95360-33-1Relevant articles and documents
Method for preparing 2-(6-trifluoromethylpyridine-2-yloxymethyl) methyl phenylacetate
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Paragraph 0067; 0069-0070; 0073-0074; 0076-0077, (2021/04/28)
The invention provides a method for preparing methyl 2-(6-trifluoromethylpyridine-2-yloxymethyl) phenylacetate, and belongs to the technical field of preparation of pesticide intermediates. The preparation method comprises the following steps: by taking 3
Discovery of the First Potent, Selective, and Orally Bioavailable Signal Peptide Peptidase-Like 2a (SPPL2a) Inhibitor Displaying Pronounced Immunomodulatory Effects in Vivo
Velcicky, Juraj,Bodendorf, Ursula,Rigollier, Pascal,Epple, Robert,Beisner, Daniel R.,Guerini, Danilo,Smith, Philip,Liu, Bo,Feifel, Roland,Wipfli, Peter,Aichholz, Reiner,Couttet, Philippe,Dix, Ina,Widmer, Toni,Wen, Ben,Brandl, Trixi
supporting information, p. 865 - 880 (2018/02/17)
Signal peptide peptidase-like 2a (SPPL2a) is an aspartic intramembrane protease which has recently been shown to play an important role in the development and function of antigen presenting cells such as B lymphocytes and dendritic cells. In this paper, we describe the discovery of the first selective and orally active SPPL2a inhibitor (S)-2-cyclopropyl-N1-((S)-5,11-dioxo-10,11-dihydro-1H,3H,5H-spiro[benzo[d]pyrazolo[1,2-a][1,2]diazepine-2,1′-cyclopropan]-10-yl)-N4-(5-fluoro-2-methylpyridin-3-yl)succinamide 40 (SPL-707). This compound shows adequate selectivity against the closely related enzymes γ-secretase and SPP and a good pharmacokinetic profile in mouse and rat. Compound 40 significantly inhibited processing of the SPPL2a substrate CD74/p8 fragment in rodents at doses ≤10 mg/kg b.i.d. po. Oral dosing of 40 for 11 days at ≥10 mg/kg b.i.d. recapitulated the phenotype seen in Sppl2a knockout (ko) and ENU mutant mice (reduced number of specific B cells and myeloid dendritic cells). Thus, we believe that SPPL2a represents an interesting and druggable pharmacological target, potentially providing a novel approach for the treatment of autoimmune diseases by targeting B cells and dendritic cells.
NOVEL CRYSTALLINE FORM OF PICOXYSTROBIN, METHOD OF PREPARING AND USE OF THE SAME
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Page/Page column 13, (2017/09/28)
A novel crystalline form of the compound of formula (I) (picoxystrobin) is provided. The novel crystalline form of picoxystrobin may be prepared by crystallization from solution in a suitable solvent. Fungicidal compositions comprising the novel crystalline form, a method for controlling fungal infestations at a locus and a use of the novel crystalline form are also provided.