850374-98-0Relevant articles and documents
Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective NaV1.7 Inhibitors for the Treatment of Pain
Luo, Guanglin,Chen, Ling,Easton, Amy,Newton, Amy,Bourin, Clotilde,Shields, Eric,Mosure, Kathy,Soars, Matthew G.,Knox, Ronald J.,Matchett, Michele,Pieschl, Rick L.,Post-Munson, Debra J.,Wang, Shuya,Herrington, James,Graef, John,Newberry, Kimberly,Sivarao, Digavalli V.,Senapati, Arun,Bristow, Linda J.,Meanwell, Nicholas A.,Thompson, Lorin A.,Dzierba, Carolyn
, p. 831 - 856 (2019/01/21)
3-Aryl-indole and 3-aryl-indazole derivatives were identified as potent and selective Nav1.7 inhibitors. Compound 29 was shown to be efficacious in the mouse formalin assay and also reduced complete Freund's adjuvant (CFA)-induced thermal hyper
RORγ MODULATORS
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Page/Page column 32-33, (2018/04/13)
The invention provides an RORγ receptor agonist comprising a compound of formula (I), wherein the variables are as defined herein. These compounds are analogous to known RORγ receptor antagonists. The invention further provides a method of activating -the nuclear receptor RORγ, comprising -contacting the RORγ with an effective amount or concentration of a compound of the invention; and a method of treating cancer in a patient, comprising administering to the patient an effective dose of a compound of the invention.
ACYL SULFONAMIDE NaV1.7 INHIBITORS
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Page/Page column 20, (2017/11/15)
The present disclosure relates to compounds of formula I which inhibit NaV1.7, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods using and making such compounds and compositions.
Design and Synthesis of 2,2′-Diindolylmethanes to Selectively Target Certain G-Quadruplex DNA Structures
Livendahl, Madeleine,Jamroskovic, Jan,Ivanova, Svetlana,Demirel, Peter,Sabouri, Nasim,Chorell, Erik
supporting information, p. 13004 - 13009 (2016/09/09)
G-quadruplex (G4) structures carry vital biological functions, and compounds that selectively target certain G4 structures have both therapeutic potential and value as research tools. Along this line, 2,2′-diindolylmethanes have been designed and synthesi
five Yuan fragrance heterocyclic structure containing the anti-hepatitis c compound and its preparation and use
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Paragraph 0125; 0130-0131, (2016/11/21)
The invention discloses an anti-HCV (hepatitis C) compound containing a five-membered heteroaromatic ring structure, as well as a preparation method and applications thereof. The compound has a structure shown as the formula I, the compound has excellent anti-HCV virus activity, can be used for preparing anti-HCV drugs, the prepared drugs can be applied by adopting oral administration, intravenous injection or intramuscular injection.
Construction of Cyclopenta[b]indol-1-ones by a Tandem Gold(I)-Catalyzed Rearrangement/Nazarov Reaction and Application to the Synthesis of Bruceolline H
Scarpi, Dina,Petrovi?, Martina,Fiser, Béla,Gómez-Bengoa, Enrique,Occhiato, Ernesto G.
supporting information, p. 3922 - 3925 (2016/08/16)
A tandem gold(I)-catalyzed rearrangement/Nazarov reaction of enynyl acetates which efficiently provides cyclopenta[b]indol-1-ones as useful precursors for the synthesis of natural and bioactive compounds is described. The synthetic potential of the method
Novel inverse binding mode of indirubin derivatives yields improved selectivity for DYRK kinases
Myrianthopoulos, Vassilios,Kritsanida, Marina,Gaboriaud-Kolar, Nicolas,Magiatis, Prokopios,Ferandin, Yoan,Durieu, Emilie,Lozach, Olivier,Cappel, Daniel,Soundararajan, Meera,Filippakopoulos, Panagis,Sherman, Woody,Knapp, Stefan,Meijer, Laurent,Mikros, Emmanuel,Skaltsounis, Alexios-Leandros
supporting information, p. 22 - 26 (2013/03/13)
DYRK kinases are involved in alternative pre-mRNA splicing as well as in neuropathological states such as Alzheimer's disease and Down syndrome. In this study, we present the design, synthesis, and biological evaluation of indirubins as DYRK inhibitors wi
Catalytic anomeric aminoalkynylation of unprotected aldoses
Kimura, Yasuaki,Ito, Soichi,Shimizu, Yohei,Kanai, Motomu
supporting information, p. 4130 - 4133 (2013/09/12)
A copper(I)-catalyzed anomeric aminoalkynylation reaction of unprotected aldoses was realized. Use of an electron-deficient phosphine ligand, boric acid to stabilize the iminium intermediate, and a protic additive (IPA) to presumably enhance reversible carbohydrate-boron complexation were all essential for efficient conversion. The reaction proceeded well even with a natural disaccharide substrate, suggesting that the developed catalytic reaction could be useful for the synthesis of glycoconjugates with minimum use of protecting groups.
Amino-zinc-ene-enolate cyclization: A short access to cis-3-substituted prolino-homotryptophane derivatives
Mothes, Celine,Lavielle, Solange,Karoyan, Philippe
, p. 6706 - 6710 (2008/12/22)
(Chemical Equation Presented) Proline chimeras are useful tools for medicinal chemistry and/or biological applications. The asymmetric synthesis of cis-3-substituted prolines can be easily achieved via amino-zinc-ene-enolate cyclization followed by transm
