52756-36-2Relevant academic research and scientific papers
Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds
Shirai, Junya,Tomata, Yoshihide,Kono, Mitsunori,Ochida, Atsuko,Fukase, Yoshiyuki,Sato, Ayumu,Masada, Shinichi,Kawamoto, Tetsuji,Yonemori, Kazuko,Koyama, Ryoukichi,Nakagawa, Hideyuki,Nakayama, Masaharu,Uga, Keiko,Shibata, Akira,Koga, Keiko,Okui, Toshitake,Shirasaki, Mikio,Skene, Robert,Sang, BiChing,Hoffman, Isaac,Lane, Wes,Fujitani, Yasushi,Yamasaki, Masashi,Yamamoto, Satoshi
, p. 483 - 500 (2018)
A series of novel phenylglycinamides as retinoic acid receptor-related orphan receptor-gamma t (RORγt) inverse agonists were discovered through optimization of a high-throughput screen hit 1. (R)-N-(2-((3,5-Difluoro-4-(trimethylsilyl)phenyl) amino)-1-(4-m
Discovery of a Novel cGAMP Competitive Ligand of the Inactive Form of STING
Siu, Tony,Altman, Michael D.,Baltus, Gretchen A.,Childers, Matthew,Ellis, J. Michael,Gunaydin, Hakan,Hatch, Harold,Ho, Thu,Jewell, James,Lacey, Brian M.,Lesburg, Charles A.,Pan, Bo-Sheng,Sauvagnat, Berengere,Schroeder, Gottfried K.,Xu, Serena
, p. 92 - 97 (2019)
Drugging large protein pockets is a challenge due to the need for higher molecular weight ligands, which generally possess undesirable physicochemical properties. In this communication, we highlight a strategy leveraging small molecule active site dimers
AZA-ARYL 1H-PYRAZOL-1-YL BENZENE SULFONAMIDES
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Paragraph 0218; 0221, (2018/02/28)
Compounds are provided that act as potent antagonists of the CCR(9) receptor for treating Sjogren's syndrome. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions.
AMIDE COMPOUND
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Paragraph 0482, (2016/08/17)
The present invention relates to compound (I) or a salt thereof which has a RORγt inhibitory action. In the formula (I), each symbol is as defined in the specification.
Heterocyclic compound
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Paragraph 0582, (2016/10/08)
The present invention relates to compound (I) or a salt thereof which has a ROR γ t inhibitory action. wherein each symbol is as defined in the specification.
Oxidative fluorination of N-arylsulfonamides
Buckingham, Faye,Calderwood, Samuel,Checa, Bego?a,Keller, Thomas,Tredwell, Matthew,Collier, Thomas Lee,Newington, Ian M.,Bhalla, Rajiv,Glaser, Matthias,Gouverneur, Véronique
supporting information, p. 33 - 39 (2015/09/22)
We report a late stage oxidative nucleophilic fluorination of N-arylsulfonamides, a class of compounds so far not considered as precursors to 4-fluorophenyl sulfonamides. By installing a para-positioned tert-butyl substituent on the aniline, oxidative fluorination takes place regioselectively in the presence of HF·pyridine and PIDA. This methodology has been shown to give good yields for a variety of ortho- and meta-functionalised N-arylsulfonamides and has been adapted for radiofluorination to give 4-[18F]fluorophenyl sulfonamides under carrier added conditions.
AZA-ARYL 1H-PYRAZOL-1-YL BENZENE SULFONAMIDES
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Paragraph 0220; 0222, (2013/09/12)
Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.
Substituted N-sulfonylaminobenzyl-2-phenoxyacetamide compounds as VR1 receptor agonists
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Page/Page column 26, (2008/06/13)
This invention provides a compound of the formula (I): wherein R1 represents a (C1-C6)alkyl group; R2 represents a hydrogen atom, a halogen atom, a hydroxy group, a (C1-C6) alkyl group or a
