1233249-35-8Relevant articles and documents
OXADIAZOLES AS FUNGICIDES
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Page/Page column 63-64, (2020/05/15)
The present invention relates to novel oxadiazoles of Formula (I) wherein, R1, L1, A1, A2, A3, A4, L2 and R2 are as defined in the detailed description. The present in
NOVEL PROCESS FOR PREPARATION OF MIRABEGRON AND IT'S INTERMEDIATE
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, (2015/11/10)
The present invention related to a novel process for preparation of Mirabegron of formula (I) and its intermediate. I
The Concise Synthesis of Unsymmetric Triarylacetonitriles via Pd-Catalyzed Sequential Arylation: A New Synthetic Approach to Tri- and Tetraarylmethanes
Nambo, Masakazu,Yar, Muhammad,Smith, Joel D.,Crudden, Cathleen M.
supporting information, p. 50 - 53 (2015/07/28)
The selective synthesis of multiarylated acetonitriles via sequential palladium-catalyzed arylations of chloroacetonitrile is reported. The three aryl groups are installed via a Pd-catalyzed Suzuki-Miyaura cross coupling reaction followed by back-to-back C-H arylations to afford triarylacetonitriles in three steps with no over-arylation at any step. The triarylacetonitrile products can be converted into highly functionalized species including tetraarylmethanes. This new strategy provides rapid access to a variety of unsymmetrical tri- and tetraarylmethane derivatives from simple, readily available starting materials. (Chemical Presented)
Isoquinoline derivatives as potent CRTH2 antagonists: Design, synthesis and SAR
Nishikawa-Shimono, Rie,Sekiguchi, Yoshinori,Koami, Takeshi,Kawamura, Madoka,Wakasugi, Daisuke,Watanabe, Kazuhito,Wakahara, Shunichi,Kimura, Kayo,Yamanobe, Susumu,Takayama, Tetsuo
, p. 7674 - 7685 (2014/01/06)
In this study, we describe the synthesis and structure-activity relationship (SAR) of a series of isoquinoline chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2) antagonists. TASP0376377 (15-20), one of the most potent compounds, showed a potent binding affinity (IC50 = 19 nM) in addition to the excellent functional antagonist activity (IC50 = 13 nM). Moreover, the efficacy of this compound in a chemotaxis assay (IC50 = 23 nM) was in good agreement with its potency as a CRTH2 antagonist. In addition, 15-20 exhibited greater selectivity in binding to CRTH2 than to the DP1 prostanoid receptor (IC 50 >1 μM) or the enzymes COX-1 and COX-2 (IC50 >10 μM).
Isoquinoline derivatives as potent CRTH2 receptor antagonists: Synthesis and SAR
Nishikawa-Shimono, Rie,Sekiguchi, Yoshinori,Koami, Takeshi,Kawamura, Madoka,Wakasugi, Daisuke,Watanabe, Kazuhito,Wakahara, Shunichi,Matsumoto, Kayo,Takayama, Tetsuo
scheme or table, p. 3305 - 3310 (2012/06/18)
Synthesis and structure-activity relationship of a novel series of isoquinoline CRTH2 receptor antagonists are described. One of the most potent compounds, TASP0376377 (6m), showed not only potent binding affinity (IC 50 = 19 nM) but also excellent functional antagonist activity (IC50 = 13 nM). TASP0376377 was tested for its ability of a chemotaxis assay to show the effectiveness (IC50 = 23 nM), which was in good agreement with the CRTH2 antagonist potency. Furthermore, TASP0376377 showed sufficient selectivity for binding to CRTH2 over the DP1 prostanoid receptor (IC50 >1 μM) and COX-1 and COX-2 enzymes (IC 50 >10 μM).
ISOQUINOLINE DERIVATIVE
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Page/Page column 22, (2011/11/01)
A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.
