CAS: 116-38-1; N-Ethyl-3-Hydroxy-N,N-Dimethylbenzenaminium Chloride

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CAS号75-03-6 碘乙烷 | CAS号99-07-0 N,N-二甲基间羟基苯胺 | CAS号74-96-4 溴乙烷

合成工艺路线路线简述

    溴乙烷,3-羟基-N,N-二甲基苯胺 反应生成依酚氯铵
    参考文献:De837098
    标题:De837098

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    专利信息


    专利号:US-9315483-B2
    优先权日:2007-09-13
    标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
    发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
    权利人:CONCERT PHARMACEUTICALS INC
    摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

    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-8063062-B2
    优先权日:2006-12-20
    标 题 :Compounds with a combination of cannabinoid-CB1 antagonism and acetylcholinesterase inhibition
    发明人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; SHADID BELAL
    权利人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; SHADID BELAL; SOLVAY PHARM BV
    摘要:Embodiments of this invention relate to compounds having a combination of cannabinoid-CB 1 antagonism and cholinesterase inhibition, to pharmaceutical compositions comprising these compounds, to methods for preparing these compounds, methods for preparing novel intermediates useful for the synthesis of these compounds, and methods for preparing compositions comprising these compounds. The invention also relates to methods of treating Alzheimer's disease, cognitive disorders, memory disorders, dementia, attention deficit disorder, traumatic brain injury, drug dependence, addiction or substance abuse by administering a pharmaceutical composition comprising these compounds to a patient in need thereof. A compound with a combination of cannabinoid-CB 1 antagonism and cholinesterase inhibition is a compound of formula (1) n nwherein the symbols have the meanings given in the specification.

    专利号:US-6048529-A
    优先权日:1991-12-19
    标 题 :PVA or PEG conjugates of peptides for epitope-specific immunosuppression
    发明人:ATASSI M ZOUHAIR; ASHIZAWA TETSUO
    摘要:The invention relates to a procedure for synthesis of well-defined conjugates of peptides to the tolerogenic polymer monomethoxypolyethylene glycol (mPEG) or polyvinyl alcohol (PVA). This method results in the preparation of conjugates in which one molecule of tolerogenic polymer is specifically coupled to one or the other or both of the termini of an otherwise unaltered peptide molecule. A synthetic peptide synthesized using this method and corresponding to a myasthenogenic region of an acetylcholine receptor was conjugated to monomethoxypolyethylene glycol. Injection of animals with the mPEG-conjugate and subsequent immunization with whole receptor suppressed the development of experimental autoimmune myasthenia gravis (EAMG) by electrophysiological criteria. Specifically-conjugated, tolerogenic peptides are also disclosed for diseases as diverse as ragweed pollen allergy and Grave's disease.

    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-6030613-A
    优先权日:1995-01-17
    标题:Receptor specific transepithelial transport of therapeutics
    发明人:BLUMBERG RICHARD S; SIMISTER NEIL E; LENCER WAYNE I
    权利人:BRIGHAM & WOMENS HOSPITAL; UNIV BRANDEIS
    摘要:The present invention relates in general to methods and products for initiating an immune response against an antigen, and in particular relates to transepithelial delivery of antigens to provoke tolerance and immunity. The present invention further relates to methods and products for the transepithelial delivery of therapeutics. In particular, the invention relates to methods and compositions for the delivery of therapeutics conjugated to a FcRn binding partner to intestinal epithelium, mucosal epithelium and epithelium of the lung. The present invention further relates to the synthesis, preparation and use of the FcRn binding partner conjugates as, or in, pharmaceutical compositions for oral systemic delivery of drugs and vaccines.
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    主要参考文献


    1: Bassotti G, Imbimbo BP, Betti C, Erbella GS, Pelli MA, Morelli A. Edrophonium chloride for testing colonic contractile activity in man. Acta Physiol Scand. 1991 Mar;141(3):289-93. doi: 10.1111/j.1748-1716.1991.tb09083.x. 119-120:129-35. doi: 10.1016/s0009-2797(99)00021-6. 235(10):1041-2. 51(6):567. doi: 10.1097/00000542-197912000-00022. 15(1):27-31. 112(13):592-5. German. 32(2):104-7. doi: 10.3109/00365529709000178. 18(1):59-65. doi: 10.1159/000115054. 56(18):2415-2421. doi: 10.2169/internalmedicine.8555-16. Epub 2017 Aug 21.
    10: MOORE H. Advantages of pyridostigmine bromide (mestinon) and edrophonium chloride (tensilon) in the treatment of transitory myasthenia gravis in the neonatal period. N Engl J Med. 1955 Dec 15;253(24):1075-6. doi: 10.1056/NEJM195512152532406. 5(2):73-5. doi: 10.3109/01658108509014425. 135(1):312-34. doi: 10.1111/j.1749-6632.1966.tb45479.x. 39(4):157-62. 44(7):689-90. doi: 10.1001/archneur.1987.00520190005002. 32(7):682-8. doi: 10.1007/BF01296132. 112(1):49. doi: 10.1093/qjmed/hcy173. 20(1):56-61. doi: 10.1159/000115206.
    182:108303. doi: 10.1016/j.neuropharm.2020.108303. Epub 2020 Sep 9. 93(5):189-97.

    合成参考文献


    摘要:Konishi T. [Myasthenia gravis with anti-acetylcholine receptor antibody or anti-muscle specific kinase antibody]. Brain Nerve. 2011 Jul;63(7):695–704.
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