6127-17-9Relevant articles and documents
Preparation method of indole compound
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Paragraph 0066-0067, (2020/12/29)
The invention discloses a preparation method of a novel efficient indole compound, which comprises the following steps: by using o-nitroalkylbenzene containing various substituents as a raw material,controlling the reaction temperature to be 70-160 DEG C in an organic solution under the protection of inert gas and the participation of inorganic base, thereby obtaining the indole compound; preparing the novel indole compound containing various substituent groups through a hydrocarbon activation reaction catalyzed by a metal rhodium catalyst. The synthetic method is not reported in literature,the raw materials are easy to synthesize, no reducing agent needs to be added additionally, the method is simple in step, the indole compound containing various substituent groups does not need to beconstructed in one step through a nitroso intermediate, and the yield is high; The method is simple in unit operation, low in equipment requirement and suitable for rapidly synthesizing the indole compounds containing various substituent groups.
FUSED BICYCLIC HETEROCYCLE DERIVATIVES AS PESTICIDES
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, (2018/11/21)
The invention relates to novel compounds of the formula (I) or (I′) in which R1, R2, R3, Aa, Ab, Ac, Ad, Ae, Q and n have the definitions given above, to the use thereof as acaricides and/or insecticides for controlling animal pests and to processes and intermediates for the preparation thereof.
AUTOTAXIN INHIBITOR COMPOUNDS
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Paragraph 00441, (2015/04/15)
Described herein are compounds that are autotaxin inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with autotaxin activity.
Synthesis of Indoles by Palladium-Catalyzed Reductive Cyclization of β-Nitrostyrenes with Carbon Monoxide as the Reductant
Ferretti, Francesco,El-Atawy, Mohamed A.,Muto, Stefania,Hagar, Mohamed,Gallo, Emma,Ragaini, Fabio
supporting information, p. 5712 - 5715 (2015/09/15)
An efficient catalytic cyclization of β-nitrostyrenes to indoles was developed. The reaction was applied to the synthesis of 3-arylindoles and 2-alkylindoles. Given that in the latter case the starting β-nitrostyrenes can be easily obtained by a Henry reaction, the present method allows indoles to be obtained in a two-step sequence starting from cheap reactants.
Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping
Hall, Adrian,Billinton, Andy,Brown, Susan H.,Chowdhury, Anita,Giblin, Gerard M.P.,Goldsmith, Paul,Hurst, David N.,Naylor, Alan,Patel, Sadhana,Scoccitti, Tiziana,Theobald, Pamela J.
, p. 2684 - 2690 (2008/12/21)
We describe the medicinal chemistry approach that generated a novel indole series of EP1 receptor antagonists. The SAR of this new template was evaluated and culminated in the identification of compound 12g which demonstrated in vivo efficacy i
INDOL-3-YL-CARBONYL-SPIRO-PIPERIDINE DERIVATIVES AS V1A RECEPTOR ANTAGONISTS
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Page/Page column 112, (2008/06/13)
The invention relates to indol-3-yl-carbonyl-spiro-piperidine derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the spiro-piperidine head group A and the residues R1, R2 and R3 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, methods for preparing the compounds and pharmaceutical compositions, and their use in the treatment of dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxious and depressive disorders.
Indol-3-y-carbonyl-piperidin and piperazin-derivatives
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Page/Page column 22, (2010/11/25)
The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention
Inhibition of cytosolic phospholipase A2α: Hit to lead optimization
McKew, John C.,Foley, Megan A.,Thakker, Paresh,Behnke, Mark L.,Lovering, Frank E.,Sum, Fuk-Wah,Tam, Steve,Wu, Kun,Shen, Marina W. H.,Zhang, Wen,Gonzalez, Mario,Liu, Shanghao,Mahadevan, Anu,Sard, Howard,Khor, Soo Peang,Clark, James D.
, p. 135 - 158 (2007/10/03)
Compound 1 was previously reported to be a potent inhibitor of cPLA 2α in both artificial monomeric substrate and cell-based assays. However, 1 was inactive in whole blood assays previously used to characterize cyclooxygenase and lipoxygenase inhibitors. The IC50 of 1 increased dramatically with cell number or lipid/detergent concentration. In an attempt to insert an electrophilic ketone between the indole and benzole acid moieties, we discovered that increasing the distance between the two moieties gave a compound with activity in the GLU (7-hydroxycoumarinyl-γ- linolenate) micelle assay, which contains lipid and detergent. Extensive structure-activity relationship work around this lead identified a potent pharmacophore for cPLA2α inhibition. The IC50s between the GLU micelle and rat whole blood assays correlated highly. No correlation was found for other parameters, including lipophilicity or acidity of the required acid functionality. Compounds 25, 39, and 94 emerged as potent, selective inhibitors of cPLA2α and represent well-validated starting points for further optimization.
1H-INDOLE-3-ACETIC ACID HYDRAZIDE SPLA2 INHIBITORS
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, (2008/06/13)
A class of novel 1H-indole-3-acetic acid hydrazides is disclosed together with the use of such indole compounds for inhibiting sPLA2 mediated release of fatty acids (e.g., arachidonic acid) for treatment of conditions such as septic shock
