CAS: 2731-06-8; 2-(2-Methyl-1H-Indol-3-yl)Ethanamine

上下游产品

CAS号1080-83-7 2-(2-methyl-1H-... | CAS号25576-63-0 Desoxy-dinor-9-... | CAS号95-20-5 2-甲基吲哚 | CAS号5891-21-4 5-氯-2-戊酮 | CAS号100-63-0 苯肼 | CAS号1353013-70-3 2,2,2-trifluoro... | CAS号104296-24-4 2-Methyl-3-(2-n... | CAS号2826-91-7 (E)-2-甲基-3-(2-硝... | CAS号22980-10-5 (2-methyl-3-ind... | CAS号5416-80-8 2-甲基吲哚-3-甲醛 | CAS号441741-65-7 (E)-3-(4-(((2-(... | CAS号442633-00-3 CK-666 | CAS号441741-66-8 Panobinostat Ca...

📜2-甲基吲哚-3-甲醛置于palladium 10% On Activated Carbon,Ammonium Acetate,甲酸铵,三乙酰氧基硼氢化钠体系中,用 四氢呋喃,甲醇 用作溶剂,化学反应生成1H-2-甲基-3-氨乙基吲哚
参考文献:Arp2/3 复合物小分子抑制剂的结构表征和计算机辅助优化,Arp2/3 复合物是肌动蛋白细胞骨架的关键调节剂
标题:Arp2/3 复合物小分子抑制剂的结构表征和计算机辅助优化,Arp2/3 复合物是肌动蛋白细胞骨架的关键调节剂
摘要:Ck-666 ( 1 ) 是最近发现的肌动蛋白相关蛋白 2/3 (Arp2/3) 复合物的小分子抑制剂,这是一种关键的肌动蛋白细胞骨架调节剂,在细菌发病机制和癌细胞运动中发挥作用.虽然1是市售的,但与1结合的 Arp2/3 复合物的晶体结构尚未见报道,因此其作用机制尚不确定.此外,其相对较低的效力增加了其体内脱靶效应的可能性,使其在细胞生物学研究中的影响解释复杂化并妨碍其临床应用.在此我们报告了与 Arp2/3 复合物结合的1的晶体结构,这表明1在 Arp2 和 Arp3 亚基之间结合以稳定复合物的无活性构象.基于晶体结构,我们使用1的单取代导数的计算对接和自由能微扰计算来指导优化工作.对十种新合成化合物进行生化分析,鉴定出化合物2,其体外抑制活性比1增加了三倍.此外,我们的计算分析揭示了 Arp2 和 Arp3 亚基界面处的表面凹槽,可用于额外的基于结构的优化.
Doi:10.1002/cmdc.201200104

专利信息

专利号:US-12371404-B2
优先权日:2016-12-08
标 题 :Fused bicyclic alkylene linked imidodicarbonimidic diamides, methods for synthesis, and uses in therapy
发明人：BATCHELOR KENNETH; COBB JEFFERY E; GUDMUNDSSON KRISTJAN S; HENKE BRAD R; TAVARES FRANCIS X
权利人:NOVATARG INC
摘要:The present invention provides novel fused bicyclic alkylene linked imidodicarbonimidic diamides. In particular, described herein are N-[2-(indol-3-yl)alkylene]-linked imidodicarbonimidic diamides and N-[2-(pyrrolopyridin-3-yl)alkylene]-linked imidodicarbonimidic diamides (compound of formula (I) or formula (II)), and uses therefor. The compounds of the present invention are believed to be organic cation transporter selective compounds, useful for the treatment of diseases and conditions caused by reduced activity of 5′ adenosine monophosphate-activated protein kinase (AMPK).

