O. Apraclonidine and clonidine: a comparison of efficacy and side effects in normal and ocular hypertensive volunteers. Int Ophthalmol. 1992 Sep;16(4-5):337–42. doi: 10.1007/bf00917987.
摘要:Medicamentos de Actualidad., 24(557), 1988
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