CAS: 23138-58-1; 1-Ethyl-3-Isocyanatobenzene

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CAS号75-44-5 光气 | CAS号587-02-0 3-乙基苯胺

📜光气,3-乙基苯胺置于碳酸氢钠体系中,用 二氯甲烷,水,甲苯 用作溶剂,化学反应生成3-乙基苯基异氰酸酯
参考文献:Structural Optimization Of A Cxcr2-Directed Antagonist That Indirectly Inhibits γ-Secretase And Reduces Aβ
标题:Structural Optimization Of A Cxcr2-Directed Antagonist That Indirectly Inhibits γ-Secretase And Reduces Aβ
摘要:Amyloid Beta(A Beta),A Key Molecule In The Pathogenesis Of Alzheimer'S Disease (Ad),Is Derived From The Amyloid Precursor Protein (App) By Sequential Proteolysis Via Beta-And Gamma-Secretases. Because Of Their Role In Generation Of A Beta,These Enzymes Have Emerged As Important Therapeutic Targets For Ad. In The Case Of Gamma-Secretase,Progress Has Been Made Towards Designing Potent Inhibitors With Suitable Pharmacological Profiles. Direct Gamma-Secretase Inhibitors Are Being Evaluated In Clinical Trials And New Strategies Are Being Explored To Block Gamma-Secretase Activity Indirectly As Well. In This Regard,We Have Previously Reported An Indirect Regulation Of Gamma-Secretase Through Antagonism Of Cxcr2,A G-Protein Coupled Receptor (Gpcr). We Demonstrated That N-(2-Hydroxy-4-Nitrophenyl)-N'-(2-Bromophenyl)Urea (Sb225002),A Selective Inhibitor Of Cxcr2 Also Plays A Role In An Indirect Inhibition Of Gamma-Secretase. Furthermore,We Reported A Similar To 5-Fold Difference In The Selective Inhibition Of App Versus Notch Processing Via Gamma-Secretase Following Treatment With Sb225002. Herein We Describe The Synthesis And Optimization Of Sb225002. By Determination Of The Structure-Activity Relationship (Sar),We Derived Small Molecules That Inhibit A Beta 40 Production With Ic(50) Values In The Sub-Micromolar Range In A Cell-Based Assay And Also Validated The Potential Of Cxcr2 As A New Target For Therapeutic Intervention In Ad. (C) 2009 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmc.2009.09.051

专利信息

专利号:US-10801022-B2
优先权日:2015-04-14
标 题:Method for solid-phase synthesis of DNA encoded compound library
发明人：LI JIN; Wan jinqiao; LIU GUANSAI; DOU DENGFENG
权利人:HITGEN LTD; HITGEN INC
摘要:The present invention provides a method of solid-phase synthesis of DNA-encoded compound library. The method includes following steps: a) reacting solid carrier G-1 with linker molecule L-1 to prepare L-G-1; b) reacting DNA with linker molecule L-0 to prepare L-2; c) reacting L-G-1 with L-2 to prepare L-G-2; d) removing protection group of the L-G-2 and obtaining L-G-2-1; e) reacting the L-G-2-1 with synthetic building block and performing DNA encoding; and f) removing the solid carrier and obtaining the DNA-encoded compound library. Compared with the prior art, the present invention can complete post-treatment purification of the reaction only by filtration and irrigation processes for several times. The present invention is simple to operate, can shorten the production cycle of DNA encoded compound library with more than 50%, significantly increases the production efficiency and the unicity as well as the purity of the final products.

专利号:US-9879050-B2
优先权日:2013-08-30
标 题 :Substituted urea depsipeptide analogs as activators of the CLPP endopeptidase
发明人：LEE RICHARD E; ZHAO YING; GRIFFITH ELIZABETH; ZHENG ZHONG; SINGH AMAN P
权利人:ST JUDE CHILDREN'S RES HOSPITAL
摘要:In one aspect, the invention relates to substituted urea depsipeptide analogs, derivatives thereof, and related compounds, which are useful as activators the ClpP endopeptidease; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating infectious disease using the compounds and compositions. 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-9833457-B2
优先权日:2008-01-25
标题:Tricyclic compounds as modulators of TNF-α synthesis and as PDE4 inhibitors
发明人：MJALLI ADNAN M M; GADDAM BAPU; POLISETTI DHARMA RAO; KOSTURA MATTHEW J; GUZEL MUSTAFA
权利人:VTV THERAPEUTICS LLC
摘要:The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-α or by PDE4, including but not limited to psoriatic arthritis.

专利号:US-10822377-B2
优先权日:2015-03-04
标 题:Substituted urea depsipeptide analogs as activators of the ClpP endopeptidase
发明人：LEE RICHARD E; ZHAO YING; JIUYU LIU
权利人:ST JUDE CHILDRENS RES HOSPITAL
摘要:In one aspect, the invention relates to substituted urea depsipeptide analogs, derivatives thereof, and related compounds, which are useful as activators the ClpP endopeptidease; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating infectious disease using the compounds and compositions. 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:EP-2323994-A1
优先权日:2008-07-25
标 题:Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1

专利号:WO-2010010150-A1
优先权日:2008-07-25
标题:Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1