专利号:US-2012053165-A1
优先权日:2009-03-03
标 题:Novel Phenyl Imidazoles and Phenyl Triazoles As Gamma-Secretase Modulators
发明人：ALLEN MARTIN PATRICK; AM ENDE CHRISTOPHER WILLIAM; BRODNEY MICHAEL AARON; DOUNAY AMY BETH; JOHNSON DOUGLAS SCOTT; PETTERSSON MARTIN YOUNGJIN; SCHWARTZ JACOB BRADLEY; TRAN TUAN PHONG
权利人:ALLEN MARTIN PATRICK; AM ENDE CHRISTOPHER WILLIAM; BRODNEY MICHAEL AARON; DOUNAY AMY BETH; JOHNSON DOUGLAS SCOTT; PETTERSSON MARTIN YOUNGJIN; SCHWARTZ JACOB BRADLEY; TRAN TUAN PHONG; PFIZER
摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:US-6974829-B2
优先权日:2002-05-07
标 题:Succinoyl aminopyrazoles and related compounds
发明人：TUNG JAY S; GUINN ASHLEY C; THORSETT EUGENE D; PLEISS MICHAEL A
权利人:ELAN PHARM INC
摘要:This invention is directed to a class of compounds (Formula I) including succinoyl amino pyrazoles, succinoyl amino thiadiazoles, succinoyl amino acid esters, succinoyl amino acid amides, succinoyl amino alcohols, succinoyl amino ketones, succinoyl amino hydantoins, succinoyl anilines, and succinoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting β-amyloid peptide release and/or synthesis, a method for inhibiting γ-secretase activity and a method for treating neurological disorders associated with β-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.

专利号:US-7053220-B2
优先权日:2002-02-01
标 题 :Hydroxyalkanoyl aminopyrazoles and related compounds
发明人：TUNG JAY S; GUINN ASHLEY C; THORSETT EUGENE D; PLEISS MICHAEL A
权利人:ELAN PHARM INC
摘要:This invention is directed to a class of compounds (Formula I) including hydroxyalkanoyl amino pyrazoles, hydroxyalkanoyl amino thiadiazoles, hydroxyalkanoyl amino acid esters, hydroxyalkanoyl amino acid amides, hydroxyalkanoyl amino alcohols, hydroxyalkanoyl amino ketoes, hydroxyalkanoyl amino hydantoins, hydroxyalkanoyl anilines, and hydroxyalkanoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting β-amyloid peptide release and/or synthesis, a method for inhibiting γ-secretase activity and a method for treating neurological disorders associated with β-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.

专利号:US-11230524-B2
优先权日:2017-08-17
标题 :Myocyte enhancer factor 2 (MEF2) modulators
发明人：ZHANG JUNHU
权利人:STANDARD LLC
摘要:The present disclosure provides novel compounds capable of functioning as Myocyte Enhancer Factor 2 (MEF2) modulators, as well as compositions, pharmaceutical formulations, methods of synthesis and kits.

专利号:US-9670305-B2
优先权日:2012-04-16
标 题 :Polyurethane dispersant and the method for its preparation
发明人：WANG ZHIJUN
权利人:WANG ZHIJUN; AFCONA CHEMICALS (HAIMEN) CO LTD
摘要:The present invention is related to a polyurethane dispersant and a preparation method thereof. The polyurethane dispersant is terminated by a nitrogen-containing heterocyclic compound during synthesis. The nitrogen-containing heterocyclic compound is prepared by subjecting anhydride and a compound containing a primary amine and a secondary amine or a hydroxyl or mercapto group to dehydration condensation. The condensed product is the nitrogen-containing heterocyclic compound, containing a reactive hydrogen. The structural formula of the compound containing the primary amine and the secondary amine or hydroxyl or mercapto group is shown as follows: n nwherein n=1 to 5, and preferably 2 to 4, R 1 and R 2 are respectively alkyls containing 1 to 8 carbons, R 1 and R 2 are independent of each other or connected by a chemical bond to form one or more saturated or unsaturated 4-member to 8-member rings, and X represents N, O, or S.