938467-02-8Relevant articles and documents
QUINOXALINE DERIVATIVES
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Page/Page column 74; 75, (2021/07/24)
The present invention relates to compounds according to general formula (I), which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties
Wang, Xiaojing,Barbosa, James,Blomgren, Peter,Bremer, Meire C.,Chen, Jacob,Crawford, James J.,Deng, Wei,Dong, Liming,Eigenbrot, Charles,Gallion, Steve,Hau, Jonathon,Hu, Huiyong,Johnson, Adam R.,Katewa, Arna,Kropf, Jeffrey E.,Lee, Seung H.,Liu, Lichuan,Lubach, Joseph W.,Macaluso, Jen,Maciejewski, Pat,Mitchell, Scott A.,Ortwine, Daniel F.,Dipaolo, Julie,Reif, Karin,Scheerens, Heleen,Schmitt, Aaron,Wong, Harvey,Xiong, Jin-Ming,Xu, Jianjun,Zhao, Zhongdong,Zhou, Fusheng,Currie, Kevin S.,Young, Wendy B.
supporting information, p. 608 - 613 (2017/06/13)
In our continued effort to discover and develop best-in-class Bruton's tyrosine kinase (Btk) inhibitors for the treatment of B-cell lymphomas, rheumatoid arthritis, and systemic lupus erythematosus, we devised a series of novel tricyclic compounds that improved upon the druglike properties of our previous chemical matter. Compounds exemplified by G-744 are highly potent, selective for Btk, metabolically stable, well tolerated, and efficacious in an animal model of arthritis.
BICYCLIC PIPERAZINE COMPOUNDS
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, (2013/05/21)
Bicyclic piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Inhibitors of Bruton's Tyrosine Kinase
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Page/Page column 125, (2010/09/07)
This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-Phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-III: wherein, variables Q, R, X, X′, Y1, Y2, Y2′, Y3, Y4, Y5, m, and n are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-III and at least one carrier, diluent or excipient.
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors
Giroux, Andre,Boulet, Louise,Brideau, Christine,Chau, Anh,Claveau, David,Cote, Bernard,Ethier, Diane,Frenette, Richard,Gagnon, Marc,Guay, Jocelyne,Guiral, Sebastien,Mancini, Joseph,Martins, Evelyn,Masse, Frederic,Methot, Nathalie,Riendeau, Denis,Rubin, Joel,Xu, Daigen,Yu, Hongping,Ducharme, Yves,Friesen, Richard W.
body text, p. 5837 - 5841 (2010/04/28)
Phenanthrene imidazoles 26 and 44 have been identified as novel potent, selective and orally active mPGES-1 inhibitors. These inhibitors are significantly more potent than the previously reported chlorophenanthrene imidazole 1 (MF63) with a human whole blood IC50 of 0.20 and 0.14 μM, respectively. It exhibited a significant analgesic effect in a guinea pig hyperalgesia model at oral doses as low as 14 mg/kg. Both active and selective mPGES-1 inhibitors (26 and 44) have a relatively distinct pharmacokinetic profile and are suitable for clinical development. Crown Copyright
A practical synthesis of m-prostaglandin E synthase-1 inhibitor MK-7285
Gosselin, Francis,Lau, Stephen,Nadeau, Christian,Trinh, Thao,O'Shea, Paul D.,Davies, Ian W.
supporting information; experimental part, p. 7790 - 7797 (2010/03/05)
(Chemical Equation Presented) A practical, kilogram-scale chromatography-free synthesis of mPGE synthase I inhibitor MK-7285 is described. The route features a convergent assembly of the core phenanthrene unit via amide-directed ortho-metalation and proxi